Schinazi R F, Chu C K, Babu J R, Oswald B J, Saalmann V, Cannon D L, Eriksson B F, Nasr M
Veterans Affairs Medical Center, Decatur, GA 30033.
Antiviral Res. 1990 May;13(5):265-72. doi: 10.1016/0166-3542(90)90071-e.
Various anthraquinones substituted with hydroxyl, amino, halogen, carboxylic acid, substituted aromatic group, and sulfonate were tested to determine their activity against human immunodeficiency virus type 1 (HIV-1) in primary human lymphocytes. Among the compounds tested, polyphenolic and/or polysulfonate substituted anthraquinones were found to possess the most potent antiviral activity. Hypericin, an anthraquinone dimer previously shown to have activity against nonhuman retroviruses also exhibited anti-HIV-1 activity in lymphocytes. the active anthraquinones inhibited HIV-1 reverse transcriptase. However, this enzyme inhibition was selective only for 1,2,5,8-tetrahydroanthraquinone and hypericin. Hypericin interacts nonspecifically with protein suggesting that this effect may dictate its inhibitory activity against the viral reverse transcriptase.
测试了各种被羟基、氨基、卤素、羧酸、取代芳基和磺酸盐取代的蒽醌，以确定它们在原代人淋巴细胞中对1型人类免疫缺陷病毒（HIV-1）的活性。在所测试的化合物中，发现多酚和/或多磺酸盐取代的蒽醌具有最强的抗病毒活性。金丝桃素，一种先前已显示对非人类逆转录病毒具有活性的蒽醌二聚体，在淋巴细胞中也表现出抗HIV-1活性。活性蒽醌抑制HIV-1逆转录酶。然而，这种酶抑制仅对1,2,5,8-四氢蒽醌和金丝桃素具有选择性。金丝桃素与蛋白质非特异性相互作用，表明这种效应可能决定其对病毒逆转录酶的抑制活性。
