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KMID : 0043319960190040286
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Archives of Pharmacal Research
1996 Volume.19 No. 4 p.286 ~ p.291
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Cytotoxicity of a Novel Biphenolic Compound, Bis(2-hydroxy-3-tert-butyl-5-methylphenyl)methane against Human Tumor Cells In vitro
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Choi Sang-Un
Kim Kwang-Hee
Kim Nam-Young
Choi Eun-Jung
Lee Chong-Ock
Son Kwang-Hee
Kim Sung-Uk
Bok Song-Hae
Kim Young-Kook
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Abstract
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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-BPO02-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, respectively. GERI-BPO02-A has also revealed cytotoxicity against P-glycoproteinexpressed 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-BPO02-A such as diphenylmethane, 1,1-bis(3,4dimethylphenyl)ethane, 2,2-diphenylpropane, 2-benzylpyridine, 3-benzylpyridine, , bibenzyl, , cis-stilbene, trans-stilbene, 3-tert-butyl-4-hydroxy-5-methylphenyisulfide, sulfadiazine and sulfisomidine for studying of structure and activity relationship, and from these data we could suppose that hydroxyl group of GERI-BPO02A conducted important role in its cytotoxicity.
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KEYWORD
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Bis(2-hydroxy-3-tert-butyl-5-methylphenyl)methane, Human tumor cell, Cy-totoxicity, Multidrug-resistance
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