RRC ID |
62910
|
著者 |
Tang R, Zhou D, Kimishima A, Setiawan A, Arai M.
|
タイトル |
Selective cytotoxicity of marine-derived fungal metabolite (3S,6S)-3,6-dibenzylpiperazine-2,5-dione against cancer cells adapted to nutrient starvation.
|
ジャーナル |
J Antibiot (Tokyo)
|
Abstract |
The cancer cells that are adapted to the hypoxic and nutrient-starved conditions of the tumor microenvironment have become a key target for anticancer therapies. In the course of search for selective cytotoxic substances against cancer cells adapted to nutrient starvation, (3S,6S)-3,6-dibenzylpiperazine-2,5-dione (1) was isolated from culture extract of marine-derived Paecilomyces formous 17D47-2. Compound 1 showed cytotoxic activity on the human pancreatic carcinoma PANC-1 cells adapted to glucose-starved conditions with IC50 value of 28 µM, whereas no effect was observed against PANC-1 cells under general culture conditions up to 1000 µM. Further studies on the mechanism of the selective cytotoxicity of 1 against the glucose-starved PANC-1 cells suggest that it may function via uncoupling of mitochondrial oxidative phosphorylation.
|
巻・号 |
73(12)
|
ページ |
873-875
|
公開日 |
2020-12-1
|
DOI |
10.1038/s41429-020-0340-3
|
PII |
10.1038/s41429-020-0340-3
|
PMID |
32587348
|
MeSH |
Antineoplastic Agents / chemistry
Antineoplastic Agents / isolation & purification*
Antineoplastic Agents / pharmacology
Aquatic Organisms / chemistry
Cell Line, Tumor
Cytotoxins / chemistry
Cytotoxins / isolation & purification*
Cytotoxins / pharmacology
Electron Transport / drug effects
Humans
Molecular Structure
Oxygen Consumption / drug effects
Paecilomyces / chemistry*
Pancreatic Neoplasms / drug therapy*
Piperazines / chemistry
Piperazines / isolation & purification
Piperazines / pharmacology
Tumor Microenvironment / drug effects
|
IF |
2.668
|
リソース情報 |
ヒト・動物細胞 |
PANC-1(RCB2095) |