Effects and Mechanism of Action of Ligustrazine on Isoprenaline-Induced Cardiomyocyte Hypertrophy

Ji, Xuan; Song, Xiao; Qian, Wei; Yu, Xijie; Zhu, Jian You

doi:10.1007/s12013-014-0086-2

Cited by 7 publications

(3 citation statements)

References 28 publications

(26 reference statements)

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“…However, these studies did not explore this inhibitory effect in vivo. In vivo research www.nature.com/aps Zhang Y et al Acta Pharmacologica Sinica npg suggested that ligustrazine improved cardiac function in rats with heart failure by inhibiting myocardial cell apoptosis and cardiomyocyte hypertrophy [8][9] . Berberine is an important alkaloid derived from Coptis chinensis Franch (Huang Lian).…”

Section: Introductionmentioning

confidence: 99%

Pretreatment with a combination of ligustrazine and berberine improves cardiac function in rats with coronary microembolization

Zhang

Guo

et al. 2016

Acta Pharmacol Sin

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Aim:We have shown that a combination of ligustrazine and berberine produces more effective inhibition on platelet activation and inflammatory reactions in rat acute myocardial infarction compared with either agent alone. In this study we evaluated the beneficial effects of a combination of ligustrazine and berberine in a rat model of coronary microembolization (CME). Methods: SD rats were treated with ligustrazine, berberine, ligustrazine+berberine, or clopidogrel for 2 weeks. When the treatment completed, CME was induced by injection of sodium laurate into the left ventricular, while obstructing the ascending aorta. All rats were intubated for hemodynamic measurements. Blood samples were collected for biochemical analyses, flow cytometry, and ELISAs. Heart tissues were isolated for histopathology and subsequent protein analyses. Results: Pretreatment with the combination of ligustrazine (27 mg·kg -1 ·d -1 ) and berberine (90 mg·kg -1 ·d -1 ) significantly improved cardiac function, and decreased myocardial necrosis, inflammatory cell infiltration, microthrombosis and serum CK-MB levels in CME rats. In addition, this combination significantly decreased plasma ET-1 levels and von Willebrand factor, inhibited ADP-induced platelet activation, and reduced TNFα, IL-1β, ICAM-1 and RANTES levels in serum and heart tissues. The protective effects of this combination were more prominent than those of ligustrazine or berberine alone, but comparable to those of a positive control clopidogrel (6.75 mg·kg -1 ·d -1 ). Conclusion: The combination of ligustrazine and berberine significantly improved cardiac function in rat CME model via a mechanism involving antiplatelet and anti-inflammatory effects.

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Section: Introductionmentioning

confidence: 99%

Pretreatment with a combination of ligustrazine and berberine improves cardiac function in rats with coronary microembolization

Zhang

Guo

et al. 2016

Acta Pharmacol Sin

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“…Tetramethylpyrazine is an alkaloid and one of the active components of Chuanxiong, which exerts a wide range of cardiovascular protective effects ( Lin et al, 2022 ). For example, tetramethylpyrazine inhibits isoproterenol-induced cardiomyocyte hypertrophy in neonatal mice by decreasing the expression of CaN ( Ji et al, 2014 ). In a study of ApoE −/− mice fed a high-fat diet, Zhang et al showed that tetramethylpyrazine (45.05 mg/kg i. g. ) to improve dyslipidemia by down-regulating progesterone and ADIPOQ receptor 3 and inhibiting the SCAP/SREBP-1c signaling pathway ( Zhang et al, 2017 ).…”

Section: Discussionmentioning

confidence: 99%

Efficacy and safety of Qiangli Dingxuan tablet combined with amlodipine besylate for essential hypertension: a randomized, double-blind, placebo-controlled, parallel-group, multicenter trial

et al. 2023

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Background: Hypertension, a major cardiovascular risk factor, severely impacts patients’ quality of life. Qiangli Dingxuan tablet (QDT) is a formally approved Chinese patent medicine, which has been widely used as an adjunctive treatment for hypertension. This study aimed to investigate the antihypertensive efficacy and safety of QDT combined with amlodipine besylate in patients with essential hypertension.Methods: In this randomized, double-blind, placebo-controlled, parallel-group, multicenter trial conducted in China, patients diagnosed with grade 1 to 2 essential hypertension were randomly assigned in a 1:1 to the treatment of QDT or placebo for 12 weeks, alongside their ongoing treatment with amlodipine besylate. The primary outcome was the change in office blood pressure (BP) from baseline to 12 weeks. In addition, safety analysis included the assessment of vital signs and laboratory values.Results: At baseline, 269 patients were randomly assigned to the QDT group (n = 133) or the placebo group (n = 136), and there were no significant differences in baseline characteristics between the two groups. The primary outcome based on the full analysis set from baseline to 12 weeks showed that the mean difference in the change of office systolic BP reduction between the two groups was 6.86 mmHg (95%CI, 4.84 to 8.88, p < 0.0001), for office diastolic BP, the mean difference in the change of office diastolic BP reduction between the two groups was 4.64 mmHg (95%CI, 3.10 to 6.18, p < 0.0001). In addition, traditional Chinese medicine symptom scores were significantly decreased in the QDT group compared with the placebo group. No severe adverse events attributable to QDT were reported.Conclusion: The combination of QDT and amlodipine besylate demonstrates superior efficacy compared to amlodipine besylate monotherapy in the management of essential hypertension. QDT shows potential as an adjunctive treatment for essential hypertension. However, further rigorous clinical trials are warranted to validate these findings.Clinical Trial Registration: [https://clinicaltrials.gov/study/NCT05521282?cond=NCT05521282&rank=1]; Identifier: [NCT05521282]

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“…Ligustrazine (LZ), a bioactive component from the traditional Chinese medicine ligusticum, is primarily used in China as a vasodilator ( 1 ). In recent years, it has been reported that LZ inhibits tumor metastasis and improves the sensitivity of multidrug resistant tumor cells to chemotherapeutic agents ( 2 ).…”

Section: Introductionmentioning

confidence: 99%

Synthesis of folate-chitosan nanoparticles loaded with ligustrazine to target folate receptor positive cancer cells

Cheng

Shao

et al. 2017

Molecular Medicine Reports

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In addition to its vasodilatory effect, ligustrazine (LZ) improves the sensitivity of multidrug resistant cancer cells to chemotherapeutic agents. To enhance the specificity of LZ delivery to tumor cells/tissues, folate-chitosan nanoparticles (FA-CS-NPs) were synthesized by combination of folate ester with the amine group on chitosan to serve as a delivery vehicle for LZ (FA-CS-LZ-NPs). The structure of folate-chitosan and characteristics of FA-CS-LZ-NPs, including its size, encapsulation efficiency, loading capacity and release rates were analyzed. MCF-7 (folate receptor-positive) and A549 (folate receptor-negative) cells cultured with or without folate were treated with FA-CS-LZ-NPs, CS-LZ-NPs or LZ to determine cancer-targeting specificity of FA-CS-LZ-NPs. Fluorescence intensity of intracellular LZ was observed by laser scanning confocal microscopy, and concentration of intracellular LZ was detected by HPLC. The average size of FA-CS-LZ-NPs was 182.7±0.56 nm, and the encapsulation efficiency and loading capacity was 59.6±0.23 and 15.3±0.16% respectively. The cumulative release rate was about 95% at pH 5.0, which was higher than that at pH 7.4. There was higher intracellular LZ accumulation in MCF-7 than that in A549 cells and intracellular LZ concentration was not high when MCF-7 cells were cultured with folate. These results indicated that the targeting specificity of FA-CS-LZ-NPs was mediated by folate receptor. Therefore, the FA-CS-LZ-NPs may be a potential folate receptor-positive tumor cell targeting drug delivery system that could possibly overcome multidrug resistance during cancer therapy.

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Effects and Mechanism of Action of Ligustrazine on Isoprenaline-Induced Cardiomyocyte Hypertrophy

Cited by 7 publications

References 28 publications

Pretreatment with a combination of ligustrazine and berberine improves cardiac function in rats with coronary microembolization

Pretreatment with a combination of ligustrazine and berberine improves cardiac function in rats with coronary microembolization

Efficacy and safety of Qiangli Dingxuan tablet combined with amlodipine besylate for essential hypertension: a randomized, double-blind, placebo-controlled, parallel-group, multicenter trial

Synthesis of folate-chitosan nanoparticles loaded with ligustrazine to target folate receptor positive cancer cells

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