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葫芦素 I
产品纠错
CAS号:2222-07-3 | 英文名称:CUCURBITACIN I
分子式 C30H42O7
分子量 515
EINECS号 218-736-8
MDL MFCD09971044
Smiles
InChIKey
乙二醇化学百科
基本信息
中文名称 葫芦素 I
英文名称 CUCURBITACIN I
CAS号 2222-07-3
分子式 C30H42O7
分子量 514.65
EINECS号 218-736-8
物化性质
熔点 148-150°C
沸点 698.3±55.0 °C(Predicted)
密度 1.26±0.1 g/cm3(Predicted)
LogP 2.330 (est)
溶解度 DMSO 中≥22.45 mg/mL;不溶于乙醇;超声检测水中≥51.2 mg/mL
形态 固体
酸度系数(pKa) 8.51±0.70(Predicted)
颜色 白色至类白色
安全信息
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
生产及用途
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。

JAK2

STAT3

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.

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.

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