葫芦素 I
中文名称 | 葫芦素 I |
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中文同义词 | 葫芦素 I;葫芦素;葫芦素I(甄准不供应);CUCURBITACIN I 葫芦素I |
英文名称 | CUCURBITACIN I |
英文同义词 | ELATERICIN B;ELATERIN B;CUCURBITACIN I WITH HPLC;Cucurbitacin I hydrate;Elatericin B, JSI-124, NSC 521777, 2,16α,20,25-Tetrahydroxy-9-methyl-19-Nor-9β,10α-lanosta-1,5,23-triene-3,11,22-trione;(9β,10α,23E)-2,16α,20,25-Tetrahydroxy-9-methyl-19-norlanosta-1,5,23-triene-3,11,22-trione;Ibamarin;2,16a,20,25-Tetrahydroxy-9b-methyl-10a-19-norlanosta-1,5,23(E)-triene-3,11,22-trione |
CAS号 | 2222-07-3 |
分子式 | C30H42O7 |
分子量 | 514.65 |
EINECS号 | 218-736-8 |
相关类别 | 植物提取物;中药对照品;对照品;小分子;Inhibitor;Herb extract;API;Tri-Terpenoids |
Mol文件 | 2222-07-3.mol |
结构式 |
葫芦素 I 性质
熔点 | 148-150°C |
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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 | DMSO 中≥22.45 mg/mL;不溶于乙醇;超声检测水中≥51.2 mg/mL |
酸度系数(pKa) | 8.51±0.70(Predicted) |
形态 | 固体 |
颜色 | 白色至类白色 |
LogP | 2.330 (est) |
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.
安全信息
危险品标志 | Xi,T+ |
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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 |