Background

Cepharanthine (CEP) is a drug used in Japan since the 1950s to treat a number of acute and chronic diseases, including treatment of leukopenia, snake bites, xerostomia and alopecia. It is the only approved drug for Human use in the large class of bisbenzylisoquinoline alkaloids. This natural product, mainly isolated from the plant Stephania cephalantha Hayata, exhibits multiple pharmacological properties including anti-oxidative, anti-inflammatory, immuno-regulatory, anti-cancer, anti-viral and anti-parasitic properties.

Purpose

The mechanism of action of CEP is multifactorial. The drug exerts membrane effects (modulation of efflux pumps, membrane rigidification) as well as different intracellular and nuclear effects. CEP interferes with several metabolic axes, primarily with the AMP-activated protein kinase (AMPK) and NFκB signaling pathways. In particular, the anti-inflammatory effects of CEP rely on AMPK activation and NFκB inhibition.

Conclusion

In this review, the historical discovery and development of CEP are retraced, and the key mediators involved in its mode of action are presented. The past, present, and future of CEP are recapitulated. This review also suggests new opportunities to extend the clinical applications of this well-tolerated old Japanese drug.

中文翻译：

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头孢兰定：作用方式，药理特性和医学应用的更新

背景

自1950年代以来，头孢兰氨酸（CEP）是一种在日本用于治疗多种急性和慢性疾病的药物，包括治疗白细胞减少症，蛇咬伤，口腔干燥症和脱发症。它是批准用于人类的大量双苄基异喹啉生物碱中的唯一药物。这种天然产物主要从植物Stephania cephalantha Hayata中分离出来，具有多种药理特性，包括抗氧化，抗炎，免疫调节，抗癌，抗病毒和抗寄生虫特性。

目的

CEP的作用机制是多因素的。该药物具有膜效应（外排泵的调节，膜硬化）以及不同的细胞内和核效应。CEP干扰几个代谢轴，主要干扰AMP激活的蛋白激酶（AMPK）和NFκB信号通路。CEP的抗炎作用尤其取决于AMPK激活和NFκB抑制。

结论

在这篇综述中，回顾了CEP的历史发现和发展，并介绍了其行动模式所涉及的关键调解人。概述了CEP的过去，现在和将来。这篇综述还提出了扩展这种耐受性良好的日本旧药物的临床应用的新机会。