穿心莲内酯磺化物体外抗腺病毒药效学研究

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

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。

Objective： To observe anti-adenovirus 3 （AdV3） effect and cytotoxicity of andrographolide sulfonated （ADS） in vitro. Method： The maximum nontoxic concentration （0% toxic concentration, TCo） and 50% toxic concentration （TC50） of ADS were analyzed by cytopathic effect （CPE） and methyl thiazolyl tetrazolium （MTT） colorimetric test. The AdV3 at 100TCIDso （50% tissue cell infection dose） attacked Hep-2 cell in 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 （ECso） and therapeutic index （TI） were used as the indicators. Result： ADS and ribavirin TC0 were 781.25 mg ·L^（-1）and 6.25 mg ·L^（-1） ; MECs were 97.66 mg·L^（-1）and 0. 390 6 mg ·L^（-1）, TIs were 8 and 16, respectively. Conclusion： ADS 97.66-781.25 mg ·L-1 can effectively inhibit the intracellular proliferation of AdV3 in vitro, and showed a significant dose-effect relationship.