五味子中的主要活性成分五味子醇 A:五味子中的主要活性成分五味子醇 A:制备、生物活性和药代动力学分析综述。

The American journal of Chinese medicine Pub Date : 2024-01-01 Epub Date: 2024-05-08 DOI:10.1142/S0192415X24500290
Ying Wu, Chao Ding, Chenwang Liu, Linwei Dan, Haonan Xu, Xinzhuo Li, Yuze Li, Xiaomei Song, Dongdong Zhang
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摘要

五味子是一种历史悠久的传统中药,具有收敛、益气、补肾、宁心安神等功效。值得注意的是,从五味子中提取的五味子甲(SA)显示出令人惊讶和满意的生物活性,包括抗炎、保肝、保护心血管和抗肿瘤等特性。在众多药理作用中,SA 对中枢受损神经的保护作用更为明显,通过保护受损神经细胞和增强抗氧化能力,可改善阿尔茨海默氏症和帕金森氏症等神经退行性疾病。药代动力学研究表明,SA 的药代动力学特征是吸收快、分布广,在肝脏中浓度最高,主要经肾脏排泄。不过,肝脏和肠道的首过代谢会影响 SA 的生物利用度。此外,SA 作为《金银花药典》中的指标成分,其含量应不低于 0.40%,而金银花复方中 SA 的含量采用高效液相色谱法(HPLC)测定,该方法稳定可靠,可为后续的质量控制奠定基础。因此,本文系统地综述了SA的制备、药理作用、药代动力学特性及含量测定,旨在更新和加深对SA的认识,并为后期SA的研究提供理论依据。
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Schisandrol A, the Major Active Constitute in Schisandra chinensis: A Review of Its Preparation, Biological Activities, and Pharmacokinetics Analysis.

Schisandra chinensis (S. chinensis) has a long history as a traditional Chinese medicine that is astringent, beneficial to vital energy, tonifies the kidney, tranquilizes the heart, etc. Significantly, Schisandrol A (SA) is extracted from S. chinensis and shows surprising and satisfactory biological activity, including anti-inflammatory, hepatoprotective, cardiovascular protection, and antitumor properties, among others. SA has a more pronounced protective effect on central damaged nerves among its numerous pharmacological effects, improving neurodegenerative diseases such as Alzheimer's and Parkinson's through the protection of damaged nerve cells and the enhancement of anti-oxidant capacity. Pharmacokinetic studies have shown that SA has a pharmacokinetic profile with a rapid absorption, wide distribution, maximal concentration in the liver, and primarily renal excretion. However, hepatic and intestinal first-pass metabolism can affect SA's bioavailability. In addition, the content of SA, as an index component of S. chinensis Pharmacopoeia, should not be less than 0.40%, and the content of SA in S. chinensis compound formula was determined with the help of high-performance liquid chromatography (HPLC), which is a stable and reliable method, and it can lay a foundation for the subsequent quality control. Therefore, this paper systematically reviews the preparation, pharmacological effects, pharmacokinetic properties, and content determination of SA with the goal of updating and deepening the understanding of SA, as well as providing a theoretical basis for the study of SA at a later stage.

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