Protective effect of quercetin against myocardial ischemia as a Ca 2+ channel inhibitor: involvement of inhibiting contr
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RESEARCH ARTICLE
Protective effect of quercetin against myocardial ischemia as a Ca2+ channel inhibitor: involvement of inhibiting contractility and Ca2+ influx via L‑type Ca2+ channels Yingran Liang1 · Yuanyuan Zhang2 · Miaomiao Liu1 · Xue Han1 · Jianping Zhang2 · Xuan Zhang2,3 · Li Chu1,4
Received: 16 March 2020 / Accepted: 1 August 2020 © The Pharmaceutical Society of Korea 2020
Abstract Many studies describe the stimulating effect of quercetin on C a2+ channels and the treatment of cardiovascular diseases such as myocardial ischemia and hypertension. However, these studies are scattered and contradictory. The aim of this study is to elucidate the protective effects of quercetin against isoproterenol (ISO)-induced myocardial ischemia and verify the cellular mechanisms based on the L-type Ca2+ channel (LTCC), C a2+ transients, and myocardial contractility. An animal model of myocardial ischemia was established by subcutaneous injection of ISO for 2 days. Quercetin significantly reduced J-point elevation, heart rate, reactive oxygen species, serum levels of myocardial enzymes, superoxide dismutase, catalase, glutathione, glutathione peroxidase, glutathione S-transferase and improved heart pathologic morphology. L-type Ca2+ current (ICa-L) was tested in an experiment with isolated rat myocardial cells by using the whole-cell patch-clamp recording technique and IonOptix Myocam detection system. Quercetin * Jianping Zhang [email protected] * Xuan Zhang [email protected] * Li Chu [email protected] 1
School of Pharmacy, Hebei University of Chinese Medicine, Shijiazhuang 050200, Hebei, China
2
School of Basic Medicine, Hebei University of Chinese Medicine, Shijiazhuang 050200, Hebei, China
3
Hebei Key Laboratory of Integrative Medicine on Liver-Kidney Patterns, Shijiazhuang 050200, Hebei, China
4
Hebei Key Laboratory of Chinese Medicine Research On Cardio-Cerebrovascular Disease, Shijiazhuang 050200, Hebei, China
reduced ICa-L in a concentration-dependent fashion with a half-maximal inhibitory concentration of 4.67 × 10–4 M. Quercetin also shifted the current–voltage curve upwards, moved the activation and inactivation curves to the left and inhibited the amplitude of the cell shortening and C a2+ transients. The results showed that quercetin acts as a LTCC inhibitor and exerts a cardioprotective effect by inhibiting Ca2+ influx and contractility in rats. Keywords Quercetin · Myocardial ischemia · L-type ca2+ channel · Ca2+ transients · Cell contractility
Introduction The polyphenolic compound quercetin is one of the most widely used flavonoids and has beneficial effects in cardiovascular diseases (Patel et al. 2018). Quercetin has several biological and pharmacological effects, such as antidepressant, anticancer, antiviral, antioxidant, antiinflammatory and analgesic effects (Hertog et al. 1993, 1995; Birt et al. 2001; Perez-Vizcaino et al. 2006). However, the possible protective mechanisms of quercetin on myocardial ischemia r
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