Antiproliferative effects of Vanilla planifolia leaf extract against breast cancer MCF-7 cells

Background: Breast cancer is the most common cancer disease among females in India and worldwide. This needs a critical research for finding the drugs to treat breast cancer with less side effects. The aim of the present study is to reveal the anti-proliferative effects of vanilla extract against MCF-7 cells.Methods: To reveal anti proliferative effects of vanilla leaf extract, MTT assay, cell cycle analysis and DNA fragmentation assay was performed as per standard protocols.Results: MTT assay showed decrease in cell viability with increase of dose of extract and revealed IC50 value at 31.2µg/ml. DNA fragmentation was seen in extract treated cells.Conclusions: The results of the present study confirm the antiproliferative property of vanilla leaf extract in MCF-7 cells. This study results conclude vanilla leaf extract as an effective plant source medicament for treating breast cancer

ALPHA-AMYLASE AND ALPHA-GLUCOSIDASE INHIBITORY EFFECTS OF CALLIANDRA HAEMATOCEPHALA AND ITS POTENTIAL ROLE IN DIABETES MELLITUS

Objective: The global burden and the high prevalence of diabetes mellitus in India signify the importance of its control with effective measures. Particularly, intestinal alpha-amylase and alpha-glucosidase enzyme inhibitors reduce postprandial hyperglycemia and play a key role in preventing diabetic complications. Herbal plants also possess greater antioxidant, enzyme inhibitory, and antihyperglycemic activities with minimal side effects. Hence, this study is done to elucidate the inhibition of alpha-amylase and alpha-glucosidase enzyme activity and antidiabetic potential of Calliandra haematocephala.Methods: The leaves of C. haematocephala extracted by ethanol as a solvent were used to elucidate the blocking of alpha-amylase and alpha-glucosidase enzymes for antidiabetic effect, and the absorbance was measured using spectrophotometry. The percentage of inhibition and half maximal inhibitory concentration (IC50) value of the plant and control were calculated.Results: The maximum percentage inhibition of C. haematocephala against alpha-amylase was 61% (IC50 value of 82.18 μg/ml) and alpha-glucosidase was 71% (31.07 μg/ml). The maximum percentage inhibition of acarbose against alpha-amylase was 92% (IC50 value of 42.65 μg/ml) and alpha-glucosidase was 89% (62.28 μg/ml).Conclusion: Hence, the above study proved the antidiabetic activity of C. haematocephala and its significant role in the pharmacotherapy of diabetes mellitus

MOLECULAR DOCKING STUDIES ON FLAVONOID COMPOUNDS: AN INSIGHT INTO AROMATASE INHIBITORS

Objective: Aromatase is a key enzyme that plays a crucial role in the synthesis of estrogen and has a major effect in pathogenesis of estrogen‑dependent disease, including breast cancer, endometrial cancer, and endometriosis. The abnormal over expression of aromatase can be inhibited by aromatase inhibitors. The objective of the present study is to evaluate the binding interaction of flavonoid compounds with cytochrome P450 enzyme aromatase, which is involved in the metabolism of estrogens and considered as a powerful target for treatment of estrogen-dependent breast cancers. Methods: To understand the mechanisms involved in the binding of flavonoid compounds and their interactions with the binding site of aromatase, molecular docking studies were carried using Autodock 4.2. Results: The docking results revealed that, benzoflavanones showed higher binding affinity compared to other class of compounds. The presence of hydrogen bond interaction and cation–π interaction contributed to their higher binding affinity. The flavonoid compounds with unsubstituted or less substituted rings showed higher binding affinity than those with substituted rings. The hydrogen bonding interactions were predominant in all the classes of compounds considered for the study and were found to be important for inhibition. The docking studies showed that the binding energies mainly depend on aromatic properties like cation–π and π–π interactions. These properties play a key role in determining the biological activity of flavonoid compounds. Conclusion: The present findings provided valuable information on the binding process of flavonoid compounds to the binding site of aromatase and revealed the structural requirement needed for binding

COMPARATIVE ANALYSIS OF THE ANTICANCER ACTIVITY OF ANGIOTENSIN RECEPTOR BLOCKERS - IRBESARTAN AND TELMISARTAN

Objective: Angiotensin receptor blockers (ARBs) are effective hypertensive drugs. Reduction in risk of lung cancer with ARBs was proven in clinical studies. Telmisartan and irbesartan are the second-generation ARBs. This study screens the anticancer activity of these two drugs in a dose-dependent manner using A549 cell line.Methods: Different concentrations of irbesartan and telmisartan were treated on A549 cells and the anticancer activity was evaluated through methylthiazolyldiphenyl-tetrazolium [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] cytotoxicity assay. The dot plot of the cytotoxicity results was used to extrapolate the half maximal inhibitory concentration (IC50) values. Microscopic changes in the cells post-treatment with these drugs were also recorded at ideal concentrations.Results: A reduction in cell viability was noted in A549 cells with increasing concentration of the drug. The IC50 values for irbesartan and telmisartan were 31.1 μg and 15.6 μg, respectively. Microscopic observation of the cells shows more rounded and deformed dead cells on telmisartan- and irbesartan-treated cells when compared with the untreated control.Conclusion: The results confirm the anticancer activity of both the drugs with telmisartan being more efficient. The anticancer activity could probably be due to the role of irbesartan and telmisartan in inhibiting mitogen-activated protein kinase cell survival pathway and local angiogenesis

A COMPARATIVE STUDY OF ANTI-ANGIOGENIC ACTIVITIES OF MEDICINAL PLANTS AND ITS THERAPEUTIC POTENTIAL IN ANGIOGENESIS-DEPENDENT DISORDERS

AbstractIntroductionAngiogenesis, the process of new vessel growth from pre-existing capillaries is involved in physiological and pathological process such as embryonic development, wound healing, diabetic retinopathy ,chronic inflammation, tumor growth and metastasis. Vascular endothelial growth factor (VEGF) induced angiogenesis plays an important role in the pathogenesis of diabetic retinopathy and cancer and anti VEGF factor agents are found to be effective . VEGF inhibitors from plant sources show promising result recently. So this study is designed to evaluate and compare the VEGF inhibitory effect of the herbs Osimum Sanctum, Andrographis paniculata, Syzygium cumini and Ginkgo biloba by using in vivo models.Methods: Both Corneal neovascularization assay and Chick Chorioallantoic membrane assays were used for evaluation. The induced neovascularization was compared with control and extract treated groups.Results: The acute and repeated dose toxicity tests showed that the extracts are safe on oral administration. And also the results showed significant antiangiogenic effect of individual extract and their combination in both in vivo models. However the combination of the extract showed excellent result (p <0.001) by reducing neovascularization in both modelsConclusion: The above results suggested that combination of the above extracts have promising future in the management of angiogenesis dependent disorders.Key words: Osimum Sanctum, Andrographis paniculata, Syzygium cumini, Ginkgo biloba,   Angiogenesis, chorioallantoic membrane, angiogenesis dependent disorders

EVALUATION OF THE RATIONALITY OF CLAIMS MADE IN DRUG PROMOTIONAL LITERATURE IN WEST CHENNAI

Objective: The study was aimed to evaluate the adequacy of information provided by drug promotional literature using WHO criteria. They were alsoevaluated for the quality, types of claims and the genuineness of these claims in this literature.Methods: 412 drug promotional literature were collected from 20 busy physicians in the western part of Chennai from their private clinics. In additionto carrying out of WHO criteria, 1988,†the brochures were examined for the quality of coverage using a pre-tested and pre-validated checklist andtypes of claims and the genuineness of these claims were evaluated for their recoverability and accuracy.Results: It was found that all the WHO criteria were not fulfilled by any of the promotional literature. 91.2% of leaflets satisfied the 4 WHO criterianamely, the brand name, generic name, approved therapeutic uses, name and address of the manufacturer. A most neglected aspect of drug promotionwas information regarding drug interactions, precautions, Adverse drug reactions and overdosage (<10%). Of 412 leaflets collected, the quantitativeresearch methods were mentioned in 67 (16.2%). Cardiovascular drugs and nutritional supplements were the most promoted drug groups (23% and17%, respectively). 412 drugs promotional literature made a total of 954 claims. References were cited in 47% of the literature of which 96% werefrom the indexed journal and were retrievable.Conclusion: Drug promotional literature analyzed by this study was inadequate in terms of their adequacy, quality and genuineness of coverage.Thus, the pharmaceutical companies did not follow the WHO guidelines while promoting their products, thus aiming to satisfy their commercialmotive rather than fulfilling the educational aspect of promotion.Keywords: Promotional literature, Ethical criteria for drug promotion, Pharmacy practice, marketing practice

Theoretical study on the structure and stability of ring inverted porphyrin isomers

B3LYP/6-31+G** and B3LYP/6-31G calculations were done on 28 isomers of ring inverted porphyrin isomers. A systematic approach is adopted by computing the effect of relative stabilities and structural reorganization upon sequential ring-inversion. While the initial and all subsequent inversions lead to severe increase in the strain, the increase find to be non-linear and in most cases, the inverted structures encounter ring fusions. Both fused and non-fused structures of the singly, doubly, triply and fully inverted isomers were located as minima on the potential energy surface. Consistently, the non-fused isomers are lower in energy compared to their fused counterparts, which indicates that even in the inverted structures the extended conjugation bring in stabilization

A theoretical study on cycloaddition reactions between [c]-annelated heterocyclic five-membered dienes and acetylene

B3LYP/6-31G∗ calculations were done on a series of [c]-annelated carbo- and heterocyclic five-membered dienes and their cycloaddition transition state structures and products with acetylene as dienophile. While the reactions of cyclobutano[c]- and cyclobuteno[c]- fused five membered rings are to be categorized as traditional [4+2] cycloadditions, those of benzo[c]-fused five-membered rings are best described as [8+2] cycloaddition reactions. High exothermicities of products of 3X are to be traced directly to the formation of an aromatic benzenoid ring. In contrast, the formation of antiaromatic cyclobutadiene moiety hinders the feasibility of the reactions with 2X dienes. The computed percentage of bond length stretching/shortening of the important bonds, frontier orbital analysis, the quantum of charge transfer from diene to dienophile at the transition state and deformation energies were used to corroborate the reactivity of masked dienes