In vitro antidiabetic activities and GC-MS phytochemical analysis of Ximenia americana extracts

Objective To ascertain various phytochemical ingredients in Ximenia americana leaves extracts by GC-MS & evaluating their antidiabetic property by using in vitro assays. Methods The serial extraction was carried out with a series of solvents: chloroform, ethyl acetate, methanol, ethanol and water with increasing polarity using Soxhlet apparatus. The concentrated and dried extracts were subjected to GC-MS analysis and also the antidiabetic activity was assessed by employing standard in vitro techniques. Results GC-MS analysis confirmed the presence of different phytochemicals in each leaf extracts of X. americana. The major phytoconstituents were found to be Oleic acid, n-Hexadecanoic acid, Non-decanoic acid and Octadecatrienoic acid in chloroform extract; and 3-Undecene, Tridecene, Trifluoroaceteoxy tetradecene, and Trichloroacetic acid-3-tridecyl-ester in ethyl acetate extract; where in 1-Tetracosanol, Behenyl alcohol, 1-Hexacosanol, Octadecanal, 4-Piperidine propanoic acid and α �D-mannofuranoside in methanol extract; 8,11,14-Eicosatrienoic acid, 7-Tetradecanal and 1-Ocytyn-3-Ol-4-Ethy in ethanol extract; aqueous extract showed the presence of 9,12-Octadecandionoic acid. In vitro antidiabetic studies show that aqueous extract exhibited significant activity when compared to other solvent extracts. Conclusion The investigation confirms that aqueous extract exhibited highest antidiabetic activity among all extracts; Additional studies on needed for purification, characterization and structural elucidation of bioactive compounds from aqueous extract & also confirm its antidiabetic property by in vivo studies. This study provides scientific evidence that leaves of Ximenia americana have anti-diabetic efficacy. Thus, considering its relative hypoglycemic potency, they may serve as useful therapeutic agents for treating diabetes. © 2017 SAA

Synthesis and biological evaluation of novel pyrazole derivatives as urease inhibitors

Studies on enzyme inhibition remain an important area of pharmaceutical research since these studies have led to the discoveries of drugs useful in a variety of physiological conditions. The enzyme inhibitors can interact with enzymes and block their activity towards natural substrates. Urease inhibitors have recently attracted much attention as potential new anti-ulcer drugs. A series of novel substituted pyrazoles 8(a-j) has been synthesized by diazotization of fluoro chloro aniline (1) and the reaction of the corresponding diazonium salt solution (2) with ethyl cyanoacetate (3) to give the intermediate, ethyl 2-((3-chloro-4-fluorophenyl) diazenyl-2- cyanoacetate (4). The intermediate is then cyclised with chloroacetonitrile (5) using triethyl amine as the base to give the final compound, ethyl 4-amino-1-(3-chloro-4-flurophenyl)-5- cyano-1H-pyrazole-3-carboxylate (6). Nucleophilic substitution group is removed from the final compound and 8(a-j) derivatives have been synthesized. All the synthesized compounds were characterized by physical data (M.P. & TLC) and spectral Data (IR & 1H NMR). The synthesized compounds were evaluated for urease-inhibition activity. Molecular docking studies were carried out for these compounds with the enzyme urease. From the observations it has been noticed that some of the compounds possesses remarkable urease-inhibitory effect

In vitro Biomedical Application of Endophytic Aspergillus melleus Isolated from Leaves of Premna serratifolia L.

Some microorganisms known as endophytes live in symbiotic relationships in the living tissues of plants without posing a health risk. As a result, they synthesize many metabolites which are helpful for the plants in many ways. So, these metabolites are known to exhibit many biological properties like antioxidant, antidiabetic anti-inflammatory, etc. Currently, many drugs are used to control inflammatory diseases like arthritis and, irritable bowel disease; however, they pose a lot of side effects. The present study was taken up to explore the anti-inflammatory properties along with the phytochemicals present, its quantification, and other in vitro biological activities of the less reported Aspergillus melleus, an endophytic fungus, isolated from Premna serratifolia L., a medicinal plant. The results of the investigation demonstrated the presence of alkaloids, phenols, terpenoids, flavonoids, tannins, cardiac glycosides and amino acids in the methanolic extract of endophytic fungus. It yielded 25.28 µg GAE/g and 19.465 µg GAE/g of total phenolic and flavonoid content, respectively. The results of anti-inflammatory activity showed 84.69+0.82% protein inhibition by BSA and also showed IC50 values of 68.53 µg/mL and 43.34 µg/mL for COX1 and COX 2, respectively. It exhibited 63.91+0.08% of radical scavenging activity by DPPH. The IC50 values of 181.41 µg/mL and 190.62 µg/mL were found for the in vitro antidiabetic activity. This study shows that the endophytic fungus A. melleus has exhibited considerably good results with respect to its in vitro biological activities. Yet, there is a scope for future researchers to isolate the bioactive metabolites to explore for future needs

A REPORT ON A POTENT ANTHELMINTIC AGENT - UNBAKED COFFEE ARABICA BEAN EXTRACTS

Objective: Evaluation of anthelmintic activity of Coffee arabica unbaked bean extracts.Methods: C. arabica is most commonly found in India and possess major economic value, as is one of the common beverage consumed worldwide. Once ripe, coffee berries are picked, processed ground and brewed to create consumable coffee. During coffee processing, coffee berry pulp was produced as waste which may contain large amount of phytochemicals. Moreover, ripe coffee bean before subjecting to processing and brewing, it contains many potential secondary metabolites with various therapeutic applications. However, these potential molecules are lost during processing. Helminthes infections have devastating impact on humans from the time immemorial. Helminthes are one of the most common infectious agents mainly in developing countries. Pherithema posthuma is a commonly known helminth used as model organism, because of identical physiology with Ascaris. In this connection the anthelmintic property of Coffee arabica bean extracts were evaluated against Pherithema posthuma as an experimental helminthes model. Albendazole was used as the standard reference.Results: Among the various concentrations of chloroform extract tested, 200 µg/ml showed efficient anthelmintic activity and among all the concentrations of ethanolic extract tested, 200 µg/ml showed significant results. This investigation revealed that chloroform extract of C. arabica proved to be significant anthelmintic activity against Pheretima posthuma when compared aqueous extract, ethanolic extract and the standard drug.Conclusion: This investigation reports a new potent anthelmintic agent that can be used as a potent drug for the treatment of helminthes infection.Keywords:  Coffee Arabica; Anthelmintic activity; Pheretima posthuma; Ethanolic extract; Chloroform extract

Cytotoxic and pro-apoptotic effects of Abrus precatorius L. on human metastatic breast cancer cell line, MDA-MB-231

Abrus precatorius is highly regarded as a universal panacea in the herbal medicine with diverse pharmacological activity spectra. This experimental study on the mechanism of the anticancer activity of A. precatorius leaf extracts, may offer new evidence for A. precatorius in the treatment of breast cancer in clinical practice. Cell death was determined by using MTT assay. Further analyses were carried out by doing DNA laddering, PARP cleavage, FACS, semi-quantitative RT-PCR and detection of cellular reactive oxygen species (ROS) by DCFDA assay. A. precatorius showed very striking inhibition on MDA-MB-231 cells. MTT assay showed more than 75 inhibition of the cells and treated cells indicated visible laddering pattern with thick compact band. PARP cleavage produced 89 kDa cleavage product which was associated with apoptosis. Flow cytometer exhibited a sub-G0/G1 peak as an indicative of apoptosis. mRNA expression level of apoptosis-related genes p21 and p53 was markedly increased in cells treated with the extract as compared to control. The up-regulation of p21 and p53 may be the molecular mechanisms by which A. precatorius extract which induces apoptosis. An increase in the concentration of A. precatorius extract does not generate ROS, instead it reduces ROS formation in MDA-MB-231 cells, as evident from the shift in fluorescence below untreated control. This is the first report showing that A. precatorius leaf extract exhibits a growth inhibitory effect by induction of apoptosis in MDA-MB-231 cells. Our results contribute towards validation of the A. precatorius extract as a potentially effective chemopreventive or therapeutic agent against breast cancer. © 2012 Springer Science+Business Media B.V