Molecules 2011, 16(12), 9983-10001; doi:10.3390/molecules16129983

Inhibitors of Testosterone Biosynthetic and Metabolic Activation Enzymes

1,* email, 2email and 1,3,* email
Received: 2 November 2011; in revised form: 21 November 2011 / Accepted: 21 November 2011 / Published: 2 December 2011
(This article belongs to the Special Issue Steroids)
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Abstract: The Leydig cells of the testis have the capacity to biosynthesize testosterone from cholesterol. Testosterone and its metabolically activated product dihydrotestosterone are critical for the development of male reproductive system and spermatogenesis. At least four steroidogenic enzymes are involved in testosterone biosynthesis: Cholesterol side chain cleavage enzyme (CYP11A1) for the conversion of cholesterol into pregnenolone within the mitochondria, 3β-hydroxysteroid dehydrogenase (HSD3B), for the conversion of pregnenolone into progesterone, 17α-hydroxylase/17,20-lyase (CYP17A1) for the conversion of progesterone into androstenedione and 17β-hydroxysteroid dehydrogenase (HSD17B3) for the formation of testosterone from androstenedione. Testosterone is also metabolically activated into more potent androgen dihydrotestosterone by two isoforms 5α-reductase 1 (SRD5A1) and 2 (SRD5A2) in Leydig cells and peripheral tissues. Many endocrine disruptors act as antiandrogens via directly inhibiting one or more enzymes for testosterone biosynthesis and metabolic activation. These chemicals include industrial materials (perfluoroalkyl compounds, phthalates, bisphenol A and benzophenone) and pesticides/biocides (methoxychlor, organotins, 1,2-dibromo-3-chloropropane and prochloraz) and plant constituents (genistein and gossypol). This paper reviews these endocrine disruptors targeting steroidogenic enzymes.
Keywords: endocrine disruptor; steroidogenic enzymes; steroidogenic inhibitors; Leydig cells; male reproduction
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MDPI and ACS Style

Ye, L.; Su, Z.-J.; Ge, R.-S. Inhibitors of Testosterone Biosynthetic and Metabolic Activation Enzymes. Molecules 2011, 16, 9983-10001.

AMA Style

Ye L, Su Z-J, Ge R-S. Inhibitors of Testosterone Biosynthetic and Metabolic Activation Enzymes. Molecules. 2011; 16(12):9983-10001.

Chicago/Turabian Style

Ye, Leping; Su, Zhi-Jian; Ge, Ren-Shan. 2011. "Inhibitors of Testosterone Biosynthetic and Metabolic Activation Enzymes." Molecules 16, no. 12: 9983-10001.

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