金合欢素

植物来源生物活性体外研究体内研究金合欢素试剂级价格

金合欢素

CAS号:480-44-4
英文名:Acacetin
中文名:金合欢素
CBNumber:CB9316535
分子式:C16H12O5
分子量:284.26
MOL File:480-44-4.mol

金合欢素化学性质

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 :DMSO (Slightly), Methanol (Very Slightly, Heated)
形态 :Solid
酸度系数(pKa) :6.51±0.40(Predicted)
颜色 :Light Yellow to Green-Yellow to Dark Yellow
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)

安全信息

危险品标志 :Xi
危险类别码 :36/37/38
安全说明 :26-36
WGK Germany :3
RTECS号 :DJ3002000
F :3-8-10
海关编码 :29329990

金合欢素性质、用途与生产工艺

植物来源
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。
生物活性 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。

体外研究

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.

体内研究

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.