| CAS NO: | 13220-57-0 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 248.2 |
| Cas No. | 13220-57-0 |
| Formula | C15H8N2O2 |
| Synonyms | NSC 349447 |
| Solubility | ≤30mg/ml in DMSO;30mg/ml in dimethyl formamide |
| Chemical Name | indolo[2,1-b]quinazoline-6,12-dione |
| Canonical SMILES | O=C1N2C(C(C3=C2C=CC=C3)=O)=NC4=C1C=CC=C4 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
Tryptanthrin, a weakly basic alkaloid tryptophan derivative originally isolated from the dried roots of medicinal indigo plants, has anti-inflammatory and anticancer activities. And, tryptanthrin blocks 5-lipoxygenase (5-LO) and cyclooxygenase-2 (Cox-2) with IC50 values of 600 and 64 nM, respectively.
5-LO and Cox-2 are involved in cancer pathobiology. 5-LO is expressed by a variety of cancer cells including colon, lung, breast, and prostate and promotes cancer cell growth and neo-angiogenesis. Cox-2, overexpressed in cancer cells, promotes tumorigenesis and induces neo-angiogenesis.
In vitro: In human hepatocyte-derived HepG2 cells, tryptanthrin inhibited the reactive oxygen species formation, mitochondrial dysfunction, and cell death triggered by tert-butyl hydroperoxide (tBHP). Furthermore, tryptanthrin reversed the reduction of glutathione (GSH) induced by tBHP. Specifically, nuclear translocation, transactivation of nuclear factor erythroid 2-related factor 2 (Nrf2), and phosphorylation of extracellular signal-regulated kinase (ERK) were evoked by the treatment of tryptanthrin. Additionally, the expression of the heme oxygenase 1 and glutamate was upregulated by tryptanthrin [1].
In vivo: BALB/c (H-2d) mice, intraperitoneally (i.p.) inoculated with leukemia WEHI-3B JCS cells, were injected i.p with tryptanthrin at doses of 0.04 mg/kg, 0.08 mg/kg and 0.16 mg/kg body weight for 5 consecutive days. Tryptanthrin inhibited the growth of WEHI-3B JCS cells in BALB/c mice, and at the dosages of 0.08 mg/kg and 0.16 mg/kg, significant inhibition was seen. Moreover, tryptanthrin, in a dose-dependent fashion, triggered cell cycle arrest of the WEHI-3B JCS cells at G0/G1 phase [2].
References:
[1]. Moon, S., Lee, J., Choi, H., Cho, I., Kim, S., & Kim, Y. Tryptanthrin Protects Hepatocytes against Oxidative Stress via Activation of the Extracellular Signal-Regulated Kinase/NF-E2-Related Factor 2 Pathway. Biological and Pharmaceutical Bulletin. 2014; 37(10): 1633-1640.
[2]. Chan, H., Yip, H., Mak, N., & Leung, K. Modulatory Effects and Action Mechanisms of Tryptanthrin on Murine Myeloid Leukemia Cells. Cellular and Molecular Immunology. 2009; 6(5): 335-342.
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