Gallic acid isolated from Spirogyra sp. improves cardiovascular disease through a vasorelaxant and antihypertensive effect.
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.
Department of Marine Life Sciences, Jeju National University, Jeju 690-756, Republic of Korea.
Nalae
N
Kang
Department of Marine Life Sciences, Jeju National University, Jeju 690-756, Republic of Korea.
Ji-Hyeok
JH
Lee
Department of Marine Life Sciences, Jeju National University, Jeju 690-756, Republic of Korea.
WonWoo
W
Lee
Department of Marine Life Sciences, Jeju National University, Jeju 690-756, Republic of Korea.
Ju-Young
JY
Ko
Department of Marine Life Sciences, Jeju National University, Jeju 690-756, Republic of Korea.
Eun-A
EA
Kim
Department of Seafood Science and Technolgy, Institute of Marine Industry, Gyeongsang National University, Tongyeong 650-160, Republic of Korea.
Jin-Soo
JS
Kim
Department of Food Science and Nutrition, Institute of Marine Industry, Gyeongsang National University, Jinju 660-701, Republic of Korea.
Min-Soo
MS
Heu
Department of Biology, Kongju National University, Kongju 314-701, Republic of Korea. Electronic address: ghkim@kongju.ac.kr.
Gwang Hoon
GH
Kim
Department of Marine Life Sciences, Jeju National University, Jeju 690-756, Republic of Korea. Electronic address: youjin2014@gmail.com.
You-Jin
YJ
Jeon
D000806:Angiotensin-Converting Enzyme Inhibitors / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D000959:Antihypertensive Agents / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D000975:Antioxidants / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D002318:Cardiovascular Diseases / Q000188:drug therapy* / Q000503:physiopathology; D002478:Cells, Cultured; D054684:Cyclic Nucleotide Phosphodiesterases, Type 3 / Q000378:metabolism; D005707:Gallic Acid / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D061307:Human Umbilical Vein Endothelial Cells / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D008297:Male; D009569:Nitric Oxide / Q000378:metabolism; D052250:Nitric Oxide Synthase Type III / Q000378:metabolism; D051381:Rats; D011918:Rats, Inbred SHR; D058131:Spirogyra / Q000737:chemistry; D014665:Vasodilator Agents / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use
D000806:Angiotensin-Converting Enzyme Inhibitors; D000959:Antihypertensive Agents; D000975:Antioxidants; D014665:Vasodilator Agents; D009569:Nitric Oxide; D005707:Gallic Acid; C496314:NOS3 protein, human; D052250:Nitric Oxide Synthase Type III; D054684:Cyclic Nucleotide Phosphodiesterases, Type 3
Antihypertensive effect; Cardiovascular diseases; Gallic acid; Spyrogira sp.; Vasorelaxation