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佛手柑内酯:药理学、药代动力学和毒性研究综述。

Bergapten: A review of its pharmacology, pharmacokinetics, and toxicity.

机构信息

School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, China.

出版信息

Phytother Res. 2021 Nov;35(11):6131-6147. doi: 10.1002/ptr.7221. Epub 2021 Aug 4.

DOI:10.1002/ptr.7221
PMID:34347307
Abstract

Bergapten is a natural furocoumarin, also known as 5-methoxypsoralen, and its medicinal value has been paid more and more attention. By sorting out the pharmacological literature of bergapten, we found that bergapten has a wide range of pharmacological effects, including neuroprotection, organ protection, anticancer, antiinflammatory, antimicrobial, and antidiabetes effects. However,bergapten has complex impacts on the hepatic metabolic enzyme. Moreover, pharmacokinetic studies showed that bergapten has higher absolute bioavailability and can cross the blood-brain barrier and has a great potential for treating brain disease, but the mechanism needs further clarification to make greater use of its ability to treat brain diseases. Furthermore, the phototoxicity of bergapten combined with ultraviolet light has always been mentioned. In view of its wide range of pharmacological activities, bergapten is expected to be a potential drug candidate for the treatment of diabetes and diabetes-induced osteoporosis, epilepsy, Alzheimer's disease, depression, and cancer. However, further studies are needed to elucidate its molecular mechanisms and targets. The phototoxicity of bergapten as a side effect should be further avoided. On the other hand, the photoactivation of bergapten in the anticancer aspect can be better utilized.

摘要

佛手柑内酯是一种天然呋喃香豆素,也被称为 5-甲氧基补骨脂素,其药用价值越来越受到重视。通过对佛手柑内酯的药理学文献进行梳理,我们发现佛手柑内酯具有广泛的药理作用,包括神经保护、器官保护、抗癌、抗炎、抗菌和抗糖尿病作用。然而,佛手柑内酯对肝代谢酶有复杂的影响。此外,药代动力学研究表明,佛手柑内酯具有较高的绝对生物利用度,可穿透血脑屏障,具有治疗脑部疾病的巨大潜力,但需要进一步阐明其机制,以更好地利用其治疗脑部疾病的能力。此外,佛手柑内酯与紫外线联合的光毒性一直受到关注。鉴于其广泛的药理活性,佛手柑内酯有望成为治疗糖尿病和糖尿病引起的骨质疏松症、癫痫、阿尔茨海默病、抑郁症和癌症的潜在药物候选物。然而,需要进一步研究来阐明其分子机制和靶点。佛手柑内酯的光毒性作为一种副作用,应进一步避免。另一方面,在抗癌方面,佛手柑内酯的光激活可以更好地利用。

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