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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
2005-3-30
pubmed:abstractText
A total of 6 newly-synthesized styrylchromones (SC-1 approximately SC-6) were compared for their cytotoxic activity against three normal oral human cells (gingival fibroblast HGF, pulp cell HPC, periodontal ligament fibroblast HPLF) and four human tumor cell lines (squamous cell carcinoma HSC-2, HSC-3, submandibular gland carcinoma HSG, promyelocytic leukemia HL-60). All compounds showed higher cytotoxic activity against tumor cell lines than against normal cells. Among the 6 compounds, SC-3, SC-4 and SC-5, which have one to three methoxy groups, showed higher tumor specificity and water solubility. The cytotoxic activity of SC-3 and SC-5 was slightly reduced by a lower concentration of NADH, a quinone reductase, but that of SC-3 was enhanced by higher concentrations of NADH, possibly due to demethylation of the methoxy groups. Agarose gel electrophoresis demonstrated that SC-3 and SC-5 induced intemucleosomal DNA fragmentation in HL-60 cells and production of large DNA fragment in HSC-2 cells. Both SC-3 and SC-5 enhanced the enzymatic activity to cleave the substrates for caspases 3, 8 and 9, suggesting the activation of both extrinsic and intrinsic apoptosis pathways. ESR spectroscopy showed that these compounds produced no detectable amount of radical and did not scavenge superoxide anion generated by the hypoxanthine-xanthine oxidase reaction. The highly tumor-specific cytotoxic action and apoptosis-inducing capability of SC-3 and SC-5 suggest their applicability for cancer chemotherapy.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0258-851X
pubmed:author
pubmed:issnType
Print
pubmed:volume
19
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
157-63
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed-meshheading:15796168-Antineoplastic Agents, pubmed-meshheading:15796168-Apoptosis, pubmed-meshheading:15796168-Carcinoma, Squamous Cell, pubmed-meshheading:15796168-Caspases, pubmed-meshheading:15796168-Cell Line, pubmed-meshheading:15796168-Cell Line, Tumor, pubmed-meshheading:15796168-Chromones, pubmed-meshheading:15796168-Dental Pulp, pubmed-meshheading:15796168-Drug Screening Assays, Antitumor, pubmed-meshheading:15796168-Electron Spin Resonance Spectroscopy, pubmed-meshheading:15796168-Electrophoresis, Agar Gel, pubmed-meshheading:15796168-Enzyme Activation, pubmed-meshheading:15796168-Fibroblasts, pubmed-meshheading:15796168-Gingiva, pubmed-meshheading:15796168-HL-60 Cells, pubmed-meshheading:15796168-Humans, pubmed-meshheading:15796168-Mouth Neoplasms, pubmed-meshheading:15796168-Periodontal Ligament, pubmed-meshheading:15796168-Structure-Activity Relationship, pubmed-meshheading:15796168-Submandibular Gland Neoplasms
pubmed:articleTitle
Cytotoxic activity of styrylchromones against human tumor cell lines.
pubmed:affiliation
Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama 350-0295, Japan.
pubmed:publicationType
Journal Article, Comparative Study, Research Support, Non-U.S. Gov't