Hudson J B, Delaey E, de Witte P A
Department of Pathology and Laboratory Medicine, University of British Columbia, Vancouver, Canada.
Photochem Photobiol. 1999 Nov;70(5):820-2.
Several hypericin derivatives, previously shown to have interesting light-mediated biological activities, were evaluated for antiviral activities against herpes simplex virus and influenza virus. Three brominated hypericins, the dibromo- and tetrabromo-derivatives and the natural compound gymnochrome B were all very active against both viruses, particularly herpes simplex virus, although light was required in all cases for maximum activity. The dibromohypericin was the most potent, under standard assay conditions, gymnochrome B was approximately as active as hypericin itself and tetrabromohypericin significantly less so. Surprisingly, hexamethylhypericin, which is known to have potent anti-protein kinase (PK) C activity, as well as anticell proliferation properties, showed no antiviral activity at all. The compounds were also evaluated in different serum concentrations. All the active compounds were inhibited by increasing concentrations of serum, but to different degrees, such that their relative antiviral potencies changed to some extent. Thus, in summary, there was no correlation between antiviral and anti-PK or anticellular activities, and consequently it is not possible at present to define those structural features of hypericin-type molecules that are required for their various biological activities.
几种金丝桃素衍生物，此前已证明具有有趣的光介导生物活性，现对其抗单纯疱疹病毒和流感病毒的抗病毒活性进行评估。三种溴化金丝桃素，即二溴和四溴衍生物以及天然化合物裸金霉素B，对这两种病毒均具有很强的活性，尤其是对单纯疱疹病毒，不过在所有情况下都需要光照才能达到最大活性。在标准测定条件下，二溴金丝桃素效力最强，裸金霉素B的活性与金丝桃素本身大致相当，而四溴金丝桃素的活性则明显较低。令人惊讶的是，已知具有强大抗蛋白激酶（PK）C活性以及抗细胞增殖特性的六甲基金丝桃素根本没有抗病毒活性。这些化合物还在不同血清浓度下进行了评估。所有活性化合物都受到血清浓度升高的抑制，但程度不同，以至于它们的相对抗病毒效力在一定程度上发生了变化。因此，总的来说，抗病毒活性与抗PK或抗细胞活性之间没有相关性，因此目前无法确定金丝桃素类分子的哪些结构特征是其各种生物活性所必需的。
