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1.
Zhongguo Zhong Yao Za Zhi ; 45(9): 2172-2179, 2020 May.
Artículo en Zh | MEDLINE | ID: mdl-32495568

RESUMEN

To explore the pathogenesis of heart and kidney imbalance insomnia and the regulatory effect of Jiaotai Pills, in order to study the changes of central and peripheral neurotransmitters in rat. Insomnia rats with heart and kidney imbalance were induced through intraperitoneal injection with p-chlorophenylalanine(PCPA, 400 mg·kg~(-1)·d~(-1)), and the model rats were intragastrically administrated with Jiaotai Pills(3.3 g·kg~(-1)·d~(-1)) for 7 days. Nine neurotransmitters were determined by UPLC-MS/MS and principal component analysis(PCA) method in serum, urine, brain, heart, liver, kidney and adrenal gland of rats. The results showed that the ratio of 5-HT and 5-HIAA in platelet of insomnia rats was significantly lower than that in the normal group, and Jiaotai Pills had a significant up-regulatory or down-regulatory effect. Compared with the normal group, the changed neurotransmitters in blood of insomnia rats were 5-HIAA, E, NE, DA, Glu and ACH, and except ACH, the changes of 7 kinds of neurotransmitters in urine were more significant, Jiaotai Pills had a significant up-regulatory or down-regulatory effect. Compared with the normal group, all of the 8 neurotransmitters in insomnia rats except HVA were changed. Jiaotai Pills could regulate the neurotransmitters in each tissue of insomnia rats, especially in brain, liver and adrenal gland. In conclusion, insomnia is caused by not only a change of neurotransmitters in brain, but also a series of changes in peripheral tissues. It indicates that insomnia is a systematic imbalance of neurotransmitters. Jiaotai Pills not only regulates the central nervous system, but also has a certain protective effect on other organs, reflecting the multi-target and systematic effect of Jiaotai Pills in the treatment of insomnia.


Asunto(s)
Trastornos del Inicio y del Mantenimiento del Sueño , Animales , Cromatografía Liquida , Medicamentos Herbarios Chinos , Neurotransmisores , Ratas , Espectrometría de Masas en Tándem
2.
Zhongguo Zhong Yao Za Zhi ; 44(22): 4918-4923, 2019 Nov.
Artículo en Zh | MEDLINE | ID: mdl-31872601

RESUMEN

Ultra performance liquid chromatography-tandem mass spectrometry( UPLC-MS/MS) was used to establish the simultaneous determination method of eight neurotransmitters in brain,liver,kidney,adrenal gland,serum and urine,including serotonin,5-hydroxyindole acetic acid,epinephrine,norepinephrine,dopamine,glutamic acid,γ-aminobutyric acid,and acetylcholine,and then investigate the distribution characteristics of neurotransmitters in rat tissues,blood and urine. Waters ACQUITY UPLC BEH C_(18) column( 2. 1 mm×100 mm,1. 7 µm) was used,with 0. 3% formic acid solution-acetonitrile as the mobile phase for gradient elution.Multiple reaction monitoring( MRM) scanning method under positive mode by atmospheric pressure electrospray ion source( ESI) was also performed to establish the detection method of neurotransmitters for methodological research. The plasma,urine and tissues of normal rats were pre-treated including homogenization,centrifuging,and protein removal,then the 2 µL supernatant was injected for analysis. The results showed that eight kinds of neurotransmitters could be accurately determined within 7 min,with linear correlation coefficients all greater than 0. 99. This method showed high accuracy and good precision,with specificity,stability,extraction recovery and matrix effects all complying with the biological sample analysis requirements. The most abundant transmitters in the brain,liver,kidney,kidney gland,blood and urine were γ-aminobutyric acid,glutamic acid,glutamic acid,adrenaline,glutamic acid and dopamine.The method is sensitive,rapid,precise,accurate and specific,and can be used for simultaneous quantitative analysis of eight neurotransmitters in biological samples. The investigation of the distribution ratio of transmitters in rats is of important significance to disease prevention and treatment.


Asunto(s)
Neurotransmisores/metabolismo , Espectrometría de Masas en Tándem , Animales , Cromatografía Líquida de Alta Presión , Cromatografía Liquida , Neurotransmisores/sangre , Neurotransmisores/orina , Ratas , Reproducibilidad de los Resultados , Sensibilidad y Especificidad
3.
Zhongguo Zhong Yao Za Zhi ; 42(18): 3591-3595, 2017 Sep.
Artículo en Zh | MEDLINE | ID: mdl-29218947

RESUMEN

To explore the possible mechanism of liver injury, the effects of Ploygoni Multiflori Caulis and its extractive on the function of bilirubin-associated transporters were investigated in normal (N) and idiosyncratic (LPS) rats (M). The normal and LPS rats were respectively administrated powder of Ploygoni Multiflori Caulis, its extractive and same volume of 0.5% CMC-Na solution for 7 d. BSP, a substrate of the transporters of Oatp1a1 and Oatp1b2 was selected, and its pharmacokinetic parameters of intravenous injection were determined to examined the activity these transporters. Meanwhile the mRNA expressions of transporters were detected. Compared with N-blank control group, besides M-powder group, the Cmax has no significantly different from other groups, t1/2, AUC0-t and AUC0-∞ were significantly increased, and CL were significantly decreased. However, compared with N- blank control group, AST and ALT decreased significantly. The expression of Oatp1a1, Oatp1b2 and MRP2 mRNA was significantly decreased (P<0.05), but there was no act synergistically when Ploygoni Multiflori Caulis and extractive were combined with LPS. The function of Oatp1a1, Oatp1b2 and MRP2 in rats were significantly inhibited by Ploygoni Multiflori Caulis and extractive, which may be an important cause of hepatotoxicity.


Asunto(s)
Bilirrubina/metabolismo , Enfermedad Hepática Inducida por Sustancias y Drogas , Medicamentos Herbarios Chinos/toxicidad , Proteínas de Transporte de Membrana/metabolismo , Polygonum/química , Transportadoras de Casetes de Unión a ATP/metabolismo , Animales , Flores/química , Hígado/efectos de los fármacos , Transportadores de Anión Orgánico Sodio-Independiente/metabolismo , Ratas , Miembro 1B3 de la Familia de los Transportadores de Solutos de Aniones Orgánicos/metabolismo
4.
Chin J Integr Med ; 27(3): 183-191, 2021 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-33420587

RESUMEN

OBJECTIVE: To reveal the effect and mechanism of Jiaotai Pill (, JTP) on insomniac rats. METHODS: The insomniac model was established by intraperitoneal injection of p-chlorophenylalanine (PCPA). In behavioral experiments, rats were divided into control, insomniac model, JTP [3.3 g/(kg•d)], and diazepam [4 mg/(kg•d)] groups. The treatment effect of JTP was evaluated by weight measurement (increasement of body weight), open field test (number of crossings) and forced swimming test (immobility time). A high performance liquid chromatography-electrochemical detection (HPLC-ECD) method was built to determine the concentration of monoamine transmitters in hypothalamus and peripheral organs from normal, model, JTP, citalopram [30 mg/(kg•d)], maprotiline [40 mg/(kg•d)] and bupropion [40 mg/(kg•d)] groups. Expressions of serotonin transporter (SERT), dopamine transporter (DAT), and norepinephrine transporter (NET) were analyzed by quantitative polymerase chain reaction (qPCR) and Western blot in normal, model and JTP groups. A high performance liquid chromatography-electrospray ionization mass spectrometry (HPLC-ESI-MS/MS) method was established to determine the pharmacokinetics, urine cumulative excretion of metformin in vivo, and tissue slice uptake in vitro, which were applied to assess the activity of organic cation transporters (OCTs) in hypothalamus and peripheral organs. RESULTS: Compared with the insomniac model group, the body weight and spontaneous locomotor were increased, and the immobility time was decreased after treatment with JTP (P<0.01). Both serotonin and dopamine contents in hypothalamus and peripheral organs were increased (P<0.01). The norepinephrine content was increased in peripheral organs and decreased in hypothalamus (P<0.05 or P<0.01). At the same time, SERT, DAT, OCT1, OCT2, and OCT3 were down-regulated in hypothalamus and peripheral organs (P<0.05). NET was down-regulated in peripheral organs and up-regulated in hypothalamus (P<0.05 or P<0.01). Moreover, the activity of OCTs in hypothalamus and peripheral organs was inhibited (P<0.05). CONCLUSION: JTP alleviates insomnia through regulation of monoaminergic system and OCTs in hypothalamus and peripheral organs.


Asunto(s)
Medicamentos Herbarios Chinos , Trastornos del Inicio y del Mantenimiento del Sueño , Animales , Proteínas de Transporte de Catión , Cationes , Ratas , Espectrometría de Masas en Tándem
5.
Drug Des Devel Ther ; 12: 57-65, 2018.
Artículo en Inglés | MEDLINE | ID: mdl-29343943

RESUMEN

Epiberberine (EPI) is a novel and potentially effective therapeutic and preventive agent for diabetes and cardiovascular disease. To evaluate its potential value for drug development, a specific, sensitive and robust high-performance liquid chromatography-tandem mass spectrometry assay for the determination of EPI in rat biological samples was established. This assay was used to study the pharmacokinetics, bioavailability and excretion of EPI in rats after oral administration. In addition, a cocktail method was used to compare the inhibition characteristics of EPI on cytochrome P450 (CYP450) isoforms in human liver microsomes (HLMs) and rat liver microsomes (RLMs). The results demonstrated that EPI was rapidly absorbed and metabolized after oral administration (10, 54 or 81 mg/kg) in rats, with Tmax of 0.37-0.42 h and T1/2 of 0.49-2.73 h. The Cmax and area under the curve values for EPI increased proportionally with the dose, and the oral absolute bioavailability was 14.46%. EPI was excreted mainly in bile and feces, and after its oral administration to rats, EPI was eliminated predominantly by the kidneys. A comparison of the current half-maximal inhibitory concentration and Ki values revealed that EPI demonstrated an obvious inhibitory effect on CYP2C9 and CYP2D6. Furthermore, its effect was stronger in HLM than in RLM, more likely to be a result of noncompetitive inhibition.


Asunto(s)
Berberina/análogos & derivados , Inhibidores del Citocromo P-450 CYP2C9/administración & dosificación , Inhibidores del Citocromo P-450 CYP2C9/farmacocinética , Inhibidores del Citocromo P-450 CYP2D6/administración & dosificación , Inhibidores del Citocromo P-450 CYP2D6/farmacocinética , Medicamentos Herbarios Chinos/administración & dosificación , Medicamentos Herbarios Chinos/farmacocinética , Eliminación Renal , Administración Oral , Animales , Berberina/administración & dosificación , Berberina/sangre , Berberina/farmacocinética , Disponibilidad Biológica , Cromatografía Líquida de Alta Presión , Citocromo P-450 CYP2C9/metabolismo , Inhibidores del Citocromo P-450 CYP2C9/sangre , Citocromo P-450 CYP2D6/metabolismo , Inhibidores del Citocromo P-450 CYP2D6/sangre , Sistema Enzimático del Citocromo P-450/metabolismo , Eliminación Hepatobiliar , Humanos , Absorción Intestinal , Eliminación Intestinal , Masculino , Microsomas Hepáticos/enzimología , Ratas Sprague-Dawley , Espectrometría de Masas en Tándem
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