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Chinese Journal of Clinical Pharmacology and Therapeutics ›› 1999, Vol. 4 ›› Issue (2): 85-92.

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Caffeic acid, ferulic acid:a new kind of non-peptide endothel in antagonist1

WANG Feng, LIU Min, YANG Lian-Chun, WANG Jing-Yuan, CAI Qing, LU Min, LI Fei   

  1. General Hospital of Air Force, PLA Bei jing 100036
  • Received:1999-04-15 Revised:1999-05-06 Online:1999-06-26 Published:2020-12-04
  • Supported by:
    1 This supported by National Natural Scientific Foundation of China

Abstract: Aim The antagonist effects of cinnamic acid compounds of caffeic acid and ferulic acid on endo thelin-1 biological responses and their antagonist mechanism to endothelin-1 were studied.Methods Caffeic acid and ferulic acid, in different dosage were separately given int raperitoneally to mice and intravenously torats.The protective effect on acute death of mouse and the vasodilatative effect on constriction of isolated rings induced by ET-1 and the change of blood pressure of normotensive rats were observed.The drugs were also administered orally to DOCA-salt hypertensive rats, and the body weight, cardio vasculartissues wet weight, gene expression of ET-1, c-fos and HSP70 mRNA, plasma levels of ET-1 in DOCA-salt hypertensive rats were measured.By binding experiment of 125I-ET-1 with 3T3 cells.The antagonism of Caffeic acid and ferulic acid on ET-1 was determined.Results Both Caffeic acid and ferulic acid could dose-dependently delay the acute death induced by ET-1, blunt the elevation of blood pressure on normotensive rats markedly, dilate the vasoconstriction of isolated aorticrings, blunt the elevation of systolic blood pressure and development of cardiov ascular hypertrophy in DOCA-salt hypertensive rats, inhibit gene expression of ET-1, c-fos, HSP70 mRNA and decrease the plasma levels of ET-1.both of them bind compet itively with 125I-ET-1 on 3T3 cells. Conclusion Caffeic acid and ferulic acid are a new kind non-peptide ET antagonists.

Key words: endothelin-1, Caffeic acid, ferulic acid, antagonist

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