Evaluation of limonoids against the murine p388 lymphocytic leukemia cell line

George Pettit; Derek H R Barton; Cherry L. Herald; Judith Polonsky; Jean M. Schmidt; Joseph D. Connolly

doi:10.1021/np50027a015

Evaluation of limonoids against the murine p388 lymphocytic leukemia cell line

George Pettit, Derek H R Barton, Cherry L. Herald, Judith Polonsky, Jean M. Schmidt, Joseph D. Connolly

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Abstract

A structure/activity study of selected limonoids from two plant families (Meliaceae and Rutaceae) of the Rutales order against the murine P-388 lymphocytic leukemia system was undertaken. The presence of both a 19-28 lactol and a 14,15(i-epoxide group was found especially important for pronounced inhibition of the PS in vitro cell line. Substitution of an A-ring α,β-unsaturated ketone (3-oxo- 1-ene) for the lactol led to diminished activity, while reduction of the olefin caused complete loss of activity. At the dose levels employed, even very good PS in vitro inhibition was not translated into PS in vivo antineoplastic effects.

Original language	English (US)
Pages (from-to)	379-390
Number of pages	12
Journal	Journal of Natural Products
Volume	46
Issue number	3
DOIs	https://doi.org/10.1021/np50027a015
State	Published - May 1983

ASJC Scopus subject areas

Analytical Chemistry
Molecular Medicine
Pharmacology
Pharmaceutical Science
Drug Discovery
Complementary and alternative medicine
Organic Chemistry

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abstract = "A structure/activity study of selected limonoids from two plant families (Meliaceae and Rutaceae) of the Rutales order against the murine P-388 lymphocytic leukemia system was undertaken. The presence of both a 19-28 lactol and a 14,15(i-epoxide group was found especially important for pronounced inhibition of the PS in vitro cell line. Substitution of an A-ring α,β-unsaturated ketone (3-oxo- 1-ene) for the lactol led to diminished activity, while reduction of the olefin caused complete loss of activity. At the dose levels employed, even very good PS in vitro inhibition was not translated into PS in vivo antineoplastic effects.",

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T1 - Evaluation of limonoids against the murine p388 lymphocytic leukemia cell line

AU - Pettit, George

AU - Barton, Derek H R

AU - Herald, Cherry L.

AU - Polonsky, Judith

AU - Schmidt, Jean M.

AU - Connolly, Joseph D.

PY - 1983/5

Y1 - 1983/5

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AB - A structure/activity study of selected limonoids from two plant families (Meliaceae and Rutaceae) of the Rutales order against the murine P-388 lymphocytic leukemia system was undertaken. The presence of both a 19-28 lactol and a 14,15(i-epoxide group was found especially important for pronounced inhibition of the PS in vitro cell line. Substitution of an A-ring α,β-unsaturated ketone (3-oxo- 1-ene) for the lactol led to diminished activity, while reduction of the olefin caused complete loss of activity. At the dose levels employed, even very good PS in vitro inhibition was not translated into PS in vivo antineoplastic effects.

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Evaluation of limonoids against the murine p388 lymphocytic leukemia cell line

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