Antitumor effect on SN-38, active form of CPT-11, on human colorectal cancer cell line

K. Aiba, S. Funakoshi, N. Mizunuma, N. Dobashi, A. Hirano, M. Sano, Y. Kuraishi, M. Kamada, N. Ohno, Yoshikazu Sugimoto, T. Tsuruo, H. Shibata, N. Horikoshi

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

The in vitro sensitivity testing for four human colorectal cancer cell lines to seven chemotherapeutic drugs including CPT-11, derivative of camptothecine, and its active form SN-38 were determined. MTT assay revealed that SN-38 was the most active for all four cell lines tested and its IC50's were very close to its clinically achievable plasma concentration. Relationship between exposure time and cytocidal effect of SN-38 was also investigated using MTT assay, topoisomerase-I (Topo-I) immunoblot analysis and DNA relaxation assay, showing that IC50 value, Topo-I protein and Topo-I activity were decreased soon after the administration of SN-38 and reached the plateau level at 24 hours. We conclude that SN-38 is very potent for colorectal cancer and the optimal schedule of CPT-11 can be the more continuous form of administration capable of as long as 24 hours exposure of its active metabolite, SN-38.

Original languageEnglish
Pages (from-to)1601-1606
Number of pages6
JournalJapanese Journal of Cancer and Chemotherapy
Volume21
Issue number10
Publication statusPublished - 1994
Externally publishedYes

Fingerprint

irinotecan
Colorectal Neoplasms
Cell Line
Type I DNA Topoisomerase
Inhibitory Concentration 50
Camptothecin

Keywords

  • CPT-11
  • human colorectal cancer cell line
  • SN-38
  • topoisomerase-I

ASJC Scopus subject areas

  • Cancer Research
  • Pharmacology

Cite this

Aiba, K., Funakoshi, S., Mizunuma, N., Dobashi, N., Hirano, A., Sano, M., ... Horikoshi, N. (1994). Antitumor effect on SN-38, active form of CPT-11, on human colorectal cancer cell line. Japanese Journal of Cancer and Chemotherapy, 21(10), 1601-1606.

Antitumor effect on SN-38, active form of CPT-11, on human colorectal cancer cell line. / Aiba, K.; Funakoshi, S.; Mizunuma, N.; Dobashi, N.; Hirano, A.; Sano, M.; Kuraishi, Y.; Kamada, M.; Ohno, N.; Sugimoto, Yoshikazu; Tsuruo, T.; Shibata, H.; Horikoshi, N.

In: Japanese Journal of Cancer and Chemotherapy, Vol. 21, No. 10, 1994, p. 1601-1606.

Research output: Contribution to journalArticle

Aiba, K, Funakoshi, S, Mizunuma, N, Dobashi, N, Hirano, A, Sano, M, Kuraishi, Y, Kamada, M, Ohno, N, Sugimoto, Y, Tsuruo, T, Shibata, H & Horikoshi, N 1994, 'Antitumor effect on SN-38, active form of CPT-11, on human colorectal cancer cell line', Japanese Journal of Cancer and Chemotherapy, vol. 21, no. 10, pp. 1601-1606.
Aiba K, Funakoshi S, Mizunuma N, Dobashi N, Hirano A, Sano M et al. Antitumor effect on SN-38, active form of CPT-11, on human colorectal cancer cell line. Japanese Journal of Cancer and Chemotherapy. 1994;21(10):1601-1606.
Aiba, K. ; Funakoshi, S. ; Mizunuma, N. ; Dobashi, N. ; Hirano, A. ; Sano, M. ; Kuraishi, Y. ; Kamada, M. ; Ohno, N. ; Sugimoto, Yoshikazu ; Tsuruo, T. ; Shibata, H. ; Horikoshi, N. / Antitumor effect on SN-38, active form of CPT-11, on human colorectal cancer cell line. In: Japanese Journal of Cancer and Chemotherapy. 1994 ; Vol. 21, No. 10. pp. 1601-1606.
@article{5d624d576e044ed9a2a72c97c1fef9c1,
title = "Antitumor effect on SN-38, active form of CPT-11, on human colorectal cancer cell line",
abstract = "The in vitro sensitivity testing for four human colorectal cancer cell lines to seven chemotherapeutic drugs including CPT-11, derivative of camptothecine, and its active form SN-38 were determined. MTT assay revealed that SN-38 was the most active for all four cell lines tested and its IC50's were very close to its clinically achievable plasma concentration. Relationship between exposure time and cytocidal effect of SN-38 was also investigated using MTT assay, topoisomerase-I (Topo-I) immunoblot analysis and DNA relaxation assay, showing that IC50 value, Topo-I protein and Topo-I activity were decreased soon after the administration of SN-38 and reached the plateau level at 24 hours. We conclude that SN-38 is very potent for colorectal cancer and the optimal schedule of CPT-11 can be the more continuous form of administration capable of as long as 24 hours exposure of its active metabolite, SN-38.",
keywords = "CPT-11, human colorectal cancer cell line, SN-38, topoisomerase-I",
author = "K. Aiba and S. Funakoshi and N. Mizunuma and N. Dobashi and A. Hirano and M. Sano and Y. Kuraishi and M. Kamada and N. Ohno and Yoshikazu Sugimoto and T. Tsuruo and H. Shibata and N. Horikoshi",
year = "1994",
language = "English",
volume = "21",
pages = "1601--1606",
journal = "Japanese Journal of Cancer and Chemotherapy",
issn = "0385-0684",
publisher = "Japanese Journal of Cancer and Chemotherapy Publishers Inc.",
number = "10",

}

TY - JOUR

T1 - Antitumor effect on SN-38, active form of CPT-11, on human colorectal cancer cell line

AU - Aiba, K.

AU - Funakoshi, S.

AU - Mizunuma, N.

AU - Dobashi, N.

AU - Hirano, A.

AU - Sano, M.

AU - Kuraishi, Y.

AU - Kamada, M.

AU - Ohno, N.

AU - Sugimoto, Yoshikazu

AU - Tsuruo, T.

AU - Shibata, H.

AU - Horikoshi, N.

PY - 1994

Y1 - 1994

N2 - The in vitro sensitivity testing for four human colorectal cancer cell lines to seven chemotherapeutic drugs including CPT-11, derivative of camptothecine, and its active form SN-38 were determined. MTT assay revealed that SN-38 was the most active for all four cell lines tested and its IC50's were very close to its clinically achievable plasma concentration. Relationship between exposure time and cytocidal effect of SN-38 was also investigated using MTT assay, topoisomerase-I (Topo-I) immunoblot analysis and DNA relaxation assay, showing that IC50 value, Topo-I protein and Topo-I activity were decreased soon after the administration of SN-38 and reached the plateau level at 24 hours. We conclude that SN-38 is very potent for colorectal cancer and the optimal schedule of CPT-11 can be the more continuous form of administration capable of as long as 24 hours exposure of its active metabolite, SN-38.

AB - The in vitro sensitivity testing for four human colorectal cancer cell lines to seven chemotherapeutic drugs including CPT-11, derivative of camptothecine, and its active form SN-38 were determined. MTT assay revealed that SN-38 was the most active for all four cell lines tested and its IC50's were very close to its clinically achievable plasma concentration. Relationship between exposure time and cytocidal effect of SN-38 was also investigated using MTT assay, topoisomerase-I (Topo-I) immunoblot analysis and DNA relaxation assay, showing that IC50 value, Topo-I protein and Topo-I activity were decreased soon after the administration of SN-38 and reached the plateau level at 24 hours. We conclude that SN-38 is very potent for colorectal cancer and the optimal schedule of CPT-11 can be the more continuous form of administration capable of as long as 24 hours exposure of its active metabolite, SN-38.

KW - CPT-11

KW - human colorectal cancer cell line

KW - SN-38

KW - topoisomerase-I

UR - http://www.scopus.com/inward/record.url?scp=0028075081&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0028075081&partnerID=8YFLogxK

M3 - Article

C2 - 8060134

AN - SCOPUS:0028075081

VL - 21

SP - 1601

EP - 1606

JO - Japanese Journal of Cancer and Chemotherapy

JF - Japanese Journal of Cancer and Chemotherapy

SN - 0385-0684

IS - 10

ER -