Ligustrazine improves blood circulation by suppressing Platelet activation in a rat model of allergic asthma

Wang, Yajuan; Zhu, Haijing; Tong, Jiabing; Li, Zegeng

doi:10.1016/j.etap.2016.06.016

Cited by 22 publications

(16 citation statements)

References 23 publications

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“…Our results of experimental in vitro ADP-induced PRP aggregation assay confirmed the anti-platelet activity of ligustrazine, the main active component of ChuanXiong. The IC50 value of ligustrazine in inhibiting platelet aggregation was determined to be 388.9 ± 21.69 μg/mL, which was consistent with previous reports (Shao et al, 2015 ; Wang et al, 2016 ). While, as shown in the results of the present study, the IC50 values of ligustrazine and other herbal components were rather high which suggested that the anti-platelet activities were weak or only moderate.…”

Section: Discussionsupporting

confidence: 90%

Application of Feedback System Control Optimization Technique in Combined Use of Dual Antiplatelet Therapy and Herbal Medicines

Liu

Feng

et al. 2018

Front. Physiol.

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Aim: Combined use of herbal medicines in patients underwent dual antiplatelet therapy (DAPT) might cause bleeding or thrombosis because herbal medicines with anti-platelet activities may exhibit interactions with DAPT. In this study, we tried to use a feedback system control (FSC) optimization technique to optimize dose strategy and clarify possible interactions in combined use of DAPT and herbal medicines.Methods: Herbal medicines with reported anti-platelet activities were selected by searching related references in Pubmed. Experimental anti-platelet activities of representative compounds originated from these herbal medicines were investigated using in vitro assay, namely ADP-induced aggregation of rat platelet-rich-plasma. FSC scheme hybridized artificial intelligence calculation and bench experiments to iteratively optimize 4-drug combination and 2-drug combination from these drug candidates.Results: Totally 68 herbal medicines were reported to have anti-platelet activities. In the present study, 7 representative compounds from these herbal medicines were selected to study combinatorial drug optimization together with DAPT, i.e., aspirin and ticagrelor. FSC technique first down-selected 9 drug candidates to the most significant 5 drugs. Then, FSC further secured 4 drugs in the optimal combination, including aspirin, ticagrelor, ferulic acid from DangGui, and forskolin from MaoHouQiaoRuiHua. Finally, FSC quantitatively estimated the possible interactions between aspirin:ticagrelor, aspirin:ferulic acid, ticagrelor:forskolin, and ferulic acid:forskolin. The estimation was further verified by experimentally determined Combination Index (CI) values.Conclusion: Results of the present study suggested that FSC optimization technique could be used in optimization of anti-platelet drug combinations and might be helpful in designing personal anti-platelet therapy strategy. Furthermore, FSC analysis could also identify interactions between different drugs which might provide useful information for research of signal cascades in platelet.

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Section: Discussionsupporting

confidence: 90%

Application of Feedback System Control Optimization Technique in Combined Use of Dual Antiplatelet Therapy and Herbal Medicines

Liu

Feng

et al. 2018

Front. Physiol.

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“…Over the past thousands of years, Chinese herbal medicine has been used to treat allergic disease, and the effect of herbal medicine has attracted increasing attention (Li et al, 2004; Lu et al, 2016; Wang et al, 2016; Yu et al, 2017; Liu et al, 2018; Yan et al, 2018). Paeoniflorin is one of the major active ingredients in Chinese peony, which is also called Paeonia lactiflora.…”

Section: Introductionmentioning

confidence: 99%

Integration of Metabolomics and Transcriptomics Reveals the Therapeutic Mechanism Underlying Paeoniflorin for the Treatment of Allergic Asthma

et al. 2019

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Objectives: Asthma is a chronic airway inflammatory disease, which is characterized by airway remodeling, hyperreactivity and shortness of breath. Paeoniflorin is one of the major active ingredients in Chinese peony, which exerts anti-inflammatory and immune-regulatory effects in multiple diseases. However, it remains unclear whether paeoniflorin treatment can suppress allergic asthma.Methods: In this study, we evaluated the effect of paeoniflorin on lung function and airway inflammation in asthmatic mice. These asthmatic Balb/c mice were first sensitized and constructed through ovalbumin (OVA) motivation. Subsequently, we determined the mechanism of action of paeoniflorin in treating allergic asthma through integrated transcriptomic and metabolomic data sets.Results: Our results demonstrated that many genes and metabolites were regulated in the paeoniflorin-treated mice. Moreover, the potential target proteins of paeoniflorin played important roles in fatty acid metabolism, inflammatory response, oxidative stress and local adhesion.Conclusion: Paeoniflorin has a beneficial effect on asthma, which may be achieved through regulating fatty acid metabolism, inflammatory response and the adhesion pathway at system level.

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“…Rhizoma chuanxiong is a famous traditional Chinese medicine whose pharmacological activity is described as positive hemodynamic effect [ 5 ]. Ligustrazine (tetramethylpyrazine, TMP) and ferulic acid as well as several other components were identified as the active compounds responsible for the holistic treatment effect of R. chuanxiong [ 6 , 7 , 8 , 9 , 10 , 11 ]. Pyragrel ( Figure 1 ) is a synthetic compound derived from the molecular combination of ligustrazine and ferulic acid.…”

Section: Introductionmentioning

confidence: 99%

Profiling and Preparation of Metabolites from Pyragrel in Human Urine by Online Solid-Phase Extraction Coupled with High Performance Liquid Chromatography Tandem Mass Spectrometry Followed by a Macroporous Resin-Based Purification Approach

et al. 2017

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Pyragrel, a new anticoagulant drug, is derived from the molecular combination of ligustrazine and ferulic acid. Pyragrel showed significant inhibitory activity against platelet aggregation induced by adenosine diphosphate (ADP), and had been approved for a phase I clinical trial by CFDA. To characterize the metabolites of Pyragrel in human urine after intravenous administration, a reliable online solid-phase extraction couple with high performance liquid chromatography tandem mass spectrometry (online SPE-HPLC-MSn) method was conceived and applied. Five metabolites were detected and tentatively identified, which suggested that the major metabolic pathways of Pyragrel in human were double-bond reduction, double-bond oxidation, and then followed by glucuronide conjugation. Two main metabolites were then prepared using β-glucuronide hydrolysis and macroporous resin purification approach followed by preparative high-performance liquid chromatography (PHPLC) method, with their structures confirmed on the basis of nuclear magnetic resonance (NMR) data. This study provided information for the further study of the metabolism and excretion of Pyragrel.

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Ligustrazine improves blood circulation by suppressing Platelet activation in a rat model of allergic asthma

Cited by 22 publications

References 23 publications

Application of Feedback System Control Optimization Technique in Combined Use of Dual Antiplatelet Therapy and Herbal Medicines

Application of Feedback System Control Optimization Technique in Combined Use of Dual Antiplatelet Therapy and Herbal Medicines

Integration of Metabolomics and Transcriptomics Reveals the Therapeutic Mechanism Underlying Paeoniflorin for the Treatment of Allergic Asthma

Profiling and Preparation of Metabolites from Pyragrel in Human Urine by Online Solid-Phase Extraction Coupled with High Performance Liquid Chromatography Tandem Mass Spectrometry Followed by a Macroporous Resin-Based Purification Approach

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