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为探讨佛波酯对胃癌细胞肿瘤坏死因子(TNF)受体的调变机制。以标记的肿瘤坏死因子突变体为配体,用放射配体结合分析法和MTT比色法研究了佛波酯对TNF受体的调节以及对肿瘤坏死因子突变体(TNF-m)细胞毒效应的影响。结果表明:佛波酯可导致胃癌细胞(SGC7901)表面TNF受体数显著减少(由0.56×10-11nmol/细胞,下降到0.25×10-11nmol/细胞,P<0.01),而对受体的亲和力无影响;佛波酯不影响TNF-m的内化率、降解率和解离率,佛波酯也不改变胞浆TNF受体数目;佛波酯处理后的SGC7901细胞对肿瘤坏死因子突变体(TNF-m)的耐受性显著增强。去除佛波酯后12h,TNF受体可恢复80%,其恢复率与胰酶处理组相似。从而提示:佛波酯可能通过清除膜TNF受体而使TNF受体下调并抑制TNF-m的细胞毒效应
To investigate the modulation mechanism of phorbol ester on tumor necrosis factor (TNF) receptor in gastric cancer cells. The tumor tumour necrosis factor mutants were used as ligands. The modulation of phorbol esters on TNF receptors and the cytotoxicity of tumor necrosis factor mutant (TNF-m) were studied by radioligand binding assay and MTT colorimetry. Impact. The results showed that phorbol ester can significantly reduce the number of TNF receptors on gastric cancer cells (SGC7901) (from 0.56×10-11 nmol/cell to 0.25×10-11 nmol/cell, P<0.01). No influence on receptor affinity; Phorbol ester does not affect the internalization rate, degradation rate, and dissociation rate of TNF-m, and phorbol ester does not change the number of cytoplasmic TNF receptors; SGB7901 cells treated with phorbol ester Tolerance to tumor necrosis factor mutants (TNF-m) was significantly enhanced. After 12 hours of phorbol ester removal, TNF receptors recovered 80%, and the recovery rate was similar to that of the pancreatic enzyme treatment group. This suggests that phorbol esters may downregulate TNF receptors and suppress the cytotoxic effects of TNF-m by eliminating membrane TNF receptors.