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Elaiophylin

CAS No. : 37318-06-2

MCE 站：Elaiophylin

产品活性：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。

研究领域：Autophagy

作用靶点：Autophagy

In Vitro: 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.

In Vivo: 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.

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