京尼泊地酸的药理活性及药代动力学研究进展

Q3 Pharmacology, Toxicology and Pharmaceutics
Zi-Wei Li, Sheng-Lan Qi, Qing-Guang Zhang, Ling Chen, Jing Hu, Guang-Bo Ge, Feng Huang
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引用次数: 0

摘要

Geniposidic acid(GA)是一种天然环烯醚萜类化合物,存在于茜草科、杜仲科和车前草科药用植物的根、茎、叶、花、树皮、果实和种子中。现代药理学研究表明,GA具有多种药理作用,包括器官保护、抗炎、抗氧化、抗骨质疏松、抗神经退行性和抗心血管作用。GA通过上调关键抗炎和抗氧化细胞因子,下调促炎信号通路中关键节点蛋白AhR、TLR4/MyD88等,增强细胞/机体的防御能力,从而发挥器官保护等药理作用。药代动力学研究表明,GA经口服后可分布于多脏器(肾、肝、心、脾、肺等)。此外,GA的药代动力学行为可以在疾病条件下显着改变,正如系统暴露的显着增加所证明的那样。本文综合总结已报道的GA的药理活性和作用机制,系统分析GA相关中成药的药动学特征和关键参数,旨在为GA相关中成药的精准临床应用以及基于GA的创新药物的研发提供理论依据和科学参考。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
[Research progress in pharmacological activities and pharmacokinetics of geniposidic acid].

Geniposidic acid(GA), a natural iridoid, exists in the roots, stems, leaves, flowers, bark, fruits, and seeds of medicinal plants of Rubiaceae, Eucommiaceae, and Plantaginaceae. Modern pharmacological studies have revealed that GA has multiple pharmacological activities, including organ-protective, anti-inflammatory, antioxidative, anti-osteoporosis, anti-neurodegenerative, and anti-cardiovascular effects. GA can enhance cell/organism defenses by upregulating key anti-inflammatory and antioxidant cytokines, while downregulating key node proteins in pro-inflammatory signaling pathways such as AhR and TLR4/MyD88, thereby exerting pharmacological effects such as organ protection. Pharmacokinetic investigations have suggested that after oral administration, GA can be distributed in multiple organs(kidney, liver, heart, spleen, lung, etc.). In addition, the pharmacokinetic behavior of GA could be significantly altered under disease conditions, as demonstrated by a marked increase in systematic exposure. This article comprehensively summarizes the reported pharmacological activities and mechanisms and systematically analyzes the pharmacokinetic characteristics and key parameters of GA, with the aim of providing a theoretical basis and scientific reference for the precise clinical application of GA-related Chinese patent medicines, as well as for the investigation and development of innovative drugs based on GA.

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来源期刊
Zhongguo Zhongyao Zazhi
Zhongguo Zhongyao Zazhi Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)
CiteScore
1.50
自引率
0.00%
发文量
581
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