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Synthesis and biological evaluation of panaxatriol derivatives against myocardial ischemia/reperfusion injury in the rat.
- Source :
-
European Journal of Medicinal Chemistry . Jan2020, Vol. 185, pN.PAG-N.PAG. 1p. - Publication Year :
- 2020
-
Abstract
- Panaxatriol (PT) is a natural product derived from ginseng that possesses cardioprotective effects in isolated rat hearts. To develop more potent therapeutic agents against myocardial ischemia/reperfusion (MI/R) injury from natural products, a novel series of heterocycle ring-fused panaxatriol derivatives were designed and synthesized. In vitro results showed that approximately half of them exhibited increased cytoprotective activity compared with PT in a cardiomyocyte model of oxygen-glucose deprivation and reperfusion (OGD/R) injury. Furthermore, the in vitro activity of the representative derivative, compound 18 , was also confirmed in a rat model of MI/R injury. In vivo results showed that 18 can markedly reduce myocardial infarction size, decrease circulating cardiac troponin I (cTnI) leakage, and alleviate cardiac tissue damage in the rats. Therefore, these findings provide the basis for further development of novel anti-MI/R injury agents. Image 1 • A series of heterocycle ring-fused panaxatriol (PT) derivatives were designed and synthesized. • The compounds were evaluated for cardioprotective activity in a cardiomyocyte model of OGD/R injury. • Approximately half of the PT derivatives exhibited more potent cytoprotective activity than PT. • Representative compound, 18 , attenuated the reperfusion injury in a rat model of myocardial infarction. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 02235234
- Volume :
- 185
- Database :
- Academic Search Index
- Journal :
- European Journal of Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 140094862
- Full Text :
- https://doi.org/10.1016/j.ejmech.2019.111729