CYTOTOXICITY OF A NOVEL BIPHENOLIC COMPOUND, BIS(2-HYDROXY-3-TERT-BUTYL-5-METHYLPHENYL)METHANE AGAINST HUMAN TUMOR-CELLS IN-VITRO

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-b utyl-5-methylphenyl)methane (GERI-BP002-A) was isolated from the ferme ntation broth of Aspergillus fumigatus F93 previously, and it has reve aled cytotoxicity against human solid tumor cells. Its effective doses that cause 50% inhibition of cell growth in vitro against non-small c ell lung rancer cell A549, ovarian cancer cell SK-OV-3, skin cancer ce ll SK-MEL-2 and central nerve system cancer cell XF498 were 8.24, 10.6 0, 8.83, 9.85 Lg/ml respectively. GERI-BP002-A has also revealed cytot oxicity 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 GER1-BP002-A such as diphenylmet hane, 1,1-bis(3,4-dimethylphenyl)ethane, 2,2-diphenylpropane, 2-benzyl pyridine, 3-benzylpyridine, 4,4'-di-tert-butylphenyl, bibenzyl, 2,2'-d imethylbibenzyl, cys-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 supp ose that hydroxyl group of GERI-BP002A conducted important role in its cytotoxicity.