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葛根素:资源、药理学、毒性和药代动力学的综述。

Tectorigenin: A Review of Its Sources, Pharmacology, Toxicity, and Pharmacokinetics.

机构信息

West China Centre of Excellence for Pancreatitis, Institute of Integrated Traditional Chinese and Western Medicine, Sichuan Provincial Pancreatitis Centre and West China-Liverpool Biomedical Research Centre, West China Hospital, Sichuan University, Chengdu 610041, China.

Advanced Mass Spectrometry Center, Research Core Facility, Frontiers Science Center for Disease-Related Molecular Network, West China Hospital, Sichuan University, Chengdu 610041, China.

出版信息

Molecules. 2023 Aug 5;28(15):5904. doi: 10.3390/molecules28155904.

Abstract

Tectorigenin is a well-known natural flavonoid aglycone and an active component that exists in numerous plants. Growing evidence suggests that tectorigenin has multiple pharmacological effects, such as anticancer, antidiabetic, hepatoprotective, anti-inflammatory, antioxidative, antimicrobial, cardioprotective, and neuroprotective. These pharmacological properties provide the basis for the treatment of many kinds of illnesses, including several types of cancer, diabetes, hepatic fibrosis, osteoarthritis, Alzheimer's disease, etc. The purpose of this paper is to provide a comprehensive summary and review of the sources, extraction and synthesis, pharmacological effects, toxicity, pharmacokinetics, and delivery strategy aspects of tectorigenin. Tectorigenin may exert certain cytotoxicity, which is related to the administration time and concentration. Pharmacokinetic studies have demonstrated that the main metabolic pathways in rats for tectorigenin are glucuronidation, sulfation, demethylation and methoxylation, but that it exhibits poor bioavailability. From our perspective, further research on tectorigenin should cover: exploring the pharmacological targets and mechanisms of action; finding an appropriate concentration to balance pharmacological effects and toxicity; attempting diversified delivery strategies to improve the bioavailability; and structural modification to obtain tectorigenin derivatives with higher pharmacological activity.

摘要

葛根素是一种众所周知的天然黄酮类苷元,也是存在于许多植物中的一种活性成分。越来越多的证据表明,葛根素有多种药理作用,如抗癌、抗糖尿病、保肝、抗炎、抗氧化、抗菌、心脏保护和神经保护。这些药理特性为治疗多种疾病提供了基础,包括多种癌症、糖尿病、肝纤维化、骨关节炎、阿尔茨海默病等。本文的目的是对葛根素的来源、提取与合成、药理作用、毒性、药代动力学和传递策略等方面进行全面总结和综述。葛根素有一定的细胞毒性,这与给药时间和浓度有关。药代动力学研究表明,葛根素在大鼠体内的主要代谢途径为葡萄糖醛酸化、硫酸化、去甲基化和甲氧基化,但生物利用度较差。从我们的角度来看,对葛根素的进一步研究应包括:探索其药理作用靶点和作用机制;寻找合适的浓度来平衡药理作用和毒性;尝试多样化的传递策略以提高生物利用度;以及进行结构修饰以获得具有更高药理活性的葛根素衍生物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b637/10421414/3652e551c6dc/molecules-28-05904-g001.jpg

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