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1.
Zhongguo Zhong Yao Za Zhi ; (24): 3294-3307, 2023.
Artigo em Chinês | WPRIM | ID: wpr-981467

RESUMO

A strategy combining collision cross section(CCS) prediction and quantitative structure-retention relationship(QSRR) model for quinoline and isoquinoline alkaloids was established based on UHPLC-IM-Q-TOF-MS and applied to Phellodendri Chinensis Cortex and Phellodendri Amurensis Cortex. The strategy included the following three steps.(1) The molecular features were extracted by the "find features" algorithm.(2) The potential quinoline and isoquinoline alkaloids were screened by filtering the original characteristic ions extracted from Phellodendri Chinensis Cortex and Phellodendri Amurensis Cortex by the established CCS vs m/z prediction interval.(3) According to the retention time of candidate compounds predicted by QSRR model, the chemical constituents were identified in combination with the characteristic fragment ions and pyrolysis law of secondary mass spectrometry. With the strategy, a total of 80 compounds were predicted, and 15 were identified accurately. The strategy is effective for the identification of small analogs of traditional Chinese medicine.


Assuntos
Cromatografia Líquida de Alta Pressão , Algoritmos , Alcaloides , Isoquinolinas , Quinolinas
2.
Chin. j. integr. med ; Chin. j. integr. med;(12): 1033-1044, 2023.
Artigo em Inglês | WPRIM | ID: wpr-1010322

RESUMO

Saposhnikovia divaricata (Turcz.) Schischk (S. divaricata, Fangfeng) is a herb in the Apiaceae family, and its root has been used since the Western Han Dynasty (202 B.C.). Chromones and coumarins are the pharmacologically active substances in S. divaricata. Modern phytochemical and pharmacological studies have demonstrated their antipyretic, analgesic, anti-inflammatory, antioxidant, anti-tumor, and anticoagulant activities. Technological and analytical strategy theory advancements have yielded novel results; however, most investigations have been limited to the main active substances-chromones and coumarins. Hence, we reviewed studies related to the chemical composition and pharmacological activity of S. divaricata, analyzed the developing trends and challenges, and proposed that research should focus on components' synergistic effects. We also suggested that, the structure-effect relationship should be prioritized in advanced research.


Assuntos
Medicamentos de Ervas Chinesas/farmacologia , Cumarínicos/farmacologia , Apiaceae/química , Cromonas
3.
Acta Pharmaceutica Sinica B ; (6): 3802-3816, 2023.
Artigo em Inglês | WPRIM | ID: wpr-1011157

RESUMO

The chemical complexity of traditional Chinese medicines (TCMs) makes the active and functional annotation of natural compounds challenging. Herein, we developed the TCMs-Compounds Functional Annotation platform (TCMs-CFA) for large-scale predicting active compounds with potential mechanisms from TCM complex system, without isolating and activity testing every single compound one by one. The platform was established based on the integration of TCMs knowledge base, chemome profiling, and high-content imaging. It mainly included: (1) selection of herbal drugs of target based on TCMs knowledge base; (2) chemome profiling of TCMs extract library by LC‒MS; (3) cytological profiling of TCMs extract library by high-content cell-based imaging; (4) active compounds discovery by combining each mass signal and multi-parametric cell phenotypes; (5) construction of functional annotation map for predicting the potential mechanisms of lead compounds. In this stud TCMs with myocardial protection were applied as a case study, and validated for the feasibility and utility of the platform. Seven frequently used herbal drugs (Ginseng, etc.) were screened from 100,000 TCMs formulas for myocardial protection and subsequently prepared as a library of 700 extracts. By using TCMs-CFA platform, 81 lead compounds, including 10 novel bioactive ones, were quickly identified by correlating 8089 mass signals with 170,100 cytological parameters from an extract library. The TCMs-CFA platform described a new evidence-led tool for the rapid discovery process by data mining strategies, which is valuable for novel lead compounds from TCMs. All computations are done through Python and are publicly available on GitHub.

4.
Artigo em Inglês | WPRIM | ID: wpr-776899

RESUMO

In the present study, two new acetylene conjugate compounds, dibutyl (2Z, 6Z)-octa-2, 6-dien-4-yne dioate (1), and dibutyl (2E, 6E)- octa-2, 6-dien-4-yne dioate (2), were isolated from the dry stem leaves of Viscum album, along with nine known compounds (3 - 11). Their structures were confirmed on the basis of spectroscopic data. Compounds 1 and 8 showed antioxidant activity against xanthine oxidase (XOD) and 1,1-diphenyl-2-picrylhydrazyl radical 2,2-diphenyl-1-(2,4,6-trinitrophenyl) hydroxyl (DPPH), with the IC of 1.22 and 1.33 μmol·L, and the SC of 4.34 and 8.22 μmol·L, respectively.


Assuntos
Acetileno , Química , Antioxidantes , Química , Farmacologia , Compostos de Bifenilo , Química , Estrutura Molecular , Picratos , Química , Extratos Vegetais , Química , Farmacologia , Folhas de Planta , Química , Viscum album , Química , Xantina Oxidase , Química
5.
Zhongguo Zhong Yao Za Zhi ; (24): 1760-1766, 2019.
Artigo em Chinês | WPRIM | ID: wpr-773170

RESUMO

Lipids have been documented to play comprehensive and significant role in many biological processes. As a branch of metabolomics,lipidomics research mainly involves the analysis of the variation of lipid metabolism profiles under different physiologic,pathologic conditions or drug intervention,the discovery of key lipid biomarkers of a disease in lipid metabolic networks,and the study of the mechanism of action of lipid metabolic regulation during disease onset and progression,and drug treatment. Traditional Chinese medicines( TCMs)are characterized with integrated effects by multi-components,multi-targets and integrated effects. It is urgent to develop methods suitable for the study of complex TCMs to reveal the active constituents and integrated mechanism of action. Systems biology such as lipidomics provides valuable strategy and approach to illustrate the complex mechanisms of TCMs. In this paper,in order to provide technical references for TCMs,we have reviewed the analytical techniques applied in lipidomics and the applications of lipidomics in TCMs researches.


Assuntos
Biomarcadores , Metabolismo dos Lipídeos , Medicina Tradicional Chinesa , Metabolômica , Métodos
6.
Artigo em Inglês | WPRIM | ID: wpr-773611

RESUMO

Guizhi Fuling capsule (GFC), a traditional Chinese medicine (TCM) with effects of promoting blood circulation and dissipating blood stasis, has been widely used in the clinic. Because of the complex matrix and various chemical structure types, quality control of GFC remains great challenge. In the present study, an ultra performance liquid chromatography hybrid triple-quadrupole mass spectrometry (UPLC-QQQ MS) method with ultrafast positive/negative ionization switching was developed for simultaneous determination of 18 bioactive components in GFC, including methyl gallate, ethyl gallate, oxypaeoniflorin, benzoic acid, albiflorin, paeonolide, paeoniflorin, 1, 2, 3, 4, 6-pentagalloylglucose, mudanpioside C, benzoyloxypaeoniflorin, benzoylpaeoniflorin, pachymic acid, amygdalin, cinnamaldehyde, paeonol, cinnamic acid, 4-hydroxybenzoic acid, and gallic acid. Separation was performed on an Agilent Zorbax Extend-C18 column (2.1 mm × 50 mm, 1.8 μm), using a gradient elution with acetonitrile and water containing 0.1% formic acid. Cholic acid was selected as the internal standard. This newly developed method was fully validated for linearity, precision, accuracy, and stability, and then applied to quality assessment of GFC. Finally, the batch-to-batch reproducibility of GFC samples was evaluated by the cosine ration and Euclidean distance method, which showed high quality consistency. The results demonstrated that the developed method pro vided a reasonable and powerful manner for quality control of GFC.


Assuntos
Fracionamento Químico , Métodos , Ácido Cólico , Padrões de Referência , Cromatografia Líquida de Alta Pressão , Cromatografia Líquida , Medicamentos de Ervas Chinesas , Química , Controle de Qualidade , Padrões de Referência , Reprodutibilidade dos Testes , Espectrometria de Massas em Tandem
7.
Artigo em Inglês | WPRIM | ID: wpr-812400

RESUMO

Guizhi Fuling capsule (GFC), a traditional Chinese medicine (TCM) with effects of promoting blood circulation and dissipating blood stasis, has been widely used in the clinic. Because of the complex matrix and various chemical structure types, quality control of GFC remains great challenge. In the present study, an ultra performance liquid chromatography hybrid triple-quadrupole mass spectrometry (UPLC-QQQ MS) method with ultrafast positive/negative ionization switching was developed for simultaneous determination of 18 bioactive components in GFC, including methyl gallate, ethyl gallate, oxypaeoniflorin, benzoic acid, albiflorin, paeonolide, paeoniflorin, 1, 2, 3, 4, 6-pentagalloylglucose, mudanpioside C, benzoyloxypaeoniflorin, benzoylpaeoniflorin, pachymic acid, amygdalin, cinnamaldehyde, paeonol, cinnamic acid, 4-hydroxybenzoic acid, and gallic acid. Separation was performed on an Agilent Zorbax Extend-C18 column (2.1 mm × 50 mm, 1.8 μm), using a gradient elution with acetonitrile and water containing 0.1% formic acid. Cholic acid was selected as the internal standard. This newly developed method was fully validated for linearity, precision, accuracy, and stability, and then applied to quality assessment of GFC. Finally, the batch-to-batch reproducibility of GFC samples was evaluated by the cosine ration and Euclidean distance method, which showed high quality consistency. The results demonstrated that the developed method pro vided a reasonable and powerful manner for quality control of GFC.


Assuntos
Fracionamento Químico , Métodos , Ácido Cólico , Padrões de Referência , Cromatografia Líquida de Alta Pressão , Cromatografia Líquida , Medicamentos de Ervas Chinesas , Química , Controle de Qualidade , Padrões de Referência , Reprodutibilidade dos Testes , Espectrometria de Massas em Tandem
8.
Zhongguo Zhong Yao Za Zhi ; (24): 1901-1906, 2018.
Artigo em Chinês | WPRIM | ID: wpr-690696

RESUMO

The study aims to analyze the mechanisms of Hirudo in promoting blood circulation and removing blood stasis based on network pharmacology. A database of chemical components of Hirudo was established through literature retrieval. The targets were predicted by using the reverse pharmacophore matching method and screened according to the antithrombotic and anticoagulant drug targets approved by FDA in the DrugBank database. Then, the targets were analyzed by KEGG pathway analysis, the protein interactions were analyzed by using BioGrid database, and the active constituents-target-pathway network model of Hirudo was established to study the mechanisms of Hirudo in promoting blood circulation and removing blood stasis. This study collected 49 chemical components of Hirudo, including amino acid, polypeptide, fatty acid ester, alkaloid, glycosides, and steroid. Totally 376 targets were predicted, and 5 critical targets related to the effects of Hirudo in promoting blood circulation and removing blood stasis were screened, including fibrinogen gamma chain, plasminogen, prothrombin, Urokinase-type plasminogen activator and coagulation factor X. The potential regulatory pathways included complement and coagulation cascades, platelet activation, VEGF signaling pathway, focal adhesion. This study reflects the multi-component, multi-target and multi-pathway features of Hirudo, and provides a scientific basis for elucidating the mechanisms of action of Hirudo in promoting blood circulation and removing blood stasis, as well as a reference for the study of mechanisms of traditional Chinese medicine.

9.
Chin J Integr Med ; 23(9): 689-695, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-28861889

RESUMO

OBJECTIVE: To observe the effects of red yeast rice (RYR) on blood lipid levels, aortic atherosclerosis (AS), and plaque stability in apolipoprotein E gene knockout (ApoE-/-) mice. METHODS: Twenty-four ApoE-/- mice were fed with a high-fat diet starting from 6 weeks of age. Mice were randomized into three groups (n = 8 in each group): model group (ApoE-/- group), RYR group (ApoE-/- + RYR group), and simvastatin group (ApoE-/- + simvastatin group). Eight 6-week-old C57BL/6 mice were assigned as the control group and fed with a basic diet. After 36 weeks, plasma lipids and inflflammatory factors were measured. Aortic atherosclerotic lesions by microscope, scanning electron microscope and transmission electron microscope were observed. Plasma levels of interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) were measured with enzyme-linked immunosorbent assay. The level of high sensitivity C-reaction protein (Hs-CRP) was detected by the scattering immunoturbidimetric assay. Protein expression of matrix metalloproteinase-9 (MMP-9) and nuclear factor κB (NF-κB) in aorta were tested by immunohistochemistry. RESULTS: Compared with the model group, treatment with RYR significantly decreased the levels of total cholesterol, triglyceride, low-density lipoprotein cholesterol, lipoprotein (a), and apolipoprotein B100 in ApoE-/- mice (P<0.01). Compared with the model group, treatment with RYR decreased the levels of Hs-CRP, IL-6, and TNF-α (P<0.01). RYR also reduced the protein levels of NF-κB and MMP-9 of the aorta. CONCLUSIONS: RYR has the anti-atherosclerotic and stabilizing unstable plaque effects. The mechanism might be related to the inflflammatory signaling pathways.


Assuntos
Aterosclerose/tratamento farmacológico , Aterosclerose/prevenção & controle , Produtos Biológicos/uso terapêutico , Inflamação/tratamento farmacológico , Transdução de Sinais , Animais , Aorta/patologia , Aorta/ultraestrutura , Aterosclerose/sangue , Aterosclerose/complicações , Produtos Biológicos/farmacologia , Inflamação/sangue , Inflamação/complicações , Mediadores da Inflamação/metabolismo , Lipídeos/sangue , Masculino , Metaloproteinase 9 da Matriz/metabolismo , Camundongos Endogâmicos C57BL , NF-kappa B/metabolismo , Transdução de Sinais/efeitos dos fármacos
10.
Artigo em Inglês | WPRIM | ID: wpr-812101

RESUMO

Aristolochiae Fructus, a Chinese herbal medicine derived from the fruit of Aristolochia contorta Bge., contains nephrotoxic aristolochic acid analogues (AAAs). According to ancient medical texts, various medicinal parts of the fruit of A. contorta were ever used. In order to reveal which part could be safely and effectively used, it is necessary to analyze the chemical profiles of different medicinal parts. Herein we compared the chemical compositions and determined aristolochic acid I (AA-I) and aristolochic acid II (AA-II) in the four parts viz. outer pericarp, inner pericarp, septum, and seed. Ultra-high performance liquid chromatography equipped with quadrupole time-of-flight mass spectrometry (UHPLC-QTOF-MS) was applied for chemical profiling. Ultra-high performance liquid coupled with triple quadrupole mass spectrometry (UHPLC-QqQ-MS) was employed to quantify AA-I and AA-II in different parts. It was found that the chemical compositions of the four parts varied both qualitatively and quantitatively. A total of 10 AAAs, including 5 aristolochic acids and 5 aristolactams, together with 3 alkaloids, were unambiguously or tentatively identified by UHPLC-QTOF-MS. The quantitatively analytical results obtained by UHPLC-QqQ-MS showed that AA-I and AA-II exclusively accumulate in the seeds of A. contorta. These findings provide supporting data for the rational selection of medicinal parts.


Assuntos
Aristolochia , Química , Ácidos Aristolóquicos , Química , Cromatografia Líquida de Alta Pressão , Medicamentos de Ervas Chinesas , Química , Frutas , Química , Estrutura Molecular , Espectrometria de Massas em Tandem
11.
Artigo em Inglês | WPRIM | ID: wpr-812440

RESUMO

To characterize and identify multiple constituents in Danhong injection (DHI), a fast ultra-high performance liquid chromatography coupled to electrospray ionization quadrupole time-of-flight tandem mass spectrometry (UHPLC-ESI-QTOF/MS) method was established and validated in the present study. A total of 63 compounds, including 33 phenolic acids, 2 C-glycosyl quinochalcones, 6 flavonoid O-glycosides, 4 iridoid glycosides, 6 organic acids, 5 amino acids, and 3 nucleosides, were identified or tentatively characterized. In conclusion, the UHPLC-ESI-QTOF/MS method is useful and efficient for in-depth structural elucidation of chemical compounds in complex matrices of herbal medicines such as DHI.


Assuntos
Cromatografia Líquida de Alta Pressão , Métodos , Medicamentos de Ervas Chinesas , Química , Espectrometria de Massas por Ionização por Electrospray , Métodos , Espectrometria de Massas em Tandem , Métodos
12.
Artigo em Chinês | WPRIM | ID: wpr-671256

RESUMO

Traditional Chinese medicines (TCM) is one of the most important sources of new drugs.The rapid development of modern science and technology has brought new opportunities for TCM.Admittedly,new academic theory is getting into a golden period of innovation.Key technologies that enbody TCM features and adapt to modern drug-screening requirements are urgently needed.After five years' endeavor,the authors' group has made great progress in the new theories and methodologies for the discovery of bioactive compounds from TCM.In this review,a total of five key technologies:library-bioactivity-structure integration,biological and chemical fishing technology,ligand-and receptor-based virtual screening,profile-bioactivity relationship and the technology for discovering bioactive equivalent combinatorial components (BECCs),were introduced.In the text,several valuable demonstrations over the TCM-based drug discovery were provided,for uncovering the scientific basis of TCM and accelerating the process of TCM modernization.

13.
Zhongguo Zhong Yao Za Zhi ; 39(6): 1115-9, 2014 Mar.
Artigo em Chinês | MEDLINE | ID: mdl-24956862

RESUMO

OBJECTIVE: To observe the effect of detoxifying and blood circulation activating Chinese herb extraction of polygonum cuspidatum and hawthorn on carotid intima-media thickness (IMT), plaque integral and plaque stability related serum indexes of patients with carotid atherosclerosis. METHOD: Sixty and four cases of carotid artery atherosclerosis patients were assigned randomly to 2 groups: detoxifying and blood circulation activating treatment group (treatment group, 32 cases) and control group (32 cases). Patients in treatment group were treated with capsules of extraction of polygonum cuspidatum and hawthorn, 1 pill po, bid (dosage of administration: polygonum cuspidatum extraction 5.33 mg x kg(-1) x d(-1), hawthorn extraction 5.0 mg x kg(-1) x d(-1)); patients in control group were treated with lovastatin 20 mg po, qd (dosage of administration: 0.33 mg x kg(-1) x d(-1)). The course of treatment was six months. To observe changes of IMT, plaque integral, and detect the level of plaque stability related serum indexes such as Hs-CRP, MMP-1 and TIMP-1. RESULT: After 6 months of treatment, in control group one patient quit the clinical trial because of liver dysfunction and one patient was rejected because of having not followed the therapeutic regimen. 32 cases in treatment group and 30 cases in control group were analyzed. The results showed that IMT and plaque integral of treatment group decreased significantly after the treatment (P < 0.05, P < 0.01), and there was no significant difference compared with control grope. Serum Hs-CRP, MMP-1 and MMP-1/TIMP-1 decreased after the treatment (P < 0.05, P < 0.01), and the treatment group was superior to control group in decreasing serum Hs-CRP (P < 0.05). CONCLUSION: Detoxifying and blood circulation activating Chinese herb extraction of polygonum cuspidatum and hawthorn has good effect of anti-atherosclerosis and promoting plaque stability. Its mechanism might be related with anti-inflammation and inhibiting degradation of extracellular matrix, and deserves further studies.


Assuntos
Doenças das Artérias Carótidas/tratamento farmacológico , Crataegus/química , Medicamentos de Ervas Chinesas/farmacologia , Fallopia japonica/química , Proteína C-Reativa/metabolismo , Doenças das Artérias Carótidas/sangue , Medicamentos de Ervas Chinesas/efeitos adversos , Medicamentos de Ervas Chinesas/uso terapêutico , Feminino , Humanos , Masculino , Metaloproteinase 1 da Matriz/sangue , Pessoa de Meia-Idade , Segurança , Inibidor Tecidual de Metaloproteinase-1/sangue
14.
Zhongguo Zhong Yao Za Zhi ; (24): 2305-2310, 2014.
Artigo em Chinês | WPRIM | ID: wpr-330301

RESUMO

This study is to determine six chlorogenic acids (chlorogenic acid, 5-O-caffeoylquinic acid, 4-O-caffeoylquinic acid, 3,4-di-O-caffeoylquinic acid, 3,5-di-O-caffeoylquinic acid and 4,5-di-O-caffeoylquinic acid) by quantitative analysis of multi-components with a single marker (QAMS). Chlorogeinc acid was used as internal reference to calculate the relative correction factors (RCF) of five compounds. Then the ruggedness of relative correction factors was tested on different instruments and columns. Meanwhile, a total of 4 batches of Lonicerae Flos and 20 batches of Lonicerae Flos extract with five different processing procedures were analyzed by external standard method (ESM) and QAMS, respectively. The ruggedness of relative correction factors was good. And the analytical results calculated by ESM and QAMS showed no difference. The quantitative method established was suitable for the quality evaluation of Lonicerae Flos extract.


Assuntos
Biomarcadores , Ácido Clorogênico , Cromatografia Líquida de Alta Pressão , Medicamentos de Ervas Chinesas , Flores , Química , Lonicera , Química
15.
Zhongguo Zhong Yao Za Zhi ; (24): 1115-1119, 2014.
Artigo em Chinês | WPRIM | ID: wpr-321355

RESUMO

<p><b>OBJECTIVE</b>To observe the effect of detoxifying and blood circulation activating Chinese herb extraction of polygonum cuspidatum and hawthorn on carotid intima-media thickness (IMT), plaque integral and plaque stability related serum indexes of patients with carotid atherosclerosis.</p><p><b>METHOD</b>Sixty and four cases of carotid artery atherosclerosis patients were assigned randomly to 2 groups: detoxifying and blood circulation activating treatment group (treatment group, 32 cases) and control group (32 cases). Patients in treatment group were treated with capsules of extraction of polygonum cuspidatum and hawthorn, 1 pill po, bid (dosage of administration: polygonum cuspidatum extraction 5.33 mg x kg(-1) x d(-1), hawthorn extraction 5.0 mg x kg(-1) x d(-1)); patients in control group were treated with lovastatin 20 mg po, qd (dosage of administration: 0.33 mg x kg(-1) x d(-1)). The course of treatment was six months. To observe changes of IMT, plaque integral, and detect the level of plaque stability related serum indexes such as Hs-CRP, MMP-1 and TIMP-1.</p><p><b>RESULT</b>After 6 months of treatment, in control group one patient quit the clinical trial because of liver dysfunction and one patient was rejected because of having not followed the therapeutic regimen. 32 cases in treatment group and 30 cases in control group were analyzed. The results showed that IMT and plaque integral of treatment group decreased significantly after the treatment (P < 0.05, P < 0.01), and there was no significant difference compared with control grope. Serum Hs-CRP, MMP-1 and MMP-1/TIMP-1 decreased after the treatment (P < 0.05, P < 0.01), and the treatment group was superior to control group in decreasing serum Hs-CRP (P < 0.05).</p><p><b>CONCLUSION</b>Detoxifying and blood circulation activating Chinese herb extraction of polygonum cuspidatum and hawthorn has good effect of anti-atherosclerosis and promoting plaque stability. Its mechanism might be related with anti-inflammation and inhibiting degradation of extracellular matrix, and deserves further studies.</p>


Assuntos
Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Proteína C-Reativa , Metabolismo , Doenças das Artérias Carótidas , Sangue , Tratamento Farmacológico , Crataegus , Química , Medicamentos de Ervas Chinesas , Farmacologia , Usos Terapêuticos , Fallopia japonica , Química , Metaloproteinase 1 da Matriz , Sangue , Segurança , Inibidor Tecidual de Metaloproteinase-1 , Sangue
16.
J Ethnopharmacol ; 146(1): 372-8, 2013 Mar 07.
Artigo em Inglês | MEDLINE | ID: mdl-23318412

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: The pericarp of Citrus reticulata possesses medical functions of regulating Qi and expelling phlegm, and has been clinically used for the treatment of lung related diseases in traditional Chinese medicine for a long time. Our previous research revealed that Citrus reticulata exhibited inhibitory effects on pulmonary fibrosis; however, its active principles are still unclear. AIM OF THE STUDY: To investigate the inhibitory effects on pulmonary fibrosis of alkaline extract from ethanol extract of Citrus reticulata and clarify its possible mechanism. MATERIALS AND METHODS: The citrus alkaline extract (CAE) was prepared from ethanol extract of Citrus reticulata and MRC-5 cells were used for the evaluation of inhibitory activity in vitro. CAE was further orally administrated to bleomycin (BLM)-induced pulmonary fibrosis rats. The rat body weight, hydroxyproline levels in serum and lung, pathological changes of lung, as well as mRNA and protein expressions of matrix metalloproteinase-9 (MMP-9), tissue inhibitor of metalloproteinase-1 (TIMP-1) and tumor necrosis factor-α (TNF-α) in rat lung tissues were analyzed. RESULTS: CAE dose-dependently inhibited the proliferation of MRC-5 cells, and the LDH assay clearly revealed that the inhibitory activity of CAE was not due to its cytotoxicity. CAE treatment significantly increased rat weight gain, ameliorated alveolitis and pulmonary fibrosis degree, and lowered hydroxyproline contents in both serum and lung tissues. RT-PCR and western blot revealed that mRNA and protein expressions of MMP-9 were significantly elevated, while mRNA and protein levels of TIMP-1 and TNF-α were markedly decreased in lung tissues of CAE treated rats. CONCLUSIONS: The results collectively demonstrated that CAE possessed an inhibitory activity on the proliferation of MRC-5 and a preventive effect on BLM-induced pulmonary fibrosis in rats. The preliminary mechanisms of the effects may be through upregulation of MMP-9 expression and inhibition of the expressions of TNF-α and TIMP-1.


Assuntos
Anti-Inflamatórios/uso terapêutico , Citrus , Extratos Vegetais/uso terapêutico , Fibrose Pulmonar/tratamento farmacológico , Animais , Anti-Inflamatórios/farmacologia , Bleomicina , Linhagem Celular , Proliferação de Células/efeitos dos fármacos , Humanos , Hidroxiprolina/metabolismo , L-Lactato Desidrogenase/metabolismo , Masculino , Metaloproteinase 9 da Matriz/genética , Metaloproteinase 9 da Matriz/metabolismo , Fitoterapia , Extratos Vegetais/farmacologia , Fibrose Pulmonar/induzido quimicamente , Fibrose Pulmonar/metabolismo , RNA Mensageiro/metabolismo , Ratos , Ratos Sprague-Dawley , Inibidor Tecidual de Metaloproteinase-1/genética , Inibidor Tecidual de Metaloproteinase-1/metabolismo , Fator de Necrose Tumoral alfa/genética , Fator de Necrose Tumoral alfa/metabolismo
17.
Chin J Integr Med ; 18(9): 714-9, 2012 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-22936326

RESUMO

Rhizoma Polygoni Cuspidati, a Chinese herbal drug, has actions of dispelling dampness, alleviating jaundice, clearing heat, subsiding toxin, activating blood, and removing stasis. Polydatin (PD), one of its chief active ingredients, has been proved by modern pharmacological studies to possess extensive cardiovascular pharmacological activity, showing marked effects on protecting cardio-myocyte, dilating blood vessel, antagonizing platelet aggregation, thrombosis, and atherosclerosis. The progress of the research on cardiovascular pharmacological actions and the acting mechanism of PD was reviewed in this paper.


Assuntos
Pesquisa Biomédica/tendências , Sistema Cardiovascular/efeitos dos fármacos , Glucosídeos/farmacologia , Estilbenos/farmacologia , Humanos , Peroxidação de Lipídeos/efeitos dos fármacos , Miócitos Cardíacos/efeitos dos fármacos , Vasodilatação/efeitos dos fármacos
18.
Chin. j. integr. med ; Chin. j. integr. med;(12): 714-719, 2012.
Artigo em Inglês | WPRIM | ID: wpr-347122

RESUMO

Rhizoma Polygoni Cuspidati, a Chinese herbal drug, has actions of dispelling dampness, alleviating jaundice, clearing heat, subsiding toxin, activating blood, and removing stasis. Polydatin (PD), one of its chief active ingredients, has been proved by modern pharmacological studies to possess extensive cardiovascular pharmacological activity, showing marked effects on protecting cardio-myocyte, dilating blood vessel, antagonizing platelet aggregation, thrombosis, and atherosclerosis. The progress of the research on cardiovascular pharmacological actions and the acting mechanism of PD was reviewed in this paper.


Assuntos
Humanos , Pesquisa Biomédica , Sistema Cardiovascular , Glucosídeos , Farmacologia , Peroxidação de Lipídeos , Miócitos Cardíacos , Estilbenos , Farmacologia , Vasodilatação
20.
Artigo em Chinês | WPRIM | ID: wpr-273635

RESUMO

<p><b>OBJECTIVE</b>To evaluate the effect of Jieze No. 1 Gel (JZ1) on the inner environment of vagina through observing its influences on vaginal levels of lactobacillus, glycogen and lactoferrin in mice.</p><p><b>METHODS</b>One hundred female Kunming mice were randomized into 5 groups, the blank control (BC) group, the blank gel (BG) group, and the three JZ1 treated groups. They were treated via vagina with saline, matrix gel, high (2 mg/microL), middle (1 mg/microL) and low (0.5 mg/microL) dose JZ1 respectively in volume of 20 microL, 72 h after being subcutaneously injected with physiological estradiol benzoate (E2) 2 microg. The 24 h and 72 h living lactobacillus in vaginal lavage fluid cultures were counted, the content of glycogen and the expression of lactoferrin in vaginal tissue were measured.</p><p><b>RESULTS</b>No significant difference was found between the BC group and the three JZ1 treated groups in terms of lactobacillus-CFU, glycogen content and lactoferrin expression, and these indices detected at 24 h were not different to those detected at 72 h in the groups treated with various doses of JZ1 respectively (P > 0.05).</p><p><b>CONCLUSION</b>Once application of JZ1 shows no effect on levels of lactobacillus, glycogen, and lactoferrin expression in the vagina of mice.</p>


Assuntos
Animais , Feminino , Camundongos , Medicamentos de Ervas Chinesas , Farmacologia , Géis , Glicogênio , Metabolismo , Lactobacillus , Lactoferrina , Metabolismo , Camundongos Endogâmicos , Vagina , Metabolismo , Microbiologia
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