弹性蛋白酶抑制剂Fw 99468是小单孢菌F IM 99468发酵产生的次级代谢产物。在37℃,0.05M T ris-HC l(pH 7.6)缓冲液中,它对弹性蛋白酶具有抑制作用。在抑制剂浓度较小(0mM^0.013mM)的情况下,抑制剂与酶的结合呈直线关系,随着抑制剂浓度...弹性蛋白酶抑制剂Fw 99468是小单孢菌F IM 99468发酵产生的次级代谢产物。在37℃,0.05M T ris-HC l(pH 7.6)缓冲液中,它对弹性蛋白酶具有抑制作用。在抑制剂浓度较小(0mM^0.013mM)的情况下,抑制剂与酶的结合呈直线关系,随着抑制剂浓度的提高,抑制活力曲线则出现漂移。根据D ixon图和L inew eaver-Burk图的研究,该抑制剂对弹性蛋白酶呈竞争性抑制,抑制常数Ki=3.5×10-5M。展开更多
A large number of protease inhibitors have been found from leeches,which are essential in various physiological and biological processes.In the curret study,a novel elastase inhibitor was purified and characterized fr...A large number of protease inhibitors have been found from leeches,which are essential in various physiological and biological processes.In the curret study,a novel elastase inhibitor was purified and characterized from the leech of Hirudinaria manillensis,which was named HMEI-A.Primary structure analysis showed that HMEI-A belonged to a new family of proteins.HMEI-A exerted inhibitory effects on elastase and showed potent abilities to inhibit elastase with an inhibition constant(Ki)of 1.69×10^(−8) mol·L^(−1).Further study showed that HMEI-A inhibited the formation of neutrophil extracellular trap(NET).These results suggested that HMEIA from the leech of H.manillensis is a novel elastase inhibitor which can suppress NET formation.It may play a significant role in blood-sucking of leeches and is a potential candidate as an anti-inflammatory agent.展开更多
在筛选弹性蛋白酶抑制剂过程中,从福建省永泰青云山土壤中分离到放线菌F IM 99468,经分类鉴定为佛罗里达小单孢菌,定名为M icrom onospora f lorid ensis F IM 99468。经发酵、提取,产生的次级代谢产物Fw 99468能够抑制弹性蛋白酶,半数...在筛选弹性蛋白酶抑制剂过程中,从福建省永泰青云山土壤中分离到放线菌F IM 99468,经分类鉴定为佛罗里达小单孢菌,定名为M icrom onospora f lorid ensis F IM 99468。经发酵、提取,产生的次级代谢产物Fw 99468能够抑制弹性蛋白酶,半数抑制浓度IC50为3.4×1-0 6m ol/L。展开更多
基金supported from the National Science Foundation of China(Nos.31630075,21761142002,and 31801975)the Strategic Leading Project and Biological Resource Platform Project from Chinese Academy of Sciences(Nos.KFZDSW-219-2,ZSTH-034 and SAJC201606)+2 种基金the Natural Science Foundation of Yunnan Province(Nos.2019-YT-053 and 202001AT070116)the Social Development Foundation of Yunnan Province(Nos.2019ZF003 and 2018ZF001)Key Research and Development Plan from the Ministry of Science and Technology of China(No.2018YFA0801403).
文摘A large number of protease inhibitors have been found from leeches,which are essential in various physiological and biological processes.In the curret study,a novel elastase inhibitor was purified and characterized from the leech of Hirudinaria manillensis,which was named HMEI-A.Primary structure analysis showed that HMEI-A belonged to a new family of proteins.HMEI-A exerted inhibitory effects on elastase and showed potent abilities to inhibit elastase with an inhibition constant(Ki)of 1.69×10^(−8) mol·L^(−1).Further study showed that HMEI-A inhibited the formation of neutrophil extracellular trap(NET).These results suggested that HMEIA from the leech of H.manillensis is a novel elastase inhibitor which can suppress NET formation.It may play a significant role in blood-sucking of leeches and is a potential candidate as an anti-inflammatory agent.
文摘在筛选弹性蛋白酶抑制剂过程中,从福建省永泰青云山土壤中分离到放线菌F IM 99468,经分类鉴定为佛罗里达小单孢菌,定名为M icrom onospora f lorid ensis F IM 99468。经发酵、提取,产生的次级代谢产物Fw 99468能够抑制弹性蛋白酶,半数抑制浓度IC50为3.4×1-0 6m ol/L。
