(5E)-7-Oxozeaenol is a resorcylic acid lactone that has been found in the fungus MSX 63935 and has enzyme inhibitory and anticancer activities.1,2 It inhibits TGF-β-activated kinase 1 (TAK-1; IC50 = 1.3 μM).1 (5E)-7-Oxozeaenol inhibits proliferation of MCF-7, H460, SF-268, HT-29, and MDA-MB-435 human cancer cells with IC50 values of 4.9, 1.2, 5.6, 4.4, and 5.5 μM, respectively.2 |1. Fakhouri, L., El-Elimat, T., Hurst, D.P., et al. Isolation, semisynthesis, covalent docking and transforming growth factor beta-activated kinase 1 (TAK1)-inhibitory activities of (5Z)-7-oxozeaenol analogues. Bioorg. Med. Chem. 23(21), 6993-6999 (2015).|2. Ayers, S., Graf, T.N., Adcock, A.F., et al. Resorcylic acid lactones with cytotoxic and NF-κB inhibitory activities and their structure-activity relationships. J. Nat. Prod. 74(5), 1126-1131 (2011).
Malformin A is a cyclopentapeptide fungal metabolite that has been found in A. niger and has diverse biological activities. It is a plant growth regulator that induces malformations in plant structure. Malformin A inhibits replication of tobacco mosaic virus (TMV) in local lesion and leaf-disc assays (IC50s = 19.7 and 45.4 μg/ml, respectively). It is cytotoxic to NCI-H460, MIA PaCa-2, MCF-7, SF-268, and WI-38 cancer cells (IC50s = 70, 50, 100, 70, and 100 nM, respectively), inhibits proliferation of PC3 and LNCaP cells (IC50s = 130 and 90 nM, respectively), and induces apoptosis and necrosis in PC3 and LNCaP cells. Malformin A also increases the accumulation of reactive oxygen species, decreases the mitochondrial membrane potential, and induces autophagy in PC3 and LNCaP cells. It is toxic to mice when administered intraperitoneally (LD50 = 3.1 mg/kg) but not orally up to doses of 50 mg/kg.
Unguinol is a depsidone originally isolated from A. unguis. It is an inhibitor of pyruvate phosphate dikinase (PPDK; IC50 = 42.3 μM). It inhibits the growth of plants utilizing C4, but not C3, carbon fixation. Unguinol also inhibits the growth of the bacteria S. aureus and V. harveyi (GI50s = 8.7 and 69.5 μM, respectively) and H460, MCF-7, and SF-268 cancer cells (GI50s = 28.2, 50.8, and 44.3 μM, respectively).
3-Oxobetulin acetate is a derivative of the cholesterol biosynthesis inhibitor betulin. It inhibits the growth of P388 murine lymphocytic leukemia cells (EC50 = 0.12 µg ml), as well as human MCF-7 breast, SF-268 CNS, H460 lung, and KM20L2 colon cancer cells (GI50s = 8, 10.6, 5.2, and 12.7 µg ml, respectively), but not BxPC-3 pancreas or DU145 prostate cancer cells (GI50s = >10 µg ml for both). 3-Oxobetulin acetate inhibits replication of X4 tropic recombinant HIV (NL4.3-Ren) in MT-2 lymphoblastoid cells (IC50 = 13.4 µM). It is also active against L. donovani amastigotes when used at a concentration of 50 µM.
Glochidiol exhibits strong inhibitory effects against all three human tumor cell lines (MCF-7, NCI-H-460 and SF-268), it exerts its antiproliferative activity through the involvement of apoptosis. It exhibits a strong inhibitory effect on mouse skin tumor
Glochidonol exhibits strong inhibitory effects against three human tumor cell lines, MCF-7, NCI-H-460 and SF-268, the GI(50) values of 9.0 +/- 3.7, 4.9 +/- 0.2 and 9.8 +/- 0.5, respectively; it also exerts its antiproliferative activity through the involv