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Artemisinin and artemisinin derivatives as anti-fibrotic therapeutics
Acta Pharmaceutica Sinica B ( IF 14.5 ) Pub Date : 2020-09-08 , DOI: 10.1016/j.apsb.2020.09.001
David Dolivo , Pamela Weathers , Tanja Dominko

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

纤维化是一种病理修复过程,可发生在大多数器官中,并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,并且在临床上已被批准用于治疗纤维化。青蒿素化合物是众所周知的抗疟疾治疗剂,但它们也显示出抗寄生虫,抗菌,抗癌和抗纤维化的作用。在这里,我们总结了描述青蒿素化合物在体内体外抗纤维化作用的文献组织纤维化的模型,我们描述了青蒿素化合物似乎可以抑制导致纤维化的细胞和组织过程的可能机制。为了考虑使用青蒿素治疗内脏器官纤维化的替代途径,我们还讨论了与可比剂量的纯化青蒿素药物相比,更直接口服青蒿素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,对青蒿素药物具有广泛的抗纤维化作用的进一步了解,将能够并促进其作为治疗纤维化疾病的疗法的用途。

更新日期:2020-09-08
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