生物活性
Garcinone E is the most active xanthone from mangosteen, which has potent cytotoxic effect against hepatocellular carcinoma cell lines. Garcinone E might inhibit metastasis of an oral cancer cell line by blocking invasion, migration and MMP production. Garcinone E (GE) significantly inhibited the proliferation in HEY, A2780, and A2780/Taxol cells. It induced endoplasmic reticulum (ER) stress and activated the protective inositol-requiring kinase (IRE)-1α pathway. Moreover, GE eliminated the migratory ability of HEY cells by reducing the expression of RhoA and Rac. It also blocked the invasion, which might be related to downregulation of matrix metalloproteinases (MMPs), i.e., MMP-9 and MMP-2, and upregulation of tissue inhibitors of metalloproteinase (TIMP) -1 and TIMP-2.
化学数据
分子量 | 464.55 |
分子式 | C28H32O6 |
CAS号 | 112649-21-5 |
纯度 | >98% |
溶解性(25°C) | DMSO 10 mM |
储存和运输条件 | 2-8°C, dry, sealed 常温运输及临时存放 |
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.1526 mL | 10.7631 mL | 21.5262 mL |
5 mM | 0.4305 mL | 2.1526 mL | 4.3052 mL |
10 mM | 0.2153 mL | 1.0763 mL | 2.1526 mL |