葫芦素 I
- CAS号:2222-07-3
- 英文名:CUCURBITACIN I
- 中文名:葫芦素 I
- CBNumber:CB6480840
- 分子式:C30H42O7
- 分子量:514.65
- MOL File:2222-07-3.mol
- 熔点 :148-150°C
- 沸点 :698.3±55.0 °C(Predicted)
- 密度 :1.26±0.1 g/cm3(Predicted)
- 储存条件 :-20°C
- 溶解度 :≥22.45 mg/mL in DMSO; insoluble in EtOH; ≥51.2 mg/mL in H2O with ultrasonic
- 酸度系数(pKa) :8.51±0.70(Predicted)
- 形态 :solid
- 颜色 :white to off-white
- LogP :2.330 (est)
- 危险品标志 :Xi,T+
- 危险类别码 :25-28
- 安全说明 :1-22-45-36/37-28
- 危险品运输编号 :UN 2811 6.1/PG 1
- WGK Germany :3
- RTECS号 :RC6200000
- 毒性 :LD50 oral in mouse: 5mg/kg
葫芦素 I性质、用途与生产工艺
- 生物活性 Cucurbitacin I 是 JAK2/STAT3 的天然选择性抑制剂,并具有有效的抗肿瘤活性。
-
靶点
JAK2
STAT3
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体外研究
Exposure of the COLO205 cells to Cucurbitacin I significantly decreases cell viability. The anticancer activity of Cucurbitacin I is accomplished by downregulating p-STAT3 and MMP-9 expression. PE-induced cell enlargement and upregulation of ANF and β-MHC are significantly suppressed by pretreatment of the cardiomyocytes with Cucurbitacin I. Notably, Cucurbitacin I also impaires connective tissue growth factor (CTGF) and MAPK signaling, pro-hypertrophic factors, as well as TGF-β/Smad signaling, the important contributing factors to fibrosis. Incubation of the Seax cell line with the Jak/Stat3 inhibitor Cucurbitacin I result in a time- and concentration-dependent decrease of P-Stat3 and Stat3. In freshly isolated Sz cells (n=3), Cucurbitacin I induces a concentration-dependent decrease in Stat3 expression whereas P-Stat3 is undetectable. Finally, incubation of freshly isolated Sz cells (n=4) with 30 μM Cucurbitacin I for 6 hours induces apoptosis in the large majority (73-91%) of tumor cells.
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体内研究
No major side effects are noted throughout the study. It is shown that average tumor volumes at the end of the study are as follows: control, 616 mm 3 (±130); CQ, 580 mm 3 (±107); Cucurbitacin I, 346mm 3 (±79); and combination, 220mm 3 (±62). The differences in tumor volume between the Cucurbitacin I and control, combination and control, and combination and Cucurbitacin I arms are significant. Furthermore, combination-treated tumors exhibit a significantly lower average tumor weight at study termination than the control. Moreover, there was no effect on the body weights of mice.
- 更新日期:2024/11/08
- 产品编号:HY-N1405
- 产品名称:葫芦素 I Cucurbitacin I
- CAS编号:2222-07-3
- 包装:1mg
- 价格:1480元
- 更新日期:2024/11/08
- 产品编号:HY-N1405
- 产品名称:葫芦素 I Cucurbitacin I
- CAS编号:2222-07-3
- 包装:5mg
- 价格:3780元
- 公司名称:MedChemexpress LLC
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