Ridley Christian P, Reddy M Venkata Rami, Rocha Genalyn, Bushman Frederic D, Faulkner D John
Scripps Institution of Oceanography, University of California at San Diego, La Jolla, CA 92093-0212, USA.
Bioorg Med Chem. 2002 Oct;10(10):3285-90. doi: 10.1016/s0968-0896(02)00237-7.
In order to explore the influence of sulfate groups on the bioactivity profiles of marine alkaloids of the lamellarin class, three such alkaloids, lamellarin alpha, lamellarin alpha 13,20-disulfate and lamellarin H, were synthesized and their activities against HIV-1 integrase and cancer cell lines were compared with those of lamellarin alpha 20-sulfate, which is a selective inhibitor of HIV-1 integrase. Lamellarin alpha does not inhibit HIV-1 integrase but shows moderate cytotoxicity with good cell line selectivity. Lamellarin alpha 13,20-disulfate is a moderate inhibitor of both HIV-1 integrase and cancer cell lines. Lamellarin H is a more potent inhibitor of HIV-1 integrase but lacked the specificity required to be medicinally useful.
为了探究硫酸根对片螺素类海洋生物碱生物活性谱的影响，合成了三种此类生物碱，即片螺素α、片螺素α 13,20 - 二硫酸盐和片螺素H，并将它们对HIV-1整合酶和癌细胞系的活性与片螺素α 20-硫酸盐（HIV-1整合酶的选择性抑制剂）进行了比较。片螺素α不抑制HIV-1整合酶，但具有中等细胞毒性且细胞系选择性良好。片螺素α 13,20 - 二硫酸盐是HIV-1整合酶和癌细胞系的中度抑制剂。片螺素H是一种更有效的HIV-1整合酶抑制剂，但缺乏作为药用所需的特异性。
