4.5 Review

Recent Progress in Andrographolide Derivatization: Structural Modification and Biological Activity

Journal

MINI-REVIEWS IN MEDICINAL CHEMISTRY
Volume 22, Issue 11, Pages 1559-1584

Publisher

BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1389557521666211022150032

Keywords

Andrographolide; modification; bioactivity; drug discovery; Andrographis paniculata; traditional chinese medicines

Funding

  1. National Megaproject for Innovative Drugs [2019ZX09721001-004-007]
  2. National Natural Science Foundation of China [U1803122, U1703111, 81473254, 81773594, 81773637]
  3. Liaoning Revitalization Talents Program [XLYC1807182]
  4. Liaoning Province Natural Science Foundation, China [2019-MS-299]

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Researchers have prepared numerous bioactive derivatives of andrographolide through chemical modification and classified them according to their biological activities. These studies contribute to the development of novel therapeutic drugs.
Natural products have remarkable structural diversity and biological characteristics, providing researchers with more possibilities to develop novel drugs for disease therapeutics. Andrographolide, an ent-labdane diterpenoid from traditional Chinese medicines, Andrographis paniculata, exhibits a broad range of biological activities, which has been a hot area of research for several years. Up to now, lots of its derivatives with multiple bioactivities have been prepared through chemical modification. This review summarizes andrographolide derivatives prepared in the last ten years (2006-present), classifies them by different biological activities, and provides some discussion about the design of novel and potent derivatives.

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