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1.
Hum Genet ; 2020 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-32239398

RESUMO

Aiming to uncover a shared genetic basis of abdominal obesity and osteoporosis, we performed a bivariate GWAS meta-analysis of femoral neck BMD (FNK-BMD) and trunk fat mass adjusted by trunk lean mass (TFMadj) in 11,496 subjects from 6 samples, followed by in silico replication in the large-scale UK Biobank (UKB) cohort. A series of functional investigations were conducted on the identified variants. Bivariate GWAS meta-analysis identified two novel pleiotropic loci 12q15 (lead SNP rs73134637, p = 3.45 × 10-7) and 10p14 (lead SNP rs2892347, p = 2.63 × 10-7) that were suggestively associated and that were replicated in the analyses of related traits in the UKB sample (osteoporosis p = 0.06 and 0.02, BMI p = 0.03 and 4.61 × 10-3, N up to 499,520). Cis-eQTL analysis demonstrated that allele C at rs73134637 was positively associated with IFNG expression in whole blood (N = 369, p = 0.04), and allele A at rs11254759 (10p14, p = 9.49 × 10-7) was negatively associated with PRKCQ expression in visceral adipose tissue (N = 313, p = 0.04) and in lymphocytes (N = 117, p = 0.03). As a proof-of-principle experiment, the function of rs11254759, which is 235 kb 5'-upstream from PRKCQ gene, was investigated by the dual-luciferase reporter assay, which clearly showed that the haplotype carrying rs11254759 regulated PRKCQ expression by upregulating PRKCQ promoter activity (p = 4.60 × 10-7) in an allelic specific manner. Mouse model analysis showed that heterozygous PRKCQ deficient mice presented decreased fat mass compared to wild-type control mice (p = 3.30 × 10-3). Mendelian randomization analysis demonstrated that both FNK-BMD and TFMadj were causally associated with fracture risk (p = 1.26 × 10-23 and 1.18 × 10-11). Our findings may provide useful insights into the genetic association between osteoporosis and abdominal obesity.

2.
J Integr Med ; 18(3): 229-241, 2020 05.
Artigo em Inglês | MEDLINE | ID: mdl-32307268

RESUMO

OBJECTIVE: Lung-toxin Dispelling Formula No. 1, referred to as Respiratory Detox Shot (RDS), was developed based on a classical prescription of traditional Chinese medicine (TCM) and the theoretical understanding of herbal properties within TCM. Therapeutic benefits of using RDS for both disease control and prevention, in the effort to contain the coronavirus disease 2019 (COVID-19), have been shown. However, the biochemically active constituents of RDS and their mechanisms of action are still unclear. The goal of the present study is to clarify the material foundation and action mechanism of RDS. METHODS: To conduct an analysis of RDS, an integrative analytical platform was constructed, including target prediction, protein-protein interaction (PPI) network, and cluster analysis; further, the hub genes involved in the disease-related pathways were identified, and the their corresponding compounds were used for in vitro validation of molecular docking predictions. The presence of these validated compounds was also measured in samples of the RDS formula to quantify the abundance of the biochemically active constituents. In our network pharmacological study, a total of 26 bioinformatic programs and databases were used, and six networks, covering the entire Zang-fu viscera, were constructed to comprehensively analyze the intricate connections among the compounds-targets-disease pathways-meridians of RDS. RESULTS: For all 1071 known chemical constituents of the nine ingredients in RDS, identified from established TCM databases, 157 passed drug-likeness screening and led to 339 predicted targets in the constituent-target network. Forty-two hub genes with core regulatory effects were extracted from the PPI network, and 134 compounds and 29 crucial disease pathways were implicated in the target-constituent-disease network. Twelve disease pathways attributed to the Lung-Large Intestine meridians, with six and five attributed to the Kidney-Urinary Bladder and Stomach-Spleen meridians, respectively. One-hundred and eighteen candidate constituents showed a high binding affinity with SARS-coronavirus-2 3-chymotrypsin-like protease (3CLpro), as indicated by molecular docking using computational pattern recognition. The in vitro activity of 22 chemical constituents of RDS was validated using the 3CLpro inhibition assay. Finally, using liquid chromatography mass spectrometry in data-independent analysis mode, the presence of seven out of these 22 constituents was confirmed and validated in an aqueous decoction of RDS, using reference standards in both non-targeted and targeted approaches. CONCLUSION: RDS acts primarily in the Lung-Large Intestine, Kidney-Urinary Bladder and Stomach-Spleen meridians, with other Zang-fu viscera strategically covered by all nine ingredients. In the context of TCM meridian theory, the multiple components and targets of RDS contribute to RDS's dual effects of health-strengthening and pathogen-eliminating. This results in general therapeutic effects for early COVID-19 control and prevention.


Assuntos
Antivirais/química , Betacoronavirus/química , Infecções por Coronavirus/tratamento farmacológico , Medicamentos de Ervas Chinesas/química , Medicina Tradicional Chinesa , Simulação de Acoplamento Molecular , Pneumonia Viral/tratamento farmacológico , Antivirais/uso terapêutico , Betacoronavirus/enzimologia , Infecções por Coronavirus/prevenção & controle , Infecções por Coronavirus/virologia , Cisteína Endopeptidases/química , Medicamentos de Ervas Chinesas/uso terapêutico , Humanos , Espectrometria de Massas , Pandemias/prevenção & controle , Pneumonia Viral/prevenção & controle , Pneumonia Viral/virologia , Mapas de Interação de Proteínas , Proteínas não Estruturais Virais/química
3.
Aging (Albany NY) ; 11(12): 4032-4049, 2019 06 19.
Artigo em Inglês | MEDLINE | ID: mdl-31219800

RESUMO

The reproductive tissues are negatively influenced by estrogens in hormone therapy. Qingyan formula ethanol extract (QYFE)'s estrogenic effects and safety on reproductive tissues after long-term administration and its mechanism via estrogen receptor (ER) pathway haven't been studied. Here, we characterized its estrogenic effects using ovariectomized rats together with in vitro studies for further molecular characterization. Ovariectomized rats were treated with QYFE at doses of 0.7, 1.4, and 2.8g/kg for 12 weeks. The results showed QYFE has a potent estrogenic activity, as indicated by restoring the disappeared estrous cycle, antagonizing the atrophy of uterus, vagina and mammary gland, and the estrogen decline in circulation caused by ovariectomy. In addition, QYFE upregulated ERα and ERß expressions and had a less stimulatory effect on PCNA and ki-67 antigen in reproductive tissues compared with estradiol valerate. QYFE components can bind to ERα and ERß, significantly increased ERα/ß-ERE luciferase reporter gene expression, upregulated the expressions of ERs, PR and pS2 in MCF-7 cells at protein and gene level. All these activities were significantly inhibited by the ER antagonist ICI182,780. QYFE's estrogenic activity maybe mediated by stimulating biosynthesis of estrogen and increasing the quantity of ERs in target tissue and via active ER to ERE-independent gene regulation.

4.
Oecologia ; 190(1): 269-272, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-30953166

RESUMO

Unfortunately, the panels of (f) in Figures 1, 2, and 4.

5.
Oecologia ; 189(3): 769-779, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30725373

RESUMO

Increasing availability of reactive nitrogen (N) threatens plant diversity in diverse ecosystems. While there is mounting evidence for the negative impacts of N deposition on one component of diversity, species richness, we know little about its effects on another one, species evenness. It is suspected that ecosystem management practice that removes nitrogen from the ecosystem, such as hay-harvesting by mowing in grasslands, would mitigate the negative impacts of N deposition on plant diversity. However, empirical evidence is scarce. Here, we reported the main and interactive effects of N deposition and mowing on plant diversity in a temperate meadow steppe with 4-year data from a field experiment within which multi-level N addition rates and multiple N compounds are considered. Across all the types of N compounds, species richness and evenness significantly decreased with the increases of N addition rate, which was mainly caused by the growth of a tall rhizomatous grass, Leymus chinensis. Such negative impacts of N addition were accumulating with time. Mowing significantly reduced the dominance of L. chinensis, and mitigated the negative impacts of N deposition on species evenness. We present robust evidence that N deposition threatened biodiversity by reducing both species richness and evenness, a process which could be alleviated by mowing. Our results highlight the changes of species evenness in driving the negative impacts of N deposition on plant diversity and the role of mowing in mediating such negative impacts of N deposition.


Assuntos
Ecossistema , Plantas , Biodiversidade , Nitrogênio , Poaceae
6.
Rejuvenation Res ; 22(6): 465-477, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30672382

RESUMO

Radix paeoniae alba (RPA) and Veratrum nigrum (VN) L. belong to the 18 incompatible medicaments and have been prohibited for thousands of years in China. Previous studies focused on the chemical constituents that induced the toxicological response of the two agents, but this study offers preliminary insight into the pharmacodynamics and mechanism on estrogenic activity, which is responsible for their incompatibility. We undertook a characterization of the interaction on estrogenic activity of RPA and VN using in vivo models of immature and ovariectomized (OVX) mice and in vitro studies focused on estrogen receptor (ER) pathway for further mechanism. VN disturbed the estrogenic efficacy of RPA in promoting development of uterus and vagina in immature mice, and reversing the atrophy of reproductive tissues in OVX mice by decreasing the increase of serum estrogen level and upregulation of ER expression in reproductive tissues by treatment with RPA. Besides, VN antagonized the estrogenic efficacy of RPA in stimulating the binding with ERα and ERß, increasing ERα/ß-estrogen response element (ERE) luciferase reporter gene expression and promoting MCF-7 cell viability. This study provided evidence that VN antagonized the estrogenic efficacy of RPA by decreasing the up-regulations of estrogen biosynthesis in circulation and ERs in target tissues caused by RPA, and through ER-ERE-dependent pathway.


Assuntos
Estrogênios/metabolismo , Ovário/metabolismo , Paeonia/química , Extratos Vegetais/farmacologia , Receptores Estrogênicos/metabolismo , Veratrum/química , Animais , Feminino , Humanos , Células MCF-7 , Camundongos , Ovariectomia , Ovário/efeitos dos fármacos , Ovário/cirurgia , Útero/efeitos dos fármacos , Útero/metabolismo , Útero/cirurgia , Vagina/efeitos dos fármacos , Vagina/metabolismo , Vagina/cirurgia
7.
Phytother Res ; 33(1): 117-129, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30375037

RESUMO

Radix Paeoniae Alba (RPA) is widely used in clinical treatment for gynecological diseases, particularly abnormal menstruation, menstrual pain, and breast tenderness; however, no scientific evidence base links RPA to estrogen replacement therapy. In this study, we characterize estrogenic activity of RPA using immature and ovariectomized (OVX) mice together with in vitro studies focus on estrogen receptor (ER) pathway for molecular mechanism. RPA treatments demonstrated significant estrogenic activity, as indicated by promoting the development of uterus and vagina in immature mice, reversing the atrophy of uterus and vagina in OVX mice, up-regulating the expressions of ERα and ERß at protein and mRNA level in reproductive tissues. Meanwhile, RPA significantly increased serum estradiol and clearly decreased serum luteinizing hormone and follicle-stimulating hormone of immature/OVX mice. Moreover, RPA could induce ER positive MCF-7 cell from S-phase to G2 stage and induce proliferation and no influence on ER negative MDA-MB-231 cell. RPA could bind with ERα and ERß and significantly stimulate ERα/ß-estrogen response element (ERE) luciferase reporter gene expression. All activities were inhibited by the ER antagonist ICI 182,780. This study illustrates RPA exerts estrogenic effects by stimulating biosynthesis of estrogen in circulation, up-regulating ERs in target tissues, and mimicking the estrogen through ER-ERE-dependent pathway.


Assuntos
Medicamentos de Ervas Chinesas/química , Estrogênios/farmacologia , Paeonia/química , Receptores Estrogênicos/metabolismo , Útero/efeitos dos fármacos , Vagina/efeitos dos fármacos , Animais , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêutico , Feminino , Humanos , Camundongos , Ovariectomia , Regulação para Cima
8.
Phytomedicine ; 43: 68-77, 2018 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-29747756

RESUMO

BACKGROUND: As recorded in the 18 incompatible medicaments of Traditional Chinese Medicine theory, the combined use of Salvia miltiorrhiza bunge (SM) and Veratrum nigrum (VN) could induce toxicity and has been prohibited for thousands of years in China. However, the theory has been validated due to lack of evidence. Previous studies have focused on the chemical constituents that are responsible for the toxicity of the two agents. PURPOSE: This study offers preliminary insight into the pharmacodynamics and mechanism of estrogenic activity responsible for their incompatibility. STUDY DESIGN: We undertook a characterization of the interaction between estrogenic activities of SM and VN using in vivo models of immature and ovariectomized (OVX) mice, and in vitro studies focused on the estrogen receptor (ER) pathway for further mechanism. METHODS: Immature and OVX mice were treated intragastrically with SM at doses of 1.6, 3.2 g/kg, or combine with 0.045 g/kg VN and 0.005 g/kg the ER antagonist ICI182, 780 for elucidating the effects on estrogenic activity in reproductive tissues, E2 secretion, and the ER mechanism. ERα/ß binding experiments and ERα/ß transcriptional activity were performed in order to evaluate the biological action exerted through ERs. RESULTS: VN decreased the estrogenic efficacy of SM in promoting the development of the uterus and vagina in immature mice, and reversing the atrophy of reproductive tissues in OVX mice. VN interfered with the estrogenic efficacy of SM by decreasing the serum estradiol and the upregulation of ERα and ERß expressions in reproductive tissues by treatment with SM. VN antagonized the estrogenic efficacy of SM in promoting the viability of MCF-7 cells and stimulating the binding ability with ERα and ERß, and increasing ERα/ß-estrogen response element (ERE) luciferase activity. CONCLUSIONS: This study provided evidence that the combined use of SM and VN could induce unfavorable effects. VN decreased the estrogenic activity of SM, which might be related to the regulation of estrogen secretion and ERs through the ER-ERE pathway.


Assuntos
Medicamentos de Ervas Chinesas/farmacologia , Interações Ervas-Drogas , Salvia miltiorrhiza , Útero/efeitos dos fármacos , Veratrum , Animais , Antagonismo de Drogas , Medicamentos de Ervas Chinesas/efeitos adversos , Estradiol/sangue , Receptor alfa de Estrogênio/metabolismo , Receptor beta de Estrogênio/metabolismo , Feminino , Humanos , Células MCF-7 , Medicina Tradicional Chinesa/métodos , Camundongos , Ovariectomia , Receptores Estrogênicos/metabolismo , Útero/patologia , Vagina/efeitos dos fármacos , Vagina/patologia
9.
J Ethnopharmacol ; 201: 56-72, 2017 Apr 06.
Artigo em Inglês | MEDLINE | ID: mdl-27838357

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Panax notoginseng (Burk.) F.H. Chen is a well known medicinal plant. Its radix is used in the history while its flower is recently used for health care. In this study we compared chemical ingredients and bioactivities in cell culture for radix and flower of Panax notoginseng (Burk.) F.H. Chen. MATERIALS AND METHODS: The liquid chromatography-mass spectrometry system was applied to determine the contents of saponins in flower and radix of Panax notoginseng (Burk.) F.H. Chen. Transcription specific luciferase reporter assay and qPCR method for selected RNA were carried out to assess the impacts of flower and radix extract on the transcription signal pathways. RESULTS: The results of chemical analysis showed that the contents of saponins in flower and radix are very different: the contents of Rg1, Rb1, Re, R1, Rg3-20R, Rh1 and Rf in radix are abundant; in contrast, the contents of Rb3, Fc, Ft1, Rb2 and Rh2-20s in flowers are plentiful. There are substantial variations of those saponin contents from one batch vs another. Based on relative content of saponins, the chemosynthesis pathway of ingredients in radix and flower are proposed: for radix, both PPT (Protopanaxatriol) and PPD (Protopanaxadiol) type triterpenoids are involved, the main pathway is PPT→Rb1→Rg1→R1 or PPD→Rh2 20s→Rg3(20s)→Rd→Rb1; for flowers, only PPD is main passage with PPD→Rh2 (20s)→Rg3(20s)→Rd→Rb2→Fc. The results of signal transcription assays demonstrated that herb water extract of radix and flower had no significant influences on most of transcription activities. However, total saponins of radix and flower which have highly content of saponins were able to inhibit the inflammatory related transcriptional activities and their related mRNA expression of IFNα, TNFα, il-6 and TGFß as well as induce anti-oxygen NrF2 activities. In summary, although chemical ingredients and chemosynthesis pathway of flower and radix for Panax notoginseng (Burk.) F.H. Chen were different, these differences might not result in their differences of pharmacological activities.


Assuntos
Flores/química , Panax notoginseng , Raízes de Plantas/química , Saponinas/análise , Saponinas/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Flores/metabolismo , Genes Reporter , Células HEK293 , Células Hep G2 , Humanos , Luciferases/genética , Luciferases/metabolismo , Panax notoginseng/metabolismo , Extratos Vegetais/química , Raízes de Plantas/metabolismo , Saponinas/metabolismo
10.
Aging (Albany NY) ; 9(1): 156-172, 2016 12 20.
Artigo em Inglês | MEDLINE | ID: mdl-27997360

RESUMO

Salvia miltiorrhiza bunge(SM) is a popular herb for alleviating menopausal symptoms, although the scientific evidence of applying SM to estrogen replacement therapy is limited. In this study, we characterized the estrogenic activity of SM using in vivo models of immature and ovariectomized (OVX) mice and performed in vitro studies focusing on the estrogen receptor (ER) pathway for further molecular characterizations. SM treatments demonstrated significant estrogenic activity by promoting the development of uterus and vagina in immature mice, restoring the estrus cycle and reversing the atrophy of reproductive tissues in OVX mice, as well as increasing the expressions of ERα and ERß at protein and mRNA level in the reproductive tissues. Meanwhile, SM significantly increased estradiol in serum, and decreased follicle-stimulating hormone (FSH) and luteinizing hormone (LH) in the circulation of immature and OVX mice. SM could stimulate the binding effect of ERα and ERß, and significantly induce ERα/ß-estrogen response element (ERE) luciferase reporter gene expression. All these activities were inhibited by the ER antagonist ICI182, 780. This study demonstrates SM exerts estrogenic effects by stimulating biosynthesis of estrogen and increasing ERs in target tissues without side effects on reproductive tissues and through ER-ERE-dependent pathway.


Assuntos
Estradiol/sangue , Receptor alfa de Estrogênio/metabolismo , Receptor beta de Estrogênio/metabolismo , Extratos Vegetais/farmacologia , Salvia miltiorrhiza , Útero/efeitos dos fármacos , Vagina/efeitos dos fármacos , Animais , Linhagem Celular , Proliferação de Células/efeitos dos fármacos , Estradiol/análogos & derivados , Estradiol/farmacologia , Antagonistas do Receptor de Estrogênio/farmacologia , Ciclo Estral/efeitos dos fármacos , Ciclo Estral/metabolismo , Feminino , Fulvestranto , Camundongos , Ovariectomia , Útero/metabolismo , Vagina/metabolismo
11.
Zhongguo Zhong Yao Za Zhi ; 41(15): 2922-2926, 2016 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-28914038

RESUMO

Neobavaisoflavone is one of flavonoids of traditional Chinese medicine Psoralea corylifolial. It has numerous biological properties such as antibacterial, anti-inflammatory, anti-cancer, and anti-osteoporosis effects. This paper aimed to investigate the absorption mechanism of neobavaisoflavone in Caco-2 cell monolayer model. The analyte and osalmide were separated on Thermo Syncronis C18 column with methanol-0.1% formic acid solution (90∶10) as the mobile phase, at a flow rate of 0.2 mL•min⁻¹. The concentration of neobavaisoflavone was determined in eletrospray ionization(ESI) positive ion mode with osalmide as an the internal standard. The effects of time, concentration, P-gp inhibitor verapamil, MRP-2 inhibitor MK-571 and BCRP inhibitor Ko143 on the absorption of neobavaisoflavone were investigated. According to the results, neobavaisoflavone showed a good linearity within the concentration of 10-2 000 µg•L⁻¹, and the results of its specificity, matrix effect, extraction recovery, precision, accuracy and stability all met the requirements. In the Caco-2 cell monolayer model, the transport volume of neobavaisoflavone was correlated positively with the time and concentration. The ER values of 15, 30, 50 µmol•L⁻¹ neobavaisoflavone were 1.64, 1.94,0.99, respectively. As compared with the control group, all of verapamil hyduochloride, MK-571 and Ko143 could promote the transportation of neobavaisoflavone, and the effect was more obvious in verapamil hyduochloride and Ko143. The absorption of neobavaisoflavone may be mainly of active transport in Caco-2 cell monolayer model, and also involve passive transport. Excretion mechanism of intestinal transport protein may be also involved.


Assuntos
Isoflavonas/farmacocinética , Transporte Biológico , Células CACO-2 , Dicetopiperazinas/farmacologia , Compostos Heterocíclicos de 4 ou mais Anéis/farmacologia , Humanos , Absorção Intestinal , Propionatos/farmacologia , Quinolinas/farmacologia
12.
Sci Rep ; 5: 17436, 2015 Dec 08.
Artigo em Inglês | MEDLINE | ID: mdl-26644197

RESUMO

The Chinese herbal preparation QiBaoMeiRan formula (QBMR) displayed estrogenic effects in ovariectomized rats after long-term administration in a previous study. The uterus and vagina are negatively influenced by estrogens in hormone therapy. While QBMR is known to be a phytoestrogen, its estrogenic effects and safety on reproductive tissues after short-term administration and its mechanism via estrogen receptor (ER) pathway haven't been studied. Here, we characterized its estrogenic effects using immature mice together with in vitro studies for further molecular characterization. Immature mice were treated with QBMR at doses of 1.125, 2.25, and 4.5 g/kg for 7 days. 1.125 and 2.25 g/kg QBMR promoted the growth and development of uterus and vagina, and upregulated ERα and ERß expression in reproductive tissues. QBMR had a stimulatory effect on proliferating cell nuclear antigen in vagina but not in uterus, and was without any influence on ki-67 antigen in uterus and vagina. QBMR significantly induced luciferase expression from the ERα/ß-estrogen response element (ERE) luciferase reporter and upregulated ERα and ERß expressions in MCF-7 cells, which were significantly inhibited by estrogen antagonist ICI182,780. This study demonstrated QBMR exerts estrogenic effects on reproductive tissues without side effects and through ER-ERE-dependent pathway.


Assuntos
Medicamentos de Ervas Chinesas/farmacologia , Reprodução/efeitos dos fármacos , Animais , Biomarcadores , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Moduladores de Receptor Estrogênico/farmacologia , Estrogênios/sangue , Estrogênios/metabolismo , Feminino , Hormônio Foliculoestimulante/sangue , Regulação da Expressão Gênica/efeitos dos fármacos , Humanos , Antígeno Ki-67/genética , Antígeno Ki-67/metabolismo , Hormônio Luteinizante/sangue , Camundongos , Membrana Mucosa/citologia , Membrana Mucosa/efeitos dos fármacos , Membrana Mucosa/metabolismo , Antígeno Nuclear de Célula em Proliferação/genética , Antígeno Nuclear de Célula em Proliferação/metabolismo , Receptores Estrogênicos/genética , Receptores Estrogênicos/metabolismo , Reprodução/genética , Útero/efeitos dos fármacos , Útero/metabolismo , Vagina/efeitos dos fármacos , Vagina/metabolismo
13.
Zhongguo Zhong Yao Za Zhi ; 40(6): 1119-22, 2015 Mar.
Artigo em Chinês | MEDLINE | ID: mdl-26226756

RESUMO

OBJECTIVE: An accurate and reliable analytical method for-simultaneous determination of six active components (scopolin, chlorogenic acid, scopoletin, isochlorogenic acid A, isochlorogenic acid B and isochlorogenic acid C) in plants of Erycibe was developed. METHOD: Scopolin, chlorogenic acid, scopoletin, isochlorogenic acid A, isochlorogenic acid B and isochlorogenic acid C in the samples were well separated in analytical HPLC by gradual elution with methanol-0.1% formic acid solution. The chromatographic condictions: Agilent Poroshell 120 EC-C18 column, flowing rate being 1 mL x min(-1), detecting wavelength at 345 nm. RESULT: Good linearities of scopolin, chlorogenic acid, scopoletin, isochlorogenic acid A, isochlorogenic acid B and isochlorogenic acid C were in the range of 0.026 8-2.68, 0.027 0-2.70, 0.008 1-0.81, 0.018 8-1.88, 0.017 6-1.76, 0.019 6-1.96 µg, respectively (r > 0.999 6). The average recoveries of the six components were 98.1%, 98.7%, 100.8%, 100.4%, 99.7%, 101.1%; the relative standard deviations were 2.67%, 2.86%, 2.62%, 1.98%, 2.76%, 2.19%. CONCLUSION: The method is simple, feasible and reproducible and can be used for the quality control of plants of Erycibe.


Assuntos
Ácido Clorogênico/análogos & derivados , Ácido Clorogênico/análise , Cromatografia Líquida de Alta Pressão/métodos , Convolvulaceae/química , Cumarínicos/análise , Medicamentos de Ervas Chinesas/análise , Glucosídeos/análise , Escopoletina/análise , China
14.
Rejuvenation Res ; 13(4): 479-88, 2010 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-20707715

RESUMO

A Chinese herbal preparation, Qing'E formula (QEF), has been used clinically for treating osteoporosis in postmenopausal women by virtue of its kidney-invigorating function; however, no evidence base links QEF to estrogen replacement therapy. In this study, we undertake a characterization of estrogenic activity of QEF using an in vivo model of ovariectomized (OVX) mice together with in vitro studies with the MCF-7 cells for further molecular characterization. OVX mice were treated intragastrically with QEF at doses of 0.85, 1.7, and 3.4 g/kg per day for 4 weeks. QEF treatments restored the estrus cycle and demonstrated significant estrogenic activity, as indicated by reversal of uterine atrophy (six-fold increase in uterine weight), reduction in rectal temperature, and increased expression (1.6-fold) of estrogen receptors (ERs) in the uterus. Notably, the largest changes in these three parameters were found at the lowest dose. At the highest dose of QEF, significant changes were found in adrenal gland weight (30% increase), serum estradiol (E(2)) (60% increase), and luteinizing hormone (LH) (17% decrease) compared with untreated OVX controls. The data suggest estrogenic responses induced by QEF show tissue variation that reflects different affinities of ERs for QEF components. QEF could significantly induce luciferase expression (2.7-fold compared with control) from an estrogen response element luciferase reporter and induced expression of ERalpha and ERbeta (1.2-fold and 1.7-fold respectively) in MCF-7 cells. Both activities were inhibited 80-90% by the estrogen antagonist ICI 182,780. This study demonstrates that QEF activity is mediated through estrogenic components and provides an evidence base for QEF treatment of postmenopausal symptoms.


Assuntos
Medicamentos de Ervas Chinesas , Estradiol/sangue , Ovariectomia , Glândulas Suprarrenais/efeitos dos fármacos , Animais , Linhagem Celular Tumoral , Relação Dose-Resposta a Droga , Estro/efeitos dos fármacos , Feminino , Humanos , Imuno-Histoquímica , Hormônio Luteinizante/metabolismo , Camundongos , Tamanho do Órgão/efeitos dos fármacos , Receptores Estrogênicos/metabolismo , Útero/metabolismo
15.
Arch Pharm Res ; 32(9): 1245-51, 2009 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-19784581

RESUMO

Acetylcholinesterase inhibitors (AChEIs) currently form the basis of the newest drugs available for the treatment of Alzheimer's disease. For the aim of screening effective AChEIs, the methanol extracts of the seeds of genus Peganum were found to show significant inhibitory activity of acetylcholinesterase enzyme (AChE) using an in vitro TLC-bioautographic assay. In further studies to seed of P. nigellastrum Bunge, activity-guided fractionation led to the isolation of two new alkaloids nigellastrine I (9) and nigellastrine II (10), and along with eight known alkaloids, vasicinone (1), vasicine (2), harmine (3), deoxyvasicinone (4), deoxyvasicine (5), harmaline (6), harmol (7), harman (8), in which harmol and harman were first isolated from species P. nigellastrum Bunge. As active constituents, all compounds showed good inhibitory activities against AChE. The results of in vitro semi-quality TLC-bioautographic assay showed that harmine, harmaline and harmol displayed a similar AChE inhibitive activities comparing to galanthamine. These results indicated that these alkaloids in P. nigellastrum Bunge could be a potent class of AChEIs.


Assuntos
Alcaloides/isolamento & purificação , Inibidores da Colinesterase/isolamento & purificação , Cromatografia em Camada Delgada/métodos , Peganum/química , Alcaloides/química , Alcaloides/farmacologia , Inibidores da Colinesterase/química , Inibidores da Colinesterase/farmacologia , Sementes/química
16.
Yao Xue Xue Bao ; 41(10): 956-62, 2006 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-17184113

RESUMO

AIM: To evaluate the antioxidant capacity and quality of traditional Chinese medicines using TLC-bioautography. METHODS: Two chromatograms of each crude drug sample were obtained, after developing, by spraying with 1,1-diphenyl-2-picrylhydrazyl (DPPH) solution in ethanol and classical stained reagents, separately. The images sprayed with DPPH solution were captured under light after the plates were heated at 40 degrees C for 30 min, and scanned using video scan software to get peak areas of active compounds. RESULTS: Total peak areas of the spots on TLC were calculated to evaluate the antioxidant capacity of the tested crude drugs from different habitats and sources. The results indicated that Radix Linderae cultivated in Tiantai (Zhejiang province), Cortex Magnoliae Officinalis cultivated in Liangshan (Sichuan province), and Fructus Perillae acquired in Shanghai have the highest scavenging properties towards DPPH in their respective TLC-autographic assays. Norisoboldine, magnolol and honokiol, luteolin, apigenin and an unknown compound "U" proved to be the major antioxidant components in the corresponding crude drugs as they contribute the dominating peak areas to the total ones. CONCLUSION: TLC-bioautography can not only be used for screening of the components with antioxidant potency but also for the purpose of quality evaluation of traditional Chinese medicines at the same time, and the method proved to be selective, simple and reproducible.


Assuntos
Antioxidantes/farmacologia , Cromatografia em Camada Delgada/métodos , Medicamentos de Ervas Chinesas/farmacologia , Lindera/química , Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Antioxidantes/isolamento & purificação , Compostos de Bifenilo/química , Compostos de Bifenilo/isolamento & purificação , Compostos de Bifenilo/farmacologia , China , Medicamentos de Ervas Chinesas/isolamento & purificação , Hidrazinas/química , Lignanas/isolamento & purificação , Lignanas/farmacologia , Luteolina/isolamento & purificação , Luteolina/farmacologia , Magnolia/química , Perilla/química , Picratos , Plantas Medicinais/química , Controle de Qualidade , Reprodutibilidade dos Testes
17.
J Opt Soc Am A Opt Image Sci Vis ; 22(11): 2516-26, 2005 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-16302403

RESUMO

By using the Debye potentials, the exact eigenvalue equations and the corresponding field distributions of the core and cladding modes for three-layered, radially stratified, and dielectric uniaxial optical fibers are derived completely; the modes include TE, TM, and hybrid HE/EH modes. The strain characteristics of long-period fiber gratings' (LPFGs') with applied axial strain are investigated theoretically by studying three-layered uniaxial optical fibers. When uniform axial strain is applied to fiber, the core, and inner and outer cladding become uniaxial crystal optically; that is, the optical axes are parallel to the fiber's axis. Analytic expressions of the strain sensitivities of LPFGs are derived. The analysis reveals that the strain sensitivities of LPFGs based on various cladding modes, including the shift value and direction of the resonance wavelength, differ greatly.

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