Zervos E E, Norman J G, Gower W R, Franz M G, Rosemurgy A S
Department of Surgery, University of South Florida, Tampa 33601, USA.
J Surg Res. 1997 May;69(2):367-71. doi: 10.1006/jsre.1997.5086.
Matrix metalloproteinases (MMP) are enzymes responsible for extracellular matrix degradation, a critical component influencing the growth and metastatic potential of cancer. The purpose of this study was to determine the in vitro effects of MMP inhibition on human pancreatic cancer cells and to document its effect on cancer growth in vivo. The effect of MMP inhibition was determined using the MMP inhibitor BB-94 and a moderately differentiated pancreatic cancer cell line (HPAC). In vitro, a dose response curve was generated over 5 days utilizing the MTT [3(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay. In vivo, using an established orthotopic model for pancreatic cancer (LD100 = 80 days), 22 nude mice with orthotopic tumors (30 were implanted) received either BB-94 or vehicle beginning 4 days prior to implantation and continuing to death or sacrifice on Day 70. Mice were weighted weekly. At death/sacrifice, tumors were weighted, volume determined, and metastases/ distant spread documented. In vitro, BB-94 had little effect on HPAC proliferation at 40 ng/ml but achieved progressively greater to near complete inhibition at doses up to 4000 ng/ml while maintaining cell viability. In vivo, BB-94 significantly increased length of survival (69 +/- 0.1 days vs. 56 +/- 3.1 days) and necropsy weight (25.7 +/- 1.67 g vs. 19.8 +/- 1.14 g) while decreasing metastatic rate (1 vs. 20) and tumor size (0.14 +/- 0.02 g vs. 0.65 +/- 0.1 g). MMP inhibition limits HPAC proliferation in a dose-dependent fashion without direct cytotoxic effects in vitro. Mice harboring orthotopic tumors treated with BB-94 demonstrated significant reductions in tumor weight, volume, and metastases which corresponded to increased animal weight and prolonged survival.
基质金属蛋白酶(MMP)是负责细胞外基质降解的酶,细胞外基质降解是影响癌症生长和转移潜能的关键因素。本研究的目的是确定MMP抑制对人胰腺癌细胞的体外作用,并记录其对体内癌症生长的影响。使用MMP抑制剂BB - 94和中度分化的胰腺癌细胞系(HPAC)来确定MMP抑制的效果。在体外,利用MTT [3(4,5 - 二甲基噻唑 - 2 - 基)- 2,5 - 二苯基四氮唑溴盐] 测定法在5天内生成剂量反应曲线。在体内,使用已建立的胰腺癌原位模型(LD100 = 80天),22只患有原位肿瘤的裸鼠(共植入30只)在植入前4天开始接受BB - 94或赋形剂治疗,并持续至第70天死亡或处死。每周对小鼠称重。在死亡/处死时,对肿瘤称重、测定体积,并记录转移/远处扩散情况。在体外,40 ng/ml的BB - 94对HPAC增殖几乎没有影响,但在高达4000 ng/ml的剂量下能逐渐产生更大的抑制作用,直至接近完全抑制,同时保持细胞活力。在体内,BB - 94显著延长了生存时间(69±0.1天对56±3.1天)和尸检时的体重(25.7±1.67 g对19.8±1.14 g),同时降低了转移率(1对20)和肿瘤大小(0.14±0.02 g对0.65±0.1 g)。MMP抑制在体外以剂量依赖的方式限制HPAC增殖,且无直接细胞毒性作用。用BB - 94治疗的患有原位肿瘤的小鼠表现出肿瘤重量、体积和转移的显著减少,这与动物体重增加和生存期延长相对应。