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1.
Pathol Res Pract ; 214(5): 691-699, 2018 May.
Artigo em Inglês | MEDLINE | ID: mdl-29567333

RESUMO

Matrine, as a natural alkaloid isolated from the traditional herb medicine sophora flavescens, has been proved to possess excellent biological activities, including anticancer effects. Now, this research aims to assess the anticancer activities and the mechanism of matrine against esophageal cancer cells, we investigated the proliferative inhibition, apoptosis induction, as well as the underlying mechanism of matrine on esophageal cancer KYSE-150 cells. It was found that matrine could suppress KYSE-150 cell proliferation and significantly mediate cell apoptosis in a dose-dependent relation by increasing intracellular reactive oxygen species level and triggering mitochondrial membrane potential disruption. More precise mechanism studies demonstrated that matrine could up-regulate the expression of Bax proteins and down-regulate the expression of Bcl-2 proteins, as well as the activation about caspase-3, 8 and 9 in KYSE-150 cells. The morphological analysis of KYSE-150 cells exhibited that matrine could destroy the F-actin and nuclei structures and induce morphological damage with increased surface height distribution and roughness of cell membrane. These results not only demonstrated the potential anticancer activity mechanism of matrine at nanoscale, but also provide preliminary guidance for the treatment of esophageal cancer using matrine.


Assuntos
Proliferação de Células/efeitos dos fármacos , Medicamentos de Ervas Chinesas/farmacologia , Mitocôndrias/efeitos dos fármacos , Espécies Reativas de Oxigênio/metabolismo , Alcaloides , Carcinoma de Células Escamosas/tratamento farmacológico , Carcinoma de Células Escamosas/metabolismo , Linhagem Celular Tumoral , Neoplasias Esofágicas/tratamento farmacológico , Neoplasias Esofágicas/metabolismo , Carcinoma de Células Escamosas do Esôfago , Humanos , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Quinolizinas , Proteína X Associada a bcl-2/metabolismo , Matrinas
2.
Bioorg Med Chem Lett ; 23(10): 2902-8, 2013 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-23570787

RESUMO

Germanium (Ge) is considered to play a key role in the pharmacological effects of some medicinal plants. Here, two new Ge(IV)-polyphenol complexes were synthesized and measured for their potential biological activities. The results indicated that these Ge(IV)-polyphenol complexes possessed great anti-oxidative activities, both showing stronger hydroxyl scavenging effects than their corresponding ligands. We also demonstrated the strong intercalating abilities of Ge(IV)-polyphenol complexes into calf thymus-DNA molecules. In addition, these two Ge(IV)-polyphenol complexes showed strong proliferative inhibition effect on HepG2 cancer cells. Moreover, the morphological changes in HepG2 cells induced by Ge(IV)-polyphenol complexes were detected by atomic force microscopy. All these results collectively suggested that Ge(IV)-polyphenol complexes could be served as promising pharmacologically active substances against cancer treatment.


Assuntos
Antineoplásicos/farmacologia , Germânio/química , Compostos Organometálicos/farmacologia , Polifenóis/química , Antineoplásicos/síntese química , Antineoplásicos/química , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Células Hep G2 , Humanos , Estrutura Molecular , Compostos Organometálicos/síntese química , Compostos Organometálicos/química , Relação Estrutura-Atividade
3.
Eur J Pharm Sci ; 47(1): 28-34, 2012 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-22579957

RESUMO

Quercetin is a popular flavonoid in plant foods, herbs, and dietary supplement. Germanium, a kind of trace elements, can enhance the body immunity. This study investigated the hydroxyl-radical-scavenging mechanism of the quercertin-germanium (IV) (Qu-Ge) complex to human erythrocytes, especially the effects on ultrastructure and mechanical properties of cell membrane, plasma membrane potential and intracellular free Ca(2+) concentration. Results showed that QuGe(2), a kind of the Qu-Ge complex, could reduce the oxidative damage of erythrocytes, change the cell-surface morphology, and partly recover the disruption of plasma membrane potential and intracellular free Ca(2+) level. Atomic force microscopy (AFM) was used to characterize the changes of the cell morphology, cell-membrane ultrastructure and biophysical properties at nanoscalar level. QuGe(2) has triggered the antioxidative factor to inhibit cellular damage. These results can improve the understanding of hydroxyl-radical-scavenging mechanism of human erythrocytes induced by the Qu-Ge complex, which can be potentially developed as a new antioxidant for treatment of oxidative damage.


Assuntos
Complexos de Coordenação/farmacologia , Eritrócitos/efeitos dos fármacos , Eritrócitos/metabolismo , Sequestradores de Radicais Livres/farmacologia , Germânio/farmacologia , Radical Hidroxila/sangue , Quercetina/farmacologia , Antioxidantes/farmacologia , Cálcio/metabolismo , Membrana Celular/efeitos dos fármacos , Membrana Celular/metabolismo , Membrana Celular/ultraestrutura , Células Cultivadas , Membrana Eritrocítica/efeitos dos fármacos , Membrana Eritrocítica/metabolismo , Citometria de Fluxo , Humanos , Potenciais da Membrana/efeitos dos fármacos , Microscopia de Força Atômica , Estresse Oxidativo/efeitos dos fármacos , Espécies Reativas de Oxigênio/metabolismo
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