RRC ID |
62106
|
著者 |
Hatano H, Takekawa F, Hashimoto K, Ishihara M, Kawase M, Qing C, Qin-Tao W, Sakagami H.
|
タイトル |
Tumor-specific cytotoxic activity of 1,2,3,4-tetrahydroisoquinoline derivatives against human oral squamous cell carcinoma cell lines.
|
ジャーナル |
Anticancer Res
|
Abstract |
The tumor-specific cytotoxicity and the type of cell death induced by thirty-eight newly synthesized tetrahydroisoquinoline derivatives in human oral squamous cell carcinoma cell lines were investigated. 6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)(3,4-dimethoxyphenyl) methanone that has bulky substituents (such as 3,4-dimethoxybenzoyl group) (TQ9) and ethyl 2-benzyloxycarbonyl-1,2,3,4-tetrahydroisoquinoline-1-carboxylate that has ethoxycarbonyl group and benzyloxycarbonyl group (TD13) showed the highest tumor-specific cytotoxicity (TS=12.5 and 5.3, respectively). This supports the importance of molecular size for the cytotoxicity induction. TQ9 induced internulceosomal DNA fragmentation and caspase-3 activation only marginally in HL-60 cells, whereas it enhanced the formation of acidic organelles (stained with acridine orange) without induction of DNA fragmentation or caspase-3 activation in human squamous cell carcinoma cell lines (HSC-2, HSC-4), suggesting the induction of autophagy in the latter cells.
|
巻・号 |
29(8)
|
ページ |
3079-86
|
公開日 |
2009-8-1
|
PII |
29/8/3079
|
PMID |
19661319
|
MeSH |
Apoptosis / drug effects*
Autophagy
Carcinoma, Squamous Cell / drug therapy*
Carcinoma, Squamous Cell / pathology*
Caspase 3 / metabolism
Enzyme Activation / drug effects
Humans
Mouth Neoplasms / drug therapy*
Mouth Neoplasms / pathology*
Organelles / drug effects
Tetrahydroisoquinolines / chemistry*
Tetrahydroisoquinolines / pharmacology*
Tumor Cells, Cultured
|
IF |
1.994
|
リソース情報 |
ヒト・動物細胞 |
HSC-4(RCB1902)
HSC-2(RCB1945)
HSC-3(RCB1975) |