Cardamomin；豆蔻明
货号：
IC1030
品牌：
Jinpan
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产品简介
| MDL | MFCD00238554 |
| 别名 | Alpinetinchalcone |
| 英文名称 | Cardamomin |
| CAS | 18956-16-6 |
| 分子式 | C16H14O4 |
| 分子量 | 270.28 |
| 纯度 | HPLC≥98% |
| 单位 | 瓶 |
| 生物活性 | Cardamonin (Alpinetin chalcone)天然存在于良姜属物种的果实中，具有抗炎和抗肿瘤活性。它是一种新型的hTRPA1离子通道拮抗剂，IC50为454 nM，而不与TRPV1和TRPV4相互作用。[1-3] |
| In Vitro | Cardamonin selectively blocks TRPA1 activation while does not interact with TRPV1 nor TRPV4 channel. A concentration-dependent inhibitory effect is observed with IC50 of 454 nM. Cardamonin does not significantly reduce HEK293 cell viability, nor does it impair cardiomyocyte constriction[1]. In vitro, cardamonin (25 and 50 μM) concentration dependently inhibits endothelium permeability and down-regulates phosphorylation of P38 in rat lung microvascular endothelial cells induced by lipopolysaccharide (LPS). In RAW 264.7 macrophage cells, cardamonin also shows selective inhibition of P38 phosphorylation induced by LPS[2]. Cardamonin inhibits the growth of several cancer cell types including breast cancer, glioblastoma, ovarian, prostate, and lung. Treatment of cardamonin in CRC cell lines induces cell cycle arrest mostly in the S phase of cell cycle. It activates both apoptosis and induces cell cycle arrest to inhibit the cell proliferation. Cardamonin is known to inhibit various signaling pathways which play a major role in the process of inflammation and cancer. This natural product inhibits the phosphorylation and translocation of both STAT3 and NF-κB. Cardamonin also inhibits angiogenesis through downregulation of miR-21 expression[3]. |
| In Vivo | Cardamonin (30 and 100 mg/kg) significantly elevates the survival rate of septic mice, alleviates ALI and lung microvascular leak, and lowers the serum levels of proinflammatory cytokines TNF-α, IL-1β,and IL-6[2]. Cardamonin inhibits Azoxymethane-induced colorectal cancer (CRC). Its treatment inhibits the tumor incidence, tumor multiplicity, Ki-67 and β-catenin positive cells. The preclinical pharmacokinetics and ADME characterization of cardamonin in mice reports that cardamonin is highly permeable with an effective permeability value in ileum is (Peff) 3?×?10?4 which is highly significant. Within 30?minutes of oral dosing, cardamonin is distributed to various tissues[3]. |
| SMILES | COC1=CC(O)=CC(O)=C1C(=O)C=CC1=CC=CC=C1 |
| 靶点 | Calcium Channel |
| 动物实验 | Animal Models: Male ICR mice; Dosages: 0, 30, and 100 mg/kg; Administration: oral[2] |
| 细胞实验 | Endothelial cells are preincubated with different concentrations of cardamonin for 12 h. Then, Trypan blue-labeled BSA is added into the upper compartments of Transwell membranes. Thirty minutes later, cells are stimulated by LPS (1 μg/mL) for 1 h. Trypan blue dye content in the lower compartment is assayed by spectrophotometry at 590 nm and expressed as a percentage of the maximum concentration that would have been achieved at equilibrium.[2] |
| 数据来源文献 | [1] Wang S, et al. Molecules. 2016, 21(9). pii: E1145. [2] Wei Z, et al. J Biochem Mol Toxicol. 2012, 26(7):282-90. [3] Shirley James, et al. Scientific Reports. 2017, 7: 13945. |
| 规格 | 5mg 10mM*1mL in DMSO 10mg |
是一种新型的hTRPA1离子通道拮抗剂。