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1.
Bioorg Chem ; 105: 104430, 2020 12.
Artigo em Inglês | MEDLINE | ID: mdl-33171407

RESUMO

For the sake to develop novel platinum(IV) complexes to reverse cisplatin (CDDP) resistence, four multifunctional platinum(IV) prodrugs via conjugating chalcones with the related platinum(IV) complexes derived from cisplatin were designed and evaluated for anti-tumor actyivities in vitro and in vivo. Among them, complex 9 exhibited excellent anticancer activities in vitro with IC50 values at the submicromolar level against the tested human cancer cells, whereas showed low cytotoxicity towards human normal liver cells HL-7702. Further mechanistic studies indicated that complex 9 induced G2/M phase arrest and apoptosis in A549 cells, which was associated with a collapse of the mitochondrial membrane potential (MMP), alterations in the expression of some apoptosis-related proteins, and enhanced level of the intracellular reactive oxygen species (ROS). More importantly, complex 9 significantly suppressed the tumor growth in the A549 xenograft model without obvious hints of toxicity.


Assuntos
Antineoplásicos/farmacologia , Chalcona/farmacologia , Complexos de Coordenação/farmacologia , Platina/farmacologia , Animais , Antineoplásicos/síntese química , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Chalcona/química , Complexos de Coordenação/síntese química , Complexos de Coordenação/química , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Humanos , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Estrutura Molecular , Neoplasias Experimentais/tratamento farmacológico , Neoplasias Experimentais/patologia , Platina/química , Relação Estrutura-Atividade
2.
Ultrason Sonochem ; 23: 53-8, 2015 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-25199445

RESUMO

Biodiesel production from soybean oil deodorizer distillate enhanced by counter-current pulsed ultrasound was studied. Effect of static probe ultrasonic enhanced transesterification (SPUE) and counter-current probe ultrasonic enhanced transesterification (CCPUE) on the biodiesel conversion were compared. The results indicated that CCPUE was a better method for enhancing transesterification. The working conditions of CCPUE were studied by single-factor experiment design and the results showed that the optimal conditions were: initial temperature 25 °C, methanol to triglyceride molar ratio 10:1, flow rate 200 mL/min, catalyst content 1.8%, ultrasound working on-time 4 s, off-time 2 s, total working time 50 min. Under these conditions, the average biodiesel conversion of three experiments was 96.1%.


Assuntos
Biocombustíveis , Resíduos Industriais , Odorantes , Sonicação , Óleo de Soja/química , Catálise , Esterificação , Temperatura
3.
Bioresour Technol ; 148: 202-7, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-24055964

RESUMO

Lipase from Burkholderia cepacia was immobilized on modified attapulgite by cross-linking reaction for biodiesel production with jatropha oil as feedstock. Effects of various factors on biodiesel production were studied by single-factor experiment. Results indicated that the best conditions for biodiesel preparation were: 10 g jatropha oil, 2.4 g methanol (molar ratio of oil to methanol is 1:6.6) being added at 3h intervals, 7 wt% water, 10 wt% immobilized lipase, temperature 35°C, and time 24h. Under these conditions, the maximum biodiesel yield reached 94%. The immobilized lipase retained 95% of its relative activity during the ten repeated batch reactions. The half-life time of the immobilized lipase is 731 h. Kinetics was studied and the Vmax of the immobilized lipases were 6.823 mmol L(-1). This immobilized lipase catalyzed process has potential industrial use for biodiesel production to replace chemical-catalyzed method.


Assuntos
Biocatálise/efeitos dos fármacos , Biocombustíveis/análise , Burkholderia cepacia/enzimologia , Jatropha/química , Lipase/metabolismo , Compostos de Magnésio/farmacologia , Óleos de Plantas/química , Compostos de Silício/farmacologia , Burkholderia cepacia/efeitos dos fármacos , Estabilidade Enzimática/efeitos dos fármacos , Enzimas Imobilizadas/metabolismo , Cinética , Metanol/farmacologia , Reciclagem , Temperatura , Fatores de Tempo , Água
4.
Int J Med Mushrooms ; 14(6): 549-56, 2012.
Artigo em Inglês | MEDLINE | ID: mdl-23510248

RESUMO

The immunomodulatory activities of different solvent extracts from the culinary-medicinal mushroom Tricholoma matsutake were studied in vivo in normal mice. The extracts were prepared using different solvents in an order of increasing polarity. The immunomodulatory activities were investigated by measuring the thymus and spleen index, phagocytic rate of macrophage phagocytosis, delayed-type hypersensitivity, plaque-forming cell, and proliferation of splenocytes. Results demonstrated that water extract (WE) and n-butyl alcohol extract (BAE) of T. matsutake could enhance the immunity of mice significantly compared with the control group. Main components of WE and BAE were polysaccharides, proteins, and flavonoids; we presume that these may be the main immunomodulating and immuno-enhancing agents in T. matsutake.


Assuntos
Fatores Imunológicos/química , Fatores Imunológicos/farmacologia , Tricholoma/química , Animais , Peso Corporal , Células Cultivadas , Feminino , Macrófagos/efeitos dos fármacos , Macrófagos/fisiologia , Camundongos , Fagocitose/efeitos dos fármacos , Organismos Livres de Patógenos Específicos , Baço/citologia , Baço/efeitos dos fármacos
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