Abstract:
:Green tea and (-)-epigallocatechin gallate (EGCG: one of the main components of green tea) are reported to have cancer-preventive activity in humans. A previous SAR study of EGCG and derivatives indicated that a galloyl group is essential for the activity. To test this hypothesis, we synthesized various alkyl gallate and gallamide derivatives and evaluated their antiproliferative effects on human leukemia HL-60 cells. Dodecyl 3,4,5-trihydroxybenzoate (6c) showed the most potent activity, being more potent than EGCG. To clarify the molecular mechanism of the antiproliferative action, we investigated the effects of 6c on various factors. Compound 6c was found to induce apoptosis mediated by endoplasmic reticulum (ER)-stress-related caspase-12. Upregulation of gadd-153, an ER-stress marker protein, was also observed. These results indicate that 6c induced apoptosis via the ER-stress-related pathway.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Dodo K,Minato T,Noguchi-Yachide T,Suganuma M,Hashimoto Ydoi
10.1016/j.bmc.2008.07.063subject
Has Abstractpub_date
2008-09-01 00:00:00pages
7975-82issue
17eissn
0968-0896issn
1464-3391pii
S0968-0896(08)00677-9journal_volume
16pub_type
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