Cochlospermum vitifolium induces vasorelaxant and antihypertensive effects mainly by activation of NO/cGMP signaling pathway

J Ethnopharmacol. 2010 Aug 9;130(3):477-84. doi: 10.1016/j.jep.2010.05.037. Epub 2010 May 27.

Abstract

Aim of the study: Cochlospermum vitifolium is a medicinal plant used for the treatment of diabetes, hepatobilary and cardiovascular illnesses. The aim of current study was to determine the in vivo antihypertensive and in vitro functional vasorelaxant mechanism of methanol extract of Cochlospermum vitifolium (MECv) and naringenin (NG).

Materials and methods: Test material was assayed on rat isolated aorta rings test with- and without-endothelium to determine their vasorelaxant mechanism. Also, the in vivo antihypertensive effect was evaluated on spontaneously hypertensive rat (SHR) model. In addition, presence of NG into the extract was confirmed by reverse phase high performance liquid chromatography (RP-HPLC) analysis.

Results: MECv (120 mg/kg) and NG (50 and 160 mg/kg) showed acute antihypertensive effects on SHR when systolic and diastolic pressure were decreased at 1 h and 24 h after administration, respectively. Vasorelaxant effect of MECv and NG was shifted to the right when endothelium-intact aortic rings were pre-incubated with L-NAME (10 microM) and ODQ (1 microM). Also, NG relaxant curves were displaced to the right in the presence of tetraethylammonium (TEA, 1 mM) and 2-aminopyridine (2-AP, 100 microM) on endothelium-denuded aortic rings.

Conclusion: Experiments described above showed that MECv play an important role in hypertension regulation through NO synthesis and may be PGI(2) production and potassium channel activation on excessive endothelial dysfunction conditions. Unfortunately, presence of NG into the extract is not significant on bioactivity of the extract; however, this compound could be tested and evaluated as structural scaffold for future drug design for development of antihypertensive agents.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antihypertensive Agents / administration & dosage
  • Antihypertensive Agents / isolation & purification
  • Antihypertensive Agents / pharmacology*
  • Aorta, Thoracic / drug effects
  • Aorta, Thoracic / metabolism
  • Bixaceae / chemistry*
  • Chromatography, High Pressure Liquid
  • Cyclic GMP / metabolism
  • Dose-Response Relationship, Drug
  • Endothelium, Vascular / drug effects
  • Endothelium, Vascular / metabolism
  • Flavanones / administration & dosage
  • Flavanones / isolation & purification
  • Flavanones / pharmacology*
  • Hypertension / drug therapy
  • Hypertension / physiopathology
  • Male
  • Nitric Oxide / metabolism
  • Plant Extracts / administration & dosage
  • Plant Extracts / pharmacology*
  • Rats
  • Rats, Inbred SHR
  • Rats, Wistar
  • Signal Transduction / drug effects
  • Vasodilator Agents / administration & dosage
  • Vasodilator Agents / isolation & purification
  • Vasodilator Agents / pharmacology

Substances

  • Antihypertensive Agents
  • Flavanones
  • Plant Extracts
  • Vasodilator Agents
  • Nitric Oxide
  • Cyclic GMP
  • naringenin