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1.
Food Chem ; 335: 127600, 2021 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-32736155

RESUMO

Toosendanin (TSN), as an important Chinese traditional insecticide, has been registered and commercialized in China. In this report, the residual analytical methods, residue dynamics and final residues of TSN in tobacco, cabbage and soil under field condition were studied by IC-ELISA and HPLC. The sensitivity, precision and repeatability of IC-ELISA method were more suitable in comparison with HPLC for the demand of TSN residue analysis. Using IC-ELISA, the half-lives (t1/2) of TSN were found to be 1.30 days in cabbage, 1.70 days in tabacco and 0.71 days in soil, respectively. At the recommended dose, the final residues of TSN detection by IC-ELISA was 0.009 mg·kg-1 in cabbage and 0.043 mg·kg-1 in tobacco, as well as was not detected in soil. Therefore, TSN is easily degradable, and IC-ELISA could be a convenient and supplemental analytical tool for monitoring TSN residue in crops and environment.


Assuntos
Brassica/metabolismo , Medicamentos de Ervas Chinesas/metabolismo , Ensaio de Imunoadsorção Enzimática/métodos , Poluentes do Solo/metabolismo , Solo/química , China , Cromatografia Líquida de Alta Pressão/métodos , Meia-Vida , Cinética , Resíduos de Praguicidas/análise , Tabaco
2.
J Chromatogr A ; 1624: 461228, 2020 Aug 02.
Artigo em Inglês | MEDLINE | ID: mdl-32540070

RESUMO

Processing of traditional Chinese medicine (TCM) can enhance the efficacy and/or reduce the toxicity. Currently available approaches regarding TCM processing generally focus on a few markers, rendering a one-sided strategy that fail to unveil the involved global chemical transformation. We herein present a strategy, by integrating enhanced multicomponent characterization, untargeted metabolomics, and mass spectrometry imaging (MSI), to visualize the chemical transformation and identify the markers associated with the wine steaming of Ligustri Lucidi Fructus (LLF), as a case. An ultra-high-performance liquid chromatography/quadrupole-Orbitrap mass spectrometry-based polarity-switching (between the negative and positive modes), precursor ions list-including data-dependent acquisition approach was developed, which enabled the simultaneous targeted/untargeted characterization of 158 components from LLF via one injection analysis. Holistic, continuous, and time-dependent chemical variation trajectory, among different processing time (0-12 h) for LLF, was depicted by principle component analysis. Pattern recognition chemometrics could unveil 20 markers, among which the peak area ratios of eight components to oleuropein aglycone, used as an internal standard, were diagnostic to identify the processed (both the commercial and in-house prepared) from the raw LLF. Four markers (10-hydroxyoleoside dimethylester, 8-demethyl-7-ketoliganin, elenolic acid, and salidroside) showed an increasing trend, while another four (neonuezhenide/isomer, verbascoside/isomer, luteoline, and nuzhenal A) decreased in LLF after processing. MSI visualized the spatial distribution in the fruit and indicated consistent variation trends for four major markers deduced by the untargeted metabolomics approach. This integral strategy, in contrast to the conventional approaches, gives more convincing data supporting the processing mechanism investigations of TCM from a macroscopic perspective.


Assuntos
Medicamentos de Ervas Chinesas/química , Ligustrum/química , Metabolômica/métodos , Cromatografia Líquida de Alta Pressão , Análise Discriminante , Medicamentos de Ervas Chinesas/metabolismo , Frutas/química , Frutas/metabolismo , Ligustrum/metabolismo , Espectrometria de Massas , Análise de Componente Principal , Vapor , Vinho
3.
Adv Exp Med Biol ; 1241: 139-166, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32383120

RESUMO

Environmental and iatrogenic exposures contribute significantly to human diseases, including cancer. The list of known human carcinogens has recently been extended by the addition of aristolochic acids (AAs). AAs occur primarily in Aristolochia herbs, which are used extensively in folk medicines, including Traditional Chinese Medicine. Ingestion of AAs results in chronic renal disease and cancer. Despite importation bans imposed by certain countries, herbal remedies containing AAs are readily available for purchase through the internet. With recent advancements in mass spectrometry, next generation sequencing, and the development of integrated organs-on-chips, our knowledge of cancers associated with AA exposure, and of the mechanisms involved in AA toxicities, has significantly improved. DNA adduction plays a central role in AA-induced cancers; however, significant gaps remain in our knowledge as to how cellular enzymes promote activation of AAs and how the reactive species selectively bind to DNA and kidney proteins. In this review, I describe pathways for AAs biotransformation, adduction, and mutagenesis, emphasizing novel methods and ideas contributing to our present understanding of AA toxicities in humans.


Assuntos
Ácidos Aristolóquicos/efeitos adversos , Ácidos Aristolóquicos/metabolismo , Medicamentos de Ervas Chinesas/efeitos adversos , Medicamentos de Ervas Chinesas/metabolismo , Aristolochia/efeitos adversos , Aristolochia/química , Ácidos Aristolóquicos/toxicidade , Biotransformação , Medicamentos de Ervas Chinesas/toxicidade , Humanos , Medicina Tradicional Chinesa/efeitos adversos
4.
Xenobiotica ; 50(11): 1323-1331, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32369406

RESUMO

The compound 20(S),25-epoxydammarane-3ß,12ß,24α-triol (24-hydroxy-panaxadiol or 24-OH-PD), isolated from the red Panax ginseng CA Meyer possesses anticancer activity. Our aim was to study the pharmacokinetic characteristics of 24-OH-PD, which is essential for pre-clinical research during the development of new drugs. In this study, a simple and sensitive ultra-performance liquid chromatography-mass spectrometry (LC-MS/MS) method was established and used for studying the pharmacokinetics, in vitro protein binding, tissue distribution, and elimination profiles of 24-OH-PD in rats. 24-OH-PD was characterized by linear pharmacokinetics in the dose range of 2.5-10 mg/kg and had relatively longer half-life (4.82-5.45 h) than the other ginsenosides. It had a wide tissue distribution profile in rats and was primarily distributed in the lung. Within 96 h of intravenous administration, 13.84% of 24-OH-PD was excreted out via feces and 0.02% via urine in its unchanged form. In conclusion, a simple LC-MS/MS method with high sensitivity and selectivity was established for the quantification of 24-OH-PD.


Assuntos
Antineoplásicos/farmacocinética , Medicamentos de Ervas Chinesas/farmacocinética , Animais , Antineoplásicos/metabolismo , Líquidos Corporais , Medicamentos de Ervas Chinesas/metabolismo , Panax , Ratos , Ratos Sprague-Dawley , Distribuição Tecidual
5.
Artigo em Inglês | MEDLINE | ID: mdl-32251992

RESUMO

In this paper, an ultra-high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF HRMS) method was developed and validated for screening, confirmation and quantitation of 31 anti-impotence compounds potentially illegally added to herbal-based dietary supplements. The analytes were well separated by the mobile phase consisted of 0.1% formic acid solution and acetonitrile with gradient elution at a flow rate of 0.3 mL/min. The MS analysis was operated in positive mode and the mass error of the 31 compounds were below 2.9 ppm. The method validation showed good linearity with coefficients of determination (r2) higher than 0.9973 for all analytes. LODs and LLOQs ranged from 0.005 to 0.50 µg/g or µg /mL and from 0.02 to 1.24 µg /g or µg/mL, respectively. The accuracy was in the range of 86.6% to 113.7%, while the intra-and inter-day precision were in the ranges of 0.9-7.6% and 0.9-11.4%, respectively. The absolute and relative matrix effect were in the range of 65.8-115.6% and 0.6-13.3%. The mean recoveries were in the range of 80.5-116.9%. The stability ranged from 0.4% to 8.5%. Among 200 batches of herbal-based dietary supplements, sildenafil and/or tadalafil were found to be added illegally in two samples, while not very high concentration of icariin was detected in one sample. The Q-TOF mass spectrometry has been proved to be a very powerful and efficient tool for rapid screening of 31 anti-impotence compounds potentially illegally added to herbal-based dietary supplements, ensuring food safety and public health.


Assuntos
Suplementos Nutricionais/análise , Medicamentos de Ervas Chinesas/química , Disfunção Erétil/induzido quimicamente , Disfunção Erétil/tratamento farmacológico , Cromatografia Líquida de Alta Pressão , Suplementos Nutricionais/efeitos adversos , Contaminação de Medicamentos , Medicamentos de Ervas Chinesas/metabolismo , Inocuidade dos Alimentos , Humanos , Limite de Detecção , Masculino , Estrutura Molecular , Citrato de Sildenafila/química , Tadalafila/química , Espectrometria de Massas em Tandem
6.
AAPS PharmSciTech ; 21(4): 124, 2020 Apr 27.
Artigo em Inglês | MEDLINE | ID: mdl-32342227

RESUMO

To achieve improved drug delivery efficiency to hepatocellular carcinoma (HCC), biodegradable poly (ethylene glycol)-poly (lactic-co-glycolic acid) (PEG-PLGA) nanoparticles (NP), surface-modified with SP94 peptide, were designed for the efficient delivery of cryptotanshinone to the tumor for the treatment of HCC. Cryptotanshinone NP and SP94-NP were prepared by using nanoprecipitation. The physicochemical and pharmaceutical properties of the NP and SP94-NP were characterized, and the release kinetics suggested that both NP and SP94-NP provided continuous, slow release of cryptotanshinone for 48 h. The in vitro cellular experiment demonstrated that SP94-NP significantly enhanced the cellular uptake of cryptotanshinone and induced high cytotoxicity and cellular apoptosis of hepatocellular carcinoma (HepG2) cells. The in vivo detecting results of targeting effect using the Cy5.5 probe evidenced that SP94-NP showed an accumulation in tumor more efficiently than that of unconjugated ones. Meanwhile, SP94-NP exhibited the smallest tumor size than other groups and showed no toxicity to body. The results of this study provide a promising nanoplatform for the targeting of HCC.


Assuntos
Carcinoma Hepatocelular/tratamento farmacológico , Neoplasias Hepáticas/tratamento farmacológico , Nanopartículas/administração & dosagem , Fragmentos de Peptídeos/administração & dosagem , Fenantrenos/administração & dosagem , Poliésteres/administração & dosagem , Polietilenoglicóis/administração & dosagem , Animais , Carcinoma Hepatocelular/metabolismo , Carcinoma Hepatocelular/patologia , Sobrevivência Celular/efeitos dos fármacos , Sobrevivência Celular/fisiologia , Relação Dose-Resposta a Droga , Sistemas de Liberação de Medicamentos/métodos , Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/síntese química , Medicamentos de Ervas Chinesas/metabolismo , Feminino , Células Hep G2 , Humanos , Neoplasias Hepáticas/metabolismo , Neoplasias Hepáticas/patologia , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Nanopartículas/química , Nanopartículas/metabolismo , Fragmentos de Peptídeos/síntese química , Fragmentos de Peptídeos/metabolismo , Fenantrenos/síntese química , Fenantrenos/metabolismo , Poliésteres/síntese química , Poliésteres/metabolismo , Polietilenoglicóis/síntese química , Polietilenoglicóis/metabolismo
7.
Drug Metab Rev ; 52(1): 139-156, 2020 02.
Artigo em Inglês | MEDLINE | ID: mdl-32116054

RESUMO

There are more than 1000 species of microbes reside in the human gut, umbering∼1014 microbes. As the invisible organ of human beings, gut microbiota can usually participate in drug metabolism by producing specific enzymes, such as reductase and hydrolytic enzyme, thus affecting the efficacy, toxicity, and bioavailability of drugs. At least 30 commercially available drugs have been shown to be substrates of gut microbes-derived enzymes, and an increasing number of drugs may have the potential to contact with the distal gut with the help of improved release systems or poor solubility/permeability, more drugs are expected to be found to be metabolized through the gut flora. By collecting examples of intestinal flora participating in the metabolism of synthetic drugs and traditional Chinese medicine components, this article provides a comprehensive reference for future researchers to study drug metabolism by intestinal flora. Noticeably, the composition and quantity of intestinal flora varies among individuals, and can be affected by some drug administration (such as antibiotics) or environmental changes (acute plateau hypoxia). This seems to suggest that intestinal flora could have the potential to be a new drug target to affect the efficacy of drugs which can be metabolized by Intestinal flora. Accordingly, understanding the impact of intestinal flora on drug metabolism and clarifying the drug transformation process is of great significance for guiding rational clinical use, individualized use, toxicological evaluation, and promoting drug discovery and development.


Assuntos
Microbioma Gastrointestinal/fisiologia , Preparações Farmacêuticas/metabolismo , Animais , Medicamentos de Ervas Chinesas/metabolismo , Trato Gastrointestinal/metabolismo , Trato Gastrointestinal/microbiologia , Humanos , Farmacocinética
8.
Biomed Chromatogr ; 34(4): e4807, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32020626

RESUMO

Periplocae Cortex, named Xiang-Jia-Pi in China, has been widely used to treat autoimmune diseases, especially rheumatoid arthritis. However, the in vivo substances of Periplocae Cortex remain unknown yet. In this study, an ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry was used for profiling the chemical components and related metabolites of Periplocae Cortex. A total of 98 constituents were identified or tentatively characterized in Periplocae Cortex: 42 C21 steroidal glycosides, 10 cardiac glycosides, 23 organic acids, 4 aldehydes, 7 triterpenes, and 12 other types. Among them, 18 components were unambiguously identified by comparison with reference standards. In addition, 176 related xenobiotics (34 prototypes and 142 metabolites) were screened out and characterized in rats' biosamples (plasma, urine, bile, and feces) after the oral administration of Periplocae Cortex. Moreover, the metabolic fate of periplocoside S-4a, a C21 steroidal glycoside, was proposed for the first time. In summary, phase II reactions (methylation, glucuronidation, and sulfation), phase I reactions (hydrolysis reactions, oxygenation, and reduction), and their combinations were the predominant metabolic reactions of Periplocae Cortex in rat. It is the first report to reveal the in vivo substances and metabolism feature of Periplocae Cortex. This study also provided meaningful information for further pharmacodynamics study of Periplocae Cortex, as well as its quality control research.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Medicamentos de Ervas Chinesas/análise , Medicamentos de Ervas Chinesas/metabolismo , Espectrometria de Massas/métodos , Periploca/química , Administração Oral , Aldeídos/análise , Aldeídos/química , Animais , Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/química , Glicosídeos/análise , Glicosídeos/química , Masculino , Casca de Planta/química , Raízes de Plantas/química , Ratos , Ratos Sprague-Dawley , Triterpenos/análise , Triterpenos/química
9.
Poult Sci ; 99(2): 744-751, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-32029159

RESUMO

Lycium barbarum polysaccharides (LBP) are considered to be the major bioactive components of L. barbarum and have been widely used as a well-known traditional Chinese medicine and functional food because of their various biological activities. However, no published research has investigated the use of LBP as a feed additive in broilers. The objective of this study was to evaluate the effects of dietary LBP supplementation on the growth performance, digestive enzyme activities, antioxidant status, and immunity of broiler chickens. A total of 256 one-day-old Arbor Acres male broiler chicks were randomly allotted into 4 groups, with 8 replicates of 8 birds each, and were fed a corn-soybean meal-type basal diet supplemented without (control group) or with 1,000, 2,000, or 4,000 mg/kg LBP for 6 wk. The results showed that compared with the control diet, a significant increase in ADG (P < 0.05) during the grower and overall periods was observed in chickens fed the basal diet supplemented with 2,000 mg/kg LBP, whereas supplementation with 1,000 or 2,000 mg/kg LBP decreased feed-to-gain ratio (P < 0.05) during the starter period. The inclusion of LBP in the broiler diets increased overall amylase, lipase, and protease activities (P < 0.05). Supplementation with increasing levels of dietary LBP increased the activities of superoxide dismutase and glutathione peroxidase but decreased malondialdehyde content in the serum and liver (P < 0.05). Broilers fed with LBP-containing diets exhibited higher serum IgG and IgA concentrations (P < 0.05) than the broilers fed with the control diet. Serum tumor necrosis factor α and IL-4 concentrations were significantly elevated in the group fed 2,000 mg/kg LBP compared with the control group (P < 0.05). Broilers fed diets supplemented with LBP showed linear (P < 0.05) and quadratic (P < 0.05) increases in serum IL-6 and interferon gamma concentrations. The results indicated that dietary LBP supplementation can improve growth performance, digestive enzyme activities, antioxidant capacity, and immune function of broilers. In conclusion, LBP may be used as a promising feed additive for broilers, and a supplementation level of 2,000 mg/kg LBP in the broiler diet is recommended.


Assuntos
Antioxidantes/metabolismo , Galinhas , Carboidratos da Dieta/metabolismo , Medicamentos de Ervas Chinesas/metabolismo , Trato Gastrointestinal/enzimologia , Ração Animal/análise , Fenômenos Fisiológicos da Nutrição Animal/efeitos dos fármacos , Animais , Galinhas/crescimento & desenvolvimento , Galinhas/imunologia , Galinhas/metabolismo , Dieta/veterinária , Carboidratos da Dieta/administração & dosagem , Suplementos Nutricionais/análise , Relação Dose-Resposta a Droga , Medicamentos de Ervas Chinesas/administração & dosagem , Masculino , Distribuição Aleatória
10.
Nat Commun ; 11(1): 971, 2020 02 20.
Artigo em Inglês | MEDLINE | ID: mdl-32080175

RESUMO

Triptolide is a trace natural product of Tripterygium wilfordii. It has antitumor activities, particularly against pancreatic cancer cells. Identification of genes and elucidation of the biosynthetic pathway leading to triptolide are the prerequisite for heterologous bioproduction. Here, we report a reference-grade genome of T. wilfordii with a contig N50 of 4.36 Mb. We show that copy numbers of triptolide biosynthetic pathway genes are impacted by a recent whole-genome triplication event. We further integrate genomic, transcriptomic, and metabolomic data to map a gene-to-metabolite network. This leads to the identification of a cytochrome P450 (CYP728B70) that can catalyze oxidation of a methyl to the acid moiety of dehydroabietic acid in triptolide biosynthesis. We think the genomic resource and the candidate genes reported here set the foundation to fully reveal triptolide biosynthetic pathway and consequently the heterologous bioproduction.


Assuntos
Sistema Enzimático do Citocromo P-450/genética , Sistema Enzimático do Citocromo P-450/metabolismo , Diterpenos/metabolismo , Fenantrenos/metabolismo , Proteínas de Plantas/genética , Proteínas de Plantas/metabolismo , Tripterygium/genética , Tripterygium/metabolismo , Abietanos/metabolismo , Antineoplásicos Fitogênicos/biossíntese , Vias Biossintéticas/genética , Medicamentos de Ervas Chinesas/metabolismo , Compostos de Epóxi/metabolismo , Perfilação da Expressão Gênica , Genoma de Planta , Humanos , Engenharia Metabólica , Metaboloma , Oxirredução , Filogenia , Plantas Medicinais/genética , Plantas Medicinais/metabolismo
11.
Anal Chim Acta ; 1099: 94-102, 2020 Feb 22.
Artigo em Inglês | MEDLINE | ID: mdl-31986282

RESUMO

In terms of ligand fishing, the amount and the relative activity recovery of enzymes immobilized on magnetic particles and nanoparticles are not preeminent. Therefore, the metal-organic framework (MOF) UiO-66-NH2 was synthesized to immobilize the porcine pancreatic lipase (PPL) via precipitation-cross-linking, and the resulting novel biological matrices named PPL@MOF manifested high PPL loading capacity (98.31 mg/g) and relative activity recovery (104.4%). Moreover, the novel enzyme-MOF composite was applied to screen lipase inhibitors from Prunella vulgaris L. to enrich and improve the techniques of ligand fishing. As a result, 13 lipase ligands were obtained, and 12 compounds were determined by HPLC-Q-TOF-MS/MS. All of these ligands were further confirmed to be potential inhibitors through the verification of the activity assay and molecular docking. The proposed approach based on PPL@MOF was superior in terms of abundant protein loading capacity, high enzyme catalytic activity and easy preparation process. Taken together, our newly developed method provided a new platform for efficient discovering bioactive molecules from natural herbs.


Assuntos
Produtos Biológicos/farmacologia , Medicamentos de Ervas Chinesas/farmacologia , Enzimas Imobilizadas/antagonistas & inibidores , Lipase/antagonistas & inibidores , Estruturas Metalorgânicas/farmacologia , Prunella/química , Animais , Produtos Biológicos/química , Produtos Biológicos/metabolismo , Descoberta de Drogas , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/metabolismo , Enzimas Imobilizadas/química , Enzimas Imobilizadas/metabolismo , Ligantes , Lipase/química , Lipase/metabolismo , Medicina Tradicional Chinesa , Estruturas Metalorgânicas/química , Estruturas Metalorgânicas/metabolismo , Simulação de Acoplamento Molecular , Pâncreas/enzimologia , Suínos
12.
J Biotechnol ; 309: 107-112, 2020 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-31926981

RESUMO

Ginsenoside Rh2, a rare protopanaxadiol (PPD)-type triterpene saponin isolated from Panax ginseng, exhibits notable anticancer and immune-system-enhancing activities. Glycosylation catalyzed by uridine diphosphate-dependent glucosyltransferase (UGT) is the final biosynthetic step of ginsenoside Rh2. In this study, UGT73C5 isolated from Arabidopsis thaliana was demonstrated to selectively transfer a glucosyl moiety to the C3 hydroxyl group of PPD to synthesize ginsenoside Rh2. UGT73C5 was coupled with sucrose synthase (SuSy) from A. thaliana to regenerate costly uridine diphosphate glucose (UDPG) from cheap sucrose and catalytic amounts of uridine diphosphate (UDP). The UGT73C5/SuSy ratio, temperature, pH, cofactor UDP, and PPD concentrations for UGT73C5-SuSy coupled reactions were optimized. Through the stepwise addition of PPD, the maximal ginsenoside Rh2 production was 3.2 mg mL-1, which was the highest yield reported to date. These promising results provided an efficient and cost-effective approach to semisynthesize the highly valuable ginsenoside Rh2.


Assuntos
Arabidopsis/enzimologia , Medicamentos de Ervas Chinesas/metabolismo , Glucosiltransferases/metabolismo , Sapogeninas/metabolismo , Arabidopsis/genética , Técnicas de Cultura Celular por Lotes , Biocatálise , Vias Biossintéticas , Ginsenosídeos/biossíntese , Panax/metabolismo , Sapogeninas/química , Saponinas , Triterpenos , Difosfato de Uridina
13.
Molecules ; 25(1)2020 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-31906332

RESUMO

Astragalin, isolated from flowers of Rosa chinensis Jacq., is a kind of flavonoid, with anti-inflammatory, antioxidant, antiviral, analgesic, antibacterial, antiallergic, and antihepatotoxic effects. However, no studieson the procoagulant effect of astragalin have been reported. This study aimed to investigate the procoagulant activity of astragalin and its mechanism. Its procoagulant effect was investigated by activated partial thromboplastin time (APTT), thrombin time (TT), prothrombin time (PT), and fibrinogen (FIB) in vitro, and a rat model established by heparin sodium was used to evaluate the mechanism for the procoagulant effect in vivo. The results showed that astragalin had good procoagulant effects compared with the control group in vitro. Compared with the model group in vivo, astragalin could shorten the coagulation time and significantly increase the number of platelets. Meanwhile, astragalin could significantly reduce the effectual time of PT and APTT and increase the content of FIB. The contents of 6-keto-PGF1α and eNOS significantly decreased. Astragalin could increase whole blood viscosity (WBV), plasma viscosity (PV), erythrocyte sedimentation rate (ESR) and packedcell volume (PCV). All of the above revealed that astragalin had good procoagulant effects by promoting the intrinsic and extrinsic coagulation system.


Assuntos
Coagulação Sanguínea/efeitos dos fármacos , Fibrinogênio/metabolismo , Quempferóis/farmacologia , Agregação Plaquetária/efeitos dos fármacos , 6-Cetoprostaglandina F1 alfa/metabolismo , Animais , Testes de Coagulação Sanguínea , Sedimentação Sanguínea/efeitos dos fármacos , Viscosidade Sanguínea/efeitos dos fármacos , Medicamentos de Ervas Chinesas/metabolismo , Medicamentos de Ervas Chinesas/farmacologia , Endotelina-1/metabolismo , Feminino , Flavonoides/metabolismo , Flavonoides/farmacologia , Quempferóis/química , Quempferóis/isolamento & purificação , Quempferóis/metabolismo , Masculino , Óxido Nítrico Sintase Tipo III/metabolismo , Tempo de Tromboplastina Parcial , Tempo de Protrombina , Coelhos , Ratos , Ratos Sprague-Dawley , Rosaceae/química , Tempo de Trombina , Tromboxano B2/metabolismo
14.
Lett Appl Microbiol ; 70(4): 318-325, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-31951031

RESUMO

Fermentation is a traditional processing method that can impact the abundance of relevant components in Chinese herbal medicines. Huafeng Dan Yaomu was processed by fermentation. In this study, we investigated changes in toxic alkaloids using high-performance liquid chromatography and analysed the changes in microbial communities during fermentation of Huafeng Dan Yaomu by Illumina MiSeq platform. The results indicated that highly toxic alkaloid compounds including aconitine, mesaconitine and hypaconitine were decreased, whereas benzoylmesaconine and benzoylhypaconitine were increased during fermentation. The dominant bacterial genera in the raw material (day 0) were Bacillus (58·38%), Enterobacter (16·05%), Enterococcus (4·10%) and others (11·48%). After 7 days of fermentation, Pediococcus predominated, increasing from 98·26 to 99·97%. The dominant fungal genera in the raw material (day 0) were Incertae_Sedis_incertae_sedis (45·36%), Eurotiales_unclassified (20·63%), Millerozyma (15·58%) and Saccharomycopsis (10·64%). After 7 days of fermentation, Saccharomycopsis was increased to 90·84%. After 14 days of fermentation, Pichia became the main fungal genera in the fermentation process. There were 16 bacterial genera and seven fungal genera that displayed significant correlation with toxic alkaloids. The dynamics of the microbiota and chemical compounds during fermentation of Huafeng Dan Yaomu were revealed, providing a foundation for further investigation of the effects of microbes on chemical compounds and insights into the manufacturing of Huafeng Dan Yaomu. SIGNIFICANCE AND IMPACT OF THE STUDY: Huafeng Dan Yaomu is a unique fermentation-based micro-organism product. This study reveals that the change in toxic alkaloids during fermentation was related to micro-organisms. The results of this study can be used to improve the Chinese herb medicine fermentation process, such as the selection of beneficial strains and their composition for modern fermentation. The results of this study may also provide new ideas for the processing of Traditional Chinese Medicine.


Assuntos
Alcaloides/metabolismo , Bactérias/metabolismo , Medicamentos de Ervas Chinesas/metabolismo , Fungos/metabolismo , Plantas Medicinais/microbiologia , Alcaloides/análise , Alcaloides/toxicidade , Bactérias/classificação , Bactérias/genética , Bactérias/isolamento & purificação , Medicamentos de Ervas Chinesas/análise , Fermentação , Fungos/classificação , Fungos/genética , Fungos/isolamento & purificação , Microbiota
15.
J Mass Spectrom ; 55(1): e4484, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31786817

RESUMO

Qixianqingming granules (QXQM) comprise a traditional Chinese medicine (TCM) formula that was developed based on the combination of TCM theory and clinical practice. This formula has been proven to effectively treat asthma. In this study, an analytical procedure using ultraperformance liquid chromatography, coupled with electrospray ionization quadrupole time-of-flight mass spectrometry, was established for the rapid separation and sensitive identification of the chemical components in QXQM and its metabolites in serum of rats. Seventy-two compounds were systematically identified in QXQM, including flavonoids, terpenoids, anthraquinones, phenylethanoid glycosides, stilbenes, alkaloids, and organic acids. Thirteen prototype compounds and 29 metabolites were detected in the serum of rats. The results provided fundamental information for further studying the mechanisms and clinical application of QXQM.


Assuntos
Medicamentos de Ervas Chinesas/farmacocinética , Espectrometria de Massas por Ionização por Electrospray/métodos , Espectrometria de Massas em Tandem/métodos , Alcaloides/análise , Alcaloides/metabolismo , Animais , Antraquinonas/análise , Antraquinonas/metabolismo , Cromatografia Líquida de Alta Pressão , Medicamentos de Ervas Chinesas/metabolismo , Flavonoides/análise , Flavonoides/metabolismo , Glicosídeos/análise , Glicosídeos/metabolismo , Masculino , Ratos , Ratos Sprague-Dawley , Estilbenos/análise , Estilbenos/metabolismo , Terpenos/análise , Terpenos/metabolismo
16.
Biomed Chromatogr ; 34(2): e4726, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31654585

RESUMO

Multicompound determination for the quality control of traditional Chinese medicine (TCM) may often be inadequate, since these compounds may not be associated with, or fully represent, the clinical effects of TCM. Moreover, the individual contributions of each constituent to the pharmacological effect are often not considered. In China, Porana sinensis is widely used as a substitute for Erycibe sources to treat joint pain and rheumatoid arthritis. The existing quality control methods for P. sinensis neither consider the individual contributions of various compounds nor control the actual quality associated with different clinical efficacies. In the present study, a novel efficacy-oriented approach, named the effect-constituent index (ECI), was established for P. sinensis. Analyses of the spectrum-effect relationship and components in rat plasma were conducted to systematically and scientifically select quality markers. Quantitative analysis of multicomponents via a single marker method was introduced to enhance the practical application value of the established ECI. The established ECI shows a good ability to distinguish and predict the bioeffect-based quality of P. sinensis. The present study also provides a reference for the establishment and application of ECI as a quality control method for TCMs.


Assuntos
Convolvulaceae/química , Medicamentos de Ervas Chinesas , Animais , Ácido Clorogênico/sangue , Ácido Clorogênico/química , Ácido Clorogênico/farmacocinética , Cromatografia Líquida de Alta Pressão , Cumarínicos/sangue , Cumarínicos/química , Cumarínicos/farmacocinética , Medicamentos de Ervas Chinesas/análise , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/metabolismo , Medicamentos de Ervas Chinesas/normas , Glucosídeos/sangue , Glucosídeos/química , Glucosídeos/farmacocinética , Modelos Lineares , Medicina Tradicional Chinesa , Controle de Qualidade , Ácido Quínico/análogos & derivados , Ácido Quínico/sangue , Ácido Quínico/química , Ácido Quínico/farmacocinética , Ratos , Ratos Sprague-Dawley , Reprodutibilidade dos Testes
17.
J Agric Food Chem ; 68(1): 409-417, 2020 Jan 08.
Artigo em Inglês | MEDLINE | ID: mdl-31833363

RESUMO

Naringin has been documented to possess various bioactivities. Due to thorny endogenous interferences, the metabolism pathways of naringin and exact amounts of derived phenolic catabolites have not been definitely assigned. In this work, stable isotope-labeling-based liquid chromatography-mass spectrometry methods were developed to eliminate the endogenous interferences. [2',3',5',6'-D4]-naringin was orally administrated to rats. Urine and feces samples were collected and then analyzed with ultrahigh-performance liquid chromatography-quadrupole-time-of-flight tandem mass spectrometry (UHPLC-Q-TOF-MS/MS). A total of 21 flavonoid metabolites and 11 phenolic catabolites were screened. The metabolism and catabolism pathways were proposed. Furthermore, deuterated naringin and its main metabolites were determined with rapid resolution liquid chromatography tandem triple quadrupole mass spectrometry (RRLC-QqQ-MS/MS). The overall recovery of ingested deuterated naringin was calculated as 56.9% without endogenous interferences. The obtained results provide essential information for further pharmacological studies of naringin.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Medicamentos de Ervas Chinesas/química , Fezes/química , Flavanonas/química , Flavanonas/metabolismo , Marcação por Isótopo/métodos , Espectrometria de Massas/métodos , Animais , Medicamentos de Ervas Chinesas/metabolismo , Feminino , Flavanonas/urina , Masculino , Ratos , Ratos Sprague-Dawley
18.
Biomed Chromatogr ; 34(3): e4778, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31826299

RESUMO

Saposhnikovia divaricata is a commonly used traditional Chinese medicine in treating various diseases such as pyrexia, rheumatism and headache. So far, there have been few reports on the metabolism of orally administered Saposhnikovia divaricate decoction (SDD), hindering further study on its bioactive components and their pharmacological characteristics. In the present study, ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOFMS) was used coupled with principal component analysis (PCA) and partial least squared discriminant analysis (PLS-DA) to rapidly discover and identify the metabolites of SDD. According to the result of PLS-DA, a total of 139 ions of interest including 87 positive ions and 52 negative ions were extracted as SDD-related xenobiotics in urine. Finally, 12 and 65 compounds were identified as absorbed parent components and metabolites of SDD, respectively. Among them, 40 new metabolites were reported for the first time. Our results suggested that hydrolysis, hydroxylation, glucuronidation and sulfation are the major metabolic pathways of chromones, while hydroxylation, hydrogenation and sulfation are the main metabolic pathways of coumarins. This study is the first to explore the absorption and metabolism of SDD using UHPLC-Q-TOFMS, with results providing a basis for further study of its pharmacokinetics and discovery of its bioactive components.


Assuntos
Apiaceae , Cromatografia Líquida de Alta Pressão/métodos , Medicamentos de Ervas Chinesas , Espectrometria de Massas/métodos , Animais , Cromonas/metabolismo , Cromonas/urina , Medicamentos de Ervas Chinesas/metabolismo , Medicamentos de Ervas Chinesas/farmacocinética , Masculino , Análise Multivariada , Ratos , Ratos Wistar
19.
Xenobiotica ; 50(5): 545-551, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-31524030

RESUMO

Hydroxysafflor yellow A (HSYA) is the most pharmaceutically relevant compound in Xuebijing (XBJ) for traumatic brain injury (TBI) treatment. We aimed to investigate biofluids pharmacokinetics of HSYA from XBJ to ensure the drug safety and to guide the clinical use.A sensitive, rapid and reliable liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was applied to investigate pharmacokinetics of HSYA in TBI patients after intravenous administration of XBJ. Non-compartmental methods using DAS 3.0 software were applied to analyse the pharmacokinetic parameters.A similar half-life (Plasmat1/2: 14.55 ± 3.51 h vs. CSFt1/2: 15.73 ± 3.63) was observed. HSYA reached the peak level rapidly, but exhibited a strongly slow absorption phase from blood to cerebrospinal fluid (CSF, PlasmaTmax: 0.69 ± 0.26 h vs. CSFTmax: 4.0 ± 2.62 h). HSYA exhibited much higher Cmax (PlasmaCmax: 9342.76 ± 2489.23 µg/L vs. CSFCmax: 98.08 ± 14.51 µg/L) and AUC0-t (PlasmaAUC0-t: 57490.5 ± 5560.3 µg h/L vs. CSFAUC0-t: 1851.6 ± 269.1 µg h/L), yet a shorter CL (PlasmaCL: 0.02 ± 0.002 L/h/kg vs. CSFCL: 0.55 ± 0.01 L/h/kg) in plasma than in CSF. The AUCCSF/AUCplasma of HSYA was almost 3.37%.In summary, the results demonstrate that part of HSYA come across blood-brain barrier after XBJ administration. This study provides evidence for better understanding the pharmacokinetics and potential for clinical guidance of XBJ for TBI treatment.


Assuntos
Lesões Encefálicas Traumáticas/metabolismo , Chalcona/análogos & derivados , Medicamentos de Ervas Chinesas/metabolismo , Quinonas/metabolismo , Administração Intravenosa , Lesões Encefálicas Traumáticas/sangue , Lesões Encefálicas Traumáticas/líquido cefalorraquidiano , Chalcona/sangue , Chalcona/líquido cefalorraquidiano , Chalcona/metabolismo , Humanos , Farmacocinética , Quinonas/sangue , Quinonas/líquido cefalorraquidiano
20.
J Sep Sci ; 43(6): 1051-1062, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31876986

RESUMO

Menthae Haplocalycis Herba has been utilized for food and medicinal purposes in China for thousands of years. It has various efficacies, including dispelling wind and heat and relieving sore throat. M. Haplocalycis Herba has been also widely used in food, cosmetics, spices, and other fields. Exploring the constituents and detecting the metabolites of M. Haplocalycis are of great significance to clarify the effective substances. However, the in vivo metabolites of M. Haplocalycis Herba water extract are still unclear. Herein, a sensitive and specific method, ultra-high performance liquid chromatography with linear ion trap-Orbitrap mass spectrometry, established in this assay was used to study the metabolism of M. Haplocalycis Herba water extract in rat plasma, urine, and feces. We characterized and identified 9, 50, and 34 metabolites in plasma, urine, and feces, respectively. Seven metabolic pathways, including phase Ⅰ (isomerization, demethylation, hydroxylation, and dehydration) and phase Ⅱ (sulfation and glucuronidation) were mainly involved in the metabolism. It is the first systematic study on the metabolism of M. Haplocalycis Herba water extract in vivo, which enrich current understanding of the metabolic behavior of M. Haplocalycis Herba water extract and provide a metabolic rationale for further in-depth in vivo biotransformation and pharmacokinetic analysis.


Assuntos
Medicamentos de Ervas Chinesas/análise , Fezes/química , Mentha/química , Compostos Fitoquímicos/análise , Extratos Vegetais/análise , Animais , Cromatografia Líquida de Alta Pressão , Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/metabolismo , Injeções Intravenosas , Masculino , Espectrometria de Massas , Medicina Tradicional Chinesa , Mentha/metabolismo , Estrutura Molecular , Compostos Fitoquímicos/administração & dosagem , Compostos Fitoquímicos/metabolismo , Extratos Vegetais/administração & dosagem , Extratos Vegetais/metabolismo , Ratos , Ratos Sprague-Dawley
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