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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, Peng; Ge, Lilin; Ma, Rui; Wei, Ran; McCrudden, Cian M.; Chen, Tianbao; Shaw, Chris; Kwok, Hang Fai
2018-09-28
Source PublicationSCIENTIFIC REPORTS
ISSN2045-2322
Volume8
AbstractAmphibian 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.
DOI10.1038/s41598-018-32947-5
URLView the original
Indexed BySCI
Language英语
WOS Research AreaScience & Technology - Other Topics
WOS SubjectMultidisciplinary Sciences
WOS IDWOS:000445894500005
PublisherNATURE PUBLISHING GROUP
The Source to ArticleWOS
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Cited Times [WOS]:3   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Recommended Citation
GB/T 7714
Lyu, Peng,Ge, Lilin,Ma, Rui,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,2018,8.
APA Lyu, Peng.,Ge, Lilin.,Ma, Rui.,Wei, Ran.,McCrudden, Cian M..,...&Kwok, Hang Fai.(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,8.
MLA Lyu, Peng,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 8(2018).
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