Abstract: Biotransformation of an aromatase inhibitor, testolactone (1), yielded four metabolites, 7?-hydroxy-3-oxo-13,17-seco-5?-androsta-1-eno-17,13?-lactone (2), 3?,11?-dihydroxy-13,17-seco-5?-androsta-17,13?-lactone (3), 4?,5?-epoxy-3?-hydroxy-13,17-secoandrosta-1-eno-17,13?-lactone (4), and 4?,5?-epoxy-3?-hydroxy-13,17-secoandrosta-1-eno-17,13?-lactone (5). Aromatase (estrogen synthase) involves in the synthesis of estrogen, and promotes the growth of breast cancerous cells. It is a key target for the discovery of chemotherapeutic agents against ER+(estrogen-positive) breast-cancers. Metabolites 2 (IC50=8.63±0.402 nM), and 3 (IC50=9.23±1.31 nM) were identified as potent inhibitors against human aromatase enzyme, in comparison to 1 (IC50=0.716±0.031 ?M), and the standard aromatase inhibiting drug, exemestane (IC50=0.232±0.031 ?M). Derivatives 4 (IC50=10.37±0.50 ?M) and 5 (IC50=0.82±0.059 ?M) also showed a good inhibition against aromatase enzyme.

Abstract: Biotransformation of medroxyprogesterone acetate (MPA) (1) with Cunninghamella blakesleeana (ATCC 8688) yielded five new analogues, i.e. 17?-acetoxy-6?-methylpregn-4-ene-3,11,20-trione (2), 17?-acetoxy-15?-hydroxy-6?-methylpregn-4-ene-3,11,20-trione (3), 17?-acetoxy-6?-hydroxy-6?-methylpregn-4-ene-3,11,20-trione (4), 17?-acetoxy-11?,15?-dihydroxy-6?-methylpregn-4-ene-3,20-dione (5), and 17?-acetoxy-6?,11?-dihydroxy-6?-methylpregn-4-ene-3,20-dione (6). In T-cell proliferation assay, metabolites 2, and 5 were found to be potent inhibitors with IC50<0.5 ?M, metabolite 6 showed a significant activity with IC50=8.64±0.02 ?M, while metabolites 3 and 4 were found to be moderately active with IC50=41.59±8.14, and 40.14±0.12 ?M, as compared to substrate 1 (IC50=6.48±5.18 ?M) and standard prednisolone (IC50=9.75±0.03 ?M) in in vitro assay. To establish the binding mode of medroxyprogesterone acetate (MPA) and the bio-transformed derivatives, molecular docking simulations were carried out using Vina.

Abstract: Biotransformation of an aromatase inhibitor, testolactone (1), yielded five new metabolites, 7?-hydroxy-3-oxo-13,17-secoandrosta-1,4-dieno-17,13?-lactone (2), 7?-hydroxy-3-oxo-13,17-seco-5?-androsta-1-eno-17,13?-lactone (3), 3?,11?-dihydroxy-13,17-seco-5?-androsta-17,13?-lactone (4), 4?,5?-epoxy-3?-hydroxy-13,17-secoandrosta-1-eno-17,13?-lactone (5), and 4?,5?-epoxy-3?-hydroxy-13,17-secoandrosta-1-eno-17,13?-lactone (6). Aromatase (estrogen synthase) involves in the synthesis of estrogen, and promotes the growth of breast cancerous cells. It is a key target for the discovery of chemotherapeutic agents against ER+ (estrogen-positive) breast-cancers and several other diseases caused by overexpression of aromatase enzyme. Metabolites 3 (IC50=8.60±0.402 nM), and 4 (IC50=9.23±1.31 nM) were identified as potent inhibitors against human aromatase enzyme, in comparison to 1 (IC50=0.716±0.031 ?M), and the standard aromatase inhibiting drug, exemestane (IC50=0.232±0.031 ?M). Derivatives 2 (IC50=11.68±0.

Abstract: A method for treating the onset of obesity, reducing dyslipidemia and improving insulin sensitivity in mammals comprising administering a therapeutically effective amount of dried alcoholic extract of Cordia latifolia orally at a dose of 300 mg/kg of body weight to mammals in need for the reducing body weight and managing diabetic conditions.

Abstract: The present invention relates to reducing insulin resistance by administering an oral dose of an ethanolic extracts of Borago officinalis Linn., wherein the treatment further reduces dyslipidemia, hypertension, cardiovascular diseases, and resistance to insulin.

Abstract: A method for treating the onset of obesity, reducing dyslipidemia and improving insulin sensitivity in mammals comprising administering a therapeutically effective amount of dried alcoholic extract of Cordia latifolia orally at a dose of 300 mg/kg of body weight to mammals in need for the reducing body weight and managing diabetic conditions.

Abstract: Novel ?-Glucosidase inhibitors include propanone substituted indole ring-containing heterocyclic compounds, which are represented by Formula I: Wherein R1 is thiophene, 2,4-di chloro phenyl, 2,6-di chloro phenyl, bromo phenyl, benzyl or nitrophenyl; and R2 is an aryl group, or stereoisomers or pharmaceutically acceptable salts thereof.

Abstract: Novel ?-Glucosidase inhibitors include propanone substituted indole ring-containing heterocyclic compounds, which are represented by Formula I: Wherein R1 is thiophene, 2,4-di chloro phenyl, 2,6-di chloro phenyl, bromo phenyl, benzyl or nitrophenyl; and R2 is an aryl group, or stereoisomers or pharmaceutically acceptable salts thereof.

Abstract: The diethylammonium salts of phenyl-substituted thiobarbituric acid as anti-diabetic agents include compounds having the formula: wherein X is: and wherein R1 is selected from the group consisting of a hydrogen, halogen, methyl, trifluoromethyl, methoxy, and nitro, and R2 is either halogen or hydrogen, the R1 and R2 substituents being independently bonded to an ortho-, meta-, or para-carbon of the phenyl substituent.

Abstract: The present invention relates to the effects of Physalis minima L. methanolic extract on dyslipidemia and insulin resistance in insulin resistant high-fat diet-induced obese rats without any systemic toxicities. The extract reversed the dyslipidemia and insulin resistance in high-fat diet-induced obese rats.

Abstract: Quinazoline derivatives 1-25, (2-[3,4-bis(methyloxy)phenyl]quinazolin-4-(3H)-one) and 2-[2-(ethyloxy)phenyl]quinazoline-4-(3H)-one) are reported as ?-glucuronidase inhibitors useful in the treatment of ?-glucuronidase hyperactivity disorders.

Abstract: Treatment of leishmaniasis in animals and humans using the methanolic extract of Physalis minima in petrolatum is described.