Chemoprotective and toxic potentials of synthetic and natural
chalcones and dihydrochalcones in vitro

J 2005

Chemoprotective and toxic potentials of synthetic and natural chalcones and dihydrochalcones in vitro

FOREJTNÍKOVÁ, Hana; Kamila LUNEROVÁ; Renata KUBÍNOVÁ; Dagmar JANKOVSKÁ; Radek MAREK et. al.

Základní údaje

Originální název

Chemoprotective and toxic potentials of synthetic and natural chalcones and dihydrochalcones in vitro

Název česky

Chemoprotektivní a toxický potenciál syntetických a přírodních chalkonů a dihyrochalkonů in vitro

Autoři

FOREJTNÍKOVÁ, Hana; Kamila LUNEROVÁ; Renata KUBÍNOVÁ; Dagmar JANKOVSKÁ; Radek MAREK ; Radovan KAREŠ; Václav SUCHÝ; Jan VONDRÁČEK a Miroslav MACHALA

Vydání

Toxicology, Amsterdam, Elsevier, 2005, 0300-483X

Další údaje

Jazyk

angličtina

Typ výsledku

Článek v odborném periodiku

Obor

30104 Pharmacology and pharmacy

Stát vydavatele

Nizozemské království

Utajení

není předmětem státního či obchodního tajemství

Odkazy

URL

Impakt faktor

Impact factor: 2.584

Kód RIV

RIV/00216224:14310/05:00025507

Organizační jednotka

Přírodovědecká fakulta

UT WoS

000226923000008

Klíčová slova anglicky

chalcone; dihydrochalcone; toxic; chemoprotective; in vitro

Štítky

chalcone, chemoprotective, dihydrochalcone, in vitro, toxic

Příznaky

Mezinárodní význam, Recenzováno

Změněno: 19. 5. 2009 21:01, prof. RNDr. Radek Marek, Ph.D.

Anotace

ORIG CZ

V originále

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.

Česky

Studie se zabývá serií 31 chalkonů a odpovídajících dihydrochalkonů. Byla studována schopnost inhibovat Fe(II)/NADPH peroxidaci a EROD aktivitu.

Návaznosti

LN00A016, projekt VaV

Název: BIOMOLEKULÁRNÍ CENTRUM

Investor: Ministerstvo školství, mládeže a tělovýchovy ČR, Biomolekulární centrum

Citovat

FOREJTNÍKOVÁ, Hana; Kamila LUNEROVÁ; Renata KUBÍNOVÁ; Dagmar JANKOVSKÁ; Radek MAREK; Radovan KAREŠ; Václav SUCHÝ; Jan VONDRÁČEK a Miroslav MACHALA. Chemoprotective and toxic potentials of synthetic and natural chalcones and dihydrochalcones in vitro. Toxicology. Amsterdam: Elsevier, 2005, roč. 208, č. 1, s. 81-93. ISSN 0300-483X.

@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 a Miroslav MACHALA. Chemoprotective and toxic potentials of synthetic and natural chalcones and dihydrochalcones in vitro. \textit{Toxicology}. Amsterdam: Elsevier, 2005, roč.~208, č.~1, s.~81-93. ISSN~0300-483X.

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