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Fitoterapia. 2016 Jun;111:66-72. doi: 10.1016/j.fitote.2016.04.014. Epub 2016 Apr 19.

Suppression of rat and human androgen biosynthetic enzymes by apigenin: Possible use for the treatment of prostate cancer.

Author information

1
Centre of Scientific Research, The Second Affiliated Hospital, Wenzhou Medical University, Wenzhou, Zhejiang 325027, China.
2
Department of Pharmacy, Zhejiang Cancer Hospital, Hangzhou, Zhejiang 310022, China. Electronic address: huangpwly@sina.com.
3
Centre of Scientific Research, The Second Affiliated Hospital, Wenzhou Medical University, Wenzhou, Zhejiang 325027, China. Electronic address: r_ge@yahoo.com.

Abstract

Apigenin is a natural flavone. It has recently been used as a chemopreventive agent. It may also have some beneficial effects to treat prostate cancer by inhibiting androgen production. The objective of the present study was to investigate the effects of apigenin on the steroidogenesis of rat immature Leydig cells and some human testosterone biosynthetic enzyme activities. Rat immature Leydig cells were incubated for 3h with 100μM apigenin without (basal) or with 1ng/ml luteinizing hormone (LH), 10mM 8-bromoadenosine 3',5'-cyclic monophosphate (8BR), and 20μM of the following steroid substrates: 22R-hydroxychloesterol (22R), pregnenolone (P5), progesterone (P4), and androstenedione (D4). The medium levels of 5α-androstane-3α, 17β-diol (DIOL), the primary androgen produced by rat immature Leydig cells, were measured. Apigenin significantly inhibited basal, 8BR, 22R, PREG, P4, and D4 stimulated DIOL production in rat immature Leydig cells. Further study showed that apigenin inhibited rat 3β-hydroxysteroid dehydrogenase, 17α-hydroxylase/17, 20-lyase, and 17β-hydroxysteroid dehydrogenase 3 with IC50 values of 11.41±0.7, 8.98±0.10, and 9.37±0.07μM, respectively. Apigenin inhibited human 3β-hydroxysteroid dehydrogenase and 17β-hydroxysteroid dehydrogenase 3 with IC50 values of 2.17±0.04 and 1.31±0.09μM, respectively. Apigenin is a potent inhibitor of rat and human steroidogenic enzymes, being possible use for the treatment of prostate cancer.

KEYWORDS:

17α-Hydroxylase/17.20-lyase; 17β-Hydroxysteroid dehydrogenase 3; 3β-Hydroxysteroid dehydrogenase; Steroidogenesis

PMID:
27102611
DOI:
10.1016/j.fitote.2016.04.014
[Indexed for MEDLINE]

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