周金煦, 胥彬, 王道苑, 刘明章, 陈瑞婷. 抗肿瘤药物的研究Ⅲ. 数种锑胺羧螯合物对实验肿瘤的作用J. 药学学报, 1959, 7(7): 259-265.
引用本文: 周金煦, 胥彬, 王道苑, 刘明章, 陈瑞婷. 抗肿瘤药物的研究Ⅲ. 数种锑胺羧螯合物对实验肿瘤的作用J. 药学学报, 1959, 7(7): 259-265.
CHOU CHIN-HS HSV BIN WANG TAO-YUAN LIU MING-CHANG CH’EN JUEI-TING, . STUDIES ON ANTITUMOR DRUGS,Ⅲ.EFFECTS OF SOME Sb-DERIVATIVES OF COMPLEXONES ON EXPERIMENTAL TUMORSJ. Acta Pharmaceutica Sinica, 1959, 7(7): 259-265.
Citation: CHOU CHIN-HS HSV BIN WANG TAO-YUAN LIU MING-CHANG CH’EN JUEI-TING, . STUDIES ON ANTITUMOR DRUGS,Ⅲ.EFFECTS OF SOME Sb-DERIVATIVES OF COMPLEXONES ON EXPERIMENTAL TUMORSJ. Acta Pharmaceutica Sinica, 1959, 7(7): 259-265.

抗肿瘤药物的研究Ⅲ. 数种锑胺羧螯合物对实验肿瘤的作用

STUDIES ON ANTITUMOR DRUGS,Ⅲ.EFFECTS OF SOME Sb-DERIVATIVES OF COMPLEXONES ON EXPERIMENTAL TUMORS

  • 摘要: 1.锑胺羧螯合物是一种新型的抗肿瘤药物,应用Sb-26(EDTA-SbNa)、Sb-57(PDTA-SbNa)、Sb-66(HEDT-Sb)和Sb-71(ATA-Sb)分别为15—20、30—50、25—30和20—40毫克/公斤剂量时,均能显著地抑制小白鼠Ehrlich 腹水瘤的生长,平均延长生存时间4—22天,延长率36—147%.上述剂量对大白鼠Guerin 氏癌也有抑制作用,抑制率为58—70%.后3个药物,还能使小白鼠梭形细胞肉瘤腹水型的生存时间延长5—16天,延长率50—160%,其中以Sb-71的疗效最著.Sb-26、Sb-57、Sb-71、Sb-66对肉瘤180和AK 肉瘤及前3者对Ehrlich 固体瘤和淋巴白血病固体型的实验结果,除Sb-71对肉瘤180有抑制作用外,其他均无疗效.2.4 类锑化合物:3个(月弟)酸化合物(Sb-8,Sb-11和Sb-42)及1个酒石酸锑(Sb-15),与螯合的间苯二酚锑(Sb-64)和8羟基喹啉锑(Sb-85)各1个,对Ehrlich 腹水瘤的实验结果,均无明显疗效.3.小白鼠的急性半数致死量,Sb-57和Sb-71分别为131和62毫克/公斤,亚急性半数致死量分别为75和58毫克/公斤.

     

    Abstract: The antitumor activity of Sb-derivatives of complexones has not yet been reported in the literature.In this work we found that Sb-26 (Sb Na ethylenediamine tetraacetate 15—20 mg/kg), Sb-57(Sb Na propylenediamine tetraacetate 30—50 mg/kg),Sb-66(Sb β-hydroxyethyl imino- diacetic acid 25—30 mg/kg)and Sb-71(Sb ammonia triacetic acid 20—40 mg/kg)could significantly inhibit the growth of Ehrlich ascites carcinoma of mice and prolonged the survival time for 4—22 days(36—147%,P<0.05)in comparison with the control group.These com- pounds at the above mentioned dosages inhibited also the growth of Guerin’s carcinoma.The degree of inhibition was about 58—70%(P<0.05).The survival time of mice bearing spindle cell sarcoma(in ascitic form)was also prolonged for 5—16 days(50—160%,P<0.05)by treatment with the latter three drugs,among which Sb-71 was most active. Experiments were carried out on mice bearing sarcoma 180 or sarcoma AK treated with Sb-26,Sb-57,Sb-71 or Sb-66 and on mice bearing Ehrlich carcinoma or lymphatic leucemia (solid form)treated with the former three drugs.It was found that only Sb-71 possessed certain inhibitory action on sarcoma 180. In the present study,Sb-8,Sb-11,Sb-42,Sb-15,Sb-64 and Sb-85 were all lacking in inhibitory effect on Ehrlich ascites carcinoma of mice. In mice,the acute LD50levels after intraperitoneal injections of Sb-57 and Sb-71 were found to be 131 and 62 mg/kg respectively;the subacute LD50(10 injections)were equal to 75 and 58 mg/kg respectively.

     

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