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: 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: This invention provides new anticancer analogs of antimicrobial peptide temporin-SHa. New analogs (SEQ ID NOs: 2-6) of temporin SHa and, two different conjugates (7 & 8) comprising of monomeric and dimeric form of SEQ ID NO 4 with cancer targeting ligand were identified as anticancer peptides.

Abstract: This invention provides new anticancer analogs of antimicrobial peptide temporin-SHa. New analogs (SEQ ID NOs: 2-6) of temporin SHa and, two different conjugates (7 & 8) comprising of monomeric and dimeric form of SEQ ID NO 4 with cancer targeting ligand were identified as anticancer peptides.

Abstract: Patuletin, a flavonoid isolated from Tagetes patula, was discovered to be a potent inhibitor of TNF-? production and thus useful in treating diseases related to TNF-? levels in the body.

Abstract: Azadirachta indica cell suspension culture was used for the biotransformation of dianabol to yield a metabolite 17?-hydroxy-17?-methyl-5?-androstan-3-one, which can also be synthesized, as a potent antiinflammatory agent.