RESUMO
Two new triterpene saponins, mandshunosides A and B (1 and 2), were isolated from the roots and rhizomes of Clematis mandshurica. Their structures were elucidated on the basis of spectroscopic evidence and hydrolysis products. Compounds 1 and 2 showed inhibitory activities against two colorectal human cancer cells HCT 116 (IC50 2.1 µM for 1 and 2.5 µM for 2) and HT-29 (IC50 3.7 µM for 1 and 3.3 µM for 2).
Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Clematis/química , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/farmacologia , Saponinas/isolamento & purificação , Saponinas/farmacologia , Triterpenos/isolamento & purificação , Triterpenos/farmacologia , Antineoplásicos Fitogênicos/química , Ensaios de Seleção de Medicamentos Antitumorais , Medicamentos de Ervas Chinesas/química , Células HCT116 , Células HT29 , Humanos , Estrutura Molecular , Raízes de Plantas/química , Rizoma/química , Saponinas/química , Triterpenos/químicaRESUMO
OBJECTIVE: To establish an instant determination method of citrinin in red kojic by high performance capillary electrophorphores for the first time. METHOD: Red kojic was extracted with the mixtrue of Toluene and ethyl acetate (70:30). Separation was carried out in an uncoated fused silica capillary (50 microm x 45.0 cm). Meanwhile, a running voltage 15 kV, 20 mmol L(-1) borax buffer with 10.0 mmol L(-1) sodium deoxycholate (pH 9.3) and a UV detector at 212 nm were adopted. RESULT: Regression equation of citrinin was Y=9434 + 16781X (r =0.990), The lower limit of quantification (S/N > or =3) was 0.5 mg mL(-1). The assay coefficients of variation ranged from 98.8% to 101.1%. The intra and inter recovery ranged from 0.83 to 1.54% and from 1.86 to 5.09%. Twenty samples were determined with the method. CONCLUSION: The method is proved to be simple, rapid and accurate, and it can be used to determine citrinin in red kojic.
Assuntos
Citrinina/análise , Eletroforese Capilar/métodos , Monascus/química , Concentração de Íons de Hidrogênio , Reprodutibilidade dos TestesRESUMO
OBJECTIVE: To investigate the inhibitory effects of RNAi expression vector suppressing the expression of survivin and inducing the apoptosis of pancreatic cancer cell PANC-1. METHODS: The expression of survivin was examined with RT-PCR and immunofluorescence protocols. The survivin gene was cloned into the T-vector and sequenced, at the same time, the RNAi expression vectors aimed survivin were successfully constructed, and then transfected into PANC-1 cells with liposomes. The expression of survivin mRNA was detected with RT-PCR and Western-blot techniques. The rate of cell apoptosis was measured with FACS. RESULTS: There was a high degree expression of survivin in PANC-1 cells. The DNA sequence was according with the survivin gene in GENE BANK. The survivin expression was inhibited about 70% by pTZU6 + 1-svv2 RNAi expression vectors, and the apoptosis cells increased. CONCLUSION: The RNAi expression vector can effectively inhibit the survivin expression and induce the apoptosis in PANC-1 cells.
Assuntos
Apoptose/fisiologia , Proteínas Associadas aos Microtúbulos/biossíntese , Proteínas de Neoplasias/biossíntese , Neoplasias Pancreáticas/metabolismo , Interferência de RNA , Sequência de Bases , Linhagem Celular Tumoral , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Regulação Neoplásica da Expressão Gênica/fisiologia , Terapia Genética , Humanos , Proteínas Inibidoras de Apoptose , Proteínas Associadas aos Microtúbulos/genética , Dados de Sequência Molecular , Proteínas de Neoplasias/genética , Neoplasias Pancreáticas/patologia , RNA Mensageiro/biossíntese , RNA Mensageiro/genética , Survivina , TransfecçãoRESUMO
AIM: To design and synthesize new phenyloxyisobutyric acid analogues as antidiabetic compounds. METHODS: Eight new target compounds were synthesized by combination of lipophilic moieties and acidic moiety with nucleophilic replacement or Mitsunobu condensation. The eight compounds were confirmed by 1H NMR, 13C NMR, IR and MS. RESULTS: In vitro insulin-sensitizing activity (3T3-L1 adipocyte) demonstrated, that the cultured glucose concentration of up-clear solution detected with GOD-POD assay were 5.942, 6.339, 6.226 and 6.512 mmol x L(-1), respectively, when rosiglitazone, pioglitazone, compounds A and B were added to the insulin-resistant system. CONCLUSION: In vitro insulin-sensitizing activity of target compound A is in between that of rosiglitazone and pioglitazone, and activity of target compound B is slightly less than that of pioglitazone.
Assuntos
Butiratos/síntese química , Hipoglicemiantes/síntese química , PPAR gama/agonistas , Células 3T3-L1 , Adipócitos/efeitos dos fármacos , Animais , Butiratos/química , Butiratos/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Insulina/farmacologia , Camundongos , Estrutura Molecular , PPAR gama/farmacologiaRESUMO
AIM: To find new peroxisome proliferator-activated y agonists with high activity and low toxicity. METHODS: Based on JTT-501 and JTT-20993, new isoxazolidine-3,5-dione and noncyclic 1,3-dicarbonyl compounds were designed and synthesized. Their insulin-sensitizing activities were evaluated. RESULTS: Eight new compounds were obtained. The structures of synthesized compounds were characterized by NMR, MS and IR. Four compounds (1A-4A) showed insulin-sensitizing activities. CONCLUSION: Compounds (1A and 3A) showed excellent insulin-sensitizing activities and should be worth further investigation.
