中国药学(英文版)
中國藥學(英文版)
중국약학(영문판)
JOURNAL OF CHINESE PHARMACEUTICAL SCIENCES
2007年
1期
47-50
,共4页
向蓉%张辅民%倪京满%田瑄
嚮蓉%張輔民%倪京滿%田瑄
향용%장보민%예경만%전선
鬼臼毒素%5-氟尿嘧啶%抗肿瘤活性%稳定性
鬼臼毒素%5-氟尿嘧啶%抗腫瘤活性%穩定性
귀구독소%5-불뇨밀정%항종류활성%은정성
Podophyllotoxin%5-Fluorouracil%Anti-tumor activity%Stabilities
目的 研究一种新型鬼臼类抗肿瘤药物.方法 根据拼合原理合成一种新的鬼臼类似物,并测定了其体外对肿瘤细胞的活性及在多种介质中的稳定性.结果 合成的化合物在体外对P-388,A-549和Bel-7402肿瘤细胞表现出比VP-16更强的抑制活性.同时固体样品对温度、光等因素的改变较稳定,而在人工胃液(AGJ)及pH较高的缓冲溶液中和高湿度条件下稳定性较差.结论 本试验的结果为该化合物的进一步研究提供了研究基础.
目的 研究一種新型鬼臼類抗腫瘤藥物.方法 根據拼閤原理閤成一種新的鬼臼類似物,併測定瞭其體外對腫瘤細胞的活性及在多種介質中的穩定性.結果 閤成的化閤物在體外對P-388,A-549和Bel-7402腫瘤細胞錶現齣比VP-16更彊的抑製活性.同時固體樣品對溫度、光等因素的改變較穩定,而在人工胃液(AGJ)及pH較高的緩遲溶液中和高濕度條件下穩定性較差.結論 本試驗的結果為該化閤物的進一步研究提供瞭研究基礎.
목적 연구일충신형귀구류항종류약물.방법 근거병합원리합성일충신적귀구유사물,병측정료기체외대종류세포적활성급재다충개질중적은정성.결과 합성적화합물재체외대P-388,A-549화Bel-7402종류세포표현출비VP-16경강적억제활성.동시고체양품대온도、광등인소적개변교은정,이재인공위액(AGJ)급pH교고적완충용액중화고습도조건하은정성교차.결론 본시험적결과위해화합물적진일보연구제공료연구기출.
Aim To study a new anti-cancer drug 5-FU-acetic podophyllic ester derivatized from podophyllotoxin. Methods A novel derivative of podophyllotoxin was synthesized. Its inhibitory effects against P-388, A-549, Bel-7402 and HL-60 in vitro were tested. The stability tests under different kinds of conditions were carried out. Results The novel derivative showed stronger inhibitory activities against P-388, A-549 and Bel-7402 in vitro than VP-16. The novel derivative was found to be stable at 60 ℃ and 4500 lx light in solid-state, but was less stable in humid condition. It was more stable in methanol (4 ℃ ) and chloroform (25 ℃ ) than in methanol (25 ℃ ), and less stable in artificial gastric juice ( AGJ, 37 ℃ ). Its stabilities were decreased while increasing the pH of buffer solutions. Conclusion These results could provide useful information for further study of this compound.