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 gestonorone acetate (1) with Cunninghamella blakesleeana (ATCC 8688) yielded a new analogue, 17?-actoxy-10?,11?-dihydroxy-progesterone (2). Compound 2 was identified as non-cytotoxic inhibitor of human aromatase enzyme (IC50=0.827±0.066 ?M). Compound 2 showed a significant aromatase inhibitory activity, as compared to the standard aromatase inhibitory drug, exemestane (IC50=0.232±0.03 ?M).

Abstract: One embodiment of the invention relates to the treatment of diseases associated with increased butyrylcholinesterase (BuChE) enzyme activity such Alzheimer's Disease (AD), involving administering an effective amount of a compound selected from a group of new N, N?-disubstituted benzylamine derivatives (1-8) of 4-aminoantipyrine (ampyrone). The kinetic studies of two potent compounds 4-(Bis(4-iodobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (5) (IC50=2.43±0.4 and Ki=5.67±0.5 ?M) and 4-(Bis(2-bromobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (6) (IC50=0.7±0.2 and Ki=2.4±0.4 ?M), revealed them as a competitive and a non-competitive inhibitor of BuChE, respectively. Galantamine Hydrobromide was used as standard inhibitor with IC50=40.83±0.4 and Ki=21.5±0.7 ?M (Mixed type Inhibitor). The metabolite of aminophenazone, 4-aminoantipyrine (A) is also being reported here as an inhibitor of BuChE for the first time.

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: The present invention identifies new steroidal analogues of formestane synthesized through biotransformation with significant aromatase inhibitory activity, and thus can serve as possible safe, effective, and selective anti-cancer agent towards estrogen-responsive (ER+) breast cancer. Four new derivatives of anticancer drug formestane (1), 4?,5?,7?-trihydroxyandrostane-3,17-dione (2), 3?,7?-dihydroxyandrostane-4,17-dione (3), 3?,5?,7?-trihydroxyandrostane-4,17-dione (4), and 4,11?-dihydroxyandrosta-1,4-diene-3,17-dione (5) were synthesized through bio-catalyzed structural modifications by Cunninghamella. blakesleeana and Fusarium lini. The new derivatives showed varying degree of inhibition of aromatase enzyme. Metabolite 4 (IC50=0.386±0.072 ?M), showed a significant inhibitory potential, comparable to substrate 1 (IC50=0.335±0.011 ?M) and standard aromatase inhibitory anti-cancer drug exemestane (IC50=0.232±0.031 ?M). Metabolites 3 (IC50=1.37±0.029 ?M), and 2 (IC50=5.229±0.

Abstract: Four new analogues, 17?-hydroxy-7?,17?-dimethylestr-4,6-diene-3-one (2), 11?,17?-dihydroxy-7?, 17?-dimethyl-estra-1,3,5-triene-3-one (3), 3?,10?,17?-trihydroxy-7?,17?-dimethyl-5?-estrane (4), and 17?-hydroxy-7?,17?-dimethyl-5?-estrane-3,6-dione (5) of anabolic drug mibolerone (1) were synthesized. Derivatives 2 (IC50=3.83 ±0.3 ?M) and 3 (IC50=4.24 ±0.2 ?M) were identified as potent anti-inflammatory agents against T-cell proliferation. Derivative 4 (IC50=28.5 ±0.07 ?M) showed a potent anti-inflammatory activity against TNF-? production. In addition, compounds 1 (IC50=46.0 ±2.4 ?M), 2 (IC50=54.4 ±0.3 ?M), 3 (IC50=49.1 ±0.4 ?M), 4 (IC50=58.0 ±0.1 ?M) and 5 (IC50=52.7 ±0.3 ?M) showed a remarkable anti-inflammatory activity against NO? production. Metabolite 4 (IC50=0.072 ±0.001 ?M) showed a potent inhibitory activity against human placental aromatase. Compound 1 (IC50=24.19 ±2.1 ?g/mL) was found to be cytotoxic against BJ normal cell line, while metabolites 2-5 were identified as non-cytotoxic.

Abstract: Due to the SARS-CoV-2 pandemic, the development and screening of novel antiviral agents are urgently required. Herein, we developed herbal extracts with promising antiviral activity against SARS-CoV-2. Antiviral effects of Mentha piperita, and Flos chrysanthemi extracts alone, in combination and their fractions were found to decrease viral load. To determine which step of the virus is inhibited by the treatment, the extracts were administered at different time points of treatment, namely prophylactic (Full-time), pre-adsorption (Entry), and post adsorption (Post-entry). Most of the fractions, exhibited high efficacy upon prophylactic administration. The viral load was lower in prophylactic-treated cells than in non-treated cells. Administration of combinations, following 2:1 molar ratio of Mentha piperita, and Flos chrysanthemi significantly reduced the viral load by increasing the Cq values.

Abstract: One embodiment of the invention relates to the treatment of diseases associated with increased butyrylcholinesterase (BuChE) enzyme activity such Alzheimer's Disease (AD), involving administering an effective amount of a compound selected from a group of new N, N?-disubstituted benzylamine derivatives (1-8) of 4-aminoantipyrine (ampyrone). The kinetic studies of two potent compounds 4-(Bis(4-iodobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (5) (IC50=2.43±0.4 and Ki=5.67±0.5 ?M) and 4-(Bis(2-bromobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (6) (IC50=0.7±0.2 and Ki=2.4±0.4 ?M), revealed them as a competitive and a non-competitive inhibitor of BuChE, respectively. Galantamine Hydrobromide was used as standard inhibitor with IC50=40.83±0.4 and Ki=21.5±0.7 ?M (Mixed type Inhibitor). The metabolite of aminophenazone, 4-aminoantipyrine (A) is also being reported here as an inhibitor of BuChE for the first time.

Abstract: A dietary herbal health supplement to reduce the symptoms of Parkinson's disease in a human subject comprising orally administering to a subject in need thereof an effective amount of the supplement comprising Mucuna puriens L. (velvet beans), Camellia sinensis L. (green tea), Allium sativum L. (ginger), Juglan regia L. (walnut), Arachis hypogaea L. (peanut), Vitis vinifera L. (red grapes), and Eugenia caryophyllata Thunb. (clove). The supplement is safe with only natural ingredients.

Abstract: New analogues of anti-cancer drugs atamestane (1), drostanolone enanthate ((3), and exemestane (6) were synthesized through biotransformation. New derivatives, 14?-hydroxy-1-methylandrosta-1,4-diene-3,17-dione ((2) (IC50, 9.7±0.72 nM) of 1 (IC50, 13.8±0.2 nM), and 2-methylandrosta-12?,17?-dihydroxy-1,4-diene-3-one (4) (IC50, 4.23±0.133 nM) of 3 (IC50, 6.4±0.06 nM) showed a potent inhibition against human aromatase enzyme and thus have the potential to treat ER+ breast-cancers and other related diseases. New metabolites, 2?-methyl-9?,17?-dihydroxy-5?-androstan-3-one ((5) (IC50=793.0±29.9 nM) of 3, 6-methylene-3?,7?,17?-trihydroxy-5?-androstane (7) (IC50, 46.1±0.81 nM), and 11?,17?-dihydroxy-6-methylene-androsta-1,4-diene-3-one (8) (IC5O=12797.0±844 nM) of exemestane (6) (IC50=232.0±31 nM) also showed a remarkable anti-aromatase activity. Aromatase is an enzyme, involves in the synthesis of estrogen (ER).

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 food supplement to reduce symptoms of Parkinson's disease is disclosed. The food supplements contains a mixture of garlic, almond, peanut, tomato, grape, clove, black eye pea turmeric, tea and velvet bean.

Abstract: A food supplement to reduce symptoms of Parkinson's disease is disclosed. The food supplements contains a mixture of garlic, almond, peanut, tomato, grape, clove, black eye pea turmeric, tea and velvet bean.

Abstract: This invention provides that Ropinirole (4-[2-(Dipropylamino)ethyl]-1,3-dihydro-2H-indol-2-one) possess potent urease inhibitory potential (in vitro) with 97.3% inhibition and IC50=11.7+0.46 ?M, when compared to the standard inhibitors i.e. acetohydroxamic acid (IC50=41.5+1.50 ?M), and thiourea (IC50=21.0+0.50 ?M).

Abstract: The present invention relates to anti-thymidine phosphorylase compounds. These compounds are derivatives of 4-hydroxybenzohydarzide or generally Schiff bases of hydrazones. The invention evaluates a series of Schiff bases of hydrazones against thymidine phosphorylase, and identified significant inhibitors of thymidine phosphorylase enzyme during in vitro studies.

Abstract: This invention provides that (2S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]pyrrolidine-2-carboxylic acid (captopril) possess potent in vitro urease inhibitory potential with 95.00% inhibition and IC50=16.6±1.52 ?M, when compared to the standard inhibitor i.e. acetohydroxamic acid (IC50=41.5±1.50 ?M).

Abstract: Inhibitors of carbonic anhydrase-II derived from sulfanilamide are reported.

Abstract: One embodiment of the invention relates to treating diseases associated with increased urease enzyme activity comprising administering an effective amount of a compound selected from a group consisting of 28 thiazoles Schiff bases. Kinetic studies were performed on ten (10) of the most active compounds.

Abstract: Two thiourea derivatives N-(3-chlorophenyl)-N?-(3,4-difluorophenyl)thiourea and N-(3-chlorophenyl)-N-(3-methoxyphenyl)-thiourea are reported as treatment of multidrug resistance infections from Staphylococcus aureus.

Abstract: One embodiment of the invention relates to treating diseases associated with increased urease enzyme activity comprising administering an effective amount of a compound selected from a group consisting of 28 thiazoles Schiff bases. Kinetic studies were performed on ten (10) of the most active compounds.