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Analgesic, Antimicrobial And Anti-Inflammatory Activities Of Lycopene Extracted From Approved Tomato Varities Cultivated In Pakistan
Abstract: Lycopene is a red colour pigment chiefly responsible for deep-red color of ripe tomato fruits and foodstuffs. It has great attention due to its biological and nutraceutical properties. In this study tomatoes are cultivated in Pakistan and paste prepared from these tomatoes was dehydrated by using methanol as dehydrating agent, then cis and trans form of lycopene was extracted with solvent mixture methanol-carbon tetrachloride. The crude lycopene obtained from benzene through addition of boiling methanol which produced pure crystalline lycopene by twice crystallization. Inflammations and immune-related common disease such as arthritis are growing in Pakistan now a day. Most of the drugs from plants become important in modern medicine even the role of lycopene in controlling inflammation and immune related disease was reported, lycopene extracted from Chlorella marina. The aim of study is to extract the lycopene from tomato fruit and then screen the analgesic and anti-inflammatory activities using respectively acetic acid writhing test in mice and carrageenan-induced paw edema assay in rats at various concentrations ( 100, 200, 400 and 600 mg/kg of bw) significantly reduction of oedema by dose dependent manner. No mortality was appeared during the acute toxicity test with the dose of 600 mg/kg. Agar disk diffusion method was engaged to find out the antibacterial activity of lycopene. Based on reliable results, we confirmed that lycopene isolated from tomato has a great potential and useful drug for treatment of rheumatoid arthritis and its folk medicinal use as an analgesic and anti-inflammatory activity.
NOVEL DAUCUS CAROTA SEEDS PROVED TO BE POTENTIAL SOURCE OF FUNCTIONAL ATTRIBUTES.
Abstract: Medicated properties of carrot seeds have been incorrigible since ancient times. The purpose of the present study was to investigate the variations in physico-chemical and functional attributes of carrot seeds of novel cultivars indigenous to Pakistan. It was investigated that carrot seeds contained moisture (6.1-7.8%), protein (21.5-24.6%), Oil (5.9-7.9%), carbohydrates (46.8-51.4%), crude fiber (1.8-4.1%) and ash (8.9-11.3%). The acidity, peroxide value, saponification number, unsaponification matter, specific gravity and refractive index of carrot seed oil were 4.9-5.6%, 15.0-16.1meq/Kg, 141.4-149.7, 8.9-10.2g/Kg, 0.972-0.991 and 1.4562-1.5321 respectively. The total phenolic acid contents in seeds of DCW, DCY, DCP, T29, DCR, DC3 and DC90 cultivars were 9.7, 7.11, 42.24, 13.77, 10.06, 19.49 and 15.41mg/100g respectively. The methanolic extracts of carrot seeds contained total antioxidant capacity (28.21-61.31mg/100g), DPPH scavenging capacity (12.35-37.61mg/100g), superoxide radical scavenging capacity (13.35-34.16mg/100g) and hydroxyl scavenging capacity (12.89-37.7mg/100g). Gas chromatography was used for the determination of fatty acids in carrot seed oil. The major fatty acids were petroselinic (57.5-61.2%), linoleic (13.89-15.34%), palmitic (11.82-14.15%) and stearic (3.7-5.26%) acids. Among all the cultivars, DCP seeds have significant functional properties due to higher phenolic content and antioxidant potential. Fatty acid profile of carrot seed oil revealed that it may be a valuable source of edible oil.
Oxidative stability of vegetable oil stabilized with pea (Pisum sativum L.) pod extract..
Abstract: The naturally occurring antioxidant have received great deal of attention because they are able to ameliorate oxidative damage induced by free radical and are safer that synthetic antioxidants like BHA and BHT. The main objectives of the study were to probe the extent of oxidative alterations in vegetable oil subjected to 65C, over a period of 60 days. The magnitude of oxidative changes was monitored by the periodical measurement of ten days by the change in color, refractive index (RI), cloud point, peroxide value (PV), sponification, free fatty acid (FFA) contents value, and iodine- values. The initial contents of FFA of control and stabilized samples were (0.169 % as oleic acid) and PV (0.31 meq/kg of oil). At the end of storage period, Samples subjected to heating treatment reached the level of FFAs 0.2021% for control and 0.186% for samples stabilized with peapod extracts, and PV values 15.96, 11.70 meq/kg of oil, respectively. The initial values of RI (40°C) (1.4655) rose to the point of (1.4684) for control and (1.4674) for samples. Sponification values reached (189.24 mg of KOH/g of oil) for control and (193.12 for samples), initial reading was (196.35) for both. Whereas, the iodine value (g of I /100 g of oil) decreased from 127.80 to 98.20 and 95.49 for control and samples stabilized with pea (Pisum stavium L.), respectively. The results of various parameters investigated in the present study demonstrated the magnitude of oxidative deterioration of the vegetable oil samples exposed to oven treatment at 65C to be significantly (P < 0.05) pronounced as compared with that of control. The overall investigations carried out regarding pea (Pisum sativum L.) pod indicates that plant has a rich potential source of natural antioxidants as described in literature and proved in this research.
CHEMICAL COMPOSITION AND PHARMACEUTICAL APPLICATIONS OF LAMIACEAE ESSENTIAL OILS: A COMPREHENSIVE STUDY
Abstract:The aim of the present study was to examine the effect of different environmental and agricultural parameters on the quality and biological activities of essential oils of Lamiaceae species. The essential oils contents from material collected from colder regions and at full bloom were higher than from temperate regions. The GC-MS analysis revealed that mostly quantitative, rather than qualitative variations were observed in the oil composition of each species with respect to harvest seasons. The principal chemical constituent determined in M. arvensis, M. piperita, M. longifolia, M. spicata essential oils from both the seasons were menthol, menthone, piperitenone oxide and carvone, respectively. The major chemical constituent of O. sanctum, O. gratissimum and O. basilicum essential oils were eugenol, β-caryophyllene, β-elemene and linalool. The antiproliferative activity has been tested on breast cancer MCF-7 and prostate cancer LNCaP cell lines by the MTT assay. The antimicrobial and antioxidant activities were determined by using broth micro dilution, DPPH radical-scavenging and inhibition of linoleic acid oxidation assays. All the tested essential oils exhibited excellent antimicrobial, antioxidant, cytotoxic potentials. The significant (p < 0.05) variations in the contents of most of the chemical components and biological activities of seasonally collected samples were documented.
Comparative evaluation of the efficacy of locally delivered Meswak irrigation and 0.2% CHX irrigation in management Chronic periodontitis patients – A Clinical & Microbiological Study
Abstract: Ayurvedic medicines like turmeric possess anti-inflammatory, anti-oxidant, and anti-microbial properties. This study was carried out using the purest form of turmeric and meswak to test their anti-plaque and anti-inflammatory properties in the form of a sub gingival irrigation. The aim of this study is to evaluate the efficacy of meswak solution and compare it with conventional irrigant i.e., 0.2% chlorhexidine (CHX) gluconate and a positive control (saline) as an adjunct to scaling and root planning in the treatment of chronic periodontitis. Materials and Method Study group consisted of patients diagnosed with chronic periodontitis, aged between 21-45 years. 90 sites with pocket depth >5mm were selected and randomly divided into 3 groups. Group A: Test group received Meswak (HIORA) irrigation along with scaling and root planing. Group B: Test group received scaling and root planing along with 0.2% chlorhexidine (CHX). Group c: Control group received Saline along with Scaling and root planning. Clinical parameters Plaque index, bleeding index, probing pocket depth and relative attachment level were elevated for each patient at baseline, 7th, 14th, 21 days and 1 months. Plaque samples were taken at baseline, 21 days and 1 month interval and total colony count was done. Results All the groups showed significant improvement in all clinical parameters from baseline to 1 month. There was statistically significant improvement in gingival index, PPD in Group A as compared to other groups. The percentage reduction in microbial load at the 1 month was highest in chlorhexidine group. Conclusion CHX and Herbal agents showed similar clinical efficacy but CHX irrigation was more effective in reducing bacterial counts.
POTENT ANTI-OXIDANT ACTIVITY OFBARK EXTRACT OF FICUS CUNIA
Abstract: Ficus Cunia also said to be the Indian fig tree,synonym ficus semicordata; Vern-‘Khaina’,Hindi-‘Jharphali’,Sanskrit-‘Kharpatra’,is an evergreen deciduous tree upto
12m height,bark dark grey.In the present study bark extract of plant was prepared
using methanol as a solvent.The radical-scavenging capacity of Methanolic extract of
Ficus cunia was determined using the DPPH radical method.2ml of test solutions was
added to 2ml of 2 x 10-4mol L-1 ethanolic DPPH solution.The mixture was shaken
vigorously and the absorbance was measured at 517nm immediately.The decrease in
absorbance was determined at 15,30 and 60min.until the absorbance reached a
steady state(after60min).All the tests were performed in triplicate and mean values
calculated.The anti oxidant activity was expressed according to the ability of an extract
to scavenge DPPH free radicals and wasdetermined using the following equation:
%Inhibition = [1-(A1-A2)/A0]x100
The extract is found to be effective in reducing the stable free radical DPPH to the
yellow-coloured diphenylpicrylhydrazine indicating that the extract is active in DPPH free
radical scavenging.With increasing the concentration of methanolic extract,inhibition
also increases Extract at the concentration of 80μg/ml demonstrated 93.52% inhibition
of the DPPH free radicals.
Finasteride Loaded Solid-SNEDDS (Self Nanoemulsifying Drug Delivery System) for Enhanced Oral Bioavailability
Abstract: The aim of this study was to improve the oral bioavailability of poorly water soluble drug, finasteride by combining the advantages of both self nanoemulsifying drug delivery system (SNEDDS) and tablets. Ternary phase diagram was constructed using selected surfactant (Cremophore RH 40), oil (Capryol 90) and co-surfactant (PEG 400) and self nanoemulsifying region was identified. Selected liquid SNEDDS formulations were subjected to particle size analysis, saturated solubility studies, self-emulsification time determination, percentage transmittance and centrifugation tests, determination of the effect of pH and Robustness to dilution and cloud point measurement. Optimized liquid formulation was then subjected to a novel test “determination of dispersion’s nature and differentiation between microemulsions and nanoemulsions”. Liquid SNEDDS formulation was solidified through simple adsorption technique using Avicel and Aerosil- 200 as adsorbents, separately and then characterized for powder flow properties. Tablets were prepared from Aerosil-200 liqui-solid powder and then characterized. Further investigation was done (XRD, FTIR, SEM and in-vitro dispersion studies). Droplet size was less than 180 nm. The dispersion produced by dilution of optimized SNEDDS was confirmed to be a nanoemulsion and not a microemulsion. SEM analysis of S-SNEDDS and regenerated liquid nanoemulsion showed successful adsorption of L-SNEDDS onto the surface of porous carrier and presence of nano size spherical droplets, respectively. FTIR and XRD results showed that drug in final formulation was intact and was converted to amorphous form in the final formulation. S-SNEDDS and L-SNEDDS showed 93% and 98% in-vitro dispersion of finasteride respectively as compared to 72% drug release from the commercial tablets. In-vivo study showed 87 % and 88 % bioavailability of finasteride from S-SNEDDS and L-SNEDDS respectively, as compared to 62% from commercial tablets. It could be concluded that Solid SNEDDS is a promising approach for improving the bioavailability of finasteride.
Variations in leaf essential oil composition and bioactivities from two cultivars of Psidium guajava L. (white and pink fruit forms)
Abstract:Essential oils (EOs) were extracted from the leaves of two Psidium guajava (P. guajava) cultivars (white and pink fruit forms) from the local fields of Faisalabad, Punjab Pakistan. EOs were analyzed by GCMS and the antioxidant, antimicrobial activities and anti-haem biocrystallisation activities were assessed. GC-MS profiles revealed 41 and 59 compounds with total percentage composition 92.68 % and 87.19% in P. guajava white and pink cultivars, respectively. The major compounds (>5%) found in EO of P. guajava white were caryophyllene (9.08%), dihydrocarveol acetate (7.04%), nerolidol (6.69%) and caryophyllene oxide (6.18%) whereas α-phellandrene (11.66%), eucalyptol (10.01%), α-terpineol (7.78%) and spathulenol (5.71%) in P. guajava pink. Essential oils showed moderate antioxidant potential. The P. guajava pink cultivar has comparatively high antioxidant potential than P. guajava white while both have comparable antimicrobial potential. Essential oils from both of the cultivars of P. guajava exhibited poor anti-haem biocrystallization activity. Results revealed that the EO of P. guajava pink cultivar has high phenolic content as compared to P. guajava white and thus the greater antioxidant potential. Whereas the antimicrobial potential of both was almost equal. The results also revealed that both EOs have poor antimalarial activity in comparison of standard drug. Both qualitative and quantitative variations were observed in chemical composition of both EOs.
PHENOLIC ACIDS AND FLAVONOIDS FROM BIORESOURSES INHIBITS MELANOGENESIS IN MELANOMA CELLS
Abstract:Phenolic compounds constitute a group of secondary metabolites which have important functions in plants. Evidence suggests that people can benefit from plant phenolics obtained either by the diet or through skin application, because they can alleviate symptoms and inhibit the development of various skin disorders. Active compounds such as arbutin, aloesin, gentisic acid, flavonoids, hesperidin, and polyphenols were isolated from different plants. In this study, we investigated the effects of these compounds on melanogenesis, including the activation of melanogenesis signaling pathways. All the phenolic acids and flavonoids tested significantly inhibited melanogenesis without melanocytotoxicity by different mechanisms and significantly inhibited tyrosinase activity in a dose- and time-dependent manner, and decreased the expression of melanogenesis-related proteins, such as microphthalmia-associated transcription factor (MITF), tyrosinase, tyrosinase-related protein-1 (TRP1), and dopachrome tautomerase (Dct). In addition, phenolic compounds and flavonoids also act by phosphorylating and activating melanogenesis inhibitory proteins such as Akt and mitogen-activated protein kinase (MEK)/extracellular signal-regulated kinase (ERK). Using inhibitors against protein, the hypopigmentation effect was suppressed, and the phenolic acids-initiated activation of MEK/ERK and PI3K/Akt was also revoked. These results suggest that activation of the MEK/ERK, PI3K/Akt, and inhibition of Wnt/β-catenin signaling pathways is involved in the melanogenesis signaling cascade, and that activation by phenolic acids reduces melanin synthesis via down-regulation of MITF and its downstream signaling pathway. In conclusion, we found that polyphenols significantly suppressed melanin content and cellular tyrosinase activity through a decrease in the expression of melanogenic enzymes and microphthalmia-associated transcription factor (Mitf) in α-melanocyte stimulating hormone-stimulated mouse melanoma cells. Moreover, these compounds decreased cyclic adenosine monophosphate (cAMP) levels and cAMP-responsive element-binding protein phosphorylation, which downregulated Mitf promoter activation and subsequently mediated the inhibition of melanogenesis.
Phenolic Profile, Lycopene Contents, and Inhibition of tyrosinase activity and melanine pigmentation by Some Newly Grown Tomato (Lycopersion esculantum) Varieties
Abstract: The present research work was conducted in order to evaluate the phenolic profile, lycopene contents, antioxidant attributes and tyrosinase inhibition and melanine pigmentation propertied of some locally grown approved and lined varieties of tomato (Lycopersion esculantum). Reverse phase high performance liquid chromatography method was developed and validated for the simultaneous quantification of phenolic acids and flavonoids from tomatoes extracts. The RP-HPLC analysis of tomatoes extracts revealed the presence of ferulic acid, vanillic acid, p-coumeric acid, gallic acid, p-hydroxy benzoic acid and chlorogenic acid being the major phenolic acids and quercetin, myricetin and catechin being the most prominent flavonoids compounds. Ripe tomatoes also contained considerable amounts of lycopene (up to 49 mg/100g dry weight). The different samples analyzed showed different contents of lycopene, flavonoids and phenolic acids. The amount of TPC and TFC extracted from different varieties of tomato were ranged from 6.75 to 9.63 and 0.76 to 2.69 g/100g, respectively. Tomatoes extracts also exhibited a good antioxidant (53.7-87.2 %) and free radical scavenging potential (IC50 16.7-50.0 μg/mL). The lycopene isolated from tomatoes was found to inhibit mushroom tyrosinase. The results of the present analytical study revealed that all the newly grown varieties of tomatoes exhibited better antioxidant potential and tyrosinase inhibition than the control variety. Significant variation in the antioxidant activity was observed with respect to approved and line varieties. The results suggest that the tomatoes extracts are rich sources of phenolic antioxidant and could be used in pharmaceutical, nutraceutical and cosmetics products.
Development and characterization of levosulpiride-loaded liquid suppositories with improved bioavailability and patient compliance.
Abstract:The purpose of this study was to develop and characterize levosulpiride loaded liquid suppository with improved dissolution and bioavailability. The levosulpiride-loaded liquid suppositories were prepared by cold method. The composition of levosulpiride-loaded liquid suppositories were optimized in a series of experiments using various weight ratios of P188, P407, Tween 80 and drug. Thee suppositories were liquid at room temperature, however, when rectally administered, they became gel at body temperature. Their rheological properties and release characteristics were determined in vitro while pharmacokinetic study was performed after its rectal administration to rats and compared with the drug powder. Poloxamer 188 and Twee 80 decreased the gelation temperature and gelation time, but increased the gel strength and mucoadhesive force of drug-loaded liquid suppositories. Thus, the liquid suppository composed of [Levosulpiride/P 188/P 407/Tween 80 (1/15/17/3 %)] with a gelation temperature of about 30.7 °C remained liquid at 25 °C, but converted to gel at 30-36.5 oC, resulting in easy administration and rapid gelation inside the body. This liquid suppository gave a considerably increased dissolution rate of drug as compared to the drug suspension. Beside this, a meaningfully higher plasma concentration and 7.1-fold AUC values were exhibited by this liquid suppository in association to the drug suspension. Hence, this liquid suppository could alternatively be used for the enhanced bioavailability of levosulpiride-loaded pharmaceutical products.
In-Vitro Assessment of Anti-Glycating Potential of HMG-CoA reductase inhibitors against D-Ribose Mediated Protein Glycation
Abstract:Non-enzymatic glycation mediated advanced glycation end products (AGEs) generation results in the pathogenesis of diabetic complications. The present study was opted to evaluate the anti-glycating potential of HMG-CoA reductase (HMG-R) inhibitors (Atorvastatin:AT, Rosuvastatin:RT, Simvastatin;ST, Pitvastatin;PT, Fluvastatin;FT, Tocotrienol:TT, Ezetimibe:EZ) alone as well in combination, using Amino-guanidine hydrochloride (AG) as reference drug. UV-Vis spectral analysis depicted that 20mM D-ribose glycated BSA caused 87% glycation with maximum restoration by 97.08%, 92.70%, 96.62 %, 92.50%, 100%, 100% and 84.62% in 50µM AT, RT, TT, EZ, EZ-AT, EZ-RT and AG treated samples, respectively. Spectrofluorometric analysis showed 99.17% BSA-AGE formation upon incubation with 20 mM D-ribose which was significantly inhibited by 98.3%, 96.5%, 98.17%, 95.9%, 99.6%, 99.2% and 86.13%, respectively, in above mentioned drugs. The carbonyl content was found to be increased by 93.12% in 20mM D-ribose glycated BSA which was decreased by 96.9%, 92.54%, 96.71%, 88.98%, 92.0%, 91.96%, and 85.08%, respectively. Similarly, all these inhibitors also resulted in significant decrease in HMF content with maximum decline in AT>TT>RT>EZ>AG in alone and EZ-AT>EZ-RT in combination. Based on above in-vitro findings, our data suggested that among all the HMG-CoA reductase inhibitors, AT, TT, RT, EZ, EZ-AT and EZ-RT inhibited the formation of AGEs. So, we concluded that these HMG-R inhibitors might be new promising anti-glycation agents for the prevention of diabetic complications via inhibition of AGEs formation and AGE-induced protein damage. Further structural and in-vivo analysis are required to substantiate the use of these inhibitor as an antiglycating agent.
Design and docking investigations of tryptophan based pseudo-peptide molecule in Leptospirosis treatment
Abstract: It is well known that peptides are the most potent bioactive naturally occurring molecules. But this inherent biological properties of peptides cannot be utilized to the fullest due to their early degradation properties seen in vivo, hence to overcome this stability issue without loss of biological activity, pseudo-peptide was designed and synthesized in a way that they retain their stability in vivo maintaining high biological viability. In the present study effort was made to unravel the potential undeciphered properties of pseudo-peptide with main focus on potential treatment of Leptospirosis, a deadly disease with very limited treatment options and related disorders which are highly lethal, by using preliminary pharmacological assays viz., MDT, TDT and hemolytic assay. In particular, all the analysis led to the conclusion that the synthesized compound not only inhibited Leptospira, the causative organism of Leptospirosis but also the life threatening disorders such as hemolysis, caused due to Leptospiral infection.
BIOACTIVITY GUIDED ISOLATION OF PHENOLIC COMPOUNDS OF SELECTED EDIBLE FLOWERS AND EVALUATION OF ANTIOXIDANT ACTIVITY
Abstract:Edible flowers are reaching intended as a new source of nutritious and bioactive compounds and subsidized the attractive appearance of foods. The effect of nutritional, shielding and chemo is the vital cause of considering edible flowers as a valuable new source of natural antioxidants in the human diet. Natural antioxidants like flavonoids, anthocyanins and other phenolic compounds have vital constituents of edible flowers. There is growing evidence to support the relief of many degenerative diseases including cardiovascular disease, cancer and aging by natural antioxidant consumption in human diet. The flowers of Moringa oleifera, Foeniculum vulgare, Ocimum basilicum, Cynara scolymus, Bauhinia purpurea, Viola odorata, Ocimum sanctum, Rosa indica, Cichorium intybus and Brassica napus have been selected for analysis of the phenolic compounds and evaluation of antioxidant activity. Antioxidant activity of edible flowers verified by checking total phenolic content (R. indica > F. vulgare > M. oleifera > B. napus > V. odorata > B. purpurea > O. basilicum > C. scolymus > O. sanctum > C. intybus), total flavonoid content (R. indica > F. vulgare > M. oleifera > B. napus > V. odorata > B. purpurea > O. basilicum > C. scolymus > O. sanctum > C. intybus), bleaching of a β-carotene-linoleic acid system, DPPH free radical scavenging activity (R. indica> B. napus > B. purpurea > O. sanctum > V. odorata > F. vulgare > C. scolymus > M. oleifera > C. intybus > O. basilicum) and determination of Reducing power. From all this study it is concluded that edible flowers are the finest emerging source of antioxidant and healthy increment in human diet. In addition, phenolic were analyzed by state-of-the-art HPLC. Several phenolic are detected in edible flowers. The data obtained were statistically analyzed using appropriate statistical techniques. In general, the outcomes of this study assist the use of examined selected edible flowers from Pakistan as a worthy source of natural antioxidants and valued phenolic.
Intelligent multifunctional Nanoparticles; Synthesize, Characterization and Applications – A review.
Abstract: The nanotechnology has concentrated to study by researchers around the world to synthesize
novelty nanoparticles which will be used in wide range of applications from industry to
medicine. In the recent years, one of the most common nanomaterial in the world is
nanoparticles. In addition, Multifunctional nanoparticles has been growing by scientists
around the world. The various metallic, ceramic and polymeric compounds like Iron Oxides,
Zinc Oxides, Iron-Cobalt, Nickel- Cobalt, Titanium Dioxide, Ag doped gold, Copper alloys,
PEG, PPA, PMMA, Chitosan, Hydroxyapatite and sort of that, will be produced by chemists,
physicians or materialist in the laboratory. There are various method to synthesize the
nanoparticles like precipitation, chemical and physical vapor deposition, thermal and
plasma spray, laser deposition, mechanical alloying and so on. Because of an impressive and
unique chemical, physical and an antimicrobial properties of nanoparticles along with their
biocompatibility; makes these materials find specific applications in various industries.
Thus, nanoparticles have lots of applications in manufacturing, agriculture, environment,
energy, electronics, and medicine. These use as an industrial coatings, lubricant oils,
catalysts, gas sensors, magnetic separators, antioxidant, break down oil, breakdown volatile
organic air pollutants, fuel cell electrodes, storage materials, lithium ion batteries,
semiconductor (photovoltaic cells), solar steam device, storing and packaging of agricultural
produces, nutrients absorber, food flavoring, perfumes, scratch resistance eyeglasses,
fluorescent biological labels, contrast imaging, bone growth, drug and gene delivery,
immunoassay, bio detection of pathogens, separation and purification of biological
molecules and cells, cancer diagnosis and treatment, tumors destruction via heat therapy
(hyperthermia), tissue engineering and etc. So, propose of this paper is detecting the
intelligent multifunctional materials and evaluating wonderful characteristics which is be
synthesized by various methods.
Nutraceuticals – A niche for Global Market
Abstract: Over the years nutraceuticals have attracted considerable interest due to their potential nutritional, safety and therapeutic effects. They possess a role in a plethora of biological processes, including antioxidant defenses, cell proliferation, gene expression, and safeguarding the regulation of cellular energy and apoptosis. They are considered to be healthy sources for prevention of life threatening diseases such as diabetes, renal and gastrointestinal disorders, as well as different infections. In global marketplace nutraceuticals and functional foods have become a multi-billion dollar industry and estimates within Canada suggest that the Indian nutraceutical and functional food industry has potential to grow to $30 billion US. Currently we focused nutraceuticals from an Indian perspective to identify the potential for distinctive niche markets and growth of Indian industry and it's potential in international markets. The limitations to growth in this area are due to paucity in proper labelling and assessment in the health effects by nutraceuticals. Deprived data in Food safety, quality (FSSAI) and a an understanding of interactions among foods, medicines and dietary supplements are central requirements in India for development of less restricted access to our national markets and expansion into the international. Exploitation of genetic and ecotype variability associated with natural populations of nutraceutical and functional foods, has potential to develop niche markets distinctive to India and global regions. Selection for consistent production of high and low productivity of active plant components within specific ecological regions will allow development of alternative nutraceuticals and functional foods with potent health benefits. These commodities have potential to stabilize economic return to local producers without having to compete with generic products being marketed. Development of better characterized and research proven products will help enhance consumer confidence in nutraceutical in India and in the globe.
Intellectual Property Rights(IPR)- Technical Know-How in India
Abstract: In the present scenario Intellectual Property Rights (IPR) play a vital role in Pharmaceutical domain, Intellectual Property Rights (IPR) or Patents are the exclusive rights given to a person for an invention in any branch of technology whether products or processes which is patentable if they meet the Criteria of being NOVEL, involving an INVENTIVE STEP and being capable of INDUSTRIAL APPLICATION. The laws which govern the intellectual property in India are well established at all levels- statutory, administrative and judicial. India is in agreement with World Trade Organisation (WTO) and also member of various treaties like Paris convention, PCT, Budapest Treaty. India is also part of Trade Related Aspects of Intellectual Property Rights (TRIPS) which came into force from 1st January 1995 which governs with minimum standards for protection and enforcement of intellectual property rights in member countries sufficiently required to promote effective and adequate protection of intellectual property rights.
The IPR are segregated into 5 different types of following areas:-
Looking at the latest amendment 2016, in Indian Patent act it is more focussed in Timelines in terms of Grant of Patent to inventor in a judicial manner
Reduction in time period for filing response to FER, Remote Hearing, Claim deletion at National Phase Entry, No extension of 31 months for NP entry, New Rules categorically deny any possibility of condonation of delay for NP entry beyond 31 months, Sequence Listing Maximum Official fees fixed, Refund of Examination Fee, Expedited Examination , Regular Examination, Pre-Grant Opposition rules ,
Foreign Filing License request to be disposed of within 21 days, and some procedural changes such as
Power of Attorney in 3 months ,Reference to deposition of Biological Material to be made within 3 months from the date of filing of the application, Electronic Submission mandatory for Agents, and new favours in case of New Entity: “Startup”
Survey on awareness, perception and extent of usage of nutraceuticals and dietary supplement in local region of Uttar Pradesh, India
Abstract: In recent years there has been growing interest in nutraceuticals which provides health benefits and is providing preventive options for the ageing population worldwide for keeping them away from various lifestyle diseases. Along with the growing healthcare industry in India there is an emerging trend in growing consumerism for ‘Fast Moving Healthcare Goods (FMHG)’; worldwide known as Nutraceuticals, which are by definition, ingredients with human health benefits beyond basic nutrition. According to available estimates, nutraceuticals market in 2007 was INR 18.75 billion and expected to grow at 20% CAGR to achieve a market size of INR 27 billion in 2009. Global nutraceuticals market is estimated at USD 120 billion in 2007 growing at 7% (CAGR). The US has been the major market for nutraceuticals with India and China becoming fastest growing markets. Indian nutraceuticals market in 2008 was USD 1.0 billion and globally this market is expected to reach USD 180 billion in 2013 growing at a CAGR of 7% driven by the fastest growing dietary supplement category. Nutraceuticals are gaining acceptance globally for their ability to address several diseases. Vitamins, Minerals and Nutrients constitute about 85% of the global market while antioxidants and anti-agents account for 10% other segments such as herbal extracts occupy 5% of the market. To actualize the growth rate and the demand of nutraceuticals in the local region of Uttar Pradesh like Ghaziabad, Noida and Greater Noida. The present survey study has been conducted and the survey data was portrait and presented in the pictorial & graphical manner for better understanding.
Validation of traditional claims of Indian Evolvulus species through in-vitro antiradical activities and estimation of neuroprotective hydroxycinnamic acids using HPTLC
Abstract: Free radicals generation is the major cause of neurodegenerative disorders and phyto-phenolic regularly being checked for Neuroprotection. There are two Evolvulus species viz. E. alsinoides L. (EA) and E. nummularius L. (EN) of the family Convolvulaceae, found in India and traditionally being used as nerve tonic. Therefore, the current study was designed to evaluate antioxidant potential by several in vitro methods viz. DPPH radical, β carotene bleaching, hydroxyl radical and ABTS radical scavenging, Anti-lipid peroxidation, NO scavenging on human macrophage cell J774A., Intracellular ROS generation, cell viability assay and to estimate total phenolic content and two hydroxycinnamic acids viz. caffeic and ferulic acid in aforesaid Evolvulus species. The results showed more phenolic content (968.527 and 342.465 mg), caffeic (415.59 and 185.56mg/100g) and ferulic acid (286.5 and 235.3mg/100g) in EN than EA respectively. Both the Evolvulus species have significant antioxidant potential, with IC50 for DPPH (86.75 and 49.46μg/ml), β carotene bleaching (550.09 and 307.41 μg/ml) for EA and EN respectively, which showed better antioxidant potential of EN. However, other in vitro and cell line assays gave varied results for EA and EN extract. The cell viability assay showed ethanolic extract of EN was safer at higher concentration. Hence, it is concluded that EN and EA may be explored for the treatment of several different neurological disorders.
DIAGNOSTIC ACCURACY OF SERUM PROADRENOMEDULLIN VERSUS SOFA SCORE IN PREDICTION OF MORTALITY IN CRITICALLY ILL SEPTIC PATIENTS
Abstract: The use of novel sepsis biomarkers has increased in recent years. However, their prognostic value with respect to illness severity has not been explored. In this work, we examined the ability of mid-regional proadrenomedullin (MR-proADM) in predicting mortality in sepsis patients with different degrees of organ failure, compared to Sequential Organ Failure Assessment (SOFA) score.
This is a cross sectional study enrolling 100 sepsis and septic shock patients admitted to Alexandria Medical University Hospital Intensive Care Units (ICUs). Serum pro-adrenomedullin was collected during first 24 hour of diagnosis of sepsis and septic shock and compared to SOFA score during first day as gold standard in prediction of mortality of critically ill septic patients. The accuracy of the serum pro-adrenomedullin for mortality was determined by area under the receiver operating characteristic curve (AUROC) analysis.
The study enrolled 100 patients with sepsis and septic shock. The pro-adrenomedullin AUC was 0.914 with p value > 0.001 and best cut off point < 7.1 with sensitivity 82.76 and specificity 85.71 with positive predictive value 88.9. As regard SOFA score in day 1 AUC was 0.968 with p value > 0.001 and best cut off point < 9 with sensitivity 84.48 and specificity 95.24 and positive predictive value 96.1. As regard comparison between serum Pro-adrenomedullin versus SOFA score, p value for Pairwise comparison was 0.053 with no significant difference.
Serum pro-adrenomedullin can be used as a predictor of mortality in critically ill septic patients during first 24 hour of diagnosis of sepsis and septic shock.
TREATMENT OF GOUT FROM NUTRITIONAL VALUES & DIFFERENT PLANT EXTRACTED COMPOUNDS.
Abstract: Gout was treated by bottle gourd and ficus Palmata specie. 24 rats were divided into 4 groups: control, model, bottle gourd treated and Ficus Palmata treated. Gout is induced by direct oral dose of uric acid as 30mg/kg body weight. Bottle gourd and Ficus Palmata extracts were prepared in ethanol separately and given to rats as 80mg/kg body weight. After 6 weeks of treatment behavioral activities were monitored by locomotor activity in open field, stimulatory activity in home cage, anxiolytic effects in light and dark apparatus, recognition memory in novel object apparatus. After decapitation, biochemical tests were determined by calcium, magnesium, phosphorus and serum uric acid. Locomotor and stimulator activities significantly increases in bottle gourd and Ficus Palmata treated group, anxiety decreases while, recognition memory of both groups significantly increases as compare to model but decreases as compare to control. Bottle gourd and Ficus Palmata specie treated rats showed good effects to enhance magnesium level in blood, significantly reduces the serum uric acid level and maintained calcium phosphorus balance in blood. Behavioral and biochemical variables were analyzed by using one-way ANOVA and p-value <0.05 was considered statistically significant. Thus, the aim of study is to prevent to cause and cure hyperuricemia and gout and increases the medicinal value of bottle gourd and Ficus Palmata specie extract by determining their active part.
Understanding the role of molecular chaperones within citrate capped gold nanoparticles induced cell stress
Abstract: The conserved native molecules which are heat shock proteins (Hsps) whose role is to facilitate proper folding of other polypeptides are also called molecular chaperones. DnaK is the most prominent and a role player molecular chaperone of the Hsps family. Another study suggested that citrated coated gold nanoparticles (cit-AuNPs) induce cytotoxicity in E. coli DnaK deficient BB1553 cells whilst cells expressing recombinant DnaK exhibit defence against cit-AuNPs cell stress. However, it remains to be understood as to the role of other molecular chaperones in facilitation of such cytoprotection. Cit-AuNPs have also been reported to act as molecular chaperones to reverse protein aggregation in-vitro, an interesting phenomenon which will be further explored in this study. Cit-AuNPs at an average size of 16 nm were synthesised following Turkevich-Frens method and characterized with Ultraviolet visible spectroscopy (UV-Vis), X-Ray Defractometer (XRD), Scanning Electron Microscopy (SEM) and Transmission Electron Microscopy (TEM). The absorption peak at 519 nm was an indication of the surface plasmon absorption spectrum of AuNPs ranging from 510 – 530 nm. When encountering cells AuNPs translocated across membrane barriers. AuNPs with less than 35 nm in diameter enters cells, nucleus and crosses difficult barriers. It is highly imperative to understand the role of molecular chaperones and co-chaperones in the interaction with cit-AuNPs and subsequent elucidation of cyto-protection. A range of analytical techniques to be employed to pursue the understanding of the interaction of AuNPs with model cells and proteins include High Resolution TEM, Mass Spectrometry (MS) based proteomics and several spectroscopic techniques such as fluorescence, circular dichroism (CD) and nuclear magnetic resonance (NMR). The use of techniques such as isothermal titration calorimetry (ITC), surface plasmon resonance (SPR) is meant to characterise AuNPs-protein binding which will enhance the manipulation of AuNPs properties to facilitate adsorption of recombinant proteins or specific drug with an intention for efficient delivery in-vivo.
DRUG UTILIZATION PATTERN OF FIXED DOSE COMBINATIONS IN THE DEPARTMENT OF MEDICINE IN A TERTIARY MEDICAL COLLEGE HOSPITAL IN ASSAM
Abstract: The synthetic and herbal drugs are commonly used by the patients in chronic diseases. The present study was designed to investigate the possible drug- drug interactions between the methanolic extract of Momordica dioica seeds and Metformin. Male Wistar rats weighing about 180-250 gms were selected for the study. The type II diabetes was induced in animals by a single intra peritoneal injection of streptozotocin (30 mg/kg body weight). The animals were divided into 8 groups of 6 rats each (n=6). Metformin was administered orally as – 20, 40 and 80 mg/kg, and metformin in combination with herbal extracts were administered in same doses. The effect of combination of both drugs on the pharmacokinetic parameters was studied in experimental animals after the treatment for a period of 21 days. The pharmacodynamic effect of combination of both the drugs was studied on the serum glucose levels of diabetic rats after multiple dosing. It is evident from the study that the serum glucose levels with metformin in the dose of 40 mg/kg along with the herbal extract was significantly decreased (*p<0.05). The bioavailability in treated groups was also analyzed and was found to be significant increase in the bioavailability of metformin (*p<0.05).The results proved that pharmacokinetic and pharmacodynamic interactions between the Metformin and Momordica dioica extract are significant. The study concludes that the dose of metformin, can be reduced in combination with herbal drug, to minimize the adverse effects in long term use in diabetes. The study undertaken has clinical significance of such drug combinations in therapy.
Pre-Clinical Evaluation of Citrullus Colocynthis roots: A promising herb to treat Type-2 Diabetes.
Abstract: Diabetes is a metabolic disorder of multiple etiologies characterised by chronic hyperglycemia with disturbances of carbohydrate, fat and protein metabolism. Diabetes also leads to the development of oxidative stress in the body by generating free radicals. Findings also indicate that it is associated with atherosclerosis and coronary hear disease. The use of herbal medicine for the treatment of diabetes mellitus has gained importance through out the world. Citrullus colocynthis which is commonly known as bitter apple belonging to the family cucurbitaecea is mainly native of Asia and Europe. The present study was designed to evaluate the anti hyperglycemic, anti hyperlipidemic and anti-oxidant efficacy of aqeous and ethanolic root extracts of C.colocynthis. Diabetes was induced by giving STZ (35mg/kg) intraperitoneally, rats which showed >250mg/100ml of blood were selected for the study. Both aqueous and ethanolic extracts of C. colocynthis were prepared and administered at a dose of 100,200,300 mg/kg oraly for a period of 15 days. Metformin was taken as a standard drug at a dose 50mg/kg orally. The extract showed controlled intestinal absorbtion of monosaccharides by inhibiting Alpha – amylase enzyme and antidiabetic activity by lowering blood glucose levels in-vivo significantly (p<0.001). The extracts showed effective anti-oxidant activities by scavenging the free radicals like SOD, Catalse and LPO. It also lowered plasma CH, TG’s, LDL and VLDL levels significantly as compared to controlled group. Thus C. colocynthis root extracts has been proved to be a promising herb in type II diabetes and its complications.
A COMPARATIVE STUDY OF GASTRIC ANTI-ULCER ACTIVITY OF THE
LEAF EXTRACTS OF MURRAYA KOENIGII AND MORINGA OLEIFERA IN
Abstract:OBJECTIVES: To evaluate the gastric anti-ulcer activity of the aqueous extracts of Murraya
koenigii (AEMK) and Moringa oleifera ( AEMO) in wistar rats
MATERIAL AND METHOD: Study animals were divided into 2 groups, and gastric ulcers
were induced using pyloric ligation and cold restraint stress models. Two doses of AEMK and
AEMO were used (200 mg/kg and 400 mg/kg per orally), in each model. Ranitidine 20 mg/kg
per oral (R20) was used as a standard. Ulcer index, free acidity, total acidity, volume of gastric
juice and pH were studied and analyzed.
RESULTS: The mean ulcer index in AEMK 400 mg/kg (p=0.059) and AEMO 400 mg/kg
(p=0.231) treated groups was comparable with R20. The mean gastric juice volume was
significantly lower in the R20, AEMK400 and AEMO400 groups than disease control (DC)
group. The mean pH in R20, AEMK200, AEMK400, AEMO200 and AEMO400 groups was
significantly higher than the DC group. The mean free acidity in R20, AEMK200, AEMK400,
AEMO200 and AEMO400 groups was significantly lower than the DC group. The mean total
acidity in R20, AEMK200, AEMK400, AEMO200 and AEMO400 groups was significantly
lower than the DC group.
CONCLUSION: The present study provides scientific evidence in support of gastric ulcer
protective activities of AEMK and AEMO. Thus both plants can be suitable natural sources in
treating gastric ulcers.
Lycopene amends LPS induced oxidative stress and hypertriglyceridemia via modulating PCSK-9 expression and Apo-CIII mediated lipoprotein lipase activity
Abstract:This study was undertaken to uncover the regulatory role of lycopene in targeting lipopolysaccharide (LPS) induced oxidative stress and inflammatory cascades and subsequent regulation of proprotein convertase subtilisin/kexin type-9 (PCSK-9) expression via sterol regulatory element binding protein-2 (SREBP-2) and hepatocyte nuclear factor-1α (HNF-1α). Further, protein-protein interaction (PPI) studies for Lycopene-Apo-CIII complex against lipoprotein lipase (LPL) were also performed to assess its regulatory role behind the enhanced circulatory TG clearance. Lycopene treatment down-regulated hepatocyte PCSK-9 expression via down-regulation of HNF-1α, whereas, LDL-receptor (LDL-R) was up-regulated by subsequent up-regulation of SREBP-2. PPI studies showed that lycopene diminishes the affinity of apo-CIII to complex with LPL (ΔG:-917.1 Kcal/mol), whereas, atorvastatin promotes and stabilizes the apo-CIII-LPL complex formation (ΔG:-1820.2 Kcal/mol) resulting in decreased LPL functionality and impaired TG clearance. Moreover, lycopene also ameliorated LPS stimulated oxidative-stress and inflammatory markers via enhanced total antioxidant and HDL associated PON-1 activity as well as suppression of PCSK-9 expression. Based on above findings we concluded that lycopene exhibits dual role in targeting LPS induced oxidative stress and hypertriglyceridemia via down-regulation of PCSK-9, making greater number of surface LDL-R available for LPS processing and clearance, as well as increased LPL activity through inhibition of apo-CIII.
Lycopene combats LPS induced oxidative stress via modulating PON-1, lipid peroxidation and hepatic antioxidant activities
Abstract:Lipopolysaccharide (LPS) induced infection and inflammation is well reckoned to alter oxidative homeostasis. The present study was undertaken to uncover he regulatory role of lycopene in targeting LPS induced oxidative stress, lipid peroxidation events and erythrocytes. LPS administration significantly decreased (50.5%) the level of HDL-associated PON-1which was significantly restored by +122.7% and +55.2%, respectively, after Lyc-1 and Lyc-2 treatment in rats. Plasma CD, LOOH and MDA were significantly increased by 25.7%, 62.3% and 119.9%, respectively, in LPS control group which were significantly ameliorated by lycopene (Lyc-1) treatment by 60.15%, 55.2% and 50%, respectively. Furthermore, hepatic lipid peroxidation events were also diminished upon lycopene treatment. We also illustrated that the enzymatic activities of hepatic CAT, SOD, Gpx and GST were significantly declined from 56.63, 5.83, 65.47 and 162.50 Units/mg-protein to 45.21, 3.96, 56.43 and 125 Units/mg protein, respectively, which were then significantly increased by 27.5%, 22%,16.4%, 81.6% and 35 % in Lyc-1 treated rats, respectively. Hepatic non-enzymatic antioxidant (GSH) was also ameliorated by an increase of 161.49% and 83.93% in Lyc-1 and Lyc-2 treated rats, respectively.In addition, lycopene treatment also resulted in the elevation of GSH in t-BHP exposed erythrocyte membrane that could explain the protective action of lycopene against oxidative stress.Further, our findings strongly suggest that lycopene, because of its potent free radical scavenging property, was able to considerably normalize all the altered oxidative events and therefore can be useful in the therapy of systemic inflammatory process which might induce atherosclerosis.
Curcuminoids improve lipids and glycemic parameters in type 2 diabetic subjects
Abstract:Background: Type 2 diabetes mellitus (T2DM) is commonly accompanied by disturbed lipid metabolism and increased cardiovascular (CV) risk. Curcuminoids are natural products with numerous biological and pharmacological activities among which are anti-diabetic, lipid-modulating and insulin-sensitizing actions. Despite numerous preclinical data, clinical evidence on the potential benefits of curcuminoids supplementation in subjects with type 2 diabetes mellitus (T2DM) is few. Here, we explored the efficacy of curcuminoids in modulating plasma lipids and glycemic parameters, as determinants of CV disease, in subjects with T2DM.
Methods: In this 12-week randomized double-blind placebo-controlled trial, subjects with T2DM were assigned to curcuminoids (1000 mg/day plus piperine 10 mg/day) or placebo. Serum concentrations of glucose, insulin, glycated hemoglobin (HbA1c), total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), triglycerides (TG) and lipoprotein(a) [Lp(a)] were measured at baseline and at the study end.
Results: Between-group comparison of change in the study parameters revealed significant reductions in serum levels of TC (p=0.023), Lp(a) (p=0.001), glucose (p=0.048), C-peptide (p<0.001) and HbA1c (p<0.001), and elevations in serum HDL-C levels (p=0.048) in the curcuminoids group versus the placebo group. Serum TG, LDL-C and insulin changes did not show any significant improvement by curcuminoids supplementation.
Conclusion: Curcuminoids supplementation can improve glycemic parameters, TG and HDL-C in subjects with T2DM and could be regarded as an effective adjunct therapy to decrease the CV risk in this population.
Regulation of serum adipokines by curcuminoids in type 2 diabetes mellitus
Abstract:Objective. Curcuminoids are active phytochemicals from that possess numerous biological effects including modulation of immune and inflammatory pathways. These phytochemicals are laos known to harness insulin resistance and exert anti-diabetic actions. Here, we tested the efefcts of supplementation with curcuminoids on circulating levels of adipokines that are implicated in the pathophysiology of type 2 duabetes mellitus (T2DM) and its complications.
Methods. In this randomized controlled trial, subjects with T2DM were assigned to either (curcuminoids 1000 mg/day plus piperine 10 mg/day) or matched placebo for 12 weeks. Adiponectin, leptin, ghrelin and tumor necrosis factor-α (TNF-α) were measured at baseline and at study end.
Results. Serum levels of leptin (p<0.001), TNF-α (p<0.001) and leptin:adiponectin ratio (p<0.001) were significantly reduced while serum adiponectin levels were increased (p=0.032) in the curcuminoids compared with placebo group. Serum ghrelin changes were not significantly different between the study groups (p=0.135) but were significantly elevated following curcuminoid supplementation after adjustment for baseline ghrelin concentrations (p=0.017) or changes in BMI (p=0.025).
Conclusion. Curcuminoids supplementation increased plasma adiponectin and reduced TNF-α leptin:adiponectin ratio and leptin levels in subjects with T2DM. This modulatory effect may explain part of the putative anti-diabetic effects of curcuminoids.
SynDiag – the new concept of prenatal diagnosis and therapy
Abstract:This work is a recently developed and patented algorithm for automatic extraction of a three-dimensional surface of fetus face from a registered stack of bi-dimensional ultrasound scans. It operates without human intervention, elaborating input data in the standard DICOM format with a two-steps statistical analysis based on volumetric histogram processing and 2D segmentation. It outputs a quantitative triangular mesh in PLY format, ready for further mathematical analysis.
By way of method validation and as an example of the application, we developed a diagnosis tool, based on the former elaboration, which succeeded in discriminating labio-schisis manifesting individuals from healthy individuals. The algorithm maps the individual’s surface with geometrical descriptors useful to identify the face’s landmarks, i.e. pronasion and labrum superior, and compute a distance measure between each faces couple.
The algorithm correctly identifies left- and right-sided cleft lips, providing the physicians with a probability of pathology affection and supporting decision making. Since the method is fully automatic and pathology independent, it allows to easily populate large database of quantitative fetus’ faces individuals, enabling objective pathologies to be characterized and normotypes defined. Finally, the fields of application of SynDiag are: gynecology and pregnancy, oral and maxillo-facial surgery, pediatrics, pharmacology and toxicology, tailored medicine, and surgery.
As antibiotic resistance continues to threaten the treatment of various infections – surgery wounds included, the following step of this work concerns the overcoming of the rise in antibiotic resistance by many bacterial pathogens (e.g. MRSA, P. aeruginosa). According to Prof P. Molan (Waikato University, NZ) studies and chemical analyses, in 2012
Jenkins and Cooper demonstrated that in vitro manuka honey with antibiotic agents have found a synergistic effect with oxacillin, tetracycline, imipenem and mupirocin against the growth of MRSA. In 2015 Roberts discovered that there was a down-regulation of proteins involved in flagellation in P. aeruginosa and the degeneration of its cell structural stability too. In addition, attempts to generate honey-resistant strains in the laboratory have not been successful and there have been no reports of clinical isolate with acquired resistance to honey (Blair et al. 2009 and Cooper et al. 2010). Nowadays hospitals and clinics using honey for wound care keep the honey in the wound by soaking it into a calcium-alginate or hydrofiber dressing, which forms a gel with the honey as it absorbs the exudate. In conclusion, the use of medical honey in wound care of patients, including the immunocompromised ones is now possible to eliminate infections caused by super bacteria.
Synthesis and Lipid Lowering Properties of Novel N-(4-Benzoylphenyl) Pyrrole-2-Carboxamide Derivatives
Abstract:Hyperlipidemia is involved in development of atherosclerosis and coronary heart disease. We synthesized two novel pyrrole carboxamide derivatives N-(4-Benzoylphenyl)-4-bromo-2,5-dihydro-1H-pyrrole-2 carboxamide (1) and 4- Amino-N-(4-benzoylphenyl)-1-methyl-1H- pyrrole-2carboxamide (2) and test them as antihypelipidemic agents. The synthesized compounds were characterized using I.R. and NMR. Biological evaluation of compound 1 and 2 showed that compound 1 significantly decreased TG, LDL-C, TC and mild increase in HDL-C in plasma. Contrarily, compound 2 appeared to be less potent compared to 1; it moderately decreased TG, LDL-C and TC with mild increase of HDL-C. The NH pyrrole mediates H-bondinteraction of 1 with the backbone of the target(s) protein(s) and this corresponds to the high potency of 1. The lower activity of 2 confirms that the presence of H-bond is essential to induce high activity. The finding of this work suggests that this scaffold might be promising as antihypelipidemic agents for future work.
Hepatic loss-of-Sirt7 promotes hepatocellular carcinogenesis in mice
Abstract:Sirt7 is one of seven mammalian NAD+-dependent protein deacetylases. Although growing evidence implies Sirt7, which is a nuclear sirtuin, has oncogenic function, its oncogenic potential in vivo is only partially explored. Early studies insist Sirt7 as an oncogenic factor maintaining oncogenic transformation, however, recent studies demonstrate Sirt7 is crucial for DNA repair and genomic stability. Here we demonstrate hepatic loss-of-function of Sirt7 accelerates hepatocellular carcinoma (HCC) formation by genotoxic drug N-diethylnitrosamine (DEN) injection. We, first, observed bigger and more hepatic tumor colonies from the micro-computed tomography of Sirt7-deficient liver. Furthermore, liver histology, qRT-PCR, and immunoblotting assays revealed the feature of hepatic cancer encompassing increased hepatic alpha-fetoprotein (AFP), Ki67, and Pcna. In serum, we also found increased cytokines including IL-6, TNFα, and AFP, which is a well-established HCC marker. In addition to in vivo studies, Bioinformatics analysis using hepatic transcriptomes of BXD mouse genetic reference populations and human transcriptome of hepatic tumors indicates Sirt7 expression positively correlated with DNA repair gene-set. Based on our observation, here we propose hepatic loss-of-Sirt7 promotes hepatocellular carcinogenesis unlike the early studies reported Sirt7 as an oncogenic factor. Targeting Sirt7 activity could be a potential therapeutic strategy against liver cancer.
Sialyllated oligosaccharides suppress cancer growth through inhibition of VEGFR-2-mediated angiogenesis
Abstract:The oligosaccharides in human milk have various biological functions. However, the molecular mechanism(s) underlying the anti-angiogenic action of sialylated human milk oligosaccharides (HMOs) are still unclear. Here, we show that sialyllactose (SL) and sialylgalactose (SG) found in human milk can inhibit the activation of vascular endothelial growth factor (VEGF)-mediated VEGF receptor-2 (VEGFR-2) by binding to its VEGF binding site (second and third IgG-like domains), thus blocking downstream signal activation. SL and SG also inhibits growth of VEGF-stimulated endothelial cells. In endothelial cells treated with VEGF, SL and SG diminished tube formation, migration, and the arrangement of actin filament. In addition, SL and SG clearly suppressed VEGF-induced neovascularization in an in vivo Matrigel plug assay. Notably, SL and SG prevented the growth of tumor cells, and angiogenesis on tumor tissues in in vivo mice models allotransplanted with Lewis lung carcinoma, melanoma, and colon carcinoma cells. Taken together, we have demonstrated that the sialylated milk oligosaccharides functions as an inhibitor of angiogenesis through suppression of VEGF-mediated VEGFR-2 activation in endothelial cells.
Effects of the Coptis Japonica and Glycyrrhiza Uralensis extract-based Hataedock treatment on Skin Fat Lipid Barrier Formation in infant mice
Abstract:The Hataedock is an orally administered treatment for infants using herbal extracts in Korean medicine to remove fetal toxic elements and meconium. This study is done to evaluate the effect of Coptis japonica and Glycyrrhiza uralensis extracts as a Hataedock treatment on the skin fat barrier formation. The 5-week-old NC/Nga mice were randomly divided into 3 groups assigned as (1) the control group (Ctrl), (2) the first Hataedock-treated group administrated the Coptis japonica and Glycyrrhiza uralensis extract (CGT), and (3) the second Hataedock-treated group with Bifidobacterium (BBT) and treated either the control solution, CGT extract or BBT. After 5 weeks of the treatment, the effect of each Hataedock treatment has been evaluated by histopathological tissue analysis. We observed, in the CGT group, the loricrin-positive reaction has been increased by 2.3 folds, along with involucrin-positive reaction by 0.9 folds, the filaggrin-positive reaction by 1.4 folds, and ASM-positive reaction by 3.4 folds in the stratum corneum.
Hataedock treatment, using the Coptis japonica and Glycyrrhiza uralensis extracts, increased the expression of proteins promoting keratinocyte differentiation. These observation leads us to conclude that Hataedock treatment has a clear potential to improve the keratinocyte formation as well as function augmenting the formation of the skin barrier.
Chemical composition, antibacterial and antioxidant properties of the flower and leaves essential oils of Bauhinia galpinii (N.E. Br) grown in South Africa.
Abstract:Background: Reactive oxygen species (ROS) and infectious diseases, particularly those due to multi-drug resistant bacterial strains are almost impossible to combat globally. Besides challenges posed by microbial resistance to synthetic antibiotics, these drugs are known to exhibit side effects. There is paucity of information of the composition and bioactivity of most indigenous plants such as Bauhinia galpinii claimed potent in folk medicine for management of diseases including diabetes, cancers, cardiovascular in Africa.This study aimed to investigate the bioactive compounds, in vitro antioxidant, antibacterial and cytotoxicity properties of B. galpinii essential oils (EOs). Methodology: The EOs obtained using modified Clevenger apparatus were characterized by high resolution GC-MS, while the radicals scavenging and antibacterial effects were examined spectrophotometric and micro-dilution techniques respectively. Results: Phytol (25.61%), azulene (12.63 %), and α -ionone (10.38 %) were the dominant compounds found in the leaf EO (LEO), while α -guaiene (13.23 %), α -ionone (5.81%) and azulene (11.46 %) were the prominent compounds in the flower EO (FEO). The EOs exhibited strong antibacterial activity against five reference bacterial strains and one laboratory confirmed multi-drug resistant bacterial strain. The FEO exhibited more activity than LEO against the test bacteria with MIC value of 0.125 - 0.25 mg /mL and 0.20-0.35 mg / mL for the LEO. The IC50 value for FEO (0. 52 mg/mL) showed higher antioxidant property than LEO (3.30 mg/ mL) and the reference compounds in reducing lipid peroxyl radical to neutral molecule. Conclusion:The study indicates that the EO has potent bioactive compounds, noteworthy antioxidant strength, significant antibacterial property and the EO could be use as natural medicine and food preservative upon further investigation.