Anticancer prodrugs of butyric acid and formaldehyde protect against doxorubicin-induced cardiotoxicity

Rephaeli, A; Waks-Yona, S; Nudelman, A; Tarasenko, I; Tarasenko, N; Phillips, DR; Cutts, SM; Kessler-Icekson, G

HERO ID

1454193

Reference Type

Journal Article

Year

2007

Language

English

PMID

17473824

HERO ID 1454193
In Press No
Year 2007
Title Anticancer prodrugs of butyric acid and formaldehyde protect against doxorubicin-induced cardiotoxicity
Authors Rephaeli, A; Waks-Yona, S; Nudelman, A; Tarasenko, I; Tarasenko, N; Phillips, DR; Cutts, SM; Kessler-Icekson, G
Journal British Journal of Cancer
Volume 96
Issue 11
Page Numbers 1667-1674
Abstract Formaldehyde has been previously shown to play a dominant role in promoting synergy between doxorubicin (Dox) and formaldehyde-releasing butyric acid (BA) prodrugs in killing cancer cells. In this work, we report that these prodrugs also protect neonatal rat cardiomyocytes and adult mice against toxicity elicited by Dox. In cardiomyocytes treated with Dox, the formaldehyde releasing prodrugs butyroyloxymethyl diethylphosphate (AN-7) and butyroyloxymethyl butyrate (AN-1), but not the corresponding acetaldehyde-releasing butyroyloxydiethyl phosphate (AN-88) or butyroyloxyethyl butyrate (AN-11), reduced lactate dehydrogenase leakage, prevented loss of mitochondrial membrane potential (DeltaPsim) and attenuated upregulation of the proapoptotic gene Bax. In Dox-treated mice, AN-7 but not AN-88 attenuated weight-loss and mortality, and increase in serum lactate dehydrogenase. These findings show that BA prodrugs that release formaldehyde and augment Dox anticancer activity also protect against Dox cardiotoxicity. Based on these observations, clinical applications of these prodrugs for patients treated with Dox warrant further investigation.
Doi 10.1038/sj.bjc.6603781
Pmid 17473824
Wosid WOS:000246816200008
Url https://www.proquest.com/scholarly-journals/anticancer-prodrugs-butyric-acid-formaldehyde/docview/70550101/se-2
Is Certified Translation No
Dupe Override No
Comments Source: Web of Science WOS:000246816200008
Is Public Yes
Language Text English
Keyword doxorubicin; cardiomyocytes; formaldehyde; prodrugs; histone acetylation