Ascochlorin (Ilicicolin D)，异戊二烯类抗生素。Ascochlorin 主要通过抑制STAT3信号级联介导其抗肿瘤作用。Ascochlorin 诱导细胞凋亡 (apoptosis)。具有抗炎活性。
| 生物活性 | Ascochlorin (Ilicicolin D), an isoprenoidantibiotic, mediates its anti-tumor effects predominantly through the suppression ofSTAT3signaling cascade. Ascochlorin inducesapoptosis. Anti-inflammatory activity[1][2][3]. |
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体外研究
(In Vitro) | Ascochlorin (Ilicicolin D) (10-50 μM; 24-72 hours) inhibits the viability of HepG2, HCCLM3 and Huh7 cells in a time and dose dependent manner[3].
Ascochlorin (50 μM; 48 hours) induces apoptosis in HCC cells[3].
Ascochlorin (1-50 μM) significantly suppresses the production of nitric oxide (NO) and prostaglandin E2 (PGE2) and decreases the gene expression of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2) in a dose-dependent manner. Ascochlorin inhibits the mRNA expression and the protein secretion of interleukin (IL)-1β and IL-6 but not tumor necrosis factor (TNF)-α in LPS-stimulated RAW 264.7 macrophage cells. Ascochlorin suppresses nuclear translocation and DNA binding affinity of nuclear factor-κB (NF-κB). Ascochlorin down-regulates phospho-extracellular signal-regulated kinase 1/2 (p-ERK1/2) and p-p38[2].
Cell Viability Assay[3] | Cell Line: | HepG2, HCCLM3, Huh7 cells | | Concentration: | 10, 25, 50 μM | | Incubation Time: | 24, 48, 72 hours | | Result: | Inhibit the viability of three different HCC cell lines tested (HepG2, HCCLM3 and Huh7) in a time and dose dependent manner. |
Western Blot Analysis[3] | Cell Line: | HepG2 cells | | Concentration: | 50 μM | | Incubation Time: | 48 hours | | Result: | Inhibited expression of the cell cycle regulator protein cyclin D1, the anti-apoptotic proteins Bcl-2, Mcl-1, survivin and XIAP, and the invasive gene product MMP-9. |
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体内研究
(In Vivo) | Ascochlorin (Ilicicolin D) (2.5-5 mg/kg; i.p.; day 0, 1, 2, 3, 13, 15, 17, 20, 22, 24, 27, 29 and 31) inhibits tumor growth in an orthotopic HCC mouse model[1].
| Animal Model: | Eight week-old athymic balb/c nude female mice (HCCLM3-Luc2 tumors)[3] | | Dosage: | 2.5 mg/kg, 5 mg/kg | | Administration: | I.p.; day 0, 1, 2, 3, 13, 15, 17, 20, 22, 24, 27, 29 and 31 | | Result: | Induced significant inhibition of tumor growth. |
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| 结构分类 | - Antibiotics
- Other Antibiotics
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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