Synthesis and Biological Evaluation of Andrographolide Derivatives as Anti-inflammatory Agent

Title:Synthesis and Biological Evaluation of Andrographolide Derivatives as Anti-inflammatory Agent

Volume: 24 Issue: 30

Author(s): Zeyu Zhu, Haibing Duan, Mei Jing, Lipeng Xu*Pei Yu*

Affiliation:

• Institute of New Drug Research and Guangzhou Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine, Jinan University College of Pharmacy, Guangzhou, 510632,China

• Institute of New Drug Research and Guangzhou Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine, Jinan University College of Pharmacy, Guangzhou, 510632,China

Keywords: Andrographolide derivative, anti-inflammatory, tetramethylpyrazine, picolinic acid, benzimidazole, MTT.

Abstract: Background: Andrographolide (Andro) is a main active ingredient of the natural plant Andrographis paniculata, which has special effects on bacterial infections and inflammatory diseases.

Objective: We previously synthesized Andrographolide derivatives AL-1 and investigated its anti-inflammatory activity. For further research, we decided to modify the structure of AL-1 and expected to have better antiinflammatory activity.

Methods: By conjugating with anti-inflammatory and anti-bacterial group, we designed and synthesized the andrographolide derivative AL-2, AL-3 and AL-4. The anti-inflammatory activity of AL-2, AL-3 and AL-4 was also evaluated by detecting cell activity and Nitric Oxide (NO) release.

Results: The new compounds AL-2, AL-3 and AL-4 increased cell viability in lipopolysaccharide (LPS)-induced RAW 264.7 cell, which could have a certain anti-inflammatory activity, and inhibited the release of NO in cells to reduce the inflammatory response of cells.

Conclusion: The new compounds AL-2, AL-3 and AL-4 may be candidates of anti-inflammatory drugs in the future.

Cite this article as:

Zhu Zeyu, Duan Haibing , Jing Mei , Xu Lipeng *, Yu Pei *, Synthesis and Biological Evaluation of Andrographolide Derivatives as Anti-inflammatory Agent, Current Pharmaceutical Design 2018; 24 (30) . https://dx.doi.org/10.2174/1381612824666180724130014