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1.
Biomed Chromatogr ; 36(1): e5254, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34605575

RESUMO

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.


Assuntos
Alcaloides , Medicamentos de Ervas Chinesas , Absorção Intestinal/efeitos dos fármacos , Alcaloides/sangue , Alcaloides/farmacocinética , Alcaloides/urina , Animais , Cromatografia Líquida , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacocinética , Limite de Detecção , Modelos Lineares , Masculino , Ratos , Ratos Sprague-Dawley , Reprodutibilidade dos Testes , Espectrometria de Massas em Tandem
2.
Food Res Int ; 150(Pt A): 110717, 2021 12.
Artigo em Inglês | MEDLINE | ID: mdl-34865748

RESUMO

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.


Assuntos
Coix , Diabetes Mellitus Tipo 2 , Microbioma Gastrointestinal , Animais , Coix/metabolismo , Diabetes Mellitus Tipo 2/tratamento farmacológico , Ácidos Graxos Voláteis , Humanos , Fator de Crescimento Insulin-Like I , Camundongos , Simulação de Acoplamento Molecular , Fosfatidilinositol 3-Quinases/metabolismo , Polissacarídeos/farmacologia , Proteínas Proto-Oncogênicas c-akt/metabolismo , Transdução de Sinais
3.
Zhongguo Zhong Yao Za Zhi ; 46(23): 6271-6277, 2021 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-34951254

RESUMO

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.


Assuntos
Alcaloides , Medicamentos de Ervas Chinesas , Animais , Cromatografia Líquida de Alta Pressão , Cromatografia Líquida , Absorção Intestinal , Ratos , Reprodutibilidade dos Testes , Espectrometria de Massas em Tandem
4.
Phytomedicine ; 82: 153458, 2021 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-33486267

RESUMO

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.


Assuntos
Colite Ulcerativa/tratamento farmacológico , Medicamentos de Ervas Chinesas/uso terapêutico , Administração Oral , Animais , Cromatografia Líquida de Alta Pressão/métodos , Modelos Animais de Doenças , Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/farmacocinética , Camundongos , Simulação de Acoplamento Molecular , Proteínas Quinases/metabolismo , Qualidade de Vida , Fator de Transcrição STAT3/metabolismo , Células Th17/efeitos dos fármacos
5.
Artigo em Inglês | MEDLINE | ID: mdl-32565854

RESUMO

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.

6.
J Immunol Res ; 2020: 6841078, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32537469

RESUMO

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.


Assuntos
Antialérgicos/uso terapêutico , Medicamentos de Ervas Chinesas/uso terapêutico , Microbioma Gastrointestinal/imunologia , Extratos Vegetais/uso terapêutico , Rinite Alérgica/terapia , Linfócitos T Reguladores/imunologia , Células Th17/imunologia , Animais , Modelos Animais de Doenças , Humanos , Imunoglobulina E/sangue , Masculino , Membro 3 do Grupo F da Subfamília 1 de Receptores Nucleares/metabolismo , Ratos , Ratos Wistar
7.
Int J Nanomedicine ; 15: 2059-2070, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32273702

RESUMO

PURPOSE: Ferulic acid (FA) is a natural compound which is used to treat insomnia. However, its use is limited because of its poor oral bioavailability caused by extremely rapid elimination. The current study aimed to develop a self-microemulsifying drug delivery system (SMEDDS) to improve the oral delivery of FA and to enhance its hypnotic efficacy. METHODS: FA-SMEDDS was prepared, and its morphology and storage stability were characterized. The formulation was also subjected to pharmacokinetic and tissue distribution studies in rats. The hypnotic efficacy of FA-SMEDDS was evaluated in p-chlorophenylalanine-induced insomnia mice. RESULTS: FA-loaded SMEDDS exhibited a small droplet size (15.24 nm) and good stability. Oral administration of FA-SMEDDS yielded relative bioavailability of 185.96%. In the kidney, SMEDDS decreased the distribution percentage of FA from 76.1% to 59.4% and significantly reduced its metabolic conversion, indicating a reduction in renal elimination. Interestingly, FA-SMEDDS showed a higher distribution in the brain and enhanced serotonin levels in the brain, which extended the sleep time by 2-fold in insomnia mice. CONCLUSION: This is the first study to show that FA-loaded SMEDDS decreased renal elimination, enhanced oral bioavailability, increased brain distribution, and improved hypnotic efficacy. Thus, we have demonstrated that SMEDDS is a promising carrier which can be employed to improve the oral delivery of FA and facilitate product development for the therapy of insomnia.


Assuntos
Ácidos Cumáricos/administração & dosagem , Sistemas de Liberação de Medicamentos/métodos , Emulsões/administração & dosagem , Hipnóticos e Sedativos/administração & dosagem , Administração Oral , Animais , Disponibilidade Biológica , Ácidos Cumáricos/química , Ácidos Cumáricos/farmacocinética , Portadores de Fármacos/química , Emulsões/química , Hipnóticos e Sedativos/química , Hipnóticos e Sedativos/farmacocinética , Masculino , Camundongos , Ratos Wistar , Distúrbios do Início e da Manutenção do Sono/tratamento farmacológico , Solubilidade , Distribuição Tecidual
8.
Front Microbiol ; 10: 825, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31057525

RESUMO

Gut microbiota and its metabolites, short-chain fatty acids (SCFAs), play important roles in diarrheal diseases. Gegen Qinlian decoction (GQD), a Chinese herb formula, has been widely used to treat infectious diarrhea for centuries. However, little is known about the mechanism underlying its efficacy and whether it is mediated by gut microbiota and SCFAs. In this study, the composition of gut microbiota from bacterial diarrheal piglets was assessed using 16S rRNA analysis. The concentrations of fecal SCFAs were determined using a gas chromatography-mass spectrometer (GC-MS). The expression of mucosal pro-inflammatory cytokines in the colon was ascertained. Results showed that GQD reverses the reduction in the richness of gut microbiota, changes its structure, and significantly increases the relative abundances of SCFA-producing bacteria, including Akkermansia, Bacteroides, Clostridium, Ruminococcus, and Phascolarctobacterium. Moreover, GQD increased the levels of fecal SCFAs, including acetic acid, propionic acid, and butyric acid. GQD thus attenuates diarrhea in piglets. Further, our results suggest that the SCFAs could help to attenuate mucosal pro-inflammatory responses following GQD treatment by inhibiting histone deacetylase and the NF-κB pathway. We thus suggseted that gut microbiota play an important role during diarrhea treatment, an effect may be promoted by the GQD-induced structural changes of the gut microbial community and production of SCFAs. The increased levels of SCFAs probably provide further help to attenuate mucosal inflammation and diarrhea. In conclusion, our study might provide evidence that GQD treats diarrhea maybe involved in modulating gut microbiota and increasing SCFA levels.

9.
Gynecol Obstet Invest ; 84(5): 503-511, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31117092

RESUMO

BACKGROUND: There are few studies on the relative factors related to postoperative recurrence. OBJECTIVES: To compare the outcomes of pelvic floor reconstruction involving Herniamesh mesh and biological grafts and to investigate the correlative factors of postoperative recurrence. METHOD: Two hundred and thirty-two patients were randomly divided into 2 groups: Herniamesh mesh group (117) and biological graft group (115). Follow-ups for 6 months and 1 year after the surgery. The primary outcomes were recurrence, perioperative complications. Secondary outcome was a questionnaire about the life habits associated with relapse. RESULTS: The recurrence rate at 6 months or 1 year did not differ substantially between the 2 groups (p = 0.787 and 0.968, respectively). Adverse events occurred with significantly different frequencies over 1 year (p = 0.005). Twelve factors were investigated and analyzed by logistic regression analysis. It showed that recurrence had a strong association with a long-term vegetarian diet (OR 0.283, 95% CI 0.117-0.683), long-term soybean product diet (OR 8.010, 95% CI 2.514-25.523), and vaginal intercourse (OR 5.154, 95% CI 1.461-18.184). CONCLUSIONS: The surgical recurrence rate for the mesh was similar to biological grafts at short-term follow-up. Eating soy products often and vaginal intercourse after surgery can reduce recurrence.


Assuntos
Prolapso de Órgão Pélvico/cirurgia , Pelve/cirurgia , Procedimentos Cirúrgicos Reconstrutivos/métodos , Telas Cirúrgicas , Transplantes , Idoso , Feminino , Humanos , Pessoa de Meia-Idade , Recidiva , Fatores de Risco , Método Simples-Cego , Inquéritos e Questionários , Resultado do Tratamento
10.
Biomed Chromatogr ; 33(3): e4421, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30362136

RESUMO

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.


Assuntos
Bactérias/metabolismo , Diarreia/microbiologia , Medicamentos de Ervas Chinesas/análise , Medicamentos de Ervas Chinesas/metabolismo , Microbioma Gastrointestinal/fisiologia , Animais , Bactérias/enzimologia , Berberina/análise , Berberina/metabolismo , Medicamentos de Ervas Chinesas/química , Flavonoides/análise , Flavonoides/metabolismo , Ácido Glicirrízico/análise , Ácido Glicirrízico/metabolismo , Modelos Lineares , Reprodutibilidade dos Testes , Sensibilidade e Especificidade , Suínos
11.
Artigo em Inglês | MEDLINE | ID: mdl-30562628

RESUMO

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.


Assuntos
Medicamentos de Ervas Chinesas/farmacocinética , Gastrodia/química , Absorção Intestinal/fisiologia , Isoflavonas/farmacocinética , Pueraria/química , Animais , Cromatografia Líquida de Alta Pressão/métodos , Medicamentos de Ervas Chinesas/química , Íleo/metabolismo , Isoflavonas/análise , Limite de Detecção , Modelos Lineares , Ratos , Reprodutibilidade dos Testes , Espectrometria de Massas em Tandem/métodos
12.
Zhongguo Zhong Yao Za Zhi ; 43(23): 4724-4734, 2018 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-30717564

RESUMO

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.


Assuntos
Medicamentos de Ervas Chinesas , Alcaloides , Animais , Cromatografia Líquida de Alta Pressão , Cromatografia Líquida , Flavonoides , Ratos , Ratos Sprague-Dawley , Reprodutibilidade dos Testes , Espectrometria de Massas em Tandem
13.
Opt Express ; 25(17): 20923-20931, 2017 Aug 21.
Artigo em Inglês | MEDLINE | ID: mdl-29041768

RESUMO

We experimentally demonstrate the generation of dissipative soliton resonance (DSR) in a passively mode-locked Bi-doped fiber ring laser based on nonlinear polarization rotation (NPR) technique. The DSR with the central wavelength of 1169.5 nm has a repetition rate of 343.7 kHz. By purely increasing the pump power, the DSR evolves from Gaussian shape to rectangular shape with the duration extending from 2.1 ns to 13.1 ns, while keeping the pulse amplitude and the 3-dB spectrum bandwidth almost constant. The single-pulse energy reaches 24.82 nJ. Furthermore, we construct a lumped model to reproduce the mode-locking process and the traits of the DSR pulse. The obtained results indicate that it could achieve higher pulse energy in mode-locked Bi-doped fiber laser by generating DSR.

14.
Opt Express ; 25(14): 16291-16299, 2017 Jul 10.
Artigo em Inglês | MEDLINE | ID: mdl-28789136

RESUMO

We demonstrate a tunable and switchable dual-waveband 100 GHz high-repetition-rate (HRR) ultrafast fiber laser based on dissipative four-wave-mixing (DFWM) mode-locked technique. Each waveband maintains HRR operation. The DFWM effect was realized by combining a Fabry-Perot (F-P) filter and a piece of highly nonlinear fiber (HNLF). The tunable and switchable operations were achieved by nonlinear polarization rotation (NPR) technique. Through appropriately controlling the filtering effect induced by NPR, the laser could operate at two kinds of tunable regimes. One is that the spacing between these two wavebands could be tuned while keeping their center at 1559 nm. The other is that the central position of the entire dual-waveband is tunable while with the same separation between these two wavebands of 13.2 nm. Moreover, the laser could switch between these two wavebands. Correspondingly, the center of the single-waveband has a tuning range of 15.2 nm. This versatile ultrafast fiber laser may find applications in fields of optical frequency combs, high speed optical communications, where HRR pulses are necessary.

15.
Chin J Integr Med ; 22(6): 445-50, 2016 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-25399307

RESUMO

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.


Assuntos
Antiasmáticos/uso terapêutico , Antipiréticos/uso terapêutico , Sulfato de Cálcio/uso terapêutico , Medicamentos de Ervas Chinesas/uso terapêutico , Ephedra/química , Extratos Vegetais/uso terapêutico , Alcaloides/análise , Animais , Asma/tratamento farmacológico , Febre/tratamento farmacológico , Pulmão/efeitos dos fármacos , Pulmão/patologia , Masculino , Tamanho do Órgão/efeitos dos fármacos , Ovalbumina , Ratos Sprague-Dawley , Ratos Wistar
16.
Zhongguo Zhong Yao Za Zhi ; 40(10): 1971-6, 2015 May.
Artigo em Chinês | MEDLINE | ID: mdl-26390658

RESUMO

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.


Assuntos
Anti-Inflamatórios/farmacologia , Medicamentos de Ervas Chinesas/farmacologia , Imunossupressores/farmacologia , Mastócitos/efeitos dos fármacos , Soro/química , Animais , Anti-Inflamatórios/química , Degranulação Celular/efeitos dos fármacos , Medicamentos de Ervas Chinesas/química , Feminino , Histamina/imunologia , Imunossupressores/química , Masculino , Espectrometria de Massas , Mastócitos/imunologia , Camundongos , Ratos , Ratos Wistar
17.
Artigo em Inglês | MEDLINE | ID: mdl-25691910

RESUMO

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.

18.
J Ethnopharmacol ; 155(1): 642-8, 2014 Aug 08.
Artigo em Inglês | MEDLINE | ID: mdl-24929107

RESUMO

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.


Assuntos
Alcaloides/farmacocinética , Cinnamomum aromaticum/química , Ephedra sinica/química , Administração Oral , Alcaloides/administração & dosagem , Alcaloides/isolamento & purificação , Animais , Disponibilidade Biológica , Cromatografia Líquida de Alta Pressão/métodos , Meia-Vida , Extração Líquido-Líquido , Ratos , Ratos Sprague-Dawley , Espectrometria de Massas em Tandem/métodos
19.
Zhong Yao Cai ; 36(4): 589-93, 2013 Apr.
Artigo em Chinês | MEDLINE | ID: mdl-24134007

RESUMO

OBJECTIVE: To establish a method to determine the concentration of formononetin, calycosin and isorhamnetin from Astragalus mongholicus in rats' plasma using LC-MS/MS and calculate their pharmacokinetic parameters. METHODS: The contents of formononetin, calycosin and isorhamnetin in plasma were detected before and 24 h after 10 rats were treated with 10 g/kg Astragalus mongholicus. Rutin was used as internal standard. Agilent 1 200 HPLC system with Alltima C18 (150 mm x 2.1 mm, 5 microm) was used. Mobile phase was methanol-water solution with gradient elute at a flow rate of 0.3 mL/min. The column temperature was 40 degrees C. The LC-MS/ MS system was operated using an electrospray ionization probe in negative ion mode; Scan mode: multiple reaction ion monitoring (MRM) mode. The ion of monitor: m/z 267.0 --> 251.9 for formononetin, m/z 283.1 --> 268.2 for calycosin, m/z 315.4 --> 300.1 for isorhamnetin and m/z 609.4 --> 300.1 for rutin (internal standard), respectively. RESULTS: The linear range of formononetin, calycosin and isorhamnetin was 5 - 1 000 (r = 0.9996), 3.91 - 500 (r = 0.9989) and 0.5 - 100 ng/mL (r = 0.9992), respectively. The lowest limit of quantification (LLOQ) of formononetin, calycosin and isorhamnetin was 0.625, 0.5 and 0.1 ng/mL, respectively. The pharmacokinetic parameter, t(1/2beta), of formononetin, calycosin and isorhamnetin was (10.43 +/- 2.94), (6.91 +/- 1.33) and (5.07 +/- 1.21) h, respectively. The C(max) of formononetin, calycosin and isorhamnetin was (398.5 +/- 103.7), (138.7 +/- 32.8) and (58.3 +/- 14.5) ng/mL, respectively. The AUC(0 -> 12h), of formononetin, calycosin and isorhamnetin was (1238.8 +/- 311.3), (669.5 +/- 159.7) and (274.1 +/- 83.9)ng x h/mL, respectively. CONCLUSION: A sensitive, accuracy and suitable LC-MS/MS method for determination of formononetin, calycosin and isorhamnetin is developed and successfully applied to the pharmacokinetic study of 10 g/kg Astragalus mongholicus after oral administration in rats.


Assuntos
Astrágalo (Planta)/química , Isoflavonas/sangue , Quercetina/análogos & derivados , Administração Oral , Animais , Cromatografia Líquida , Isoflavonas/química , Isoflavonas/farmacocinética , Masculino , Quercetina/sangue , Quercetina/química , Quercetina/farmacocinética , Ratos , Ratos Sprague-Dawley , Reprodutibilidade dos Testes , Espectrometria de Massas em Tandem
20.
Zhong Yao Cai ; 35(5): 686-9, 2012 May.
Artigo em Chinês | MEDLINE | ID: mdl-23213726

RESUMO

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.


Assuntos
Anticoagulantes/farmacologia , Artrópodes , Materia Medica/química , Materia Medica/farmacologia , Trombina/análise , Animais , Anticoagulantes/química , Anticoagulantes/isolamento & purificação , Arginina/análise , Artrópodes/química , Cromatografia em Camada Delgada/métodos , Materia Medica/isolamento & purificação , Controle de Qualidade , Reprodutibilidade dos Testes , Serina/análise , Tecnologia Farmacêutica/métodos , Trombina/antagonistas & inibidores , Titulometria/métodos
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