In vitro anti-diabetic effect of flavonoids and pheophytins from Allophylus cominia Sw. on the glucose uptake assays by HepG2, L6, 3T3-L1 and fat accumulation in 3T3-L1 adipocytes
Based on ethno-botanical information collected from diabetic patients in Cuba and firstly reported inhibition of PTP1B and DPPIV enzymes activities, Allophylus cominia (A. cominia) was identified as possible source of new drugs that could be used for the treatment of type 2 diabetes mellitus (T2-DM)...
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| Veröffentlicht in: | Journal of ethnopharmacology 2018-04, Vol.216, p.8-17 |
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| creator | Semaan, D.G. Igoli, J.O. Young, L. Gray, A.I. Rowan, E.G. Marrero, E. |
| description | Based on ethno-botanical information collected from diabetic patients in Cuba and firstly reported inhibition of PTP1B and DPPIV enzymes activities, Allophylus cominia (A. cominia) was identified as possible source of new drugs that could be used for the treatment of type 2 diabetes mellitus (T2-DM).
in this study, the activity of the characterised extracts from A. cominia was tested on the glucose uptake using HepG2 and L6 cells, 3T3-L1 fibroblasts and adipocytes as well as their effect on the fat accumulation using 3T3-L1 adipocytes.
on 2-NBDG glucose uptake assay using HepG2 and L6 cells, extracts from A. cominia enhanced insulin activity by increasing glucose uptake. On HepG2 cells Insulin EC50 of 93 ± 21nM decreased to 13 ± 2nM in the presence of the flavonoids mixture from A.cominia. In L6 cells, insulin also produced a concentration-dependent increase with an EC50 of 28.6 ± 0.7nM; EC50 decreased to 0.08 ± 0.02nM and 5 ± 0.9nM in the presence of 100μg/ml of flavonoids and pheophytins mixtures, respectively. In 3T3-L1 fibroblasts, insulin had an EC50 of >1000nM that decreased to 38 ± 4nM in the presence of the flavonoids extract. However, in adipocytes, insulin produced a significant concentration-dependent increase and an EC50 of 30 ± 8nM was a further confirmation of the insulin responsiveness of the adipocytes to the insulin. At 100µg/ml, flavonoids and pheophytins extracts decreased fat accumulation in 3T3-L1 adipocytes by two folds in comparison to the control differentiated cells (p < 0.05). The crude extract of A. cominia did not show any enhancement of 2-NBDG uptake by 3T3-L1 adipocytes in the presence or absence of 100nM insulin. In addition, in fully differentiated adipocytes, both extracts produced significant decrease in lipid droplets in the cells and no lipid accumulation were seen after withdrawal of the extracts from the cell growth medium. However, there was no effect of both extracts on total protein concentration in cells as well as on Glut-4 transporters.
the pharmacological effects of the extracts from A. cominia observed in experimental diabetic models were shown in this study. A. cominia is potentially a new candidate for the treatment and management of T2-DM.
[Display omitted] |
| doi_str_mv | 10.1016/j.jep.2018.01.014 |
| format | Article |
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in this study, the activity of the characterised extracts from A. cominia was tested on the glucose uptake using HepG2 and L6 cells, 3T3-L1 fibroblasts and adipocytes as well as their effect on the fat accumulation using 3T3-L1 adipocytes.
on 2-NBDG glucose uptake assay using HepG2 and L6 cells, extracts from A. cominia enhanced insulin activity by increasing glucose uptake. On HepG2 cells Insulin EC50 of 93 ± 21nM decreased to 13 ± 2nM in the presence of the flavonoids mixture from A.cominia. In L6 cells, insulin also produced a concentration-dependent increase with an EC50 of 28.6 ± 0.7nM; EC50 decreased to 0.08 ± 0.02nM and 5 ± 0.9nM in the presence of 100μg/ml of flavonoids and pheophytins mixtures, respectively. In 3T3-L1 fibroblasts, insulin had an EC50 of >1000nM that decreased to 38 ± 4nM in the presence of the flavonoids extract. However, in adipocytes, insulin produced a significant concentration-dependent increase and an EC50 of 30 ± 8nM was a further confirmation of the insulin responsiveness of the adipocytes to the insulin. At 100µg/ml, flavonoids and pheophytins extracts decreased fat accumulation in 3T3-L1 adipocytes by two folds in comparison to the control differentiated cells (p < 0.05). The crude extract of A. cominia did not show any enhancement of 2-NBDG uptake by 3T3-L1 adipocytes in the presence or absence of 100nM insulin. In addition, in fully differentiated adipocytes, both extracts produced significant decrease in lipid droplets in the cells and no lipid accumulation were seen after withdrawal of the extracts from the cell growth medium. However, there was no effect of both extracts on total protein concentration in cells as well as on Glut-4 transporters.
the pharmacological effects of the extracts from A. cominia observed in experimental diabetic models were shown in this study. A. cominia is potentially a new candidate for the treatment and management of T2-DM.
[Display omitted]</description><identifier>ISSN: 0378-8741</identifier><identifier>EISSN: 1872-7573</identifier><identifier>DOI: 10.1016/j.jep.2018.01.014</identifier><identifier>PMID: 29339110</identifier><language>eng</language><publisher>Ireland: Elsevier B.V</publisher><subject><![CDATA[3T3-L1 Cells ; 3T3-L1 differentiation ; 4-Chloro-7-nitrobenzofurazan - analogs & derivatives ; 4-Chloro-7-nitrobenzofurazan - metabolism ; Adipocytes - drug effects ; Adipocytes - metabolism ; Adipogenesis - drug effects ; Allophylus cominia ; Animals ; Deoxyglucose - analogs & derivatives ; Deoxyglucose - metabolism ; Dose-Response Relationship, Drug ; Flavonoids - isolation & purification ; Flavonoids - pharmacology ; Glucose Transporter Type 4 - metabolism ; Glucose uptake ; Hep G2 Cells ; Hepatocytes - drug effects ; Hepatocytes - metabolism ; HepG2 cells ; Humans ; Hypoglycemic Agents - isolation & purification ; Hypoglycemic Agents - pharmacology ; Insulin - pharmacology ; L6 cells ; Lipid Droplets - drug effects ; Lipid Droplets - metabolism ; Mice ; Muscle, Skeletal - drug effects ; Muscle, Skeletal - metabolism ; Pheophytins - isolation & purification ; Pheophytins - pharmacology ; Phytotherapy ; Plant Extracts - isolation & purification ; Plant Extracts - pharmacology ; Plants, Medicinal ; Rats ; Sapindaceae - chemistry ; Time Factors]]></subject><ispartof>Journal of ethnopharmacology, 2018-04, Vol.216, p.8-17</ispartof><rights>2018 Elsevier B.V.</rights><rights>Copyright © 2018 Elsevier B.V. All rights reserved.</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c396t-a7a769dbfb8a9cebd6f9964e4f20057f9ef6055900fc088201fbd9ae92fe960c3</citedby><cites>FETCH-LOGICAL-c396t-a7a769dbfb8a9cebd6f9964e4f20057f9ef6055900fc088201fbd9ae92fe960c3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0378874117333317$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/29339110$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Semaan, D.G.</creatorcontrib><creatorcontrib>Igoli, J.O.</creatorcontrib><creatorcontrib>Young, L.</creatorcontrib><creatorcontrib>Gray, A.I.</creatorcontrib><creatorcontrib>Rowan, E.G.</creatorcontrib><creatorcontrib>Marrero, E.</creatorcontrib><title>In vitro anti-diabetic effect of flavonoids and pheophytins from Allophylus cominia Sw. on the glucose uptake assays by HepG2, L6, 3T3-L1 and fat accumulation in 3T3-L1 adipocytes</title><title>Journal of ethnopharmacology</title><addtitle>J Ethnopharmacol</addtitle><description>Based on ethno-botanical information collected from diabetic patients in Cuba and firstly reported inhibition of PTP1B and DPPIV enzymes activities, Allophylus cominia (A. cominia) was identified as possible source of new drugs that could be used for the treatment of type 2 diabetes mellitus (T2-DM).
in this study, the activity of the characterised extracts from A. cominia was tested on the glucose uptake using HepG2 and L6 cells, 3T3-L1 fibroblasts and adipocytes as well as their effect on the fat accumulation using 3T3-L1 adipocytes.
on 2-NBDG glucose uptake assay using HepG2 and L6 cells, extracts from A. cominia enhanced insulin activity by increasing glucose uptake. On HepG2 cells Insulin EC50 of 93 ± 21nM decreased to 13 ± 2nM in the presence of the flavonoids mixture from A.cominia. In L6 cells, insulin also produced a concentration-dependent increase with an EC50 of 28.6 ± 0.7nM; EC50 decreased to 0.08 ± 0.02nM and 5 ± 0.9nM in the presence of 100μg/ml of flavonoids and pheophytins mixtures, respectively. In 3T3-L1 fibroblasts, insulin had an EC50 of >1000nM that decreased to 38 ± 4nM in the presence of the flavonoids extract. However, in adipocytes, insulin produced a significant concentration-dependent increase and an EC50 of 30 ± 8nM was a further confirmation of the insulin responsiveness of the adipocytes to the insulin. At 100µg/ml, flavonoids and pheophytins extracts decreased fat accumulation in 3T3-L1 adipocytes by two folds in comparison to the control differentiated cells (p < 0.05). The crude extract of A. cominia did not show any enhancement of 2-NBDG uptake by 3T3-L1 adipocytes in the presence or absence of 100nM insulin. In addition, in fully differentiated adipocytes, both extracts produced significant decrease in lipid droplets in the cells and no lipid accumulation were seen after withdrawal of the extracts from the cell growth medium. However, there was no effect of both extracts on total protein concentration in cells as well as on Glut-4 transporters.
the pharmacological effects of the extracts from A. cominia observed in experimental diabetic models were shown in this study. A. cominia is potentially a new candidate for the treatment and management of T2-DM.
[Display omitted]</description><subject>3T3-L1 Cells</subject><subject>3T3-L1 differentiation</subject><subject>4-Chloro-7-nitrobenzofurazan - analogs & derivatives</subject><subject>4-Chloro-7-nitrobenzofurazan - metabolism</subject><subject>Adipocytes - drug effects</subject><subject>Adipocytes - metabolism</subject><subject>Adipogenesis - drug effects</subject><subject>Allophylus cominia</subject><subject>Animals</subject><subject>Deoxyglucose - analogs & derivatives</subject><subject>Deoxyglucose - metabolism</subject><subject>Dose-Response Relationship, Drug</subject><subject>Flavonoids - isolation & purification</subject><subject>Flavonoids - pharmacology</subject><subject>Glucose Transporter Type 4 - metabolism</subject><subject>Glucose uptake</subject><subject>Hep G2 Cells</subject><subject>Hepatocytes - drug effects</subject><subject>Hepatocytes - metabolism</subject><subject>HepG2 cells</subject><subject>Humans</subject><subject>Hypoglycemic Agents - isolation & purification</subject><subject>Hypoglycemic Agents - pharmacology</subject><subject>Insulin - pharmacology</subject><subject>L6 cells</subject><subject>Lipid Droplets - drug effects</subject><subject>Lipid Droplets - metabolism</subject><subject>Mice</subject><subject>Muscle, Skeletal - drug effects</subject><subject>Muscle, Skeletal - metabolism</subject><subject>Pheophytins - isolation & purification</subject><subject>Pheophytins - pharmacology</subject><subject>Phytotherapy</subject><subject>Plant Extracts - isolation & purification</subject><subject>Plant Extracts - pharmacology</subject><subject>Plants, Medicinal</subject><subject>Rats</subject><subject>Sapindaceae - chemistry</subject><subject>Time Factors</subject><issn>0378-8741</issn><issn>1872-7573</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2018</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kcFu1DAQhi0EokvhAbigOXJowjjJJrE4VRW0lVbiQDlbjj1mvSRxiJ1FeS5eEC9bekQaaaTxN580_hl7yzHnyOsPh_xAU14gb3PkqapnbMPbpsiabVM-ZxssmzZrm4pfsFchHBCx4RW-ZBeFKEvBOW7Y7_sRji7OHtQYXWac6ig6DWQt6Qjegu3V0Y_emZAQA9Oe_LRfoxsD2NkPcN33p0G_BNB-cKNT8PVXDn6EuCf43i_aB4JliuoHgQpBrQG6Fe5oui2uYFdfQflQZjv-125VBKX1Miy9ii453Pj0bNzk9RopvGYvrOoDvXnsl-zb508PN3fZ7svt_c31LtOlqGOmGtXUwnS2a5XQ1JnaClFXVNkCcdtYQbbG7VYgWo1tm77RdkYoEoUlUaMuL9n7s3ea_c-FQpSDC5r6Xo3klyC5aMVWVBUWCeVnVM8-hJmsnGY3qHmVHOUpK3mQKSt5ykoiT1WlnXeP-qUbyDxt_AsnAR_PAKUjj45mGbSjUZNxcwpHGu_-o_8DtJulnA</recordid><startdate>20180424</startdate><enddate>20180424</enddate><creator>Semaan, D.G.</creator><creator>Igoli, J.O.</creator><creator>Young, L.</creator><creator>Gray, A.I.</creator><creator>Rowan, E.G.</creator><creator>Marrero, E.</creator><general>Elsevier 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>7X8</scope></search><sort><creationdate>20180424</creationdate><title>In vitro anti-diabetic effect of flavonoids and pheophytins from Allophylus cominia Sw. on the glucose uptake assays by HepG2, L6, 3T3-L1 and fat accumulation in 3T3-L1 adipocytes</title><author>Semaan, D.G. ; Igoli, J.O. ; Young, L. ; Gray, A.I. ; Rowan, E.G. ; Marrero, E.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c396t-a7a769dbfb8a9cebd6f9964e4f20057f9ef6055900fc088201fbd9ae92fe960c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2018</creationdate><topic>3T3-L1 Cells</topic><topic>3T3-L1 differentiation</topic><topic>4-Chloro-7-nitrobenzofurazan - analogs & derivatives</topic><topic>4-Chloro-7-nitrobenzofurazan - metabolism</topic><topic>Adipocytes - drug effects</topic><topic>Adipocytes - metabolism</topic><topic>Adipogenesis - drug effects</topic><topic>Allophylus cominia</topic><topic>Animals</topic><topic>Deoxyglucose - analogs & derivatives</topic><topic>Deoxyglucose - metabolism</topic><topic>Dose-Response Relationship, Drug</topic><topic>Flavonoids - isolation & purification</topic><topic>Flavonoids - pharmacology</topic><topic>Glucose Transporter Type 4 - metabolism</topic><topic>Glucose uptake</topic><topic>Hep G2 Cells</topic><topic>Hepatocytes - drug effects</topic><topic>Hepatocytes - metabolism</topic><topic>HepG2 cells</topic><topic>Humans</topic><topic>Hypoglycemic Agents - isolation & purification</topic><topic>Hypoglycemic Agents - pharmacology</topic><topic>Insulin - pharmacology</topic><topic>L6 cells</topic><topic>Lipid Droplets - drug effects</topic><topic>Lipid Droplets - metabolism</topic><topic>Mice</topic><topic>Muscle, Skeletal - drug effects</topic><topic>Muscle, Skeletal - metabolism</topic><topic>Pheophytins - isolation & purification</topic><topic>Pheophytins - pharmacology</topic><topic>Phytotherapy</topic><topic>Plant Extracts - isolation & purification</topic><topic>Plant Extracts - pharmacology</topic><topic>Plants, Medicinal</topic><topic>Rats</topic><topic>Sapindaceae - chemistry</topic><topic>Time Factors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Semaan, D.G.</creatorcontrib><creatorcontrib>Igoli, J.O.</creatorcontrib><creatorcontrib>Young, L.</creatorcontrib><creatorcontrib>Gray, A.I.</creatorcontrib><creatorcontrib>Rowan, E.G.</creatorcontrib><creatorcontrib>Marrero, E.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Journal of ethnopharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Semaan, D.G.</au><au>Igoli, J.O.</au><au>Young, L.</au><au>Gray, A.I.</au><au>Rowan, E.G.</au><au>Marrero, E.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>In vitro anti-diabetic effect of flavonoids and pheophytins from Allophylus cominia Sw. on the glucose uptake assays by HepG2, L6, 3T3-L1 and fat accumulation in 3T3-L1 adipocytes</atitle><jtitle>Journal of ethnopharmacology</jtitle><addtitle>J Ethnopharmacol</addtitle><date>2018-04-24</date><risdate>2018</risdate><volume>216</volume><spage>8</spage><epage>17</epage><pages>8-17</pages><issn>0378-8741</issn><eissn>1872-7573</eissn><abstract>Based on ethno-botanical information collected from diabetic patients in Cuba and firstly reported inhibition of PTP1B and DPPIV enzymes activities, Allophylus cominia (A. cominia) was identified as possible source of new drugs that could be used for the treatment of type 2 diabetes mellitus (T2-DM).
in this study, the activity of the characterised extracts from A. cominia was tested on the glucose uptake using HepG2 and L6 cells, 3T3-L1 fibroblasts and adipocytes as well as their effect on the fat accumulation using 3T3-L1 adipocytes.
on 2-NBDG glucose uptake assay using HepG2 and L6 cells, extracts from A. cominia enhanced insulin activity by increasing glucose uptake. On HepG2 cells Insulin EC50 of 93 ± 21nM decreased to 13 ± 2nM in the presence of the flavonoids mixture from A.cominia. In L6 cells, insulin also produced a concentration-dependent increase with an EC50 of 28.6 ± 0.7nM; EC50 decreased to 0.08 ± 0.02nM and 5 ± 0.9nM in the presence of 100μg/ml of flavonoids and pheophytins mixtures, respectively. In 3T3-L1 fibroblasts, insulin had an EC50 of >1000nM that decreased to 38 ± 4nM in the presence of the flavonoids extract. However, in adipocytes, insulin produced a significant concentration-dependent increase and an EC50 of 30 ± 8nM was a further confirmation of the insulin responsiveness of the adipocytes to the insulin. At 100µg/ml, flavonoids and pheophytins extracts decreased fat accumulation in 3T3-L1 adipocytes by two folds in comparison to the control differentiated cells (p < 0.05). The crude extract of A. cominia did not show any enhancement of 2-NBDG uptake by 3T3-L1 adipocytes in the presence or absence of 100nM insulin. In addition, in fully differentiated adipocytes, both extracts produced significant decrease in lipid droplets in the cells and no lipid accumulation were seen after withdrawal of the extracts from the cell growth medium. However, there was no effect of both extracts on total protein concentration in cells as well as on Glut-4 transporters.
the pharmacological effects of the extracts from A. cominia observed in experimental diabetic models were shown in this study. A. cominia is potentially a new candidate for the treatment and management of T2-DM.
[Display omitted]</abstract><cop>Ireland</cop><pub>Elsevier B.V</pub><pmid>29339110</pmid><doi>10.1016/j.jep.2018.01.014</doi><tpages>10</tpages><oa>free_for_read</oa></addata></record> |
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| ispartof | Journal of ethnopharmacology, 2018-04, Vol.216, p.8-17 |
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| subjects | 3T3-L1 Cells 3T3-L1 differentiation 4-Chloro-7-nitrobenzofurazan - analogs & derivatives 4-Chloro-7-nitrobenzofurazan - metabolism Adipocytes - drug effects Adipocytes - metabolism Adipogenesis - drug effects Allophylus cominia Animals Deoxyglucose - analogs & derivatives Deoxyglucose - metabolism Dose-Response Relationship, Drug Flavonoids - isolation & purification Flavonoids - pharmacology Glucose Transporter Type 4 - metabolism Glucose uptake Hep G2 Cells Hepatocytes - drug effects Hepatocytes - metabolism HepG2 cells Humans Hypoglycemic Agents - isolation & purification Hypoglycemic Agents - pharmacology Insulin - pharmacology L6 cells Lipid Droplets - drug effects Lipid Droplets - metabolism Mice Muscle, Skeletal - drug effects Muscle, Skeletal - metabolism Pheophytins - isolation & purification Pheophytins - pharmacology Phytotherapy Plant Extracts - isolation & purification Plant Extracts - pharmacology Plants, Medicinal Rats Sapindaceae - chemistry Time Factors |
| title | In vitro anti-diabetic effect of flavonoids and pheophytins from Allophylus cominia Sw. on the glucose uptake assays by HepG2, L6, 3T3-L1 and fat accumulation in 3T3-L1 adipocytes |
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