Biomolecules & Therapeutics
The Effect of Luteolin on the Modulation of Vascular Contractility via ROCK and CPI-17 Inactivation
Hyuk-Jun Yoon1,†, Dae Hong Kang1,†, Fanxue Jin2, Joon Seok Bang3, Uy Dong Sohn4 and Hyun Dong Je1,*
1Department of Pharmacology, College of Pharmacy, Daegu Catholic University, Gyeongsan 38430, 2Department of Pharmacology, Kyungpook National University School of Medicine, Daegu 41944, 3College of Pharmacy, Sookmyung Women’s University, Seoul 04310, 4Department of Pharmacology, College of Pharmacy, Chung-Ang University, Seoul 06974, Republic of Korea
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The first two authors contributed equally to this work.
Received: June 29, 2022; Revised: August 17, 2022; Accepted: August 18, 2022; Published online: September 6, 2022.
© The Korean Society of Applied Pharmacology. All rights reserved.

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In this investigation, we made a study of the efficacy of luteolin (a flavonoid found in plants such as vegetables, herbs and fruits) on vascular contractibility and to elucidate the mechanism underlying the relaxation. Isometric contractions of denuded muscles were stored and combined with western blot analysis which was conducted to assess the phosphorylation of myosin phosphatase targeting subunit 1 (MYPT1) and phosphorylation-dependent inhibitory protein for myosin phosphatase (CPI-17) and to examine the effect of luteolin on the RhoA/ROCK/CPI-17 pathway. Luteolin significantly alleviated phorbol ester-, fluoride- and thromboxane mimetic-elicited contractions regardless of endothelial nitric oxide synthesis, implying its direct effect on smooth muscle. It also significantly alleviated the fluoride-elicited elevation in pCPI-17 and pMYPT1 levels and phorbol 12,13-dibutyrate-elicited increase in pERK1/2 level, suggesting depression of ROCK and PKC/MEK activity and ensuing phosphorylation of MYPT1, CPI-17 and ERK1/2. Taken together, these results suggest that luteolin-elicited relaxation includes myosin phosphatase reactivation and calcium desensitization, which seems to be arbitrated by CPI-17 dephosphorylation via ROCK/PKC inhibition.
Keywords: CPI-17, Fluoride, Luteolin, MYPT1, Phorbol ester, ROCK

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