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1.
Int Immunopharmacol ; 116: 109825, 2023 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-36764277

RESUMEN

Acute cardiovascular events increase significantly in postmenopausal women. The relationship between estrogen receptor (ER) and plaque stability in the postmenopausal stage remains to be elucidated. We aimed to explore whether ERα activation improves plaque instability in the postmenopausal stage. Here, we report that postmenopausal women showed increased macrophage activation and plaque instability with increased MCP-1, MMP9, TLR4, MYD88 and NF-κB p65 and decreased ERα and TIMP1 expression in the vascular endothelium. Moreover, ovariectomy in LDLR-/- mice resulted in a significant increase in plaque area and necrotic core area, as well as a significant decrease in collagen content and an increase in macrophage accumulation in the artery. Ovariectomy also reduced serum estrogen levels and ERα expression and upregulated TLR4 and MMP9 expression in arteries in LDLR-/- mice. Estrogen or phytoestrogen therapy upregulated the expression level of ERα in ovariectomized mice and increased plaque stability by inhibiting macrophage accumulation and TLR4 signaling. In vitro, LPS incubation of RAW264.7 cells resulted in a significant decrease in ERα and TIMP1 expression and an increase in TLR4 activation, and estrogen or phytoestrogen treatment increased ERα and TIMP1 expression and inhibited TLR4 activation and MMP9 expression in LPS-treated RAW264.7 cells. Compared to control siRNA transfected RAW264.7 cells, TLR4 siRNA promoted TIMP1 expression in RAW264.7 cells with LPS incubation, but did not affect ERα expression in RAW264.7 cells with or without LPS treatment. The ERα inhibitor MPP abolished the regulatory effect of estrogen or phytoestrogen on LPS-induced RAW264.7 cells. In conclusion, the present study demonstrates that decreased ERα expression promotes macrophage infiltration and plaque instability in the postmenopausal stage, and activation of ERα in the postmenopausal stage alleviates atherosclerotic plaque instability by inhibiting TLR4 signaling and macrophage-related inflammation.


Asunto(s)
Receptor alfa de Estrógeno , Placa Aterosclerótica , Receptor Toll-Like 4 , Animales , Femenino , Ratones , Receptor alfa de Estrógeno/genética , Receptor alfa de Estrógeno/metabolismo , Lipopolisacáridos , Macrófagos , Metaloproteinasa 9 de la Matriz/genética , Metaloproteinasa 9 de la Matriz/metabolismo , FN-kappa B/metabolismo , Fitoestrógenos , Posmenopausia , ARN Interferente Pequeño/metabolismo , Receptor Toll-Like 4/genética , Receptor Toll-Like 4/metabolismo , Humanos , Células RAW 264.7
2.
Front Pharmacol ; 13: 926291, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36176430

RESUMEN

Primary dysmenorrhea (PDM) is a common disorder among women around the world. Two processed products of Curcuma aromatica Salisb. [Zingiberaceae] (CAS) are traditional Chinese medicine (TCM) that have long been used to treat gynecological blood stasis syndrome such as primary dysmenorrhea. The mechanisms and active substances of CAS are still largely unknown. The study aimed to establish a rat model of primary dysmenorrhea which investigates the differences between the pharmacodynamics and mechanisms of raw CAS (RCAS) and vinegar-processed CAS (VCAS). Histopathology, cytokinetics, and metabolomics were adopted to evaluate the anti-blood stasis effect of RCAS and VCAS. In metabolomics, endogenous differential metabolites in plasma, urine, and feces are the essential steps to evaluate the effect of RCAS and VCAS. In this study, the rat model of primary dysmenorrhea was successfully established. After RCAS and VCAS intervention, the uterine tissue morphology of dysmenorrhea model rats was improved, and gland hypertrophy and myometrial hyperplasia were reduced as well as neutrophil content. Compared with the RCAS group, the VCAS group had better uterine morphology, few inflammatory factors, and significantly improved amino acid and lipid metabolism. The aforementioned results support the conclusion that VCAS performed better than RCAS in primary dysmenorrhea and that vinegar processing increases the efficacy of CAS.

3.
Front Pharmacol ; 13: 950749, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36016561

RESUMEN

Curcuma aromatica Salisb. rhizome (CASR) has multifunctional characteristics worldwide and a long history of use as a botanical drug with. Currently, it is often used clinically to treat coronary heart disease (CHD) caused by blood stasis syndrome. However, the therapeutic mechanism of CASR in the treatment of CHD remains poorly understood. In study, the main chemical constituents of CASR were analyzed using UPLC-Q-TOF-MS/MS. Then, its potential therapeutic mechanism against CHD was predicted. Subsequently, pharmacological evaluation was performed using CHD rat model. Finally, a lipidomics approach was applied to explore the different lipid metabolites to verify the regulation of CASR on lipid metabolism disorders in CHD. A total of 35 compounds was identified from CASR. Seventeen active components and 51 potential targets related to CHD were screened by network pharmacology, involving 13 key pathways. In vivo experiments showed that CASR could significantly improve myocardial infarction, blood stasis, and blood lipid levels and regulate the PI3K/AKT/mTOR signaling pathway in CHD rats. Lipidomics further showed that CASR could regulate abnormal sphingolipid, glycerophospholipid, and glycerolipid metabolism in CHD rats. The therapeutic mechanism of CASR against CHD was initially elucidated and included the regulation of lipid metabolism. Its effects may be attributed to active ingredients, such as curzerene, isoprocurcumenol, and (+)-curcumenol. This study reveals the characteristics of multi-component and multi-pathway of CASR in the treatment of CHD, which provides a basis for the follow-up development and utilization of CASR.

4.
Zhongguo Zhong Yao Za Zhi ; 47(12): 3270-3284, 2022 Jun.
Artículo en Chino | MEDLINE | ID: mdl-35851121

RESUMEN

Coronary heart disease(CHD) is a common cardiovascular disease in clinical practice. Curcumae Rhizoma(CR), an important herbal medicine for breaking blood stasis and resolving mass, is often used for the treatment of CHD caused by blood stasis syndrome. However, the anti-CHD components, targets, and mechanism are still unclear. Therefore, in this study, the chemical components of CR were separated and identified by ultra high performance liquid chromatography-quadrupole-time-of-flight mass spectrometry(UPLC-Q-TOF-MS/MS). Based on the identified components, network pharmacology analysis, including target prediction and functional enrichment, was applied to screen out the main active components against CHD, and the potential mechanism was discussed. Finally, molecular docking was performed to verify the binding between the active components and the targets. The results showed that among the 52 chemical components identified in CR, 28 were related to CHD, involving 75 core targets. The core components included(4S)-4-hydroxy-gweicurculactone, curcumadione, and curcumenone, and the core targets included phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit alpha(PIK3 CA), mitogen-activated protein kinase 1(MAPK1), and mitogen-activated protein kinase 3(MAPK3). In summary, through the active components, such as(4S)-4-hydroxy-gweicurculactone, curcumadione, and curcumenone, CR regulates the nerve repair, vasoconstriction, lipid metabolism, and inflammatory response, thereby exerts therapeutic effect on CHD.


Asunto(s)
Enfermedad Coronaria , Medicamentos Herbarios Chinos , Enfermedad Coronaria/tratamiento farmacológico , Curcuma/química , Medicamentos Herbarios Chinos/farmacología , Humanos , Simulación del Acoplamiento Molecular , Espectrometría de Masas en Tándem
5.
Front Mol Biosci ; 9: 762224, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35309515

RESUMEN

Carbonizing by stir-frying (CSF) is the most common technology in botanical folk medicines to enhance the convergence, hemostasis, and antidiarrheal effects. Sanguisorbae Radix (SR), a well-known herbal medicine in China, has extensive therapeutic functions, while charred SR is known as an additional product obtained from SR after CSF. In this study, mass spectrometry was used to investigate the effect of charring on tannins transformation of SR. The findings showed that the content level of tannins in SR decreased significantly after carbonizing process, while their three categories, gallotannins, ellagitannins, and procyanidins, had downward trends in general. Moreover, CSF also induced the polyphenol in SR to release relevant monomers from its origins. Significant amount of hydrolyzable tannins were detected by mass spectrometry, including gallotannins and ellagitannins, suggesting that hydrolysis during CSF yielded gallic and ellagic acid and their derivatives, in addition to sugar moieties. Subsequently, gallic and ellagic acid can further polymerize to form sanguisorbic acid dilactone. The amount of proanthocyanidins, the oligomers of catechin, including procyanidin, procyanidin C2, procyanidin B3, and 3-O-galloylprocyanidin B3, decreased to form catechin and its derivatives, which may further degrade to protocatechualdehyde. Quantitative analysis illustrated that the amount of gallic, pyrogallic, and ellagic acid and methyl gallate, the essential effectors in SR, significantly increased after CSF, with increased ratios of 1.36, 4.28, 10.33, and 4.79, respectively. In contrast, the contents of cathechin and epigallocatechin dropped remarkably with increased ratios of 0.04 and 0.02. Tannins exhibit moderate absorption, while their relevant monomers have a higher bioavailability. Therefore, CSF is proved here to be an effective technique to the release of active monomers from the original polyphenol precursor. This study explored the mechanism by which tannins are transformed upon CSF of SR.

6.
Zhongguo Zhong Yao Za Zhi ; 47(1): 188-202, 2022 Jan.
Artículo en Chino | MEDLINE | ID: mdl-35178926

RESUMEN

This study aims to study the effective substance and mechanism of Ziziphi Spinosae Semen extract in the treatment of insomnia based on serum metabolomics and network pharmacology. The rat insomnia model induced by p-chlorophenylalanine(PCPA) was established. After oral administration of Ziziphi Spinosae Semen extract, the general morphological observation, pentobarbital sodium-induced sleep test, and histopathological evaluation were carried out. The potential biomarkers of the extract in the treatment of insomnia were screened by ultra-high performance liquid chromatography-mass spectrometry(UHPLC-MS) combined with multivariate analysis, and the related metabolic pathways were further analyzed. The "component-target-pathway" network was constructed by ultra-high performance liquid chromatography coupled with quadrupole-Exactive mass spectrometry(UHPLC-Q-Exactive-MS/MS) combined with network pharmacology to explore the effective substances and mechanism of Ziziphi Spinosae Semen in the treatment of insomnia. The results of pentobarbital sodium-induced sleep test and histopathological evaluation(hematoxylin and eosin staining) showed that Ziziphi Spinosae Semen extract had good theraputic effect on insomnia. A total of 21 endogenous biomarkers of Ziziphi Spinosae Semen extract in the treatment of insomnia were screened out by serum metabolomics, and the metabolic pathways of phenylalanine, tyrosine and tryptophan biosynthesis, phenylalanine metabolism, and nicotinate and nicotinamide metabolism were obtained. A total of 34 chemical constituents were identified by UHPLC-Q-Exactive-MS/MS, including 24 flavonoids, 2 triterpenoid saponins, 4 alkaloids, 2 triterpenoid acids, and 2 fatty acids. The network pharmacological analysis showed that Ziziphi Spinosae Semen mainly acted on target proteins such as dopamine D2 receptor(DRD2), 5-hydroxytryptamine receptor 1 A(HTR1 A), and alpha-2 A adrenergic receptor(ADRA2 A) in the treatment of insomnia. It was closely related to neuroactive ligand-receptor interaction, serotonergic synapse, and calcium signaling pathway. Magnoflorine, N-nornuciferine, caaverine, oleic acid, palmitic acid, coclaurine, betulinic acid, and ceanothic acid in Ziziphi Spinosae Semen may be potential effective compounds in the treatment of insomnia. This study revealed that Ziziphi Spinosae Semen extract treated insomnia through multiple metabolic pathways and the overall correction of metabolic disorder profile in a multi-component, multi-target, and multi-channel manner. Briefly, this study lays a foundation for further research on the mechanism of Ziziphi Spinosae Semen in treating insomnia and provides support for the development of innovative Chinese drugs for the treatment of insomnia.


Asunto(s)
Medicamentos Herbarios Chinos , Trastornos del Inicio y del Mantenimiento del Sueño , Ziziphus/química , Animales , Cromatografía Líquida de Alta Presión , Medicamentos Herbarios Chinos/química , Metabolómica , Farmacología en Red , Ratas , Semillas/química , Trastornos del Inicio y del Mantenimiento del Sueño/tratamiento farmacológico , Espectrometría de Masas en Tándem
7.
Artículo en Inglés | MEDLINE | ID: mdl-34933255

RESUMEN

Curcuma wenyujin Y.H. Chen et C. Ling rhizome (also called EZhu in China) has long been used as plant medicine for its traditional effect on promoting blood circulation and remove blood stasis. However, the active components of EZhu are still unclear at present. This research is managed to investigate the pharmacodynamics material basis on removing blood stasis of EZhu by exploring the spectrum-effect relationship between UPLC-Q/TOF-MS fingerprints and pharmacologic actions. Hemorheology and related functional parameters were detected to evaluate the pharmacologic actions of EZhu. Relative content Changes of components in rat plasma were detected by UPLC-Q/TOF-MS. A compound-target-pathway network was built to predict the pharmacological activity of components in plasma. Then, bivariate correlation analysis (BCA) was used to explore the correlation degree between components in plasma and pharmacologic actions of EZhu. In UPLC-Q/TOF-MS fingerprints of rat plasma, 10 prototype components were identified. BCA results show that 8 components were concerned with the pharmacological activity for treating blood stasis syndrome (BSS) in varying degrees (R > 0.5, P < 0.05). Among them, zedoarofuran and curzerenone have shown correlation with more pharmacological indicators. The network predicted that 80 targets were closely related to 10 components, in which 48 targets were connected with 159 metabolic pathways including arachidonic acid metabolism, sphingolipid signaling pathway, and linoleic acid metabolism. Overall, this study provided a scientific basis for TCM quality control to ensure its safety and efficacy.


Asunto(s)
Curcuma/química , Medicamentos Herbarios Chinos , Redes y Vías Metabólicas/efectos de los fármacos , Animales , Medicamentos Herbarios Chinos/análisis , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/farmacología , Hemorreología/efectos de los fármacos , Masculino , Farmacología en Red , Fitoquímicos/sangre , Fitoquímicos/metabolismo , Fitoquímicos/farmacología , Ratas , Ratas Sprague-Dawley
8.
Phytomedicine ; 86: 153558, 2021 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-33866197

RESUMEN

BACKGROUND: Curcumae Rhizoma (CR) has a clinical efficacy in activating blood circulation to dissipate blood stasis and has been used for the clinical treatment of qi stagnation and blood stasis (QSBS) primary dysmenorrhea for many years. However, its molecular mechanism is unknown. OBJECTIVE: The present study aimed to demonstrate the multicomponent, multitarget and multipathway regulatory molecular mechanisms of CR in the treatment of QSBS primary dysmenorrhea. METHODS: Observations of pathological changes in uterine tissues and biochemical assays were used to confirm that a rat model was successfully established and that CR was effective in the treatment of QSBS primary dysmenorrhea. The main active components of CR in rat plasma were identified and screened by ultra-performance liquid chromatography-quadrupole/time-of-flight mass spectrometry (UPLC-Q/TOF-MS). The component-target-disease network and protein-protein interaction (PPI) network of CR were constructed by a network pharmacology approach. Then, we performed Gene Ontology (GO) functional enrichment analysis and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analysis. Molecular docking was adopted to verify the interactions between the core components and targets of CR to confirm the accuracy of the network pharmacology prediction results. Furthermore, we evaluated the bioactive constituents of CR and molecular mechanism of by which CR promote blood circulation and remove blood stasis via platelet tests in vivo and in vitro and Western blot analysis. RESULTS: The results of HE staining and biochemical assays of PGF2α, TXB2 and Ca2+ showed that CR was effective in the treatment of QSBS primary dysmenorrhea. A total of 36 active components were identified in CR, and 329 common targets were obtained and used to construct the networks. Of these, 14 core components and 10 core targets of CR in the treatment of primary dysmenorrhea were identified. The GO and KEGG enrichment analyses revealed that the common targets were involved in multiple signaling pathways, including the calcium, cAMP, MAPK, and PI3K-Akt signaling pathways, as well as platelet activation, which is closely related to platelet aggregation. The molecular docking results showed that the 14 core components and 10 core targets could bind spontaneously. Two core targets (MAPK1 and CCR5) and 7 core components (Isoprocurcumenol, Curcumadione, Epiprocurcumenol, (+)-Curdione, Neocurdione, Procurcumenol, and 13-Hydroxygermacrone) were closely related to CR in the treatment of primary dysmenorrhea. Furthermore, the in vivo platelet test showed that CR clearly inhibited platelet aggregation. Five core components ((+)-Curdione, Neocurdione, Isoprocurcumenol, Curcumadione and Procurcumenol) obviously inhibited platelet aggregation in vitro. In addition, based on the relationships among the signaling pathways, we confirmed that CR can effectively inhibit the expression of MAPK and PI3K-Akt signaling pathway-related proteins and decrease the protein expression levels of ERK, JNK, MAPK, PI3K, AKT and CCR5, thereby inhibiting platelet aggregation. CONCLUSION: This study demonstrated the bioactive constituents and mechanisms of CR in promoting blood circulation and removing blood stasis and its multicomponent, multitarget and multipathway treatment characteristics in primary dysmenorrhea. The results provide theoretical evidence for the development and utilization of CR.


Asunto(s)
Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/farmacología , Dismenorrea/tratamiento farmacológico , Animales , Calcio/metabolismo , Cromatografía Líquida de Alta Presión , Dinoprost/metabolismo , Modelos Animales de Enfermedad , Dismenorrea/metabolismo , Femenino , Humanos , Simulación del Acoplamiento Molecular , Fosfatidilinositol 3-Quinasas , Agregación Plaquetaria/efectos de los fármacos , Mapas de Interacción de Proteínas , Ratas Sprague-Dawley , Transducción de Señal/efectos de los fármacos , Útero/efectos de los fármacos , Útero/fisiopatología
9.
Cell Biol Int ; 45(9): 1866-1875, 2021 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-33835632

RESUMEN

Liver fibrosis is a primary threat to public health, owing to limited therapeutic options. Germacrone (GM) has been shown to exert various curative effects against human diseases, including liver injury. The aim of this study was to investigate the pharmacological effects of GM in the pathophysiology of hepatic fibrosis and determine its potential mechanisms of action. A liver fibrosis rat model was established via carbon tetrachloride (CCl4 ) treatment, and LX-2 cells were stimulated with TGF-ß1. The effects of GM on liver fibrosis and its relationship with the phosphatidylinositol 3-kinase (PI3K)/protein kinase B (AKT)/mammalian target of rapamycin (mTOR) signalling pathway were investigated. In the CCl4 fibrosis-induced rat model, GM improved histological damage, inhibited the activity of hepatic α-smooth muscle actin and improved serum alanine aminotransferase and aspartate aminotransferase levels in a dose-dependent manner. GM potently inhibited hepatic stellate cells (HSCs) growth and epithelial-mesenchymal transition (EMT) progression, as reflected by the altered expression of proliferative (Ki-67, PCNA and cleaved caspase-3) and EMT-related (E-cadherin and vimentin) proteins. In TGF-ß1-stimulated LX-2 cells, GM significantly inhibited the survival and activation of HSCs and induced cell apoptosis. GM also suppressed the migration ability and reversed the EMT process in HSCs. Following GM treatment, the phosphorylation of the PI3K, AKT and mTOR proteins was reduced in the liver of CCl4 -treated rats and TGF-ß1-stimulated LX-2 cells, indicating that GM may attenuate hepatic fibrosis via the PI3K/AKT/mTOR signalling pathway. These outcomes highlight the anti-fibrotic effects of GM and suggest that it is a potential therapeutic agent for the treatment of liver fibrosis.


Asunto(s)
Medicamentos Herbarios Chinos/farmacología , Cirrosis Hepática/tratamiento farmacológico , Hígado/efectos de los fármacos , Aceites de Plantas/farmacología , Sesquiterpenos de Germacrano/farmacología , Animales , Línea Celular , Células Estrelladas Hepáticas , Humanos , Hígado/patología , Masculino , Ratas , Ratas Sprague-Dawley
10.
Zhongguo Zhong Yao Za Zhi ; 46(6): 1393-1400, 2021 Mar.
Artículo en Chino | MEDLINE | ID: mdl-33787137

RESUMEN

L~*, a~* and b~* values of prepared slices of Curcumae Rhizoma were measured by spectrophotometer. SPSS 21.0 was used for discriminant analysis to establish the color range and mathematical prediction model of prepared slices of Curcumae Rhizoma. The values of L~*, a~* and b~* of kwangsiensis ranged from 58.09-62.40, 4.53-5.66 and 23.61-24.29, while the values of L~*, a~* and b~* of phaeocaulis were between 64.02-70.71,-0.89-4.13 and 44.59-54.52, respectively. The values of L~*, a~* and b~* of wenyujin were 68.55-70.99,-0.11-1.47 and 28.26-32.19, respectively. The mathematical prediction model was proved to be able to realize 100% identification of Curcumae Rhizome of different origins through original and cross validation and external samples validation. A dual wavelength HPLC was established; the contents of 9 sesquiterpenoids and 3 Curcumae Rhizomes were determined simultaneously; and the contents of Curcumae Rhizome of different origins were determined. The results showed that kwangsiensis had higher contents of neocurdione, ß-elemene and isocurcumaenol, phaeocaulis curcumin, furadienone, demethoxycurcumin and curcumin; and wenyujin mainly contained curdione, furadienes and guimarone. Pearson correlation analysis on L~*, a~*, b~* value and content of 12 components showed that curcumin, furadienone, demethoxycurcumin and curcumin had a significant positive correlation with b~* value(P<0.01). There was a significant negative correlation between neocurdione, ß-elemene and isocurcumaenol and L~* value(P<0.01). Curdione, furadienes and guimarone were significantly correlated with L~* value(P<0.01),indicating that the appearance co-lor of Curcumae Rhizoma could reflect the change of the content of the internal components. This study provided reference for the rapid recognition of Curcumae Rhizoma and the establishment of quality evaluation system.


Asunto(s)
Curcumina , Rizoma , Cromatografía Líquida de Alta Presión , Color , Curcuma
11.
J Nanobiotechnology ; 18(1): 86, 2020 Jun 08.
Artículo en Inglés | MEDLINE | ID: mdl-32513194

RESUMEN

Hepatic stellate cells (HSCs) were activated and secreted excessive amounts of extracellular matrix (ECM) proteins during pathogenetic progress of liver fibrosis. Germacrone (GMO) and miR-29b can play an important role in inhibiting growth of HSCs and production of type I collagen. GMO and miR-29b were co-encapsulated into nanoparticles (NPs) based on poly(ethylene glycol)-block-poly(lactide-co-glycolide) (PEG-PLGA). Then, NPs were modified with cyclic RGD peptides (cRGDfK). cRGDfK is an effective ligand to bind integrin αvß3 and increase the targeting ability for fibrotic liver. GMO- and miR-29b-loaded NPs exhibited great cytotoxicity to activated HSCs and significantly inhibited production of type I collagen. Liver fibrosis model of mice was induced by administration of carbon tetrachloride. Great targeting ability was achieved in liver fibrotic mice treated with cRGD-modified NPs. Significant ant-fibrotic effects have been presented based on hematoxylin and eosin (H&E), Masson and Sirius Red staining results of liver tissues collected from mice treated with drug-loaded NPs. All these results indicate GMO- and miR-29b-loaded cRGD-modified NPs have the potential for clinical use to treat liver fibrosis.


Asunto(s)
Cirrosis Hepática/metabolismo , MicroARNs , Nanopartículas , Péptidos Cíclicos , Sesquiterpenos de Germacrano , Animales , Tetracloruro de Carbono/efectos adversos , Células Cultivadas , Células Estrelladas Hepáticas/efectos de los fármacos , Células Estrelladas Hepáticas/metabolismo , Hígado/efectos de los fármacos , Cirrosis Hepática/inducido químicamente , Masculino , Ratones , Ratones Endogámicos C57BL , MicroARNs/química , MicroARNs/farmacocinética , MicroARNs/farmacología , Nanopartículas/química , Nanopartículas/metabolismo , Péptidos Cíclicos/química , Péptidos Cíclicos/farmacocinética , Sesquiterpenos de Germacrano/química , Sesquiterpenos de Germacrano/farmacocinética , Sesquiterpenos de Germacrano/farmacología , Distribución Tisular
12.
Zhongguo Zhong Yao Za Zhi ; 45(5): 1135-1141, 2020 Mar.
Artículo en Chino | MEDLINE | ID: mdl-32237457

RESUMEN

There are many chemical components in the volatile oil of Dictamni Cortex. The complex network relationship of "component-target-disease" can be revealed by using the network pharmacology method, and the mechanism of the efficacy of Dictamni Cortex can be revealed. In this study, we used Swiss Target Prediction database to predict the target of action, STRING database to build protein interaction network, and Cytoscape software to build "component-target-disease" network. The results showed that the antibacterial, anti-inflammatory and antiallergic effects of Dictamni Cortex were closely related to the components of thymol methyl ether, elemenol, anethole, and the related targets of each component were cross-linked to play a multi-target pharmacodynamic role. This study laid a foundation for the study of the effective substance basis and quality control evaluation of the Dictamni Cortex, and provided a scientific basis for further revealing its mechanism.


Asunto(s)
Dictamnus/química , Medicamentos Herbarios Chinos/farmacología , Aceites Volátiles/farmacología , Mapas de Interacción de Proteínas , Control de Calidad , Programas Informáticos
13.
Front Pharmacol ; 10: 1543, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-32009955

RESUMEN

Schisandra chinensis (SC) is a well-known important traditional Chinese medicine (TCM) that has been used to treat liver disease in China for a long time. However, its overall effects and mechanism of action are unclear. The present study aimed to explore the potential mechanism of SC in protection against alcoholic liver injury (ALI). In this research, to enable a full assessment of metabolic changes in ALI in Sprague-Dawley rats and to increase our understanding of physiological changes in normal and pathological states, ultra-high performance liquid chromatography combined with quadrupole time of flight mass spectrometry (UHPLC-Q/TOF-MS) was used to probe potential biomarkers to learn more about ALI and to evaluate the overall effect of SC for ALI in rats. Principal component analysis (PCA) and orthogonal partial least squares discriminant analysis (OPLS-DA) were used to investigate global metabolomic alterations and to evaluate the therapeutic effects of SC in rats. The component-target-pathway network of SC was then constructed on the basis of the network pharmacology, and the liver injury-relevant signaling pathways were thus dissected and validated. The results showed that SC has conspicuous therapeutic efficacy for ALI, as suggested by the results of the pathological section and biochemical index assays, such as those for Alanine aminotransferase (ALT), Aspartate transaminase (AST), Alkaline phosphatase (AKP), γ-glutamyl transferase (γ-GT/GGT), Reactive oxygen species (ROS), and Malondialdehyde (MDA). Furthermore, 21 kinds of potential biomarkers were identified in plasma samples of ALI rats, and 20 kinds of potential biomarkers were identified in their bile samples. The biomarkers were mainly related to inflammation and dysfunctions of amino acids and energy metabolism. The recovery of these dysfunctions partly led to the curative effect of SC on ALI.

14.
Zhong Xi Yi Jie He Xue Bao ; 7(4): 354-9, 2009 Apr.
Artículo en Chino | MEDLINE | ID: mdl-19361366

RESUMEN

OBJECTIVE: To evaluate the effects of San'ao decoction (SAD) and its analogous prescriptions (APs), compounds of traditional Chinese herbal medicine for asthma, on airway inflammation in mice with respiratory syncytial virus (RSV)- and ovalbumin (OVA)-induced asthma. METHODS: A total of 110 mice were randomly divided into control group, untreated group, dexamethasone (DM) group, small-dose SAD (SAD-S) group, large-dose SAD (SAD-L) group, AP I-S group, AP I-L group, AP II-S group, AP II-L group, AP III-S group, and AP III-L group. The asthma model was reproduced by sensitization with multipoint intraperitoneal injection of OVA, followed by repeated inhalation of OVA combined with intranasal instillation of RSV. Cells in bronchoalveolar lavage fluid (BALF) were counted and classified. The supernatant of the BALF was used for detecting the contents of interleukin-4 (IL-4), interleukin-5 (IL-5) and interferon-gamma (IFN-gamma) by enzyme-linked immunosorbent assay. Pathological changes in lung tissue were observed by hematoxylin and eosin staining and the scores of pathological changes were also calculated to determine the degree of inflammation. RESULTS: Compared with the control group, the amounts of lymphocytes, eosinophils, neutrophils in BALF in the untreated group were increased significantly (P<0.01); the changes of lung histopathology in the untreated group were much more serious, and the content of IFN-gamma was sharply decreased, while the contents of IL-4 and IL-5 were significantly increased (P<0.05). The counts of eosinophils in BALF of the treated groups all decreased obviously (P<0.01) as compared with the untreated group. The count of the neutrophils in BALF of the AP II-L group was obviously lower than that in the untreated group (P<0.01). Most of Chinese herbal formulas and DM could increase the level of IFN-gamma, and decrease the level of IL-4. All concentrations of the APs and SAD could decrease the level of IL-5 as compared with the untreated group, especially of the AP II-L and AP I-L (P<0.05, P<0.01). CONCLUSION: SAD and its APs had some therapeutic effects on RSV-induced asthma in mice. Among the formulas, AP II has a better therapeutic efficacy in treatment of asthma by decreasing the amount of neutrophils.


Asunto(s)
Asma/metabolismo , Asma/patología , Medicamentos Herbarios Chinos/farmacología , Infecciones por Virus Sincitial Respiratorio/metabolismo , Infecciones por Virus Sincitial Respiratorio/patología , Animales , Asma/tratamiento farmacológico , Asma/virología , Líquido del Lavado Bronquioalveolar/citología , Medicamentos Herbarios Chinos/uso terapéutico , Eosinófilos/citología , Inflamación/patología , Interferón gamma/metabolismo , Interleucina-4/metabolismo , Interleucina-5/metabolismo , Pulmón/patología , Linfocitos/citología , Ratones , Ratones Endogámicos BALB C , Neutrófilos/citología , Infecciones por Virus Sincitial Respiratorio/tratamiento farmacológico , Virus Sincitiales Respiratorios
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