Liver Cancer
Copyright ©The Author(s) 2003. Published by Baishideng Publishing Group Inc. All rights reserved.
World J Gastroenterol. Aug 15, 2003; 9(8): 1675-1678
Published online Aug 15, 2003. doi: 10.3748/wjg.v9.i8.1675
Study on the possibility of insulin as a carrier of IUdR for hepatocellular carcinoma-targeted therapy
Xiao-Hong Ou, An-Ren Kuang, Xian Peng, Yu-Guo Zhong
Xiao-Hong Ou, An-Ren Kuang, Department of Nuclear Medicine, West China Hospital of Sichuan University, Sichuan Province, China
Xian Peng, Yu-Guo Zhong, Department of Pharmaceutical, Sichuan University, Sichuan Province, China
Author contributions: All authors contributed equally to the work.
Supported by The National Natural Science Foundation of China, Grant No 30270415
Correspondence to: An-Ren Kuang, Department of Nuclear Medicine, West China Hospital of Sichuan University, Chengdu, China. ouxiaohong2002@xinhuanet.com
Telephone: +86-28-85422696 Fax: +86-28-85422696
Received: January 4, 2003
Revised: January 16, 2003
Accepted: February 17, 2003
Published online: August 15, 2003
Abstract

AIM: To evaluate the possibility of using insulin as a carrier for carcinoma-targeted therapy mediated by receptor, and to investigate the expression of insulin receptor in human hepatocellular carcinoma and the receptor binding characteristics of insulin-IUdR (iododeoxyuridine).

METHODS: IUdR was covalently conjugated to insulin. Receptor binding assays of 125I-insulin to human hepatocellular carcinoma and its adjacent tissue were performed. Competitive displacements of 125I-insulin by insulin and insulin-IUdR to bind to insulin receptor were respectively carried out. Statistical comparisons between the means were made with paired t-test at a confidence level of 95%.

RESULTS: The data indicated that there were high- and low- affinity binding sites for 125I-insulin on both hepatocellular carcinoma and its adjacent tissue. Hepatocellular carcinoma had a significantly higher Bmax for high affinity binding site than its adjacent liver tissue (P < 0.05, t = 2.275). Insulin-IUdR competed as effectively as insulin with 125I-insulin for binding to insulin receptor. Values of IC501, C502, KI1 and KI2 for insulin-IUdR were 11.50 ± 2.83 nmol·L-1, 19.35 ± 5.11 nmol·L-1, 11.26 ± 2.65 nmol·L-1 and 19.30 ± 5.02 nmol·L-1 respectively, and for insulin were 5.01 ± 1.24 nmol·L-1,17.75 ± 4.86 nmol·L-1, 4.85 ± 1.12 nmol·L-1 and 17.69 ± 4.81 nmol·L-1, respectively. Values of IC501 and KI1 for insulin-IUdR were significantly higher than that for insulin (P < 0.01, t = 4.537 and 4.813).

CONCLUSION: It is possible to use insulin as a carrier for carcinoma-targeted therapy mediated by receptor.

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