Antitumor effect and toxicity of two new active-site-directed irreversible ornithine decarboxylase and extrahepatic arginase inhibitors

José Trujillo-Ferrara; Guadalupe Koizumi; Olga Muñnoz; Pedro Joseph-Nathan; Ricardo Yañez

doi:10.1016/0304-3835(92)90143-J

Antitumor effect and toxicity of two new active-site-directed irreversible ornithine decarboxylase and extrahepatic arginase inhibitors

José Trujillo-Ferrara, Guadalupe Koizumi, Olga Muñnoz, Pedro Joseph-Nathan, Ricardo Yañez

Escuela Superior de Medicina (ESM)

Research output: Contribution to journal › Article › peer-review

12 Scopus citations

Abstract

The irreversible ornithine decarboxylase and extrahepatic arginase inhibitors (+)-S-2-amino-5-iodoacetamidopentanoic acid (2-AIPA) and(+)-S-2-amino-6-iodoacetamido-hexanoic acid (2-AIHA) were evaluated. The LD ₅₀ tests were made in rats and mice using both compounds. Rats and mice were treated with either 2-AIPA or 2-AIHA i.p. for a period of 180 days. The treated animals showed a decrease of total serum proteins and increased ALT and AST levels. CK was also modified but inversely related to dose. Protection tests were carried out using L5178Y mouse lymphosarcoma. The mean survival time for each treated group was calculated and the percentage T C was determined. For 2-AIPA it was 170 and for 2-AIHA it was 210 at 15 mg/kg.

Original language	English
Pages (from-to)	193-197
Number of pages	5
Journal	Cancer Letters
Volume	67
Issue number	2-3
DOIs	https://doi.org/10.1016/0304-3835(92)90143-J
State	Published - 24 Dec 1992

Keywords

(+)-S-2-amino-5-iodoacetamidopentanoic acid
(+)-S-2-amino-6-iodoacetamidohexanoic acid
lymphosarcoma, toxicity, polyamines

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10.1016/0304-3835(92)90143-J

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title = "Antitumor effect and toxicity of two new active-site-directed irreversible ornithine decarboxylase and extrahepatic arginase inhibitors",

abstract = " The irreversible ornithine decarboxylase and extrahepatic arginase inhibitors (+)-S-2-amino-5-iodoacetamidopentanoic acid (2-AIPA) and(+)-S-2-amino-6-iodoacetamido-hexanoic acid (2-AIHA) were evaluated. The LD 50 tests were made in rats and mice using both compounds. Rats and mice were treated with either 2-AIPA or 2-AIHA i.p. for a period of 180 days. The treated animals showed a decrease of total serum proteins and increased ALT and AST levels. CK was also modified but inversely related to dose. Protection tests were carried out using L5178Y mouse lymphosarcoma. The mean survival time for each treated group was calculated and the percentage T C was determined. For 2-AIPA it was 170 and for 2-AIHA it was 210 at 15 mg/kg.",

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doi = "10.1016/0304-3835(92)90143-J",

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AU - Trujillo-Ferrara, José

AU - Koizumi, Guadalupe

AU - Muñnoz, Olga

AU - Joseph-Nathan, Pedro

AU - Yañez, Ricardo

PY - 1992/12/24

Y1 - 1992/12/24

N2 - The irreversible ornithine decarboxylase and extrahepatic arginase inhibitors (+)-S-2-amino-5-iodoacetamidopentanoic acid (2-AIPA) and(+)-S-2-amino-6-iodoacetamido-hexanoic acid (2-AIHA) were evaluated. The LD 50 tests were made in rats and mice using both compounds. Rats and mice were treated with either 2-AIPA or 2-AIHA i.p. for a period of 180 days. The treated animals showed a decrease of total serum proteins and increased ALT and AST levels. CK was also modified but inversely related to dose. Protection tests were carried out using L5178Y mouse lymphosarcoma. The mean survival time for each treated group was calculated and the percentage T C was determined. For 2-AIPA it was 170 and for 2-AIHA it was 210 at 15 mg/kg.

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KW - (+)-S-2-amino-5-iodoacetamidopentanoic acid

KW - (+)-S-2-amino-6-iodoacetamidohexanoic acid

KW - lymphosarcoma, toxicity, polyamines

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DO - 10.1016/0304-3835(92)90143-J

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SN - 0304-3835

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JO - Cancer Letters

JF - Cancer Letters

IS - 2-3

ER -

Antitumor effect and toxicity of two new active-site-directed irreversible ornithine decarboxylase and extrahepatic arginase inhibitors

Abstract

Keywords

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