hemolytic

Iptacopan hydrochloride (LNP023 hydrochloride) is an orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 of 10 nM. Iptacopan hydrochloride shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM.

Antimicrobial agent-22 (THI 6c) is a broad-spectrum, multi-target antibacterial with rapid bactericidal efficacy, effective anti-biofilm activity, and low cytotoxicity and hemolytic properties [1].

Surfactin is a potent cyclic lipopeptide biosurfactants that mediates flux of mono-and divalent cations, such as calcium, across lipid bilayer membranes, with anti-bacterial, anti-fungal, antimycoplasma and hemolytic effects.

Phenazopyridine hydrochloride (Pyridium) is used orally as a urinary tract analgesic. Side effects of phenazopyridine hydrochloride administration can include nausea, interference with the oxygen-carrying capacity of red blood cells (methemoglobinemia), hemolytic anemia as well as renal and hepatic toxicity. It is reasonably anticipated to be a human carcinogen.

Tafenoquine (WR 238605) is an antimalarial prophylactic agent with schizonticidal activity, useful in hemolytic anemia research.

Taribavirin hydrochloride is an orally active inosine monophosphate dehydrogenase inhibitor designed to concentrate within the liver to target HCV-infected hepatocytes, while minimizing distribution within red blood cells and the development of hemolytic anemia [2].

Taribavirin is an orally active inosine monophosphate dehydrogenase inhibitor designed to concentrate within the liver to target HCV-infected hepatocytes, while minimizing distribution within red blood cells (RBCs) and thereby reducing the risk of developing hemolytic anemia.

Antibacterialagent 244 is a compound that exhibits broad-spectrum antibacterial activity and oral efficacy, primarily targeting Gram-positive bacteria with a minimum inhibitory concentration (MIC) of 1-4 μg mL. It possesses low hemolytic toxicity (HC50 of 111.6 μg mL). The mode of action for Antibacterialagent 244 involves disrupting the bacterial transmembrane potential and increasing membrane permeability, which leads to the leakage of cellular contents such as DNA and proteins, ultimately causing bacterial death. This compound is useful in research related to infections caused by Gram-positive bacteria.

Benzobarbital is utilized in the treatment of convulsive forms of epilepsy, hemolytic disease of the newborn, and insomnia.

LB 11058 is a novel injectable cephalosporin featuring a C-3 pyridyl-substituted vinyl sulfide and a C-7 2-amino-5-chloro-1,3-thiazole group. This compound exhibits exceptional activity against Streptococcus pneumoniae and demonstrates similar efficacy against β-hemolytic streptococci. The inhibition pattern for LB 11058 with S. aureus is consistent, as all isolates are inhibited under this pattern.

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.

Antibacterialagent 258 (Compound 11e) is an antimicrobial agent capable of disrupting bacterial cell membranes and inhibiting various Gram-positive bacteria, with a MIC of 1-2 μg mL against Staphylococcus aureus. It exhibits low hemolytic activity and cytotoxicity, and demonstrates anti-infective properties in mouse models.

FtsZ-IN-12 (Compound 16e) is an inhibitor of filamentous temperature-sensitive mutant Z (FtsZ) that promotes the polymerization of the FtsZ protein and suppresses its GTPase activity, thus disrupting the bacterial cell division process. This compound exhibits broad-spectrum antibacterial activity, effectively inhibiting B. subtilis ATCC 9372, B. pumilus CMCC 63202, S. aureus ATCC 25923, E. coli BW25113, and A. baumannii ATCC 19606 with MIC values ranging from 0.062-1 µg mL. Additionally, FtsZ-IN-12 can inhibit biofilm formation and eliminate mature biofilms. It possesses bactericidal properties and shows no hemolytic toxicity to mammalian red blood cells at a dosage of 15 mg kg.

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.

Alpha-Hederin (Tauroside E) is a water-soluble pentacyclic triterpenoid saponin found in the seeds of Nigella sativa, with hemolytic and apoptotic properties.

Gramicidin A is a peptide antibiotic isolated from B. brevis.Gramicidin A is a highly hydrophobic channel-forming ion carrier that forms monovalent cation-permeable channels in artificial membranes.Gramicidin A induces the degradation of hypoxia-inducible factor 1 alpha (HIF-1 alpha) and reduces the growth of a mouse xenograft model of human renal cell carcinoma. Gramicidin A has antibacterial, antimalarial and hemolytic activities.

CAP 3 is a cholic acid-peptide conjugate (CAP) with antibacterial activity. It is active against the Gram-negative bacteria E. coli, K. pneumoniae, and A. baumanii (MIC99s = 8, 16, and 16 μM, respectively). CAP 3 increases the fluidity of model Gram-negative bacterial membranes and binds to LPS in vitro. It reduces the biomass and number of colony-forming units in E. coli biofilms in a concentration-dependent manner. CAP 3 inhibits E. coli biofilm formation on catheters implanted in mice infected with E. coli at the incision site when applied as a coating on the catheters. CAP 3 (40 mg/kg) also reduces bacterial load in E. coli-infected wounds in mice. It is cytotoxic to A459 cells (IC50 = 56.4 μM) and has hemolytic activity against human red blood cells with a 50% lysis (HC50) value of 48 μM.

Oroxylin A-7-O-glucuronide (Oroxylin A Glucoronide) and wogonoside should also be served as the chemical markers together with baicalin for the quality control of herbs and proprietary traditional Chinese medicine (PTCM) products of radix Scutellariae. Oroxylin A 7-O-glucuronide, Oroxin A, and Oroxin B can bind to the stem region of α-hemolysin (α-HL), when inhibiting the hemolytic activity of α-HL. Oroxylin A 7-O-glucuronide and 4', 5, 7-trihydroxy-6-methoxyflavone at a concentration of 100 microM inhibit 34 and 43% of total prolyl oligopeptidase (POP) activity, respectively.

Prosaikogenin H, an intestinal metabolite derived from saikosaponin, exhibits weak hemolytic activity.

FtsZ-IN-1 is a potent FtsZ inhibitor with a quinoline ring, exhibiting a strong inhibitory effect on Gram-positive bacteria (MIC: 0.5-8 μg mL). It enhances FtsZ polymerization and significantly promotes cell elongation in Bacillus subtilis. FtsZ-IN-1 has low hemolytic toxicity and demonstrates anti-drug-resistant bacterial effects due to its low tendency to induce drug resistance.

Omadacycline, also known as PTK 0796 and Amadacyclin, is a novel first-in-class aminomethylcycline with potent activity against important skin and pneumonia pathogens, including community-acquired methicillin-resistant Staphylococcus aureus (MRSA), β-hemolytic streptococci, penicillin-resistant Streptococcus pneumoniae, Haemophilus influenzae, and Legionella. Omadacycline is active against strains expressing the two main forms of tetracycline resistance (efflux and ribosomal protection). The primary effect of omadacycline is on bacterial protein synthesis, inhibiting protein synthesis with a potency greater than that of tetracycline. The binding site for omadacycline is similar to that for tetracycline.

C16-K-cBB1 is a potent, selective antimicrobial agent effective against Methicillin-resistant Staphylococcus aureus (MRSA), demonstrated by its minimal inhibitory concentration (MIC) of 1 µg mL. This compound exhibits excellent selectivity with minimal hemolytic activity, and can eradicate MRSA cells within 120 minutes when applied at a concentration of 12.5 μg mL.

Anti-MRSA agent 4 (compound 7a), a selective and potent inhibitor of Gram-positive Methicillin-resistant Staphylococcus aureus (MRSA) growth, demonstrates a minimum inhibitory concentration (MIC) of ≤ 0.26 µM and exhibits neither cytotoxic nor hemolytic activity in HEK293 cells [1].

YSK 05, a pH-sensitive cationic lipid, enhances the intracellular trafficking of non-viral vectors, significantly improves gene silencing and hemolytic activities in its modified form YSK 05-MEND, and effectively overcomes the suppression of endosomal escape caused by PEGylation, thereby enhancing siRNA delivery both in vitro and in vivo [1].