Uses
Elaiophylin is a highly characteristic metabolite produced by Streptomyces hygroscopicus. Elaiophylin inhibits testosterone 5-reductase. Elaiophylin is synergistic with its co-metabolite, rapamycin, as an antifungal. Elaiophylin also has anthelmintic and immunosuppressive activity and inhibits NO synthesis. Elaiophylin displays broad, albeit weak, biological activity against bacteria, nematodes, protozoa and mammalian tumor cells.
Uses
Elaiophylin is a macrodiolide antibiotic that can be isolated from various strains of Streptomyces. It displays in vitro anti-protozoal activity against both Plasmodium and Trypanosoma (IC50s = 370 and 460 ng/ml, respectively) and cytotoxicity against human fetal lung fibroblast MRC-5 cells (IC50 = 870 ng/ml). Elaiophylin alone has no activity against Candida, although it enhances the anti-fungal activity of rapamycin . Elaiophylin also forms stable, long-lasting ion channels in bilayer membranes that are selective for cations.
Uses
Elaiophyllin is a highly characteristic metabolite produced by Streptomyces hygroscopicus. Elaiophylin inhibits testosterone 5-reductase. Elaiophylin is synergistic with its co-metabolite, rapamycin, as an antifungal. Elaiophylin also has anthelminthic and immunosuppressive activity and inhibits NO synthesis. Elaiophylin displays broad, albeit weak, biological activity against bacteria, nematodes, protozoa and mammalian tumour cells.
Definition
ChEBI: A macrolide that is isolated from several bacteria including Streptomyces violaceoniger and other soil actinomycetes.
Biological Activity
Macrolide antibiotic inhibiting testosterone 5-reductase and plasma-proton ATPase (P-ATPase). Shows antifungal, antiprotozoal, antitumor, antihelmintic and immunosuppressive activity.
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 [1].
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[1].
| Animal Model: | 4-wk-old BALB/C athymic mice with ovarian cancer SKOV3 cells[1] |
| 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. |
