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1.
J Nat Prod ; 81(12): 2638-2646, 2018 12 28.
Artigo em Inglês | MEDLINE | ID: mdl-30543429

RESUMO

Ten new formyl-phloroglucinol-terpene meroterpenoids, eucalypglobulusals A-J (1-10), and ten known analogues were isolated from  Eucalyptus globulus fruits. The structures of 1-10 were determined by spectroscopic analysis, while their absolute configurations were established using calculated and experimental electronic circular dichroism (ECD) spectra. Eucalypglobulusal A was assigned as a new formyl-phloroglucinol-terpene meroterpenoid with a rearranged sesquiterpene skeleton, and an aldol condensation between C-3 and C-5 of the germacrene C moiety was proposed to be a key step in its putative biosynthetic pathway. Eucalypglobulusal F exhibited cytotoxicity against the human acute lymphoblastic cell line (CCRF-CEM) with an IC50 value of 3.3 µM, while eucalypglobulusal A, eucarobustol C, macrocarpal A, macrocarpal B, and macrocarpal D exhibited DNA topoisomerase I (Top1) inhibition. The compounds eucalypglobulusal A and macrocarpal A act as Top1 catalytic inhibitors and delay Top1 poison-mediated DNA double-strand damage.


Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Eucalyptus/química , Terpenos/isolamento & purificação , Inibidores da Topoisomerase I/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , DNA Topoisomerases Tipo I , Ensaios de Seleção de Medicamentos Antitumorais , Frutas/química , Humanos , Estrutura Molecular , Inibidores da Topoisomerase I/química , Inibidores da Topoisomerase I/farmacologia
2.
Nat Prod Bioprospect ; 6(4): 205-10, 2016 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-27255683

RESUMO

Phytochemical investigation of the rhizomes of Paris polyphylla var. stenophylla led to the isolation of two new highly oxygenated spirostanol saponins, named paristenosides A (1) and B (2), together with seven known compounds. Their structures were established mainly on the base of NMR spectroscopic techniques and mass spectrometry, as well as chemical methods. In addition, the cytotoxicity of the two new saponins was tested. Two new highly oxygenated spirostanol saponins, paristenosides A (1) and B (2), were isolated from the rhizomes of Paris polyphylla var. stenophylla. Their structures were established mainly based on NMR spectroscopic techniques and mass spectrometry, as well as chemical methods.

3.
Phytochemistry ; 131: 165-173, 2016 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-27665149

RESUMO

Ten spirostanol glycosides, trillikamtosides A-J, together with eleven known analogues, were isolated from the hemostatic fraction of the 75% aqueous EtOH extract of the whole herbs of Trillium kamtschaticum. Their structures were established by extensive spectroscopic data analysis and chemical methods. The aglycones of three of these compounds had unique 3ß,17α-dihydroxy-spirostanes featuring a double bond between C-4 and C-5, while two others represent a rare class of spirostanol glycosides which possess a 5(6 â†’ 7) abeo-steroidal aglycone. All the compounds were evaluated for their hemostatic and antimicrobial activities. Three of the spirostanol glycosides exhibited induced-platelet aggregation at a concentration of 300 µg/mL with maximal induced-platelet aggregation rates of 72%, 71%, and 62% in rabbits, respectively, and their EC50 values were 492.7, 203.3, and 109.8 µM. Five of the spirostanol glycosides showed an anti-Candida albicans effect with MIC values of 21.1, 10.6, 8.8, 21.6, and 11.0 µM, respectively.


Assuntos
Anti-Infecciosos/isolamento & purificação , Glicosídeos/isolamento & purificação , Glicosídeos/farmacologia , Hemostáticos/isolamento & purificação , Hemostáticos/farmacologia , Espirostanos/isolamento & purificação , Espirostanos/farmacologia , Trillium/química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Candida albicans/efeitos dos fármacos , Relação Dose-Resposta a Droga , Glicosídeos/química , Hemostáticos/química , Agregação Plaquetária/efeitos dos fármacos , Espirostanos/química
4.
Journal of Medical Postgraduates ; (12): 963-967, 2019.
Artigo em Chinês | WPRIM | ID: wpr-818356

RESUMO

Objective The up-regulated expression of miR-182 is associated with poor prognosis of triple-negative breast cancer. This study explored the biological function of the miR-182/MTSS1 signaling pathway in three-negative breast cancer (TNBC) and the mechanism of its regulation. Methods The relative quantitative expressions of miR-182 and MTSS1 were detected in the cancerous and adjacent tissues of 30 cases of TNBC, the influence of miR-182 and MTSS1 on the proliferation and invasiveness of the cells evaluated by cell function tests, the potential binding sites of miR-182 to MTSS1 predicted with the Targetscan software, and MTSS1 confirmed to be the target gene by the dual luciferase reporter system. After transfection of miR-182 into the MCF-7 cells, RT-PCR and Western blot were used to determine the gene and protein expressions of MTSS1 and verify the regulatory effect of miR-182 targeting MTSS1. Results The expression of miR-182 was significantly higher (t=-8.409, P=0.000), while that of MTSS1 lower in the cancerous than in the adjacent tissue (t=2.961, P=0.006). The over expression of miR-182 and silenced expression of MTSS1 markedly enhanced the proliferation and migration of the MCF-7 cells compared with those of the control (P<0.01), while inhibition of miR-182 and over expression of MTSS1 remarkably suppressed their proliferation and migration of the MDA-MB-231 cells (P<0.01). The base sequences of 1083-1089 of the MTSS1 gene were confirmed to be the target binding sites of miR-182. After transfection of miR-182, the expression of MTSS1 in the MCF-7 cells was significantly down-regulated as compared with that in the control (t=-5.918, P= 0.027). Conclusion Target binding of miR-182 to MTSS1 down-regulates the expression of MTSS1 and promotes cell proliferation and migration, which may play an important biological role in the metastasis of TNBC.

5.
Surg Innov ; 15(2): 95-9, 2008 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-18480087

RESUMO

The aim of this study is to verify the feasibility of another option: transumbilical endoscopic cholecystectomy by using the trichannel trocar technique. Eight domestic pigs were submitted to transumbilical endoscopic cholecystectomy by using the trichannel trocar technique. A fine grasper of 2 mm in diameter was inserted through a small skin incision on the right upper abdomen for grasping the gallbladders. The natural scar of the umbilicus was restored after extract of the specimen. All the gallbladders were removed successfully without severe bleeding during dissection, intraoperative, and postoperative complications. Postmortem examination revealed that the gallbladder fossa was clean, the clips on the cystic duct and artery were secure, and neither bile nor blood leakage was found at the operative field. The feasibility and safety of transumbilical endoscopic cholecystectomy are demonstrated by this study. It is possible to use this approach in patients with gallbladder diseases.


Assuntos
Colecistectomia Laparoscópica/métodos , Animais , Colecistectomia Laparoscópica/instrumentação , Estudos de Viabilidade , Suínos , Umbigo
6.
Chinese Journal of Endemiology ; (6): 173-176, 2013.
Artigo em Chinês | WPRIM | ID: wpr-643259

RESUMO

Objective To study the association of TCF7L2 gene rs11196218,rs290487 polymorphisms with metabolic syndrome in type 2 diabetes mellitus population.Methods According to the diagnostic criteria of international diabetes federation (IDF),680 cases of type 2 diabetes patients were divided into metabolic syndrome (MS) group and non metabolic syndrome (control) group.DNA was extracted from peripheral mononuclear cells,and then PCR was performed to specifically amplify TCF7L2 gene fragments.Gene polymorphisms were determined by connected enzyme detection reaction.After population representative was checked by Hardy-Weinberg equilibrium,statistical analysis was completed by software SPSS 13.0.Results The population was accorded with Hardy-Weinberg equilibrium and possessed the population representative.Frequency distributions of genotypes (GG,AG and AA) in TCF7L2 gene rs11196218 in MS and control groups were 55.6%(233/419),35.8%(150/419),8.6% (36/419) and 54.8% (126/230),39.1% (90/230),6.1% (14/230),respectively.Frequency distributions of alleles(G and A) in TCF7L2 gene rs11196218 in MS and control groups were 73.5%(616/838),26.5%(222/838)and 74.3%(342/460),25.7%(118/460),respectively.Frequency distributions of genotypes (GG,AG and AA) in TCF7L2 gene rs290487 in MS and control groups were 14.8%(62/418),42.3%(177/418),42.9%(179/418) and 15.0%(34/226),48.2%(109/226),36.8%(83/226),respectively.Frequency distributions of alleles(G and A) in TCF7L2 gene rs11196218 in MS and control groups were 36.0% (301/836),64.0% (535/836) and 39.1% (177/452),60.9% (275/452),respectively.Frequency distribution of allele and genotype in TCF7L2 genes rsl 1196218 and rs290487 between the two groups were not associated with metabolic syndrome in type 2 diabetes population (P > 0.05).Conclusions TCF7L2 gene rs11196218,rs290487 polymorphisms has not association with metabolic syndrome of type 2 diabetes.

7.
Artigo em Chinês | WPRIM | ID: wpr-642163

RESUMO

Objective To investigated the effects of combined arsenic trioxide(ATO) and resveratrol(Res)on the viability of NB4 human leukemia cells. Methods NB4 human leukemia cell was used in this experiment.Cells were cultured in ATO (0,0.1875,0.3750,0.7500, 1.1250, 1.5000,2.2500,3.0000,5.0000 μmol/L) and Res (0, 1.5625,3.1250,6.2500, 12.5000, 18.7500,25.0000,37.5000,50.0000 μmol/L). Cell viabilities were measured by MTT in different treatment groups. Half inhibitory concentration(IC50) was calculated. The ratio of concentration of ATO and Res 1.5∶ 18,1.5∶ 25,1.5∶ 35 was added to cells, and the combination index(CI) was calculated. The level of ROS in control, ATO( 1.5000 μmol/L), Res(25.0000 μmol/L) and ATO(0.9000 μmol/L) + Res( 12.5000μmol/L) groups was measured by chemiluminescence assay. Results ①ATO( ≥0.7500 μmol/L) reduced the viability of NB4 cells in a concentration-dependent manner(P < 0.05 ), and IC50 was (1.78 ± 0.11 )μmol/L. ②)Res (≥18.7500 μ mol/L) dose-dependently decreased the viability of NB4 cells (P < 0.05 ), and IC50 was ( 18.71 ±0.18)μ mol/L. ③Combination of ATO and Res showed an antagonistic effect on NB4 cells viability. ④The ROS in Res group( 1670.55 ± 13.97) was significantly lower than that in control group(2345.88 ± 14.48,P < 0.05). The ROS in ATO group (3092.42 ± 94.84) was significantly higher than that in control group(P < 0.05). The ROS in ATO + Res group (1860.27 ± 15.99) was significantly lower than that in ATO group(P < 0.05). Conclusions NB4 cell survival rate can be decreased by ATO and Res. The combination of arsenic trioxide and Res presents an antagonistic effect on NB4 cell viability, in part by reducing intracellular ROS formation.

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