Azaphilones with endothelin receptor binding activity produced by Penicillium sclerotiorum: taxonomy, fermentation, isolation, structure elucidation and biological activity
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- PAIRET L.
- Xenova Ltd
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- WRIGLEY S. K.
- Xenova Ltd
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- CHETLAND I.
- Xenova Ltd
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- REYNOLDS E. E.
- Parke-Davis Pharmaceutical Research, Division of Warner Lambert Company
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- HAYES M. A.
- Xenova Ltd
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- HOLLOWAY J.
- Xenova Ltd
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- AINSWORTH A. M.
- Xenova Ltd
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- KATZER W.
- Xenova Ltd
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- CHENG X-M.
- Parke-Davis Pharmaceutical Research, Division of Warner Lambert Company
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- HUPE D. J.
- Parke-Davis Pharmaceutical Research, Division of Warner Lambert Company
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- CHARLTON P.
- Xenova Ltd
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- DOHERTY A. M.
- Parke-Davis Pharmaceutical Research, Division of Warner Lambert Company
書誌事項
- タイトル別名
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- Azapbilones with Endothelin Receptor Binding Activity Produced by Penicillium sclerotiorum: Taxonomy, Fermentation, Isolation, Structure Elucidation and Biological Activity.
- 公開日
- 1995
- 資源種別
- journal article
- DOI
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- 10.7164/antibiotics.48.913
- 公開者
- 公益財団法人 日本感染症医薬品協会
この論文をさがす
説明
A series of azaphilones produced by Penicillium sclerotiorum (Xenova culture collection number XI1853) active in assays for the detection of antagonists of the endothelin-A (ETA) and endothelin-B (ETB) receptors has been identified. The series includes two novel sclerotiorin analogues, (8S, 8a-R)-7-deacetyl-1, O8, 8, 8a-tetrahydro-7-epi-sclerotiorin, 1, and its 5-dechloro analogue, 2. It also includes 5-chloroisorotiorin, 6, previously unreported as a natural product, in addition to the major product of these fermentations, (+)-sclerotiorin, 5. Data for the inhibition of endothelin-1 (ET-1) and endothelin-3 (ET-3) binding in the ETA and ETB receptor assays respectively are reported for this series. Compounds 1 and 2 were more selective for the rabbit ETA receptor than for the rat ETB receptor. The IC50 values for 1 and 2 were 9 and 28 μM respectively in an assay based on binding of ET-1 to rabbit ETA receptors. In an assay based on the binding of ET-3 to the rat ETB receptor compounds 1 and 2 exhibited IC50's of 77 and 172 μM. Members of this series of compounds demonstrated antagonist behavior in a secondary assay based on blockade of ET-1 stimulated arachidonic acid release from rabbit renal artery smooth muscle cells, when present at concentrations of ≥30μM.
収録刊行物
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- The Journal of Antibiotics
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The Journal of Antibiotics 48 (9), 913-923, 1995
公益財団法人 日本感染症医薬品協会
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詳細情報 詳細情報について
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- CRID
- 1390282679128668416
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- NII論文ID
- 130003410166
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- COI
- 1:CAS:528:DyaK2MXotlKmt70%3D
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- ISSN
- 18811469
- 00218820
- https://id.crossref.org/issn/00218820
- http://id.crossref.org/issn/00218820
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- PubMed
- 7592055
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- 本文言語コード
- en
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- 資料種別
- journal article
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- データソース種別
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- JaLC
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可
