Gallic acid isolated from Spirogyra sp. improves cardiovascular disease through a vasorelaxant and antihypertensive effect

Environ Toxicol Pharmacol. 2015 Mar;39(2):764-72. doi: 10.1016/j.etap.2015.02.006. Epub 2015 Feb 16.

Abstract

In this study, we investigated the vasorelaxant and antihypertensive effects of gallic acid (GA), a polyphenol isolated from the green alga Spirogyra sp., to assess its suitability as a therapeutic for cardiovascular diseases (CVDs). We examined the effect of GA on endothelium-dependent vasorelaxation in human umbilical vein endothelial cells (HUVECs). GA increased nitric oxide (NO) levels by increasing phosphorylation of endothelial nitric oxide synthase (eNOS), and its effect on NO production was attenuated by pretreatment with the eNOS inhibitor N(G)-nitro-L-arginine methyl ester (L-NAME). We also investigated its antihypertensive effect by examining GA-mediated inhibition of angiotensin-I converting enzyme (ACE). GA inhibited ACE with a half-maximal inhibitory concentration (IC50) value of 37.38 ± 0.39 μg/ml. In silico simulations revealed that GA binds to the active site of ACE (PDB: 1O86) with a binding energy of -270.487 kcal/mol. Furthermore, GA clearly reduced blood pressure in spontaneously hypertensive rats (SHR) to an extent comparable to captopril. These results suggest that GA isolated from Spirogyra sp. exerts multiple therapeutic effects and has potential as a CVD treatment.

Keywords: Antihypertensive effect; Cardiovascular diseases; Gallic acid; Spyrogira sp.; Vasorelaxation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiotensin-Converting Enzyme Inhibitors / isolation & purification
  • Angiotensin-Converting Enzyme Inhibitors / pharmacology*
  • Angiotensin-Converting Enzyme Inhibitors / therapeutic use
  • Animals
  • Antihypertensive Agents / isolation & purification
  • Antihypertensive Agents / pharmacology*
  • Antihypertensive Agents / therapeutic use
  • Antioxidants / isolation & purification
  • Antioxidants / pharmacology*
  • Antioxidants / therapeutic use
  • Cardiovascular Diseases / drug therapy*
  • Cardiovascular Diseases / physiopathology
  • Cells, Cultured
  • Cyclic Nucleotide Phosphodiesterases, Type 3 / metabolism
  • Gallic Acid / isolation & purification
  • Gallic Acid / pharmacology*
  • Gallic Acid / therapeutic use
  • Human Umbilical Vein Endothelial Cells / drug effects
  • Human Umbilical Vein Endothelial Cells / metabolism
  • Humans
  • Male
  • Nitric Oxide / metabolism
  • Nitric Oxide Synthase Type III / metabolism
  • Rats
  • Rats, Inbred SHR
  • Spirogyra / chemistry
  • Vasodilator Agents / isolation & purification
  • Vasodilator Agents / pharmacology*
  • Vasodilator Agents / therapeutic use

Substances

  • Angiotensin-Converting Enzyme Inhibitors
  • Antihypertensive Agents
  • Antioxidants
  • Vasodilator Agents
  • Nitric Oxide
  • Gallic Acid
  • NOS3 protein, human
  • Nitric Oxide Synthase Type III
  • Cyclic Nucleotide Phosphodiesterases, Type 3