The inhibitory effects of an eight-herb formula (RCM-107) on pancreatic lipase: enzymatic, HPTLC profiling and in silico approaches
Aims: Obesity is a global, public health issue that causes or exacerbates serious medical disorders. Chinese herbal therapies have become one of the most popular alternatives due to intolerances of current anti-obesity treatments. The RCM-107 formula (granule) is modified from our previous studied R...
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| Format: | Article |
| Language: | English |
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Elsevier
2019-09-01
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| Series: | Heliyon |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2405844019361134 |
| _version_ | 1811196680783003648 |
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| author | Shiqi Luo Harsharn Gill Daniel Anthony Dias Mingdi Li Andrew Hung Linh Toan Nguyen George Binh Lenon |
| author_facet | Shiqi Luo Harsharn Gill Daniel Anthony Dias Mingdi Li Andrew Hung Linh Toan Nguyen George Binh Lenon |
| author_sort | Shiqi Luo |
| collection | DOAJ |
| description | Aims: Obesity is a global, public health issue that causes or exacerbates serious medical disorders. Chinese herbal therapies have become one of the most popular alternatives due to intolerances of current anti-obesity treatments. The RCM-107 formula (granule) is modified from our previous studied RCM-104 formula, which has demonstrated significant effects on weight reduction in randomized clinical trials. Up to date, there is no published scientific evidence to evaluate the effect of this formula on the weight-loss target pancreatic lipase and therefore, the aim of this study is to investigate the inhibitory effect of RCM-107 and respective individual ingredient on the pancreatic lipase activities. Main methods: Fluorometric based enzymatic assays, high-performance thin-layer chromatography (HPTLC) profiling and in silico molecular docking techniques were used to investigate the lipase inhibitory effects of the RCM-107 herbal formula and its respective individual herbs. Principle findings: The results demonstrated the potent lipase suppressing effect of the RCM-107 formula. The majority of the ingredients from this formula also showed pancreatic lipase inhibitory activities. The presence of the known weight-loss compounds such as (-)-epigallocatechin-3-gallate (EGCG), epicatechin-3-gallate (ECG), (-)-epicatechin (EC), rutin, crocin and caffeine were identified in the RCM-107 and related single herbs using HPTLC profiling approaches. In addition, EGCG, EC and the known lipase antagonist orlistat acted on the same site. These compounds form hydrogen bonds with corresponding residues HIS152, ASP80 and GLY77, which can be considered as markers of important areas in the ligand-binding site. This may explain the details of their roles in inhibiting pancreatic lipase activities. Conclusion: Our data has provided new knowledge to the mechanistic properties of the RCM-107 formula and its respective individual herbal ingredients for weight loss, in terms of reducing lipid absorption via the inhibition of pancreatic lipase. |
| first_indexed | 2024-04-12T01:03:02Z |
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| institution | Directory Open Access Journal |
| issn | 2405-8440 |
| language | English |
| last_indexed | 2024-04-12T01:03:02Z |
| publishDate | 2019-09-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Heliyon |
| spelling | doaj.art-0c0d0dc474bb4aa887e97e626436a5a92022-12-22T03:54:23ZengElsevierHeliyon2405-84402019-09-0159e02453The inhibitory effects of an eight-herb formula (RCM-107) on pancreatic lipase: enzymatic, HPTLC profiling and in silico approachesShiqi Luo0Harsharn Gill1Daniel Anthony Dias2Mingdi Li3Andrew Hung4Linh Toan Nguyen5George Binh Lenon6School of Health and Biomedical Sciences, RMIT University, Bundoora West Campus, Victoria, 3083, AustraliaSchool of Science, RMIT University, Bundoora West Campus, Victoria, 3083, AustraliaSchool of Health and Biomedical Sciences, RMIT University, Bundoora West Campus, Victoria, 3083, AustraliaSchool of Health and Biomedical Sciences, RMIT University, Bundoora West Campus, Victoria, 3083, AustraliaSchool of Science, RMIT University, Bundoora West Campus, Victoria, 3083, AustraliaDepartment of Endocrine, 103 Military Hospital, Vietnam Military Medical University, Hanoi, Viet NamSchool of Health and Biomedical Sciences, RMIT University, Bundoora West Campus, Victoria, 3083, Australia; Corresponding author.Aims: Obesity is a global, public health issue that causes or exacerbates serious medical disorders. Chinese herbal therapies have become one of the most popular alternatives due to intolerances of current anti-obesity treatments. The RCM-107 formula (granule) is modified from our previous studied RCM-104 formula, which has demonstrated significant effects on weight reduction in randomized clinical trials. Up to date, there is no published scientific evidence to evaluate the effect of this formula on the weight-loss target pancreatic lipase and therefore, the aim of this study is to investigate the inhibitory effect of RCM-107 and respective individual ingredient on the pancreatic lipase activities. Main methods: Fluorometric based enzymatic assays, high-performance thin-layer chromatography (HPTLC) profiling and in silico molecular docking techniques were used to investigate the lipase inhibitory effects of the RCM-107 herbal formula and its respective individual herbs. Principle findings: The results demonstrated the potent lipase suppressing effect of the RCM-107 formula. The majority of the ingredients from this formula also showed pancreatic lipase inhibitory activities. The presence of the known weight-loss compounds such as (-)-epigallocatechin-3-gallate (EGCG), epicatechin-3-gallate (ECG), (-)-epicatechin (EC), rutin, crocin and caffeine were identified in the RCM-107 and related single herbs using HPTLC profiling approaches. In addition, EGCG, EC and the known lipase antagonist orlistat acted on the same site. These compounds form hydrogen bonds with corresponding residues HIS152, ASP80 and GLY77, which can be considered as markers of important areas in the ligand-binding site. This may explain the details of their roles in inhibiting pancreatic lipase activities. Conclusion: Our data has provided new knowledge to the mechanistic properties of the RCM-107 formula and its respective individual herbal ingredients for weight loss, in terms of reducing lipid absorption via the inhibition of pancreatic lipase.http://www.sciencedirect.com/science/article/pii/S2405844019361134Analytical chemistryComputational chemistryMolecular biologyAlternative medicineEvidence-based medicineObesity |
| spellingShingle | Shiqi Luo Harsharn Gill Daniel Anthony Dias Mingdi Li Andrew Hung Linh Toan Nguyen George Binh Lenon The inhibitory effects of an eight-herb formula (RCM-107) on pancreatic lipase: enzymatic, HPTLC profiling and in silico approaches Heliyon Analytical chemistry Computational chemistry Molecular biology Alternative medicine Evidence-based medicine Obesity |
| title | The inhibitory effects of an eight-herb formula (RCM-107) on pancreatic lipase: enzymatic, HPTLC profiling and in silico approaches |
| title_full | The inhibitory effects of an eight-herb formula (RCM-107) on pancreatic lipase: enzymatic, HPTLC profiling and in silico approaches |
| title_fullStr | The inhibitory effects of an eight-herb formula (RCM-107) on pancreatic lipase: enzymatic, HPTLC profiling and in silico approaches |
| title_full_unstemmed | The inhibitory effects of an eight-herb formula (RCM-107) on pancreatic lipase: enzymatic, HPTLC profiling and in silico approaches |
| title_short | The inhibitory effects of an eight-herb formula (RCM-107) on pancreatic lipase: enzymatic, HPTLC profiling and in silico approaches |
| title_sort | inhibitory effects of an eight herb formula rcm 107 on pancreatic lipase enzymatic hptlc profiling and in silico approaches |
| topic | Analytical chemistry Computational chemistry Molecular biology Alternative medicine Evidence-based medicine Obesity |
| url | http://www.sciencedirect.com/science/article/pii/S2405844019361134 |
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