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( Daulat Bikram Khadka ),( Giap Huu Tran ),( Somin Shin ),( Hang Thi Minh Nguyen ),( Hue Thi Cao ),( Chao Zhao ),( Yifeng Jin ),( Hue Thi My Van ),( Minh Van Chau ),( Youngjoo Kwon ),( Thanh Nguyen Le 전남대학교 약품개발연구소 2015 약품개발연구지 Vol.24 No.-
A series of 2-arylquinazolinones with structural homology to known 3-arylisoquinolines were designed and synthesized in order to develop safe. effective, and selective cytotoxic agents targeting topoisomerases (topos). 2-Arylquinzolinones with various substitutions on the aromatic rings were obtained by thermal cyclodehydration/dehydrogenation on reacting anthranilamides and benzaldehydes. The compounds had superior topo l-inhibitory activities but were generally inactive against topo IIα, Among the 6-methyl-, 6-amino-, and 7-methylquinazolinones, 6-amino-substituted derivatives displayed potent cytotoxicity at submicromolar to nanomolar concentrations against human colorectal adenocarcinoma cells (HCT-15), human ductal breast epithelial tumor cells (T47D), and cervical cancer cells (HeLa). There was a good correlation between topo I inhibition and the cytotoxic effects of 6-aminoquinazolinones. Docking models demonstrated that topo I inhibition by these compounds is owing to intercalation and H-bond interactions with the DNA bases and amino acid residues at the enzymatic site.
Tung Nguyen-Thach,Nguyen Canh-Hung,Nguyen Van-Duong,Nguyen Thi-Hong-Thuy,Nguyen Van-Lam,Tran Cao-Son,Pham Thi-Minh-Hue 한국약제학회 2020 Journal of Pharmaceutical Investigation Vol.50 No.4
Purpose The study aimed firstly to determine the release behavior of the model drug (berberine chloride) from the dry coated tablets. The second objective of this study was to evaluate the exact location of the dry coated tablets in in vivo. Methods The colon targeting tablets were developed by dry powder coating technique on pan coater. The drug release behavior was determined in the three continuous mediums: pH 1.2; 7.4 and 6.8 plus pectinase. The location of the dry coated tablets in the gastrointestinal tract of human volunteers was observed through the X-ray imaging of the dry coated tablets containing the optimized radiocontrast agents. Results The release kinetics of berberine chloride from the dry coated tablets was mainly controlled by erosion and enzyme sensitive mechanism. The optimum dry coated tablets having the coating powders of pectin 102:HPMC K4 M (2:1) with the coating level of 200%, and the tablet core with BaSO4 10% and iobitridol 30% as radiocontrast agents were observed in the caecum and ascending colon of human volunteers after 5–6 h of oral administration. Conclusion The successful development of these dosage forms is believed to have a high potential in precisely monitoring the release of highly potent drugs such as anti-inflammatory drugs in bowel diseases.