Inhibition of Acetylcholinesterase (AChE): A Potential Therapeutic Target to Treat Alzheimer's Disease
A new series of icariin derivatives were synthesized and evaluated for their in vitro acetylcholinesterase (AChE) inhibitory activity. Most of the tested compounds exhibited high AChE inhibition and low toxicity, and among which compounds 1, 2, and 10 were the most potent (IC50 = 71.52 ± 22.43, 8.28...
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| Veröffentlicht in: | Chemical biology & drug design 2015-10, Vol.86 (4), p.776-782 |
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| container_title | Chemical biology & drug design |
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| creator | Li, Yong Zhang, Xiao-xiao Jiang, Li-juan Yuan, Li Cao, Ting-ting Li, Xia Dong, Lin Li, Ying Yin, Shu-Fan |
| description | A new series of icariin derivatives were synthesized and evaluated for their in vitro acetylcholinesterase (AChE) inhibitory activity. Most of the tested compounds exhibited high AChE inhibition and low toxicity, and among which compounds 1, 2, and 10 were the most potent (IC50 = 71.52 ± 22.43, 8.28 ± 1.45, 5.830 ± 1.78 nm, respectively).
A new series of icariin derivatives were synthesized and evaluated for their in vitro acetylcholinesterase (AChE) inhibitory activity. Most of the tested compounds exhibited high AChE inhibition and low toxicity, and among which compounds 1, 2, and 10 were the most potent (IC50 = 71.52 ± 22.43, 8.28 ± 1.45, 5.830 ± 1.78 nm, respectively). |
| doi_str_mv | 10.1111/cbdd.12550 |
| format | Article |
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A new series of icariin derivatives were synthesized and evaluated for their in vitro acetylcholinesterase (AChE) inhibitory activity. Most of the tested compounds exhibited high AChE inhibition and low toxicity, and among which compounds 1, 2, and 10 were the most potent (IC50 = 71.52 ± 22.43, 8.28 ± 1.45, 5.830 ± 1.78 nm, respectively).</description><identifier>ISSN: 1747-0277</identifier><identifier>EISSN: 1747-0285</identifier><identifier>DOI: 10.1111/cbdd.12550</identifier><identifier>PMID: 25736722</identifier><language>eng</language><publisher>England: Blackwell Publishing Ltd</publisher><subject>Acetylcholinesterase - chemistry ; Acetylcholinesterase - metabolism ; AChE inhibition ; Alzheimer Disease - drug therapy ; Alzheimer Disease - enzymology ; Alzheimer's disease ; Cell Line ; Cholinesterase Inhibitors - chemistry ; Cholinesterase Inhibitors - pharmacology ; derivatives ; Drug Design ; Drugs, Chinese Herbal - chemistry ; Drugs, Chinese Herbal - pharmacology ; Epimedium - chemistry ; Flavonoids - chemistry ; Flavonoids - pharmacology ; Humans ; icariin ; Structure-Activity Relationship ; synthesis</subject><ispartof>Chemical biology & drug design, 2015-10, Vol.86 (4), p.776-782</ispartof><rights>2015 John Wiley & Sons A/S</rights><rights>2015 John Wiley & Sons A/S.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c3670-5126fb830ef7ea9e324b6dbbc6cfb81c7817d82031ee8decdd965e638e58cbfd3</citedby><cites>FETCH-LOGICAL-c3670-5126fb830ef7ea9e324b6dbbc6cfb81c7817d82031ee8decdd965e638e58cbfd3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1111%2Fcbdd.12550$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1111%2Fcbdd.12550$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,780,784,1416,27922,27923,45572,45573</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/25736722$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Li, Yong</creatorcontrib><creatorcontrib>Zhang, Xiao-xiao</creatorcontrib><creatorcontrib>Jiang, Li-juan</creatorcontrib><creatorcontrib>Yuan, Li</creatorcontrib><creatorcontrib>Cao, Ting-ting</creatorcontrib><creatorcontrib>Li, Xia</creatorcontrib><creatorcontrib>Dong, Lin</creatorcontrib><creatorcontrib>Li, Ying</creatorcontrib><creatorcontrib>Yin, Shu-Fan</creatorcontrib><title>Inhibition of Acetylcholinesterase (AChE): A Potential Therapeutic Target to Treat Alzheimer's Disease</title><title>Chemical biology & drug design</title><addtitle>Chem Biol Drug Des</addtitle><description>A new series of icariin derivatives were synthesized and evaluated for their in vitro acetylcholinesterase (AChE) inhibitory activity. Most of the tested compounds exhibited high AChE inhibition and low toxicity, and among which compounds 1, 2, and 10 were the most potent (IC50 = 71.52 ± 22.43, 8.28 ± 1.45, 5.830 ± 1.78 nm, respectively).
A new series of icariin derivatives were synthesized and evaluated for their in vitro acetylcholinesterase (AChE) inhibitory activity. Most of the tested compounds exhibited high AChE inhibition and low toxicity, and among which compounds 1, 2, and 10 were the most potent (IC50 = 71.52 ± 22.43, 8.28 ± 1.45, 5.830 ± 1.78 nm, respectively).</description><subject>Acetylcholinesterase - chemistry</subject><subject>Acetylcholinesterase - metabolism</subject><subject>AChE inhibition</subject><subject>Alzheimer Disease - drug therapy</subject><subject>Alzheimer Disease - enzymology</subject><subject>Alzheimer's disease</subject><subject>Cell Line</subject><subject>Cholinesterase Inhibitors - chemistry</subject><subject>Cholinesterase Inhibitors - pharmacology</subject><subject>derivatives</subject><subject>Drug Design</subject><subject>Drugs, Chinese Herbal - chemistry</subject><subject>Drugs, Chinese Herbal - pharmacology</subject><subject>Epimedium - chemistry</subject><subject>Flavonoids - chemistry</subject><subject>Flavonoids - pharmacology</subject><subject>Humans</subject><subject>icariin</subject><subject>Structure-Activity Relationship</subject><subject>synthesis</subject><issn>1747-0277</issn><issn>1747-0285</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2015</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kMlOwzAURS0EYt7wAcg7BilgO3Uc2IW2DKICioKQurES-4UY0qayXUH5elJCu8QbW--de2UdhA4oOaPNOVe51meUcU7W0DYVHREQFvP11VuILbTj3DshnQ5n8SbaYlyEkWBsGxV3k9Lkxpt6gusCJwr8vFJlXZkJOA82c4CPk27ZP7nECX6qPUy8ySqcls1uCjNvFE4z-wYe-xqnFjKPk-q7BDMGe-RwzzhoOvbQRpFVDvb_7l30ct1Pu7fB4PHmrpsMAtX8hwScsqjI45BAISC7gJB18kjnuYpUM6ZKxFTomJGQAsQalNYXEYcojIHHKi90uItO215la-csFHJqzTizc0mJXMiSC1nyV1YDH7bwdJaPQa_QpZ0GoC3waSqY_1Mlu1e93rI0aDOm0fe1ymT2Q0YiFFy-PtzI4fPg_rU3HMlR-APWw4Tp</recordid><startdate>201510</startdate><enddate>201510</enddate><creator>Li, Yong</creator><creator>Zhang, Xiao-xiao</creator><creator>Jiang, Li-juan</creator><creator>Yuan, Li</creator><creator>Cao, Ting-ting</creator><creator>Li, Xia</creator><creator>Dong, Lin</creator><creator>Li, Ying</creator><creator>Yin, Shu-Fan</creator><general>Blackwell Publishing Ltd</general><scope>BSCLL</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope></search><sort><creationdate>201510</creationdate><title>Inhibition of Acetylcholinesterase (AChE): A Potential Therapeutic Target to Treat Alzheimer's Disease</title><author>Li, Yong ; Zhang, Xiao-xiao ; Jiang, Li-juan ; Yuan, Li ; Cao, Ting-ting ; Li, Xia ; Dong, Lin ; Li, Ying ; Yin, Shu-Fan</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c3670-5126fb830ef7ea9e324b6dbbc6cfb81c7817d82031ee8decdd965e638e58cbfd3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2015</creationdate><topic>Acetylcholinesterase - chemistry</topic><topic>Acetylcholinesterase - metabolism</topic><topic>AChE inhibition</topic><topic>Alzheimer Disease - drug therapy</topic><topic>Alzheimer Disease - enzymology</topic><topic>Alzheimer's disease</topic><topic>Cell Line</topic><topic>Cholinesterase Inhibitors - chemistry</topic><topic>Cholinesterase Inhibitors - pharmacology</topic><topic>derivatives</topic><topic>Drug Design</topic><topic>Drugs, Chinese Herbal - chemistry</topic><topic>Drugs, Chinese Herbal - pharmacology</topic><topic>Epimedium - chemistry</topic><topic>Flavonoids - chemistry</topic><topic>Flavonoids - pharmacology</topic><topic>Humans</topic><topic>icariin</topic><topic>Structure-Activity Relationship</topic><topic>synthesis</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Li, Yong</creatorcontrib><creatorcontrib>Zhang, Xiao-xiao</creatorcontrib><creatorcontrib>Jiang, Li-juan</creatorcontrib><creatorcontrib>Yuan, Li</creatorcontrib><creatorcontrib>Cao, Ting-ting</creatorcontrib><creatorcontrib>Li, Xia</creatorcontrib><creatorcontrib>Dong, Lin</creatorcontrib><creatorcontrib>Li, Ying</creatorcontrib><creatorcontrib>Yin, Shu-Fan</creatorcontrib><collection>Istex</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><jtitle>Chemical biology & drug design</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Li, Yong</au><au>Zhang, Xiao-xiao</au><au>Jiang, Li-juan</au><au>Yuan, Li</au><au>Cao, Ting-ting</au><au>Li, Xia</au><au>Dong, Lin</au><au>Li, Ying</au><au>Yin, Shu-Fan</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Inhibition of Acetylcholinesterase (AChE): A Potential Therapeutic Target to Treat Alzheimer's Disease</atitle><jtitle>Chemical biology & drug design</jtitle><addtitle>Chem Biol Drug Des</addtitle><date>2015-10</date><risdate>2015</risdate><volume>86</volume><issue>4</issue><spage>776</spage><epage>782</epage><pages>776-782</pages><issn>1747-0277</issn><eissn>1747-0285</eissn><abstract>A new series of icariin derivatives were synthesized and evaluated for their in vitro acetylcholinesterase (AChE) inhibitory activity. Most of the tested compounds exhibited high AChE inhibition and low toxicity, and among which compounds 1, 2, and 10 were the most potent (IC50 = 71.52 ± 22.43, 8.28 ± 1.45, 5.830 ± 1.78 nm, respectively).
A new series of icariin derivatives were synthesized and evaluated for their in vitro acetylcholinesterase (AChE) inhibitory activity. Most of the tested compounds exhibited high AChE inhibition and low toxicity, and among which compounds 1, 2, and 10 were the most potent (IC50 = 71.52 ± 22.43, 8.28 ± 1.45, 5.830 ± 1.78 nm, respectively).</abstract><cop>England</cop><pub>Blackwell Publishing Ltd</pub><pmid>25736722</pmid><doi>10.1111/cbdd.12550</doi><tpages>7</tpages></addata></record> |
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| source | Wiley Online Library - AutoHoldings Journals; MEDLINE |
| subjects | Acetylcholinesterase - chemistry Acetylcholinesterase - metabolism AChE inhibition Alzheimer Disease - drug therapy Alzheimer Disease - enzymology Alzheimer's disease Cell Line Cholinesterase Inhibitors - chemistry Cholinesterase Inhibitors - pharmacology derivatives Drug Design Drugs, Chinese Herbal - chemistry Drugs, Chinese Herbal - pharmacology Epimedium - chemistry Flavonoids - chemistry Flavonoids - pharmacology Humans icariin Structure-Activity Relationship synthesis |
| title | Inhibition of Acetylcholinesterase (AChE): A Potential Therapeutic Target to Treat Alzheimer's Disease |
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