Proteomics and Molecular Docking Analyses Reveal the Bio-Chemical and Molecular Mechanism Underlying the Hypolipidemic Activity of Nano-Liposomal Bioactive Peptides in 3T3-L1 Adipocytes
Obesity is a global health concern. Physical activities and eating nutrient-rich functional foods can prevent obesity. In this study, nano-liposomal encapsulated bioactive peptides (BPs) were developed to reduce cellular lipids. The peptide sequence NH<sub>2</sub>-PCGVPMLTVAEQAQ-CO<su...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-02-01
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| Series: | Foods |
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| Online Access: | https://www.mdpi.com/2304-8158/12/4/780 |
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| author | Sucheewin Krobthong Yodying Yingchutrakul Patompon Wongtrakoongate Hathaichanok Chuntakaruk Thanyada Rungrotmongkol Chartchai Chaichana Thanisorn Mahatnirunkul Thitikorn Chomtong Kiattawee Choowongkomon Chanat Aonbangkhen |
| author_facet | Sucheewin Krobthong Yodying Yingchutrakul Patompon Wongtrakoongate Hathaichanok Chuntakaruk Thanyada Rungrotmongkol Chartchai Chaichana Thanisorn Mahatnirunkul Thitikorn Chomtong Kiattawee Choowongkomon Chanat Aonbangkhen |
| author_sort | Sucheewin Krobthong |
| collection | DOAJ |
| description | Obesity is a global health concern. Physical activities and eating nutrient-rich functional foods can prevent obesity. In this study, nano-liposomal encapsulated bioactive peptides (BPs) were developed to reduce cellular lipids. The peptide sequence NH<sub>2</sub>-PCGVPMLTVAEQAQ-CO<sub>2</sub>H was chemically synthesized. The limited membrane permeability of the BPs was improved by encapsulating the BPs with a nano-liposomal carrier, which was produced by thin-layer formation. The nano-liposomal BPs had a diameter of ~157 nm and were monodispersed in solution. The encapsulation capacity was 61.2 ± 3.2%. The nano-liposomal BPs had no significant cytotoxicity on the tested cells, keratinocytes, fibroblasts, and adipocytes. The in vitro hypolipidemic activity significantly promoted the breakdown of triglycerides (TGs). Lipid droplet staining was correlated with TG content. Proteomics analysis identified 2418 differentially expressed proteins. The nano-liposomal BPs affected various biochemical pathways beyond lipolysis. The nano-liposomal BP treatment decreased the fatty acid synthase expression by 17.41 ± 1.17%. HDOCK revealed that the BPs inhibited fatty acid synthase (FAS) at the thioesterase domain. The HDOCK score of the BPs was lower than that of orlistat, a known obesity drug, indicating stronger binding. Proteomics and molecular docking analyses confirmed that the nano-liposomal BPs were suitable for use in functional foods to prevent obesity. |
| first_indexed | 2024-03-11T08:49:57Z |
| format | Article |
| id | doaj.art-81b7fb31f4cc4d188900f380ede641ac |
| institution | Directory Open Access Journal |
| issn | 2304-8158 |
| language | English |
| last_indexed | 2024-03-11T08:49:57Z |
| publishDate | 2023-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Foods |
| spelling | doaj.art-81b7fb31f4cc4d188900f380ede641ac2023-11-16T20:30:25ZengMDPI AGFoods2304-81582023-02-0112478010.3390/foods12040780Proteomics and Molecular Docking Analyses Reveal the Bio-Chemical and Molecular Mechanism Underlying the Hypolipidemic Activity of Nano-Liposomal Bioactive Peptides in 3T3-L1 AdipocytesSucheewin Krobthong0Yodying Yingchutrakul1Patompon Wongtrakoongate2Hathaichanok Chuntakaruk3Thanyada Rungrotmongkol4Chartchai Chaichana5Thanisorn Mahatnirunkul6Thitikorn Chomtong7Kiattawee Choowongkomon8Chanat Aonbangkhen9Center of Excellence in Natural Products Chemistry (CENP), Department of Chemistry, Faculty of Science, Chulalongkorn University, Bangkok 10330, ThailandNational Omics Center, NSTDA, Pathum Thani 12120, ThailandCenter for Neuroscience, Faculty of Science, Mahidol University, Bangkok 10400, ThailandCenter of Excellence in Biocatalyst and Sustainable Biotechnology, Department of Biochemistry, Faculty of Science, Chulalongkorn University, Bangkok 10330, ThailandCenter of Excellence in Biocatalyst and Sustainable Biotechnology, Department of Biochemistry, Faculty of Science, Chulalongkorn University, Bangkok 10330, ThailandSiriraj Center of Research Excellence for Diabetes and Obesity (SiCORE-DO), Faculty of Medicine Siriraj Hospital, Mahidol University, Bangkok 10700, ThailandNational Nanotechnology Center, NSTDA, Pathum Thani 12120, ThailandNational Nanotechnology Center, NSTDA, Pathum Thani 12120, ThailandDepartment of Biochemistry, Faculty of Science, Kasetsart University, Bangkok 10900, ThailandCenter of Excellence in Natural Products Chemistry (CENP), Department of Chemistry, Faculty of Science, Chulalongkorn University, Bangkok 10330, ThailandObesity is a global health concern. Physical activities and eating nutrient-rich functional foods can prevent obesity. In this study, nano-liposomal encapsulated bioactive peptides (BPs) were developed to reduce cellular lipids. The peptide sequence NH<sub>2</sub>-PCGVPMLTVAEQAQ-CO<sub>2</sub>H was chemically synthesized. The limited membrane permeability of the BPs was improved by encapsulating the BPs with a nano-liposomal carrier, which was produced by thin-layer formation. The nano-liposomal BPs had a diameter of ~157 nm and were monodispersed in solution. The encapsulation capacity was 61.2 ± 3.2%. The nano-liposomal BPs had no significant cytotoxicity on the tested cells, keratinocytes, fibroblasts, and adipocytes. The in vitro hypolipidemic activity significantly promoted the breakdown of triglycerides (TGs). Lipid droplet staining was correlated with TG content. Proteomics analysis identified 2418 differentially expressed proteins. The nano-liposomal BPs affected various biochemical pathways beyond lipolysis. The nano-liposomal BP treatment decreased the fatty acid synthase expression by 17.41 ± 1.17%. HDOCK revealed that the BPs inhibited fatty acid synthase (FAS) at the thioesterase domain. The HDOCK score of the BPs was lower than that of orlistat, a known obesity drug, indicating stronger binding. Proteomics and molecular docking analyses confirmed that the nano-liposomal BPs were suitable for use in functional foods to prevent obesity.https://www.mdpi.com/2304-8158/12/4/780liposomenanoparticlesadipocyteglycerollipolysisorlistat |
| spellingShingle | Sucheewin Krobthong Yodying Yingchutrakul Patompon Wongtrakoongate Hathaichanok Chuntakaruk Thanyada Rungrotmongkol Chartchai Chaichana Thanisorn Mahatnirunkul Thitikorn Chomtong Kiattawee Choowongkomon Chanat Aonbangkhen Proteomics and Molecular Docking Analyses Reveal the Bio-Chemical and Molecular Mechanism Underlying the Hypolipidemic Activity of Nano-Liposomal Bioactive Peptides in 3T3-L1 Adipocytes Foods liposome nanoparticles adipocyte glycerol lipolysis orlistat |
| title | Proteomics and Molecular Docking Analyses Reveal the Bio-Chemical and Molecular Mechanism Underlying the Hypolipidemic Activity of Nano-Liposomal Bioactive Peptides in 3T3-L1 Adipocytes |
| title_full | Proteomics and Molecular Docking Analyses Reveal the Bio-Chemical and Molecular Mechanism Underlying the Hypolipidemic Activity of Nano-Liposomal Bioactive Peptides in 3T3-L1 Adipocytes |
| title_fullStr | Proteomics and Molecular Docking Analyses Reveal the Bio-Chemical and Molecular Mechanism Underlying the Hypolipidemic Activity of Nano-Liposomal Bioactive Peptides in 3T3-L1 Adipocytes |
| title_full_unstemmed | Proteomics and Molecular Docking Analyses Reveal the Bio-Chemical and Molecular Mechanism Underlying the Hypolipidemic Activity of Nano-Liposomal Bioactive Peptides in 3T3-L1 Adipocytes |
| title_short | Proteomics and Molecular Docking Analyses Reveal the Bio-Chemical and Molecular Mechanism Underlying the Hypolipidemic Activity of Nano-Liposomal Bioactive Peptides in 3T3-L1 Adipocytes |
| title_sort | proteomics and molecular docking analyses reveal the bio chemical and molecular mechanism underlying the hypolipidemic activity of nano liposomal bioactive peptides in 3t3 l1 adipocytes |
| topic | liposome nanoparticles adipocyte glycerol lipolysis orlistat |
| url | https://www.mdpi.com/2304-8158/12/4/780 |
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