五味子酯甲

中文名称:

五味子酯甲

中文同义词:

五味子酯甲;五味子酯甲, 来源于五味子;SCHISANTHERIN A 五味子酯甲 标准品;北五味子提取物,五味子酯甲(标准品);SCHISANTHERIN A 五味子酯甲;北五味子提取物;五味子酯甲(标准品);五味子酯甲SCHISANTHERIN A

英文名称:

Schisantherin A

英文同义词:

SCHISANTHERIN A 98.0% BY HPLC;Schisantherin A (Gomisin-C;Gomisin C(Schisantherin A);Schisantherin A;SCHISANTHERINGOMISIN;Gomisin, 98%, from Schisandra chinensis;Benzo[3,4]cycloocta[1,2-f][1,3]benzodioxole-5,6-diol, 5,6,7,8-tetrahydro-1,2,3,13-tetramethoxy-6,7-dimethyl-, 5-benzoate, (5S,6S,7S,13aS)-;(5S,6S,7S)-6-Hydroxy-1,2,3,13-tetramethoxy-6,7-dimethyl-5,6,7,8-tetrahydrobenzo[3,4]cycloocta[1,2:4,5]benzo[1,2-d][1,3]dioxol-5-yl Benzoate

CAS号:

58546-56-8

分子式:

C30H32O9

分子量:

536.57

EINECS号:

相关类别:

中药对照品;标准品;对照品,标准品;分析标准品;植物提取物;中药标准品;chemical reagent;对照品;植提标准品;小分子抑制剂;Inhibitors;小分子抑制剂，天然产物;标准品-中药标准品;标准品，对照品;木脂素;标准品 -中药标准品;分析试剂-标准品;五味子系列;Heterocycles;pharmaceutical intermediate;phytochemical;reference standards from Chinese medicinal herbs (TCM).;standardized herbal extract

Mol文件:

58546-56-8.mol

熔点 

110～112℃

沸点 

675.6±55.0 °C(Predicted)

密度 

1.33±0.1 g/cm3(Predicted)

酸度系数(pKa)

13.70±0.60(Predicted)

化学性质

长方形结晶 (乙醇)，mp 122℃～124℃，[α]D23 -175°(c=0.12，氯仿)。易溶于苯、氯仿、丙酮，可溶于甲醇、乙醇，难溶于石油醚，不溶于水。 五味子果仁的乙醇提取物中分离得到去氧五味子素、五味子素、五味子乙素、五味子丙素、五味子醇乙、五味子酯甲和五味子酯乙等7个有降转氨酶活性的联苯环辛烯类木脂素。七种成份都有降低SGPT、促进肝糖元生成和延长戊巴比妥睡眠时间的作用。五味子酯乙降SGPT作用最强，五味子醇乙促进肝糖元生成作用最显著，五味子丙素延长戊巴比妥睡眠时间作用最突出。

五味子药材的总木脂素含量测定

五味子为木兰科植物五味子Schisandra chinensis (Turcz.) Baill. 的干燥成熟果实。主要含有木脂素类、挥发油类、多糖类等成分。 南五味子中木脂素类成分主要有五味子酯甲、乙、丙、丁、戊和去氧五味子素。主要是五味子酯甲，含量较高。木脂素成分除五味子酯戊外，结构式在B环上都有亚甲二氧基，都可与变色酸反应。所以用五味子酯甲为对照，测得的结果基本上反映了南五味子中总木脂素的含量。 (1) 对照品溶液的配制：取五味子酯甲对照品适量，精密称定，用甲醇配制成5mg/ml的溶液即得。 (2) 样品溶液的制备：取华中五味子 (南五味子) 果实粉末约1g，精密称定。置具塞瓶中，精密加入甲醇20ml，超声处理20min，放冷至室温，摇匀，过滤，弃去初滤液，取续滤液即得。 (3) 测定：精密吸取对照品溶液20μl，供试品溶液20μl，甲醇20μl分别置具塞试管中，水浴挥去甲醇，在三个残留物中分别各精密加入10%变色酸澄清水溶液0.5ml，浓硫酸3.0ml，蒸馏水1.5ml，摇匀，同置沸水浴中加热30min，迅速冷却，以上述甲醇管为空白，照分光光度法，在570nm波长处分别测定吸收度，计算即得。 (4) 测定结果：对不同产地的南五味子药材，按所拟定的方法操作，测得其结果。

生物活性

Schisantherin A (Gomisin C, Schisanwilsonin H, Arisanschinin K)是一种五味子红素，具有止咳、镇静、消炎、抗骨质疏松、神经保护、增强认知和心脏保护活性。Schisantherin A 也可通过IκBα降解抑制p65-NF-κB向核内移位。

靶点

Target Value NF-κB ()

Target

Value

NF-κB ()

体外研究

The concentrations of TNF-α and IL-6 in the supernatant of cells pretreated with 2.5 or 25 mg/L of Schisantherin A are significantly decreased compared to the LPS control group (p<0.05, p<0.01). The potential cytotoxicity of Schisantherin A is evaluated by the MTT assay after incubating cells for 24 h in the absence or presence of LPS, result shows cell viabilities are not affected by the cytokines at concentrations used (0.5, 2.5, 25 mg/L). RAW 264.7 murine macrophage cells are pre-incubated with Schisantherin A for 1 h and then stimulated with 1 mg/L LPS for 12 h. Both LPS and samples are untreated in control group. After the cell culture media are collected, nitrite and PGE 2 levels are determined, and Schisantherin A is found to reduce NO and PGE 2 production in a dose-dependent manner.

体内研究

Schisantherin A, a dibenzocyclooctadiene lignan isolated from the fruit of Schisandra sphenanthera , has been reported to possess varied beneficial pharmacological effects. Schisantherin A protects lipopolysaccharide-induced acute respiratory distress syndrome in mice through inhibiting NF-κB and MAPKs signaling pathways. Pretreatment with Schisantherin A markedly ameliorates LPS-induced histopathologic changes and decreases the levels of TNF-α, IL-6 and IL-1β in the BALF. In addition, the phosphorylation of NF-κB p65, IκB-α, JNK, ERK and p38 induced by LPS are suppressed by Schisantherin A. The lung wet/dry weight ratio is evaluated at 7 h after the intranasal instillation of LPS. The results show that there are no differences between control group and Schisantherin A (40 mg/kg) group (p>0.05). LPS causes a significant increase in lung wet/dry weight ratio (p<0.01) compared with the control group. Schisantherin A dose-dependently decreases the lung wet/dry weight ratio (p<0.05) compared to those in the LPS group.

安全说明 

24/25

海关编码 

29329990