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阿霉素 - 铝络合物修饰抗癌剂的实验研究

[Experimental study on an adriamycin-aluminum complex modified anticancer agent].

作者信息

Shintomi Y

出版信息

Nihon Gan Chiryo Gakkai Shi. 1989 Jan 20;24(1):69-77.

PMID:2738441
Abstract

We produced the chelated Adriamycin-Aluminum complex (ADM-Al complex) for experimented evaluation. Human gastric cancer was transplanted into nude mice divided into 4 groups for drug injections; 1) Control (0.9% NaCl), 2) Al acetate (1 mg/ml), 3) ADM only (1 mg/ml) and 4) ADM-Al complex (ADM 1 mg/ml + Al 1 mg/ml), 0.2 ml of each was administered through several injections simultaneously into the tumor periphery. Long term retention of ADM in the tumor was observed pathologically in Group 4. The concentration (microgram/g) of ADM after injection (5, 7, 28 days) was 22.3, 12.6, and 3.5 in Group 4, against 8.4, 2.0, and 0.0 in Group 3 (p less than 0.01). The estimated tumor weight inhibition rate was 66.6% in Group 4, compared with 21.4% in Group 3, and only 3% in Group 2. DNA tritium thymidine uptake inhibition rate was 43.8% in Group 4, compared with 21.2% in Group 3, and in 9.4% Group 2. No side-effect due to Al-chelation was observed. These results demonstrate the effectiveness of ADM-Al complex as a topical anticancer agent. Clinical use must be explored.

摘要

我们制备了螯合阿霉素 - 铝复合物(阿霉素 - 铝复合物)用于实验评估。将人胃癌移植到裸鼠体内,分为4组进行药物注射;1)对照组(0.9%氯化钠),2)醋酸铝组(1mg/ml),3)仅阿霉素组(1mg/ml),4)阿霉素 - 铝复合物组(阿霉素1mg/ml + 铝1mg/ml),每组0.2ml通过多次注射同时注入肿瘤周边。在第4组中通过病理观察到阿霉素在肿瘤中的长期滞留。注射后(5、7、28天)第4组阿霉素的浓度(微克/克)分别为22.3、12.6和3.5,而第3组分别为8.4、2.0和0.0(p小于0.01)。估计第4组的肿瘤重量抑制率为66.6%,第3组为21.4%,第2组仅为3%。DNA氚胸腺嘧啶摄取抑制率第4组为43.8%,第3组为21.2%,第2组为9.4%。未观察到铝螯合引起的副作用。这些结果证明了阿霉素 - 铝复合物作为局部抗癌剂的有效性。必须探索其临床应用。

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