从中华蛇菰根茎中分离得到的木脂素、倍半木脂素和二木脂素，新型 HIV-1 蛋白酶和致细胞病变效应抑制剂。
Lignan, sesquilignans and dilignans, novel HIV-1 protease and cytopathic effect inhibitors purified from the rhizomes of Saururus chinensis.
机构信息
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, 599 Kwanangno, Kwanak-gu, Seoul 151-742, Republic of Korea.
出版信息
Antiviral Res. 2010 Feb;85(2):425-8. doi: 10.1016/j.antiviral.2009.11.002. Epub 2009 Nov 10.
Five lignans were isolated from the ethyl acetate extracts of Saururus chinensis rhizomes and evaluated for anti-HIV-1 activity. Their structures were elucidated as two dilignans, manassantin A (1), manassantin B (2), two sesquilignans, saucerneol B (3) and saucerneol C (4), and a new lignan, saururin B (5) by spectroscopic analysis. Of these components, manassantin A (1) and saururin B (5) showed dose-dependent inhibitory activities on HIV-1 protease with IC(50) values of 38.9 and 5.6 microM. In addition, manassantins A (1), B (2) and saucerneol B (3) inhibited HIV-1-induced cytopathic effects in a human T lymphoblastoid cell line with IC(100) values of 1.0, 1.0 and 0.2 microM, respectively. Of these active constituents, saucerneol B (3) showed the most potent and selective anti-HIV-1 activity (IC(100) of 0.2 microM, CC(0) of >125.0 microM, and SI of >520.8).
从中华石龙尾根茎的乙酸乙酯提取物中分离得到 5 种木脂素，并对其抗 HIV-1 活性进行了评价。通过光谱分析，将它们的结构鉴定为 2 种二木脂素，即马桑亭 A（1）和马桑亭 B（2），2 种倍半木脂素，即薤白醇 B（3）和薤白醇 C（4），以及 1 种新的木脂素，即 Saururin B（5）。其中，马桑亭 A（1）和 Saururin B（5）对 HIV-1 蛋白酶表现出剂量依赖性抑制活性，IC50 值分别为 38.9 和 5.6 μM。此外，马桑亭 A（1）、B（2）和薤白醇 B（3）在人 T 淋巴母细胞系中抑制 HIV-1 诱导的细胞病变效应，IC100 值分别为 1.0、1.0 和 0.2 μM。在这些活性成分中，薤白醇 B（3）表现出最强和最具选择性的抗 HIV-1 活性（IC100 为 0.2 μM，CC0 为 >125.0 μM，SI 为 >520.8）。
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