Synthesis of andrographolide derivatives and their TNF-alpha and IL-6 expression inhibitory activities

Jing Li; Wenlong Huang; Huibin Zhang; Xinyang Wang; Huiping Zhou

doi:10.1016/j.bmcl.2007.10.009

Synthesis of andrographolide derivatives and their TNF-alpha and IL-6 expression inhibitory activities

Bioorg Med Chem Lett. 2007 Dec 15;17(24):6891-4. doi: 10.1016/j.bmcl.2007.10.009. Epub 2007 Oct 5.

Authors

Jing Li¹, Wenlong Huang, Huibin Zhang, Xinyang Wang, Huiping Zhou

Affiliation

¹ Center of Drug Discovery, College of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.

PMID: 17962017
DOI: 10.1016/j.bmcl.2007.10.009

Abstract

The synthesis of a series of andrographolide derivatives was described and their inhibitory effects on TNF-alpha and IL-6 secretion in mouse macrophages were also evaluated. Most of the tested compounds showed inhibitory effects, and the compounds with the structure of 12-hydroxy-14-dehydroandrographolide showed better inhibitory activity than the compounds with the structure of isoandrographolide.

MeSH terms

Animals
Cell Line
Diterpenes / chemical synthesis*
Diterpenes / chemistry
Diterpenes / pharmacology*
Interleukin-6 / metabolism*
Macrophages / drug effects
Macrophages / metabolism
Mice
Molecular Structure
Structure-Activity Relationship
Tumor Necrosis Factor-alpha / metabolism*

Substances

Diterpenes
Interleukin-6
Tumor Necrosis Factor-alpha
andrographolide