Tang J, Colacino J M, Larsen S H, Spitzer W
Lilly Research Laboratories, Indianapolis, IN 46285.
Antiviral Res. 1990 Jun;13(6):313-25. doi: 10.1016/0166-3542(90)90015-y.
Hypericin is a polycyclic anthrone first isolated from the plant St. Johnswort and was shown to have dramatic anti-retroviral activity against Friend leukemia virus and radiation leukemia virus in mice. Hypericin displayed marginal activity (IC50 = 6 micrograms/ml) against Moloney murine leukemia virus (Mo-MuLV) in vitro. Hypericin did not display selective antiviral activity against herpes simplex virus, influenza A, adenovirus, or poliovirus. The 50% cytotoxic concentration was approximately 25 micrograms/ml. When virus was incubated with hypericin before infecting cells, the drug was virucidal to all enveloped viruses tested (herpes simplex, influenza virus A, and Mo-MuLV) at concentrations of 1.56 micrograms/ml to 25 micrograms/ml. Hypericin was not virucidal to the non-enveloped viruses tested (adenovirus and poliovirus). These data indicate that the mechanism of viral inactivation for hypericin is dependent upon the presence of a viral lipid envelope. In vivo, hypericin (50 mg/ml) was effective against FLV or HSV-1 if incubated with the virus for 1 h at 37 degrees C before infecting mice, but was not effective if pre-incubated with virus for 1 h at 4 degrees C or if administered concurrently with virus.
金丝桃素是一种多环蒽酮，最初从贯叶连翘植物中分离出来，已证明其对小鼠体内的弗氏白血病病毒和辐射白血病病毒具有显著的抗逆转录病毒活性。金丝桃素在体外对莫洛尼鼠白血病病毒（Mo-MuLV）表现出微弱的活性（IC50 = 6微克/毫升）。金丝桃素对单纯疱疹病毒、甲型流感病毒、腺病毒或脊髓灰质炎病毒没有表现出选择性抗病毒活性。50%细胞毒性浓度约为25微克/毫升。当病毒在感染细胞前与金丝桃素一起孵育时，该药物在1.56微克/毫升至25微克/毫升的浓度下对所有测试的包膜病毒（单纯疱疹病毒、甲型流感病毒和Mo-MuLV）具有杀病毒作用。金丝桃素对测试的非包膜病毒（腺病毒和脊髓灰质炎病毒）没有杀病毒作用。这些数据表明，金丝桃素使病毒失活的机制取决于病毒脂质包膜的存在。在体内，如果在感染小鼠前将金丝桃素（50毫克/毫升）与病毒在37℃下孵育1小时，则对弗氏白血病病毒或单纯疱疹病毒1型有效，但如果在4℃下与病毒预孵育1小时或与病毒同时给药则无效。
