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1.
Zhongguo Zhong Yao Za Zhi ; 48(23): 6509-6518, 2023 Dec.
Artículo en Chino | MEDLINE | ID: mdl-38212008

RESUMEN

This study investigated the differences in excretion kinetics of three alkaloids and their four metabolites from Simiao Pills in normal and type 2 diabetic rats. The diabetes model was established in rats by injection of streptozotocin, and the alkaloids in urine, feces, and bile of normal and diabetic rats were detected by LC-MS/MS to explore the effect of diabetes on alkaloid excretion of Simiao Pills. The results showed that 72 h after intragastric administration of the extract of Simiao Pills, feces were the main excretion route of alkaloids from Simiao Pills. The total excretion rates of magnoflorine and berberine in normal rats were 4.87% and 56.54%, which decreased to 2.35% and 35.53% in diabetic rats, which had statistical significance(P<0.05). The total excretion rates of phellodendrine, magnoflorine, and berberine in the urine of diabetic rats decreased significantly, which were 53.57%, 60.84%, and 52.78% of those in normal rats, respectively. After 12 h of intragastric administration, the excretion rate of berberine in the bile of diabetic rats increased significantly, which was 253.33% of that of normal rats. In the condition of diabetes, the excretion rate of berberine metabolite, thalifendine significantly decreased in urine and feces, but significantly increased in bile. The total excretion rates of jateorrhizine and palmatine in the urine increased significantly, and t_(1/2) and K_e changed significantly. The results showed that diabetes affected the in vivo process of alkaloids from Simiao Pills, reducing their excretion in the form of prototype drug, affecting the biotransformation of berberine, and ultimately increasing the exposure of alkaloids in vivo, which would be conducive to the hypoglycemic effect of alkaloids. This study provides references for the clinical application and drug development of Simiao Pills in diabetes.


Asunto(s)
Alcaloides , Berberina , Diabetes Mellitus Experimental , Diabetes Mellitus Tipo 2 , Ratas , Animales , Bilis/metabolismo , Cromatografía Liquida/métodos , Diabetes Mellitus Experimental/tratamiento farmacológico , Diabetes Mellitus Experimental/metabolismo , Cromatografía Líquida de Alta Presión/métodos , Espectrometría de Masas en Tándem/métodos , Heces , Alcaloides/metabolismo , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Diabetes Mellitus Tipo 2/metabolismo
2.
Drug Des Devel Ther ; 16: 4325-4341, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36578822

RESUMEN

Background: Ermiao Wan (EMW) is commonly used to treat atopic dermatitis (AD) in China. However, the pharmacological mechanisms underlying the action of EMW against AD remain unclear. Purpose: We aimed to determine the mechanisms underlying the effectiveness of EMW in the treatment of AD. Methods: We evaluated the effect of EMW on AD induced by dinitrochlorobenzene (DNCB) in BALB/C mice. To clarify the key components of EMW in AD treatment, the main components of EMW were identified using HPLC. Serum pharmacochemistry was used to analyze the absorbed ingredients from blood. Based on the phytochemical results, network pharmacology and molecular docking were used to predict the action of EMW. Skin transcriptomic analysis was used to validate the network pharmacology results. RT-qPCR,ELISA, and immunohistochemical were performed to validate the results of skin transcriptomics. Results: EMW improved the symptoms of AD, with less rashes, less spontaneous scratching, less inflammatory cell infiltration, and fewer allergic reactions. The established HPLC method is simple and reliable. Chlorogenic acid, phellodendrine, magnoflorine, jatrorrhizine, palmatine, berberine, and atractylodin were the key effective ingredients with a high blood concentration. Fifty-seven primary causal targets of EMW against AD were identified. These targets are mainly involved in ErbB signaling pathways including EGFR, AKT1, MAPK8, JUN, MAPK1. Molecular docking showed that EGFR, AKT1, MAPK8, JUN, MAPK1 had good binding force with EMW. In AD mice, EMW regulated the EGFR/AKT signaling through upregulation of Grb2, GAB1, Raf-1, EGFR, and AKT, and downregulation of MAPK1 and JUN, compared to that in the MD group. Conclusion: EMW could alleviate AD through activating EGFR/AKT signaling and suppressing MAPK. This study provides a theoretical basis for the clinical use of EMW.


Asunto(s)
Dermatitis Atópica , Medicamentos Herbarios Chinos , Ratones , Animales , Dermatitis Atópica/tratamiento farmacológico , Dermatitis Atópica/metabolismo , Proteínas Proto-Oncogénicas c-akt/metabolismo , Simulación del Acoplamiento Molecular , Farmacología en Red , Transcriptoma , Antiinflamatorios/farmacología , Ratones Endogámicos BALB C , Medicamentos Herbarios Chinos/uso terapéutico , Receptores ErbB/genética , Receptores ErbB/metabolismo
3.
Biomed Chromatogr ; 36(1): e5254, 2022 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-34605575

RESUMEN

Phellodendri Chinensis Cortex (PCC) and Atractylodis Rhizoma (AR) are frequently used as herb pair to treat eczema and gout owing to their synergistic effects. Alkaloids are the major ingredients from PCC and the effect of their combination on the in vivo processing of alkaloids remains unclear. In this study, a simple and reliable UPLC-MS/MS method for simultaneous determination of six alkaloids in rat plasma was developed. This method was applied to a comparative pharmacokinetic study between PCC and PCC-AR in rats. Effect of AR on absorption of alkaloids was investigated by a single-pass intestinal perfusion study. The effect of AR on urinary excretion of alkaloids was studied. Pharmacokinetic studies showed that the values of rea under the concentration-time curve of phellodendrine, magnoflorine and palmatine were greater in the PCC-AR group than in the PCC group. The intestinal absorptive parameters absorption rate constant and effective permeability of phellodendrine and jatrorrhizine in PCC-AR groups were higher than those in the PCC group. Urinary excretion studies revealed that the excreted amount of alkaloids in the PCC-AR group was lower than that in the PCC group. The results revealed that the combination of PCC and AR improves intestinal absorption of alkaloids and reduces their urinary excretion, which enhances their systemic exposure. This study may explain the synergetic effects of PCC and AR in clinical applications.


Asunto(s)
Alcaloides , Medicamentos Herbarios Chinos , Absorción Intestinal/efectos de los fármacos , Alcaloides/sangre , Alcaloides/farmacocinética , Alcaloides/orina , Animales , Cromatografía Liquida , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/farmacocinética , Límite de Detección , Modelos Lineales , Masculino , Ratas , Ratas Sprague-Dawley , Reproducibilidad de los Resultados , Espectrometría de Masas en Tándem
4.
Front Nutr ; 9: 1012961, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36698459

RESUMEN

Background: Type 2 diabetes mellitus (T2DM) is a metabolic disease. Simiao Wan (SMW) is a commonly used clinical drug for hyperuricemia treatment. SMW has been confirmed to improve insulin resistance and is expected to be a novel hypoglycemic agent. However, the hypoglycemic bioactive ingredients and mechanisms of action of SMW are unclear. Objective: To explore the hypoglycemic effects and reveal the mechanisms of SMW and bioactive ingredients (SMW-BI). Study design and methods: The hypoglycemic effects of SMW and SMW-BI were verified in a mouse model of T2DM induced by streptozotocin (STZ) and a high-fat and high-sugar diet (HFSD). Network pharmacology was used to predict the mechanisms of SMW and SMW-BI. Histological analysis and real-time quantitative polymerase chain reaction (RT-qPCR) verified network pharmacology results. RT-qPCR results were further verified by immunofluorescence (IFC) and molecular docking. The correlation between proteins and biochemical indicators was analyzed by Spearman's correlation. Results: Chlorogenic acid, phellodendrine, magnoflorine, jateorhizine, palmatine, berberine, and atractydin were identified as SMW-BI. After 8 weeks of treatment, SMW and SMW-BI decreased the levels of fasting blood glucose (FBG), total cholesterol (TC), triacylglycerols (TG) and low-density lipoprotein cholesterol (LDL-C), increased the level of high-density lipoprotein cholesterol (HDL-C), alleviated weight loss, and increased serum insulin levels in T2DM mice. In addition, SMW and SMW-BI improved hepatocyte morphology in T2DM mice, decreased the number of adipocytes, and increased liver glycogen. Network pharmacological analysis indicated that SMW and SMW-BI may exert hypoglycemic by regulating insulin receptor substrate 1 (IRS1)/RAC-beta serine/threonine-protein kinase (AKT2)/forkhead box protein O1 (FOXO1)/glucose transporter type 2 (GLUT2) signaling. Moreover, correlation analysis showed that SMW and SMW-BI were associated with activation of IRS1, AKT2, and GLUT2, and inhibiting FOXO1. RT-qPCR revealed that SMW and SMW-BI could increase levels of IRS1, AKT2, and GLUT2 in the livers of T2DM mice and lower the level of FOXO1. Furthermore, immunofluorescence analysis showed that FOXO1 expression in the livers of T2DM mice decreased after oral administration of SMW and SMW-BI. Furthermore, molecular docking showed that SMW-BI could bind directly to IRS1 and AKT2. Conclusion: SMW and SMW-BI are potential hypoglycemic drugs that alleviate T2DM by regulating IRS1/AKT2/FOXO1 signaling. Our study provides a research idea for screening the bioactive ingredients in traditional Chinese medicine (TCM).

5.
Food Res Int ; 150(Pt A): 110717, 2021 12.
Artículo en Inglés | MEDLINE | ID: mdl-34865748

RESUMEN

Type 2 diabetes mellitus (T2DM) has become a worldwide concern in recent years. Coix seed (CS) as a homologous substance of traditional Chinese medicine and food, its polysaccharides can improve the symptoms of patients with metabolic disorders. Since most plant polysaccharides are difficult to digest and absorb, we hypothesized that Coix seed polysaccharides (CSP) exert hypoglycemic effects through the gut. In this study, the underlying mechanisms regulating hypoglycemic effects of CSP on a T2DM mouse model were investigated. After treatment with CSP, serum insulin and high-density lipoprotein cholesterol levels were increased, while total cholesterol, triglycerides and low-density lipoprotein cholesterol levels were decreased in T2DM mice. In addition, CSP treatment helped repair the intestinal barrier and modulated the gut microbial composition in T2DM mice, mainly facilitating the growth of short-chain fatty acid (SCFA)-producing bacteria, Spearman's analysis revealed these bacteria were positively related with the hypoglycemic efficacy of CSP. Colonic transcriptome analysis indicated the hypoglycemic effect of CSP was associated with the activation of the IGF1/PI3K/AKT signaling pathway. Correlative analysis revealed that this activation may result from the increase of SCFAs-producing bacteria by CSP. GC-MS detection verified that CSP treatment increased fecal SCFAs levels. Molecular docking revealed that SCFAs could bind with IGF1, PI3K, and AKT. Our findings demonstrated that CSP treatment modulates gut microbial composition, especially of the SCFAs-producing bacteria, activates the IGF1/PI3K/AKT signaling pathways, and exhibits hypoglycemic efficacy.


Asunto(s)
Coix , Diabetes Mellitus Tipo 2 , Microbioma Gastrointestinal , Animales , Coix/metabolismo , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Ácidos Grasos Volátiles , Humanos , Factor I del Crecimiento Similar a la Insulina , Ratones , Simulación del Acoplamiento Molecular , Fosfatidilinositol 3-Quinasas/metabolismo , Polisacáridos/farmacología , Proteínas Proto-Oncogénicas c-akt/metabolismo , Transducción de Señal
6.
Zhongguo Zhong Yao Za Zhi ; 46(23): 6271-6277, 2021 Dec.
Artículo en Chino | MEDLINE | ID: mdl-34951254

RESUMEN

The present study investigated the differences in pharmacokinetics and intestinal absorption of six alkaloids in Sanmiao Pills and Simiao Pills in rats and explored the different efficacies of the two formulae. After oral administration of Sanmiao Pills and Simiao Pills in rats, blood samples were collected at different time points. Samples were prepared for the determination of six alkaloids in plasma by UPLC-MS/MS. The chromatography was performed on an ACE Excel 3 C_(18 )column with acetonitrile-0.1% formic acid in water as the mobile phase for gradient elution. Analytes were detected in the positive ion mode. Plasma concentrations and pharmacokinetic parameters were calculated. Intestinal absorption of alkaloids was investigated by single-pass intestinal perfusion and absorption parameters of ingredients were calculated. The results showed that the UPLC-MS/MS method for simultaneous determination of concentrations of six alkaloids in plasma was developed and validated by methodological investigations, such as specificity, calibration curves, precision, accuracy, recovery, matrix effect, and stability. The results of the pharmacokinetic assay revealed that C_(max) and AUC values of phellodendrine, berberine, magnoflorine, berberrubine, and jatrorrhizine in Simiao Pills were significantly increased, and CL/F values were reduced as compared with those in Sanmiao Pills, which indicated the increase in plasma concentrations of alkaloids. The intestinal absorption parameters K_(a )and P_(eff) values of phellodendrine, berberine, and jatrorrhizine in Simiao Pills were higher than those in Sanmiao Pills. The intestinal absorption and plasma concentrations of alkaloids in Simiao Pills were significantly higher than those in Sanmiao Pills, suggesting that the composition of Simiao Pills was more conducive to the alkaloids into the blood to resist inflammation and lower uric acid.


Asunto(s)
Alcaloides , Medicamentos Herbarios Chinos , Animales , Cromatografía Líquida de Alta Presión , Cromatografía Liquida , Absorción Intestinal , Ratas , Reproducibilidad de los Resultados , Espectrometría de Masas en Tándem
7.
Phytomedicine ; 82: 153458, 2021 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-33486267

RESUMEN

BACKGROUND: Ulcerative colitis (UC) is a chronic inflammatory bowel disease with high morbidity, which leads to poor quality of life. The Xianglian pill (XLP) is a classical Chinese patent medicine and has been clinically proven to be an effective treatment for UC. PURPOSE: The pharmacological mechanism of the key bioactive ingredients of XLP for the treatment of UC was investigated by a network pharmacology and pharmacokinetics integrated strategy. STUDY DESIGN AND METHODS: Network pharmacology was used to analyze the treatment effect of nine quantified XLP ingredients on UC. Key pathways were enriched and analyzed by protein-protein interaction and Kyoto Encyclopedia of Genes and Genomes analyses. The effect of XLP on Th17 cell differentiation was validated using a mouse model of UC. The binding of nine compounds with JAk2, STAT3, HIF-1α, and HSP90AB1 was assessed using molecular docking. A simple and reliable ultra-high-performance liquid chromatography-tandem mass spectrometry method was developed for the simultaneous quantification of nine ingredients from XLP in plasma and applied to a pharmacokinetic study following oral administration. RESULTS: Nine compounds of XLP, including coptisine, berberine, magnoflorine,berberrubine, jatrorrhizine, palmatine, evodiamine, rutaecarpine, and dehydrocostus lactone, were detected. Network pharmacology revealed 50 crossover genes between the nine compoundsand UC. XLP treats UC mainly by regulating key pathways of the immune system, including Th17 cell differentiation, Jak-Stat, and PI3K-Akt signaling pathways. An in vivo validation in mice found that XLP inhibits Th17 cell differentiation by suppressing the Jak2-Stat3 pathway, which alleviates mucosal inflammation in UC. Molecular docking confirmed that eight compounds are capable of binding with JAk2, HIF-1α, and HSP90AB1, further confirming the inhibitory effect of XLP on the Jak2-Stat3 pathway. Moreover, apharmacokinetic study revealed that the nine ingredients of XLP are exposed in the plasma and colon tissue, which demonstrates its pharmacological effect on UC. CONCLUSION: This study evaluates the clinical treatment efficacy of XLP for UC. The network pharmacology and pharmacokinetics integrated strategy evaluation paradigm is efficient in discovering the key pharmacological mechanism of herbal formulae.


Asunto(s)
Colitis Ulcerosa/tratamiento farmacológico , Medicamentos Herbarios Chinos/uso terapéutico , Administración Oral , Animales , Cromatografía Líquida de Alta Presión/métodos , Modelos Animales de Enfermedad , Medicamentos Herbarios Chinos/administración & dosificación , Medicamentos Herbarios Chinos/farmacocinética , Ratones , Simulación del Acoplamiento Molecular , Proteínas Quinasas/metabolismo , Calidad de Vida , Factor de Transcripción STAT3/metabolismo , Células Th17/efectos de los fármacos
8.
Artículo en Inglés | MEDLINE | ID: mdl-32565854

RESUMEN

The decoction is an important dosage form of traditional Chinese medicine (TCM) administration. The Mahuang Fuzi Xixin decoction (MFXD) is widely used to treat allergic rhinitis (AR) in China. However, its active compounds and therapeutic mechanisms are unclear. The aim of this study was to establish an integrative method to identify the bioactive compounds and reveal the mechanisms of action of MFXD. LC-MS/MS was used to identify the compounds in MFXD, followed by screening for oral bioavailability. TCMSP, BindingDB, STRING, DAVID, and KEGG databases and algorithms were used to gather information. Cytoscape was used to visualize the networks. Twenty-four bioactive compounds were identified, and thirty-seven predicted targets of these compounds were associated with AR. DAVID analysis suggested that these compounds exert their therapeutic effects by modulating the Fc epsilon RI, B-cell receptor, Toll-like receptor, TNF, NF-κB, and T-cell receptor signaling pathways. The PI3K/AKT and cAMP signaling pathways were also implicated. Ten of the identified compounds, quercetin, pseudoephedrine, ephedrine, ß-asarone, methylephedrine, α-linolenic acid, cathine, ferulic acid, nardosinone, and higenamine, seemed to account for most of the beneficial effects of MFXD in AR. This study showed that LC-MS/MS followed by network pharmacology analysis is useful to elucidate the complex mechanisms of action of TCM formulas.

9.
J Immunol Res ; 2020: 6841078, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32537469

RESUMEN

Mahuang Fuzi Xixin Decoction (MFXD), a Chinese traditional herbal formulation, has been used to treat allergic rhinitis (AR) in China for centuries. However, the mechanism underlying its effect on AR is unclear. This study investigated the mechanism underlying the therapeutic effects of MFXD on AR. Ovalbumin-induced AR rat models were established, which were then treated with MFXD for 14 days. Symptom scores of AR were calculated. The structure of the gut microbiota was analyzed by 16S rRNA gene sequencing and qPCR. Short-chain fatty acid (SCFA) content in rat stool and serum was determined by GC-MS. Inflammatory and immunological responses were assessed by histopathology, ELISA, flow cytometry, and western blotting. Our study demonstrated that MFXD reduced the symptom scores of AR and serum IgE and histamine levels. MFXD treatment restored the diversity of the gut microbiota: it increased the abundance of Firmicutes and Bacteroidetes and decreased the abundance of Proteobacteria and Cyanobacteria. MFXD treatment also increased SCFA content, including that of acetate, propionate, and butyrate. Additionally, MFXD administration downregulated the number of Th17 cells and the levels of the Th17-related cytokines IL-17 and RORγt. By contrast, there was an increase in the number of Treg cells and the levels of the Treg-related cytokines IL-10 and Foxp3. MFXD and butyrate increased the levels of ZO-1 in the colon. This study indicated MFXD exerts therapeutic effects against AR, possibly by regulating the gut microbial composition and Th17/Treg balance.


Asunto(s)
Antialérgicos/uso terapéutico , Medicamentos Herbarios Chinos/uso terapéutico , Microbioma Gastrointestinal/inmunología , Extractos Vegetales/uso terapéutico , Rinitis Alérgica/terapia , Linfocitos T Reguladores/inmunología , Células Th17/inmunología , Animales , Modelos Animales de Enfermedad , Humanos , Inmunoglobulina E/sangre , Masculino , Miembro 3 del Grupo F de la Subfamilia 1 de Receptores Nucleares/metabolismo , Ratas , Ratas Wistar
10.
Biomed Chromatogr ; 33(3): e4421, 2019 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-30362136

RESUMEN

Diarrhoeal diseases alter the composition of intestinal flora, thereby affecting the efficacy of herbal medicinal formulations. Gegen Qinlian decoction (GQD), a Chinese traditional herbal formulation, is widely used to treat infectious diarrhoea. However, little is known about the microbial disposition of GQD in the diarrhoeal state. In this study, the comparative metabolism of components of GQD by diarrhoeal and normal intestinal flora was investigated in vitro. UPLC-MS/MS was performed for simultaneous analysis of eight ingredients of GQD in bacterial solution. The type, activities, and sources of microbial enzymes were also investigated. Microbial metabolism of daidzin, genistin and liquiritin (metabolized by ß-glucosidase); baicalin, wogonoside and glycyrrhizin (metabolized by ß-glucuronidase); and berberine and coptisine (metabolized via nitroreductase) was faster in the diarrhoeal group than in the normal group. Moreover, the activities of these enzymes in the diarrhoeal group were higher than those in the normal group. This difference might be associated with the increase in Escherichia spp. Thus, a change in the metabolism of components by diarrhoeal intestinal flora is associated with a preponderance of Escherichia spp., which might improve the efficacy of GQD. These findings have implications for understanding the action mechanism of GQD for diarrhoea treatment in terms of the microbial milieu.


Asunto(s)
Bacterias/metabolismo , Diarrea/microbiología , Medicamentos Herbarios Chinos/análisis , Medicamentos Herbarios Chinos/metabolismo , Microbioma Gastrointestinal/fisiología , Animales , Bacterias/enzimología , Berberina/análisis , Berberina/metabolismo , Medicamentos Herbarios Chinos/química , Flavonoides/análisis , Flavonoides/metabolismo , Ácido Glicirrínico/análisis , Ácido Glicirrínico/metabolismo , Modelos Lineales , Reproducibilidad de los Resultados , Sensibilidad y Especificidad , Porcinos
11.
Artículo en Inglés | MEDLINE | ID: mdl-30562628

RESUMEN

Puerariae Radix (PR) and Gastrodiae Rhizome (GR) is frequently used in traditional herbal formulas to treat cardio-cerebral vascular diseases due to their synergistic effects. In this study, to elucidate the action mechanism of PR-GR in vivo, a simple and reliable ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method for simultaneous determination of nine bioactive ingredients from PR-GR in plasma was developed and applied to a comparative pharmacokinetic study following oral administration of PR, GR, and PR-GR aqueous extracts in rats. The effect of GR on the absorption of components of PR was also investigated by single-pass intestinal perfusion study. Results showed that comparing to the single herbs, PR-GR extract significantly increased the systemic exposure of puerarin, 3'-hydroxypuerarin, 3'-methoxypuerarin, 6″-O-xylosylpuerarin, daidzin, genistein, and gastrodin. Moreover, the intestinal absorption of puerarin and daidzin could be improved by GR extract and inhibitors of P-glycoprotein and multidrug resistanceassociated protein 2, respectively. These results indicate that the combination of PR and GR increases the levels of their bioactive ingredients exposed in the blood, and GR increases the absorption of ingredients of PR may by inhibition of the efflux mediated by P-glycoprotein and multidrug resistanceassociated protein 2. This is the first report for the pharmacokinetics and intestinal absorption of PR-GR, which may explain their synergetic effects in the treatment of circulatory systematic diseases and provide a meaningful insight for their clinical applications.


Asunto(s)
Medicamentos Herbarios Chinos/farmacocinética , Gastrodia/química , Absorción Intestinal/fisiología , Isoflavonas/farmacocinética , Pueraria/química , Animales , Cromatografía Líquida de Alta Presión/métodos , Medicamentos Herbarios Chinos/química , Íleon/metabolismo , Isoflavonas/análisis , Límite de Detección , Modelos Lineales , Ratas , Reproducibilidad de los Resultados , Espectrometría de Masas en Tándem/métodos
12.
Zhongguo Zhong Yao Za Zhi ; 43(23): 4724-4734, 2018 Dec.
Artículo en Chino | MEDLINE | ID: mdl-30717564

RESUMEN

A specific and selective UPLC-MS/MS method was developed and validated for the simultaneous determination of isoflavonoids(3'-hydroxy puerarin, puerarin, daidzin, daidzein, genistin, genistein), flavonoids (baicalin, baicalein, wogonoside, wogonin, liquiritin)and alkaloids(berberine, jatrorrhizine, palmatine)(14 bioactive compounds) of Gegen Qinlian Decoction(GQD) in plasma. The pharmacokinetics characteristics of 14 bioactive compounds were study after oral administration of GQD at a single dose to rats. Prednisolone was used as the internal standard of liquiritin, and naringin was used as the internal standard of the other thirteen analytes. After the plasma samples were processed by precipitation protein method, the constituents and internal standards were gradient eluted by using a Zorbax SB-18 column with a mobile phase of acetonitrile(A) and 0.1% formic acid aqueous solution(B) using a gradient elution of 0-2.5 min, 15%-30% A; 2.5-3.5 min, 30%-35% A; 3.5-5.0 min, 35%-40% A; 5.0-9.0 min, 40%-60% A; 9.0-11.0 min, 60%-15% A, and the flow rate was 0.4 mL·min⁻¹. The auto sampler was conditioned at 25 °C and the sample injection volume was 5 µL. A mass spectrometry was applied with electrospray ionization (ESI) ion source in the positive and negative ion multiple reaction monitoring(MRM) mode. All pharmacokinetic parameters were processed by non-compartmental analysis with DAS 3.2.2 software. The results showed that the linear correlation coefficient of the 14 components were all greater than 0.99, indicating that the method had good linearity in their respective concentration ranges. Post-preparative stability (25 °C, 24 h), short-term stability(25 °C, 12 h), long-term stability (-20 °C, 7 d), and freeze and thaw stability (3-cycles) of the fourteen constituents were examined to evaluate the stability of methodology. The results of the inner and inter-day relative standard deviations were both less than 10%, indicating legitimate precise and accuracy to the requirement of biological sample analysis. The assay method is proved to be sensitive, accurate and convenient. It can be applied to the pharmacokinetic study of the fourteen analytes. The kinetic parameters of the related drugs were calculated according to the blood concentration of the 14 components. The results showed that the MRT0-t of the isoflavones and flavonoids was 7.5-11.8 h, T1/2z were mainly in 11.0-29.7 h, and the AUC0-t flavonoids were larger than the isoflavones. The MRT0-t of alkaloids were between 4.3-7.2 h, T1/2z were 1.0-5.0 h, AUC0-t were less than flavonoids and isoflavones. The results suggest that flavonoids and isoflavones have a high concentration of blood and long time of action, which are beneficial to the anti-inflammatory and antipyretic effects. The concentration of alkaloids in the body is low and the time of action is short, and it may play its bacteriostasis in the intestinal tract.


Asunto(s)
Medicamentos Herbarios Chinos , Alcaloides , Animales , Cromatografía Líquida de Alta Presión , Cromatografía Liquida , Flavonoides , Ratas , Ratas Sprague-Dawley , Reproducibilidad de los Resultados , Espectrometría de Masas en Tándem
13.
Chin J Integr Med ; 22(6): 445-50, 2016 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-25399307

RESUMEN

OBJECTIVE: Mahuang-Shigao herb-pair is a famous formula composed of Ephedra and Gypsum. The herb-pair is frequently used for treating cold symptoms and bronchial asthma in the clinical practice of Chinese medicine (CM). In the present study, we evaluated evidence for the benefit of combined use of Ephedra and Gypsum by analyzing the antipyretic and anti-asthmatic activities of Ephedra-Gypsum. METHODS: The antipyretic effects of Ephedra-Gypsum were evaluated in yeast-induced hyperthermia test. Thirty male Wistar rats were randomly divided into 5 groups, including control group, standard aspirin group, and 3 Ephedra- Gypsum groups of different doses (6, 12, 24 g/kg). Ephedra-Gypsum extract and asprin were administered orally 6 h after the injection of yeast solution and body temperature was measured every 1 h for 8 h. The antiasthmatic effects of Ephedra-Gypsum were evaluated using an ovalbumin (OVA)-induced asthmatic rat model. Thirty-six male SD rats were randomly divided into 6 groups. Rats were alternately sensitized and OVA+Al(OH) challenged by exposure to mists of ovalbumin. Ephedra-Gypsum extracts (6, 12, 24 g/kg) or dexamethasone were administered 45 min prior to the allergen challenge for 8 days. Latent period and the weight of wet to dry ratio of lung were determined. In addition, the eosinophils in blood and white blood cell (WBC) were counted by an YZ-Hemavet Analyzer. RESULTS: The Ephedra-Gypsum extracts at test dose (6, 12, 24 g/kg) significantly and dose-dependently attenuated yeast-induced fever in rats. The Ephedra-Gypsum extracts also prolonged the latent period, reduced OVA-induced increases in eosinophils and WBC, and decreased the wet and dry weight ratio of the lungs in the anti-asthmatic test. CONCLUSIONS: These findings indicate that the Ephedra-Gypsum extract has antipyretic and anti-asthmatic properties. Hence, the results support additional scientific evidence in prescriptions.


Asunto(s)
Antiasmáticos/uso terapéutico , Antipiréticos/uso terapéutico , Sulfato de Calcio/uso terapéutico , Medicamentos Herbarios Chinos/uso terapéutico , Ephedra/química , Extractos Vegetales/uso terapéutico , Alcaloides/análisis , Animales , Asma/tratamiento farmacológico , Fiebre/tratamiento farmacológico , Pulmón/efectos de los fármacos , Pulmón/patología , Masculino , Tamaño de los Órganos/efectos de los fármacos , Ovalbúmina , Ratas Sprague-Dawley , Ratas Wistar
14.
Zhongguo Zhong Yao Za Zhi ; 40(10): 1971-6, 2015 May.
Artículo en Chino | MEDLINE | ID: mdl-26390658

RESUMEN

To investigate me material basis of Mahuang Fuzi Xixin decoction (MFXD) for anti-inflammation and immune-suppression based on the combined method of serum chemical and serum pharmacological. The LC-MS/MS fingerprints of MFXD, drug-containing serum and blank serum were compared to define the components in plasma. Histamine, ß-hexosaminidase released from RBL-2H3 cell infulenced by drug-containing serum at different time points were measured by ELISA. The effect of drug-containing serum on lipopolysaccharide-induced splenocyte proliferation at different time points were determined by MTT. A correlation analysis was made on components of MFXD and pharmacological indexes based the stepwise regression method. After the intragastrical administration with MFXD, 32 components were discovered in rat serum, including 27 prototype components (10 from Mahuang, 13 from Fuzi and four from Xixin) and five unknown components. Compared with blank serum, drug-containing serum could reduce the release of histamine from RBL-2H3 induced by antigen at different time points (P < 0.05); except the 4-hour drug-containing serum, all of the remaining drug-containing serums could inhibit the RBL-2H3 mastocyte degranulation induced by antigen at different time points (P < 0.05). Drug-containing serum could significantly lipopolysaccharide-induced mouse splenocyte proliferation at 15 and 30 min (P < 0.05). A regression analysis was made on the chemical data of components absorbed into blood and pharmacological indexes, i. e. release rate of histamine, release rate of ß-hexosaminidase and inhibition rate of splenocyte. This suggested the close correlations among methyl pseudo-ephedrine, pseudoephedrine and histamine released from RBL-2H3 induced by antigen; pseudoephedrine, hypaconine, methyl pseudoephedrine and ß-hexosaminidase released from RBL-2H3 induced by antigen; as well as benzoyl hypaconine, benzoylaconine, 14-benzoyl-10-OH-mesaconine, mesaconine and lipopolysaccharide-induced mouse splenocyte proliferation. Methylpseudoephedrine, pseudoephedrine, benzoyl hypaconine, benzoylaconine and mesaconine may be part of material basis of MFXD on anti-inflammation and immune suppression.


Asunto(s)
Antiinflamatorios/farmacología , Medicamentos Herbarios Chinos/farmacología , Inmunosupresores/farmacología , Mastocitos/efectos de los fármacos , Suero/química , Animales , Antiinflamatorios/química , Degranulación de la Célula/efectos de los fármacos , Medicamentos Herbarios Chinos/química , Femenino , Histamina/inmunología , Inmunosupresores/química , Masculino , Espectrometría de Masas , Mastocitos/inmunología , Ratones , Ratas , Ratas Wistar
15.
Artículo en Inglés | MEDLINE | ID: mdl-25691910

RESUMEN

Herb Ephedra (Ma Huang in Chinese) and Ramulus Cinnamomi (Gui Zhi in Chinese) are traditional Chinese herbs, often used together to treat asthma, nose and lung congestion, and fever with anhidrosis. Due to the adverse effects of ephedrine, clinical use of Ma Huang is restricted. However, Gui Zhi extract has been reported to decrease spontaneous activity in rats and exert anti-inflammatory and neuroprotective effects. The present study explored the possible inhibitory effect of Gui Zhi on Ma Huang-induced neurotoxicity in rats when the two herbs were used in combination. All Ma Huang and Ma Huang-Gui Zhi herb pair extracts were prepared using methods of traditional Chinese medicine and were normalized based on the ephedrine content. Two-month-old male Sprague-Dawley rats (n = 6 rats/group) were administered Ma Huang or the Ma Huang-Gui Zhi herb pair extracts for 7 days (ephedrine = 48 mg/kg), and locomotor activity was measured. After 7 days, oxidative damage in the prefrontal cortex was measured. Gui Zhi decreased hyperactivity and sensitization produced by repeated Ma Huang administration and attenuated oxidative stress induced by Ma Huang. The results of this study demonstrate the neuroprotective potential of Gui Zhi in Ma Huang-induced hyperactivity and oxidative damage in the prefrontal cortex of rats when used in combination.

16.
J Ethnopharmacol ; 155(1): 642-8, 2014 Aug 08.
Artículo en Inglés | MEDLINE | ID: mdl-24929107

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Herba Ephedra (Mahuang in Chinese), is derived from dried Ephedra sinica Stapf stems and has been widely used to treat the common cold, coughs, asthma, and edema for thousands of years. The Mahuang-Guizhi herb-pair is a famous formula composed of Mahuang and Ramulus Cinnamomi (Guizhi in Chinese, the dried twig of Cinnamomum cassia Presl.), used to improve pharmacological effects and reduce toxicity. In order to investigate the influence of Mahuang-Guizhi herb-pair ratios on bioavailability, the plasma pharmacokinetics profiles of five ephedrine alkaloids were compared following oral administration of four different ratios to rats. MATERIALS AND METHODS: Sprague-Dawley rats were randomly assigned to four groups and orally administered Mahuang-Guizhi (ratios 3:0; 3:1; 3:2; 3:4, w/w). Assays for five ephedrine alkaloids (ephedrine, pseudoephedrine, methylephedrine, norephedrine, and norpseudoephedrine) were developed and validated using ultra-high-performance liquid chromatography tandem mass spectrometry coupled with liquid-liquid extraction. RESULTS: Key pharmacokinetic parameters of the five ephedrine alkaloids (maximal plasma concentration, mean residence time, and half-life) were significantly different (p<0.05) after oral administration of Mahuang-Guizhi herb-pair ratios, as compared to those of Mahuang. CONCLUSION: Ephedrine alkaloid pharmacokinetic differences in rat plasma could help explain previous findings of pharmacological and toxicity differences between Mahuang and Mahuang-Guizhi herb-pair preparations. These results could facilitate future studies to increase the efficacy and decrease the toxicity of Mahuang and Guizhi.


Asunto(s)
Alcaloides/farmacocinética , Cinnamomum aromaticum/química , Ephedra sinica/química , Administración Oral , Alcaloides/administración & dosificación , Alcaloides/aislamiento & purificación , Animales , Disponibilidad Biológica , Cromatografía Líquida de Alta Presión/métodos , Semivida , Extracción Líquido-Líquido , Ratas , Ratas Sprague-Dawley , Espectrometría de Masas en Tándem/métodos
17.
Zhong Yao Cai ; 35(5): 686-9, 2012 May.
Artículo en Chino | MEDLINE | ID: mdl-23213726

RESUMEN

OBJECTIVE: To improve the quality standard of Scolopendra subspinipes mutilans by researching the methods of the TLC identification and anti-coagulant activity quantitatively. METHODS: Identified the free arginine (Arg) and serine (Ser) in scolopendra by TLC, screened the samples preparation process and developed solvent systems; Determined the anti-coagulant activity by method of titration with thrombin and screened the pretreatment methods. RESULTS: When medicinal materials was extracted by formic acid and 95% ethanol (1:1) with ultrasonic method and developed by n-butanol-acetic acid-water (12:5:4), the spots of Arg and Ser were well separated. Ultrasonic method was suitable for preparation of the anti-coagulant components in Scolopendra subspinipes mutilans and their anti-coagulant activity was determined by method of titration with thrombin could get a well reproducibility, the anti-thrombin activity of testing sample was (14.00 +/- 1.53) U/g and those of three different batch were (13.00 +/- 0.58) U/g, (17.00 +/- 1.15) U/g, (15.67 +/- 1.53) U/g respectively. CONCLUSION: The methods of TLC identification and anti-coagulant activity quantitatively could be used as a basis for improving the quality standard of Scolopendra subspinipes mutilans.


Asunto(s)
Anticoagulantes/farmacología , Artrópodos , Materia Medica/química , Materia Medica/farmacología , Trombina/análisis , Animales , Anticoagulantes/química , Anticoagulantes/aislamiento & purificación , Arginina/análisis , Artrópodos/química , Cromatografía en Capa Delgada/métodos , Materia Medica/aislamiento & purificación , Control de Calidad , Reproducibilidad de los Resultados , Serina/análisis , Tecnología Farmacéutica/métodos , Trombina/antagonistas & inhibidores , Volumetría/métodos
18.
Zhong Yao Cai ; 34(6): 896-901, 2011 Jun.
Artículo en Chino | MEDLINE | ID: mdl-22017005

RESUMEN

OBJECTIVE: To evaluate the correlativity between volatile oils of Mahuang Fuzi Xixin decoction and its major constituted herbs in composition and proportion. METHODS: The chemical compositions of volatile oils obtained by wet distillation from Mahuang Fuzi Xixin decoction and its major constituted herbs (Herba Ephedrae, processed Radix Aconiti Lateralis, Herba Asari) were analyzed by GC-MS. RESULTS: 44 volatile components of Mahuang Fuzi Xixin decoction were identified, which mainly derived from its constituted herbs Mahuang and Xixin. 68, 8, 39 volatile components were respectively identified from volatile oils of Herba Epherae, processd Radix Aconiti Lateralis and Herba Asari. There were apparent changes in composition and proportion between volatile oils of Mahuang Fuzi Xixin decoction and its major constituted herbs. CONCLUSION: There are apparent changes not only in quantity but also in quality between decoction and its major constituted herbs. Meanwhile any changes in composition may lead to a change in efficacy.


Asunto(s)
Aconitum/química , Asarum/química , Medicamentos Herbarios Chinos/química , Ephedra sinica/química , Aceites Volátiles/análisis , Medicamentos Herbarios Chinos/análisis , Cromatografía de Gases y Espectrometría de Masas/métodos , Aceites Volátiles/química , Plantas Medicinales/química
19.
Zhong Yao Cai ; 33(11): 1791-4, 2010 Nov.
Artículo en Chino | MEDLINE | ID: mdl-21434444

RESUMEN

OBJECTIVE: To investigate the multiple bioactive constituents in Gegen Qinlian decoction and evaluate its bioactivity and quality control. METHODS: A high performance liquid chromatography with diode array detection (HPLC-DAD) method for the simultaneous qualitative determination of multiple components was developed. The separation was performed on a Kromasil C18 column by gradient elution with acetonitrile and ammonium acetate (containing 0.3% triethylamine, and adjusted pH 4. 3 using 1% glacial acetic acid) as the mobile phase at a flow-rate of 0.7 mL/min, the column temperature was maintained at 30 degrees C, HPLC chromatographic comparison between Gegen Qinlian decoction, four medicinal material and 14 components were carried out to investigate components in the composite formula. RESULTS: 23 characteristic peaks were identified and could be dated back to four medicinal materials from Gegen Qinlian decoction, in which 12 peaks were identifed by standards. CONCLUSION: This readily available, low-cost and reliable HPLC-DAD method can be used for simultaneous analysis of multiple bioactive constituents of Gegen Qinlian decoction and will improve the quality control of Gegen Qinlian decoction.


Asunto(s)
Cromatografía Líquida de Alta Presión/métodos , Medicamentos Herbarios Chinos/química , Flavonas/análisis , Plantas Medicinales/química , Alcaloides/análisis , Combinación de Medicamentos , Medicamentos Herbarios Chinos/aislamiento & purificación , Raíces de Plantas/química , Control de Calidad , Reproducibilidad de los Resultados , Saponinas/análisis
20.
Zhong Yao Cai ; 30(3): 297-9, 2007 Mar.
Artículo en Chino | MEDLINE | ID: mdl-17634037

RESUMEN

OBJECTIVE: To identify Eevodia rutaecarpa (Juss.) Benth and determine the contents of the total alkaloid of Rhizoma Coptidis in Yuhuanglian extract. METHODS: Thin layer chromatography (TLC) was used for the identification of Evodia rutaecarpa (Juss.) Benth with a mixed solvent of cyclohexane-ethyl acetate-methanol-triethylamine (19:5:1:1) as the developer and spraying with 10% sulfuric acid ethanol solution as colorimetric method. The contents of the total alkaloid of Rhizoma Coptidis was determined by UV spectrophometry in Yuhuanglian extract and the detection wavelength was 349 nm. RESULTS: Special spots could be observed at 365 nm on positions corresponding to Evodia rutaecarpa (Juss.) Benth, and the preparation, while the negative control showed no spots. The linear range of berberine hydrochloric was 1.04-11.44 microg/ml, r = 0.9999; the average recovery was 99.2%, and RSD was 1.0% (n=5). CONCLUSIONS: Evodia rutaecarpa (Juss.) Benth can be identified simply and fast using TLC and the method to determine the contents of the total alkalid of Rhizoma Coptidis by UV spectrophometry is accurate, rapid and simple. It can be used for quality control of Yuhuanglian extract.


Asunto(s)
Alcaloides/análisis , Evodia/química , Extractos Vegetales/análisis , Cromatografía en Capa Delgada , Control de Calidad
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