硒化蓖麻酸多相脂质体抗癌作用的初步报告

A PRELIMINARY REPORT ON ThHE ANTITUMOR EFFECTS OF POLYPHASE LIPOSOME OF RICINOLEIC ACID CONTAINING SELENIUM

将作者首次合成的硒化蓖麻酸及蓖麻酸分别制成乳剂和多相脂质体,进行各种剂型的动物体内外抗癌活性研究。结果,在体外500μg/ml的浓度下,蓖麻酸乳剂和硒化蓖麻酸乳剂都能100％地杀伤S^(180)腹水型瘤细胞,而对照组瘤细胞有97％存活。在体内蓖麻酸乳剂给小鼠腹腔注射200mg/kg,对S^(180)实体瘤的抑制率为30.6％(P<0.05);相同剂量下硒化蓖麻酸乳剂的抑瘤率为33.3％(P<0.05);蓖麻酸多相脂质体给小鼠腹腔注射400mg/kg,对S_(180)实体瘤的抑制率为58％(P<0.01),硒化蓖麻酸多相脂质体在同等剂量下对S1_(180)实体瘤的抑制率为61.4％(P<0.01),蓖麻酸硒化后与未硒化蓖麻酸相比疗效并无显著性差异,但比无机硒(Na2 SeO3毒性减低。用~3H-TdR作前体标记物研究表明,硒化蓖麻酸的抑制机理可能是影响~3H-TdR掺入。瘤细胞并抑制其细胞DNA的合成。

I Emulsion and polyphase liposome(PL) of ricinoteic acid (RA) and selenium um containing RA(Se-RA) were prepared by tween-80treatment and injection-ultrasonic met- bod. Their antitumor effects were tested in vitro and in vivo. As a result, the emulsion of RA and Se-RA can completely kill the mouse ascites tumor cells of S180 in vitro (500 uuuuuuu g/ml),(?)e, 97% cells of the control group still survived. When tested in vivo, the emulsion of RA and Se-RA were injected to .mice intra-peritoneally ( 200mg. kg-1/d) for 7 days their inhibition rates on S180 were 30.6% (p<0. 05) and .33.3% (p<0. 05) respectively. For the PL of RA and Se-RA, the inhibition rates were 58% (p<0.001), and 61 .4% (p<0. 001), respectively (400mg.kg-1/d). There was no significant difference between the inhibition rates of RA and Se-RA. The result of 3H-TdR incorporation exnperiment indicated that the possible antitumor mechanism of Se-RA was the inhibition of the incorporation of 3H-TdR into tumor cells and henee inhibit the DNA synthesis of the tumor cells.