洋橄榄叶素

洋橄榄叶素

中文名称洋橄榄叶素
中文同义词洋橄榄叶素;阿扎霉素
英文名称elaiophylin
英文同义词elaiophylin;Azalomycin B;EfoMycin E;EfoMycine E;GopalaMicin;255-E, 5001B, 56-62, 846 I, SNA 4606-3, AzaloMycin B, GopalaMicin, SalboMycin;Elaiophylin (Azalomycin B);Salbomycin
CAS号37318-06-2
分子式C54H88O18
分子量1025.27
EINECS号
相关类别微生物代谢物;中药对照品
Mol文件37318-06-2.mol
结构式洋橄榄叶素 结构式

洋橄榄叶素 性质

熔点179-182℃
沸点1080.5±65.0 °C(Predicted)
密度1.25
储存条件-20°C Freezer
溶解度可溶于DMSO(少许)、甲醇(少许)
酸度系数(pKa)12.18±0.70(Predicted)
形态白色至类白色固体。
颜色白色至类白色

洋橄榄叶素 用途与合成方法

盐霉素(Salinomycin)是由白色链霉菌经发酵产生的聚醚类动物专用抗生素,具有防治动物球虫病和促进畜禽生长发育的功能,被广泛地用于国内外的畜牧业中。但是,在盐霉素产品中,如果发酵工艺或菌种发生变化,将会有洋橄榄叶素的伴生,当含量超出一定限度,将对饲养对象产生不良反应,一定程度上会影响盐霉素的使用效果。洋橄榄叶素是一种微生物代谢物,可用作对照品。Elaiophylin (Azalomycin B; Gopalamicin; Efomycin E) 是一种自噬 (autophagy) 抑制剂,在卵巢癌细胞中作为单一药剂发挥抗肿瘤活性。

Autophagy

Elaiophylin-mediated autophagy inhibition and lysosomal dysfunction affect ovarian cancer cell survival during hypoxia. Exposure to Elaiophylin (0.025-0.5 μM; 24 hours) causes a significant increase in ovarian cancer SKOV3 cell death in hypoxia conditions.
In both the SKOV3 and A2780 cell lines, Elaiophylin (0.25, 0.5, 0.75 μM; 24 hours) treatment leads to significant activation of cleaved CASP9/caspase-9 and PARP1 and downregulation of BIRC5/survivin in a concentration-dependent manner.

Cell Viability Assay

Cell Line: Ovarian cancer SKOV3 cells.
Concentration: 0.025, 0.05, 0.1, 0.2, 0.5 μM
Incubation Time: 24 hours
Result: Caused a significant increase in ovarian cancer SKOV3 cells death in hypoxia conditions.

Western Blot Analysis

Cell Line: Ovarian cancer SKOV3 cells; A2780 cells
Concentration: 0.25, 0.5, 0.75 μM
Incubation Time: 24 hours
Result: Treatment led to significant activation of cleaved CASP9/caspase-9 and PARP1 and downregulation of BIRC5/survivin in a concentration-dependent manner.

Treatment with 2 mg/kg Elaiophylin (given i.p. every 2 days for 21 days; in BALB/C athymic mice) significantly suppresses ovarian cancer SKOV3 cells growth compared with DMSO treatment, resulting in a 72% decrease in the average daily tumor growth rate compared with DMSO treatment .
Lower doses of Elaiophylin as a single agent exert significant antitumor activity, while higher doses lead to intestinal toxicity. Administration of a lower dose (2 mg/kg) of Elaiophylin as a single agent achieves a significant antitumor effect without toxicity in an orthotopic ovarian cancer model with metastasis. Toxic reactions are observed only in the 8 mg/kg group.

Animal Model: 4-wk-old BALB/C athymic mice with ovarian cancer SKOV3 cells
Dosage: 1 or 2 mg/kg
Administration: Given i.p. every 2 days for 21 days
Result: Treatment with 2 mg/kg significantly suppressed ovarian cancer SKOV3 cells growth compared with DMSO treatment.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/01/25HY-15184洋橄榄叶素
Elaiophylin
37318-06-21mg1050元
2024/01/25HY-15184洋橄榄叶素
Elaiophylin
37318-06-25mg3200元

洋橄榄叶素 上下游产品信息

"洋橄榄叶素"相关产品信息
beta-七叶素 阿西替尼 伯舒替尼 PCI-24781 CHIR-99021
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