穿心莲内酯磺化物体外抗腺病毒药效学研究

目的:研究穿心莲内酯磺化物(ADS)体外抗腺病毒-3(AdV3)活性及细胞毒性。方法:采用细胞病变法(CPE)、四甲基偶氮唑蓝比色法(MTT)检测ADS的最大无毒浓度(TC0)和半数中毒浓度(TC50),以AdV3100倍半数组织细胞感染量(100TCID50)攻击体外培养的人喉癌上皮细胞(Hep-2)造成AdV3感染模型,以利巴韦林注射液为对照药,以最小有效浓度(MEC)、半数有效浓度(EC50)及治疗指数(TI)为指标,测定了ADS在6.10,12.21,24.41,48.23,97.66,195.31,390.63,871.25 mg.L-1的体外抑制腺病毒活性。结果:ADS、利巴韦林注射液TC0分别为781.25,6.25 mg.L-1;MEC分别为97.66,0.390 6 mg.L-1;TI分别为8,16。结论:ADS97.66～781.25 mg.L-1可有效抑制细胞内AdV3体外增殖,并呈明显的量效关系。

A Study of Anti-adenovirus Effect of Andrographolide Sulfonated in Vitro

Objective: To observe anti-adenovirus 3 (AdV₃) effect and cytotoxicity of andrographolide sulfonated (ADS) in vitro. Method: The maximum nontoxic concentration (0% toxic concentration, TC₀) and 50% toxic concentration (TC₅₀) of ADS were analyzed by cytopathic effect (CPE) and methyl thiazolyl tetrazolium (MTT) colorimetric test. The AdV₃ at 100TCID₅₀(50% tissue cell infection dose) attacked Hep-2 cellin vitro culture to cause AdV₃ infection model. The anti-adenovirus activity of ADS at 6.10,12.21,24.41,48.23,97.66,195.31,390.63,871.25 mg·L^-1 in vitro were measured with ribavirin as control, and the minimum effective concentration (MEC), 50% effective concentration (EC₅₀) and therapeutic index (TI) were used as the indicators. Result: ADS and ribavirin TC₀ were 781.25 mg·L^-1and 6.25 mg·L^-1; MECs were 97.66 mg·L^-1and 0.390 6 mg·L^-1, TIs were 8 and 16, respectively. Conclusion: ADS 97.66-781.25 mg·L^-1can effectively inhibit the intracellular proliferation of AdV₃ in vitro, and showed a significant dose-effect relationship.