Thiocillin I is a thiopeptide antibiotic and has in vitro antibacterial activity against Gram-positive bacterial strains(MIC of Thiocillin I against S. aureus 1974149, E. faecalis 1674621, B. subtilis ATCC 6633 and S. pyogenes 1744264 are 2 μg/mL, 0.5 μg/mL, 4 μg/mL and 0.5 μg/mL, respectively).
Leucomycin a5 is a metabolite from the leucomycin complex, which was originally isolated from S. kitasatoensis. It is active against a variety of Gram-positive and Gram-negative bacteria (MICs = 0.04-0.8 µg/ml) but not against K. pneumoniae, S. typhimuriu
10'-Desmethoxystreptonigrin is an antibiotic originally isolated from Streptomyces and a derivative of the antibiotic streptonigrin. It is active against a variety of bacteria, including S. aureus, S. faecalis, E. coli, K. pneumoniae, and P. vulgaris (MICs = 0.4, 1.6, 3.1, 3.1 and 0.4 μg/ml, respectively). 10'-Desmethoxystreptonigrin is cytotoxic to HCT116 colon and A2780 ovarian cancer cells (IC50s = 0.004 and 0.001 μg/ml, respectively), as well as HCT116 cells resistant to etoposide and teniposide and cisplatin-resistant A2780 cells (IC50s = 0.003, 0.001, and 0.01 μg/ml, respectively). 10'-Desmethoxystreptonigrin is also an inhibitor of p21ras farnesylation (IC50 = 21 nM).
Aszonapyrone A is a meroditerpene fungal metabolite that has been found in Neosartorya and has diverse biological activities.1,2,3 It inhibits the growth of MCF-7, NCI H460, and A375-C5 cancer cells (GI50s = 13.6, 11.6, and 10.2 μM, respectively).1 Aszonapyrone A is active against multidrug-resistant isolates of S. aureus, E. faecalis, and E. faecium (MICs = 8, 16, and 16 μg/ml, respectively) and inhibits S. aureus biofilm formation.2 It is also active against P. falciparum in vitro (IC50 = 1.34 μg/ml).3
Flumequine-13C3 is intended for use as an internal standard for the quantification of flumequine by GC- or LC-MS. Flumequine (T1060) is a fluoroquinolone antibiotic.1It is active againstS. aureus,S. pyogenes,B. subtilis,E. coli,P. aeruginosa,S. faecalis,andK. pneumoniae (MICs = 1-100 μg/ml). Flumequine (T1060) is also active against field isolates of B. hyodysenteriae (MICs = 6.25-200 μg/ml).2It inhibits DNA gyrase,disrupting supercoiling of bacterial DNA to block transcription and replication.3
Quinaldopeptin is a quinomycin antibiotic. It is active against a variety of bacteria, including S. pyogenes, S. aureus, C. perfringens, S. faecalis, E. coli, and K. pneumoniae (MICs = 0.2, 0.4, 0.8, 1.6, 3.1 and 6.3 μg/ml, respectively). It is cytotoxic to B16/F10 and Moser cells (IC50s = 0.0008 and 0.04 μg/ml, respectively) and increases survival in a P388 leukemia mouse model. Quinaldopeptin is a bis-intercalator depsipeptide (NPBID) that binds to and intercalates into DNA (Kd = 32 nM).
Leoidin is a depsidone originally isolated from L. gangaleoides that has antibacterial and enzyme inhibitory activities.1,2,3 It is active against the bacteria E. faecalis, H. influenzae, M. catarrhalis, S. aureus, and S. pneumoniae (MICs = 8, 32, 1, 128, and 64 μg/ml, respectively).2 Leoidin inhibits phenylalanyl-tRNA synthetase (PheRS) isolated from P. aeruginosa (IC50 = 42 μM). It also inhibits organic anion-transporting polypeptide 1B1 (OATP1B1) and OATP1B3 with Ki values of 0.08 and 1.84 μM, respectively, in CHO cells expressing the human transporters.3
Betulinic aldehyde oxime is a pentacyclic triterpenoid and derivative of the cholesterol biosynthesis inhibitor betulin .1It is active againstE. aerogenes,E. coli,E. faecalis,P. aeruginosa,S. aureus, andC. albicans, as well asL. donovaniamastigotes, when used at a concentration of 50 μM.1,2Betulinic aldehyde oxime (50 μM) is cytotoxic to Huh7 hepatocellular carcinoma cells.2
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
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)
Siamycin I is a tricyclic peptide originally isolated from Streptomyces and has antiviral and antibacterial activities. It is active against laboratory strains and clinical isolates of HIV-1 (ED50s = 0.05-0.45 and 0.89-5.7 μM, respectively), as well as the CBL-20 strain of HIV-2 (ED50 = 0.45 μM), in vitro. Siamycin I inhibits HIV-induced fusion of C8166 T cells with HIV-1-infected CEM-SS cells with an ED50 value of 0.08 μM. It is also active against B. subtilis, M. luteus, and S. aureus (MICs = 1.6-6.3 μg/ml). Siamycin I inhibits autophosphorylation of the E. faecalis quorum sensing kinase FsrC induced by gelatinase biosynthesis-activating pheromone (GBAP).