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Anti-tumour activity and toxicity of the new prodrug 9-aminocamptothecin glucuronide (9ACG) in mice.

Prijovich ZM, Chen BM, Leu YL, Chern JW, Roffler SR - Br. J. Cancer (2002)

Bottom Line: Cancer chemotherapy is limited by the modest therapeutic index of most antineoplastic drugs.Beta-glucuronidase activated 9-aminocamptothecin glucuronide to produce similar cell killing as 9-aminocamptothecin or topotecan.The in vivo toxicity of 9-aminocamptothecin glucuronide in BALB/c mice was dose-, route-, sex- and age-dependent. 9-aminocamptothecin glucuronide was significantly less toxic to female than to male mice but the difference decreased with age. 9-aminocamptothecin glucuronide and 9-aminocamptothecin produced similar inhibition (approximately 80%) of LS174T human colorectal carcinoma tumours. 9-aminocamptothecin glucuronide cured a high percentage of CL1-5 human lung cancer xenografts with efficacy that was similar to or greater than 9-aminocamptothecin, irinotecan and topotecan.

View Article: PubMed Central - PubMed

Affiliation: Institute of Biomedical Sciences, Academia Sinica, Taipei, Taiwan 115, and ICTM, Center for Chemistry, Belgrade, Yugoslavia.

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Anti-tumour activity of 9ACG against LS174T xenografts. (A, B) BALB/c nu/nu mice bearing LS174T tumours were i.v. injected with PBS, i.v. injected with 50 mg kg−1 9ACG or s.c. injected with 3 mg kg−1 9AC in Lipiodol on day 10. Mean tumour sizes (A) and weights (B) of six mice relative to mean values at the initiation of therapy (day 10) are shown. The mean size of drug-treated (9AC and 9ACG) tumours was significantly (P⩽0.05) smaller than control tumours after day 13. (C) BALB/c nu/nu mice bearing LS174T tumours were untreated, i.v. injected with 50 mg kg−1 9ACG or s.c. injected with 5 mg kg−1 9AC in Lipiodol on day 10, or i.v. injected with 10 mg kg−1 9ACG or irinotecan on days 10, 12 and 14. Results represent mean tumour size of 7–8 mice relative to mean tumour size on day 10. The mean size of drug-treated (9AC, 9ACG and irinotecan) tumours was significantly (P⩽0.05) smaller than control tumours after day 12. Bars, s.e.
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fig3: Anti-tumour activity of 9ACG against LS174T xenografts. (A, B) BALB/c nu/nu mice bearing LS174T tumours were i.v. injected with PBS, i.v. injected with 50 mg kg−1 9ACG or s.c. injected with 3 mg kg−1 9AC in Lipiodol on day 10. Mean tumour sizes (A) and weights (B) of six mice relative to mean values at the initiation of therapy (day 10) are shown. The mean size of drug-treated (9AC and 9ACG) tumours was significantly (P⩽0.05) smaller than control tumours after day 13. (C) BALB/c nu/nu mice bearing LS174T tumours were untreated, i.v. injected with 50 mg kg−1 9ACG or s.c. injected with 5 mg kg−1 9AC in Lipiodol on day 10, or i.v. injected with 10 mg kg−1 9ACG or irinotecan on days 10, 12 and 14. Results represent mean tumour size of 7–8 mice relative to mean tumour size on day 10. The mean size of drug-treated (9AC, 9ACG and irinotecan) tumours was significantly (P⩽0.05) smaller than control tumours after day 12. Bars, s.e.

Mentions: BALB/c nu/nu mice bearing established LS174T tumours were i.v. injected with 50 mg kg−1 9ACG in PBS or s.c. injected with 3 mg kg−1 9AC as a suspension in lipiodol. Both 9ACG and 9AC inhibited LS174T tumour growth by about 80% (Figure 3AFigure 3


Anti-tumour activity and toxicity of the new prodrug 9-aminocamptothecin glucuronide (9ACG) in mice.

Prijovich ZM, Chen BM, Leu YL, Chern JW, Roffler SR - Br. J. Cancer (2002)

Anti-tumour activity of 9ACG against LS174T xenografts. (A, B) BALB/c nu/nu mice bearing LS174T tumours were i.v. injected with PBS, i.v. injected with 50 mg kg−1 9ACG or s.c. injected with 3 mg kg−1 9AC in Lipiodol on day 10. Mean tumour sizes (A) and weights (B) of six mice relative to mean values at the initiation of therapy (day 10) are shown. The mean size of drug-treated (9AC and 9ACG) tumours was significantly (P⩽0.05) smaller than control tumours after day 13. (C) BALB/c nu/nu mice bearing LS174T tumours were untreated, i.v. injected with 50 mg kg−1 9ACG or s.c. injected with 5 mg kg−1 9AC in Lipiodol on day 10, or i.v. injected with 10 mg kg−1 9ACG or irinotecan on days 10, 12 and 14. Results represent mean tumour size of 7–8 mice relative to mean tumour size on day 10. The mean size of drug-treated (9AC, 9ACG and irinotecan) tumours was significantly (P⩽0.05) smaller than control tumours after day 12. Bars, s.e.
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Related In: Results  -  Collection

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fig3: Anti-tumour activity of 9ACG against LS174T xenografts. (A, B) BALB/c nu/nu mice bearing LS174T tumours were i.v. injected with PBS, i.v. injected with 50 mg kg−1 9ACG or s.c. injected with 3 mg kg−1 9AC in Lipiodol on day 10. Mean tumour sizes (A) and weights (B) of six mice relative to mean values at the initiation of therapy (day 10) are shown. The mean size of drug-treated (9AC and 9ACG) tumours was significantly (P⩽0.05) smaller than control tumours after day 13. (C) BALB/c nu/nu mice bearing LS174T tumours were untreated, i.v. injected with 50 mg kg−1 9ACG or s.c. injected with 5 mg kg−1 9AC in Lipiodol on day 10, or i.v. injected with 10 mg kg−1 9ACG or irinotecan on days 10, 12 and 14. Results represent mean tumour size of 7–8 mice relative to mean tumour size on day 10. The mean size of drug-treated (9AC, 9ACG and irinotecan) tumours was significantly (P⩽0.05) smaller than control tumours after day 12. Bars, s.e.
Mentions: BALB/c nu/nu mice bearing established LS174T tumours were i.v. injected with 50 mg kg−1 9ACG in PBS or s.c. injected with 3 mg kg−1 9AC as a suspension in lipiodol. Both 9ACG and 9AC inhibited LS174T tumour growth by about 80% (Figure 3AFigure 3

Bottom Line: Cancer chemotherapy is limited by the modest therapeutic index of most antineoplastic drugs.Beta-glucuronidase activated 9-aminocamptothecin glucuronide to produce similar cell killing as 9-aminocamptothecin or topotecan.The in vivo toxicity of 9-aminocamptothecin glucuronide in BALB/c mice was dose-, route-, sex- and age-dependent. 9-aminocamptothecin glucuronide was significantly less toxic to female than to male mice but the difference decreased with age. 9-aminocamptothecin glucuronide and 9-aminocamptothecin produced similar inhibition (approximately 80%) of LS174T human colorectal carcinoma tumours. 9-aminocamptothecin glucuronide cured a high percentage of CL1-5 human lung cancer xenografts with efficacy that was similar to or greater than 9-aminocamptothecin, irinotecan and topotecan.

View Article: PubMed Central - PubMed

Affiliation: Institute of Biomedical Sciences, Academia Sinica, Taipei, Taiwan 115, and ICTM, Center for Chemistry, Belgrade, Yugoslavia.

Show MeSH
Related in: MedlinePlus