論文 - 詳細
| RRC ID | 47067 |
|---|---|
| 著者 | Kushida N, Watanabe N, Okuda T, Yokoyama F, Gyobu Y, Yaguchi T. |
| タイトル | PF1270A, B and C, novel histamine H3 receptor ligands produced by Penicillium waksmanii PF1270. |
| ジャーナル | J Antibiot (Tokyo) |
| Abstract |
Three novel histamine H3 receptor (H3R) ligands, PF1270A (1), PF1270B (2) and PF1270C (3) were isolated from the culture broth of the fungal strain PF1270. The strain was identified as Penicillium waksmanii on the basis of morphological characteristics. These compounds were obtained from the culture broth by solvent extraction and chromatographic purification. Their structures were established by spectroscopic methods and X-ray crystallographic analysis. They possess pentacyclic spiroindolinone skeletons. 1, 2 and 3 displayed high affinity for the rat H3R (Ki=0.058, 0.17 and 0.19 microM, respectively) and human H3R (Ki=0.047, 0.12 and 0.22 microM, respectively). Moreover, 1, 2 and 3 acted as potent agonists with the EC50 values of 0.12, 0.15 and 0.20 microM, respectively. |
| 巻・号 | 60(11) |
| ページ | 667-73 |
| 公開日 | 2007-11-1 |
| DOI | 10.1038/ja.2007.85 |
| PII | JST.JSTAGE/antibiotics/60.667 |
| PMID | 18057695 |
| MeSH | Animals Bridged-Ring Compounds / isolation & purification Bridged-Ring Compounds / pharmacology* CHO Cells Cell Membrane / drug effects Cell Membrane / metabolism Chemical Phenomena Chemistry, Physical Classification Cricetinae Cricetulus Crystallography, X-Ray Fermentation Guanosine 5'-O-(3-Thiotriphosphate) / metabolism Heterocyclic Compounds, 3-Ring / isolation & purification Heterocyclic Compounds, 3-Ring / pharmacology* Humans In Vitro Techniques Ligands Mass Spectrometry Microscopy, Electron, Scanning Models, Molecular Molecular Conformation Penicillium / chemistry* Penicillium / classification Penicillium / metabolism Rats Rats, Sprague-Dawley Receptors, Histamine H3 / drug effects* Receptors, Histamine H3 / genetics Spectrometry, Mass, Fast Atom Bombardment |
| IF | 2.668 |
| 引用数 | 26 |
| WOS 分野 | PHARMACOLOGY & PHARMACY BIOTECHNOLOGY & APPLIED MICROBIOLOGY IMMUNOLOGY MICROBIOLOGY |
| リソース情報 | |
| 病原微生物 | |