Umezawa K, Taniguchi T, Toi M, Ohse T, Tsutsumi N, Yamamoto T, Koyano T, Ishizuka M
Department of Applied Chemistry, Faculty of Science and Technology, Keio University, Yokohama, Japan.
Drugs Exp Clin Res. 1996;22(2):35-40.
Conophylline, a new vinca alkaloid isolated from the plant Ervatamia microphylla induced normal flat morphology in K-ras-NRK and K-ras-NIH cell lines, and lowered the increased uptake of 2-deoxyglucose in K-ras-NRK cells. Conophylline inhibited the growth of K-ras-NRK cells, but this inhibition was reversible. The alkaloid also inhibited the growth of K-ras-NRK and K-ras-NIH3T3 tumours transplanted into nude mice. On the other hand, it showed no effect on survival of the mice loaded with L1210 leukaemia. Thus, conophylline is a new antitumour vinca alkaloid that induced normal phenotypes in ras-expressing cells.
从植物小叶狗牙花中分离得到的一种新的长春花生物碱——锥丝碱，可诱导K-ras-NRK和K-ras-NIH细胞系呈现正常扁平形态，并降低K-ras-NRK细胞中2-脱氧葡萄糖摄取量的增加。锥丝碱抑制K-ras-NRK细胞的生长，但这种抑制是可逆的。该生物碱还抑制移植到裸鼠体内的K-ras-NRK和K-ras-NIH3T3肿瘤的生长。另一方面，它对荷L1210白血病小鼠的存活没有影响。因此，锥丝碱是一种新的抗肿瘤长春花生物碱，可在表达ras的细胞中诱导正常表型。
