金合欢素
金合欢素 性质
熔点 | 260-265 °C(lit.) |
---|---|
沸点 | 346.76°C (rough estimate) |
密度 | 1.2160 (rough estimate) |
折射率 | 1.6200 (estimate) |
储存条件 | 2-8°C |
溶解度 | 可溶于DMSO(轻微)、甲醇(非常轻微,加热) |
形态 | 固体 |
酸度系数(pKa) | 6.51±0.40(Predicted) |
颜色 | 淡黄色至绿黄色至深黄色 |
最大波长(λmax) | 335nm(EtOH)(lit.) |
Merck | 14,13 |
BRN | 277879 |
InChIKey | DANYIYRPLHHOCZ-UHFFFAOYSA-N |
LogP | 2.443 (est) |
CAS 数据库 | 480-44-4(CAS DataBase Reference) |
金合欢素 用途与合成方法
金合欢 (Acacia farnesiana (Linn.) Willd.) (Mimosa) 豆科。灌木,高2-4米;枝具刺,刺长可达1-2厘米。二回羽状复叶,羽片4-8对,每羽片具小叶10-20对,小叶片线状长椭圆形。头状花序腋生,直径1.5厘米,常多个簇生。荚果圆柱形,长3-7厘米,直径8-15毫米。种子多数,黑色。 花极香,供提取香精。 刺灌术或小乔木,二回羽状复叶,头状花序簇生于叶腋,盛开时,好像金色的绒球一般。
Acacetin (5,7-Dihydroxy-4'-methoxyflavone) 是一种口服有效的类黄酮,来自 Tephroseris kirilowii (Turcz.) Holub。Acacetin 停在 PI3Kγ 的 ATP 结合口袋中。Acacetin 导致癌细胞周期停滞,并诱导细胞凋亡和自噬。Acacetin 具有有效的抗癌和抗炎活性,有用于疼痛相关疾病研究的潜力。
Acacetin (5,7-Dihydroxy-4'-methoxyflavone; 10-200 μM; 24 hours) decreases cell viabilities in a dose-dependent manner. Acacetin has little effect on human normal glial cell line HEB and non-tumorigenic epithelial cell line MCF-10A.
Acacetin (50-150 μM; 24 hours) causes G2/M cell cycle arrest and induces apoptosis and autophagy.
Acacetin (50-150 μM; 24 hours) leads to decreases in levels of PI3Kγ-p110, p-AKT, p-mTOR, p-p70S6K, and p-ULK in a dose-dependent manner.
Cell Viability Assay
Cell Line: | Breast cancer MCF-7 cells, hepatocellular carcinoma SMMC-7721 cells, lung adenocarcinoma A549 cells, esophageal carcinoma Eca109 cells |
Concentration: | 10, 20, 40, 60, 80, 100, 150, 200 μM |
Incubation Time: | 24 hours |
Result: |
Decreased cancer cell viabilities in a dose-dependent manner.
Had IC 50 values of 82.75 μM, 103.9 μM, 157.4 μM, 54.7 μM in MDA-MB-231, MCF-7, A549, Eca109 cells, respectively. |
Cell Cycle Analysis
Cell Line: | MDA-MB-231 cells |
Concentration: | 50, 100, 150 μM |
Incubation Time: | 24 hours |
Result: | Resulted in increase in percentage of cells at G2/M phase and decrease in percentage of cells at G1 and S phase in a dose-dependent manner. |
Apoptosis Analysis
Cell Line: | MDA-MB-231 cells |
Concentration: | 50, 100, 150 μM |
Incubation Time: | 24 hours |
Result: | Induced apoptosis. |
Cell Autophagy Assay
Cell Line: | MDA-MB-231 cells |
Concentration: | 50, 100, 150 μM |
Incubation Time: | 24 hours |
Result: |
Induced autophagy.
Resulted in marked increases in EGFP-LC3 puncta formation and a dose-dependent accumulation of LC3-II. |
Western Blot Analysis
Cell Line: | MDA-MB-231 cells |
Concentration: | 50, 100, 150 μM |
Incubation Time: | 24 hours |
Result: |
Resulted in decrease in levels of Bcl-2 and Bcl-xL and increase in levels of p53.
Led to decreases in levels of PI3Kγ-p110, p-AKT, p-mTOR, p-p70S6K, and p-ULK in a dose-dependent manner. Had little or no effect on expression of PI3Kα, PI3Kβ, PI3Kδ, p-ERK, p-p38, and p-JNK. |
Acacetin (5,7-Dihydroxy-4'-methoxyflavone; 5, 20 mg/kg/day; orally; for 3 days) significantly suppresses microglial activation in an LPS-induced neuroinflammation mouse model.
Acacetin (25 mg/kg/day; orally; for 3 days) reduces neuronal cell death in an animal model of ischemia.
Acacetin (1.8-56.2 mg/kg/day; ip; single dose) decreases visceral and inflammatory nociception and prevented the formalin-induced oedema.
Animal Model: | Male C57BL/6 mice, 7 weeks of age |
Dosage: | 5, 20 mg/kg |
Administration: | Orally; once a day for 3 days |
Result: | Significantly suppressed microglial activation in an LPS-induced (ip; 5mg/kg) neuroinflammation mouse model. |
药理药效:舒郁,理气,安神,活络之功效。
金合欢素 价格(试剂级)
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024-11-08 | 46523 | 金合欢素; 刺槐素 | 480-44-4 | 250mg | 1075 |
2024-11-08 | 46523 | 金合欢素; 刺槐素 | 480-44-4 | 1g | 2813 |