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Artemisinin and artemisinin derivatives as anti-fibrotic therapeutics
Acta Pharmaceutica Sinica B ( IF 14.7 ) Pub Date : 2020-09-08 , DOI: 10.1016/j.apsb.2020.09.001
David Dolivo 1 , Pamela Weathers 2 , Tanja Dominko 2
Affiliation  

Fibrosis is a pathological reparative process that can occur in most organs and is responsible for nearly half of deaths in the developed world. Despite considerable research, few therapies have proven effective and been approved clinically for treatment of fibrosis. Artemisinin compounds are best known as antimalarial therapeutics, but they also demonstrate antiparasitic, antibacterial, anticancer, and anti-fibrotic effects. Here we summarize literature describing anti-fibrotic effects of artemisinin compounds in in vivo and in vitro models of tissue fibrosis, and we describe the likely mechanisms by which artemisinin compounds appear to inhibit cellular and tissue processes that lead to fibrosis. To consider alternative routes of administration of artemisinin for treatment of internal organ fibrosis, we also discuss the potential for more direct oral delivery of Artemisia plant material to enhance bioavailability and efficacy of artemisinin compared to administration of purified artemisinin drugs at comparable doses. It is our hope that greater understanding of the broad anti-fibrotic effects of artemisinin drugs will enable and promote their use as therapeutics for treatment of fibrotic diseases.



中文翻译:


青蒿素和青蒿素衍生物作为抗纤维化治疗剂



纤维化是一种病理性修复过程,可发生在大多数器官中,导致发达国家近一半的死亡。尽管进行了大量研究,但很少有疗法被证明有效并被临床批准用于治疗纤维化。青蒿素化合物最著名的用途是抗疟疗法,但它们还具有抗寄生虫、抗菌、抗癌和抗纤维化作用。在这里,我们总结了描述青蒿素化合物在体内体外组织纤维化模型中抗纤维化作用的文献,并描述了青蒿素化合物抑制导致纤维化的细胞和组织过程的可能机制。为了考虑青蒿素治疗内脏器官纤维化的替代给药途径,我们还讨论了与同等剂量的纯化青蒿素药物相比,更直接口服青蒿植物材料以增强青蒿素的生物利用度和功效的潜力。我们希望,对青蒿素药物广泛的抗纤维化作用有更深入的了解,将能够并促进它们作为治疗纤维化疾病的药物的使用。

更新日期:2020-09-08
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