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Title 

Cytotoxicity of a novel biphenolic compound, bis(2-hydroxy-3-tert-butyl-5-methylphenyl)methane against human tumor cells In vitro

Authors 

Sang Un ChoiKwang Hee KimNam Young KimEun Jung ChoiChong Ock LeeKwang Hee SonSung Uk KimSong Hae BokYoung Kook Kim

Publisher 

Pharmaceutical Society of Korea

Issue Date 

1996

Citation 

Archives of Pharmacal Research, vol. 19, no. 4, pp. 286-291

Keywords 

Bis(2-hydroxy-3-tert-butyl-5-methylphenyl)methaneCytotoxicityHuman tumor cellMultidrug-resistance

Abstract 

Phenolic compounds are prevalent as toxins or environmental pollutants, but they are also widely used as drugs for various purpose including anticancer agent. A novel biphenolic compound, bis(2-hydroxy-3-tert-butyl-5-methylphenyl)methane (GERI-BP002-A) was isolated from the fermentation broth of Aspergillus fumigatus F93 previously, and it has revealed cytotoxicity against human solid tumor cells. Its effective doses that cause 50% inhibition of cell growth in vitro against non-small cell lung cancer cell A549, ovarian cancer cell SK-OV-3, skin cancer cell SK-MEL-2 and central nerve system cancer cell XF498 were 8.24, 10.60, 8.83, 9.85 μg/ml respectively. GERI-BP002-A has also revealed cytotoxicity against P-glycoprotein-expressed human colon cancer cell HCT15 and its multidrug-resistant subline HCT15/CL02, and its cytotoxicity was not affected by P-glycoprotein. We have also tested cytotoxicities of structurally related compounds of GERI-BP002-A such as diphenylmethane, 1,1-bis(3,4-dimethylphenyl)ethane, 2,2-diphenylpropane, 2-benzylpyridine, 3-benzylpyridine, 4,4′-di-tert-butylphenyl, bibenzyl, 2,2′-dimethylbibenzyl, cis-stilbene, trans-stilbene, 3-tert-butyl-4-hydroxy-5-methylphenylsulfide, sulfadiazine and sulfisomidine for studying of structure and activity relationship, and from these data we could suppose that hydroxyl group of GERI-BP002-A conducted important role in its cytotoxicity.

ISSN 

0253-6269

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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