Abstract
AimsObesity 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 methodsFluorometric 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 findingsThe 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. ConclusionOur 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.
Highlights
Obesity is a worldwide epidemic leading to disorders such as hypertension, Type 2 diabetes, cardiovascular diseases and non-alcoholic fatty liver disease (Xu et al, 2015)
Chemical references EGCG, ECG, EC, caffeine, rutin, crocin, solvents used for high-performance thin layer chromatography (HPTLC) mobile phase, derivatization reagents: Fast Blue Salt B, Natural Products Reagent (NP reagent), Polyethylene glycol (PEG solution), 10% sulphuric acid reagent and p-anisaldehyde-sulfuric acid reagent were purchased from Sigma-Aldrich, Australia
All samples were screened at a concentration of 100 μg/mL and lipase activity was presented as a percentage of the control
Summary
Obesity is a worldwide epidemic leading to disorders such as hypertension, Type 2 diabetes, cardiovascular diseases and non-alcoholic fatty liver disease (Xu et al, 2015). At least 2.8 million adults die due to being overweight or obese each year (World Health Organization (WHO), 2019). Over 1.9 billion adults were overweight while more than 650 million adults were obese in 2016 (World Health Organization (WHO), 2019). Pancreatic lipase (PL), a known enzyme playing a crucial role in lipolysis, promotes fatty acids absorption in the small intestine (Buchholz and Melzig, 2015; Luo et al, 2019). Orlistat is a known effective pancreatic lipase inhibitor that has been used for the long-term weight management since 1999 (Luo et al, 2019; Rodgers et al, 2012). It can lead to gastrointestinal intolerances, including faecal urgency and faecal incontinence (Chen, 2016; Lucas and Kaplan-Machlis, Heliyon 5 (2019) e02453
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