AIM: To study the isoflavonoids and their glycosides from the fruits of Sophora japonica L.and to investigate the anticancer activity in vitro of these compounds.METHOD: The constituents were isolated and purified by ...AIM: To study the isoflavonoids and their glycosides from the fruits of Sophora japonica L.and to investigate the anticancer activity in vitro of these compounds.METHOD: The constituents were isolated and purified by chromatographic techniques and their structures were elucidated by physico-chemical evidence and spectra data.The inhibitory activity on cultured human cancer cell lines was determined by MTT assay.RESULTS: Nine compounds were isolated and identified as:genistein（Ⅰ）,sophororicoside（Ⅱ）,genistin（Ⅲ）,sophorabioside（Ⅳ）,genistein 7,4′-di-O-βD-glucoside（Ⅴ）,formononetin（Ⅵ）,ononin（Ⅶ）,daidzin（Ⅷ） and afrormosin （Ⅸ）.Results showed that tumor inhibitory rate of compounds Ⅰ～Ⅲ on(100 Hg·mL-1) A549 reached 82.01%,38.87% and 32.97% respectively,and on BGC-823 reached 91.25%,23.26% and 13.98% respectively.CONCLUSION: Compounds Ⅶ and Ⅷ were isolated from this plant for the first time;compound Ⅸ was isolated from the fruits of the plant for the first time.The study showes that genistein has inhibitory effect on A549 and BGC-823 cell in vitro.展开更多
BACKGROUND： Ulinastatin （UTI） is a urinary trypsin inhibitor extracted and purified from urine of males. This study aimed to explore the effects of UTI on paraquat-induced-oxidative stress in human type II alveolar...BACKGROUND： Ulinastatin （UTI） is a urinary trypsin inhibitor extracted and purified from urine of males. This study aimed to explore the effects of UTI on paraquat-induced-oxidative stress in human type II alveolar epithelial cells. METHODS： The human type II alveolar epithelial cells, A549 cells, were cultured in vitro. The A549 cells were treated with different concentrations of paraquat （200, 400, 600, 800, 1 000, 1 200 pmol/L） and ulinastatin（0, 2 000, 4 000, 6 000, 8 000 U/mL） for 24 hours, the cell viability was measured by cell counting kit-8 and the median lethal concentration was selected. In order to establish an in vitro model of paraquat intoxication and to determine the safe dose of ulinastatin, we calculated LD50 using cell counting kit-8 to determine the survival rate of the cells. A549 cells were divided into normal control group, paraquat group and paraquat＋ulinastatin group. The levels of malondialdehyde （MDA） and myeloperoxidase （MPO） were detected by biochemistry colorimetry, while the level of reactive oxygen spies （ROS） was detected by DCFH-DA assay. RESULTS： The survival rate of A549 cells treated with different concentrations of paraquat decreased in a concentration-dependent manner. Whereas there was no decrease in the survival rate of cells treated with 0-4 000 U/mL ulinastatin. The levels of MDA, MPO, and ROS were significantly higher in the paraquat group than in the normal control group after 24-hour-exposure. And the survival rate of the paraquat＋ulinastatin group was higher than that of the paraquat group, but lower than that of the normal control group. The levels of MDA, MPO, and ROS were lower than those of the paraquat group. CONCLUSION： Ulinastatin can alleviate the paraquat-induced A549 cell damage by reducing oxidative stress.展开更多
Icaritin, a prenylflavonoid derivative from Epimedium Genus, has been shown to exhibit many pharmacological and biological activities. However, the function and the underlying mechanisms of icaritin in human non-small...Icaritin, a prenylflavonoid derivative from Epimedium Genus, has been shown to exhibit many pharmacological and biological activities. However, the function and the underlying mechanisms of icaritin in human non-small cell lung cancer have not been fully elucidated. The purpose of this study was to investigate the anticancer effects of icaritin on A549 cells and explore the underlying molecular mechanism. The cell viability after icaritin treatment was tested by MTT assay. The cell cycle distribution, apoptosis and reactive oxygen species（ROS） levels were analyzed by flow cytometry. The mRNA and protein expression levels of the genes involved in proliferation and apoptosis were respectively detected by RT-PCR and Western blotting. The results demonstrated that icaritin induced cell cycle arrest at S phase, and down-regulated the expression levels of S regulatory proteins such as Cyclin A and CDK2. Icaritin also induced cell apoptosis characterized by positive Hoechst 33258 staining, accumulation of the Annexin V-positive cells, increased ROS level and alteration in Bcl-2 family proteins expression. Moreover, icaritin induced sustained phosphorylation of ERK and p38 MAPK. These findings suggested that icaritin might be a new potent inhibitor by inducing S phase arrest and apoptosis in human lung carcinoma A549 cells.展开更多
文摘AIM: To study the isoflavonoids and their glycosides from the fruits of Sophora japonica L.and to investigate the anticancer activity in vitro of these compounds.METHOD: The constituents were isolated and purified by chromatographic techniques and their structures were elucidated by physico-chemical evidence and spectra data.The inhibitory activity on cultured human cancer cell lines was determined by MTT assay.RESULTS: Nine compounds were isolated and identified as:genistein（Ⅰ）,sophororicoside（Ⅱ）,genistin（Ⅲ）,sophorabioside（Ⅳ）,genistein 7,4′-di-O-βD-glucoside（Ⅴ）,formononetin（Ⅵ）,ononin（Ⅶ）,daidzin（Ⅷ） and afrormosin （Ⅸ）.Results showed that tumor inhibitory rate of compounds Ⅰ～Ⅲ on(100 Hg·mL-1) A549 reached 82.01%,38.87% and 32.97% respectively,and on BGC-823 reached 91.25%,23.26% and 13.98% respectively.CONCLUSION: Compounds Ⅶ and Ⅷ were isolated from this plant for the first time;compound Ⅸ was isolated from the fruits of the plant for the first time.The study showes that genistein has inhibitory effect on A549 and BGC-823 cell in vitro.
基金supported by grants from National Natural Science Foundation(81272071)Techpool Foundation(01201111)
文摘BACKGROUND： Ulinastatin （UTI） is a urinary trypsin inhibitor extracted and purified from urine of males. This study aimed to explore the effects of UTI on paraquat-induced-oxidative stress in human type II alveolar epithelial cells. METHODS： The human type II alveolar epithelial cells, A549 cells, were cultured in vitro. The A549 cells were treated with different concentrations of paraquat （200, 400, 600, 800, 1 000, 1 200 pmol/L） and ulinastatin（0, 2 000, 4 000, 6 000, 8 000 U/mL） for 24 hours, the cell viability was measured by cell counting kit-8 and the median lethal concentration was selected. In order to establish an in vitro model of paraquat intoxication and to determine the safe dose of ulinastatin, we calculated LD50 using cell counting kit-8 to determine the survival rate of the cells. A549 cells were divided into normal control group, paraquat group and paraquat＋ulinastatin group. The levels of malondialdehyde （MDA） and myeloperoxidase （MPO） were detected by biochemistry colorimetry, while the level of reactive oxygen spies （ROS） was detected by DCFH-DA assay. RESULTS： The survival rate of A549 cells treated with different concentrations of paraquat decreased in a concentration-dependent manner. Whereas there was no decrease in the survival rate of cells treated with 0-4 000 U/mL ulinastatin. The levels of MDA, MPO, and ROS were significantly higher in the paraquat group than in the normal control group after 24-hour-exposure. And the survival rate of the paraquat＋ulinastatin group was higher than that of the paraquat group, but lower than that of the normal control group. The levels of MDA, MPO, and ROS were lower than those of the paraquat group. CONCLUSION： Ulinastatin can alleviate the paraquat-induced A549 cell damage by reducing oxidative stress.
基金supported by grants from Wuhan Municipal Science and Technology Research Project,China(No.201260523185)the Public Science and Technology Research Funds Projects of Ocean,China(No.201005013)
文摘Icaritin, a prenylflavonoid derivative from Epimedium Genus, has been shown to exhibit many pharmacological and biological activities. However, the function and the underlying mechanisms of icaritin in human non-small cell lung cancer have not been fully elucidated. The purpose of this study was to investigate the anticancer effects of icaritin on A549 cells and explore the underlying molecular mechanism. The cell viability after icaritin treatment was tested by MTT assay. The cell cycle distribution, apoptosis and reactive oxygen species（ROS） levels were analyzed by flow cytometry. The mRNA and protein expression levels of the genes involved in proliferation and apoptosis were respectively detected by RT-PCR and Western blotting. The results demonstrated that icaritin induced cell cycle arrest at S phase, and down-regulated the expression levels of S regulatory proteins such as Cyclin A and CDK2. Icaritin also induced cell apoptosis characterized by positive Hoechst 33258 staining, accumulation of the Annexin V-positive cells, increased ROS level and alteration in Bcl-2 family proteins expression. Moreover, icaritin induced sustained phosphorylation of ERK and p38 MAPK. These findings suggested that icaritin might be a new potent inhibitor by inducing S phase arrest and apoptosis in human lung carcinoma A549 cells.
