RESUMO
As no study about the combined effect of low levels of Cd2+ with procymidone (PCM) on organs and organisms, we investigated their actions on mouse-ovary in vivo and in vitro. Four-week mice were treated with corn oil for the control group, corn oil + 0.0045 mg/L Cd2+ (CdCl2 was dissolved in ultrapure water and freely consumed by mice) for Cd2+ group, 50 mg/kg/d PCM (suspended in corn oil and administered orally to mice) for PCM group, and 50 mg/kg/d PCM + 0.0015 (0.0045 and 0.0135) mg/L Cd2+ for L+ (M+ and H+) PCM group for 21 days. For in vitro experiment, the cultured ovaries were treated with acetone for the control group, 0.1% acetone + 8.4 µg/L Cd2+ for the Cd2+ group, 0.63 mg/L PCM (dissolved in acetone) for the PCM-group, and 0.63 mg/L PCM + 2.8 (8.4 and 25.2) µg/L Cd2+ for L+ (M+ and H+) PCM group for 7 days. Mouse body weight in each treatment group, the weight and volume of ovaries in all PCM groups were lower than the control. Both in vivo and in vitro, all-stage follicle numbers were lower in M+PCM and H+PCM groups, whereas the atretic follicles and CASPASE3/8 were higher; meanwhile, lower estradiol and progesterone and higher unfolded protein response (UPR) members in all PCM groups. L+, M+, and H+PCM groups had further ovarian damage and stronger UPR than PCM groups, as did M+PCM groups over Cd2+ groups. It is hypothesized low-level PCM and Cd2+ may mutually promote each other's triggered UPR and exacerbate ovarian damage.
Assuntos
Compostos Bicíclicos com Pontes , Cádmio , Ovário , Feminino , Camundongos , Animais , Cádmio/metabolismo , Acetona/metabolismo , Acetona/farmacologia , Óleo de Milho/metabolismo , Óleo de Milho/farmacologiaRESUMO
Recently, polysaccharides from Bletilla striata, a member of the orchidaceous family, aroused the wide interest of people, especially their isolation, chemical properties, and bioactivities. It is reported that these polysaccharides are the most important biologically active components of B. striata, exhibiting various biological activities, such as immunomodulatory, antioxidant, antifibrotic, and hemostatic effects. This review appraised the available literatures which described different aspects of B. striata polysaccharides, including the extraction, separation, purification, structural characterization, and biological activities. We expect to lay the foundation for further investigation of the application of B. striata polysaccharides in the field of functional foods and biomedicine.
Assuntos
Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/isolamento & purificação , Orchidaceae/química , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Polissacarídeos/química , Polissacarídeos/isolamento & purificação , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificaçãoRESUMO
BACKGROUND: Statin combined with ezetimibe demonstrates significant benefit in lowering low density lipid cholesterol (LDL-C) and cardiovascular events abroad, but whether intermediate intensity statins combined with ezetimibe is superior to high-intensity statin monotherapy in Chinese people is unknown. METHODS: A total of 125 patients were randomly assigned to a intermediate intensity rosuvastatin group (rosuvastatin 10mg/d, n=42), high-dose rosuvastatin group (rosuvastatin 20mg/d, n=41) or combination therapy group (ezetimibe 10mg/d and rosuvastatin 10mg/d, n=42) with a 12-week follow-up. The primary end point was the proportion of patients who achieved the 2011 ESC/EAS LDL-C goal <70mg/dL (1.8mmol/L) at week 12. Secondary end points included changes from baseline in lipids, the occurrence of all cardiovascular events, high-sensitivity C-reactive protein and safety markers. RESULTS: The combination therapy group in the primary end point was significantly higher than rosuvastatin (20mg) and rosuvastatin (10mg) at week 12 (81.0% vs 68.3% vs 33.3%, P<0.001). And the similar change was observed in reducing LDL-C levels at week 12 (67.28% vs 52.80% vs 43.89%, P<0.001). The incidence of drug-related adverse events was much higher in the rosuvastatin 20mg group than the rosuvastatin 10mg group and the combination therapy group (17.0% vs 2.4% vs 4.8%, P<0.05). CONCLUSIONS: The combination of rosuvastatin 10mg/ezetimibe 10mg was an effectively alternative therapy superior to rosuvastatin 20mg or 10mg with a greater effect on lowering LDL-C and a lower incidence of drug-related adverse events in Chinese patients.
Assuntos
Síndrome Coronariana Aguda , LDL-Colesterol/sangue , Ezetimiba , Rosuvastatina Cálcica , Síndrome Coronariana Aguda/sangue , Síndrome Coronariana Aguda/diagnóstico , Síndrome Coronariana Aguda/epidemiologia , Síndrome Coronariana Aguda/prevenção & controle , Idoso , Anticolesterolemiantes/administração & dosagem , Anticolesterolemiantes/efeitos adversos , Proteína C-Reativa/análise , China/epidemiologia , Relação Dose-Resposta a Droga , Monitoramento de Medicamentos/métodos , Quimioterapia Combinada/métodos , Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos/epidemiologia , Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos/etiologia , Eletrocardiografia/métodos , Ezetimiba/administração & dosagem , Ezetimiba/efeitos adversos , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Rosuvastatina Cálcica/administração & dosagem , Rosuvastatina Cálcica/efeitos adversosRESUMO
Two pairs of rare benzofuran glucoside epimers, indicuses A and B and indicuses C and D, three biogenetically related compounds indicuses E-G, and one coumarin indicus H, as well as 11 known compounds, were isolated from the bark of Streblus indicus (Bur.) Corner. The structures of indicuses A-H were elucidated by NMR and MS data, as well as by CD. (S)-Marmesinin exhibited moderate antimicrobial activity in vitro against Bacillus subtilis and Saccharomyces cerevisiae. 7,8-Dihydroxy-3-(3-methyl-2-butenyl) coumarin, umbelliferone, and scopoletin displayed strong cytotoxic activity in vitro against human bladder carcinoma cell line EJ. The structure-activity relationships indicate that hydroxylation at C-7 in the cytotoxic compounds is crucial to their activities.
Assuntos
Benzofuranos/química , Cumarínicos/química , Glicosídeos/química , Moraceae/química , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Bacillus subtilis/efeitos dos fármacos , Benzofuranos/isolamento & purificação , Linhagem Celular Tumoral , Cumarínicos/isolamento & purificação , Furanos/química , Furanos/isolamento & purificação , Glicosídeos/isolamento & purificação , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Casca de Planta/química , Extratos Vegetais/química , Saccharomyces cerevisiae/efeitos dos fármacos , Escopoletina/química , Escopoletina/isolamento & purificação , Relação Estrutura-Atividade , Umbeliferonas/química , Umbeliferonas/isolamento & purificaçãoRESUMO
A pair of enantiomers and a pair of 2,3-dihydro-1H-indene epimers, rac-indidene A (rac-1), indidenes B and C (2, 3); four new coumarin glucosides (4-7); and four known coumarin glucosides (8-11) were isolated from the bark of Streblus indicus (Bur.) Corner. The structures of 1-11 were defined by physical data analyses, including MS, NMR, and single-crystal X-ray diffraction. The absolute configurations of the 2,3-dihydro-1H-indene derivatives were defined via experimental and calculated ECD data. rac-Indidene A and indidenes B and C showed inhibitory activity against A549 and MCF-7 tumor cells with IC50 values in the range of 2.2 ± 0.1 to 7.2 ± 0.9 µM.
Assuntos
Cumarínicos/isolamento & purificação , Cumarínicos/farmacologia , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/farmacologia , Glucosídeos/isolamento & purificação , Glucosídeos/farmacologia , Indenos/isolamento & purificação , Indenos/farmacologia , Moraceae/química , Casca de Planta/química , Células A549 , Cromatografia Líquida de Alta Pressão , Cumarínicos/química , Cristalografia por Raios X , Ensaios de Seleção de Medicamentos Antitumorais , Medicamentos de Ervas Chinesas/química , Glucosídeos/química , Humanos , Indenos/química , Concentração Inibidora 50 , Células MCF-7 , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , EstereoisomerismoRESUMO
Acupuncture has been shown to lessen the inflammatory reaction after acute spinal cord injury and reduce secondary injury. However, the mechanism of action remains unclear. In this study, a rat model of spinal cord injury was established by compressing the T8-9 segments using a modified Nystrom method. Twenty-four hours after injury, Zusanli (ST36), Xuanzhong (GB39), Futu (ST32) and Sanyinjiao (SP6) were stimulated with electroacupuncture. Rats with spinal cord injury alone were used as controls. At 2, 4 and 6 weeks after injury, acetylcholinesterase (AChE) activity at the site of injury, the number of medium and large neurons in the spinal cord anterior horn, glial cell line-derived neurotrophic factor (GDNF) mRNA expression, and Basso, Beattie and Bresnahan locomotor rating scale scores were greater in the electroacupuncture group compared with the control group. These results demonstrate that electroacupuncture increases AChE activity, up-regulates GDNF mRNA expression, and promotes the recovery of motor neuron function in the anterior horn after spinal cord injury.
RESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Extracts from Ginkgo biloba L. leaves confer their therapeutic effects through the synergistic actions of flavonoid and terpenoid components, but some non-flavonoid and non-terpenoid components also exist in this extract. In the study of this paper, an investigation was carried out to compare the pharmacokinetic parameters of fourteen compounds to clarify the influences of non-flavonoid and non-terpenoid fraction (WEF) on the pharmacokinetics profile of the flavonoid fraction (FF) and the terpene lactone fraction (TLF) from Ginkgo biloba extracts. MATERIALS AND METHODS: A selective and sensitive UPLC-MS/MS method was established to determine the plasma concentrations of the fourteen compounds to compare the pharmacokinetic parameters after orally administration of FF, TLF, FF-WEF, FF-TLF, TLF-WEF and FF-TLF-WEF with approximately the same dose. At different time points, the concentration of rutin (1), isoquercitrin (2), quercetin 3-O-[4-O-(-ß-D-glucosyl)-α-L-rhamnoside] (3), ginkgolide C (4), bilobalide (5), quercitrin (6), ginkgolide B (7), ginkgolide A (8), luteolin (9), quercetin (10), apigenin (11), kaempferol (12), isorhamnetin (13), genkwanin (14) in rat plasma were determined and main pharmacokinetic parameters including T1/2, Tmax, Cmax and AUC were calculated using the DAS 3.2 software package. The statistical analysis was performed using the Student׳s t-test with P<0.05 as the level of significance. RESULTS: FF and WEF had no effect on the pharmacokinetic behaviors and parameters of the four terpene lactones, but the pharmacokinetic profiles and parameters of flavonoids changed while co-administered with non-flavonoid components. It was found that Cmax and AUC of six flavonoid aglycones in group FF-WEF, FF-TLF and FF-TLF-WEF had varying degrees of reduction in comparison with group FF, especially in group FF-TLF-WEF. On the contrary, the values of Cmax, Tmax and AUC of four flavonoid glycosides in group FF-TLF-WEF were significantly increased compared with those in group FF. CONCLUSIONS: These results indicate that non-flavonoid components in Ginkgo biloba extracts could increase the absorption and improve the bioavailability of flavonoid glycosides but decrease the absorption and reduce the bioavailability of flavonoid aglycones.
Assuntos
Flavonoides/farmacocinética , Ginkgo biloba/química , Extratos Vegetais/farmacocinética , Terpenos/farmacocinética , Animais , Área Sob a Curva , Disponibilidade Biológica , Cromatografia Líquida de Alta Pressão/métodos , Interações Medicamentosas , Flavonoides/isolamento & purificação , Glicosídeos/isolamento & purificação , Glicosídeos/farmacocinética , Meia-Vida , Masculino , Extratos Vegetais/química , Ratos , Ratos Sprague-Dawley , Sensibilidade e Especificidade , Espectrometria de Massas em Tandem/métodos , Terpenos/isolamento & purificaçãoRESUMO
ß-Asarone is an active component of the Acori graminei rhizome that is a traditional Chinese medicine clinically used in treating dementia in China. However, the cognitive effect of ß-asarone and its mechanism has remained elusive. Here, we used asenescence-accelerated prone 8 (SAMP8) mice, which mimic many of the salient features of Alzheimer׳s disease (AD), to further investigate whether modulation of the ROCK signaling pathway and/or autophagy, synaptic loss is involved in the effects of ß-asarone on learning and memory. SAMP8 mice at the age of 6 months were intragastrically administered by ß-asarone or a vehicle daily for 2 months. Senescence-accelerated-resistant (SAMR1) mice were used as the control. Our results demonstrate that autophagy and ROCK expression were increased significantly in 8 months SAMP8 mice, which were concomitant with that SAMP8 mice at the same age displayed a significant synaptic loss and cognitive deficits. The up-regulation of ROCK expression and autophage in the hippocampus of SAMP8 were significantly reduced by ß-asarone, and prevents synaptic loss and improved cognitive function of the SAMP8 mice. ß-asarone decreased neuronophagia and lipofuscin in the hippocampus of SAMP8 mice, but did not reduce Aß42 levels and malondialdehyde levels and superoxide dismutase activities. Moreover, suppression of ROCK2 by siRNA significantly reduced the effects of ß-asarone on the autophage and synaptic proteins expression in PC12 cells damage induced by Aß1-40. Taken together, ß-asarone prevents autophagy and synaptic loss by reducing ROCK expression in SAMP8 mice.
Assuntos
Senilidade Prematura/tratamento farmacológico , Anisóis/uso terapêutico , Autofagia/efeitos dos fármacos , Região CA3 Hipocampal/efeitos dos fármacos , Medicamentos de Ervas Chinesas/farmacologia , Proteínas do Tecido Nervoso/biossíntese , Fármacos Neuroprotetores/uso terapêutico , Sinapses/efeitos dos fármacos , Quinases Associadas a rho/biossíntese , Senilidade Prematura/enzimologia , Senilidade Prematura/psicologia , Derivados de Alilbenzenos , Peptídeos beta-Amiloides/análise , Animais , Anisóis/farmacologia , Região CA3 Hipocampal/química , Transtornos Cognitivos/etiologia , Transtornos Cognitivos/prevenção & controle , Avaliação Pré-Clínica de Medicamentos , Indução Enzimática/efeitos dos fármacos , Lipofuscina/análise , Potenciação de Longa Duração/efeitos dos fármacos , Malondialdeído/análise , Aprendizagem em Labirinto/efeitos dos fármacos , Camundongos , Proteínas Associadas aos Microtúbulos/análise , Proteínas do Tecido Nervoso/genética , Proteínas do Tecido Nervoso/fisiologia , Fármacos Neuroprotetores/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Células PC12 , Fragmentos de Peptídeos/análise , Interferência de RNA , RNA Interferente Pequeno/farmacologia , Ratos , Superóxido Dismutase/análise , Sinapses/enzimologia , Regulação para Cima/efeitos dos fármacos , Quinases Associadas a rho/antagonistas & inibidores , Quinases Associadas a rho/genética , Quinases Associadas a rho/fisiologiaRESUMO
OBJECTIVE: To establish the UPLC specific chromatogram of Lily and analyze the specific peaks compositions by ESI-QTOF-MS. METHODS: The samples were conducted by ACQUITY UPLC BEH C18 Column (2.1 mm x 100 mm, 1.7 microm) and eluted with acetonitrile and 0.1% formic acid at the flow rate of 0.4 mL/min. The detection wavelength was set at 320 nm and column temperature was 35 degrees C. Negative ion mode was chosen for qualitative analysis. The capillary voltage was set at 3.0 kV. The nebulization gas was set to 600 L/h at 350 degrees C, and the source temperature was 120 degrees C. RESULTS: The specific chromatogram of Lily was obtained. There were 19 common peaks. Twelve phenylpropenoid glycerides compositions were identified. Among them, 6 compositions were identified by comparison with the reference substances and others were identified by MS and MS2 data. CONCLUSION: UPLC specific chromatogram can be used for the quality evaluation of Lily, giving support to quality control comprehensively.
Assuntos
Cromatografia Líquida de Alta Pressão , Medicamentos de Ervas Chinesas/química , Glicerídeos/análise , Lilium/química , Medicamentos de Ervas Chinesas/análise , Controle de Qualidade , Reprodutibilidade dos Testes , Espectrometria de Massas por Ionização por ElectrosprayRESUMO
To study the consensuses on lung cancer treatment by Chinese medicine experts from North China and South China, and to analyze their medication features from viewpoints such as the medication frequency, combination laws, medication classification by collecting 800 recipes on the treatment of lung cancer patients prescribed by 8 Chinese oncologists from Guanganmen Hospital of China Academy of Chinese Medical Sciences, the Affiliated Hospital of Guangzhou University of Traditional Chinese Medicine, and Guangdong Provincial Hospital of Traditional Chinese Medicine. Results showed that coix seed, poria, pinelliae tuber were the three herbs most commonly used in treatment of lung cancer by all experts. They generally accepted Pi invigorating and phlegm removing method as the basic treatment method for treating lung cancer. Secondly, they usually used white peony root, heterophylla falsestarwort root, and ophiopogonis tuber, etc. (with higher medication frequency) to nourish yin and moisten Fei. Thirdly, consistency was also shown in clearing heat, detoxication, and anticancer. Smilacis glabra, Rhizoma Smilacis Glabrae, Herba Hedyotis diffusae, Herba Scutellariae Barbatae were herbs used by all experts. However, there were differences between oncologists in North China and South China. Oncologists in South China paid more attention to heat toxin and blood stasis, while those in North China paid more attention to supplementing both qi and yin.
Assuntos
Medicamentos de Ervas Chinesas/uso terapêutico , Neoplasias Pulmonares/tratamento farmacológico , Fitoterapia/métodos , China , Humanos , Medicina Tradicional Chinesa/métodosRESUMO
Upon the background of new medical model being formed, to make measurement/evaluation with subjective indices (SIM/E) has become a new hot-spot in Western medical researches and much methodological achievements have been made, but difficulties in comprehensive evaluation and result interpretation are still encountered. SIM/E has played important guideline roles in Chinese medicine (CM) clinical practice, and since it is characterized by holism and syndrome differentiation, it showed great advantage in comprehensive evaluation and result interpretation, though further standardization is yet required. To analyze the related tools and scientific regulations of SIM/E in Western medicine, and establish the concept, domain and conceptual framework of a SIM/E system based on the CM syndrome theory should be feasible to realize the mutual compensation between advantages of the two medical sciences, and promote the progress of SIM/E.