Peptide name : Dermaseptin-PS1

Source/Organism : Rock Kribensis Cichlid

Linear/Cyclic : Linear

Chirality : Not found

Peptide length: 31

C-terminal modification: Linear

N-terminal modification : Not found

Non-natural peptide information: None

Assay type : Lactate dehydrogenase (LDH) assay, MTT cell proliferation assay

Assay time : 24h

Activity : MIC : 10−5 M and above

Cell line : U251MG

Cancer type : Human glioblastoma

Other activity : Anti-bacterial activity; Anti-microbial activity

Amino acid composition bar chart :

Molecular mass : 3164.7621 Dalton

Aliphatic index : 1.167

Instability index : 2.2484

Hydrophobicity (GRAVY) : 0.5032

Isoelectric point : 10.001

Charge (pH 7) : 2.8802

Aromaticity : 0.032

Molar extinction coefficient (cysteine, cystine): (5500, 5500)

Hydrophobic/hydrophilic ratio : 1.81818181

hydrophobic moment : -0.669

Missing amino acid : C,R,P,E,F,Y,N

Most occurring amino acid : A

Most occurring amino acid frequency : 7

Least occurring amino acid : W

Least occurring amino acid frequency : 1

Secondary structure fraction (Helix, Turn, Sheet): (0.5, 0.1, 0.3)

SMILES Notation: CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)N)[C@@H](C)O)[C@@H](C)O)C(C)C)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)O

1 : Long Q, et al. Novel peptide dermaseptin-PS1 exhibits anticancer activity via induction of intrinsic apoptosis signalling. J Cell Mol Med. 2019; 23:1300-1312. doi: 10.1111/jcmm.14032

Paper title : Novel peptide dermaseptin-PS1 exhibits anticancer activity via induction of intrinsic apoptosis signalling.

Doi : https://doi.org/10.1111/jcmm.14032

Abstract : Antimicrobial peptides (AMP) secreted by the granular glands of frog skin have been widely reported to exhibit strong bacteriostatic and bactericidal activities. Many of them have been documented with potent antiproliferative effects on multiple cancer cells, many studies also suggested that AMPs exert their functions via disrupting cell membranes. However, whether and how other cell death induction mechanism is involved in mammalian cancer cells has rarely been investigated. In this study, a novel AMP named Dermaseptin-PS1 was isolated and identified from Phyllomedusa sauvagei, it showed strong antimicrobial activities against three types of microorganisms. In vitro antiproliferative studies on human glioblastoma U-251 MG cells indicated that Dermaseptin-PS1 disrupted cell membranes at the concentrations of 10-5  M and above, while the cell membrane integrity was not affected when concentrations were decreased to 10-6  M or lower. Further examinations revealed that, at the relatively low concentration (10-6  M), Dermaseptin-PS1 induced apoptosis through mitochondrial-related signal pathway in U-251 MG cells. Thus, for the first time, we report a novel frog skin derived AMP with anticancer property by distinct mechanisms, which largely depends on its concentration. Together, our study provides new insights into the mechanism-illustrated drug design and the optimisation of dose control for cancer treatment in clinic.