葫蘆素 I
| 中文名稱 | 葫蘆素 I |
|---|---|
| 中文同義詞 | 葫蘆素 I;葫蘆素;葫蘆素I(甄準(zhǔn)不供應(yīng));CUCURBITACIN I 葫蘆素I;葫蘆素I 117793;葫蘆素 I,10 MM DMSO 溶液;CUCURBITACIN I 葫蘆素I/ELATERICIN B(NSC-521777) |CAS 2222-07-3;Cucurbitacin I試劑 |
| 英文名稱 | CUCURBITACIN I |
| 英文同義詞 | ELATERICIN B;ELATERIN B;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;2,16α,20,25-tetrahydroxy-9β-methyl-10α-19-norlanosta-1,5,23(E)-triene-3,11,22-trione |
| CAS號(hào) | 2222-07-3 |
| 分子式 | C30H42O7 |
| 分子量 | 514.65 |
| EINECS號(hào) | 218-736-8 |
| 相關(guān)類別 | 植物提取物;中藥對(duì)照品;對(duì)照品;小分子;Inhibitor;Herb extract;API;Tri-Terpenoids |
| Mol文件 | 2222-07-3.mol |
| 結(jié)構(gòu)式 | ![]() |
葫蘆素 I 性質(zhì)
| 熔點(diǎn) | 148-150°C |
|---|---|
| 沸點(diǎn) | 698.3±55.0 °C(Predicted) |
| 密度 | 1.26±0.1 g/cm3(Predicted) |
| 儲(chǔ)存條件 | -20°C |
| 溶解度 | DMSO 中≥22.45 mg/mL;不溶于乙醇;超聲檢測(cè)水中≥51.2 mg/mL |
| 酸度系數(shù)(pKa) | 8.51±0.70(Predicted) |
| 形態(tài) | 固體 |
| 顏色 | 白色至類白色 |
| InChIKey | NISPVUDLMHQFRQ-KUIOOTTBNA-N |
| SMILES | [C@@]12(C)CC(O)C(C(O)(C)C(=O)/C=C/C(O)(C)C)[C@@]1(C)CC(=O)[C@]1(C)C3C=C(C(=O)C(C)(C)C3=CC[C@@]21[H])O |&1:0,17,22,35,r| |
| 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
| 危險(xiǎn)品標(biāo)志 | Xi,T+ |
|---|---|
| 危險(xiǎn)類別碼 | 25-28 |
| 安全說明 | 1-22-45-36/37-28 |
| 危險(xiǎn)品運(yùn)輸編號(hào) | UN 2811 6.1/PG 1 |
| WGK Germany | 3 |
| RTECS號(hào) | RC6200000 |
| 存儲(chǔ)類別 | 6.1A - 可燃,急性毒性物質(zhì)(類別1和類別2) 劇毒的危險(xiǎn)物質(zhì) |
| 危險(xiǎn)性類別 | 急性毒性 類別1 經(jīng)口 |
| 毒性 | LD50 oral in mouse: 5mg/kg |
