title: Induction of apoptosis and caspase-3 activation by chemopreventive [6]-paradol and structurally related compounds in KB cells.
abstract: [6]-paradol, a pungent phenolic substance found in ginger and other Zingiberaceae plants, has been demonstrated to be an effective inhibitor of tumor promotion in mouse skin carcinogenesis. In the present study, we found that [6]-paradol and other structurally related derivatives, [10]-paradol, [3]-dehydroparadol, [6]-dehydroparadol, and [10]-dehydroparadol, with the exception of [3]-paradol induce apoptosis in an oral squamous carcinoma cell line, KB, in a dose-dependent manner. [10]-paradol and [10]-dehydroparadol exhibited a similar extent of cytotoxicity to that of [6]-paradol. [6]-Dehydroparadol and [3]-dehydroparadol appeared to be more potent, with an IC50 less than 40 microM. Treatment of KB cells with an apoptosis-inducing concentration of [6]-dehydroparadol caused induction of proteolytic cleavage of pro-caspase-3. These results suggest that [6]-paradol and structurally related derivatives induce apoptosis through a caspase-3-dependent mechanism.
authors.affiliation: Oral Cancer Research Institute, Department of Oral Pathology and Oral Biology, College of Dentistry, Yonsei University, Seoul 120-752, South Korea.
authors.forename: Young Sam
authors.initials: YS
authors.lastname: Keum
authors.forename: Jin
authors.initials: J
authors.lastname: Kim
authors.forename: Keun Hyung
authors.initials: KH
authors.lastname: Lee
authors.forename: Kwang Kyun
authors.initials: KK
authors.lastname: Park
authors.forename: Young Joon
authors.initials: YJ
authors.lastname: Surh
authors.forename: Jong Min
authors.initials: JM
authors.lastname: Lee
authors.forename: Sang Sup
authors.initials: SS
authors.lastname: Lee
authors.forename: Jung Hoon
authors.initials: JH
authors.lastname: Yoon
authors.forename: So Yeon
authors.initials: SY
authors.lastname: Joo
authors.forename: In Ho
authors.initials: IH
authors.lastname: Cha
authors.forename: Jong In
authors.initials: JI
authors.lastname: Yook
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D015153:Blotting, Western; D002294:Carcinoma, Squamous Cell / Q000201:enzymology* / Q000517:prevention & control; D053148:Caspase 3; D020169:Caspases / Q000378:metabolism*; D002470:Cell Survival / Q000187:drug effects; D053938:DNA Fragmentation; D004790:Enzyme Induction; D005434:Flow Cytometry; D006139:Guaiacol / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007659:Ketones / Q000737:chemistry / Q000494:pharmacology*; D009062:Mouth Neoplasms / Q000201:enzymology* / Q000517:prevention & control; D014407:Tumor Cells, Cultured / Q000166:cytology / Q000187:drug effects*
chemical_list: D000970:Antineoplastic Agents; D007659:Ketones; D006139:Guaiacol; C421614:6-paradol; C505407:CASP3 protein, human; C505409:Casp3 protein, mouse; D053148:Caspase 3; D020169:Caspases