hemolysis

beta-Amyrin acetate inhibits HMG-CoA Reductase (HMGCR) and sEH activity with IC50 of 3.4 μM. beta-Amyrin acetate has anti-inflammatory, antifungal, antioxidant, and anti-hyperlipidemic activities.

Polyporusterone B ((1R,2R,4S,5R,7R,11R,14S,15R)-14-[(2R,3R)-2,3-dihydroxy-6-methyl-5-methylideneheptan-2-yl]-4,5,11-trihydroxy-2,15-dimethyltetracyclo[8.7.0.02,?.011,1?]heptadec-9-en-8-one) is a triterpene carboxylic acid isolated from Polyporus umbellatus Fries known as pentahydroxy bile acids, alcohols, and derivatives. Polyporusterone B Polyporusterone B has an inhibitory effect on free radical-induced lysis of red blood cells (hemolysis).

Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis/erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.

Homovanillyl alcohol, a biological metabolite of Hydroxytyrosol, is a phenolic compound found in virgin olive oil (VOO) and wine. It exhibits high scavenging activities, protects red blood cells from hemolysis in a dose-dependent manner, and has a protective effect on cardiovascular disease and total mortality.

SMase-IN-1 (Compound 4) is a bacterial sphingomyelinase (SMase) inhibitor with an IC50 value of 6.43 µM against Bacillus cereus SMase. It also inhibits eqBuChE with an inhibition rate of 59.50% at a concentration of 50 µM. SMase-IN-1 forms a complex with Cu2+ through bio-metal interactions and can inhibit hemolysis of sheep red blood cells induced by Bacillus cereus.

Refinicopan is a complement factor D inhibitor with an IC50 of 10 nM, demonstrating an inhibition activity on rabbit erythrocyte hemolysis with an IC50 of 41 nM. It possesses excellent pharmacokinetic and pharmacodynamic properties.

Palmitoylcholine is an acyl choline.1It inhibits protein kinase C activity when used at a concentration of 100 μM.2Palmitoylcholine induces hemolysis in rat erythrocytes.3Plasma levels of palmitoylcholine are decreased in female patients with myalgic encephalomyelitis/chronic fatigue syndrome (ME/CFS).1 1.Germain, A., Barupal, D.K., Levine, S.M., et al.Comprehensive circulatory metabolomics in ME/CFS reveals disrupted metabolism of acyl lipids and steroidsMetabolites10(1)34(2020) 2.Nakadate, T., and Blumberg, P.M.Modulation by palmitoylcarnitine of protein kinase C activationCancer Res.47(24 Pt 1)6537-6542(1987) 3.Cho, K.S., and Proulx, P.Interactions of acyl carnitines and other lysins with erythrocytes and reconstituted erythrocyte lipoproteinsBiochim. Biophys. Acta318(1)50-60(1973)

Filipin II is a polyene and an active component of the polyene antibiotic filipin complex . [1] It has broad-spectrum antifungal activity, reducing growth of various fungi, including B. dermatitidis, C. neoformans, and H. capsulatum (MICs = 1-10 μg/ml). Filipin II inhibits ADP-stimulated respiration in rat liver mitochondria when used at a concentration of 3.5 mg/ml. [2] It also induces hemolysis of liposomes in a cholesterol-independent manner (IC50 = 0.5 μg/ml).[3]

Vamifeport (VIT-2763) is a novel orally active inhibitor that targets iron transport proteins and reduces markers of hemolysis in the SCD Townes model.VIT-2763 improves anemia and erythropoiesis, ameliorates vascular inflammation, and can be studied in β-thalassemia.

Pelecopan (BCX9930) is a potent, selective, orally active inhibitor of complement factor D (IC50=14.3 nM) that prevents both intravascular and extravascular hemolysis in PNH.

PX-316 is a AKT inhibior. PX-316, when administered intraperitoneally to mice at 150 mg/kg, inhibits Akt activation in HT-29 human tumor xenografts up to 78% at 10 h with recovery to 34% at 48 h. PX-316 has antitumor activity against early human MCF-7 breast cancer and HT-29 colon cancer xenografts in mice. PX-316 formulated in 20% hydroxypropyl-beta-cyclodextrin for intravenous administration is well tolerated in mice and rats with no hemolysis and no hematological toxicity. Thus, PX-316 is the lead compound of a new class of potential agents that inhibit Akt survival signaling.

Pyridoxatin is a fungal metabolite that inhibits production of thiobarbituric acid reactive substance (TBARS). Pyridoxatin inhibits hemolysis induced by the free radical generator AAPH and is active against C. albicans.

LL-37 GKE acetate, a peptide with 21 amino acids and the active structural domain of LL-37, inhibits lps-induced vascular nitric oxide production, is less toxic than LL-37 for hemolysis and apoptosis in human cultured smooth muscle cells, and possesses antimicrobial activity and therapeutic potential for sepsis.

Sutimlimab is a novel monoclonal antibody targeting complement protein C1. Sutimlimab is commonly used as a C1 inhibitor to treat cold agglutina-associated hemolysis.

Tesidolumab (LFG316) is a fully human IgG1/λ anti-C5 monoclonal antibody. Tesidolumab (LFG316) has an inhibitory effect on crovalimab and C5, blocking the cutting of C5 and preventing the subsequent formation of membrane attack complex, which can be used to study extravascular hemolysis.

Convicine, a pyrimidine glycoside found in faba beans [1] [2], serves as the precursor for the aglycones Divicine and Isouramil, alongside Vicine. It is a principal factor in favism, a genetic disorder that causes severe hemolysis following the consumption of faba beans.

Cathelicidin-2 (CATH-2) (128-153) is a synthetic antimicrobial peptide derived from amino acids 128-153 of chicken CATH-2, demonstrating activity against pathogens such as E. coli, S. aureus, S. enteritidis, and B. globigii in a dose-dependent manner. At a concentration of 40 µM, it induces hemolysis in chicken erythrocytes without exhibiting cytotoxicity towards human peripheral blood mononuclear cells (PBMCs). Additionally, it stimulates the production of the chemokine CCL2 and suppresses LPS-induced secretion of TNF-α, IL-6, IL-8, and IL-10 in human PBMCs.

Bovine Myeloid Antimicrobial Peptide (BMAP) 28, a synthetic peptide derived from bovine cathelicidin-5 (amino acids 132-158), exhibits antimicrobial activity against E. coli, S. aureus, MRSA, S. epidermidis, and the fungus C. albicans, with minimum inhibitory concentrations (MICs) of 2, 2, 4, 1, and 8 µM respectively. At a concentration of 200 nM, BMAP 28 permeabilizes the inner membrane of E. coli, and at 5 µM, it inhibits herpes simplex virus 1 (HSV-1) replication in Vero 76 cells. Furthermore, at 30 µM, it causes hemolysis in human erythrocytes and cytotoxicity in human neutrophils. In vivo, a dose of 0.8 mg/kg enhances survival in mice infected with E. coli or MRSA, but not P. aeruginosa.

SMAP 29, a bactericidal antimicrobial peptide and a cleavage product from the C-terminus of an ovine cathelicidin prepropeptide, is effective against P. aeruginosa strain PAO1 in both low- and high-salt conditions, as demonstrated in an energy-dependent luminescence assay with half-maximal effective concentrations (EC50s) of 0.05 and 0.06 µM, respectively. Additionally, it induces hemolysis in ovine red blood cells in a concentration-dependent manner.

RW2, an antimicrobial peptide, demonstrates activity against E. coli and S. aureus, with IC50 values of 730 µM and 210 µM, respectively. Additionally, it induces hemolysis in isolated ovine erythrocytes.

RW3, an antimicrobial peptide, exhibits activity against E. coli and S. aureus with IC50 values of 16 µM and 8 µM, respectively. Additionally, it induces hemolysis in isolated ovine erythrocytes.

RW4, an antimicrobial peptide, exhibits activity against E. coli and S. aureus, with IC50 values of 9.6 and 5.1 µM, respectively. Additionally, it induces hemolysis of isolated ovine erythrocytes.

L-K6L9, a cytolytic peptide comprised of L-isomer leucine and lysine, demonstrates cytotoxicity against both androgen-independent (LNCaP-CL1) and androgen-dependent (22Rv1 and LNCaP) human prostate cancer cells, with LC50 values of 4, 4, and 6 µM, respectively. It also affects non-cancerous cells, including NIH3T3 mouse fibroblasts and OL human foreskin fibroblasts, with LC50s of 7 and 5 µM, respectively. Furthermore, at a concentration of 100 µM, L-K6L9 induces hemolysis in isolated human erythrocytes.

Compound 174 (Compound 5g), an antibacterial agent, exhibits potent anti-infective properties in vivo along with appreciable pharmacokinetic profiles. This highly active substance demonstrates favorable biofilm removal capabilities, low hemolysis, and acceptable mammalian cell toxicity [1].