Yamada K, Hino K, Tomoyasu S, Honma Y, Tsuruoka N
Department of Hematology, Showa University School of Medicine, Shinagawa, Tokyo, Japan.
Leuk Res. 1998 Jul;22(7):589-95. doi: 10.1016/s0145-2126(98)00044-7.
Bufalin, a cardiotonic steroid isolated from the Chinese toad venom preparation Chan'su, has differentiation-inducing activity in several myeloid leukemia cell lines. We examined the effect of bufalin on differentiation of leukemic cells from acute myeloid leukemia (AML) patients in primary culture. Bufalin significantly stimulated functional and morphologic differentiation of leukemia cells in four of 20 cases, suggesting that bufalin alone is only a modest inducer of differentiation of AML cells in primary culture. In contrast, acute promyelocytic leukemia (APL) cells showed synergistic differentiation after treatment with all-trans retinoic acid (RA) and bufalin. In some cases, bufalin restored RA sensitivity to previously resistant APL cells. The effective concentration of bufalin for differentiation-inducing activity in APL cells was lower than for its cardiac action. Combined treatment with bufalin and RA may be more effective than RA alone in differentiation therapy of APL.
蟾毒灵是从中国蟾蜍毒液制剂蟾酥中分离出的一种强心甾体，在多种髓系白血病细胞系中具有诱导分化活性。我们检测了蟾毒灵对原代培养的急性髓系白血病（AML）患者白血病细胞分化的影响。蟾毒灵在20例中的4例中显著刺激了白血病细胞的功能和形态分化，这表明单独使用蟾毒灵只是原代培养中AML细胞分化的适度诱导剂。相比之下，急性早幼粒细胞白血病（APL）细胞在用全反式维甲酸（RA）和蟾毒灵处理后表现出协同分化。在某些情况下，蟾毒灵恢复了先前耐药的APL细胞对RA的敏感性。蟾毒灵在APL细胞中诱导分化活性的有效浓度低于其心脏作用的有效浓度。蟾毒灵和RA联合治疗在APL的分化治疗中可能比单独使用RA更有效。
