Elaiophylin

Research use only, not for human use.

Elaiophylin shows antiprotozoal activity against Plasmodium falciparum K1a and Trypanosoma brucei brucei GUTat 3.1 strains with IC50 of 0.36 μM and 0.45 μM, respectively.

Elaiophylin is a macrolide antibiotic first isolated from Streptomyces melanosporus. Elaiophylin demonstrates antifungal activity as well as cytotoxicity against mammalian tumor cells, protozoa, and nematodes. This compound has displayed immunosuppressive activity through inhibition of B-cell stimulation and inhibiting proliferation of lymphocytes stimulated by mitogens. Elaiophylin is an inhibitor of 5 α-Reductase and NOS.

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.

Elaiophylin

Others

Other Targets

Others

Others-Field

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37318-06-2

1025.27

C54H88O18

>98% (HPLC)

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CC[C@H]1[C@@H](C[C@](O[C@@H]1C)(O)[C@H]([C@H](O)[C@@H]([C@H]2OC(=O)/C=C/C=C/[C@@H]([C@H](OC(=O)/C=C/C=C/[C@@H]2C)[C@H]([C@@H](O)[C@@H]([C@@]3(O[C@@H]([C@H]([C@@H](C3)O[C@@H]4O[C@H]([C@H]([C@H](C4)O)O)C)CC)C)O)C)C)C)C)C)O[C@@H]5O[C@H]([C@H]([C@H](C5)O)O)C

(3E,5E,7S,8S,11E,13E,15S,16S)-8,16-bis((2S,3R,4S)-4-((2R,4R,5R,6R)-4-(((2R,4S,5S,6S)-4,5-dihydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-5-ethyl-2-hydroxy-6-methyltetrahydro-2H-pyran-2-yl)-3-hydroxypentan-2-yl)-7,15-dimethyl-1,9-dioxacyclohexadeca-3,5,11,13-tetraene-2,10-dione

(-20℃)

With Ice Pack

≥ 2 years