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.

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鸢尾皂甙元：其来源、药理学、毒性和药代动力学综述

鸢尾皂甙元是一种众所周知的天然黄酮苷元，也是存在于多种植物中的活性成分。越来越多的证据表明鸢尾皂苷元具有多种药理作用，例如抗癌、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，包括几种类型的癌症、糖尿病、肝纤维化、骨关节炎、阿尔茨海默病等。本文的目的是对来源进行全面的总结和回顾，鸢尾苷元的提取和合成、药理作用、毒性、药代动力学和递送策略方面。鸢尾皂苷元可能产生一定的细胞毒性，其与给药时间和浓度有关。药代动力学研究表明，鸢尾皂苷元在大鼠体内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，但其生物利用度较差。从我们的角度来看，鸢尾皂苷元的进一步研究应该包括：探索药理靶点和作用机制；寻找适当的浓度以平衡药理作用和毒性；尝试多样化的递送策略以提高生物利用度；并进行结构修饰，得到具有更高药理活性的鸢尾素衍生物。