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Dependence of Anticancer Activity of Camptothecins on Maintaining Their Lactone Function
Author(s) -
GIOVANELLA B. C.,
HARRIS N.,
MENDOZA J.,
CAO Z.,
LIEHR J.,
STEHLIN J. S.
Publication year - 2000
Publication title -
annals of the new york academy of sciences
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.712
H-Index - 248
eISSN - 1749-6632
pISSN - 0077-8923
DOI - 10.1111/j.1749-6632.2000.tb07022.x
Subject(s) - chemistry , human plasma , lactone , human serum albumin , function (biology) , albumin , stereochemistry , biochemistry , chromatography , biology , genetics
A bstract : Camptothecins contain a lactone ring that exists in the closed form below ph 7. Above 7, the open (CPT + ) and the closed (CPT) form coexist in a 50–50 ratio in mouse plasma and in a 90–10 ratio in human plasma due to the high affinity of human serum albumin (HSA) for CPT + . CPT + is much less toxic than CPT and it is excreted much faster. In complete RPMI 1640 culture medium, the equilibrium CPT + ‐CPT is 50–50. If 4% HSA is added, it moves to 90–10 modeling for the human physiological situation.