Anti-androgenic effect of sesquiterpenes isolated from the rhizomes of Curcuma aeruginosa Roxb.

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• 作者：Nungruthai Suphrom^a ; Ganniga Pumthong^b ; Nantaka Khorana^c ; Neti Waranuch^b ; Nanteetip Limpeanchob^d ; Kornkanok Ingkaninan^a ; ^c ; ^{k_ingkaninan@yahoo.com}
• 关键词：Anti-androgen ; Curcuma aeruginosa ; 5¦Á-reductase ; Germacrone ; LNCaP cell ; Sesquiterpenes
• 刊名：Fitoterapia
• 出版年：2012
• 出版时间：July, 2012
• 年：2012
• 卷：83
• 期：5
• 页码：864-871
• 全文大小：1000 K

文摘

Six sesquiterpenes: germacrone (1), zederone (2), dehydrocurdione (3), curcumenol (4), zedoarondiol (5) and isocurcumenol (6) were isolated from rhizomes of Curcuma aeruginosa Roxb. (Zingiberaceae). They inhibited 5¦Á-reductase which converts testosterone to dihydrotestosterone (DHT). Germacrone (1) was the most potent (IC₅₀ = 0.42 ¡À 0.05 mg/mL). Compound 1 was anti-androgenic in LNCaP cells when proliferation was testosterone-induced. The growth of flank gland of male Syrian hamsters is dependent on circulating androgen and when maintained with testosterone, 1 (3, 30, 100 ¦Ìg) inhibited growth but was ineffective against DHT. The similar activity profile was observed on the 5¦Á-reductase inhibitor, finasteride (100 ¦Ìg) treatment group. The androgen receptor binding assay showed that 1 did not bind to the androgen receptor. In conclusion, 1 showed anti-androgenic effect on in vitro and in vivo assays. One of the possible mechanisms was inhibition 5¦Á-reductase activity. Thus, 1 is a potential lead compound for treatment of androgen-dependent disorders.