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Identification and molecular characterization of the tubulin-podophyllotoxin-type lignans binding site on Giardia lamblia.
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2019-09-12 , DOI: 10.1111/cbdd.13605
Filiberto Gutiérrez-Gutiérrez 1 , Antonio Romo-Mancillas 2 , Ana María Puebla-Pérez 1 , José Manuel Hernández-Hernández 3 , Araceli Castillo-Romero 4
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2019-09-12 , DOI: 10.1111/cbdd.13605
Filiberto Gutiérrez-Gutiérrez 1 , Antonio Romo-Mancillas 2 , Ana María Puebla-Pérez 1 , José Manuel Hernández-Hernández 3 , Araceli Castillo-Romero 4
Affiliation
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There are several drugs for the treatment of giardiasis; however, there is a tendency for patients to abandon treatment because of drug-related adverse effects, resulting in relapses, acquired resistance, and higher rates of treatment failure. Recently, we reported some podophyllotoxin-type lignans from Bursera fagaroides var. fagaroides showing antigiardial activity. In the present work, we demonstrated that 5'-desmethoxy-peltatin-A-methylether (5-DES), acetylpodophyllotoxin (APOD), and podophyllotoxin (POD) affect the distribution and staining pattern of microtubular structures on Giardia trophozoites. Virtual screening results revealed that the lignans act via binding in a hydrophobic pocket in the heterodimer interface of tubulin in Giardia. This study provides useful insight to understand the action mechanism of 5DES, APOD, and POD on Giardia lamblia. The optimization of these podophyllotoxin-type lignans will lead to promising candidates for antigiardial drugs.
中文翻译:
贾第鞭毛虫的微管蛋白-鬼臼毒素型木脂体结合位点的鉴定和分子表征。
有几种治疗贾第鞭毛虫病的药物。然而,由于药物相关的不良反应,患者倾向于放弃治疗,导致复发,获得性耐药和更高的治疗失败率。最近,我们报道了来自Bursera fagaroides var的一些鬼臼毒素型木脂素。表现出抗菊苣活性的黄aga类。在目前的工作中,我们证明了5'-去甲氧基-peltatin-A-甲基醚(5-DES),乙酰鬼臼毒素(APOD)和鬼臼毒素(POD)影响贾第鞭毛虫滋养体上微管结构的分布和染色模式。虚拟筛选结果显示木脂素通过贾第鞭毛虫微管蛋白异二聚体界面的疏水口袋中的结合起作用。这项研究为了解5DES,APOD,和贾第鞭毛虫兰上的POD。这些鬼臼毒素型木脂素的优化将产生抗真菌药物的有希望的候选者。
更新日期:2019-09-12
中文翻译:
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贾第鞭毛虫的微管蛋白-鬼臼毒素型木脂体结合位点的鉴定和分子表征。
有几种治疗贾第鞭毛虫病的药物。然而,由于药物相关的不良反应,患者倾向于放弃治疗,导致复发,获得性耐药和更高的治疗失败率。最近,我们报道了来自Bursera fagaroides var的一些鬼臼毒素型木脂素。表现出抗菊苣活性的黄aga类。在目前的工作中,我们证明了5'-去甲氧基-peltatin-A-甲基醚(5-DES),乙酰鬼臼毒素(APOD)和鬼臼毒素(POD)影响贾第鞭毛虫滋养体上微管结构的分布和染色模式。虚拟筛选结果显示木脂素通过贾第鞭毛虫微管蛋白异二聚体界面的疏水口袋中的结合起作用。这项研究为了解5DES,APOD,和贾第鞭毛虫兰上的POD。这些鬼臼毒素型木脂素的优化将产生抗真菌药物的有希望的候选者。