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1.
Endokrynol Pol ; 73(1): 81-86, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35119092

RESUMO

INTRODUCTION: Metabolic syndrome (MetS) is a clinical syndrome with several characteristics. Steroid receptor RNA activator (SRA) is a long non-coding RNA (lncRNA), which can increase the expression of steroid receptor-dependent gene. This study aimed to explore the changes in metabolic parameters and the predictive value of the peripheral blood mononuclear cells (PBMCs) to SRA ratios as new indicators in subjects with and without MetS in southern China. MATERIAL AND METHODS: There were 81 participants (39 with MetS and 42 without MetS) in this cross-sectional study. The expression of lncRNAs in PBMCs was evaluated by quantitative reverse transcription polymerase chain reaction (qRT-PCR). The risks of SRA and PBMCs to SRA ratios contributing to the presence of MetS were estimated by univariate and multivariate logistic regression models. The area under the receiver (AUC) operating characteristic curve was employed to evaluate diagnostic accuracy. RESULTS: MetS was positively correlated with cortisol, interleukin 6 (IL-6), white blood cell to SRA ratio (WTSR), lymphocyte to SRA ratio (LTSR), monocyte to SRA ratio (MTSR), and PBMC to SRA ratio (PTSR). A receiver operating characteristic (ROC) curve analysis was performed to assess the value of LTSR (OR: 0.722; p < 0.001) for predicting MetS. The area under the curve yielded a cut-off value of 0.483, with a sensitivity of 76.9% and a specificity of 71.4% (p < 0.001). CONCLUSION: In summary, SRA in PBMCs may be an important biomarker of stress reaction and may play a role in vulnerability to MetS. Also, the lymphocyte to SRA ratio demonstrated high accuracy in the diagnosis of MetS.


Assuntos
Síndrome Metabólica , RNA Longo não Codificante , Estudos Transversais , Humanos , Leucócitos/metabolismo , Leucócitos Mononucleares/metabolismo , RNA Longo não Codificante/genética , RNA Longo não Codificante/metabolismo , Curva ROC
2.
Artigo em Inglês | MEDLINE | ID: mdl-29936367

RESUMO

BuyangHuanwu decoction (BHD) is widely used as a traditional herbal medicine because of its antithrombotic effect, which is attributed to the inhibition of platelet aggregation; however, its active compounds remain unknown. In this study, we developed a method involving platelet binding, solid-phase extraction, and HPLC-MS/MS for screening BHD compounds with potential anti-platelet aggregation properties. Five compounds showing platelet binding affinity were identified as 6-hydroxykaempferol-di-O-glucoside, paeoniflorin, calycosin-7-O-ß-d-glucoside, galloylpaeoniflorin, and formononetin-7-O-ß-d-glucoside. The results of anti-platelet aggregation experiments in vitro confirmed that these compounds inhibited adenosine diphosphate-induced platelet aggregation. Our results suggest that a platelet binding assay combined with solid-phase extraction and HPLC-MS/MS is an effective method for screening anti-platelet aggregation agents in traditional Chinese medicines.


Assuntos
Plaquetas/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão/métodos , Medicamentos de Ervas Chinesas , Inibidores da Agregação Plaquetária , Agregação Plaquetária/efeitos dos fármacos , Animais , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Camundongos , Inibidores da Agregação Plaquetária/química , Inibidores da Agregação Plaquetária/farmacologia , Ratos Sprague-Dawley , Extração em Fase Sólida/métodos , Espectrometria de Massas em Tandem/métodos
3.
Talanta ; 179: 490-500, 2018 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-29310265

RESUMO

Buyang Huanwu decoction (BHD) was reported to exert angiogenesis-promoting effects, but its active ingredients remain unknown. In this study, we developed a method to screen potential angiogenesis-promoting compounds in BHD, which involved biospecific isolation using live rat brain microvascular endothelial cells (rBMECs) and characterization using solid-phase extraction (SPE) and high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS). Six compounds showed binding affinity to rBMECs and were further identified as 6-hydroxykaempferol-di-O-glucoside, paeoniflorin, calycosin-7-O-ß-D-glucoside, galloylpaeoniflorin, formononetin-7-O-ß-D-glucoside, and (3R)-7,2'-hydroxy-3',4'-dimethoxy-isoflavan. The results indicated that five of them except 6-hydroxykaempferol-di-O-glucoside showed a protective effect against oxygen glucose deprivation/reperfusion injury in rBMECs and upregulated the secretion of vascular endothelial growth factor and basic fibroblast growth factor, suggesting a mechanism underlying their angiogenic activity. Our findings suggest that biospecific live cell-based isolation combined with SPE and HPLC-MS/MS is an effective method for screening potential bioactive components in traditional Chinese medicines.


Assuntos
Indutores da Angiogênese/isolamento & purificação , Compostos Bicíclicos Heterocíclicos com Pontes/isolamento & purificação , Medicamentos de Ervas Chinesas/química , Células Endoteliais/efeitos dos fármacos , Glucosídeos/isolamento & purificação , Isoflavonas/isolamento & purificação , Monoterpenos/isolamento & purificação , Indutores da Angiogênese/química , Indutores da Angiogênese/farmacologia , Animais , Animais Recém-Nascidos , Encéfalo/irrigação sanguínea , Encéfalo/citologia , Compostos Bicíclicos Heterocíclicos com Pontes/química , Compostos Bicíclicos Heterocíclicos com Pontes/farmacologia , Cromatografia Líquida de Alta Pressão/métodos , Células Endoteliais/citologia , Células Endoteliais/metabolismo , Glucosídeos/química , Glucosídeos/farmacologia , Isoflavonas/química , Isoflavonas/farmacologia , Monoterpenos/química , Monoterpenos/farmacologia , Cultura Primária de Células , Ratos , Ratos Sprague-Dawley , Extração em Fase Sólida/métodos , Espectrometria de Massas em Tandem/métodos
4.
J Tradit Chin Med ; 37(4): 503-509, 2017 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-32188209

RESUMO

OBJECTIVE: To investigate the effect of stimulating the acupoints Feishu (BL 13) and Dazhui (GV 14) on the transdermal uptake of sinapine thiocyanate contained in a gel used for the management of asthma. METHODS: Thirty Sprague-Dawley rats were randomly divided into three equal groups using a random number table: the Feishu (BL 13) acupoint group, the Dazhui (GV 14) acupoint group, and the nonacupoint group or control group. Using microdialysis technology, preprocessed skin probes were implanted into the rats at Feishu (BL 13), Dazhui (GV 14), and a nonacupoint site. Asthma gel was then placed on the skin at Feishu (BL 13), Dazhui (GV 14) acupoints, and the nonacupoint for all groups. Dialysate was collected every 30 min for 12 h. The normalized concentration of sinapine thiocyanate in the skin was determined by high-performance liquid chromatography. RESULTS: The rat in vivo transdermal experiment demonstrated that the quantity-time equation showed a good linear correlation with zero-order kinetics (r > 0.99). The transdermal behavior was in accordance with the first-order rate open model in which the transdermal penetration rates and the accumulative amounts of sinapine thiocyanate in the skin at the acupoint sites were greater than those through the skin of the nonacupoint site. The systemic maximum concentration and the area under the curve of sinapine thiocyanate in the acupoint groups were significantly greater than in the nonacupoint group. A lag time was observed in both acupoint groups, but not in the nonacupoint group. CONCLUSION: Stimulating the acupoints promotes the percutaneous absorption of sinapine thiocyanate and also controls its release, reducing concentration fluctuations in the blood.

5.
Xenobiotica ; 47(11): 973-979, 2017 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-27827094

RESUMO

1. In traditional Chinese medicine, Angelica sinensis is often coprescribed with Ligusticum chuanxiong Hort for the treatment of ischemic cerebrovascular diseases. Tetramethylpyrazine (TMP) is one of the most important active ingredients isolated from Ligusticum chuanxiong Hort; ferulic acid (FA) is the main water-soluble component of Angelica sinensis. 2. The purpose of this study is to investigate the possible effect of FA on the brain pharmacokinetics of TMP in conscious Sprague-Dawley rats. The pharmacokinetic parameters of TMP were investigated in brain microdialysates after oral and intravenous administration of TMP (4 mg/kg) to rats in the absence and presence of FA (5 mg/kg). Samples were collected at timed intervals for the measurement of TMP by a rapid and sensitive UPLC-MS/MS method. 3. The pharmacokinetic parameters were calculated by noncompartmental analysis for brain microdialysates. The brain pharmacokinetic data for TMP showed significant increases in Cmax, t1/2, AUC0-inf and MRT0-inf after combination with FA. After intragastric administration with FA, there were significant decreases in the Tmax (from 38.33 ± 5.77 to 21 ± 5.48 min; p < 0.01) of TMP. This study indicated that potential drug-drug interaction between TMP and FA should be taken into consideration and the combined administration is beneficial in improving the bioavailability of TMP in the brain.


Assuntos
Encéfalo/metabolismo , Medicamentos de Ervas Chinesas/farmacocinética , Pirazinas/farmacocinética , Animais , Ratos , Ratos Sprague-Dawley
6.
J Pharm Biomed Anal ; 128: 510-518, 2016 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-27389185

RESUMO

A rapid, sensitive and selective ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method has been developed for the simultaneous determination and pharmacokinetic investigation of Tetramethylpyrazine (TMP) and Ferulic acid (FA) in rat striatum. The method was validated over the concentration range of 1.15-505ng/mL for TMP and 3.23-101ng/mL for FA, with a lower limit of quantitation (LLOQ) of 1.15ng/mL and 3.23ng/mL, respectively. This method can be successfully applied in pharmacokinetic studies of TMP and FA in striatum of awake and anesthetic rats. The cerebral blood flow velocity (CBF) during middle cerebral artery occlusion (MCAO) was monitored by Laser speckle contrast imaging, to observe whether the compatibility of TMP and FA could improve CBF against cerebral ischemia/reperfusion (I/R) injury. Infarct volume was examined to evaluate severity of ischemic brain injury. The pharmacokinetic study indicated that T1/2, Cmax, MRT and AUC0-inf were changed after combined administration of TMP and FA, when compared with either drug alone both in awake and anesthetic groups. The pharmacodynamics results showed that co-administration of drugs could enhance the CBF during middle cerebral artery occlusion and reduced the infarct volume. Taken together, the compatibility treatment of TMP and FA might be a promising therapeutic strategy for ischemic stroke. Further study is required to optimize the compatibility proportion.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Corpo Estriado/metabolismo , Ácidos Cumáricos/farmacocinética , Microdiálise/métodos , Pirazinas/farmacocinética , Traumatismo por Reperfusão/metabolismo , Espectrometria de Massas em Tandem/métodos , Animais , Circulação Cerebrovascular/fisiologia , Ácidos Cumáricos/farmacologia , Sinergismo Farmacológico , Limite de Detecção , Masculino , Pirazinas/farmacologia , Ratos , Traumatismo por Reperfusão/fisiopatologia , Traumatismo por Reperfusão/prevenção & controle , Sensibilidade e Especificidade
7.
Pharm Dev Technol ; 21(5): 535-45, 2016 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-25757643

RESUMO

The purpose of the present study was to prepare and optimize sinomenine (SIN) pluronic lecithin organogels system (PLO), and to evaluate the permeability of the optimized PLO in vitro and in vivo. Box-Behnken design was used to optimize the PLO and the optimized formulation was pluronic F127 of 19.61%, lecithin of 3.60% and SIN of 1.27%. The formulation was evaluated its skin permeation and drug deposition both in vitro and in vivo compared with gel. Permeation and deposition studies of PLO were carried out with Franz diffusion cells in vitro and with microdialysis in vivo. In vitro studies, permeation rate (Jss) of SIN from PLO was 146.55 ± 2.93 µg/cm(2)/h, significantly higher than that of gel (120.39 µg/cm(2)/h) and the amount of SIN deposited in skin from the PLO was 10.08 ± 0.86 µg/cm(2), significantly larger than that from gel (6.01 ± 0.04 µg/cm(2)). In vivo skin microdialysis studies showed that the maximum concentration (Cmax) of SIN from PLO in "permeation study" and "drug-deposition study" were 150.27 ± 20.85 µg/ml and 67.95 µg/ml, respectively, both significantly higher than that of SIN from gel (29.66 and 6.73 µg/ml). The results recommend that PLO can be used as an advantageous transdermal delivery vehicle to enhance the permeation and skin deposition of SIN.


Assuntos
Antirreumáticos/metabolismo , Sistemas de Liberação de Medicamentos/métodos , Lecitinas/metabolismo , Morfinanos/metabolismo , Poloxâmero/metabolismo , Absorção Cutânea/fisiologia , Administração Cutânea , Animais , Antirreumáticos/administração & dosagem , Avaliação Pré-Clínica de Medicamentos/métodos , Géis , Lecitinas/administração & dosagem , Masculino , Morfinanos/administração & dosagem , Técnicas de Cultura de Órgãos , Poloxâmero/administração & dosagem , Ratos , Ratos Sprague-Dawley , Absorção Cutânea/efeitos dos fármacos
8.
Zhongguo Zhong Yao Za Zhi ; 40(21): 4275-80, 2015 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-27071270

RESUMO

To establish a method for detecting microdialysis recovery of tetramethylpyrazine (TMP) and ferulic acid (FA) and investigating the influencing factors, providing the basis for further in vivo microdialysis experiments. The concentration of FA and TMP in dialysates were determined by high pressure liquid chromatography ( HPLC) and probe recovery were calculated respectively. The influence of the flow rates, medium concentration, temperature and in vivo probe stability on the recovery of FA and TMP were investigated by using concentration difference method (incremental method and decrement method). The recovery obtained by incremental method were similar to by decrement method. The in vitro recovery rate of FA and TMP decreased with the increase of 1-2.5 µL min(-1), and increased obviously with the temperature of 25-42 degrees C under the same conditions. The concentration of FA and TMP had no obvious effect on the probe recovery under the same flow rate. In addition, the recovery of TMP and FA remained stable and showed similar trends under the condition of four concentration cycles, indicating that the intra day reproducibility of the concentration difference method was good. The recovery of brain microdialysis probes in vivo 8 h maintained a relatively stable, but certain differences existed between different brain microdialysis probes, demonstrating that each probe was required for recovery correction in vivo experiment. Microdialysis sampling can be used for the local brain pharmacokinetic study of FA and TMP, and retrodialysis method can be used in probe recovery of FA and TMP in vivo.


Assuntos
Encéfalo/metabolismo , Ácidos Cumáricos/isolamento & purificação , Microdiálise/métodos , Pirazinas/isolamento & purificação , Animais , Cromatografia Líquida de Alta Pressão , Ácidos Cumáricos/análise , Ácidos Cumáricos/farmacocinética , Medicamentos de Ervas Chinesas , Humanos , Pirazinas/análise , Pirazinas/farmacocinética , Ratos
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