The analgesic activity of Bestatin as a potent APN inhibitor
Bestatin, a small molecular weight dipeptide, is a potent inhibitor of various aminopeptidases as well as LTA4 hydrolase. Various physiological functions of Bestatin have been identified, viz.: (1) an immunomodifier for enhancing the proliferation of normal human bone marrow granulocyte–ma...
Main Authors: | , , |
---|---|
Format: | Article |
Language: | English |
Published: |
Frontiers Media S.A.
2010-06-01
|
Series: | Frontiers in Neuroscience |
Subjects: | |
Online Access: | http://journal.frontiersin.org/Journal/10.3389/fnins.2010.00050/full |
id |
doaj-aa92a7a7a90a4d7f8c6e45c9209e7070 |
---|---|
record_format |
Article |
spelling |
doaj-aa92a7a7a90a4d7f8c6e45c9209e70702020-11-25T00:12:21ZengFrontiers Media S.A.Frontiers in Neuroscience1662-453X2010-06-01410.3389/fnins.2010.000501750The analgesic activity of Bestatin as a potent APN inhibitorMei-Rong Jia0Tao Wei1Wen-Fang Xu2Shandong UniversityShandong UniversityShandong UniversityBestatin, a small molecular weight dipeptide, is a potent inhibitor of various aminopeptidases as well as LTA4 hydrolase. Various physiological functions of Bestatin have been identified, viz.: (1) an immunomodifier for enhancing the proliferation of normal human bone marrow granulocyte–macrophage progenitor cells to form CFU-GM colonies; Bestatin exerts a direct stimulating effect on lymphocytes via its fixation on the cell surface and an indirect effect on monocytes via aminopeptidase B inhibition of tuftsin catabolism; (2) an immunorestorator and curative or preventive agent for spontaneous tumor; Bestatin alone or its combination with chemicals can prolongate the disease-free interval and survival period in adult acute or chronic leukemia, therefore, it was primarily marketed in 1987 in Japan as an anticancer drug and servers as the only marketed inhibitor of Aminopeptidase N (APN/CD13) to cure leukemia to date; (3) a pan-hematopoietic stimulator and restorator; Bestatin promotes granulocytopoiesis and thrombocytopoiesis in vitro and restores them in myelo-hypoplastic men; (4) an inhibitor of several natural opioid peptides. Based on the knowledge that APN can cleave several bioactive neuropeptides such as Met-enkaphalins, Leu-enkaphalins, β-Endorphin, and so on, the antiaminopeptidase action of Bestatin also allows it to protect endopeptides against their catabolism, exhibiting analgesic activity. Although many scientific studies and great accomplishments have been achieved in this field, a large amount of problems are unsolved. This article reviews the promising results obtained for future development of the analgesic activity of Bestatin that can be of vital interest in a number of severe and chronic pain syndromes.http://journal.frontiersin.org/Journal/10.3389/fnins.2010.00050/fullNeuropeptidesMechanismanalgesic activityapplicationBestatin |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Mei-Rong Jia Tao Wei Wen-Fang Xu |
spellingShingle |
Mei-Rong Jia Tao Wei Wen-Fang Xu The analgesic activity of Bestatin as a potent APN inhibitor Frontiers in Neuroscience Neuropeptides Mechanism analgesic activity application Bestatin |
author_facet |
Mei-Rong Jia Tao Wei Wen-Fang Xu |
author_sort |
Mei-Rong Jia |
title |
The analgesic activity of Bestatin as a potent APN inhibitor |
title_short |
The analgesic activity of Bestatin as a potent APN inhibitor |
title_full |
The analgesic activity of Bestatin as a potent APN inhibitor |
title_fullStr |
The analgesic activity of Bestatin as a potent APN inhibitor |
title_full_unstemmed |
The analgesic activity of Bestatin as a potent APN inhibitor |
title_sort |
analgesic activity of bestatin as a potent apn inhibitor |
publisher |
Frontiers Media S.A. |
series |
Frontiers in Neuroscience |
issn |
1662-453X |
publishDate |
2010-06-01 |
description |
Bestatin, a small molecular weight dipeptide, is a potent inhibitor of various aminopeptidases as well as LTA4 hydrolase. Various physiological functions of Bestatin have been identified, viz.: (1) an immunomodifier for enhancing the proliferation of normal human bone marrow granulocyte–macrophage progenitor cells to form CFU-GM colonies; Bestatin exerts a direct stimulating effect on lymphocytes via its fixation on the cell surface and an indirect effect on monocytes via aminopeptidase B inhibition of tuftsin catabolism; (2) an immunorestorator and curative or preventive agent for spontaneous tumor; Bestatin alone or its combination with chemicals can prolongate the disease-free interval and survival period in adult acute or chronic leukemia, therefore, it was primarily marketed in 1987 in Japan as an anticancer drug and servers as the only marketed inhibitor of Aminopeptidase N (APN/CD13) to cure leukemia to date; (3) a pan-hematopoietic stimulator and restorator; Bestatin promotes granulocytopoiesis and thrombocytopoiesis in vitro and restores them in myelo-hypoplastic men; (4) an inhibitor of several natural opioid peptides. Based on the knowledge that APN can cleave several bioactive neuropeptides such as Met-enkaphalins, Leu-enkaphalins, β-Endorphin, and so on, the antiaminopeptidase action of Bestatin also allows it to protect endopeptides against their catabolism, exhibiting analgesic activity. Although many scientific studies and great accomplishments have been achieved in this field, a large amount of problems are unsolved. This article reviews the promising results obtained for future development of the analgesic activity of Bestatin that can be of vital interest in a number of severe and chronic pain syndromes. |
topic |
Neuropeptides Mechanism analgesic activity application Bestatin |
url |
http://journal.frontiersin.org/Journal/10.3389/fnins.2010.00050/full |
work_keys_str_mv |
AT meirongjia theanalgesicactivityofbestatinasapotentapninhibitor AT taowei theanalgesicactivityofbestatinasapotentapninhibitor AT wenfangxu theanalgesicactivityofbestatinasapotentapninhibitor AT meirongjia analgesicactivityofbestatinasapotentapninhibitor AT taowei analgesicactivityofbestatinasapotentapninhibitor AT wenfangxu analgesicactivityofbestatinasapotentapninhibitor |
_version_ |
1725399608492818432 |