In the fight against androgen-sensitive prostate cancer, the enzyme 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) is an attractive therapeutic target considering its key role in the formation of androgenic steroids. In this study, we attempted to assess the in vivo efficacy of the compound RM-532-105, an androsterone derivative developed as an inhibitor of 17β-HSD3, in the prostate cancer ...

The metabolism of some steroids has been investigated in liver microsomal preparations from male germ-free and conventional rats. Hydroxylation of 4-[4-14C]androstene3,17-dione in positions 60 and 16~~ is about 2 and 1.5 times more efficient in germ-free than in conventional rats. The same is true for 6/3and Zol-hydroxylation of 4-[4J4C]pregnene-3,20-dione (about 1.6 and 1.2 times larger, respe...

There are no translations available. The inviolable assumption that obesity is simply a thermodynamic problem of calories in/calories out is being dissembled by the science linking environmental t oxins to obesity and diabetes. Exposure to environmental toxins in the absence of increased caloric intake induces weight gain and insulin resistance. Stated simply, toxins are an invisible, unappreci...

Methylenetetrahydrofolate reductase (MTHFR) is a critical folate-metabolising enzyme which requires riboflavin as its co-factor. A common polymorphism (677C T) in the MTHFR gene results in reduced MTHFR activity in vivo which in turn leads to impaired folate metabolism and elevated homocysteine concentrations. Homozygosity for this polymorphism (TT genotype) is associated with an increased risk...

Pyrene degradation is known in bacteria. In this study, Mycobacterium sp. strain KMS was used to study the metabolites produced during, and enzymes involved in, pyrene degradation. Several key metabolites, including pyrene-4,5-dione, cis-4,5-pyrene-dihydrodiol, phenanthrene-4,5-dicarboxylic acid, and 4-phenanthroic acid, were identified during pyrene degradation. Pyrene-4,5-dione, which accumul...

Mycobacteria have been modified to transform sterols to produce valuable steroids. Here, we demonstrated that the oxidation of sterols to sterones is a rate-limiting step in the catabolic pathway of sterols in Mycobacterium neoaurum. Two cholesterol oxidases ChoM1 and ChoM2 involved in the step were identified in M. neoaurum and the ChoM2 shared up to 45% identity with other cholesterol oxidase...

A series of N-[(4-arylpiperazin-1-yl)-alkyl]-2-azaspiro[4.5]decane-1,3-dione derivatives were synthesized and evaluated for their anticonvulsant and neurotoxic properties. The main modifications to that series of compounds consisted in the introduction of an aromatic area to the cyclohexane ring as a flexible fragment with conformational freedom (1a-h), or as a rigidified skeleton (2a-h). Excep...

DNA intercalators belong to aromatic heterocyclic compounds interacting reversibly with DNA. These compounds have been used extremely as cytotoxic agents against cancer. In this study, the synthesis and biological activity of some novel derivatives of cyclopenta [b] quinoline-1, 8-dione as new intercalating agent were investigated. Twenty novel derivatives of cyclopenta [b] quinoline-1, 8-dione...