European Journal of Medicinal Chemistry p. 805 - 816 (2018)
Update date:2022-07-29
Topics: Characterization Biological testing Structure-Activity Relationship (SAR) Analysis Clinical Trials Literature Review Design and Synthesis Toxicity and Safety Formulation Patent Application Pharmacokinetics and Pharmacodynamics Publication and Presentation
Song, Zhiqiang
Huang, Sujie
He, Yuchen
Li, Jiabin
Lin, Kejiang
Xue, Xiaowen
A series of 14-deoxyandrographolide-19-oic acid and 14-deoxy-11,12 (or 14,15)-didehydroandrographolide-19-oic acid derivatives were designed, synthesized and screened in vitro against the mouse fibroblast cell lines NIH-3T3. Thirteen compounds 8a-f, 14a-c, 14e-f, and 18a-b were found to exhibit better anti-fibrotic activities than andrographolide, with compounds 8b and 14e displaying best activity with IC50 values of 12.86 and 13.57 μM against NIH-3T3 respectively. Further anti-fibrotic investigation was performed in terms of PCR and western bolt analysis. Our study demonstrated that compounds 8b and 14e suppressed effectively the expression of α-smooth muscle actin, fibronectin and collagen in NIH-3T3. Preliminary structure-activity analysis revealed that 14-deoxygenation and 19-carboxylation of andrographolide could significantly improve its anti-fibrotic effect, which made 14-deoxyandrographolide-19-oic acid and 14-deoxy-11,12-didehydroandrographolide-19-oic acid promising leads for the development of new anti-fibrotic agents.
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