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題 名 | Structure-Activity Relationships of Five Myricetin Galloylglycosides from Leaves of Acacia Confusa=相思樹葉子五種楊梅樹皮素配糖體之結構-活性關係 |
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作 者 | 李宗徽; 劉得任; 徐鳳麟; 吳紋君; 侯文琪; | 書刊名 | Botanical Studies |
卷 期 | 47:1 民95.01 |
頁 次 | 頁37-43 |
分類號 | 373.8 |
關鍵詞 | 相思樹; DPPH自由基; Semicarbazide-sensitive胺酶; 血管收縮素轉化酶; 楊梅樹皮素配糖體; 結構-活性關係; Acacia confusa; Angiotensin converting enzyme; ACE; 1,1-diphenyl-2-picrylhydrazyl; DPPH; Myricetin galloylglycoside; Semicarbazide-sensitive amine oxidase; SSAO; Structure-activity relationships; SAR; |
語 文 | 英文(English) |
中文摘要 | 從相思樹葉子分離五種楊梅樹皮素配糖體在之前就已經有報告(Lee et al., 2000, J. Nat. Prod., 63, 710-712),但是結構-活性之間的關係並沒有報告。本篇研究將比較五種分離的化合物,包括myricetin 3-O-(3"-O-galloyl)-α-rhamnopyranoside 7-methyl ether(化合物1,分子量630 Da), myricetin 3-O-(2"-O-galloyl)-α-rhamnopyranoside 7-methyl ether(化合物2,分子量630 Da), myricetin 3-O-(2"-O-galloyl)-α-rhamnopyranoside(化合物3,分子量616 Da), myricetin 3-O-(3"-O-galloyl)-α-rhamnopyranoside(化合物4,分子量616 Da), 及myricetin 3-O-(2", 3"-di-O-galloyl)-α-rhamnopyranoside(化合物5,分子量768 Da),對於清除DPPH自由基與抑制Semicarbazide-sensitive胺酶(SSAO)及血管收縮素轉化酶(ACE)活性的關係。就清除DPPH自由基方面,五種化合物50%抑制所需濃度分別為591, 1522, 3210, 1389,及867 μM。就抑制Semicarbazide-sensitive胺酶方面,五種化合物 50%抑制所需濃度分別為36.16, 93.20, 119.50, 88.20,及39.35 μM。就上面清除DPPH自由基與抑制Semicarbazide-sensitive胺酶的結果可以發現,五種結構相關化合物顯現出以下相同次序:化合物1>化合物5>化合物4>化合物2>化合物3,而gallic acid位在R3的位置,與上述兩種活性有密切的關係。就抑制血管收縮素轉化酶(ACE)方面,只有化合物1,化合物2,及化合物5具有濃度相關抑制活性,三種化合物50% 抑制所需濃度分別為60.32, 151.90,及 19.82 μM。 |
英文摘要 | Five structure-related myricetin galloylglycosides isolated from leaves of Acacia confusa were previously reported (Lee et al., 2000, J. Nat. Prod., 63, 710-712). However, the structure-activity relationships were not reported. In this research, the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity, and inhibitory activities against semicarbazide-sensitive amine oxidase (SSAO) and angiotensin converting enzyme (ACE) were compared among five compounds, namely, myricetin 3-O-(3"-O-galloyl)-α-rhamnopyranoside 7-methyl ether (compound 1, 630 Da), myricetin 3-O-(2"-O-galloyl)-α-rhamnopyranoside 7-methyl ether (compound 2, 630 Da), myricetin 3-O-(2"-O-galloyl)-α-rhamnopyranoside (compound 3, 616 Da), myricetin 3-O-(3"-O-galloyl)-α-rhamnopyranoside (compound 4, 616 Da), myricetin 3-O-(2", 3"-di-O-galloyl)-α-rhamnopyranoside (compound 5, 768 Da). For DPPH scavenging activity, the IC50 for five compounds was 591, 1522, 3210, 1389, and 867 μM, respectively. For SSAO inhibitory activity, the IC50 for five compounds was 36.16, 93.20, 119.50, 88.20, and 39.35 μM, respectively. The IC50 of positive control of semicarbazide was 34.21 μM. The five compounds have the same orders of compound 1> compound 5> compound 4> compound 2> compound 3 for DPPH scavenging activity and SSAO inhibitiony. It was found that gallic acid in the R3 position was the key role for both biological activities. For ACE inhibitory activity, compound 1, compound 2, and compound 5 showed dose-dependent inhibitory modes and the IC50 was 60.32, 151.90, and 19.82 μM, respectively. |
本系統中英文摘要資訊取自各篇刊載內容。