College of Pharmacy, Shandong University of Traditional Chinese Medicine, Shandong 250355, P. R. China.
Zhaoyuan Inspection and Testing Center, Shandong 265400, P. R. China.
Am J Chin Med. 2023;51(8):2095-2120. doi: 10.1142/S0192415X23500908. Epub 2023 Oct 20.
[Formula: see text]-Escin is an oleanane-type pentacyclic triterpenoid saponin extracted from the seeds of (AH), which is more widely distributed. [Formula: see text]-Escin sodium has been approved by the American FDA for clinical usage. This paper is intended to summarize an updated and comprehensive review of the pharmacological activities, pharmacokinetic properties, toxicity, and analytical methods of [Formula: see text]-escin. Studies have shown that [Formula: see text]-escin has significant antitumor, antiviral, anti-inflammatory, and other activities alongside less adverse effects and higher safety than other compounds. The review shows that the pharmacological effects of [Formula: see text]-escin involve mechanisms such as ATM/[Formula: see text]H2AX, RhoA/Rock, GSK-3[Formula: see text]/[Formula: see text]-Catenin, HER2/HER3/Akt, and PI3K/Akt signaling pathways, and Cyclin A, p21[Formula: see text], survivin, Bcl-2, Mcl-1, Caspases, TGF-[Formula: see text], MMPs, and TNF-[Formula: see text] among other inflammatory factors. [Formula: see text]-Escin has significant cytotoxicity; the use of the chitosan/xanthan gum-based polyelectrolyte complexes PA1 and PC-11 to modify it not only to reduces its toxicity, but also improves its drug efficacy. Because of this, these compounds may become a new research hotspot. [Formula: see text]-Escin metabolism can be converted by the CYP1A2 enzyme in the intestinal flora to produce [Formula: see text]-escin, deacylated, deglycosylated, and 21[Formula: see text]-[Formula: see text]-crotonoyl-protoescin, and the binding rate of the plasma proteins is higher than 90%. These are mainly metabolized by the liver, kidneys, and other organs, and excreted in the form of urine and feces. The number of reports on the specific mediators of the metabolism of [Formula: see text]-escin and their mechanisms and metabolites is relatively small; furthermore, the results are vague. Therefore, a complete and in-depth exploration of the pharmacokinetic characteristics of [Formula: see text]-escin is needed to provide a more complete and effective theoretical reference for the study of its pharmacodynamic activity.
[化学式：见正文]-七叶皂苷是从[植物名称]种子中提取的一种齐墩果烷型五环三萜皂苷，分布更为广泛。[化学式：见正文]-七叶皂苷钠已被美国 FDA 批准用于临床。本文旨在对[化学式：见正文]-七叶皂苷的药理活性、药代动力学特性、毒性和分析方法进行综述。研究表明，[化学式：见正文]-七叶皂苷具有显著的抗肿瘤、抗病毒、抗炎等活性，且不良反应较少，安全性较高。综述表明，[化学式：见正文]-七叶皂苷的药理作用涉及 ATM/[化学式：见正文]H2AX、RhoA/Rock、GSK-3[化学式：见正文]/[化学式：见正文]-Catenin、HER2/HER3/Akt 和 PI3K/Akt 信号通路，以及细胞周期蛋白 A、p21[化学式：见正文]、存活素、Bcl-2、Mcl-1、半胱天冬酶、TGF-[化学式：见正文]、MMPs 和 TNF-[化学式：见正文]等炎症因子。[化学式：见正文]-七叶皂苷具有显著的细胞毒性；使用壳聚糖/黄原胶基聚电解质复合物 PA1 和 PC-11 对其进行修饰，不仅降低了其毒性，而且提高了其药效。因此，这些化合物可能成为新的研究热点。[化学式：见正文]-七叶皂苷的代谢可以被肠道菌群中的 CYP1A2 酶转化为[化学式：见正文]-七叶皂苷、去酰基、去糖基化和 21[化学式：见正文]-[化学式：见正文]-丁烯酸原七叶皂苷，其与血浆蛋白的结合率高于 90%。这些主要在肝脏、肾脏等器官中代谢，并以尿液和粪便的形式排泄。关于[化学式：见正文]-七叶皂苷代谢的具体介质及其机制和代谢物的报道数量相对较少，而且结果也比较模糊。因此，需要对[化学式：见正文]-七叶皂苷的药代动力学特征进行全面深入的探索，为其药效学研究提供更完整、更有效的理论参考。
