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在体外和体内药物敏感性试验中,人结肠直肠癌对HCFU比5-氟尿嘧啶和替加氟更敏感。

[Human colorectal carcinoma is more sensitive to HCFU than 5-FU and tegafur in in vitro and in vivo drug sensitivity tests].

作者信息

Kusumoto T, Maehara Y, Anai H, Kusumoto H, Miyamoto K, Fukuchi K, Sugimachi K

机构信息

Second Dept. of Surgery, Faculty of Medicine, Kyushu University.

出版信息

Gan To Kagaku Ryoho. 1988 Feb;15(2):257-61.

PMID:3124767
Abstract

The sensitivity of human colorectal cancer to 5-fluorouracil (5-FU) and its derivatives: 1-(tetrahydro-2-furyl)-5-FU (tegafur) and 1-hexylcarbamoyl-5-FU (HCFU) was determined by in vitro succinate dehydrogenase inhibition (SDI) test and in vivo subrenal capsule (SRC) assay. Using the SDI test with 25 colorectal cancer specimens, the succinate dehydrogenase (SD) activity decreased to 73.6 +/- 17.8% for 5-FU-treated cells and 37.2 +/- 17.0% for HCFU-treated cells, compared to that of control cells. The chemosensitivity-positive rates were 16% for 5-FU and 68% for HCFU. Using the SRC assay with 7 colorectal cancer specimens, the relative variation of tumor size, which was calculated by delta TS/TS0 = (TS6-TS0)/TS0 X 100 (%), decreased to -12.6 +/- 10.1% for 5-FU, -14.9 +/- 12.4% for tegafur and -23.9 +/- 14.2% for HCFU, and the inhibition of tumor growth following exposure to HCFU was evident. The chemosensitivity-positive rates were 49% for 5-FU, 57% for tegafur and 71% for HCFU. Our results show that HCFU is more effective to colorectal cancer than 5-FU and FT-207, and the chemosensitivity test of HCFU will be useful in determining the effective drug for the treatment of colorectal cancer.

摘要

通过体外琥珀酸脱氢酶抑制(SDI)试验和体内肾包膜下(SRC)测定,确定了人类结直肠癌对5-氟尿嘧啶(5-FU)及其衍生物1-(四氢-2-呋喃基)-5-FU(替加氟)和1-己基氨基甲酰基-5-FU(HCFU)的敏感性。使用SDI试验检测25份结直肠癌标本,与对照细胞相比,5-FU处理的细胞琥珀酸脱氢酶(SD)活性降至73.6±17.8%,HCFU处理的细胞降至37.2±17.0%。5-FU的化学敏感性阳性率为16%,HCFU为68%。使用SRC测定检测7份结直肠癌标本,通过δTS/TS0 =(TS6 - TS0)/TS0×100(%)计算的肿瘤大小相对变化,5-FU降至-12.6±10.1%,替加氟降至-14.9±12.4%,HCFU降至-23.9±14.2%,暴露于HCFU后肿瘤生长的抑制作用明显。5-FU的化学敏感性阳性率为49%,替加氟为57%,HCFU为71%。我们的结果表明,HCFU对结直肠癌比5-FU和替加氟更有效且HCFU化疗敏感性试验将有助于确定治疗结直肠癌的有效药物。

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