华南师范大学学报(自然科学版)
華南師範大學學報(自然科學版)
화남사범대학학보(자연과학판)
JOURNAL OF SOUTH CHINA NORMAL UNIVERSITY (NATURAL SCIENCE EDITION)
2014年
3期
82-86
,共5页
周代营%田宇光%杜志云%赵肃清%郑希%张焜
週代營%田宇光%杜誌雲%趙肅清%鄭希%張焜
주대영%전우광%두지운%조숙청%정희%장혼
单羰基姜黄素类似物%合成%抗肿瘤活性
單羰基薑黃素類似物%閤成%抗腫瘤活性
단탄기강황소유사물%합성%항종류활성
mono-carbonyl curcumin analogues%synthesis%anticancer activity
采用氮烷基化、羟基保护、醛酮缩合的三步反应合成了8个新型单羰基姜黄素类似物,结构经质谱、核磁共振氢谱和核磁共振碳谱等手段进行确认.并采用 MTT 染色法体外检测所合成的单羰基姜黄素类似物对肺癌细胞 H1299、结肠癌细胞 HT-29、胰腺癌细胞 BxPC-3和前列腺癌细胞 PC-3的抗肿瘤活性.半数抑制浓度 IC50值结果显示:所合成的8个姜黄素类似物对4种肿瘤细胞均有较强的抑制作用,其中化合物 A6半数抑制浓度 IC50均在0.65μmol/ L 以下,抗癌活性比姜黄素提高40倍以上.
採用氮烷基化、羥基保護、醛酮縮閤的三步反應閤成瞭8箇新型單羰基薑黃素類似物,結構經質譜、覈磁共振氫譜和覈磁共振碳譜等手段進行確認.併採用 MTT 染色法體外檢測所閤成的單羰基薑黃素類似物對肺癌細胞 H1299、結腸癌細胞 HT-29、胰腺癌細胞 BxPC-3和前列腺癌細胞 PC-3的抗腫瘤活性.半數抑製濃度 IC50值結果顯示:所閤成的8箇薑黃素類似物對4種腫瘤細胞均有較彊的抑製作用,其中化閤物 A6半數抑製濃度 IC50均在0.65μmol/ L 以下,抗癌活性比薑黃素提高40倍以上.
채용담완기화、간기보호、철동축합적삼보반응합성료8개신형단탄기강황소유사물,결구경질보、핵자공진경보화핵자공진탄보등수단진행학인.병채용 MTT 염색법체외검측소합성적단탄기강황소유사물대폐암세포 H1299、결장암세포 HT-29、이선암세포 BxPC-3화전렬선암세포 PC-3적항종류활성.반수억제농도 IC50치결과현시:소합성적8개강황소유사물대4충종류세포균유교강적억제작용,기중화합물 A6반수억제농도 IC50균재0.65μmol/ L 이하,항암활성비강황소제고40배이상.
Eight mono-carbonyl curcumin analogues were synthesized by a three-step reaction of alkylation,hydrox-yl protection,and aldehyde ketone condensation. Their structures were characterized by 1 H NMR and ESI-MS tech-niques. All the compounds were evaluated for their effects on cultured prostate cancer PC-3 cells,pancreas cancer BxPC-3 cells,colon cancer HT-29 cells and lung cancer H1299 cells. These compounds exhibited inhibitory effects on the growth of cultured PC-3,BxPC-3,HT-29 and H1299 cells. The IC50 of compound A6 was lower than 0. 65μmol/ L in all four cell lines,and A6 was 40-fold more active than curcumin.