The Safety and Anti-Hypercholesterolemic Effect of Coptisine in Syrian Golden Hamsters
Current work was conducted to evaluate the cholesterol-lowering effect of coptisine extracted from Rhizoma coptidis in Syrian golden hamsters. The safety results indicated that coptisine was a safe and low-toxic compound. Coptisine showed a beneficial effect in the abnormal serum lipid levels induce...
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creator | He, Kai Ye, Xiaoli Wu, Hao Wang, YanZhi Zou, Zongyao Ning, Na Hu, Yinran Chen, Biao Fang, Xuedong Li, Xuegang |
description | Current work was conducted to evaluate the cholesterol-lowering effect of coptisine extracted from
Rhizoma
coptidis
in Syrian golden hamsters. The safety results indicated that coptisine was a safe and low-toxic compound. Coptisine showed a beneficial effect in the abnormal serum lipid levels induced by a high-fat and high-cholesterol diet (HFHC): at a concentration of 70.05 mg/kg, coptisine significantly led to a decrease in total cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-c) levels by 26.70, 15.38, and 22.22 %, respectively, and high-density lipoprotein cholesterol (HDL-c) was increased by 41.74 % in serum of hamsters (
p
|
doi_str_mv | 10.1007/s11745-014-3983-7 |
format | Article |
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Rhizoma
coptidis
in Syrian golden hamsters. The safety results indicated that coptisine was a safe and low-toxic compound. Coptisine showed a beneficial effect in the abnormal serum lipid levels induced by a high-fat and high-cholesterol diet (HFHC): at a concentration of 70.05 mg/kg, coptisine significantly led to a decrease in total cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-c) levels by 26.70, 15.38, and 22.22 %, respectively, and high-density lipoprotein cholesterol (HDL-c) was increased by 41.74 % in serum of hamsters (
p
< 0.01). In addition, total bile acid (TBA) levels in feces of hamsters were elevated after coptisine administration. Further investigation has suggested that the mRNA and protein expression of 3-hydroxy-3-methyl-glutaryl-CoA reductase (HMGCR) in the liver of hamsters was down-regulated by high-dosage coptisine treatment (
p
< 0.05); mRNA and protein expression of low-density lipoprotein receptor (LDLR) and cholesterol 7α-hydroxylase (CYP7A1) were dramatically up-regulated by coptisine administration. The apical sodium-dependent bile salt transporter expression was down-regulated in the coptisine-treated animals, but showed no significant differences from the HFHC groups. Taken together, our results demonstrate that a high dosage of coptisine could inhibit cholesterol synthesis via suppressing the HMGCR expression and promoting the use and excretion of cholesterol via up-regulating LDLR and CYP7A1 expression. These findings suggest a critical role for coptisine in anti- hypercholesterolemia, and thus it needs to be considered as a potential natural cholesterol lowering agent.</description><identifier>ISSN: 0024-4201</identifier><identifier>EISSN: 1558-9307</identifier><identifier>DOI: 10.1007/s11745-014-3983-7</identifier><identifier>PMID: 25547428</identifier><language>eng</language><publisher>Berlin/Heidelberg: Springer Berlin Heidelberg</publisher><subject>Animals ; Anticholesteremic Agents - adverse effects ; Anticholesteremic Agents - therapeutic use ; Berberine - adverse effects ; Berberine - analogs & derivatives ; Berberine - therapeutic use ; Biomedical and Life Sciences ; Cholesterol ; Cholesterol - blood ; Coptisine ; Cricetinae ; CYP7A1 ; Diet, High-Fat - adverse effects ; Down-Regulation - drug effects ; Female ; HMGCR ; Hydroxymethylglutaryl CoA Reductases - genetics ; Hypercholesterolemia - blood ; Hypercholesterolemia - drug therapy ; Hypercholesterolemia - etiology ; Hypercholesterolemia - genetics ; LDLR ; Life Sciences ; Lipidology ; Lipids - blood ; Lipoproteins, HDL - blood ; Lipoproteins, LDL - blood ; Liver - drug effects ; Liver - metabolism ; Male ; Medical Biochemistry ; Medicinal Chemistry ; Mesocricetus ; Microbial Genetics and Genomics ; Neurochemistry ; Nutrition ; Original Article ; Rhizomacoptidis ; RNA, Messenger - genetics ; Triglycerides - blood</subject><ispartof>Lipids, 2015-02, Vol.50 (2), p.185-194</ispartof><rights>AOCS 2014</rights><rights>2015 American Oil Chemists' Society (AOCS)</rights><rights>AOCS 2015</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4905-ca94d0221a27ea78d01ecb2a716ead9a67be7f31dbed1f139521913aba62ca863</citedby><cites>FETCH-LOGICAL-c4905-ca94d0221a27ea78d01ecb2a716ead9a67be7f31dbed1f139521913aba62ca863</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s11745-014-3983-7$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s11745-014-3983-7$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>314,776,780,1411,27903,27904,41467,42536,45553,45554,51298</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/25547428$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>He, Kai</creatorcontrib><creatorcontrib>Ye, Xiaoli</creatorcontrib><creatorcontrib>Wu, Hao</creatorcontrib><creatorcontrib>Wang, YanZhi</creatorcontrib><creatorcontrib>Zou, Zongyao</creatorcontrib><creatorcontrib>Ning, Na</creatorcontrib><creatorcontrib>Hu, Yinran</creatorcontrib><creatorcontrib>Chen, Biao</creatorcontrib><creatorcontrib>Fang, Xuedong</creatorcontrib><creatorcontrib>Li, Xuegang</creatorcontrib><title>The Safety and Anti-Hypercholesterolemic Effect of Coptisine in Syrian Golden Hamsters</title><title>Lipids</title><addtitle>Lipids</addtitle><addtitle>Lipids</addtitle><description>Current work was conducted to evaluate the cholesterol-lowering effect of coptisine extracted from
Rhizoma
coptidis
in Syrian golden hamsters. The safety results indicated that coptisine was a safe and low-toxic compound. Coptisine showed a beneficial effect in the abnormal serum lipid levels induced by a high-fat and high-cholesterol diet (HFHC): at a concentration of 70.05 mg/kg, coptisine significantly led to a decrease in total cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-c) levels by 26.70, 15.38, and 22.22 %, respectively, and high-density lipoprotein cholesterol (HDL-c) was increased by 41.74 % in serum of hamsters (
p
< 0.01). In addition, total bile acid (TBA) levels in feces of hamsters were elevated after coptisine administration. Further investigation has suggested that the mRNA and protein expression of 3-hydroxy-3-methyl-glutaryl-CoA reductase (HMGCR) in the liver of hamsters was down-regulated by high-dosage coptisine treatment (
p
< 0.05); mRNA and protein expression of low-density lipoprotein receptor (LDLR) and cholesterol 7α-hydroxylase (CYP7A1) were dramatically up-regulated by coptisine administration. The apical sodium-dependent bile salt transporter expression was down-regulated in the coptisine-treated animals, but showed no significant differences from the HFHC groups. Taken together, our results demonstrate that a high dosage of coptisine could inhibit cholesterol synthesis via suppressing the HMGCR expression and promoting the use and excretion of cholesterol via up-regulating LDLR and CYP7A1 expression. These findings suggest a critical role for coptisine in anti- hypercholesterolemia, and thus it needs to be considered as a potential natural cholesterol lowering agent.</description><subject>Animals</subject><subject>Anticholesteremic Agents - adverse effects</subject><subject>Anticholesteremic Agents - therapeutic use</subject><subject>Berberine - adverse effects</subject><subject>Berberine - analogs & derivatives</subject><subject>Berberine - therapeutic use</subject><subject>Biomedical and Life Sciences</subject><subject>Cholesterol</subject><subject>Cholesterol - blood</subject><subject>Coptisine</subject><subject>Cricetinae</subject><subject>CYP7A1</subject><subject>Diet, High-Fat - adverse effects</subject><subject>Down-Regulation - drug effects</subject><subject>Female</subject><subject>HMGCR</subject><subject>Hydroxymethylglutaryl CoA Reductases - genetics</subject><subject>Hypercholesterolemia - blood</subject><subject>Hypercholesterolemia - drug therapy</subject><subject>Hypercholesterolemia - etiology</subject><subject>Hypercholesterolemia - genetics</subject><subject>LDLR</subject><subject>Life Sciences</subject><subject>Lipidology</subject><subject>Lipids - blood</subject><subject>Lipoproteins, HDL - blood</subject><subject>Lipoproteins, LDL - blood</subject><subject>Liver - drug effects</subject><subject>Liver - metabolism</subject><subject>Male</subject><subject>Medical Biochemistry</subject><subject>Medicinal Chemistry</subject><subject>Mesocricetus</subject><subject>Microbial Genetics and Genomics</subject><subject>Neurochemistry</subject><subject>Nutrition</subject><subject>Original Article</subject><subject>Rhizomacoptidis</subject><subject>RNA, Messenger - genetics</subject><subject>Triglycerides - blood</subject><issn>0024-4201</issn><issn>1558-9307</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2015</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>AZQEC</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><sourceid>GNUQQ</sourceid><recordid>eNqFkEtLxDAUhYMoOj5-gBsJuI7mpkmTLGV8jDCg4GMb0vZWKzPtmHSQ_nszVMWNuLoEzndy-Ag5Bn4GnOvzCKClYhwky6zJmN4iE1DKMJtxvU0mnAvJpOCwR_ZjfEtPkFbtkj2hlNRSmAl5fnxF-uBr7Afq24petH3DZsMKQ_naLTD2GNJZNiW9qmsse9rVdNqt-iY2LdKmpQ9DaHxLb7pFhS2d-eUGiYdkp_aLiEdf94A8XV89TmdsfndzO72Ys1Jarljpray4EOCFRq9NxQHLQngNOfrK-lwXqOsMqgIrqCGzSoCFzBc-F6U3eXZATsfeVeje12mue-vWoU1fOsilNsZYKVMKxlQZuhgD1m4VmqUPgwPuNibdaNIlk25j0unEnHw1r4slVj_Et7oU0GPgo1ng8H-jm9_eX3IwKpFiJGOC2hcMv0b_uecTpaKOmg</recordid><startdate>201502</startdate><enddate>201502</enddate><creator>He, Kai</creator><creator>Ye, Xiaoli</creator><creator>Wu, Hao</creator><creator>Wang, YanZhi</creator><creator>Zou, Zongyao</creator><creator>Ning, Na</creator><creator>Hu, Yinran</creator><creator>Chen, Biao</creator><creator>Fang, Xuedong</creator><creator>Li, Xuegang</creator><general>Springer Berlin Heidelberg</general><general>Springer Nature B.V</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>3V.</scope><scope>7QL</scope><scope>7QP</scope><scope>7QR</scope><scope>7T7</scope><scope>7TK</scope><scope>7U9</scope><scope>7X7</scope><scope>7XB</scope><scope>88A</scope><scope>88E</scope><scope>8AO</scope><scope>8C1</scope><scope>8FD</scope><scope>8FE</scope><scope>8FH</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AEUYN</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BBNVY</scope><scope>BENPR</scope><scope>BHPHI</scope><scope>BKSAR</scope><scope>C1K</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>FR3</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>H94</scope><scope>HCIFZ</scope><scope>K9.</scope><scope>LK8</scope><scope>M0S</scope><scope>M1P</scope><scope>M7N</scope><scope>M7P</scope><scope>P64</scope><scope>PCBAR</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope></search><sort><creationdate>201502</creationdate><title>The Safety and Anti-Hypercholesterolemic Effect of Coptisine in Syrian Golden Hamsters</title><author>He, Kai ; Ye, Xiaoli ; Wu, Hao ; Wang, YanZhi ; Zou, Zongyao ; Ning, Na ; Hu, Yinran ; Chen, Biao ; Fang, Xuedong ; Li, Xuegang</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4905-ca94d0221a27ea78d01ecb2a716ead9a67be7f31dbed1f139521913aba62ca863</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2015</creationdate><topic>Animals</topic><topic>Anticholesteremic Agents - adverse effects</topic><topic>Anticholesteremic Agents - therapeutic use</topic><topic>Berberine - adverse effects</topic><topic>Berberine - analogs & derivatives</topic><topic>Berberine - therapeutic use</topic><topic>Biomedical and Life Sciences</topic><topic>Cholesterol</topic><topic>Cholesterol - blood</topic><topic>Coptisine</topic><topic>Cricetinae</topic><topic>CYP7A1</topic><topic>Diet, High-Fat - adverse effects</topic><topic>Down-Regulation - drug effects</topic><topic>Female</topic><topic>HMGCR</topic><topic>Hydroxymethylglutaryl CoA Reductases - genetics</topic><topic>Hypercholesterolemia - blood</topic><topic>Hypercholesterolemia - drug therapy</topic><topic>Hypercholesterolemia - etiology</topic><topic>Hypercholesterolemia - genetics</topic><topic>LDLR</topic><topic>Life Sciences</topic><topic>Lipidology</topic><topic>Lipids - blood</topic><topic>Lipoproteins, HDL - blood</topic><topic>Lipoproteins, LDL - blood</topic><topic>Liver - drug effects</topic><topic>Liver - metabolism</topic><topic>Male</topic><topic>Medical Biochemistry</topic><topic>Medicinal Chemistry</topic><topic>Mesocricetus</topic><topic>Microbial Genetics and Genomics</topic><topic>Neurochemistry</topic><topic>Nutrition</topic><topic>Original Article</topic><topic>Rhizomacoptidis</topic><topic>RNA, Messenger - genetics</topic><topic>Triglycerides - blood</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>He, Kai</creatorcontrib><creatorcontrib>Ye, Xiaoli</creatorcontrib><creatorcontrib>Wu, Hao</creatorcontrib><creatorcontrib>Wang, YanZhi</creatorcontrib><creatorcontrib>Zou, Zongyao</creatorcontrib><creatorcontrib>Ning, Na</creatorcontrib><creatorcontrib>Hu, Yinran</creatorcontrib><creatorcontrib>Chen, Biao</creatorcontrib><creatorcontrib>Fang, Xuedong</creatorcontrib><creatorcontrib>Li, Xuegang</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>ProQuest Central (Corporate)</collection><collection>Bacteriology Abstracts (Microbiology B)</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Chemoreception Abstracts</collection><collection>Industrial and Applied Microbiology Abstracts (Microbiology A)</collection><collection>Neurosciences Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Biology Database (Alumni Edition)</collection><collection>Medical Database (Alumni Edition)</collection><collection>ProQuest Pharma Collection</collection><collection>Public Health Database</collection><collection>Technology Research Database</collection><collection>ProQuest SciTech Collection</collection><collection>ProQuest Natural Science Collection</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest One Sustainability</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central Essentials</collection><collection>Biological Science Collection</collection><collection>ProQuest Central</collection><collection>Natural Science Collection</collection><collection>Earth, Atmospheric & Aquatic Science Collection</collection><collection>Environmental Sciences and Pollution Management</collection><collection>ProQuest One Community College</collection><collection>ProQuest Central Korea</collection><collection>Engineering Research Database</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Central Student</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>SciTech Premium Collection</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>ProQuest Biological Science Collection</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Medical Database</collection><collection>Algology Mycology and Protozoology Abstracts (Microbiology C)</collection><collection>Biological Science Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>Earth, Atmospheric & Aquatic Science Database</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><jtitle>Lipids</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>He, Kai</au><au>Ye, Xiaoli</au><au>Wu, Hao</au><au>Wang, YanZhi</au><au>Zou, Zongyao</au><au>Ning, Na</au><au>Hu, Yinran</au><au>Chen, Biao</au><au>Fang, Xuedong</au><au>Li, Xuegang</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The Safety and Anti-Hypercholesterolemic Effect of Coptisine in Syrian Golden Hamsters</atitle><jtitle>Lipids</jtitle><stitle>Lipids</stitle><addtitle>Lipids</addtitle><date>2015-02</date><risdate>2015</risdate><volume>50</volume><issue>2</issue><spage>185</spage><epage>194</epage><pages>185-194</pages><issn>0024-4201</issn><eissn>1558-9307</eissn><abstract>Current work was conducted to evaluate the cholesterol-lowering effect of coptisine extracted from
Rhizoma
coptidis
in Syrian golden hamsters. The safety results indicated that coptisine was a safe and low-toxic compound. Coptisine showed a beneficial effect in the abnormal serum lipid levels induced by a high-fat and high-cholesterol diet (HFHC): at a concentration of 70.05 mg/kg, coptisine significantly led to a decrease in total cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-c) levels by 26.70, 15.38, and 22.22 %, respectively, and high-density lipoprotein cholesterol (HDL-c) was increased by 41.74 % in serum of hamsters (
p
< 0.01). In addition, total bile acid (TBA) levels in feces of hamsters were elevated after coptisine administration. Further investigation has suggested that the mRNA and protein expression of 3-hydroxy-3-methyl-glutaryl-CoA reductase (HMGCR) in the liver of hamsters was down-regulated by high-dosage coptisine treatment (
p
< 0.05); mRNA and protein expression of low-density lipoprotein receptor (LDLR) and cholesterol 7α-hydroxylase (CYP7A1) were dramatically up-regulated by coptisine administration. The apical sodium-dependent bile salt transporter expression was down-regulated in the coptisine-treated animals, but showed no significant differences from the HFHC groups. Taken together, our results demonstrate that a high dosage of coptisine could inhibit cholesterol synthesis via suppressing the HMGCR expression and promoting the use and excretion of cholesterol via up-regulating LDLR and CYP7A1 expression. These findings suggest a critical role for coptisine in anti- hypercholesterolemia, and thus it needs to be considered as a potential natural cholesterol lowering agent.</abstract><cop>Berlin/Heidelberg</cop><pub>Springer Berlin Heidelberg</pub><pmid>25547428</pmid><doi>10.1007/s11745-014-3983-7</doi><tpages>10</tpages></addata></record> |
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subjects | Animals Anticholesteremic Agents - adverse effects Anticholesteremic Agents - therapeutic use Berberine - adverse effects Berberine - analogs & derivatives Berberine - therapeutic use Biomedical and Life Sciences Cholesterol Cholesterol - blood Coptisine Cricetinae CYP7A1 Diet, High-Fat - adverse effects Down-Regulation - drug effects Female HMGCR Hydroxymethylglutaryl CoA Reductases - genetics Hypercholesterolemia - blood Hypercholesterolemia - drug therapy Hypercholesterolemia - etiology Hypercholesterolemia - genetics LDLR Life Sciences Lipidology Lipids - blood Lipoproteins, HDL - blood Lipoproteins, LDL - blood Liver - drug effects Liver - metabolism Male Medical Biochemistry Medicinal Chemistry Mesocricetus Microbial Genetics and Genomics Neurochemistry Nutrition Original Article Rhizomacoptidis RNA, Messenger - genetics Triglycerides - blood |
title | The Safety and Anti-Hypercholesterolemic Effect of Coptisine in Syrian Golden Hamsters |
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