Biomedicine Research and Development Center of Jinan University, Guangzhou 510632, China.
Virol Sin. 2010 Apr;25(2):107-14. doi: 10.1007/s12250-010-3092-6. Epub 2010 Apr 9.
Herpes simplex virus type 1 (HSV-1) is a commonly occurring human pathogen worldwide. There is an urgent need to discover and develop new alternative agents for the management of HSV-1 infection. Tripterygium hypoglaucum (level) Hutch (Celastraceae) is a traditional Chinese medicine plant with many pharmacological activities such as anti-inflammation, anti-tumor and antifertility. The usual medicinal part is the roots which contain about a 1% yield of alkaloids. A crude total alkaloids extract was prepared from the roots of T. hypoglaucum amd its antiviral activity against HSV-1 in Vero cells was evaluated by cytopathic effect (CPE) assay, plaque reduction assay and by RT-PCR analysis. The alkaloids extract presented low cytotoxicity (CC(50) = 46.6 μg/mL) and potent CPE inhibition activity, the 50% inhibitory concentration (IC(50)) was 6.5 μg/mL, noticeably lower than that of Acyclovir (15.4 μg /mL). Plaque formation was significantly reduced by the alkaloids extract at concentrations of 6.25 μg/mL to 12.5 μg/mL, the plaque reduction ratio reached 55% to 75 which was 35% higher than that of Acyclovir at the same concentration. RT-PCR analysis showed that, the transcription of two important delayed early genes UL30 and UL39, and a late gene US6 of HSV-1 genome all were suppressed by the alkaloids extract, the expression inhibiting efficacy compared to the control was 74.6% (UL30), 70.9% (UL39) and 62.6% (US6) respectively at the working concentration of 12.5 μg/mL. The above results suggest a potent anti-HSV-1 activity of the alkaloids extract in vitro.
单纯疱疹病毒 1 型（HSV-1）是一种广泛存在于全球的人类病原体。因此，迫切需要发现和开发新的替代药物来治疗 HSV-1 感染。昆明山海棠（卫矛科）是一种传统的中药植物，具有许多药理活性，如抗炎、抗肿瘤和抗生育。常用的药用部位是根，根中约含有 1%的生物碱。从昆明山海棠的根中提取了一种粗总生物碱提取物，并通过细胞病变效应（CPE）测定、蚀斑减少测定和 RT-PCR 分析评价其对 Vero 细胞中 HSV-1 的抗病毒活性。生物碱提取物的细胞毒性较低（CC50 = 46.6μg/ml），对 CPE 的抑制活性较强，半数抑制浓度（IC50）为 6.5μg/ml，明显低于阿昔洛韦（15.4μg/ml）。生物碱提取物在 6.25μg/ml 至 12.5μg/ml 浓度下显著抑制蚀斑形成，蚀斑减少率达到 55%至 75%，与相同浓度的阿昔洛韦相比提高了 35%。RT-PCR 分析表明，该生物碱提取物可抑制 HSV-1 基因组中两个重要的延迟早期基因 UL30 和 UL39 以及一个晚期基因 US6 的转录，与对照相比，其表达抑制率在 12.5μg/ml 的工作浓度下分别为 74.6%（UL30）、70.9%（UL39）和 62.6%（US6）。上述结果表明，该生物碱提取物在体外具有较强的抗 HSV-1 活性。
