Anti-Candida albicans activity and pharmacokinetics of pogostone isolated from Pogostemonis Herba

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• 作者：Yu-Cui Li^a ; ¹ ; Hai-Chun Liang^a ; ¹ ; Hai-Ming Chen^a ; Li-Rong Tan^a ; Yu-Yang Yi^a ; Zhen Qin^a ; Wei-Min Zhang^b ; Dian-Wei Wu^a ; Chu-Wen Li^c ; Rong-Feng Lin^a ; Zi-Ren Su^a ; ^c ; ^{suziren@gzhtcm.edu.cn} ; Xiao-Ping Lai^a ; ^c ; ^{lxp88@gzhtcm.edu.cn}
• 关键词：Pogostone ; Anti-Candida albicans activity ; Pharmacokinetics ; Acute toxicity
• 刊名：Phytomedicine
• 出版年：2012
• 出版时间：15 December, 2012
• 年：2012
• 卷：20
• 期：1
• 页码：77-83
• 全文大小：1024 K

文摘

The present work was designed to evaluate the in vitro and in vivo anti-Candida activity of pogostone (PO), a natural product isolated from Pogostemon cablin (Blanco) Benth. PO showed potent in vitro activity against clinical Candida spp. isolates tested in this study. PO and the reference drug voriconazole (VRC) were equally effective against all the fluconazole-resistant Candida albicans strains, with MIC ranging from 3.1 ¦Ìg/ml to 50 ¦Ìg/ml. Besides, PO was fungicidal against all Candida isolates with MFC ranging from 50 ¦Ìg/ml to 400 ¦Ìg/ml. By contrast, VRC was fungistatic as it failed to elicit a fungicidal effect against the Candida spp. isolates at the highest tested concentration (400 ¦Ìg/ml). Furthermore, oral and topical PO administration effectively reduced the fungal load in vagina of vulvovaginal candidiasis mouse models. Topical PO administration (1.0-4.0 mg/kg) demonstrated higher activity against the vulvovaginal candidiasis than VRC (4.0 mg/kg). The pharmacokinetics and safety profile of PO were also investigated. The pharmacokinetics assay revealed that PO was easily absorbed after oral administration in mice, which might account for its in vivo anti-Candida effect. The acute toxicity test showed that the median lethal dose of PO in mice was 355 mg/kg, which was much higher than the daily dose used for the therapeutic experiments. This study demonstrated the potential of PO as a promising candidate for the treatment of Candida infections, particularly for vulvovaginal candidiasis.