Pancreatic Lipase Inhibitory Effect Research Articles

Biodiversity in nutrients and biological activities of 14 highbush blueberry (Vaccinium corymbosum L.) cultivars

The present study aimed to identify nutrients (UPLC-PDA-ESI-MS/MS, HPLC-RI method) and biological activities (antioxidant activity to reduce Fe3+ and ABTS·+, pancreatic lipase inhibitory effect, α-amylase, and α-glucosidase, anti-bacterial) of 14 highbush blueberries (Vaccinium corymbosum L.) cultivars (Northern type) as well as a principal component analysis (PCA) to assess the variation of these properties in the context of biodiversity. Most of the cultivars in this research have been first presented in this paper. Phytochemical profiling of the tested highbush blueberry fruit revealed 75 bioactive compounds, including 5 macroelements, 7 microelements, 7 monophosphate nucleotides, 15 anthocyanins, 1 phenolic acid, 14 flavonols, 11 essential amino acids, 8 non-essential amino acids, 2 sugars, 7 organic acids. The PCA showed that the profile and contents of the analyzed compounds as well as their anti-bacterial, antioxidant, anti-diabetic, and anti-obesity potentials depended significantly on the tested cultivars. Thus, the study provides comprehensive data on cultivar-specific biodiversity and correlations that can be used to design novel extracts rich in polyphenolic, amino acids, and/or minerals extracts from the selected cultivars of highbush blueberry as natural and alternative sources to fulfill the growing industry demand for supplements, pharmaceuticals, and nutraceutical products.

Metabolites profiling of Sapota fruit pulp via a multiplex approach of gas and ultra performance liquid chromatography/mass spectroscopy in relation to its lipase inhibition effect.

Sapota, Manilkara zapota L., are tasty, juicy, and nutrient-rich fruits, and likewise used for several medicinal uses. The current study represents an integrated metabolites profiling of sapota fruits pulp via GC/MS and UPLC/MS, alongside assessment of antioxidant capacity, pancreatic lipase (PL), and α-glucosidase enzymes inhibitory effects. GC/MS analysis of silylated primary polar metabolites led to the identification of 68 compounds belonging to sugars (74%), sugar acids (18.27%), and sugar alcohols (7%) mediating the fruit sweetness. Headspace SPME-GC/MS analysis led to the detection of 17 volatile compounds belonging to nitrogenous compounds (72%), ethers (7.8%), terpenes (7.6%), and aldehydes (5.8%). Non-polar metabolites profiling by HR-UPLC/MS/MS-based Global Natural Products Social (GNPS) molecular networking led to the assignment of 31 peaks, with several novel sphingolipids and fatty acyl amides reported for the first time. Total phenolic content was estimated at 6.79 ±0.12 mg gallic acid equivalent/gram extract (GAE/g extract), but no flavonoids were detected. The antioxidant capacities of fruit were at 1.62 ±0.2, 1.49 ±0.11, and 3.58 ±0.14 mg Trolox equivalent/gram extract (TE/g extract) via DPPH, ABTS, and FRAP assays, respectively. In vitro enzyme inhibition assays revealed a considerable pancreatic lipase inhibition effect (IC50 = 2.2 ±0.25 mg/mL), whereas no inhibitory effect towards α-glucosidase enzyme was detected. This study provides better insight into sapota fruit's flavor, nutritional, and secondary metabolites composition mediating for its sensory and health attributes.

Identification and molecular binding mechanism of novel pancreatic lipase and cholesterol esterase inhibitory peptides from heat-treated adzuki bean protein hydrolysates

Heat-treated adzuki bean protein hydrolysates exhibit lipid-reducing properties; however, few studies have reported pancreatic lipase (PL) and cholesterol esterase (CE) inhibitory effects and elucidated the underlying mechanisms. In this study, we accomplished the identification of antiobesity peptides through peptide sequencing, virtual screening, and in vitro experiments. Furthermore, the mechanisms were investigated via molecular docking. The findings reveal that the action of pepsin and pancreatin resulted in the transformation of intact adzuki bean protein into smaller peptide fragments. The < 3 kDa fraction exhibited a high proportion of hydrophobic amino acids and displayed superior inhibitory properties for both PL and CE. Five novel antiobesity peptides (LLGGLDSSLLPH, FDTGSSFYNKPAG, IWVGGSGMDM, YLQGFGKNIL, and IFNNDPNNHP) were identified as PL and CE inhibitors. Particularly, IFNNDPNNHP exhibited the most robust biological activity. These peptides exerted their inhibitory action on PL and CE by occupying catalytic or substrate-binding sites through hydrogen bonds, hydrophobic interactions, salt bridges, and π-π stacking.

QSAR model of pancreatic lipase inhibition by phenolic acids and their derivatives based on machine learning and multi-descriptor strategy

Inhibition of pancreatic lipase can be effective in controlling or treating obesity. Phenolic acids have good pancreatic lipase inhibitory effects and are widely found in plants. The identification of phenolic acids and their derivatives that can efficiently inhibit pancreatic lipase has attracted widespread attention. Therefore, it is crucial to screen natural pancreatic lipase inhibitors efficiently by establishing quantitative structure-activity relationships (QSAR) models. In this study, machine learning was used to perform multiple computational analyses of 28 phenolic acids and their derivatives with pancreatic lipase inhibitory activity, and multiple QSAR models were established. Molecular parameters were analyzed, IC50 was predicted, and molecular docking and molecular dynamics simulations analysis were done for the screened natural compounds. The results showed that the model with the highest level of accuracy is the 2D-3D mix model with a numerator parameter value of 8 (R2fitting of 0.9537 and MAE of 0.2230), and MATS6c is a key descriptor. Further screened 5 compounds that have not yet been reported and have the potential to inhibit lipase activity (IC50pre ≤ 16.69 μM), these all bound to key residues (Tyr114 and Ser152) of pancreatic lipase, of which 3–4,1,5-carboxylic acid bound the most tightly (affinity of −9.8 kJ/mol). And the compounds-pancreatic lipase complexes (2-3-2-enoate) had good stability. The three compounds with high bioavailability have the potential to become novel pancreatic lipase inhibitors. This study provides a novel approach for the prediction of phenolic acids and their derivatives capable of inhibiting pancreatic lipase.

Antioxidant, Antidiabetic, and Anti-Obesity Properties of Apple Pulp Extracts (Malus domestica Bork): A Comparative Study of 15 Local and Commercial Cultivars from Spain.

Apples (Malus domestica Borkh.) have a great agricultural and economic impact worldwide; they also present an interesting nutritional value, and their consumption has been associated with beneficial health effects. In this study, 15 apple varieties (three commercial, 12 autochthonous genotypes) were collected from mountainous areas in Spain and were evaluated for their phenolic content, antioxidant, anti-obesity and antidiabetic activities. Quercetin was tested as the reference substance in bioassays due to its role as one of the most common flavonoids in apples and other vegetables. Total Phenolic Content (TPC) of apple pulp extracts was quantified using the Folin-Ciocalteu method. The antioxidant activity was determined by using 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenging and xanthine/xanthine oxidase (X/XO) scavenging assays. Antidiabetic and anti-obesity potential were evaluated by inhibition of alpha-glucosidase (α-GLU), advance glycation end products (AGEs) formation and pancreatic lipase. The results showed in general higher phenol content in autochthonous varieties than in commercial apple pulp extracts. Phenolic-rich extracts showed better antioxidant profiles and significantly inhibited AGEs production and the α-glucosidase enzyme in a dose-dependent manner. None of them showed pancreatic lipase inhibitory effects but in general, the genotype known as "Amarilla de Octubre" was the best in terms of TPC and bioactive properties.

In Vitro Antidiabetic, Antioxidant, and Cytotoxic Evaluation of Honeybush Tea (Cyclopia genistoides) Extracts

Background. This study evaluated in vitro antidiabetic and antioxidant properties of different extracts (n-hexane, dichloromethane (DCM), and 70% ethanol) of honeybush tea (Cyclopia genistoides). Over a period of 28 days, antiprotein glycation was evaluated and some antidiabetic indicators (α-amylase, α-glucosidase, and pancreatic lipase inhibitory effects) and antioxidant activities (DPPH, ABTS, hydroxyl radical, metal ion chelating, and reducing power) for each of the crude extracts were also investigated. The results showed that all of the tested C. genistoides extracts had strong α-amylase and lipase inhibitory activity in a concentration-dependent manner with IC50 values from 0.018 μg/ml (DCM extract) to 9.93 μg/ml (n-hexane extract), respectively. The extracts also displayed inhibitory effects on protein glycation between the 14th and 28th days. The DCM and ethanolic extracts further exhibited strong antioxidant activities as they effectively scavenged most of the radicals tested, with IC50 values ranging from 0.014–0.048 mg/ml to 0.019–0.043 mg/ml. Two hundred and seventy-four chemical constituents had been identified by GC-MS, with the n-hexane extract having the highest number of peaks (127) followed by the DCM extract (107). Six compounds were identified across all the following three extracts: decane (RT: 6.4), undecane (RT: 7.7), dodecane (RT: 9.00), phytol (RT: 21.32), heptadecanoic acid, 9-methyl, methyl ester (RT: 21.65), and 9-octadecenamide (RT: 24.30). The cytotoxicity of the extracts against C3A cell lines was determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) (MTT) assay, which demonstrated that honeybush tea had a toxicity effect ranging from 66.3–88.4 μg/ml on C3A cell lines. The results showed that honeybush has antioxidant and antidiabetic activities, which could be partially attributed to the phytochemical compounds identified within the extracts.

Pancreatic lipase inhibitory effects of peptides derived from sesame proteins: In silico and in vitro analyses

Pancreatic lipase (PL) is the main digestive enzyme that is responsible for breaking triglycerides into smaller components for absorption. Inhibition of PL can effectively reduce triglyceride absorption, helping to prevent the development of obesity. The objective of this study was to investigate the PL inhibitory activity of peptides derived from sesame (Sesamum indicum L.) in silico and in vitro. In silico proteolysis of sesame proteins with pepsin, trypsin and chymotrypsin was performed with ExPASy PeptideCutter. Six peptides (TF, EW, QWM, NIF, AGY and PIF) were screened out by PeptideRanker, SwissADME and AutoDock. Molecular docking analysis showed that these six peptides could interact directly with Phe77, His151, Ser152, Phe215 and His263 at the key sites of PL. The six peptides were further synthesized to verify their PL-inhibitory effects in vitro, and TF, EW, QWM, NIF and AGY exhibited inhibitory activity on PL with IC50 values of 751 ± 75, 907 ± 91, 986 ± 170, 1044 ± 179 and 1183 ± 179 μM, respectively. Inhibitory kinetics indicated that TF, QWM and NIF were mixed-type inhibitors of PL, while EW and AGY were uncompetitive inhibitors. Our results suggest that peptides from sesame could potentially inhibit the activity of PL.

Characterization, Antioxidant Activities, and Pancreatic Lipase Inhibitory Effect of Extract From the Edible Insect Polyrhachis vicina.

Oxidative stress and obesity are critical risk factors for metabolic syndrome. The consumption of functional food ingredients can a viable strategy to alleviate oxidative stress and obesity. In this study, the hydro-ethanolic extract of the edible insect Polyrhachis vicina was prepared and its bioactive components were characterized. The total polyphenol contents, total flavonoid contents, antioxidant and pancreatic lipase (PL) inhibitory activities of the extract were determined in vitro. In total, 60 bioactive components were tentatively identified in the P. vicina extract. Polyphenols and fatty acids were further quantified using LC-MS and GC-MS, respectively. P. vicina extract possessed excellent antioxidant and PL inhibition activities. Salicylic acid, gallic acid, liquiritigenin, and naringenin, which were the major polyphenols in the P. vicina extract, interacted with PL through hydrogen bonding, hydrophilic or hydrophobic and pi-cation interactions. Thus, P. vicina extract can be used as a nutraceutical to alleviate oxidative stress-induced disease and manage obesity.

In Vitro Antioxidant, Hypolipidemic and Anti-Lipase Potential of Joha Rice of Assam India

Present research accounts for in vitro antioxidant, hypolipidemic and pancreatic lipase inhibitory potential of two scented rice of Assam, India, namely ketoki joha and kola joha. Our result showed that ethanol extract of ketoki joha and kola joha (whole rice), particularly ketoki joha, exhibits a potent antioxidant potential when tested through DPPH•, NO•, H2O2 scavenging and lipid peroxidation inhibition assay. Among different whole rice extracts, ethanol extract of ketoki joha and kola joha at 100 μg/ml produced 76.67 % and 62.47 % inhibition of β-Hydroxy β-methylglutaryl-CoA reductase activity respectively. Ethanol and petroleum ether extracts potently inhibit cholesterol esterase. Ethyl acetate extract of ketoki joha showed the highest pancreatic lipase half maximal inhibitory concentration (IC50)= 254.28 μg/ml). In conclusion, the results showed that both rice varieties, mainly ketoki joha, possess potent antioxidant, β-Hydroxy β-methylglutaryl- CoA reductase, pancreatic lipase inhibitory effect, and cholesterol esterase inhibitory effect. Observations might suggest the role of whole joha rice in combating oxidative stress and obesity-related cardiovascular diseases, including atherosclerosis.

Phenolic Composition, In Vitro Alpha-Amylase and Pancreatic Lipase Inhibitory Effects, Anti-Inflammatory and Antioxidant Activities of Ephedra altissima

This study aimed to investigate the phytochemical composition, alpha-amylase and pancreatic lipase inhibitory activities and anti-inflammatory and antioxidant properties of the crude extracts (petroleum ether, ethyl acetate and n-butanol) obtained from the aerial parts of Ephedra altissima. The characterization of the phenolic compounds in crude extracts was performed by high performance liquid chromatographyphotodiode array detection-electrospray ionization-mass spectrometry and the in vitro alpha-amylase and pancreatic lipase inhibitory activities were evaluated using starch and p-nitrophenyl butyrate as substrates, respectively. Furthermore, the anti-inflammatory activity was carried out by bovine serum albumin denaturation method and the antioxidant capacity was assessed using five different assays. Flavonol and ï¬avone glycoside derivatives and phenolic acids, especially isovitexin-2-O-rhamnoside and vicenin II were the major compounds in the n-butanol extract. Otherwise, the ethyl acetate extract presented kaempferol-3-O-rhamnoside, quercetin-3-O-rhamnoside and protocatechuic acid as its main compounds. The n-butanol extract revealed the highest content of total phenolic compounds. The results for antioxidant activity showed that ethyl acetate extract possesses the strongest activity in all the tested methods. Moreover, the ethyl acetate extract displayed the best anti-inflammatory, alpha-amylase and pancreatic lipase inhibitory activities with half-maximal inhibitory concentration values of 126.43, 9.02 and 289.11 μg/ml, respectively. These results give obvious support to the use of Ephedra altissima in traditional medicine for the treatment of diabetic diseases. Also, the moderate alpha-amylase inhibitory activity of Ephedra altissima extracts make advantage of its therapeutic applications compared to the synthetic drugs, since their strong alphaamylase inhibitory effects are associated to many digestive adverse effects including the abnormal bacterial fermentation in the colon.

Green Synthesis of SP-SeNPs as Promising Antioxidant Agent and Pancreatic Lipase Inhibitor

The purpose of this study was to evaluate pancreatic lipase inhibitory activity and antioxidant effect of Spirulina platensis containing selenium nanoemulsion nanoparticles (SP-SeNPs). The SP-SeNPs were prepared and characterized to find mean particle size and zeta potential to evaluate the possible lipoprotein lipase and pancreatic lipase inhibitory as well as antioxidant and free radical scavenging activities. Different antioxidant tests were employed, namely, reducing power, chelating activity on Fe2+, free radical-scavenging and total antioxidant activities. The obtained results showed that the shapes of SP-SeNPs were spherical and the mean particle size was 39.86 ± 0.14 nm and negative zeta potential was +33.14. The SP-SeNP at 60 ppm and epicatechin (100 ppm) produce the same ratio of inhibition 18%. However, lipoprotein lipase activity was increased to less than 20 and 27 % at 80 and 100 ppm SP-SeNPs. Also, the present results indicate that the SP-SeNPs at concentration of 80 and 100 ppm showed inhibitory effects more than epicatechin (100 ppm) against pancreatic lipase activity. However, the reducing power of SP-SeNPs and butylated hydroxytoluene (BHT), butylated hydroxy anisole (BHA) and α-tocopherol decreased in the order of BHA&gt; SP-SeNPs &gt;BHT &gt; α-tocopherol. The chelating activity of samples increased with increasing incubation times with FeCl2. However, the chelating activity of SP-SeNPs of 1.50 mg/mL was nearly equal to EDTA at 0.037 mg/mL (43.67%) for an incubation time of 60 min. This indicates that the chelation property of the samples on Fe2+ ions may afford protection against oxidative damage. The SP-SeNPs of 6 mg/mL had the highest radical scavenging activity when compared with 0.6 mg/mL Trolox. The antioxidant activity of SP-SeNPs and both standards decreased in the order of SP-SeNPs &gt; α-tocopherol &gt; Trolox &gt; BHA &gt; BHT. The results suggested that the inhibitory activity of SP-SeNPs is closely related to the tertiary structural change in lipoprotein lipase and pancreatic lipase. Also, the antioxidant activity of SP-SeNPs could be due to presence of carotenoids, ω-3 or ω-6 polyunsaturated fatty acid, γ-linolenic acid, sulpholipides, glycolipids, potassium, zinc and selenium, vitamin A, vitamin E and a variety of minerals.

α-Glucosidase and pancreatic lipase inhibitory effects and anti-adipogenic activity of dendrofalconerol B, a bisbibenzyl from Dendrobium harveyanum

Pancreatic lipase is the key enzyme for lipid digestion. Inhibition of this enzyme can reduce lipid absorption and prevent obesity disease. A methanol extract prepared from the whole plant of Dendrobium harveyanum exhibited strong anti-lipase effect. Chromatographic separation of this plant results in the isolation of 5 known compounds including 3,4-dihydroxy-5,4′-dimethoxybibenzyl (1), dendrofalconerol A (2), dendrofalconerol B (3), daucosterol (4) and dendrocandin B (5). The structures were determined by analysis of their spectroscopic data. All compounds were evaluated for their lipase and α-glucosidase inhibitory activities. Dendrofalconerol B (3) showed noticeable lipase and α-glucosidase inhibitory effects when compared with the positive controls. Dendrofalconerol B was further studied and found to show strong anti-adipogenic activity through the suppression of PPARγ and C/EBPα expression, resulting in the reduction of cellular lipid accumulation in preadipocyte 3T3-L1 cells. Taken together, these results strongly support the potential development of dendrofalconerol B as a safe and effective treatment for metabolic diseases.

Effect of Defatting and Extraction Solvent on the Antioxidant and Pancreatic Lipase Inhibitory Activities of Extracts from Hermetia illucens and Tenebrio molitor.

Simple SummaryThe food industry is notably investing more resources on the production of nutritious, healthy, safe and sustainable products derived from edible insects. In this sense, natural extracts (or concentrated forms of compounds from natural sources) are usually food ingredients with added value for human health. This is due to their intrinsic beneficious biological activities; however, bioactive extracts from edible insects have been scarcely explored. Due to that and considering that the bioactivities of extracts might be conditioned by parameters of the technological process, we assessed how different extraction conditions, such as the defatting of the raw insect flours or the extraction solvents employed, affected two bioactivities of the resulting extracts from insects: the blocking of the digestion of fats from the diet by evaluating the inhibition of the responsible enzyme (pancreatic lipase), as well as their antioxidant activity. T. molitor and H. illucens were used, as they are two of the most known edible species for both feed and food. We observed a multibioactivity for all the extracts. Both tested processing factors differentially modulated the bioactivity of extracts from both species. We also analysed the composition of the H. illucens extracts and detected amino acids, lipids, carbohydrates, sterols and organic acids.The production of specific insect extracts with bioactive properties for human health is an emerging and innovative field for the edible insects industry, but there are unexplored extraction factors that might modulate the bioactivity of the extracts. Ultrasound-assisted extracts from T. molitor and H. illucens were produced. Effects of defatting pre-treatment and extraction solvent were evaluated on extraction yield, antioxidant activity and pancreatic lipase inhibitory effect. Chemical characterisation of defatted extracts from H. illucens was performed by GC-MS-FID. Non-defatted extracts showed higher extraction yields. Defatted extracts had similar extraction yields (around 3%). Defatted extracts had higher antioxidant activity, T. molitor being stronger than H. illucens. Antioxidant activity of T. molitor methanol extract was higher than the rest of solvents. Aqueous ethanol improved the antioxidant activity of H. illucens extracts. All extracts inhibited lipase, but no significant effect of defatting and solvent was observed for T. molitor. A significant higher inhibitory activity was observed for H. illucens, the strongest being defatted 100% and 70% ethanol H. illucens extracts. H. illucens extracts contained free amino acids and disaccharides, together with minor fractions of lipids, sterols and organic acids. These results evidence the potential of extracts obtained from edible insects as antioxidants and inhibitors of the pancreatic lipase, a simultaneous multibioactivity that might be favoured by the defatting pre-treatment of the samples and the solvent of extraction.

Phenanthrenes from Dendrobium senile and their pancreatic lipase inhibitory activity

From the whole plant of Dendrobium senile, a new phenanthrene namely 2,5,7-trihydroxy-4-methoxyphenanthrene (1) was isolated, together with seven known compounds including moscatin (2), 2,5-dihydroxy-4,9-dimethoxyphenanthrene (3), moscatilin (4), aloifol I (5), 4,4′,8,8′-tetramethoxy[1,1′-biphenanthrene]-2,2′,7,7′-tetrol (6), 2,2′,7,7′-tetrahydroxy-4,4′-dimethoxy-1,1′-biphenanthrene (7) and bleformin G (8). The structure of the new compound was elucidated by analysis of its spectroscopic data. Moscatin (2) and 2,5-dihydroxy-4,9-dimethoxyphenanthrene (3) showed appreciable pancreatic lipase inhibitory effects when compared with the positive control orlistat.

Phytochemical analysis, antioxidant activity, and pancreatic lipase inhibitory effect of ethanolic extract of Trigonella foenumgraceum L. leaves

Obesity is known as a chronic metabolic disease that can be controlled by inhibition activities of the digestive enzymes like pancreatic lipase (PL). Trigonella foenumgraceum L. named commonly as fenugreek is widely used in traditional therapies owing to its abundant health benefits. The current study aimed to characterize the phytochemical components of fenugreek leaves extract (FLE) and evaluate its inhibitory activity against PL activity. As evidence from chromatography/mass spectrometry (GC-MS) the FLE possesses various valuable bioactive compounds. In addition, phytochemical analyses using colorimetric assays validate high content of phenolic (18.32 mg of gallic acid equivalent per g dry extract) and flavonoid (41.89 mg equivalent to quercetin (EQ) per g of dry extract) compounds in FLE. PL inhibitory results revealed that the FLE competitively inhibited the activity of PL in a concentration-dependent manner within the evaluated dose ranges. Moreover, FLE demonstrated free radical scavenging ability with IC50 of 89.44 μg/mL against 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals. These findings present FLE as a natural antioxidant with inhibitory activity against PL.

Do Flavonoids from Durum Wheat Contribute to Its Bioactive Properties? A Prospective Study.

A clear gap with respect to the potential biological properties of wheat flavonoids exists in the available literature. This information is crucial for breeding programs aiming to produce new varieties presenting improved health benefits. Accordingly, advanced breeding lines of whole durum wheat were evaluated in this contribution. The highest recovery of phenolics was achieved using aqueous acetone (50:50, v/v), as verified by multi-response optimization, thus showing that phenolics could be largely underestimated by employing an inappropriate extraction. The concentration of derivatives of apigenin, the main phenolics present, ranged from 63.5 to 80.7%, as evaluated by LC–ESI-QTOF-MS. Phenolics from the breeding line 98 exhibited the highest ability in scavenging peroxyl radicals, reducing power as well as in terms of inhibition of pancreatic lipase activity, a key enzyme regulating the absorption of triacylglycerols. In contrast, none of the samples exhibited a significant anti-diabetic potential. Despite their high concentration compared to that of phenolic acids, results of this work do not support a significant antioxidant and pancreatic lipase inhibitory effect of durum wheat flavonoids. Therefore, breeding programs and animal and/or human trials related to the effect of durum wheat flavonoids on oxidative stress and absorption of triacylglycerols are discouraged at this point.

Cocoa (Theobroma cacao L.) Seed Proteins' Anti-Obesity Potential through Lipase Inhibition Using In Silico, In Vitro and In Vivo Models.

The aim of this study was to determine the pancreatic lipase (PL) inhibitory effect of cocoa protein (CP) hydrolysates (CPH) using in silico and in vitro approaches, and an in vivo high-fat diet (HF) obese rat model. The results showed better theoretical affinity on PL for cocoa peptides EEQR, GGER, QTGVQ, and VSTDVNIE released from vicilin and albumins (−6.5, −6.3, −6.2, and −6.1 kcal/mol, respectively). Absorption, distribution, metabolism, and excretion (ADMET) prediction showed the human intestinal absorption (HIA) capacity of orlistat and eight cocoa peptides, demonstrating that they presented a low probability of toxicity with values lower than 0.6, while the orlistat has a high probability of hepatotoxicity with a mean value of 0.9. CPH (degree of hydrolysis of 55%) inhibited PL with an IC50 (concentration needed to inhibit 50% of enzyme activity) value of 1.38 mg/mL. The intragastric administration of 150 mg CP/kg/day to rats increased total lipids and triglycerides excretion in feces, ranging from 11% to 15% compared to the HF-diet. The HF + CP-diet also significantly decreased (p < 0.05) the apparent rate of fat absorption compared with the HF group. These results suggest that CP has anti-obesity potential by inhibiting PL, thus helping to prevent the development of non-communicable diseases.

Pancreatic lipase and cholesterol esterase inhibitory effect of Camellia nitidissima Chi flower extracts in vitro and in vivo

Camellia nitidissima Chi is an edible medicinal plant that has potential antiobesity effects. However, the underlying mechanism is unclear. The results showed that Camellia nitidissima Chi flower extracts (CNFE) had a strong inhibitory effect on pancreatic lipase (PL), pancreatic cholesterol esterase (CEase) and cholesterol micellization in a significant dose-dependent manner. The IC50 of PL, CEase, and cholesterol solubility were 320, 200, and 600 μg/mL, respectively. Kinetic analysis showed that CNFE inhibited PL and CEase activity as a noncompetitive inhibitor. CNFE changed the microenvironment and conformation of both enzymes, which caused a decrease in enzymatic activities. Furthermore, experiments in rats showed that CNFE effectively reduced food intake and increased feces total triglycerides and total cholesterol excretion. These results not only highlight the inhibitory effect of CNFE against PL and CEase in vitro and in vivo, but also provide a starting point for the application of CNFE in weight reduction programs.

Antioxidant and pancreatic lipase inhibitory effects of flavonoids from different citrus peel extracts: An in vitro study

Obesity and oxidative damage are two important risk factors associated closely with metabolic syndrome. Utilization of functional food ingredients is considered as a feasible way to tackle these challenges. In the present study, eight representative species of citrus peel extracts (CPEs) were evaluated and compared for their flavonoid profiles, antioxidant activities, and pancreatic lipase (PL) inhibitory capacities and mechanisms. Results indicated that hesperidin, naringin, neohesperidin, narirutin and eriocitrin were the five major flavonoids in CPEs, among which hesperidin was the main active PL inhibitor. Moreover, hesperidin could interact with PL by hydrogen bonds and van der Waals forces, and the interaction would not obviously change the secondary structure of PL. Overall, ponkan peel extract, having the strongest overall antioxidant activity, the highest content of hesperidin and total phenolic compounds among all tested CPEs, is a promising natural ingredient to scavenge free radicals and manage obesity.

Melipatulinones A-C, Three Lignan-Phloroglucinol Hybrids from Melicope patulinervia.

(±)-Melipatulinones A-C (1-3), three unique enantiomeric pairs of lignan-phloroglucinol hybrids along with the biogenetically related compound melipatulignan A (4), were isolated from the leaves of Melicope patulinervia. Melipatulinones A (1) and B (2) share a novel spiro[hydrobenzofuran-2,3'-furan] 5/5/6 tricyclic ring system, while melipatulinone C (3) features an unprecedented spiro[cyclopenta[b]hydrofuran-2,3'-furan] 5/5/5 tricyclic framework. Their structures were determined by spectroscopic methods, electronic circular dichroism (ECD) calculations, and X-ray diffraction. Compounds 1-3 exhibited a pancreatic lipase inhibitory effect.