一种新型苯二氮䓬衍生物对实验性恶性黑色素瘤的作用
[Effect of a new benzodiazepine derivative on experimental malignant melanomas].
作者信息
Werner W, Wohlrabe K, Fichtner I, Wohlrab W
出版信息
Arch Geschwulstforsch. 1987;57(1):17-23.
It was found, that (+)cis-3,4-dimethoxy-10,11-dimethyl-6,6aR,7,8,13, 13aS-hexahydro-[I]-benzopyrano-[4,3-b]-1,5-benzodiazepine (ZIMET 54/79) increased the life span (ILS) of C57BL/6/Jena mice suffering from transplanted B16 melanoma (ip.) by 57% (9 times ip. 250 mg/kg) and 90% (9 times ip. 500 mg/kg) respectively. In B6D2F1/Bln mice with transplanted B16 melanoma there was no ILS registered when a dose of 100-500 mg/kg was applied (ip. and p.o.). Using the Harding Passey melanoma (B6D2F1/Bln mice) only 59% tumour volume inhibition (500 mg/kg) without ILS was obtained. Finally ZIMET 54/79 tested on AMel 3 hamster melanoma (strain Z3) decreased the mean tumour volume by 72% (125 mg/kg).
研究发现，（+）顺式-3,4-二甲氧基-10,11-二甲基-6,6aR,7,8,13,13aS-六氢-[I]-苯并吡喃并-[4,3-b]-1,5-苯并二氮杂䓬（ZIMET 54/79）可使患有移植性B16黑色素瘤（腹腔注射）的C57BL/6/Jena小鼠的寿命延长（ILS）分别提高57%（腹腔注射9次，每次250 mg/kg）和90%（腹腔注射9次，每次500 mg/kg）。在移植了B16黑色素瘤的B6D2F1/Bln小鼠中，当给予100 - 500 mg/kg剂量（腹腔注射和口服）时，未观察到寿命延长。使用哈丁·帕西黑色素瘤（B6D2F1/Bln小鼠），仅获得了59%的肿瘤体积抑制率（500 mg/kg），且未延长寿命。最后，在AMel 3仓鼠黑色素瘤（Z3品系）上测试的ZIMET 54/79使平均肿瘤体积减少了72%（125 mg/kg）。
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