苦木素 A-M:药理学、作用机制、合成进展和药代动力学综述。
The quassinoids bruceines A-M: pharmacology, mechanism of action, synthetic advance, and pharmacokinetics-a review.
发表日期:2024 Jul 10
作者:
Nguyen Quang Hop, Ninh The Son
来源:
CLINICAL PHARMACOLOGY & THERAPEUTICS
摘要:
布鲁斯碱 A-L 是在药用植物鸦胆子 (L.) 中发现的苦木素代表之一。其药理活性的概述仍然未知。该研究重点关注其药理结果、分子作用机制、合成进展和药代动力学。根据先前的证据,马钱子碱衍生物是抗癌治疗的潜在药物,并且适用于治疗炎症、糖尿病和寄生虫感染,并保护神经元、肾脏和肺部。细胞因子抑制、氧化应激反应和各种信号通路,例如 MAPK(丝裂原激活蛋白激酶)和 NF-κB(核因子-κ B),已被认为是潜在的作用机制。合成具有增强活性的新衍生物的合成方法基于游离羟基修饰。鸦胆子碱通过口服和静脉注射似乎都能迅速吸收,但其生物利用度不高(低于 6%)。证明其抗癌潜力和其他活性的临床前和临床研究刻不容缓。结构修改、纳米组合和协同效应是必要的。© 2024。作者获得 Springer-Verlag GmbH 德国(Springer Nature 旗下公司)的独家许可。
Bruceines A-L are among the quassinoid representatives found in the medicinal plant Brucea javanica (L.). An overview of their pharmacological activities is still unknown. The given research deals with highlights in their pharmacological result, molecular mechanism of action, synthetic progress, and pharmacokinetics. From previous evidence, bruceine derivatives are potential agents for anticancer treatments, as well as they are appropriate to treat inflammation, diabetes, and parasitic infections, and protect the neurons, kidneys, and lungs. Cytokine inhibitions, oxidative stress responses, and various signaling pathways, such as MAPK (mitogen-activated protein kinase) and NF-κB (nuclear factor-kappa B), have been proposed as the underlying mechanisms of action. Synthetic approaches to synthesize new derivatives with enhancement activities are based on free hydroxyl group modifications. Bruceines seem to be promptly absorbed by both oral and intravenous administrations, but their bioavailability is not high (less than 6%). Pre-clinical and clinical studies to prove their anticancer potential and other activities are urgent. Structural modifications, nano-combinations, and synergistic effects are necessary.© 2024. The Author(s), under exclusive licence to Springer-Verlag GmbH Germany, part of Springer Nature.