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穿心莲内酯磺化物与喜炎平:化学成分、药理活性、临床应用及不良反应综述

Andrographolide Sulfonates and Xiyanping: A Review of Chemical Composition, Pharmacological Activities, Clinical Applications, and Adverse Reactions.

作者信息

Li Zihong, Yao Lihao, Liu Zhenjie, Wang Liuping, Ruan Huini, Shen Yuanle, Zhang Peng, Li Kaitong, Wang Honglan, Fan Lili, Tu Liangxing, Feng Jianfang

机构信息

School of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530200, China.

Guangxi Engineering Technology Research Center of Advantage Chinese Patent Drug and Ethnic Drug Development, Nanning 530020, China.

出版信息

Pharmaceuticals (Basel). 2025 Jan 29;18(2):183. doi: 10.3390/ph18020183.

Abstract

is a plant of the Acanthaceae family and its primary bioactive constituent, andrographolide, exhibits a broad spectrum of pharmacological activities and notable clinical efficacy. However, its poor solubility and limited bioavailability pose significant challenges for therapeutic applications. To overcome these limitations, researchers have synthesized andrographolide sulfonates by reacting andrographolide with ethanol and sulfuric acid. This sulfonated derivative significantly enhances water solubility and bioavailability while retaining key pharmacological properties such as anti-inflammatory and antiviral activities. As a representative formulation, Xiyanping injection has been widely employed in the treatment of respiratory infections, pneumonia, and related conditions, playing a critical role during the COVID-19 pandemic. Despite its widespread application, there has yet to be a comprehensive review of its chemical composition and pharmacological mechanisms. Additionally, the safety of Xiyanping injection remains a topic of some debate. This review systematically examines the chemical composition, pharmacological activities, clinical applications, and adverse reactions of andrographolide sulfonates and their formulation in Xiyanping injection to provide a scientific basis for further research and applications, while also offering valuable insights for the development of similar sulfonated drugs.

摘要

是一种爵床科植物,其主要生物活性成分穿心莲内酯具有广泛的药理活性和显著的临床疗效。然而,其溶解度差和生物利用度有限给治疗应用带来了重大挑战。为了克服这些限制,研究人员通过将穿心莲内酯与乙醇和硫酸反应合成了穿心莲内酯磺酸盐。这种磺化衍生物在保留抗炎和抗病毒活性等关键药理特性的同时,显著提高了水溶性和生物利用度。作为一种代表性制剂,喜炎平注射液已广泛用于治疗呼吸道感染、肺炎及相关病症,在新冠疫情期间发挥了关键作用。尽管其应用广泛,但尚未对其化学成分和药理机制进行全面综述。此外,喜炎平注射液的安全性仍是一个存在一定争议的话题。本综述系统地研究了穿心莲内酯磺酸盐及其在喜炎平注射液中的制剂的化学成分、药理活性、临床应用和不良反应,为进一步研究和应用提供科学依据,同时也为类似磺化药物的开发提供有价值的见解。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d662/11859262/2d97c64fbc02/pharmaceuticals-18-00183-g001.jpg

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