具有HIV抑制作用的天然产物。11. 海洋无脊椎动物中硫酸化甾醇的比较研究。
HIV-inhibitory natural products. 11. Comparative studies of sulfated sterols from marine invertebrates.
作者信息
McKee T C, Cardellina J H, Riccio R, D'Auria M V, Iorizzi M, Minale L, Moran R A, Gulakowski R J, McMahon J B, Buckheit R W
机构信息
Laboratory of Drug Discovery Research and Development, National Cancer Institute, Frederick, Maryland 21702-1201.
出版信息
J Med Chem. 1994 Mar 18;37(6):793-7. doi: 10.1021/jm00032a012.
A total of 22 sulfated sterols isolated from marine sponges, ophiuroids (brittle stars), and asteroids (sea stars) were comparatively evaluated for their antiviral activity against HIV-1 and HIV-2. In general, sterols with sulfate groups at position 2, 3, or 6 were the most active, with EC50 values of 3-13 microM against HIV-1 (RF) and 2-8 microM against HIV-2 (CBL20). Those compounds which were sulfated on the sterol D ring were completely inactive against both HIV-1 and HIV-2. Overall, sulfated sterols active against HIV-1 were also active against HIV-2.
从海洋海绵、蛇尾纲动物（脆星）和海星纲动物（海星）中分离出的总共22种硫酸化甾醇，针对其对HIV-1和HIV-2的抗病毒活性进行了比较评估。一般来说，在2、3或6位带有硫酸基团的甾醇活性最高，对HIV-1（RF）的EC50值为3-13微摩尔，对HIV-2（CBL20）的EC50值为2-8微摩尔。那些在甾醇D环上硫酸化的化合物对HIV-1和HIV-2均完全无活性。总体而言，对HIV-1有活性的硫酸化甾醇对HIV-2也有活性。
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