研究动态
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广藿香素(Tectorigenin):来源、药理学、毒性与药代动力学的综述。

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

发表日期:2023 Aug 05
作者: Juan Rong, Fei Fu, Chenxia Han, Yaling Wu, Qing Xia, Dan Du
来源: Alzheimers & Dementia

摘要:

铁角固醇是一种众所周知的天然黄酮单体,并存在于许多植物中。越来越多的证据表明,铁角固醇具有多种药理效应,如抗癌、抗糖尿病、肝保护、抗炎、抗氧化、抗菌、心脏保护和神经保护作用。这些药理特性为多种疾病的治疗提供了基础,包括多种癌症、糖尿病、肝纤维化、骨关节炎、阿尔茨海默病等。本文的目的是对铁角固醇的来源、提取和合成、药理效应、毒性、药物动力学和输送策略进行全面总结和评述。铁角固醇可能表现出一定的细胞毒性,这与给药时间和浓度有关。药物动力学研究表明,大鼠对铁角固醇的主要代谢途径是葡萄糖醛酸化、硫酸化、去甲基化和甲氧基化,但其生物利用度较低。从我们的角度来看,进一步研究铁角固醇应包括:探索药理靶点和作用机制;寻找适当的浓度来平衡药理效应和毒性;尝试多样化的输送策略以提高生物利用度;并进行结构修饰以获得具有更高药理活性的铁角固醇衍生物。
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.