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Meleagrin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Meleagrin图片
CAS NO:71751-77-4
包装与价格:
包装价格(元)
1mg电议
5mg电议

产品介绍

化学性质

Physical AppearanceA light tan to tan solid
StorageStore at -20°C
M.Wt433.5
Cas No.71751-77-4
FormulaC23H23N5O4
Synonyms6-O-Methyloxaline
SolubilitySoluble in ethanol;Soluble in methanol;Soluble in DMSO;Soluble in dimethyl formamide
Chemical Name(3E,7aR,12aS)-7a-(1,1-dimethyl-2-propen-1-yl)-7a,12-dihydro-6-hydroxy-3-(1H-imidazol-5-ylmethylene)-12-methoxy-1H,5H-imidazo[1',2':1,2]pyrido[2,3-b]indole-2,5(3H)-dione
Canonical SMILESOC1=CC2(C(C)(C)C=C)C3(N(OC)C4=C2C=CC=C4)N(/C(C(N3)=O)=C\C5=CNC=N5)C1=O
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。

资料参考

MIC: 32-64 μg/ml for S. aureus, E. coli, and S. pneumoniae

Meleagrin is an antibiotic.

Meleagrin is an antibiotic derived from a deep ocean, penicillin-producing P. chrysogenum.

In vitro: It was found that consistent with their selective inhibition of Staphylococcus aureus FabI, meleagrin and its more active derivatives could directly bind to S. aureus FabI that was measured in a fluorescence quenching assay, inhibit intracellular fatty acid biosynthesis and growth of S. aureus, and increase the minimum inhibitory concentration (MIC) for fabI-overexpressing S. aureus. The compounds that were not effective against the FabK isoform, however, were able to inhibit the growth of Streptococcus pneumoniae containing only the FabK isoform. In addition, no resistant mutant to these compounds was obtained. Notely, fabK-overexpressing Escherichia coli was found to be not resistant to these compounds, but was resistant to triclosan [1]. Another study found that meleagrin was able to inhibit the growth of the human breast cancer cell lines, while similar treatment doses had no effect on the growth and viability of the non-tumorigenic human mammary epithelial cells MCF10A. Meleagrin also displayed good ATP competitive c-Met inhibitory activity in Z-Lyte assay [2].

In vivo: Up to now, there is no animal in vivo data reported.

Clinical trial: So far, no clinical study has been conducted.

References:
[1] Zheng, C. J.,Sohn, M.J.,Lee, S., et al. Meleagrin, a new FabI inhibitor from Penicillium chryosogenum with at least one additional mode of action. PLoS One 8(11), (2013).
[2] Mady MS et al.  The indole alkaloid meleagrin, from the olive tree endophytic fungus Penicillium chrysogenum, as a novel lead for the control of c-Met-dependent breast cancer proliferation, migration and invasion. Bioorg Med Chem. 2016 Jan 15;24(2):113-22.

试验操作

细胞实验 [1]:

细胞系

人类乳腺癌细胞系

溶解方法

在DMSO中是可溶的。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

0~50 μM

应用

Meleagrin抑制人乳腺癌细胞MDA-MB-231,MDA-468,BT-474,SK BR-3,MCF7和MCF7-dox的生长,同时发现相似的治疗剂量对非致瘤性人乳腺上皮细胞MCF10A的生长和生存力没有影响。Meleagrin在Z-Lyte分析中还表现出出色的ATP竞争性c-Met抑制活性,这已通过分子对接研究和Western blot分析进一步证实。

References:

[1]. Mady MS, Mohyeldin MM, Ebrahim HY, Elsayed HE, Houssen WE, Haggag EG, Soliman RF, El Sayed KA. The indole alkaloid meleagrin, from the olive tree endophytic fungus Penicillium chrysogenum, as a novel lead for the control of c-Met-dependent breast cancer proliferation, migration and invasion. Bioorg Med Chem. 2016 Jan 15;24(2):113-22. doi: 10.1016/j.bmc.2015.11.038. Epub 2015 Nov 28. PMID: 26692349; PMCID: PMC4703546.