論文 - 詳細
| RRC ID | 39194 |
|---|---|
| 著者 | Prasain JK, Tezuka Y, Hase K, Basnet P, Dong H, Namba T, Kadota S. |
| タイトル | Inhibitory effect of diarylheptanoids on nitric oxide production in activated murine macrophages. |
| ジャーナル | Biol Pharm Bull |
| Abstract |
Thirteen novel diarylheptanoids bearing a chalcone or a flavanone moiety (1-13), a new curcumin derivative, 1,2-dihydrobis(de-O-methyl)curcumin (14), and two known flavonoids (15 and 16) isolated from the seeds of Alpinia blepharocalyx K. Schum. were tested for their inhibitory effects on nitric oxide (NO) production in lipopolysaccaride (LPS)-activated murine macrophages J774.1 in vitro. All the tested compounds inhibited NO production in a concentration-dependent manner (IC50=36-568 microM). Among the compounds examined, blepharocalyxin B (13) was the most potent inhibitor of NO production (IC50=36 microM). Analysis of the structure activity relationship among these novel diarylheptanoids led to the conclusion that the position of attachment of a chalcone or a flavanone to a diarylheptanoid does not affect their inhibitory potency although their presence in association causes a substantial enhancement of the inhibitory activity. Moreover, a conjugated double bond in a chalcone moiety potentiated the inhibitory activity. On the other hand, hexamethoxydeoxycalyxin A (17) and pentamethoxycalyxin B (18), a methylated product of calyxin A (1) and an epimeric mixture of calyxin B, showed greatly reduced activity suggesting that phenolic hydroxyl groups are involved in the inhibitory activity. |
| 巻・号 | 21(4) |
| ページ | 371-4 |
| 公開日 | 1998-4-1 |
| DOI | 10.1248/bpb.21.371 |
| PMID | 9586575 |
| MeSH | Animals Cell Line Cell Survival / drug effects Chalcone / analogs & derivatives Chalcone / chemical synthesis* Chalcone / pharmacology Enzyme Inhibitors / chemical synthesis* Enzyme Inhibitors / pharmacology Flavonoids / chemical synthesis* Flavonoids / pharmacology Lipopolysaccharides / pharmacology Macrophage Activation / physiology Macrophages / drug effects Macrophages / metabolism* Mice Nitric Oxide / biosynthesis* Nitric Oxide Synthase / antagonists & inhibitors* |
| IF | 1.863 |
| 引用数 | 14 |
| WOS 分野 | PHARMACOLOGY & PHARMACY |
| オルトメトリクス指標 |
オルトメトリクス指標項目
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| 最多言及媒体 | Patent(IFI CLAIMS) |
| 各媒体での言及数の合計 | 6 |
| 過去6か月間でのオルトメトリクス指標の変動値 | 0.0 |
| リソース情報 | |
| ヒト・動物細胞 | J774.1(RCB0434) |