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
- 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)
金合欢素性质、用途与生产工艺
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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。
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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. - 化学性质 黄色针状结晶，可溶于甲醇、乙醇、DMSO等有机溶剂，来源于飞机草，大蓟，金合欢。
- 用途 金合欢素具有镇静，抗癌的作用。
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用途
用于含量测定/鉴定/药理实验等。
药理药效:舒郁，理气，安神，活络之功效。
- 更新日期：2024/11/08
- 产品编号：46523
- 产品名称：金合欢素； 刺槐素 Acacetin
- CAS编号：480-44-4
- 包装：250mg
- 价格：1075元
- 更新日期：2024/11/08
- 产品编号：46523
- 产品名称：金合欢素； 刺槐素 Acacetin
- CAS编号：480-44-4
- 包装：1g
- 价格：2813元
- 公司名称：TOKYO CHEMICAL INDUSTRY CO., LTD.
- 联系电话：03-36680489
- 电子邮件：Sales-JP@TCIchemicals.com
- 国家：日本
- 产品数：28387
- 优势度：80
- 公司名称：Apollo Scientific Limited
- 联系电话：--
- 电子邮件：
- 国家：日本
- 产品数：74
- 优势度：58
- 公司名称：NACALAI
- 联系电话：--
- 电子邮件：info-tech@nacalai.co.jp
- 国家：日本
- 产品数：6046
- 优势度：75
