Department of Pharmacology, Kunming University, Yunnan, Republic of China.
Indian J Pharmacol. 2011 Sep;43(5):536-40. doi: 10.4103/0253-7613.84967.
The root of Cynanchum otophyllum-also known as Qing Yang Sheng-is a traditional ethnical Chinese medicine. The objective of this study was to evaluate in vitro activities and safety of C. otophyllum glucan sulfate (PS20) against Human Immunodeficiency Virus (HIV) and Herpes Simplex Virus (HSV).
Anti-HIV activity was detected with syncytial formation assay and quantitative P24 Enzyme-Linked Immunosorbent Assay (ELISA). Anti-HSV activity was detected with plaque reduction assay; cytotoxicity was tested with MTT colorimetric assay; and anti-bacterial activity was tested with microdilution method. Anti-HIV mechanism was investigated with fusion inhibition, time of addition, and pretreatment.
The 50% Inhibition Concentration (IC(50)) of PS20 for HIV-1(IIIB), HIV-(Ada-M), HIV-1(Bal), HSV-I, and -II were 0.26 ± 0.02 mM, 0.46 ± 0.02 mM, 0.90 ± 0.04 mM, 3.45 ± 0.85 μM, and 0.70 ± 0.22 mM, respectively. Selectivity Indices (SI) were 653, 50, 39, 85, and 362, respectively. Studies on anti-HIV mechanism of PS20 showed that the target molecule should be the envelope protein. The 50% Cytotoxicity Concentrations (CC(50)) of PS20 for HeLa and ME-180 cell lines and human foreskin fibroblast cells was more than 70 μM. The Minimum Inhibitory Concentration (MIC) for vaginal lactobacilli was more than 1000 μM.
PS20 possesses anti-HIV and HSV effect and low cytotoxicity to epithelium cells and vaginal lactobacilli. It may be considered as a potential microbicide agent for further investigation.
青阳参的根是一种传统的中国民族药。本研究的目的是评估青阳参硫酸葡聚糖(PS20)对人类免疫缺陷病毒(HIV)和单纯疱疹病毒(HSV)的体外活性及安全性。
采用合胞体形成试验和定量P24酶联免疫吸附测定(ELISA)检测抗HIV活性。采用蚀斑减少试验检测抗HSV活性;采用MTT比色法检测细胞毒性;采用微量稀释法检测抗菌活性。通过融合抑制、添加时间和预处理研究抗HIV机制。
PS20对HIV-1(IIIB)、HIV-(Ada-M)、HIV-1(Bal)、HSV-I和-II的50%抑制浓度(IC50)分别为0.26±0.02 mM、0.46±0.02 mM、0.90±0.04 mM、3.45±0.85 μM和0.70±0.22 mM。选择性指数(SI)分别为653、50、39、85和362。PS20抗HIV机制研究表明,靶分子应为包膜蛋白。PS20对HeLa和ME-180细胞系以及人包皮成纤维细胞的50%细胞毒性浓度(CC50)大于70 μM。对阴道乳酸杆菌的最低抑菌浓度(MIC)大于1000 μM。
PS20具有抗HIV和HSV作用,对上皮细胞和阴道乳酸杆菌的细胞毒性较低。它可能被认为是一种有潜力的杀微生物剂,有待进一步研究。