喹诺酮类药物抗乙型肝炎病毒体外实验研究

The inhibitory Effects of Quinolones on Hepatitis B Virus in Vitro

本文以２．２．１５细胞株为模型，以ＨＢｓＡｇ、ＨＢｅＡｇ、ＨＢＶＤＮＡ、细胞存活率为观察指标，综合评价了喹诺酮类药物吡哌酸（ＰｉｐｅｍｉｄｉｃＡｃｉｄ）、氟哌酸（Ｎｏｒｆｌｏｘａｃｉｎ）、环丙氟哌酸（Ｃｉｐｒｏｆｌｏｓｘａｃｉｎ）、氟嗪酸（Ｏｆｌｏｘａｃｉｎ）体外抗ＨＢＶ效果。结果表明：吡哌酸、氟哌酸、环丙氟哌酸、氟嗪酸对ＨＢｓＡｇ、ＨＢｅＡｇ５０％抑制浓度（ＩＤ＿（５０））分别为１１μｇ／ｍｌ、６４μｇ／ｍｌ、９３μｇ／ｍｌ、１０５μｇ／ｍｌ和１９９μｇ／ｍｌ、１１１μｇ／ｍｌ、２４μｇ／ｍｌ、２１７μｇ／ｍｌ，细胞存活率为５０％时的药物浓度（ＣＤ＿（５０））分别为２１９μｇ／ｍｌ、９０μｇ／ｍｌ、１８１μｇ／ｍｌ、１６９μｇ／ｍｌ，在所选定的用药浓度范围内不同程度抑制培养上清液及细胞内ＨＢＶＤＮＡ及其复制中间体的产生。尤其对超螺旋结构ＤＮＡ（ｓｃＤＮＡ）有不完全抑制作用。

uinolones were studied for their ability to inhibit hepatitis B virus DNA replicatiun,HBsAg andHBeAg exporssion in a HBV-transfeeted eell line(2.2.15 cell).The survival cell rate was determinedby MTT assay.The result shows that ID50(the drug concentration that inhibits HBsAg or HBeAg secretion by 50%) were 110μg/ml and 199μg/ml with Pipemidic Acid,64μg/ml and 111μg/ml with Norfloxacin,93μg/ml and 210μg/ml with Ciprofloxacin,105μg/ml and 217μg/ml with Ofloxacin.CD_50(the drug concentration that reduces cell growth by 50%) were 219μg/ml,90μg/ml,181μg/ml,160μg/ml,reepectively.In the range of drug concentration selected,they partially or completelybleeked the production of HBV particles and its replicative interniediates,especially the seneration of suporcoiled viral DNA((sc DNA).