Biomol Ther.
2023 Mar;31(2):193-199. 10.4062/biomolther.2022.087.
The Effect of Luteolin on the Modulation of Vascular Contractility via ROCK and CPI-17 Inactivation
- Affiliations
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- 1Department of Pharmacology, College of Pharmacy, Daegu Catholic University, Gyeongsan 38430, Republic of Korea
- 2Department of Pharmacology, Kyungpook National University School of Medicine, Daegu 41944, Republic of Korea
- 3College of Pharmacy, Sookmyung Women’s University, Seoul 04310, Republic of Korea
- 4Department of Pharmacology, College of Pharmacy, Chung-Ang University, Seoul 06974, Republic of Korea
- KMID: 2539588
- DOI: http://doi.org/10.4062/biomolther.2022.087
Abstract
- 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 in-crease 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.
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