s. faecalis

Dermaseptin acetate, a peptide isolated from frog skin, exhibits potent antimicrobial activity against bacteria, fungi, and protozoa at micromolar concentration[1].

Gentamicin sulfate (SCH9724) is a broad-spectrum, orally administered aminoglycoside antibiotic that exhibits inhibitory activity against aerobic Gram-negative bacteria by interfering with mRNA translation.

Sclareolide (Norambreinolide) is a sesquiterpene lactone natural product derived from various plant sources including Salvia yosgadensis, Salvia sclarea, and cigar tobacco. It is a close analog of Sclareol, a plant antifungal compound.

Cefuroxime (Cephuroxime) is an orally active second-generation cephalosporin antibiotic with antimicrobial activity that inhibits both Gram-positive and Gram-negative bacteria, and is used in the study of soft tissue infections.

Blasticidin S HCl is a natural product and an inhibitor of protein synthesis. Blasticidin S HCl is a broad-spectrum antibiotic that can inhibit the cell growth of prokaryotes, fungi, plants and mammalian cells.

Cefuroxime Sodium is the sodium salt form of cefuroxime and a semi-synthetic, broad-spectrum, beta-lactamase resistant, second-generation cephalosporin antibiotic with bactericidal activity. Cefuroxime sodium (Cefuroxime sodium salt) inhibits bacterial cell wall synthesis by inactivating penicillin binding proteins (PBPs) thereby interfering with the final transpeptidation step required for cross-linking of peptidoglycan units which are a component of the cell wall. Lack of cross-linking results in a reduction of cell wall stability and leads to cell lysis.

Thiocillin I, a thiopeptide antibiotic, demonstrates potent in vitro antibacterial effects against Gram-positive bacteria. This compound exhibits minimum inhibitory concentrations (MICs) of 2 μg/mL, 0.5 μg/mL, 4 μg/mL, and 0.5 μg/mL against S. aureus 1974149, E. faecalis 1674621, B. subtilis ATCC 6633, and S. pyogenes 1744264, respectively.

Antibacterialagent 256 (Compound C09) is an inhibitor of Type I signal peptidase (SPase I). It targets Gram-positive bacteria, effectively inhibiting S. aureus ATCC 29213, E. faecium QF31, E. faecalis SF23-1, and S. suis P1/7, with MIC values ranging from 1-16 μg/mL. In cancer cells HEp-2 and Caco-2, Antibacterialagent 256 exhibits cytotoxicity with CC50 values of 14.65 μg/mL and 21.93 μg/mL, respectively. Additionally, it shows hemolytic activity on mouse red blood cells with an HC50 of 13.29 μg/mL and can improve MRSA skin infections in mouse models.

Gramicidin S 2HCl, is an antibiotic. At concentrations of 40-80 μg/mL, GS can reduce planktonic cell numbers within 20-40 minutes. For established biofilms, it effectively kills cells at concentrations of 100-200 μg/mL without regrowth. This anti-biofilm effect results from peptide transmembrane transport and complexation with intracellular nucleotides (including the alarmone ppGpp). GS demonstrates wide-ranging activity against biofilm-forming, drug-resistant infections caused by E. faecalis, proving its efficacy in endodontic treatment. The successful treatment of persistent infections in two volunteer cases further confirms GS's potent therapeutic performance. These studies indicate that GS can be applied in certifying compounds used in endodontics.

Antimicrobial agent-35 (Compound c9) demonstrates antibacterial activity, effectively inhibiting S. aureus, E. coli, E. faecalis, and S. maltophilia with a MIC of 0.5-2 μg/mL. Additionally, Antimicrobial agent-35 shows cytotoxicity towards HT-22 cells, with an IC50 value of 130.4 μg/mL.

ROS inducer 8 (Compound 11g) acts as an inhibitor of glutathione (GSH) and promotes the accumulation of reactive oxygen species (ROS) in Enterococcus faecalis, exhibiting antibacterial properties. It is capable of disrupting biofilms and inhibiting S. aureus and E. faecalis with minimum inhibitory concentrations (MICs) of 8 μg/mL and 2 μg/mL, respectively, demonstrating a post-antibiotic effect. Additionally, ROS inducer 8 shows low hemolytic toxicity on sheep red blood cells with an HC50 greater than 1280 μg/mL.

Florfenicol-propanoate-piperidin (Compound 1) is a derivative of Florfenicol. This compound exhibits antibacterial activity, effectively inhibiting strains such as E. coli ATCC25922, Salmonella CICC110420, S. aureus ATCC29213, B. subtilis CMCC(B)63501, E. faecalis ATCC29212, S. suis CVCC606, and Haemophilus parasuis, with a minimum inhibitory concentration (MIC) ranging from 2 to 8 μM.

Pyrrofolic acid shows high anti-folate biological activity for S. faecalis.

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, 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).