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用于评估抗隐孢子虫药物疗效的具有成本效益的体内和体外小鼠模型:评估伏立诺他、多西他赛和黄芩苷。

Cost-effective In Vivo and In Vitro Mouse Models for Evaluating Anticryptosporidial Drug Efficacy: Assessing Vorinostat, Docetaxel, and Baicalein.

作者信息

Liu Mingxiao, Zhang Di, Wang Dongqiang, Wu Xiaodong, Zhang Ying, Yin Jigang, Zhu Guan

机构信息

State Key Laboratory for Diagnosis and Treatment of Severe Zoonotic Infectious Diseases, Key Laboratory of Zoonosis Research of the Ministry of Education, Institute of Zoonosis, and College of Veterinary Medicine, Jilin University, Changchun, Jilin, China.

出版信息

J Infect Dis. 2023 Nov 11;228(10):1430-1440. doi: 10.1093/infdis/jiad243.

Abstract

BACKGROUND

Cryptosporidiosis is a significant diarrheal disease in humans and animals. Immunodeficient mice are the primary small animal models, but their high costs and specialized breeding/housing requirements limit in vivo drug testing. Numerous anticryptosporidial lead compounds identified in vitro remain untested in vivo.

METHODS

Cryptosporidium tyzzeri, a natural mouse parasite closely related to Cryptosporidium parvum and Cryptosporidium hominis, was isolated to establish an infection model in immunocompetent mice. The model was validated using classic anticryptosporidial drugs (paromomycin and nitazoxanide) and then employed to assess the efficacy of 3 new leads (vorinostat, docetaxel, and baicalein). An in vitro culture of C. tyzzeri was also developed to complement the animal model.

RESULTS

Chronic C. tyzzeri infection was established in chemically immunosuppressed wild-type mice. Paromomycin (1000 mg/kg/d) and nitazoxanide (100 mg/kg/d) demonstrated efficacy against C. tyzzeri. Vorinostat (30 mg/kg/d), docetaxel (25 mg/kg/d), and baicalein (50 mg/kg/d) were highly effective against C. tyzzeri infection. In vitro, nitazoxanide, vorinostat, docetaxel, and baicalein exhibited low to submicromolar efficacy against C. tyzzeri.

CONCLUSIONS

Novel in vivo and in vitro models have been developed for cost-effective anticryptosporidial drug testing. Vorinostat, docetaxel, and baicalein show potential for repurposing and/or optimization for developing new anticryptosporidial drugs.

摘要

背景

隐孢子虫病是人和动物中一种重要的腹泻疾病。免疫缺陷小鼠是主要的小动物模型,但它们成本高昂且对饲养/ housing有特殊要求,限制了体内药物测试。许多在体外鉴定出的抗隐孢子虫先导化合物尚未在体内进行测试。

方法

分离出与微小隐孢子虫和人隐孢子虫密切相关的天然小鼠寄生虫泰泽隐孢子虫,以在免疫 competent小鼠中建立感染模型。使用经典抗隐孢子虫药物(巴龙霉素和硝唑尼特)对该模型进行验证,然后用于评估3种新先导化合物(伏立诺他、多西他赛和黄芩苷)的疗效。还开发了泰泽隐孢子虫的体外培养物以补充动物模型。

结果

在化学免疫抑制的野生型小鼠中建立了慢性泰泽隐孢子虫感染。巴龙霉素(1000mg/kg/d)和硝唑尼特(100mg/kg/d)对泰泽隐孢子虫显示出疗效。伏立诺他(30mg/kg/d)、多西他赛(25mg/kg/d)和黄芩苷(50mg/kg/d)对泰泽隐孢子虫感染非常有效。在体外,硝唑尼特、伏立诺他、多西他赛和黄芩苷对泰泽隐孢子虫表现出低至亚微摩尔的疗效。

结论

已开发出新型体内和体外模型用于具有成本效益的抗隐孢子虫药物测试。伏立诺他、多西他赛和黄芩苷在开发新的抗隐孢子虫药物方面显示出重新利用和/或优化的潜力。

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