去水淫羊藿黄素

生物活性体外研究体内研究去水淫羊藿黄素试剂级价格

去水淫羊藿黄素

CAS号:118525-40-9
英文名:Icaritin
中文名:去水淫羊藿黄素
CBNumber:CB2982508
分子式:C21H20O6
分子量:368.38
MOL File:118525-40-9.mol

去水淫羊藿黄素化学性质

熔点 :239℃
沸点 :582.0±50.0 °C(Predicted)
密度 :1.359
闪点 :206.7℃
储存条件 :2-8°C
溶解度 :DMSO: soluble5mg/mL, clear (warmed)
形态 :powder
酸度系数(pKa) :6.44±0.40(Predicted)
颜色 :light yellow to dark yellow
最大波长(λmax) :368nm(MeOH)(lit.)
InChI :InChI=1S/C21H20O6/c1-11(2)4-9-14-15(22)10-16(23)17-18(24)19(25)20(27-21(14)17)12-5-7-13(26-3)8-6-12/h4-8,10,22-23,25H,9H2,1-3H3
InChIKey :TUUXBSASAQJECY-UHFFFAOYSA-N
SMILES :C1(C2=CC=C(OC)C=C2)OC2=C(C/C=C(/C)\C)C(O)=CC(O)=C2C(=O)C=1O

安全信息

WGK Germany :3
RTECS号 :DJ3100870
海关编码 :29329990

去水淫羊藿黄素性质、用途与生产工艺

生物活性 Icaritin (Anhydroicaritin) 是 Epimedium Genusis 的异戊二烯类黄酮衍生物，有效抑制 K562 细胞 (IC50 为 8 µM) 和原代 CML 细胞 (对 CML-CP 的 IC50 值为 13.4 µM，对 CML-BC 的 IC50 值为 18 µM) 的增殖。Icaritin 可以调节 MAPK/ERK/JNK 和 JAK2/STAT3/AKT 信号传导，并具有增强成骨的作用。

体外研究

Icaritin (4-64 µM; 48 hours; K562, imatinib-resistant cells and primary CML cells) treatment inhibits proliferation of K562, imatinib-resistant cells and primary CML cells .
Icaritin (0-64 µM; 48 hours; K562 and primary cells) treatment induces K562 or primary cells apoptosis in an concentration dependent manner.
Icaritin (32 µM; K562 cells) treatment increases cell population in the sub-G1 phase in K562 cells.
Icaritin (0-64 µM; 48 hours; K562 cells) treatment inhibits MAPK/ERK/JNK downstream signaling and diminishes Jak2/Stat3/Akt expression. Icaritin treatment also significantly inhibits Bcl-2 protein expression and up-regulated Bax protein expression in K562 with a dose-dependent manner accompanied by the cleavage activation of caspase-3 or caspase-9, and a down-regulated expression of Apaf-1.

Cell Proliferation Assay

Cell Line:	K562, imatinib-resistant cells and primary CML cells
Concentration:	4 µM, 8 µM, 16 µM, 32 µM and 64 µM
Incubation Time:	48 hours
Result:	Inhibited cell proliferation.

Apoptosis Analysis

Cell Line:	K562 or primary cells
Concentration:	0 µM, 4 µM, 8 µM, 16 µM, 32 µM and 64 µM
Incubation Time:	48 hours
Result:	Induced K562 or primary cells apoptosis.

Cell Cycle Analysis

Cell Line:	K562 cells
Concentration:	32 µM
Incubation Time:
Result:	Cell population in the sub-G1 phase was increased.

Western Blot Analysis

Cell Line:	K562 cells
Concentration:	0 µM, 4 µM, 8 µM, 16 µM, 32 µM and 64 µM
Incubation Time:	48 hours
Result:	Inhibited MAPK/ERK/JNK downstream signaling and diminishes Jak2/Stat3/Akt expression.

体内研究

Icaritin (4-8 mg/kg; intraperitoneal injection; daily; for 10 weeks; female NOD-SCID nude mice) treatment could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells without suppression of bone marrow in mouse leukemia model.

Animal Model:	Female NOD-SCID nude mice (6-8 weeks old) with K562 cells
Dosage:	4 mg/kg and 8 mg/kg
Administration:	Intraperitoneal injection; daily; for 10 weeks
Result:	Could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells without suppression of bone marrow.