Identification and pharmaceutical evaluation of novel frog skin-derived serine proteinase inhibitor peptide -- PE-BBI (Pelophylax esculentus Bowman-Birk inhibitor) for the potential treatment of cancer

UM > Faculty of Health Sciences > DEPARTMENT OF BIOMEDICAL SCIENCES

Residential College	false
Status	已發表Published
	Identification and pharmaceutical evaluation of novel frog skin-derived serine proteinase inhibitor peptide -- PE-BBI (Pelophylax esculentus Bowman-Birk inhibitor) for the potential treatment of cancer
	Lyu, P.; Ge, L.; Ma, R.; Wei, R.; McCrudden, C. M.; Chen, T.; Shaw, C.; Kwok, H. F.
	2018-09-01
Source Publication	Scientific Reports
ISSN	2045-2322
Pages	14502---
Abstract	Amphibian venom-derived peptides have high potential in the field of anticancer drug discovery. We have isolated a novel Bowman-Birk proteinase inhibitor (BBI)-type peptide from the skin secretion of Pelophylax esculentus (PE) named PE-BBI, and evaluated its bio-functions and anti-cancer activity in vitro. PE-BBI is a heptadecapeptide with C-terminal amidation. The mRNA sequence and primary structure of PE-BBI were identified using RT-PCR and LC/MS, respectively. A trypsin inhibitory assay was used to characterize the serine proteinase inhibitory activity of synthetic PE-BBI. PE-BBI’s myotropic activity was analyzed using isolated rat bladder and rat-tail artery smooth muscle tissues, and the anti-cancer ability of PE-BBI using human colorectal cancer cells. PE-BBI’s mechanism of action was investigated using Discovery studio software. PE-BBI showed trypsin inhibitory activity (K¬i=310±72 nM), strong myotropic activity, and cytotoxicity that were specific to cancer cells, and no side effect to normal epithelial cells. The docking stimulation showed that PE-BBI had high affinity to several members of human kallikrein related peptidase (KLK) family. This finding helps to enrich our understanding of BBI peptides’ mode of action. Moreover, the data presented here validates frog secretions as sources of potential novel proteinase inhibitors for cancer treatment.
Keyword	Amphibian skin peptide Pelophylax esculentus Bowman-Birk-like trypsin inhibitor Anticancer peptide Drug discovery
URL	View the original
Language	英語English
The Source to Article	PB_Publication
PUB ID	41999
Document Type	Journal article
Collection	DEPARTMENT OF BIOMEDICAL SCIENCES
Corresponding Author	Kwok, H. F.
Recommended Citation GB/T 7714	Lyu, P.,Ge, L.,Ma, R.,et al. Identification and pharmaceutical evaluation of novel frog skin-derived serine proteinase inhibitor peptide -- PE-BBI (Pelophylax esculentus Bowman-Birk inhibitor) for the potential treatment of cancer[J]. Scientific Reports, 2018, 14502---.
APA	Lyu, P.., Ge, L.., Ma, R.., Wei, R.., McCrudden, C. M.., Chen, T.., Shaw, C.., & Kwok, H. F. (2018). Identification and pharmaceutical evaluation of novel frog skin-derived serine proteinase inhibitor peptide -- PE-BBI (Pelophylax esculentus Bowman-Birk inhibitor) for the potential treatment of cancer. Scientific Reports, 14502---.
MLA	Lyu, P.,et al."Identification and pharmaceutical evaluation of novel frog skin-derived serine proteinase inhibitor peptide -- PE-BBI (Pelophylax esculentus Bowman-Birk inhibitor) for the potential treatment of cancer".Scientific Reports (2018):14502---.

Files in This Item:
There are no files associated with this item.

If you have any objections to this item, please fill out the form below and the administrator will contact you as soon as possible.
Content:
Email：	*
Affiliation No.
Verification Code:	Refresh

Any comments and suggestions are welcomed.
Title:	*
Content:
Email：	*
Verification Code:	Refresh