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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

Choi, Sang-Un   (Pharmaceutical Screening Team, Korea Research Institute of Chemical TechnologyCC0186998  ); Kim, Kwang-Hee   (Pharmaceutical Screening Team, Korea Research Institute of Chemical TechnologyCC0186998  ); Kim, Nam-Young   (Pharmaceutical Screening Team, Korea Research Institute of Chemical TechnologyCC0186998  ); Choi, Eun-Jung   (Pharmaceutical Screening Team, Korea Research Institute of Chemical TechnologyCC0186998  ); Lee, Chong-Ock   (Pharmaceutical Screening Team, Korea Research Institute of Chemical TechnologyCC0186998  ); Son, Kwang-Hee   (Bioproducts Research Group, Korea Research Institute of Bioscience and Technology, KIST  ); Kim, Sung-Uk   (Bioproducts Research Group, Korea Research Institute of Bioscience and Technology, KIST  ); Bok, Song-Hae   (Bioproducts Research Group, Korea Research Institute of Bioscience and Technology, KIST  ); Kim, Young-Kook   (Bioproducts Research Group, Korea Research Institute of Bioscience and Technology, KIST  );
  • 초록

    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, $9.85\mug/ml$ 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, $4,4^I-di-tert-butylphenyl$ , bibenzyl, $2,2^I-dimethylbibenzyl$ , 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.


  • 주제어

    Bis(2-hydroxy-3-tert-butyl-5-methylphenyl)methane .   Human tumor cell .   Cy-totoxicity .   Multidrug-resistance.  

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    1. 1990 "생쥐 대식세포의 종양세포 치사활성에 미치는 인삼분획물과 지방다당류의 영향" 고려인삼학회지 = Korean journal of ginseng science 14 (3): 364~372    
    2. 1992 "새로운 엽산 대사 길항제의 합성 및 약리활성" 약학회지 = Yakhak hoeji 36 (4): 326~333    
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    5. 1994 "Antitumor Triterpense from Medicinal Plants" Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea 17 (5): 375~377    
    6. 1994 "Synthesis of Mannich Bases of Antineoplaston A10 and their Antitumor Activity" Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea 17 (6): 467~469    
    7. 1995 "지모(知母)의 항암활성성분에 관한 연구" 생약학회지 26 (1): 47~50    
    8. 1996 "Establishment of Doxorubicin-resistant Subline Derived from HCT15 Human Colorectal Cancer Cells" Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea 19 (5): 342~347    
    9. 1996 "Synthesis and Evaluation of Cytotoxicity of Novel Arylsulfonylimidazolidinones Containing Sulfonylurea Pharmacophore" Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea 19 (6): 570~580    
    10. 1997 "유포르비아속 식물로부터 단리한 가수분해형 탄닌의 인체고형암 세포에 대한 세포독성효과" 약학회지 = Yakhak hoeji 41 (4): 524~529    
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