Abstract |
The prenyl- phenol antibiotics ascochlorin-related compounds, are known to reduce serum cholesterol and triglyceride, suppress hypertension, and ameliorate types-I and II diabetes. However, little is known about the molecular mechanism for these physiological effects. Here we report that the ascochlorin derivative, 4-O-carboxymethyl ascochlorin (AS-6) acts as a potent activator of the nuclear hormone receptor, PPARgamma, although it does not activate the related receptors, PPARalpha, PPARdelta or RARalpha. AS-6 interacts directly with the PPARgamma molecule in vitro, and induces differentiation of the mouse preadipocyte cell line 3T3-L1. Our results suggest that AS-6 is a partial agonist for PPARgamma with a novel chemical structure.
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Authors | Marie Togashi, Hiromi Masuda, Teruo Kawada, Masao Tanaka, Kaname Saida, Kunio Ando, Gakuzo Tamura, Junji Magae |
Journal | The Journal of antibiotics
(J Antibiot (Tokyo))
Vol. 55
Issue 4
Pg. 417-22
(Apr 2002)
ISSN: 0021-8820 [Print] England |
PMID | 12061550
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Glycolates
- Hypoglycemic Agents
- Receptors, Cytoplasmic and Nuclear
- Transcription Factors
- 4-O-carboxymethylascochlorin
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Topics |
- Adipocytes
(cytology, drug effects, metabolism)
- Animals
- Cell Differentiation
(drug effects, physiology)
- Cell Line
- Glycolates
(pharmacology)
- Humans
- Hypoglycemic Agents
(pharmacology)
- Mice
- Receptors, Cytoplasmic and Nuclear
(genetics, metabolism)
- Transcription Factors
(genetics, metabolism)
- Transfection
- Tumor Cells, Cultured
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