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1.
Environ Monit Assess ; 191(3): 171, 2019 Feb 19.
Artigo em Inglês | MEDLINE | ID: mdl-30783770

RESUMO

Little is known about the extent of heavy metal accumulation in traditional Chinese medicines (TCMs). In this study, the levels of lead (Pb), cadmium (Cd), arsenic (As), and mercury (Hg) in traditional animal medicines were monitored using inductively coupled plasma mass spectroscopy (ICP-MS). Additionally, for the first time, a heavy metal risk assessment strategy was used to evaluate the potential risks of traditional animal medicines by calculating estimated daily intake (EDI), target hazard quotient (THQ), and cancer risk (CR). To obtain a refined risk assessment, the frequency of exposure to traditional animal medicines was determined from questionnaire data, and the safe factor for TCM was applied. Based on the standard levels for leech, it was found that earthworm, hive, scorpion, and leech accumulated high levels of heavy metals. The combined THQ (cTHQ) values indicated that ingestion of most traditional animal medicines would not pose a risk to the health of either male or female human beings. However, it was indicated that attention should be paid to the potential risk associated with cicada slough, earthworm, scorpion, turtle shells, and hive. Among heavy metals, As and Hg contributed to a major extent to the risk to human health. The CR assessment for Pb and As indicated that, with the exception of earthworm, the cancer risk was less than the acceptable lifetime risk for both males and females. Owing to the higher body weight, both THQ and CR were generally lower for males than for females.


Assuntos
Arsênio/análise , Monitoramento Ambiental/métodos , Materia Medica/química , Medicina Tradicional Chinesa , Metais Pesados/análise , Animais , Feminino , Humanos , Masculino , Materia Medica/normas , Medicina Tradicional Chinesa/normas , Medição de Risco
2.
ChemSusChem ; 11(1): 185-192, 2018 01 10.
Artigo em Inglês | MEDLINE | ID: mdl-29193841

RESUMO

Supported liquid membranes (SLMs) based on ionic liquids (ILs) with not only high gas permeability and selectivity, but also high stability under high pressure, are highly desired for gas separation applications. In this work, permeable and selective polyamide network (PN) layers are deposited on the surface of SLMs by utilizing the cross-linking reaction of trimesoyl chloride, which was pre-dispersed in the SLMs, and vapor of amine linkers. The vapor cross-linking method makes it easy to control the growth and aggregation of PN layers, owing to the significantly reduced reaction rate, and thereby ensuring the good distribution of PN layers on the surface of SLMs. With rational choice of amine linkers and optimization of vapor cross-linking conditions, the prepared sandwich-like PN@SLMs with ILs embedded homogeneously within polymeric matrices displayed much-improved CO2 permeability and CO2 /N2 selectivity in relation to the pristine SLMs. Moreover, those SLMs with ILs impregnated into porous supports physically displayed improved stability under high pressure after vapor cross-linking, because the PN layers formed on the surface of SLMs help prevent the ILs from being squeezed out. This interfacial engineering strategy represents a significant advance in the surface modification of SLMs to endow them with promising applications in CO2 capture.


Assuntos
Dióxido de Carbono/isolamento & purificação , Líquidos Iônicos , Membranas Artificiais , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Reagentes para Ligações Cruzadas/química , Microscopia Eletrônica de Varredura , Polímeros/química , Porosidade , Espectroscopia de Infravermelho com Transformada de Fourier , Termogravimetria
3.
Int Immunopharmacol ; 28(2): 1018-25, 2015 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-26330101

RESUMO

Ferulic acid (FA) is a dietary phenolic acid and has a wide range of therapeutic effects, including anti-aging, antitumor activity and antihypertensive effects. The aim of present study was to evaluate the inhibitory effects of FA on cell inflammation and oxidative stress against hydrogen peroxide (H2O2)-induced injury in rat vascular smooth muscle cells (VSMCs) in vitro. VSMCs were pretreated with FA 2h before H2O2 incubation. The results suggested that FA inhibited H2O2-induced cell injury by reducing the MDA and increasing the SOD activity and GSH content. In rat VSMCs exposed to H2O2, FA increased the cell viability and restored the mitochondrial membrane depolarization. The level of ROS generation was reduced by pretreatment with FA through inhibiting the expression of NADPH oxidase and down-regulating MAPK and AKT pathways. We found that H2O2 stimulated the production of IL-6, IL-1ß, TNF-α and NO, which could be reduced by pretreatment with FA through inhibiting the p-NF-κB as well as the iNOS expression. In conclusion, our results show that FA may serve as a novel drug in the treatment of these pathologies by inhibiting NADPH oxidase and NF-κB and subsequently decreasing VSMC oxidative stress and inflammation. These suggest that the inhibitory effect of FA on VSMC inflammation and oxidative stress is partially attributed to depressing NADPH and NF-κB expressions in VSMCs, decreasing the ROS production and reducing apoptosis of VSMCs.


Assuntos
Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Ácidos Cumáricos/farmacologia , Células Endoteliais/efeitos dos fármacos , Ligusticum , Miócitos de Músculo Liso/efeitos dos fármacos , NADPH Oxidases/metabolismo , Animais , Células Cultivadas , Citocinas/metabolismo , Células Endoteliais/fisiologia , Ativação Enzimática/efeitos dos fármacos , Peróxido de Hidrogênio/metabolismo , Masculino , Medicina Tradicional Chinesa , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Miócitos de Músculo Liso/fisiologia , NADPH Oxidases/genética , NF-kappa B/metabolismo , Ratos , Ratos Sprague-Dawley
4.
Phytomedicine ; 20(12): 1048-54, 2013 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-23746952

RESUMO

The 2-kidney, 1-clip (2K,1C) model of hypertension was used to investigate the potential antihypertensive and antioxidant effect of imperatorin extracted from the root of radix angelicae. After 10 weeks treatment of imperatorin, mean blood pressure (MBP) of 2K,1C hypertensive rats was obtained, and superoxide dismutase (SOD), nitric oxide (NO) and nitric oxide synthase (NOS) were measured. Malondialdehyde (MDA) and glutathione (GSH) levels, catalase (CATA), xanthine oxidase (XOD), angiotensinII (Ang II) and endothelin (ET) levels of kidney were evaluated with commercial kits. Nicotinamide adenine dinucleotidephosphate (NADPH) oxidase subunits of the renal cortial tissues were determined by RT-PCR and Western blot. 8-Iso-prostaglandin F2α (8-iso-PGF2α) of 24h urinary excretion was also measured by ELISA. MBP was significantly reduced by treatment with IMP (6.25, 12.5 and 25 mg/kg/day, i.g.) in 2K,1C hypertensive rats. Meanwhile, we found that renal CATA and XOD activities, GSH levels, plasma NO and NOS contents were significantly increased in IMP-treated groups. Plasma ET, renal Ang II levels, MDA and the 24h urinary excretion of 8-iso-PGF2α in the IMP treated group were lower than control SD group. After that, we found the mRNA expressions and protein levels of NADPH oxidase subunits in the clipped kidney were markedly reduced after IMP treated in 2K,1C hypertensive rats. IMP showed antihypertensive and antioxidant effects in the renal injury of renovascular hypertensive rats, suggesting that IMP could be of therapeutic use in preventing renal injury related hypertension.


Assuntos
Angelica/química , Anti-Hipertensivos/farmacologia , Antioxidantes/metabolismo , Furocumarinas/farmacologia , Hipertensão Renovascular/tratamento farmacológico , Animais , Anti-Hipertensivos/administração & dosagem , Anti-Hipertensivos/isolamento & purificação , Antioxidantes/análise , Pressão Sanguínea/efeitos dos fármacos , Modelos Animais de Doenças , Furocumarinas/administração & dosagem , Furocumarinas/isolamento & purificação , Hipertensão Renovascular/metabolismo , Hipertensão Renovascular/fisiopatologia , Rim/efeitos dos fármacos , Rim/metabolismo , Rim/fisiopatologia , Masculino , Glicoproteínas de Membrana/efeitos dos fármacos , Glicoproteínas de Membrana/metabolismo , NADPH Oxidase 2 , NADPH Oxidases/efeitos dos fármacos , NADPH Oxidases/genética , NADPH Oxidases/metabolismo , Óxido Nítrico/análise , Óxido Nítrico/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Raízes de Plantas/química , Ratos , Ratos Sprague-Dawley
5.
J Sep Sci ; 36(13): 2096-103, 2013 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-23640922

RESUMO

The epidermal growth factor receptors (EGFRs) are significant targets for screening active compounds. In this work, an analytical method was established for rapid screening, separation, and identification of EGFRs antagonists from Curcuma longa. Human embryonic kidney 293 cells with a steadily high expression of EGFRs were used to prepare the cell membrane stationary phase in a cell membrane chromatography model for screening active compounds. Separation and identification of the retention chromatographic peaks was achieved by HPLC-MS. The active sites, docking extents and inhibitory effects of the active compounds were also demonstrated. The screening result found that ar-turmerone, curcumin, demethoxycurcumin, and bisdemethoxycurcumin from Curcuma longa could be active components in a similar manner to gefitinib. Biological trials showed that all of four compounds can inhibit EGFRs protein secretion and cell growth in a dose-dependent manner, and downregulate the phosphorylation of EGFRs. This analytical method demonstrated fast and effective characteristics for screening, separation and identification of the active compounds from a complex system and should be useful for drug discovery with natural medicinal herbs.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Curcuma/química , Curcumina/análogos & derivados , Receptores ErbB/antagonistas & inibidores , Espectrometria de Massas/métodos , Curcumina/isolamento & purificação , Curcumina/farmacologia , Células HEK293 , Humanos
6.
Zhong Yao Cai ; 34(7): 1094-7, 2011 Jul.
Artigo em Chinês | MEDLINE | ID: mdl-22066407

RESUMO

OBJECTIVE: To analyse the inhibition effect of taspine derivatives on human Liver cancer SMMC7721 cell and its mechanism. METHODS: The effects of five taspine derivatives on SMMC7721 cell growth were determined by MTT. The flow cytometry was used to determine the cell cycle. The effects of Tas-D1 on the EGF and VEGF in SMMC7721 cell were determined by ELISA. The mRNA level of EGF and VEGF in SMMC7721 cell was determined by RT-PCR. RESULTS: The MTT assay demonstrated that the taspine derivative Tas-D1 significantly inhibited the growth of SMMC7721 cell in a dose-dependent manner. Cell was stopped at S phase by Tas-D1. Tas-D1 inhibited the expression of EGF and VEGF and their mRNA in a dose-dependent manner (P<0.05). CONCLUSIONS: The taspine derivative Tas-D1 can inhibit the growth of human Liver cancer SMMC7721 cell and change cell cycle, which may be related to the inhibition of EGF and VEGF expression.


Assuntos
Alcaloides/farmacologia , Antineoplásicos/farmacologia , Proliferação de Células/efeitos dos fármacos , Fator de Crescimento Epidérmico/metabolismo , Neoplasias Hepáticas/patologia , Fator A de Crescimento do Endotélio Vascular/metabolismo , Alcaloides/administração & dosagem , Antineoplásicos/administração & dosagem , Carcinoma Hepatocelular/metabolismo , Carcinoma Hepatocelular/patologia , Caulophyllum/química , Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Fator de Crescimento Epidérmico/genética , Citometria de Fluxo , Humanos , Neoplasias Hepáticas/metabolismo , Reação em Cadeia da Polimerase , RNA Mensageiro/genética , RNA Mensageiro/metabolismo
7.
J Pharm Anal ; 1(2): 81-91, 2011 May.
Artigo em Inglês | MEDLINE | ID: mdl-29403684

RESUMO

In China, traditional Chinese medicines (TCMs) have been used in clinical applications for thousands of years. The successful hyphenation of high-Performance liquid chromatography (HPLC) and mass spectrometry (MS) has been applied widely in TCMs and biological samples analysis. Undoubtedly, HPLC/MS technique has facilitated the understanding of the treatment mechanism of TCMs. We reviewed more than 350 published papers within the last 5 years on HPLC/MS in the analysis of TCMs. The present review focused on the applications of HPLC/MS in the component analysis, metabolites analysis, and pharmacokinetics of TCMs etc. 50% of the literature is related to the component analysis of TCMs, which show that this field is the most populär type of research. In the metabolites analysis, HPLC coupled with electrospray ionization quadrupole time-of-flight tandem mass spectrometry has been demonstrated to be the powerful tool for the characterization of structural features and fragmentation behavior patterns. This paper presented a brief overview of the applications of HPLC/MS in the analysis of TCMs. HPLC/MS in the fingerprint analysis is reviewed elsewhere.

8.
Eur J Pharmacol ; 647(1-3): 126-31, 2010 Nov 25.
Artigo em Inglês | MEDLINE | ID: mdl-20813104

RESUMO

Store-operated Ca(2+) entry (SOCE) has recently been proposed to contribute to Ca(2+) influx in vascular smooth muscle cells (VSMCs). Imperatorin is known for its potent vasodilatory effects as a dietary furanocoumarin. The study was designed to examine the hypothesis that SOCE have a functional role in imperatorin-induced vasodilation. Small mesenteric resistance arteries and mesenteric VSMCs were obtained from rats. Isometric tensions of isolated artery rings were measured by a sensitive myograph system. Laser scanning confocal microscopy was used to determine the intracellular Ca(2+) concentration of fluo-3-loaded VSMCs. Imperatorin (1-100 µM) relaxed artery rings precontracted by phenylephrine in a concentration-dependent manner. In cultured mesenteric VSMCs, passive store depletion by thapsigargin and active store depletion by phenylephrine both induced Ca(2+) influx due to SOCE. Imperatorin didn't inhibit SOCE-mediated increases in cytosolic Ca(2+) levels evoked by the emptying of the stores. In isolated artery rings, imperatorin didn't inhibit SOCE-induced contractions due to store depletion. Our results exclude SOCE mechanism of vasodilatation by imperatorin. But imperatorin is partly similar with nifedipine in vasorelaxation effect.


Assuntos
Cálcio/metabolismo , Cálcio/farmacologia , Furocumarinas/metabolismo , Artérias Mesentéricas/efeitos dos fármacos , Vasodilatadores/metabolismo , Compostos de Anilina/metabolismo , Animais , Canais de Cálcio/efeitos dos fármacos , Canais de Cálcio/metabolismo , Canais de Cálcio/fisiologia , Sinalização do Cálcio/efeitos dos fármacos , Furocumarinas/farmacologia , Transporte de Íons/efeitos dos fármacos , Masculino , Artérias Mesentéricas/metabolismo , Músculo Liso Vascular/efeitos dos fármacos , Músculo Liso Vascular/metabolismo , Ratos , Ratos Sprague-Dawley , Vasodilatação/efeitos dos fármacos , Vasodilatação/fisiologia , Vasodilatadores/farmacologia , Xantenos/metabolismo
9.
Basic Clin Pharmacol Toxicol ; 107(6): 976-81, 2010 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-20649558

RESUMO

Caulophine is a novel fluorenone alkaloid isolated from the radix of Caulophyllum robustum Maxim. Caulophine showed high affinity for the rat myocardial cell membrane as assessed by cell membrane chromatography, suggesting that the compound may exert bioactivity in the heart. It is known that calcium plays an important role in the pathogenesis of ischaemic heart disease, and caffeine can cause calcium overload in cardiomyocytes by inducing calcium release from the sarcoplasmic reticulum. Therefore, the present study evaluated the effects of caulophine on caffeine-induced injury and calcium homeostasis in cardiomyocytes. Cardiomyocytes were pre-treated with caulophine before exposure to caffeine or potassium chloride (KCl). Cell viability was assayed using the MTT method, and lactate dehydrogenase (LDH) and malondialdehyde (MDA) were measured spectrophotometrically. Caulophine-pre-treated cardiomyocytes were incubated with Fluo-3/AM, and then caffeine or KCl was used to induce Ca(2+) overload. The total intracellular Ca(2+) concentration was measured by flow cytometry. Fluorescence densities of single cardiomyocytes were detected using a confocal microscope. Caulophine increased the viability of caffeine-injured cardiomyocytes and decreased LDH activity and MDA level in cardiomyocytes. Furthermore, caulophine significantly decreased the total intracellular free Ca(2+) concentration and intracellular calcium release in cardiomyocytes in response to caffeine. However, the same concentrations of caulophine did not affect KCl-induced calcium influx. Our results suggest that caulophine protects cardiomyocytes from caffeine-induced injury as a result of calcium antagonism. This finding provides a basis for further study and development of caulophine as a new calcium antagonist for treating ischaemic cardiovascular diseases.


Assuntos
Cafeína/efeitos adversos , Cálcio/metabolismo , Fluorenos/farmacologia , Homeostase , Miócitos Cardíacos/citologia , Compostos de Anilina/metabolismo , Animais , Sobrevivência Celular , Células Cultivadas , Corantes Fluorescentes/metabolismo , Miócitos Cardíacos/metabolismo , Cloreto de Potássio/metabolismo , Ratos , Retículo Sarcoplasmático/metabolismo , Xantenos/metabolismo
10.
Zhong Yao Cai ; 33(8): 1290-2, 2010 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-21213543

RESUMO

OBJECTIVE: To investigate the effects of Bai-Chuan capsule (BC) on the left ventricular hypertrophy in spontaneously hypertensive rats (SHR). METHODS: Taking SHR and Wistar Kyoto rats (WKY) as the model group and the control group respectively, Captopril as positive drug, administered BC 0.3 g/kg, Captopril 3.75 mg/kg or 0.5% CMC-Na to each group by ig for 3 months, and measured the change of blood pressure. The left ventricular mass index was calculated after rats were sacrificed. Left ventricle was used to pathological observations, plasma angiotensin II and aldosterone were measured by radioimmunoassay. CONCLUSION: BC can inhibit left ventricular hypertrophy, plasma level of angiotensin II and aldosterone to some extent in SHR.


Assuntos
Aldosterona/sangue , Angiotensina II/sangue , Anti-Hipertensivos/farmacologia , Medicamentos de Ervas Chinesas/farmacologia , Hipertensão/tratamento farmacológico , Hipertrofia Ventricular Esquerda/tratamento farmacológico , Animais , Anti-Hipertensivos/administração & dosagem , Apiaceae/química , Pressão Sanguínea/efeitos dos fármacos , Cápsulas , Captopril/farmacologia , Medicamentos de Ervas Chinesas/administração & dosagem , Ventrículos do Coração/efeitos dos fármacos , Ventrículos do Coração/patologia , Hipertensão/sangue , Hipertrofia Ventricular Esquerda/sangue , Hipertrofia Ventricular Esquerda/prevenção & controle , Masculino , Miocárdio/patologia , Radioimunoensaio , Distribuição Aleatória , Ratos , Ratos Endogâmicos SHR , Ratos Endogâmicos WKY
11.
Nan Fang Yi Ke Da Xue Xue Bao ; 29(12): 2362-6, 2009 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-20034876

RESUMO

OBJECTIVE: To improve the accuracy and sensitivity of cell membrane chromatography (CMC) and evaluate the feasibility of CMC in the study of subtype receptors. METHODS: Plasmids were used to transfer alpha(1B)-AR cDNA into human embryonic kidney 293 (HEK293) cell lines to obtain cell lines stably overexpressing the subtype receptors. HEK293 alpha(1B) cell membrane stationary phase (CMSP) was prepared by immobilizing the cell membrane on silica. The retention time of 9 alpha(1)-adrenoceptor ligands and capacity factors(kappa'(HEK293 alpha1B)) were calculated. The capacity factors of rat liver tissue and primary cultured rat hepatocytes were also calculated for a correlation analysis. RESULTS: The calculated capacity factors (kappa') were positively correlated to the published pKi values. The affinity rank orders were identical. The longest retention of the 9 alpha(1)-adrenoceptor ligands occurred on CMSP prepared with HEK293 alpha(1B) cell lines, while CMSP obtained from rat liver tissue showed the shortest retention of the ligands. CONCLUSION: CMC proves practical in the study of the subtype adrenoceptors. The accuracy and sensitivity of CMC can be improved using HEK293 alpha(1B) cell membrane.


Assuntos
Membrana Celular/metabolismo , Cromatografia de Afinidade/métodos , Receptores Adrenérgicos alfa 1/metabolismo , Animais , DNA Complementar/metabolismo , Feminino , Células HEK293 , Humanos , Rim/citologia , Rim/embriologia , Ligantes , Masculino , Ratos , Ratos Sprague-Dawley , Sensibilidade e Especificidade
12.
Phytother Res ; 22(12): 1605-9, 2008 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-19003951

RESUMO

The purpose of this study was to investigate the molecular mechanisms that are responsible for the antiinflammatory effect of usnic acid (UA). UA is one of the most common and abundant lichen metabolites. The present study examined the effects of UA on the tumor necrosis factor-alpha (TNF-alpha) and nitric oxide (NO) production induced by lipopolysaccharide (LPS) in RAW264.7 macrophages and the underlying molecular mechanisms. UA decreased the TNF-alpha level in LPS-stimulated RAW264.7 macrophages in dose-dependent manner, the IC(50) value was 12.8 microM. RT-PCR analysis indicated that it inhibited TNF-alpha mRNA expression. Furthermore, it inhibited NO production in LPS-activated RAW264.7 macrophages, the IC(50) value was 4.7 microM. Western blot analysis showed that UA attenuated LPS-induced synthesis of iNOS protein and nuclear translocation of NF-kappaB p65 in the macrophages, in parallel. UA also inhibited LPS-mediated I-kappaBalpha degradation. Taken together, this suggests that UA has an antiinflammatory effect by inhibiting TNF-alpha and iNOS expression, possibly through suppression of nuclear translocation of NF-kappaB p65 and I-kappaBalpha degradation.


Assuntos
Anti-Inflamatórios/farmacologia , Benzofuranos/farmacologia , Lipopolissacarídeos/farmacologia , NF-kappa B/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Fator de Necrose Tumoral alfa/biossíntese , Análise de Variância , Animais , Linhagem Celular , Sobrevivência Celular , Regulação para Baixo , Regulação da Expressão Gênica , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , Óxido Nítrico/biossíntese , RNA/genética , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Usnea/química
13.
Int J Biol Macromol ; 43(3): 320-4, 2008 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-18619484

RESUMO

Taspine solid lipid nanoparticles (Ta-SLN) and taspine solid lipid nanoparticles modified by galactoside (Ta-G2SLN) were prepared by the film evaporation-extrusion method. The nanoparticles were spherical or near-spherical particles with smooth surface, small size and high encapsulation efficiency. Ta-G2SLN and Ta-SLN showed significant inhibition on 7721 cell growth. Intravenous injection of either Ta-SLN or Ta-G2SLN resulted in a higher plasma and liver concentration and a longer retention time in mice compared with the administration of Ta. These results suggested that SLN tended to be preferentially delivered to the liver and Ta-G2SLN may further enhance liver targeting.


Assuntos
Alcaloides/administração & dosagem , Alcaloides/metabolismo , Portadores de Fármacos/administração & dosagem , Portadores de Fármacos/metabolismo , Lipídeos/química , Fígado/metabolismo , Nanopartículas/química , Alcaloides/farmacocinética , Alcaloides/farmacologia , Animais , Proliferação de Células/efeitos dos fármacos , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Galactosídeos/química , Injeções Intravenosas , Fígado/citologia , Fígado/efeitos dos fármacos , Camundongos
14.
J Pharm Biomed Anal ; 46(1): 170-6, 2008 Jan 07.
Artigo em Inglês | MEDLINE | ID: mdl-17889477

RESUMO

Taspine is a bioactive aporphine alkaloid, which has many potent pharmacological effects. A simple, rapid HPLC method to quantify taspine in mouse plasma and tissue homogenates containing either taspine solution or liposome was developed and validated. Sample preparation was achieved by liquid-liquid extraction with acetoacetate. Taspine was separated on a C(18) reversed phase HPLC column, and quantified by its absorbance at 245 nm. The pharmacokinetics and tissue distribution after intravenous administrations of taspine liposome (L-Ta) and taspine solution (Ta) to ICR mice were then compared. The area under the plasma concentration-time curve (AUC) was higher for L-Ta than for Ta. In contrast, the total body clearance (CL), apparent volume of distribution V(c) and plasma half-life for the distribution (t(1/2 alpha)) and elimination phase (t(1/2 beta)) were lower for L-Ta, in comparison to the respective parameter of Ta. The AUC values were higher in the lung than in other organs for both L-Ta and Ta. The AUC in the spleen, kidney and liver of L-Ta were higher than those of Ta. However, the heart and brain AUC of Ta was higher than that of L-Ta. It can thus be concluded that incorporation into liposomes prolonged taspine retention within the systemic circulation, increased its distribution to the spleen and liver but reduced its distribution to the heart and brain.


Assuntos
Alcaloides/farmacocinética , Aporfinas/farmacocinética , Cromatografia Líquida de Alta Pressão/métodos , Alcaloides/sangue , Alcaloides/química , Animais , Aporfinas/sangue , Aporfinas/química , Área Sob a Curva , Disponibilidade Biológica , Estabilidade de Medicamentos , Liofilização/métodos , Meia-Vida , Injeções Intravenosas , Lipossomos/química , Masculino , Taxa de Depuração Metabólica , Camundongos/sangue , Camundongos Endogâmicos ICR , Estrutura Molecular , Solubilidade , Soluções/química , Temperatura , Fatores de Tempo , Distribuição Tecidual
15.
J Ethnopharmacol ; 114(2): 212-7, 2007 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-17869038

RESUMO

The aim of this study was to screen for the anti-inflammatory activity of fractions and compounds from Atractylodes macrocephala Koidz. The rhizomes of Atractylodes macrocephala were treated with supercritical CO(2) fluid and the extract was separated by normal-phase and reverse-phase column chromatography. The separated samples were screened with white blood cell membrane (WBCM) chromatography (WBCM-C). The anti-inflammatory effects of these fractions and components were tested pharmacologically in vivo. The results indicated that the retention characteristics of the petrol-ether (1:1, v/v) fraction (BZC-2) of the supercritical CO(2) extract, the atractylenolide I and 14-acetoxy-12-senecioyloxytetradeca-2E,8E,10E-trien-4, 6-diyn-1-ol isolated from BZC-2 as active fractions and components were similar to that of dexamethasone in WBCM-C. Therefore, they may act on WBCM and its receptors. BZC-2 has shown anti-inflammatory effects in acute and chronic inflammation models in rats and mice. Oral administration of atractylenolide I and 14-acetoxy-12-senecioyloxytetradeca-2E,8E,10E-trien-4,6-diyn-1-ol produced significant anti-inflammatory effects in acute and chronic inflammation models in mice. The screening results with WBCM-C were correlated significantly with pharmacological effects in vivo. Atractylenolide I and 14-acetoxy-12-senecioyloxytetradeca-2E,8E,10E-trien-4,6-diyn-1-ol were the main components of Atractylodes macrocephala that were effective as anti-inflammatory agents.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Atractylodes/química , Ácido Acético/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Permeabilidade Capilar/efeitos dos fármacos , Carragenina , Membrana Celular/efeitos dos fármacos , Cromatografia , Fibra de Algodão , Dexametasona/farmacologia , Avaliação Pré-Clínica de Medicamentos , Edema/induzido quimicamente , Edema/prevenção & controle , Feminino , Granuloma/patologia , Granuloma/prevenção & controle , Leucócitos/química , Leucócitos/efeitos dos fármacos , Espectroscopia de Ressonância Magnética , Masculino , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Coelhos
16.
Yao Xue Xue Bao ; 42(5): 525-8, 2007 May.
Artigo em Chinês | MEDLINE | ID: mdl-17703777

RESUMO

To analyze the constituents in supercritical fluid CO2 extraction (SFE-CO2) of Radix caulophylli, the Radix caulophylli was extracted with SFE-CO2, and analyzed by gas chromatography-mass spectrometry (GC-MS). The GC-MS analysis with a DB-5MS capillary column (30 mm x 0.32 mm ID, 0.25 microm film thickness) was used. The inlet temperature was maintained at 280 degrees C. The column oven was held at 80 degrees C for 2 min, then programmed from 80 to 280 degrees C at 5 degrees C x min(-1) and, finally, held for 4 min. Helium at a constant flow rate of 2.0 mL x min(-1) was used as the carrier gas. The mass spectrometry conditions were as follows: ionization energy, 70 eV; ion source temperature, 200 degrees C. The mass selective detector was operated in the TIC mode (m/z was from 40 - 500). For the first time 49 peaks were separated and identified, the compounds were quantitatively determined by normalization method, and the identified compounds represent 97.44% of total GC peak areas. Viz, n-hexadecanoic acid (31.4%), (E, E) -9, 12-octadecadienoic acid (26.54%), (Z)-7-tetradecenal (9.4%), hexadecenoic acid (3.23%), 10-undecenal (3.22%), octadecanoic acid (2.25%), and caulophylline (1.76%) etc. The results will provide important foundation for understanding the constituents and further exploitation of Radix caulophylli.


Assuntos
Caulophyllum/química , Ácido Palmítico/análise , Dióxido de Carbono , Cromatografia com Fluido Supercrítico , Cromatografia Gasosa-Espectrometria de Massas , Ácido Linoleico/análise , Raízes de Plantas/química , Plantas Medicinais/química
17.
Zhong Yao Cai ; 30(4): 429-32, 2007 Apr.
Artigo em Chinês | MEDLINE | ID: mdl-17674796

RESUMO

OBJECTIVE: To investigate the effect of thaspine on the cellular proliferation, apoptosis and cell cycle in A549 cell line. METHODS: A549 cell was cultured with different concentrations of thaspine. Cellular proliferation was detected with MTT, apoptosis and cell cycle were checked with Flow Cytometer, and change of microstructure was observed by transmission electron microscope. RESULTS: Thaspine could inhibit the proliferation and induce apoptosis of A549 cell in a time-dose dependent manner. Cell cycle was significantly stopped at the S phase by thaspine with FCM technology. Under electronic microscope, the morphology of A549 cell showed nuclear karyopycnosis, chromatin agglutination and typical apoptotic body when the cell was treated with thaspine. CONCLUSION: Thaspine has the effects of anti-tumor and inducing apoptosis.


Assuntos
Alcaloides/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Citometria de Fluxo , Humanos , Neoplasias Pulmonares/patologia , Neoplasias Pulmonares/ultraestrutura , Microscopia Eletrônica de Transmissão , Plantas Medicinais/química
18.
Zhongguo Zhong Yao Za Zhi ; 32(10): 953-6, 2007 May.
Artigo em Chinês | MEDLINE | ID: mdl-17655156

RESUMO

OBJECTIVE: To study the inhibition effect of taspine on mouse S180 sarcoma and its mechanism. METHOD: The mouse S180 sarcoma model was established and used to observe the antitumor activity of taspine. The microvessel density and protein expressing of the VEGF, bFGF, Bcl-2 and Bax in the tumor were measured by immunohistochemistry. RESULT: Taspine showed antitumor activity on the mouse S180 sarcoma in a good dose-dependent manner. The inhibition rates on tumor of taspine at low, middle and high concentrations were 39.08% , 43.99% and 48.60%, respectively. The microvessel density and protein expressing of the VEGF, bFGF, Bcl-2 and Bax in the tumor were decreased compared with the negative control. The ratio of Bax to Bcl-2 was increased. CONCLUSION: Taspine has antitumor effect on the S180 sarcoma, and the mechanism may be through the way of decreasing the expressing of the VEGF, bFGF, Bcl-2 and Bax and inducing the vascular endothelial cell apoptosis.


Assuntos
Alcaloides/uso terapêutico , Antineoplásicos Fitogênicos/uso terapêutico , Sarcoma 180/prevenção & controle , Alcaloides/isolamento & purificação , Animais , Antineoplásicos Fitogênicos/isolamento & purificação , Berberidaceae/química , Linhagem Celular Tumoral , Relação Dose-Resposta a Droga , Fator 2 de Crescimento de Fibroblastos/metabolismo , Masculino , Camundongos , Neovascularização Patológica/metabolismo , Neovascularização Patológica/prevenção & controle , Fitoterapia , Raízes de Plantas/química , Plantas Medicinais/química , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Sarcoma 180/irrigação sanguínea , Sarcoma 180/patologia , Fator A de Crescimento do Endotélio Vascular/metabolismo , Proteína X Associada a bcl-2/metabolismo
19.
Eur J Pharmacol ; 573(1-3): 170-5, 2007 Nov 14.
Artigo em Inglês | MEDLINE | ID: mdl-17662269

RESUMO

The purpose of the present study was to investigate the effect of imperatorin on vasodilatation and its possible mechanisms. Isometric tension of rat mesenteric arterial rings was recorded by a myograph system in vitro. The results showed that imperatorin at more than 10 muM concentration-dependently relaxed rat mesenteric arteries pre-contracted by potassium chloride (KCl) and endothelin-1, and human omental arteries pre-contracted by noradrenaline and U46619. Removal of the endothelium did not affect imperatorin-induced relaxant responses, suggesting that the vasodilatation effect is independent of the endothelium. Co-incubation with imperatorin resulted in rightward shift of concentration-response curves of KCl, calcium chloride (CaCl(2)) and noradrenaline in a non-parallel manner; 5-hydroxytryptamine (5-HT) concentration-response curves were shifted towards right in a parallel manner by imperatorin 10 and 30 muM, but markedly suppressed by imperatorin 100 muM. These results suggest that the inhibitory effect of imperatorin is mainly via voltage dependent calcium channel and possibly receptor operated calcium channel. beta-adrenoceptor, ATP-sensitive potassium channel and inwardly rectifying potassium channel were not involved in the vasodilatation, whereas blockage of calcium-activated potassium channel with tetraethylammonium had effect. Furthermore, in Ca(2+)-free medium, imperatorin concentration-dependently depressed the vasoconstrictions derived from noradrenaline and CaCl(2), and resulted in a decreased contractile response induced by caffeine, indicating a role of inhibiting extracellular Ca(2+) influx and intracellular Ca(2+) release from Ca(2+) store. Taken together, our results suggest that imperatorin induces vasodilatation by possible mechanisms inhibiting voltage dependent calcium channel and receptor-mediated Ca(2+)influx and Ca(2+)release. Opening calcium-activated potassium channel and competitive antagonism of 5-HT receptors may also contribute to this vasodilatation effect.


Assuntos
Canais de Cálcio/fisiologia , Cálcio/metabolismo , Furocumarinas/farmacologia , Vasodilatação/efeitos dos fármacos , Ácido 15-Hidroxi-11 alfa,9 alfa-(epoximetano)prosta-5,13-dienoico/farmacologia , Animais , Artérias/efeitos dos fármacos , Artérias/metabolismo , Artérias/fisiologia , Compostos de Bário/farmacologia , Cafeína/farmacologia , Cloreto de Cálcio/farmacologia , Cloretos/farmacologia , Dimetil Sulfóxido/farmacologia , Relação Dose-Resposta a Droga , Endotelina-1/farmacologia , Endotélio Vascular/fisiologia , Epinefrina/farmacologia , Glibureto/farmacologia , Técnicas In Vitro , Artérias Mesentéricas/efeitos dos fármacos , Artérias Mesentéricas/metabolismo , Artérias Mesentéricas/fisiologia , Omento/irrigação sanguínea , Cloreto de Potássio/farmacologia , Propranolol/farmacologia , Ratos , Ratos Sprague-Dawley , Serotonina/farmacologia , Tetraetilamônio/farmacologia
20.
Zhong Yao Cai ; 30(2): 220-3, 2007 Feb.
Artigo em Chinês | MEDLINE | ID: mdl-17571776

RESUMO

OBJECTIVE: To study the technological parameters of the extraction process of the total alkaloids from Caulopyhllum robstum. METHODS: Taspine, whiVh is main component of the total alkaloids from Caulopyhllum robustum, was selected as an evaluating marker and determined by HPLC. The orthogonal test was used to optimize extracting conditions in the process of acid water extraction. Then the optimized conditions for purification using cation exchange resin were investigated. RESULTS: The optimized conditions in the process of acid water extraction were 1% hydrochloric acid as much as seven times of the medicine amount for 24hs and three times. Then the extraction of acid water was purified with a column of macroporous cation exchange resin LSD001 at 2 ml/min of flow rate, then eluted with 10BV of 4% aqueous ammonia ethanol. The extraction ratio of the total alkaloids was 1. 35% and the content of taspine of the total alkaloids was 6. 80%. CONCLUSION: This technology is simply, cheap effective and feasible for manufacture in great scale.


Assuntos
Alcaloides/isolamento & purificação , Caulophyllum/química , Plantas Medicinais/química , Tecnologia Farmacêutica/métodos , Alcaloides/análise , Alcaloides/química , Resinas de Troca de Cátion , Cromatografia Líquida de Alta Pressão , Etanol/administração & dosagem , Concentração de Íons de Hidrogênio , Raízes de Plantas/química , Caules de Planta/química , Solventes
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