title: Anti-elastolytic activity of a honeybee (Apis cerana) chymotrypsin inhibitor.
abstract: The honeybee is an important insect species in global ecology, agriculture, and alternative medicine. While chymotrypsin and trypsin inhibitors from bees show activity against cathepsin G and plasmin, respectively, no anti-elastolytic role for these inhibitors has been elucidated. In this study, we identified an Asiatic honeybee (Apis cerana) chymotrypsin inhibitor (AcCI), which was shown to also act as an elastase inhibitor. AcCI was found to consist of a 65-amino acid mature peptide that displays ten cysteine residues. When expressed in baculovirus-infected insect cells, recombinant AcCI demonstrated inhibitory activity against chymotrypsin (K(i) 11.27 nM), but not trypsin, defining a role for AcCI as a honeybee-derived chymotrypsin inhibitor. Additionally, AcCI showed no detectable inhibitory effects on factor Xa, thrombin, plasmin, or tissue plasminogen activator; however, AcCI inhibited human neutrophil elastase (K(i) 61.05 nM), indicating that it acts as an anti-elastolytic factor. These findings constitute molecular evidence that AcCI acts as a chymotrypsin/elastase inhibitor.
authors.affiliation: College of Natural Resources and Life Science, Dong-A University, Busan 604-714, Republic of Korea.
authors.forename: Bo Yeon
authors.initials: BY
authors.lastname: Kim
authors.forename: Kwang Sik
authors.initials: KS
authors.lastname: Lee
authors.forename: Hu
authors.initials: H
authors.lastname: Wan
authors.forename: Feng Ming
authors.initials: FM
authors.lastname: Zou
authors.forename: Yong Soo
authors.initials: YS
authors.lastname: Choi
authors.forename: Hyung Joo
authors.initials: HJ
authors.lastname: Yoon
authors.forename: Hyung Wook
authors.initials: HW
authors.lastname: Kwon
authors.forename: Yeon Ho
authors.initials: YH
authors.lastname: Je
authors.forename: Byung Rae
authors.initials: BR
authors.lastname: Jin
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D001516:Bees / Q000235:genetics / Q000378:metabolism*; D002918:Chymotrypsin / Q000037:antagonists & inhibitors*; D019476:Insect Proteins / Q000235:genetics / Q000378:metabolism / Q000494:pharmacology*; D008969:Molecular Sequence Data; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors*; D015842:Serine Proteinase Inhibitors / Q000235:genetics / Q000378:metabolism / Q000494:pharmacology*
chemical_list: D019476:Insect Proteins; D015842:Serine Proteinase Inhibitors; D002918:Chymotrypsin; D010196:Pancreatic Elastase