A Multitarget Approach to Evaluate the Efficacy of <i>Aquilaria</i> <i>sinensis</i> Flower Extract against Metabolic Syndrome
<i>Aquilaria sinensis</i> (Lour.) Spreng is known for its resinous secretion (agarwood), often secreted in defense against injuries. We investigated the effects of <i>A. sinensis</i> flower extract (AF) on peroxisome proliferator-activated receptors alpha and gamma (PPARα and...
| Main Authors: | , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2022-01-01
|
| Series: | Molecules |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1420-3049/27/3/629 |
| _version_ | 1797486203712307200 |
|---|---|
| author | Hee-Sung Chae Olivia Dale Tahir Maqbool Mir Bharathi Avula Jianping Zhao Ikhlas A. Khan Shabana I. Khan |
| author_facet | Hee-Sung Chae Olivia Dale Tahir Maqbool Mir Bharathi Avula Jianping Zhao Ikhlas A. Khan Shabana I. Khan |
| author_sort | Hee-Sung Chae |
| collection | DOAJ |
| description | <i>Aquilaria sinensis</i> (Lour.) Spreng is known for its resinous secretion (agarwood), often secreted in defense against injuries. We investigated the effects of <i>A. sinensis</i> flower extract (AF) on peroxisome proliferator-activated receptors alpha and gamma (PPARα and PPARγ), liver X receptor (LXR), glucose uptake, and lipid accumulation (adipogenesis). Activation of PPARα, PPARγ and LXR was determined in hepatic (HepG2) cells by reporter gene assays. Glucose uptake was determined in differentiated muscle (C2C12) cells using 2-NBDG (2-deoxy-2-[(7-nitro-2,1,3-benzoxadiazol-4-yl)amino]-D-glucose). Adipogenesis was determined in adipocytes (3T3-L1 cells) by Oil red O staining. At a concentration of 50 µg/mL, AF caused 12.2-fold activation of PPARα and 5.7-fold activation of PPARγ, while the activation of LXR was only 1.7-fold. AF inhibited (28%) the adipogenic effect induced by rosiglitazone in adipocytes and increased glucose uptake (32.8%) in muscle cells at 50 μg/mL. It was concluded that AF acted as a PPARα/γ dual agonist without the undesired effect of adipogenesis and exhibited the property of enhancing glucose uptake. This is the first report to reveal the PPARα/γ dual agonistic action and glucose uptake enhancing property of AF along with its antiadipogenic effect, indicating its potential in ameliorating the symptoms of metabolic syndrome. |
| first_indexed | 2024-03-09T23:29:53Z |
| format | Article |
| id | doaj.art-0f2204dc11bd46c3af68079e84e00d28 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-09T23:29:53Z |
| publishDate | 2022-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-0f2204dc11bd46c3af68079e84e00d282023-11-23T17:09:50ZengMDPI AGMolecules1420-30492022-01-0127362910.3390/molecules27030629A Multitarget Approach to Evaluate the Efficacy of <i>Aquilaria</i> <i>sinensis</i> Flower Extract against Metabolic SyndromeHee-Sung Chae0Olivia Dale1Tahir Maqbool Mir2Bharathi Avula3Jianping Zhao4Ikhlas A. Khan5Shabana I. Khan6National Center for Natural Products Research, School of Pharmacy, The University of Mississippi, Oxford, MS 38677, USANational Center for Natural Products Research, School of Pharmacy, The University of Mississippi, Oxford, MS 38677, USANational Center for Natural Products Research, School of Pharmacy, The University of Mississippi, Oxford, MS 38677, USANational Center for Natural Products Research, School of Pharmacy, The University of Mississippi, Oxford, MS 38677, USANational Center for Natural Products Research, School of Pharmacy, The University of Mississippi, Oxford, MS 38677, USANational Center for Natural Products Research, School of Pharmacy, The University of Mississippi, Oxford, MS 38677, USANational Center for Natural Products Research, School of Pharmacy, The University of Mississippi, Oxford, MS 38677, USA<i>Aquilaria sinensis</i> (Lour.) Spreng is known for its resinous secretion (agarwood), often secreted in defense against injuries. We investigated the effects of <i>A. sinensis</i> flower extract (AF) on peroxisome proliferator-activated receptors alpha and gamma (PPARα and PPARγ), liver X receptor (LXR), glucose uptake, and lipid accumulation (adipogenesis). Activation of PPARα, PPARγ and LXR was determined in hepatic (HepG2) cells by reporter gene assays. Glucose uptake was determined in differentiated muscle (C2C12) cells using 2-NBDG (2-deoxy-2-[(7-nitro-2,1,3-benzoxadiazol-4-yl)amino]-D-glucose). Adipogenesis was determined in adipocytes (3T3-L1 cells) by Oil red O staining. At a concentration of 50 µg/mL, AF caused 12.2-fold activation of PPARα and 5.7-fold activation of PPARγ, while the activation of LXR was only 1.7-fold. AF inhibited (28%) the adipogenic effect induced by rosiglitazone in adipocytes and increased glucose uptake (32.8%) in muscle cells at 50 μg/mL. It was concluded that AF acted as a PPARα/γ dual agonist without the undesired effect of adipogenesis and exhibited the property of enhancing glucose uptake. This is the first report to reveal the PPARα/γ dual agonistic action and glucose uptake enhancing property of AF along with its antiadipogenic effect, indicating its potential in ameliorating the symptoms of metabolic syndrome.https://www.mdpi.com/1420-3049/27/3/629<i>Aquilaria sinensis</i>ThymelaeaceaePPARLXRadipogenesisglucose uptake |
| spellingShingle | Hee-Sung Chae Olivia Dale Tahir Maqbool Mir Bharathi Avula Jianping Zhao Ikhlas A. Khan Shabana I. Khan A Multitarget Approach to Evaluate the Efficacy of <i>Aquilaria</i> <i>sinensis</i> Flower Extract against Metabolic Syndrome Molecules <i>Aquilaria sinensis</i> Thymelaeaceae PPAR LXR adipogenesis glucose uptake |
| title | A Multitarget Approach to Evaluate the Efficacy of <i>Aquilaria</i> <i>sinensis</i> Flower Extract against Metabolic Syndrome |
| title_full | A Multitarget Approach to Evaluate the Efficacy of <i>Aquilaria</i> <i>sinensis</i> Flower Extract against Metabolic Syndrome |
| title_fullStr | A Multitarget Approach to Evaluate the Efficacy of <i>Aquilaria</i> <i>sinensis</i> Flower Extract against Metabolic Syndrome |
| title_full_unstemmed | A Multitarget Approach to Evaluate the Efficacy of <i>Aquilaria</i> <i>sinensis</i> Flower Extract against Metabolic Syndrome |
| title_short | A Multitarget Approach to Evaluate the Efficacy of <i>Aquilaria</i> <i>sinensis</i> Flower Extract against Metabolic Syndrome |
| title_sort | multitarget approach to evaluate the efficacy of i aquilaria i i sinensis i flower extract against metabolic syndrome |
| topic | <i>Aquilaria sinensis</i> Thymelaeaceae PPAR LXR adipogenesis glucose uptake |
| url | https://www.mdpi.com/1420-3049/27/3/629 |
| work_keys_str_mv | AT heesungchae amultitargetapproachtoevaluatetheefficacyofiaquilariaiisinensisiflowerextractagainstmetabolicsyndrome AT oliviadale amultitargetapproachtoevaluatetheefficacyofiaquilariaiisinensisiflowerextractagainstmetabolicsyndrome AT tahirmaqboolmir amultitargetapproachtoevaluatetheefficacyofiaquilariaiisinensisiflowerextractagainstmetabolicsyndrome AT bharathiavula amultitargetapproachtoevaluatetheefficacyofiaquilariaiisinensisiflowerextractagainstmetabolicsyndrome AT jianpingzhao amultitargetapproachtoevaluatetheefficacyofiaquilariaiisinensisiflowerextractagainstmetabolicsyndrome AT ikhlasakhan amultitargetapproachtoevaluatetheefficacyofiaquilariaiisinensisiflowerextractagainstmetabolicsyndrome AT shabanaikhan amultitargetapproachtoevaluatetheefficacyofiaquilariaiisinensisiflowerextractagainstmetabolicsyndrome AT heesungchae multitargetapproachtoevaluatetheefficacyofiaquilariaiisinensisiflowerextractagainstmetabolicsyndrome AT oliviadale multitargetapproachtoevaluatetheefficacyofiaquilariaiisinensisiflowerextractagainstmetabolicsyndrome AT tahirmaqboolmir multitargetapproachtoevaluatetheefficacyofiaquilariaiisinensisiflowerextractagainstmetabolicsyndrome AT bharathiavula multitargetapproachtoevaluatetheefficacyofiaquilariaiisinensisiflowerextractagainstmetabolicsyndrome AT jianpingzhao multitargetapproachtoevaluatetheefficacyofiaquilariaiisinensisiflowerextractagainstmetabolicsyndrome AT ikhlasakhan multitargetapproachtoevaluatetheefficacyofiaquilariaiisinensisiflowerextractagainstmetabolicsyndrome AT shabanaikhan multitargetapproachtoevaluatetheefficacyofiaquilariaiisinensisiflowerextractagainstmetabolicsyndrome |