STUDIES ON THE ANTITUMOR ACTIVITY OF POLYPHASE LIPOSOME OF RICINOLEIC ACID CONTAINING SELENIUM

Emulsion and polyphase liposome (PL) of ricinoleic acid (RA) and RA containing selenium (Se-RA) were prepared by tween-80 treatment and injection-ultrasonic method. Their antitumor effects were tested in vitro and in vivo. As a result, the emulsion of RA (91 ) and Sc-RA (92) can completely kill the mouse ascites tumor cells of S180 in vitro (500 μg/ml). While. 97% cells of the control group still survive. When tested in vivo, 91 and 92 were injected into mice peritoneally (200 mg/Kg/day) for 7 days, their inhibit rate on S180 are 30. 6% (P<0. 05) and 33. 3% (P<0. 05) respectively. For the PL of RA (113) and Se-RA (114), the inhibit rate are 58% (P< 0.001) and 61.4% (P<0. 001) respectively (400 mg/kg/day). The result of 3H-TdR incorporation experiment indicates that the possible antitumor mechanism of Se-Ra is that it can inhibit the incorporation of 3H- TdR into tumor cells and hense inhibit the DNA synthesis of the tumor cells.

硒化亚油酸多相脂质体的抗肿瘤作用研究

将作者首次合成的硒化亚油酸分别制成乳剂和多相脂质体两种剂型,对移植性动物实验肿瘤进行抑瘤试验。结果:硒化亚油酸乳剂(62)对小鼠每天腹腔注射200mg/kg,对荷艾氏腹水瘤小鼠的治愈率达80％,使其生命延长率大于70％(P<0.01);对荷ARS腹水瘤小鼠的治愈率达56％,使其生命延长率大于143％(P<0.001);对小鼠S_(180)实体瘤的抑制率为28～30％;而硒化亚油酸多相脂质体(118)每天腹腔注射300mg/kg对小鼠S_(180)实体瘤的抑制率则可达51～67％(P<0.001)。这些结果提示,由人体必需的营养素硒与亚油酸合成的硒化亚油酸所组成的多相脂质体具有明显的抗肿瘤作用。