Myxochelin A is a microbial metabolite that has been found inA. disciformisand has diverse biological activities.1It is active against Gram-positive bacteria, includingB. cereus,S. aureus, andM. luteus, but not Gram-negative bacteria or fungi in an agar diffusion assay when used at a concentration of 80 μg disc. Myxochelin A inhibits 5-lipoxygenase (5-LO) activity with an IC50value of 1.9 μM for the recombinant human enzyme.2It is cytotoxic to 26-L5 colon cancer cells when used at a concentration of 3 μg ml.3
Neospiramycin I is a macrolide antibiotic and derivative of spiramycin I.1It is active against the macrolide-sensitive KB210, but not the macrolide-resistant KB224, strain ofS. aureus(MICs = 3.12 and >100 μg/ml, respectively), as well asB. cereus,B. subtilis,M. luteus,E. coli, andK. pneumoniae(MICs = 1.56, 3.12, 3.12, 0.2, 50, and 12.5 μg/ml, respectively). Neospiramycin I binds toE. coliribosomes with an IC50value of 1.2 μM. It protects against mortality in a mouse model ofS. pneumoniaetype III infection (ED50= 399.8 mg/kg).2
Terpendole I is a fungal metabolite that has been found in A. yamanashiensis.1 It is a weak inhibitor of acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 145 μM) and is active against the bacteria B. cereus and B. subtilis (MICs = 100 μg/ml for both) but not S. aureus, P. aeruginosa, or K. pneumoniae (MICs = >200 μg/ml for all) or the fungus C. albicans (MIC = 200 μg/ml).1,2 It is cytotoxic to HeLa cells with an IC50 value of 52.6 μM.3 |1. Tomoda, H., Tabata, N., Yang, D.-J., et al. Terpendoles, novel ACAT inhibitors produced by Albophoma yamanashiensis. III. Production, isolation and structure elucidation of new components. J. Antibiot. (Tokyo) 48(8), 793-804 (1995).|2. Zhao, J.-C., Wang, Y.-L., Zhang, T.-Y., et al. Indole diterpenoids from the endophytic fungus Drechmeria sp. as natural antimicrobial agents. Phytochemistry 148, 21-28 (2018).|3. Nagumo, Y., Motoyama, T., Hayashi, T., et al. Structure-activity relationships of terpendole E and its natural derivatives. ChemistrySelect 2(4), 1533-1536 (2017).
TAN 420E is a bacterial metabolite originally isolated from Streptomyces. It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay (IC50 = 1.3 μM) and reduces thiobarbituric acid reactive substances (TBARS) in rat liver microsomes by 72% when used at a concentration of 100 μg/ml. TAN 420E is active against B. brevis, B. cereus, M. flavus, and S. aureus (MICs = 50-100 μg/ml). It is cytotoxic to P388 and KB lymphocytic leukemia cells (EC50s = 0.022 and 0.3 μg/ml, respectively).
Rugulotrosin A is an antibiotic originally isolated from Penicillium. It is active against the Gram-positive bacteria E. faecalis, B. cereus, B. subtilis, and S. aureus with 99% lethal dose (LD99) values of 1.6, 3.1, 5.5, and 200 μg ml, respectively. Rugulotrosin A is inactive against Gram-negative bacteria.
1-Undecanoyl-rac-glycerol is a monoacylglycerol that contains undecanoic acid at the sn-1 position. It completely inhibits the growth of the bacteria B. cereus, B. subtilis, M. luteus, E. faecalis, and S. aureus when used at concentrations ranging from 250 to 1,500 mg L.1 1-Undecanoyl-rac-glycerol (0.1 and 0.3 mg ml) also has antifungal activity against K. marxianus, S. cerevisiae, and C. maltosa.2
Aspergillin PZ is a fungal metabolite originally isolated from A. awamori. It induces morphological deformation of P. oryzae conidia when used at a concentration of 89 nM. Aspergillin PZ is active against S. epidermidis (MIC = 20 μM) but not S. aureus, E. coli, or B. cereus (MICs = >20 μM). It is cytotoxic to HL-60 promyelocytic leukemia cells (IC50 = 56.61 μM) but not THP-1 acute monocytic leukemia or PC3 prostate cancer cells (IC50s = >80 μM).
CAY10742 is an orally bioavailable oxadiazole antibiotic.1It is active against the Gram-positive bacteriaS. aureus,S. epidermidis,S. haemolyticus,B. cereus,B. licheniformis,E. faecalis, andE. faecium(MICs = 1-4 μg/ml), including laboratory strains and clinical isolates with varying degrees of resistance to methicillin, vancomycin, linezolid, and other antibiotics. CAY10742 (40 mg/kg) reduces the number of bacteria in mouse neutropenic thigh models of linezolid-sensitive or -resistant methicillin-resistantS. aureus(MRSA) infection. 1.Boudreau, M.A., Ding, D., Meisel, J.E., et al.Structure-activity relationship for the oxadiazole class of antibacterialsMed. Chem. Lett.11(3)322-326(2019)
Galbinic acid is a depsidone lichen metabolite that has been found in U. undulata.1,2 It is active against the Gram-positive bacteria B. cereus, B. subtilis, and S. aureus, but not S. epidermidis (MICs = 62.5, 62.5, 250, and >250 μg/ml, respectively), as well as the Gram-negative bacterium E. coli, but not S. sonnei (MICs = 125 and >250 μg/ml, respectively).3 |1. Salgado, F., Albornoz, L., Cortéz, C., et al. Secondary metabolite profiling of species of the genus Usnea by UHPLC-ESI-OT-MS-MS. Molecules 23(1), E54 (2017).|2. Elix, J.A., and Engkaninan, U. The structure of galbinic acid. A depsidone from the lichen Usnea undulata. Aust. J. Chem. 28(8), 1793-1797 (1975).|3. Sultana, N., and Afolayan, A.J. A new depsidone and antibacterial activities of compounds from Usnea undulata Stirton. J. Asian Nat. Prod. Res. 13(12), 1158-1164 (2011).
Nybomycin is a fungal metabolite originally isolated from Streptomyces sp. A717 and has antibacterial activity. It is active against B. subtilis, B. cereus, B. mycoides, M. smegmatis, and K. pneumoniae (MICs = 0.025, 2, 0.8, 0.2, and 0.003 μg/ml, respectively). Nybomycin is also active against M. tuberculosis and M. bovis (MICs = 4.5 and 1 μg/ml, respectively).
BE-24566B is a polyketide fungal metabolite originally isolated fromS. violaceusniger.1It is active againstB. subtilis,B. cereus,S. aureus,M. luteus,E. faecalis, andS. thermophilus(MICs = 1.56, 1.56, 1.56, 1.56, 3.13, and 3.13 μg/ml, respectively). BE-24566B is an endothelin (ET) receptor antagonist (IC50s = 11 and 3.9 μM for ETAand ETBreceptors, respectively).2 1.Kojiri, K., Nakajima, S., Fuse, A., et al.BE-24566B, a new antibiotic produced by Streptomyces violaceusnigerJ. Antibiot. (Tokyo)48(12)1506-1508(1995) 2.Lam, Y.K.T., Hensens, O., Helms, G., et al.L-755,805, a new polyketide endothelin binding inhibitor from an actinomyceteTetrahedron Lett.36(12)2013-2016(1995)
Phanerosporic acid is a fungal secondary metabolite originally isolated from P. chrysosporum that has antibacterial activity against B. cereus, B. subtilis, and E. coli and antifungal activity against S. cerevisiae, A. niger, O. ulmi, U. maydis, C. cucmerinum, C. cladosporioides, and B. cinerea.1 It has been used in the synthesis of macrolide derivatives.References1. Arnone, A., Assante, G., Nasini, G., et al. Phanerosporic acid, a β-resorcylate obtained from Phanerochaete chrysosporium. Phytochemistry 28(10), 2803-2806 (1989). Phanerosporic acid is a fungal secondary metabolite originally isolated from P. chrysosporum that has antibacterial activity against B. cereus, B. subtilis, and E. coli and antifungal activity against S. cerevisiae, A. niger, O. ulmi, U. maydis, C. cucmerinum, C. cladosporioides, and B. cinerea.1 It has been used in the synthesis of macrolide derivatives. References1. Arnone, A., Assante, G., Nasini, G., et al. Phanerosporic acid, a β-resorcylate obtained from Phanerochaete chrysosporium. Phytochemistry 28(10), 2803-2806 (1989).
Antibacterial agent 111 (Compound 3) exhibits potent antibacterial activity against B. cereus and K. pneumonia, with MIC values of 3.90 μg mL and 0.49 μg mL, respectively. It achieves this antibacterial effect by strongly binding to specific residues of tyrosyl-tRNA synthetase [1].
Euchrestaflavanone B shows antibacterial activity against Gram positive bacteria, Staphylococcus aureus, Bacillus subtilis and Bacillus cereus. Euchrestaflavanone B may function by inhibiting oncogenic disease, at least in part, through the inhibition of