4.6 Article

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

Journal

ENVIRONMENTAL TOXICOLOGY AND PHARMACOLOGY
Volume 39, Issue 2, Pages 764-772

Publisher

ELSEVIER SCIENCE BV
DOI: 10.1016/j.etap.2015.02.006

Keywords

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

Funding

  1. Ministry of Education (MOE)
  2. National Research Foundation of Korea (NRF) through Human Resource Training Project for Regional Innovation [NRF - 2012H1B8A2025863]
  3. Ministry of Agriculture, Food and Rural Affairs (MAFRA)
  4. Ministry of Oceans and Fisheries (MOP)
  5. Rural Development Administration (RDA)
  6. Korea Forest Service (KFS) [213004-04-2-SB930]
  7. National Research Foundation of Korea [2012H1B8A2025863] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)

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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 mu g/ml. In silico simulations revealed that GA binds to the active site of ACE (PDB: 1086) 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. (C) 2015 Elsevier B.V. All rights reserved.

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