Synthesis and Biological Evaluation of Andrographolide Derivatives as Potential Anti-Inflammatory Agents
Journal Title: Journal of Pharmaceutical and Biomedical Sciences - Year 2017, Vol 7, Issue 4
Abstract
Background Persistent inflammation might induce lipid metabolism disorders, which affected a significant proportion of the population worldwide, such as serious infections, cardiovascular diseases and autoimmune diseases. 14-Alpha-Lipoic acylandrographolide (AL-1) was previously synthesized and shown good activity to treat inflammatory diseases in our lab. However, AL-1 has a poor solubility in water and hygroscopicity, which brings problems in drug delivery. Aim To enhance the water solubility of AL-1 and its anti-inflammatory activity. Method By modifying its structure, we designed and synthesized the andrographolide derivative hydrochloric salt AL-2, which contains two glycine groups compared with AL-1. Then, the anti-inflammatory activity of AL-2 was evaluated in vitro. Results and Conclusions Both AL-1 and AL-2 could inhibit the release of NO in inflammatory cells. In addition, the water-solubility of AL-2 was improved as well as its cytotoxicity was reduced. Therefore, these results suggested that AL-2 may be a potential drug candidate in the treatment of inflammation
Authors and Affiliations
Haibing Duan, Mei Jing, Zhenshen Li, Zaijun Zhang, Yuqiang Wang, Lipeng Xu, Pei Yu
Keywords
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