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Antitumor activity of a novel bis-aziridinylnaphthoquinone (AZ4) mediating cell cycle arrest and apoptosis in non-small cell lung cancer cell line NCl-H460

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Acta Pharmacologica Sinica 2007年第4期28卷 559-566页

作者： kou-gea shyu Hsien-shou KUO Yuh-ling LIN Division of Cardiac Shin Kong Wu Ho-Su Memorial HospitalTaipei 106TaiwanChina Department of Biochemistry Taipei Medical UniversityTaipei City 110TaiwanChina Department of Medicine Fu-Jen Catholic UniversityHsin-ChuangTaipei Hsien 242TaiwanChina

Aim:The cytotoxic activities of a series of bis-aziridinylnaphthoquinone,AZ1 toAZ4,on human lung carcinoma cell lines,H460,and normal lung cells fibroblastcell line,MRC-5,and the mechanisms of H460 cells induced by AZ4 ***:The MTT assay was used to determine the *** cycle was analysed by *** activity of caspase 3,8 and 9was determined by cell-permeable fluorogenic detection *** blotassay was used to evaluate the regulation of cyclin B,Cdc-2,p53,p21,and the Bcl-2 ***:AZ1 to AZ4 displayed various cytotoxicity activities againstH460 and MRC-5 *** to those compounds,AZ4 was with the mosteffective agent among the 5 tested analogues at reducing H460 cell viability with anIC50value of 1.23 μmol/L;it also exhibited weak cytotoxicity against MRC-5 cells withan IC50value of 12.7 μmol/*** results show that growth arrest on the G2-M phaseof H460 cells induced by AZ4 for 24 h was discovered,and this might be alteredwith the reduced Cdc-2 protein expression of 47% at 2.0 μmol/L AZ4,but not withcyclin B protein *** AZ4 treated cells were then led to apoptosis after48 *** was associated with the activation of apoptotic enzyme caspase 3 andmediated by caspase 8,but not caspase 9 at various concentrations of AZ4 afterbeing cultured for 48 h and 30 h,*** anti-apoptotic protein （Bcl-2）expression in H460 cells altered by 39% with downregulation,and the p53 proteinby 25% with upregulation after being cultured with 2.0 μmol/L AZ4 for 48 *** atime-dependent wanrer,the expression of the p53 and p21 proteins were increasedto the maximum at 24 h,and then decreased at ***:AZ4 represents anovel antitumor aziridinylnaphthoquinone with therapeutic potential against thenon-small cell lung cancer cells.

关键词： cell cycle apoptosis Bcl-2 protein aziridinylnaphthoquinone

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Preparation of slab-shaped lactose carrier particles for dry powder inhalers by air jet milling

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Asian Journal of Pharmaceutical Sciences 2017年第1期12卷 59-65页

作者： Xiang kou Lai Wah Chan Changquan Calvin Sun Paul Wan Sia Heng gea-NUS Pharmaceutical Processing Research Laboratory Department of PharmacyNational University of Singapore18 Science Drive 4Singapore 117543Singapore Pharmaceutical Materials Science and Engineering Laboratory Department of PharmaceuticsUniversity of Minnesota308 Harvard St.SEMinneapolisMN 55455USA

Dry powder inhalers are often formulated by attaching micronized drug particles onto carrier particles, which are generally lactose. In this study, commercially available lactose was air jet milled to produce unique slab-like coarse carrier particles, which have larger and rougher surfaces compared to other commercially available lactose. Two key processing factors, i.e.,classifier speed and jet milling pressure, were systematically investigated. The largest fraction of slab-like particles in the resulting powder was obtained at a classifier speed of 3000 *** slab-like coarse carrier particles are expected to exhibit superior performance than commercial lactose due to their unique surface properties.

关键词： Particle engineering Shape modification Lactose Dry powder inhaler

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2010年台湾心脏病学会高血压管理指南

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中华高血压杂志 2011年第1期19卷 9-23页

作者： Chern-En Chiang Tzung-Dau Wang Yi-Heng Li Tsung-Hsien Lin Kuo-Liong Chien Hung-I Yeh kou-Gi shyu Wei-Chuen Tsai Ting-Hsing Chao Juey-Jen Hwang Fu-Tien Chiang Jyh-Hong Chen Unknown unit

高血压是心血管疾病和心血管死亡的重要危险因素。从2003年美国高血压预防、检测、评价和治疗全国联合委员会第7次报告（the seventh report of the joint national committee on prevention,detection,evaluation,and treatment of hig... 详细信息

关键词：欧洲心脏病学会高血压协会管理指南 prevention 心血管疾病台湾地区联合委员会危险因素

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