Jenkins V K, Mayer R T, Perry R R
Invest New Drugs. 1984;2(1):19-27. doi: 10.1007/BF00173783.
The insect growth regulator diflubenzuron (DFB), which may also inhibit growth of imaginal epidermal cells in insects, was studied for antitumor activity in two mouse tumor models of epidermal origin. DFB inhibits chitin deposition, but the mechanisms by which DFB controls chitin deposition or regulates growth of insect epidermal cells are unknown. A single injection of 20 mg (800 mg/kg) of DFB into C57BL/6 mice with B16 malignant melanomas or AKR mice with skin tumors (CA 1025) induced a rapid (24 h) decrease in tumor volume in 78% and 66% of the tumors, respectively. In contrast, 85% of the melanomas and 91% of skin tumors in control mice increased in volume during the same 24-h period. Tumor volume decreased by as much as 55% for about 1% of the tumors, but the median decrease was 20% for both types of tumors. Since control tumors concommitantly increased, DFB-treated tumors decreased, relatively, to 60% of the volume of matched control tumors. After the initial volume decrease, both types of tumors resumed exponential growth resulting in an average growth curve delay, calculated for 12-14 days, of about 2.0 days. Subsequent treatment of melanomas with DFB 24 h after the initial treatment resulted in a further decrease in relative tumor volume to 40-50% of control tumor volume and a growth curve delay of 2.6 days. The most effective regimen used was 5 daily, 20-mg doses of DFB. Melanomas decreased to 40% of control tumor volume after the third injection and the mean growth curve delay was extended to 4.3 days.(ABSTRACT TRUNCATED AT 250 WORDS)
昆虫生长调节剂敌灭灵(DFB)可能还会抑制昆虫成虫表皮细胞的生长,该药剂在两种表皮起源的小鼠肿瘤模型中进行了抗肿瘤活性研究。DFB可抑制几丁质沉积,但其控制几丁质沉积或调节昆虫表皮细胞生长的机制尚不清楚。向患有B16恶性黑色素瘤的C57BL/6小鼠或患有皮肤肿瘤(CA 1025)的AKR小鼠单次注射20毫克(800毫克/千克)DFB,分别使78%和66%的肿瘤体积在24小时内迅速减小。相比之下,在同一24小时内,对照小鼠中85%的黑色素瘤和91%的皮肤肿瘤体积增大。约1%的肿瘤体积减小多达55%,但两种肿瘤类型的体积减小中位数均为20%。由于对照肿瘤同时增大,经DFB处理的肿瘤相对减小至匹配对照肿瘤体积的60%。在最初的体积减小之后,两种肿瘤类型均恢复指数生长,导致计算12 - 14天的平均生长曲线延迟约2.0天。在初始治疗后24小时用DFB对黑色素瘤进行后续治疗,导致相对肿瘤体积进一步减小至对照肿瘤体积的40 - 50%,生长曲线延迟2.6天。最有效的给药方案是每日5次,每次20毫克DFB。第三次注射后,黑色素瘤减小至对照肿瘤体积的40%,平均生长曲线延迟延长至4.3天。(摘要截断于250字)