Fumagillol

Fumagillol is a sesquiterpenoid that has been found in P. jensenii and has diverse biological activities.^1,2,3,4 It is an inhibitor of methionyl aminopeptidase 2 (METAP2; IC₅₀ = 230 nM for the human enzyme).¹ Fumagillol is active against the parasite G. lamblia (IC₅₀ = 3.4 µM).² It reduces the proliferation of isolated calf pulmonary artery endothelial cells (IC₅₀ = 8.09 µM) and human umbilical vein endothelial cells (HUVECs; EC₅₀ = 49 nM).^3,1 Fumagillol inhibits the proliferation of isolated mouse splenocytes in a mixed lymphocyte reaction (IC₅₀ = 250 nM).⁴

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1. Fardis, M., Pyun, H.-J., Tario, J., et al. Design, synthesis and evaluation of a series of novel fumagillin analogues. Bioorg. Med. Chem. 11(23), 5051-5058 (2003).

2. Padia, J., Kulakova, L., Galkin, A., et al. Discovery and preclinical development of antigiardiasis fumagillol derivatives. Antimicrob. Agents Chemother. 64(10), e00582-00520 (2020).

3. Kim, D., Min, J., Ahn, S.K., et al. 5-Demethoxyfumagillol, a potent angiogenesis inhibitor isolated from Aspergillus fumigatus. Chem. Pharm. Bull. (Tokyo) 52(4), 447-450 (2004).

4. Hatanaka, H., Hashimoto, M., Tsurimi, Y., et al. FR65814, a novel immunosuppressant isolated from a Penicillium strain. Taxonomy, fermentation, isolation, physico-chemical and biological characteristics and structure assignment. J. Antibiot. (Tokyo) 41(8), 999-1008 (1988).