The novel compound liguzinediol exerts positive inotropic effects in isolated rat heart via sarcoplasmic reticulum Ca 2+ ATPase-dependent mechanism

Chen, Long; Xu, Yi; Li, Wei; Wu, Hao; Luo, Zhuoka; Li, Xuehua; Huang, Feifei; Young, Clint; Liu, Zheng; Zhou, Shuyuan

doi:10.1016/j.lfs.2012.08.001

Cited by 16 publications

(8 citation statements)

References 32 publications

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“…Liguzinediol, 2, 5-dimethyl-3, 6-dimethyl-pyrazine, is a derivative that takes ligustrazine as the lead compound for structural modi cation [8,9] (Figure 1). Liguzinediol could signi cantly enhance left ventricular contractility and improve the diastolic function of rat heart without arrhythmia and other adverse effects [10,11]. Liguzinediol has the advantages of low toxicity and good water solubility, which has laid a good foundation for the research and development of non-digitalis positive inotropic drugs [12].…”

Section: Introductionmentioning

confidence: 99%

The protective effects of liguzinediol on congestive heart failure induced by myocardial infarction and its relative mechanism

Chen

Zhang

et al. 2020

Preprint

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Background: Heart failure (HF) is one of the most common causes of cardiovascular diseases in the world. Currently, the drugs used to treat HF in the clinic may cause serious side effects. Liguzinediol, 2, 5-dimethyl-3, 6-dimethyl-pyrazine, is a compound synthesized after the structural modification of ligustrazine (one active ingredient of Szechwan Lovage Rhizome). We aimed to observe the effects of liguzinediol on preventing HF and explore the related mechanisms.Methods: The ligation of left anterior descending coronary artery was operated to established the myocardial infarction (MI) model in Sprague–Dawley rats. Cardiac functions were recorded by echocardiography and hemodynamics. The changes in the Renin-Angiotensin-Aldosterone System (RAAS), inflammation, and oxidative stress were detected by radioimmunoassay and Elisa kits. Western blot and real-time PCR were applied to determine the expressions of the TGF-β1/Smads pathway.Results: Firstly, liguzinediol enhanced the systolic and diastolic functions of the heart in MI rats. Liguzinediol improved ventricular remodeling by reducing myocardial cell necrosis, as well as reducing collagen deposition and myocardial fibrosis. Then, liguzinediol suppressed the activation of RAAS, inhibited the synthesis of pro-inflammation factors, and reduced oxidative stress. In the end, liguzinediol also down-regulated the expressions of the TGF-β1/Smads pathway.Conclusions: Liguzinediol could alleviate HF caused by MI in rats, and the protective effect was associated with the regulation of the TGF-β1/Smads pathway.

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Section: Introductionmentioning

confidence: 99%

The protective effects of liguzinediol on congestive heart failure induced by myocardial infarction and its relative mechanism

Chen

Zhang

et al. 2020

Preprint

View full text Add to dashboard Cite

show abstract

“…Liguzinediol, 2, 5-dimethyl-3, 6-dimethyl-pyrazine, is a derivative that takes ligustrazine as the lead compound for structural modification [8,9]. Liguzinediol could significantly enhance left ventricular contractility and improve the diastolic function of rat heart without arrhythmia and other adverse effects [10,11]. Liguzinediol has the advantages of low toxicity and good water solubility, which has laid a good foundation for the research and development of non-digitalis positive inotropic drugs [12].…”

Section: Introductionmentioning

confidence: 99%

The protective effects of liguzinediol on congestive heart failure induced by myocardial infarction and its relative mechanism

Chen

Zhang

et al. 2020

Preprint

View full text Add to dashboard Cite

Background : Heart failure (HF) is one of the most common causes of cardiovascular diseases in the world. Currently, the drugs used to treat HF in the clinic may cause serious side effects. Liguzinediol, 2, 5-dimethyl-3, 6-dimethyl-pyrazine, is a compound synthesized after the structural modification of ligustrazine (one active ingredient of Szechwan Lovage Rhizome ). We aimed to observe the effects of liguzinediol on preventing HF and explore the related mechanisms. Methods : The ligation of left anterior descending coronary artery was operated to established the myocardial infarction (MI) model in Sprague–Dawley rats. Cardiac functions were recorded by echocardiography and hemodynamics. The changes in the Renin-Angiotensin-Aldosterone System (RAAS), inflammation, and oxidative stress were detected by radioimmunoassay and Elisa kits. Western blot and real-time PCR were applied to determine the expressions of the TGF-β1/Smads pathway. Results : Firstly, liguzinediol enhanced the systolic and diastolic functions of the heart in MI rats. Liguzinediol improved ventricular remodeling by reducing myocardial cell necrosis, as well as reducing collagen deposition and myocardial fibrosis. Then, liguzinediol suppressed the activation of RAAS, inhibited the synthesis of pro-inflammation factors, and reduced oxidative stress. In the end, liguzinediol also down-regulated the expressions of the TGF-β1/Smads pathway. Conclusions : Liguzinediol could alleviate HF caused by MI in rats, and the protective effect was associated with the regulation of the TGF-β1/Smads pathway.

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“…Out of all the derivatives, liguzinediol ( Fig. 1) 2,5-dihydroxymethyl-3,6-dimethylpyrazine has shown smaller toxicity and higher bioavailability, which exerts positive inotropic effects in isolated rat heart via sarcoplasmic reticulum Ca 2+ ATPase-dependent mechanism without arrhythmia risk [7]. Preclinical studies have also shown that liguzinediol shows promise for the treatment of heart failure [8].…”

Section: Introductionmentioning

confidence: 99%

Study on Pharmacokinetics of Liguzinediol and Four Metabolites in Rats by UFLC–MS/MS

et al. 2016

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The novel compound liguzinediol exerts positive inotropic effects in isolated rat heart via sarcoplasmic reticulum Ca 2+ ATPase-dependent mechanism

Cited by 16 publications

References 32 publications

The protective effects of liguzinediol on congestive heart failure induced by myocardial infarction and its relative mechanism

The protective effects of liguzinediol on congestive heart failure induced by myocardial infarction and its relative mechanism

The protective effects of liguzinediol on congestive heart failure induced by myocardial infarction and its relative mechanism

Study on Pharmacokinetics of Liguzinediol and Four Metabolites in Rats by UFLC–MS/MS

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