盐屋霉素A
中文名称 | 盐屋霉素A |
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中文同义词 | 盐屋霉素A;盐霉素 A;硅霉素A |
英文名称 | siomycin A |
英文同义词 | Antibiotic 6741-21;Mutabillicin;Mutabilycin;siomycin A;Mutabilycin, SporangioMycin, 6741-21, Mutabillicin;AKFVOKPQHFBYCA-OFENGFFDSA-N;Alaninamide, N-[(7R,8S)-2-carboxy-7,8-dihydro-8-hydroxy-4-[(1S)-1-hydroxyethyl]-7-quinolinyl]-L-valyl-2,3-didehydroalanyl-2,3-didehydroalanyl-L-alanyl-2-[(4aR,11S,14Z,18S,21S,28S,32aS)-4a-amino-21-[(1S,2R)-1,2-dihydroxy-1-methylpropyl]-14-ethylidene-3,4,4a,9,10,11,12,13,14,18,19,20,21,27,28,32a-hexa...;Salomycin A |
CAS号 | 12656-09-6 |
分子式 | C71H81N19O18S5 |
分子量 | 1648.84 |
EINECS号 | |
相关类别 | 微生物代谢物 |
Mol文件 | 12656-09-6.mol |
结构式 |
盐屋霉素A 性质
密度 | 1.65±0.1 g/cm3(Predicted) |
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储存条件 | -20°C |
溶解度 | 完全溶于DMSO,溶解度为10mg/ml,透明,无色至淡黄色 |
形态 | 白色固体。 |
酸度系数(pKa) | 10.43±0.46(Predicted) |
Forkhead box M1(FOXM1)
Siomycin A (0-10 µM; 24-72 hours; K562, MCF7 and MiaPaCa-2 cells) treatment markedly reduces cell viability in a dose-dependent and a time-dependent association in K562, MCF7 and MiaPaCa-2 cells. Among the three cell lines, the
IC
50
of the human leukemia K562 cells is the lowest at 6.25 µM at 24 h, while that for the human pancreatic cancer MiaPaCa-2 cells is 6.38 µM. However, the
IC
50
of the human pancreatic cancer MiaPaCa-2 cells at 48 and 72 h are the lowest of the three cell lines, which are 0.76 and 0.54 µM, respectively.
Siomycin A (0-10 µM; MiaPaCa-2 cells) treatment has potent proapoptotic effect in MiaPaCa-2 cells.
Siomycin A (0-10 µM; 24 hours; MiaPaCa-2 cells) treatment significantly reduces the expression levels of MMP-2, MMP-9 and α-tubulin protein in the MiaPaCa-2 cells.
Cell Viability Assay
Cell Line: | K562, MCF7 and MiaPaCa-2 cells |
Concentration: | 0 µM, 0.625 µM, 1.25 µM, 2.5 µM, 5 µM or 10 µM |
Incubation Time: | 24, 48 and 72 hours |
Result: | Cell viability was markedly reduced in a dose-dependent and a time-dependent association. |
Apoptosis Analysis
Cell Line: | MiaPaCa-2 cells |
Concentration: | 0 µM, 0.625 µM, 1.25 µM, 2.5 µM, 5 µM or 10 µM |
Incubation Time: | |
Result: | Promoted apoptosis of MiaPaCa-2 cells. |
Western Blot Analysis
Cell Line: | MiaPaCa-2 cells |
Concentration: | 0 µM, 0.625 µM, 1.25 µM, 2.5 µM, 5 µM or 10 µM |
Incubation Time: | 24 hours |
Result: | The expression levels of MMP-2 and MMP-9 protein in the MiaPaCa-2 cells were significantly reduced in the 2.5, 5 and 10 µM groups. |
Siomycin A (1 µM; subcutaneous injection; for 4 weeks; male Balb/c nude mice) pretreatment decreases tumour growth in an in vivo mouse model.
Animal Model: | Four- to five-week old male Balb/c nude mice with IOMM-LEE cells |
Dosage: | 1 µM-pretreated IOMM-Lee cells |
Administration: | Subcutaneous injection; for 4 weeks |
Result: | Decreased tumour growth in an in vivo mouse model. |
安全信息
WGK Germany | 3 |
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