virulence

MAC-545496 is a glycopeptide-resistance-associated protein R (GraR) inhibitor, is an antivirulence agent.

4-(tert-Butyl)-benzhydroxamic Acid is a PqsR antagonist with IC50s of 12.5 μM and 23.6 μM for E. coli and P. aeruginosa, respectively, and it reduces the production of the virulence factor pyocyanin in P. aeruginosa with an IC50 of 87.2 μM[1].

Anti-virulence factor-IN-2 (compound C7) is an inhibitor targeting the virulence factor KpsM in Escherichia coli. KpsM facilitates the translocation of capsular polysaccharides to the cell surface, enabling KpsM-positive E. coli to evade phagocytosis by the scavenger receptor Marco on liver Kupffer cells, promoting bacterial dissemination. These bacteria can exacerbate ethanol-induced liver disease. Anti-virulence factor-IN-2 demonstrates anti-infective activity by inhibiting KpsM-dependent capsulation in a mouse model of ethanol-induced liver disease. This compound is applicable for alcoholic hepatitis research.

D-Cysteine, the D-isomer of cysteine, is a powerful inhibitor of E. coli growth and is mediated by D-amino acid oxidase to produce H2S, serving as a neuroprotective agent against cerebellar ataxia. Additionally, D-cysteine can inhibit the growth and cariogenicity of a two-species biofilm formed by Streptococcus mutans and Streptococcus hemoglobin.

Clindamycin hydrochloride monohydrate (Clindamycin alcoholate) is a protein synthesis inhibitor used orally, capable of diminishing virulence factor expression in Staphylococcus aureus at sub-minimum inhibitory concentrations (sub-MICs). It acts by suppressing Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1), and alpha-haemolysin (Hla) production. Resistance to this compound emerges through enzymatic methylation at the antibiotic's 50S ribosomal subunit binding site (23S rRNA).

Sodium lauryl sulfoacetate (Sodium houttuyfonate) is anti-pseudomonas agents, inhibits virulence-related motility of Pseudomonas.

Sodium new houttuyfonate is anti-pseudomonas agents, inhibits virulence-related motility of Pseudomonas.

Methyl 2-amino-5-bromobenzoate (Methyl 5-Bromoanthranilate) is a hepatitis C virus NS5b RNA polymerase inhibitor with antimicrobial activity that inhibits Pseudomonas aeruginosa infections and is involved in the production of many virulence factors and biofilm formation.

Biotin (S)-sulfoxide is an inactive metabolite of the coenzyme biotin .1,2It has also been found inE. coliand is reduced by the biotin sulfoxide reduction system as a source of biotin.3 1.Denkel, L.A., Rhen, M., and Bange, F.-C.Biotin sulfoxide reductase contributes to oxidative stress tolerance and virulence in Salmonella enterica serovar TyphimuriumMicrobiology (Reading)159(Pt 7)1447-1458(2013) 2.Carling, R.S., and Turner, C.Methods for assessment of biotin (Vitamin B7)Laboratory assessment of vitamin status193-217(2019) 3.del Campillo-Campbell, A., Dykhuizen, D., and Clearly, P.P.Enzymic reduction of d-biotin d-sulfoxide to d-biotinMethods Enzymol.62379-385(1979)

Cyclic-di-GMP, a STING agonist and ubiquitous second messenger, regulates biofilm formation, motility, and virulence in various bacterial species.

Equisetin, an N-methylserine-derived acyl tetramic acid isolated from the terrestrial fungus Fusarium equiseti NRRL 5537, functions as a Quorum-sensing inhibitor (QSI) that specifically attenuates QS-regulated virulence phenotypes in P. aeruginosa, presenting a potent lead for treating P. aeruginosa infections without hindering bacterial growth. This tetramate-containing natural product possesses antibiotic and cytotoxic properties, effectively inhibiting the growth of Gram-positive bacteria and HIV-1 integrase activity, yet it does not impact Gram-negative bacteria.

Cyclo(L-Pro-L-Val), a 2,5-diketopiperazine extracted from the fruits of Mycobacterium chiliolyticum AZ2 and Mycobacterium leprae, possesses anti-inflammatory activity and virulence activity against phytopathogenic microorganisms (e.g., R. fascians LMG 3605) and inhibits Gram-positive plant pathogens.Cyclo(L-Pro-L-Val) significantly inhibited IKKα phosphorylation and IκBα and NF-κB activation as well as iNOS and COX-2 activation in a concentration Cyclo(L-Pro-L-Val) significantly inhibited the phosphorylation of IKKα, IKKβ, IκBα, and NF-κB, as well as the activation of iNOS and COX-2 in a concentration-dependent manner, and is a potential therapeutic agent for the treatment of inflammation-related diseases.

Inz-5 is a fungal-selective inhibitor of mitochondrial cytochrome bc1 that impairs fungal virulence and prevents the evolution of drug resistance.

Antibacterialagent 247 (compound 30b) is a bacterium (bacterial) antagonist that significantly inhibits the formation of biofilms by Pseudomonas aeruginosa (IC50=5.8 μM) and various virulence phenotypes. It also enhances the antibacterial activity of combined treatments with tobramycin and polymyxin B.

Quorum sensing-IN-9 (Compound 7d) inhibits quorum sensing in Pseudomonas aeruginosa by binding to the PqsR protein. It suppresses the expression of quorum sensing system-related genes lasB, rhlA, and pqsA, thereby preventing the production of virulence factors elastase, pyocyanin, and rhamnolipid. Quorum sensing-IN-9 disrupts the motility of P. aeruginosa, inhibits biofilm formation, and reduces the bacterium's virulence and pathogenicity. Additionally, it exhibits anti-infective activity in the Galleria mellonella larval model.

CYP51/Hsp90-IN-1 (Compound MM4) is a dual inhibitor of CYP51 and Hsp90. This compound exhibits antifungal activity against Candida albicans and effectively suppresses key fungal virulence factors. CYP51/Hsp90-IN-1 shows potential for research in treating invasive candidiasis.

Methyl 3-oxodecanoate exhibits virulence factor activity against human pathogens and shows effects on Synechococcus elongatus (a species of fluorescent algae) as well as on culture supernatant. Additionally, Methyl 3-oxodecanoate inhibits DNA synthesis by suppressing protein synthesis at the translation initiation level.

Antibacterialsynergist 3 is a dual-function biofilm inhibitor with an IC50 of 0.40 μM for PAO1 and 1.45 μM for PA14. It reduces virulence in Pseudomonas aeruginosa PAO1 by inhibiting the quorum sensing (QS) system and inducing iron deficiency. Additionally, Antibacterialsynergist 3 enhances the efficacy of Tobramycin and Ciprofloxacin in a mouse wound infection model. This compound is useful for research on Pseudomonas aeruginosa infections.

Hemipyocyanine (528-71-2) is the virulence factor of Gram-negative, aerobic rod bacterium Pseudomonas aeruginosa. Hemipyocyanine is an α-Amylase inhibitor.

T3SS-1-IN-1 is an inhibitor of T3SS-1. It suppresses the secretion of SipA and the activity of HilD with IC50 values of 29.2 μM and 16.9 μM, respectively. T3SS-1-IN-1 can be utilized in studies related to combating Salmonella virulence.

Antifungalagent 130 (Compound A7) is an orally active antifungal agent exhibiting significant inhibitory activity against Candida glabrata [MIC= 0.12 ng/mL] and Cryptococcus neoformans [MIC= 0.12 ng/mL]. It effectively disrupts fungal cell iron homeostasis and induces oxidative stress, leading to antifungal effects. Additionally, Antifungalagent 130 inhibits the formation of fungal virulence factors, such as biofilms, capsules, urease, and melanin. This compound shows strong antifungal properties, making it suitable for research on drug-resistant fungal infections.

Quorum sensing-IN-10 (10p) is an antimicrobial adjuvant that significantly inhibits the virulence, biofilm formation, and motility of Pseudomonas aeruginosa, while exhibiting low toxicity. It is applicable for research related to drug-resistant Pseudomonas aeruginosa infections.

PqsR-IN-3 (compound 16e) is a selective inhibitor of the pqs system (IC50=3.7 μM) and its associated virulence factor pyocyanin (IC50=2.7 μM). This compound inhibits the synthesis of bacterial biofilms and is significantly cytotoxic to Pseudomonas aeruginosa. Additionally, PqsR-IN-3 exhibits synergistic effects with various antibiotics, such as Ciprofloxacin and Tobramycin.

MoTPS1/2-IN-1 (Compound A1-4) is a dual-specificity inhibitor targeting MoTps1 and MoTps2. It demonstrates antifungal properties, effectively inhibiting the growth and virulence of both B. cinerea and F. graminearum.