阿苯达唑亚砜及其对映体体外抗细粒棘球绦虫原头蚴作用

In Vitro Observation on Albendazole Sulfoxide and its Enantiomers against Echinococcus granulosus Protoscolex

目的观察阿苯达唑亚砜消旋体(ASOX)、左旋体(L-ASOX)和右旋体(D-ASOX)体外抗细粒棘球绦虫原头蚴作用。方法将细粒棘球绦虫原头蚴随机分为8组(每组约6000个),分别置含6mlDMEM培养液(含15%胎牛血清,青霉素和链霉素各500U/ml)的培养瓶中,ASOX、L-ASOX和D-ASOX的各50μg/ml和100μg/ml组分别加入各药液150μl和300μl(配制液含0.1%二甲基亚砜和0.1%吐温-80的蒸馏水),DMSO组中加入等量配制液,并设空白对照组,每组设2个平行组。每隔1d观察1次,取样滴于玻片,用0.03%美蓝染色,显微镜下计数原头蚴约400个,计算死亡率。直至其中一组的原头蚴全部死亡为止。结果ASOX、L-ASOX和D-ASOX两个浓度(50μg/ml和100μg/ml)组不同作用时间原头蚴的死亡率分别与空白对照组和溶剂组相比,差异均有统计学意义(P<0.01);ASOX组与D-ASOX组相比,差别无统计学意义(P>0.05),而与L-ASOX组相比,差异有统计学意义(P<0.05);D-ASOX与L-ASOX相比,差异有统计学意义(P<0.05)。各药物作用至第9天时,ASOX、L-ASOX、D-ASOX的50μg/ml组原头蚴死亡率分别为(93.6±3.7)%、(56.2±3.9)%和(99.0±1.9)%,各药的100μg/ml组死亡率分别为100%、(74.5±3.7)%和100%,对照组为(19.1±1.3)%,溶剂组为(22.5±1.9)%。结论ASOX、L-ASOX和D-ASOX在体外均有抗细粒棘球绦虫原头蚴作用,D-ASOX抗原头蚴作用较L-ASOX强。

Objective To investigate in vitro anti-hydatid efficacy on Echinococcus granulosus protoscolex （EgPSC） by using albendazole sulfoxide （ASOX） and its two enantiomeric antipodes, L-ASOX and D-ASOX. Methods Eg protoscoleces were divided into eight groups and cultured in the DMEM culture media under two concentrations（50 μg/ml and 100μg/ml） of ASOX, L-ASOX and D-ASOX respectively. The appropriate controls included （i） a culture containing an equal amount of DMSO and （ii） a cuhure medium alone. The mortality of EgPSC in each group was daily counted until 100% EgPSC death in some groups. Results Significant difference of EgPSC mortality was found among the three drugs with various concentrations compared to control group （P〈0.01）, and a significant difference between L-ASOX group and D-ASOX group （P〈0.05）. There were no statistical difference between ASOX group and D-ASOX group （PM）.05）, but between ASOX group and L-ASOX group （P〈0.05）. On the 9th day of culture, the mortality of protoscleces with the concentration of 50μg/ml was 93.6%, 56.2% and 99.0% in ASOX, L-ASOX and D-ASOX groups respectively, and those under the concentration of 100 μg/ml were 100%, 74.5% and 100% respectively. The mortality was 19.1% and 22.5% respectively in the control and solvent groups. Conclusion ASOX, L-ASOX and D-ASOX demonstrate significant effect of anti-Eg protoscolex in vitro. D-ASOX shows stronger effect than L-ASOX.