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@article{571529,
author = {Forejtníková, Hana and Lunerová, Kamila and Kubínová, Renata and Jankovská, Dagmar and Marek, Radek and Kareš, Radovan and Suchý, Václav and Vondráček, Jan and Machala, Miroslav},
article_location = {Amsterdam},
article_number = {1},
keywords = {chalcone; dihydrochalcone; toxic; chemoprotective; in vitro},
language = {eng},
issn = {0300-483X},
journal = {Toxicology},
title = {Chemoprotective and toxic potentials of synthetic and natural chalcones and dihydrochalcones in vitro},
url = {http://www.sciencedirect.com/science?_ob=JournalURL&_cdi=5175&_auth=y&_acct=C000045159&_version=1&_urlVersion=0&_userid=835458&md5=160d52ffea677d79bea5f26abc26f23c},
volume = {208},
year = {2005}
}
TY - JOUR
ID - 571529
AU - Forejtníková, Hana - Lunerová, Kamila - Kubínová, Renata - Jankovská, Dagmar - Marek, Radek - Kareš, Radovan - Suchý, Václav - Vondráček, Jan - Machala, Miroslav
PY - 2005
TI - Chemoprotective and toxic potentials of synthetic and natural chalcones and dihydrochalcones in vitro
JF - Toxicology
VL - 208
IS - 1
SP - 81-93
EP - 81-93
PB - Elsevier
SN - 0300483X
KW - chalcone
KW - dihydrochalcone
KW - toxic
KW - chemoprotective
KW - in vitro
UR - http://www.sciencedirect.com/science?_ob=JournalURL&_cdi=5175&_auth=y&_acct=C000045159&_version=1&_urlVersion=0&_userid=835458&md5=160d52ffea677d79bea5f26abc26f23c
N2 - Cytochrome P4501A activity, oxidative stress and inhibition of gap junctional intercellular communication (GJIC) are involved in metabolic activation of promutagens and tumor-promoting activity of various xenobiotics, and their prevention is considered to be an important characteristic of chemoprotective compounds. In this study, a series of 31 chalcones and their corresponding dihydroderivatives, substituted in 2,2_-, 3,3_-, 4- or 4_-position by hydroxyl or methoxy group, were tested for their ability to inhibit Fe(II)/NADPH-enhanced lipid peroxidation and cytochrome P4501A-dependent 7-cethoxyresorufin-O-deethylase (EROD) activity in rat hepatic microsomes. Effects of the compounds on GJIC were determined in rat liver epithelial WBF344 cells. Most of the chalcones and dihydrochalcones inhibited EROD activity in a dose-dependent manner at the range 0.2525_M, which was comparable to model flavonoid inhibitors _-naphthoflavone and quercetin. The chalcones exhibited higher inhibition activity than the corresponding dihydroderivatives. Mono and dihydroxylated chalcones, and dihydrochalcones showed none or only a weak antioxidant activity; trihydroxyderivatives inhibited in vitro lipid peroxidation significantly only at 50_M concentration. Potential adverse effects, namely inhibition of GJIC and/or cytotoxicity were detected after treatment of WB-F344 cells with a number of chalcone and dihydrochalcone derivatives, suggesting that they should be excluded from additional screening as chemoprotective compounds. Chalcones and dihydrochalcones substituted at 4- and/or 4_-position, which elicited no inhibition of GJIC, were further tested for the potential enhancing effects on GJIC.
ER -
FOREJTNÍKOVÁ, Hana, Kamila LUNEROVÁ, Renata KUBÍNOVÁ, Dagmar JANKOVSKÁ, Radek MAREK, Radovan KAREŠ, Václav SUCHÝ, Jan VONDRÁČEK and Miroslav MACHALA. Chemoprotective and toxic potentials of synthetic and natural chalcones and dihydrochalcones in vitro. \textit{Toxicology}. Amsterdam: Elsevier, 2005, vol.~208, No~1, p.~81-93. ISSN~0300-483X.
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