β-defensin-3

Human β-defensin-3 (HβD-3) is an antibiotic antimicrobial peptide synthesized by epithelial cells. It exhibits potent antimicrobial properties, mitigates inflammatory cytokine responses, and targets various microorganisms with IC90 values ranging from 6 to 25 μg/ml.

β-Defensin-3 (human) trifluoroacetate salt (hBD-3) is a key antimicrobial peptide in the human innate immune system, exhibiting broad-spectrum bactericidal, immunomodulatory, and tissue-repairing activities. β-Defensin-3 (human) trifluoroacetate salt can be used in the treatment of skin diseases and cancer, as well as in research on drug-resistant bacterial infections.

β-Defensin-1 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth ofB. adolescentis,L. acidophilus,B. breve,B. vulgatus,L. fermentum,B. longum, andS. thermophilusin an antimicrobial radial diffusion assay.2β-Defensin-1 also inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius, and of susceptibleM. tuberculosisH37Rv but not of resistantM. tuberculosisRM22 when used at a concentration of 128 μg/ml.3,4It blocks human and mouse Kv1.3 voltage-gated potassium channels (IC50s = 11.8 and 13.2 μM, respectively).5Overexpression of β-defensin-1 in the human oral squamous cell carcinoma (OSCC) cell lines HSC-3, UM-1, and SCC-9 increases migration and invasion but not proliferation.6 1.Lehrer, R.I.Primate defensinsNat. Rev. Microbiol.2(9)727-738(2004) 2.Schroeder, B.O., Ehmann, D., Precht, J.C., et al.Paneth cell α-defensin 6 (HD-6) is an antimicrobial peptideMucosal Immunol.8(3)661-671(2015) 3.Ouhara, K., Komatsuzawa, H., Yamada, S., et al.Susceptibilities of periodontopathogenic and cariogenic bacteria to antibacterial peptides, β-defensins and LL37, produced by human epithelial cellsJ. Antimicrob. Chemother.55(6)888-896(2005) 4.Fattorini, L., Gennaro, R., Zanetti, M., et al.In vitro activity of protegrin-1 and beta-defensin-1, alone and in combination with isoniazid, against Mycobacterium tuberculosisPeptides25(7)1075-1077(2004) 5.Feng, J., Xie, Z., Yang, W., et al.Human beta-defensin 1, a new animal toxin-like blocker of potassium channelToxicon113(2016) 6.Han, Q., Wang, R., Sun, C., et al.Human beta-defensin-1 suppresses tumor migration and invasion and is an independent predictor for survival of oral squamous cell carcinoma patientsPLoS One9(3)e91867(2014)

β-Defensin-2 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius.2β-Defensin-2 (30 μg/ml) stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes.3It also stimulates calcium mobilization, migration, and proliferation of keratinocytes when used at concentrations of 30, 10, and 40 μg/ml, respectively. β-Defensin-2 induces IL-31 production by human peripheral blood-derived mast cellsin vitrowhen used at a concentration of 10 μg/ml and by rat mast cellsin vivofollowing a 500 ng intradermal dose.4Expression of β-defensin-2 is increased in psoriatic skin and chronic wounds.5,6 1.Lehrer, R.I.Primate defensinsNat. Rev. Microbiol.2(9)727-738(2004) 2.Ouhara, K., Komatsuzawa, H., Yamada, S., et al.Susceptibilities of periodontopathogenic and cariogenic bacteria to antibacterial peptides, β-defensins and LL37, produced by human epithelial cellsJ. Antimicrob. Chemother.55(6)888-896(2005) 3.Niyonsaba, F., Ushio, H., Nakano, N., et al.Antimicrobial peptides human β-defensins stimulate epidermal keratinocyte migration, proliferation and production of proinflammatory cytokines and chemokinesJ. Invest. Dermatol.127(3)594-604(2007) 4.Niyonsaba, F., Ushio, H., Hara, M., et al.Antimicrobial peptides human β-defensins and cathelicidin LL-37 induce the secretion of a pruritogenic cytokine IL-31 by human mast cellsJ. Immunol.184(7)3526-3534(2010) 5.Huh, W.-K., Oono, T., Shirafuji, Y., et al.Dynamic alteration of human β-defensin 2 localization from cytoplasm to intercellular space in psoriatic skinJ. Mol. Med. (Berl.)80(10)678-684(2002) 6.Butmarc, J., Yufit, T., Carson, P., et al.Human β-defensin-2 expression is increased in chronic woundsWound Repair Regen.12(4)439-443(2004)

CHRG01, a biologically active peptide, originates from the C-terminal amino acids 54 to 67 of human β-defensin 3 (hBD-3), with a modified structure wherein all cysteine (Cys) residues are replaced by serine (Ser) to eliminate disulfide bond linkages. Like its parent compound hBD-3, CHRG01 exhibits antimicrobial properties that are dependent on electrostatic interactions.

SAP15 (Synthetic anti-inflammatory peptide 15) is a synthetic peptide composed of 15 amino acids, derived from human beta-defensin 3, with the ability to penetrate cells and mitigate intracellular inflammation. It achieves its anti-inflammatory effects by blocking the phosphorylation of HDAC5, which in turn reduces NF-κB p65 phosphorylation. In macrophages stimulated with LPS, SAP15 suppresses the phosphorylation of both HDAC5 and NF-κB p65, demonstrating potent anti-inflammatory actions. Furthermore, treatment with SAP15 in LPS-induced chondrocytes elevates aggrecan and type II collagen levels while reducing osteocalcin expression. This peptide is valuable for exploring inflammation regulation and the development of anti-inflammatory therapies in biomaterials.

SAP15 (Synthetic anti-inflammatory peptide 15) acetate is a synthetic anti-inflammatory peptide composed of 15 amino acids, designed from human β-defensin 3. It can penetrate cells and downregulate intracellular inflammation by inhibiting the phosphorylation of HDAC5, thereby reducing the phosphorylation of NF-κBp65, which in turn suppresses inflammatory responses. Additionally, SAP15 acetate inhibits the phosphorylation of HDAC5 and NF-κBp65 in LPS-induced macrophages. Treatment with SAP15 acetate enhances the expression of aggrecan and type II collagen while reducing osteocalcin expression in LPS-induced chondrocytes. This compound is useful for research related to the modulation of inflammation and anti-inflammatory properties in biomaterials.