五味子酯甲

化学性质五味子药材的总木脂素含量测定生物活性靶点体外研究体内研究五味子酯甲试剂级价格

五味子酯甲

CAS号:58546-56-8
英文名:Schisantherin A
中文名:五味子酯甲
CBNumber:CB5462083
分子式:C30H32O9
分子量:536.57
MOL File:58546-56-8.mol

五味子酯甲化学性质

熔点 :110～112℃
沸点 :675.6±55.0 °C(Predicted)
密度 :1.33±0.1 g/cm3(Predicted)
储存条件 :Inert atmosphere,Store in freezer, under -20°C
溶解度 :Chloroform (Slightly), Methanol (Slightly, Sonicated)
形态 :Solid
酸度系数(pKa) :13.70±0.60(Predicted)
颜色 :White to Off-White
水溶解性 :insoluble in water

安全信息

安全说明 :24/25
海关编码 :29329990

五味子酯甲性质、用途与生产工艺

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
()
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.