MOLECULES
·
2018
·Vol. 23
·期 7
·1650
·
IF 3.098
Jing Tan,Cuizhu Wang,Hailin Zhu,Baisong Zhou,Lingxin Xiong,Fang Wang,Pingya Li,Jinping Liu
Blood stasis syndrome (BSS) is one of the most common Chinese medicine patterns in coronary heart disease. Our previous work proved that Xueshuan Xinmaining Tablet (XXT) could treat blood stasis through regulating the expression of F13a1, Car1 and Tbxa2r. In the current study, the effect and mechanism of XXT on BSS was comprehensively and holistically investigated based on a metabolomics approach. Urine and plasma samples of 10 BBS rats treated with XXT (XT), 9 BSS model rats (BM) and 11 normal control (NC) rats were collected and then determined by UPLC-Q/TOP-MS. Multivariate analyses were applied to distinguish differentiate urinary and plasma metabolite patterns between three groups. Results showed that a clear separation of three groups was achieved. XT group was located between BM group and NC group, and showing a tendency of recovering to NC group, which was consistent with the results of hemorheological studies. Some significantly changed metabolites like cortexolone, 3α,21-dihydroxy-5β-pregnane-11,20-dione and 19S-hete and leukotriene A4, chiefly involved in steroid hormone biosynthesis, arachidonic acid metabolism and lipid metabolism, were found and identified to explain the mechanism. These potential markers and their corresponding pathways will help explain the mechanism of BSS and XXT treatment. This work also proves that metabolomics is effective in traditional Chinese medicinal research.Keywords:blood stasis syndrome;Xueshuan Xinmaining tablet;UPLC-Q/TOF-MS;rats;metabolomics
研究领域:
中医药学
·
代谢组学
·
生物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2025
·Vol. 39
·期 2
·e6060
·
IF 1.7
Chen Wang,Xueying Qin,Ying Wang,Weiping Wang,Shuai Sun,Hongsen Wang,Shiyu Li,Xiao Dai,Xianhong Zhu,Xun Gao,Kunming Qin,Qing Zhang
Choerospondias axillaris is a medicinal plant used for treating coronary heart disease (CHD) due to its broad spectrum of anti-inflammatory activities. Cyclooxygenase 2 (COX-2) and lipoxygenase 5 (5-LOX) were immobilized on magnetic nanoparticles for selective ligand-extraction of these two enzymes present in C. axillaris . Sixteen extracted components were identified and analyzed using ultraperformance liquid chromatography plus Q-Exactive Orbitrap tandem mass spectrometry (UHPLC-Q-ExactiveOrbitrap-MS/MS), including flavonoids Curcumin and Epicatechin. The metabolization of the aforementioned 16 components in rats with acute blood stasis indicated a solid pharmacodynamic foundation. This method offers an effective approach for conducting basic research on the enrichment, analysis, and efficacy evaluation of active components in complex natural products.
研究领域:
药理学
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分析化学
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天然产物研究
✓ 已验证
DOI
PubMed
高影响因子
PHYTOCHEMICAL ANALYSIS
·
2025
·
IF 2.6
Yv Wang,Zhewen Zhang,Liu Yang,Pei Ye,Yv Ye,Xiaoning Li,Weifeng Du
Introduction A major limitation in current Traditional Chinese Medicine (TCM) research lies in its overreliance on single-factor analyses of chemical composition or pharmacodynamics, or simplistic combined models. While these approaches partially elucidate TCM characteristics, they fail to comprehensively capture its holistic complexity and inherent quality. Objectives The three-dimensional comprehensive evaluation method of “morphology-composition-efficacy (MCE)” was creatively introduced in this study, and the quality of four different varieties of Curcumae Radix was deeply and meticulously studied. Materials and Methods Curcumae Radix from different sources was collected, and its external morphology (volume and weight, color and smell), internal composition (extract, fingerprint and literature knowledge network diagram) and drug effect (efficacy of zebrafish on improving qi stagnation and blood stasis) were analyzed. The differences in composition and morphology of four kinds of Curcumae Radix were studied by HPLC fingerprint, chromaticity identification model, and BP-ANN classification model. Secondly, through the experiment of zebrafish “qi stagnation and blood stasis” model, the improvement effect of four kinds of turmeric on “qi stagnation and blood stasis” was explored. Finally, the relationship between the three dimensions of MCE of Curcumae Radix was discussed through Pearson analysis. Results The pharmacodynamic experiment of zebrafish confirmed that all four kinds of Curcumae Radix showed the activity of treating “qi stagnation and blood stasis” and Curcuma phaeocaulis Val. (LSYJ) had the best effect comprehensively. And through Pearson analysis, it can be concluded that the smaller the external volume and weight of Curcumae Radix, the stronger the characteristic odor (W5S, W1W, and W2W), the closer the powder color is to red and yellow, the higher the internal extract (JCW) content of Curcumae Radix , the higher the contents of germacrone (JMT), furanodiene (FNEX), and β-elemene (β-LXX), and the better the efficacy of improving the disease of “qi stagnation and blood stasis,” among which JMT is the key drug component. Conclusion The research demonstrates the value of a three-dimensional evaluation system for TCM quality assessment, providing insights into the relationship between morphology, composition, and efficacy. It offers a new perspective for quality control and evaluation of Curcumae Radix and provides a scientific basis for the clinical treatment of “qi stagnation and blood stasis” related diseases.
研究领域:
中药学
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药理学
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分析化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PHYTOMEDICINE
·
2024
·
IF 6.7
Wenjia CHEN,Chu ZHANG,Mingzhu XU,Tao LI,Xin LI,Peihao LI,Xun GONG,Yang QU,Chunling ZHOU,Xia MAO,Na LIN,Wei LIU,Quan JIANG,Haiyu XU,Yanqiong ZHANG
Background : Specific treatment for rheumatoid arthritis (RA) is still an unmet need. Yu-Xue-Bi (YXB) capsule effectively treats RA with blood stasis syndrome (BS). However, its mechanism remains unclear. Purpose : Exploring and elucidating the therapeutic effect and pharmacological mechanism of YXB capsule in treating RA. Methods : This study identified differentially expressed genes (DEGs) in patients with RA and BS compared to healthy controls using clinical transcriptomics data. Clinical symptoms of RA and BS, and the related genes were collected from the SoFDA and HPO databases. Candidate bioactive constituents in YXB were identified via UPLC-QTOF/MS and evaluated using ADMET rules. Putative targets were predicted, and a network linking disease-related DEGs and drug targets was constructed. Key targets were screened utilizing random walk-with-restart (RWR) algorithms and verified through experiments using rat models of collagen-induced arthritis with BS (CIA-BS model) in vivo . Results : We found 1220 DEGs along with 976 clinical symptom-related genes, as RA with BS-related genes. Chemical profiling identified 193 YXB constituents, with 98 meeting optimal ADMET criteria. We predicted 459 putative targets for these constituents. Network calculations screened 209 key targets, 129 RA with BS-related genes and 92 YXB targets involved in immune inflammation, blood stagnation, and hyperalgesia imbalance. Notably, the SUCNR1/HIF-1α/TRPV1 axis was enriched by YXB targets against RA with BS. Experimentally, YXB inhibited inflamed joint deterioration, including synovial inflammation, cartilage damage and bone erosion, relieving mechanical and cold allodynia hyperglasia. It reversed hemorrheology and vascular function in CIA-BS rats, restoring SDHB and eNOS expression, preventing SDHA, SUCNR1 and HIF-1α activation, reducing SUCN, TNF-1α and IL-1β production, and TRPV1 and TRPA1 expression. Conclusion : Our data support YXB's therapeutic effects on aggressive RA-BS by modulating the SUCNR1/HIF-1α/TRPV1 axis.
研究领域:
药理学
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分子生物学
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风湿病学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
·
2017
·
IF 2.981
Yi Chen,Pei-Dong Chen,Bei-Hua Bao,Ming-Qiu Shan,Kai-Cheng Zhang,Fang-Fang Cheng,Yu-Dan Cao,Li Zhang,An-Wei Ding
Ethnopharmacological relevance Rubia cordifolia is a common traditional Chinese medicine that promotes blood circulation and eliminates blood stasis , and has been used to cure diseases related to blood stasis syndrome (BSS) clinically for many years. It has been previously demonstrated that anti-thrombosis and pro-angiogenesis can improve BSS. However, the anti-thrombotic and pro-angiogenic activities of Rubia cordifolia have not been well investigated. Aim of study To determine the potential anti-thrombotic and pro-angiogenic activities of Rubia cordifolia and to elucidate the underlying mechanisms. In addition, the major chemical constituents of Rubia cordifolia extract (QC) were qualitatively analysed by UPLC-Q-TOF/MS to explore the association between pharmacological activity and chemical constituents. Material and methods The QC samples were composed of a 95% ethanol extract and an aqueous extract following extraction using 95% ethanol. UPLC-Q-TOF/MS was used to analyse the major chemical constituents of QC. For the anti-thrombotic experiment of QC, a phenylhydrazine (PHZ)-induced AB strain zebrafish thrombosis model was used. The zebrafish larvae were stained using O-dianisidine, and the heart and caudal vein of the zebrafish were observed and imaged with a fluorescence microscope. The staining intensity of erythrocytes in the heart (SI) of each group and the morphology of thrombus in the caudal vein were used to assess the anti-thrombotic effect of QC. For the pro-angiogenic assay of QC, the intersegmental blood vessel (ISV) insufficiency model of Tg(fli-1: EGFP)y1 transgenic zebrafish (Flik zebrafish), which was induced by the VEGF receptor tyrosine kinase inhibitor II (VRI), was used. The morphology of the intact ISVs and defective ISVs was observed to evaluate the pro-angiogenic activity of QC. The mechanism involved in promoting angiogenesis was studied with real-time PCR. Results A total of 12 components in QC were identified based on standard compounds and references, including nine anthraquinones and three naphthoquinones . After treatment with QC, the PHZ-induced thrombosis in AB strain zebrafish larvae decreased to a certain degree, which we believe was related to its dosages, and the therapeutic effect within the 50–200 µg/mL QC treatment groups was especially prominent (P < 0.01, P < 0.001) compared to that in the PHZ model group. Similarly, QC also recovered the loss of the ISVs, which was induced by VRI in Flik zebrafish larvae, which have a certain dose-effect relationship. The pro-angiogenic activity of QC was also conspicuous (P < 0.01, P < 0.001) compared to that of the VRI model group. The following real-time PCR assay proved that QC significantly restored the VRI-induced downregulation of vWF, VEGF-A, kdrl, and flt-1 in Flik zebrafish (P < 0.05, P < 0.01, P < 0.001). Conclusions A total of 12 compounds from QC were analysed by UPLC-Q-TOF/MS. The data of the pharmacological experiments demonstrated that QC presented anti-thrombotic and pro-angiogenic activities in zebrafish, and the principal active components were likely anthraquinones and naphthoquinones. Thus, the current study provided a theoretical basis for the clinical use of Rubia cordifolia as a traditional Chinese medicine in promoting blood circulation and eliminating stasis.
研究领域:
药理学
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民族药理学
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斑马鱼生物学
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传统中药
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化学分析
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Yongfang Sun,Jinmei Xie,Canzheng Wang,Shaoxue Qin,Kun Ren,Dongmei Wang,Yingni Pan,Shumeng Ren,Xiaoqiu Liu
Curcumae wenyujin Rhizoma (CWR) is extensively implemented in clinical practice for treating primary dysmenorrhea (PD) resulting from qi stagnation and blood stasis. However, the development of CWR-derived polysaccharides remains poorly investigated. In this study, the polysaccharide CWP-3 was isolated from CWR, and structurally characterized through FT-IR, HPLC, GC–MS, and NMR, which identified it as an RG-I-type pectin polysaccharide with a molecular weight of 423.6 kDa. CWP-3 consists of the monosaccharides Rha, GalA, Gal, and Ara (25.7: 28.6:42.8:2.9). The main backbone consisted of alternating 1,2-linked Rha p and 1,4-linked GalA p residues, with Gal and Ara forming the side chains, respectively. SEM revealed a porous, sheet-like morphology, while Congo Red staining and AFM analyses confirmed a triple helix structure with a height of 3.37 nm, and TG-DSC analysis indicated good thermal stability. In a mouse model of PD, 160 mg/kg CWP-3 reduced writhing by 70.3 %, prolonged coagulation time by 37.5 %, restored uterine and hepatic indices, and decreased AST, ALT, D2D, TXB2, IL-6, IL-1β, and TNF-α, while normalizing PGF₂α/PGE₂ levels. These results indicate that CWP-3 exerts blood-activating and analgesic effects through cytokine-mediated COX-2 suppression, suggesting its potential as a therapeutic candidate for PD with qi stagnation and blood stasis.
研究领域:
药理学
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生物化学
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药物化学
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妇科学
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结构生物学
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多糖研究
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Frontiers in Pharmacology
·
2021
·
IF 5.811
Li Jun,Liu Hao,Yang Zhenzhong,Yu Qingqing,Zhao Lu,Wang Yi
Thrombosis is a key pathological event in cardiovascular diseases, and is also the most important targeting process for their clinical management. New drug development in thrombosis treatment is still in great demand. According to the traditional Chinese medicine (TCM) theory, thrombosis belongs to the syndrome of blood stasis. Salvia miltiorrhiza Bunge and Ligusticum striatum DC. are two common TCM herbs with long-term documented function in promoting blood circulation and inhibiting thrombosis, especially when used together. Guanxinning Tablet, a modern Chinese drug which contains extracts of the two herbs, also showed strong therapeutic effects in coronary heart disease. However, the pharmacological mechanism is still lacking for the compatibility of the two herbs. Here, through zebrafish-based in vivo fluorescence screening, we demonstrated the synergistic effects between S. miltiorrhiza Bunge and L. striatum DC. in regulating endogenous thrombosis. Moreover, combined with high-resolution mass spectrometry, the main compounds of the botanical drugs were analyzed and screened in our model system. Interestingly, cryptotanshinone and senkyunolide I, two representative compounds, respectively derived from the two herbs, also showed synergistic antithrombotic effects. Further analysis suggested that they may regulate thrombi formation at different levels via multiple signaling pathways, including oxidative stress, platelet activation and coagulation cascade. Taken together, our findings provided solid biological supports toward the drug compatibility theory of TCM, and suggested cryptotanshinone and senkyunolide I as promising drug candidates in thrombosis management.
研究领域:
药理学
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心血管疾病
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传统中药
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斑马鱼模型
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药物开发
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
·
2023
·
IF 5.4
Yuting Huang,Qianru Chen,Weijie Pan,Ying Zhang,Jiasheng Li,Xingyang Xue,Xinhe lei,Shumei Wang,Jiang Meng
Ethnopharmacological relevance As a traditional Chinese medicine , raw Moutan Cortex (RMC) has been used in clinical practice for thousands of years. However, its blood-cooling and blood-activating medicinal effects as well as the underlying mechanisms have not been preliminarily verified until recent years. Aim of the study Our group's previous network pharmacological studies suggested that RMC might exert its blood-activating and anti-inflammatory effects by modulating the coagulation-inflammation cascade pathway. Therefore, the present study aimed to further investigate the mechanisms relevant to the blood-activating and anti-inflammatory effects of RMC so as to provide more robust data supporting its clinical application. Materials and methods The inflammation and coagulation models of human umbilical vein endothelial cells (HUVECs) were induced by TNF-α; The rat models with blood-heat and blood-stasis syndrome (BHS) were constructed by ice-water bath with a combined use of epinephrine hydrochloride and dried yeast; The thrombus models of zebrafish were induced by arachidonic acid , and the inflammation models were established using LPS and CuSO 4 . The regulatory effects of RMC on the key targets in the pathway of the coagulation-inflammation cascade were investigated by combining ELISA , RT-PCR, and western blot techniques in an attempt to provide multiple validations concerning RMC's pharmacological efficacy and mechanism associated with cooling blood and activating blood circulation. Result The findings from the pharmacodynamic research demonstrated that RMC could inhibit the coagulation and inflammation process of HUVECs. Besides, it lowered the anal temperature and whole blood viscosity in BHS rats in addition to a prolongation of their prothrombin time (PT), thrombin time (TT), and activated partial thromboplastin time (APTT). Successfully constrained thrombotic area and reduced inflammatory cell counts were also observed in zebrafish models. Meanwhile, ELISA, RT-PCR and WB showed that RMC were capable of inhibiting the factors related to coagulation-MARK inflammation pathway—FⅡ, TF, FⅦ, FⅧ, FⅩ, and PAI, as well as down-regulating the expression of IL-6, COX-2, iNOS, TNF-α, ERK, JNK and p38. Conclusion RMC exerts blood-activating and anti-inflammatory effects through regulating the target genes of the coagulation-MARK inflammation cascade pathway.
研究领域:
民族药理学
·
药理学
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中药
·
细胞生物学
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动物模型
✓ 已验证
DOI
PubMed
高影响因子
MOLECULES
·
2019
·Vol. 24
·期 13
·2380
·
IF 3.06
Dongshuai Shen,Ning Ma,Yajun Yang,Xiwang Liu,Zhe Qin,Shihong Li,Zenghua Jiao,Xiaojun Kong,Jianyong Li
Aspirin eugenol ester (AEE) is a novel compound that is formed from the esterification of aspirin (acetylsalicylic acid (ASA)) and eugenol. This study aimed to investigate the effects of AEE on blood stasis in rats and to characterize the underlying mechanisms using a plasma metabolomic study. The results indicate that AEE and ASA could modulate whole blood viscosity (WBV), plasma viscosity (PV), blood coagulation parameters, platelet count, platelet aggregation, lactate dehydrogenase (LDH), creatinine (CR) and the levels of thromboxane A2 (TXA2) and 6-keto prostaglandin F1α (6-keto-PGF1α). The metabolic profiles of the plasma samples from all groups were clearly separated in the score plots. Nineteen potential metabolites were selected and identified, and disordered levels of these metabolites could be regulated by AEE and ASA. Pathway analysis showed that the mechanism of action of AEE on blood stasis might be principally related to the metabolism of amino acid, fatty acid, energy and glycerophospholipid. The above results indicate that AEE protected the rats against blood stasis, and that this effect might have been caused by the anticoagulation activity of AEE and its abilities to maintain a balance between TXA2and PGI2, reduce blood viscosity, inhibit platelet aggregation and normalize the plasma metabolic profile.Keywords:blood stasis;AEE;aspirin;metabolomics;UPLC-Q-TOF/MS
研究领域:
药理学
·
代谢组学
·
药物化学
·
血液学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）