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标题：Antitumor Activity of Liposomal Naphthoquinone Esters Isolated from Thai Medicinal Plant: Rhinacanthus nasutus KURZ.
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作者：Pongpun Siripong ; Jantana Yahuafai ; Kosuke Shimizu 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2006
卷号：29
期号：11
页码：2279-2283
DOI：10.1248/bpb.29.2279
出版社：The Pharmaceutical Society of Japan
摘要：We previously observed that rhinacanthins-C, -N and -Q, three main naphthoquinone esters isolated from the roots of Thai medicinal plant; Rhinacanthus nasutus K URZ . (Acanthaceae) induced apoptosis of human cervical carcinoma HeLaS3 cells. Since these rhinacanthins showed limited solubility in aqueous medium, we attempted to entrap them into liposomal membrane: Liposomalization enabled injection of the drugs and the drugs were expected to transfer to lipoproteins in the bloodstream. Liposomal formulations of rhinacanthins-C, -N and -Q showed strong antiproliferative activity against HeLaS3 cells with the IC₅₀ values of 32, 17, 70 μ M ; 19, 17, 52 μ M and 2.7, 2.0 and 5.0 μ M for the exposure time of 24, 48, and 72 h, respectively. These liposomes suppressed the tumor growth in Meth-A sarcoma-bearing BALB/c mice at the dose of 5.0 mg/kg/d for 10 d. Among rhinacanthins, liposomal rhinacanthin-N significantly suppressed solid tumor growth. Based on these results, our findings demonstrated that rhinacanthin-N suppressed tumor growth in vivo , and suggested that liposomes are useful for preparing injectable formulation of hydrophobic drugs.
关键词：Rhinacanthus nasutus;naphthoquinone ester;rhinacanthin;liposome;antitumor activity