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Vetiveria zizanioides, known as vetiver grass, is renowned for its ecological significance in soil erosion control and the restoration of lands polluted by heavy metals. Additionally, this plant is extensively harvested for vetiver oil, widely utilized in both medicine and perfumery. The study was designed to investigate the phytochemicals, antilipase, hemoglobin antiglycation, antihyperglycemic, antifungal, and antibacterial properties of V. zizanioides. The GC-MS analysis revealed the presence of various volatile compounds, among which the most predominant ones, which are, 4,6,6-Trimethyl-2-(3-methylbuta-1,3-dienyl) −3-oxatricyclo [5.1.0.0(2,4)] octane, Cycloisolongifolene (8,9-dehydro-), and 9 H-Cycloisolongifolene (8-oxo-). It is noteworthy that this essential oil has shown significant inhibitory activity against α-amylase, α-glucosidase, pancreatic lipase, and glycation, with respective IC50 values of 0.47 ± 0.01, 0.42 ± 0.004, 0.58 ± 0.008, and 0.49 ± 0.005 mg/mL. Additionally, the antimicrobial activity of EoVZ was assessed against a diverse spectrum of Gram+ and Gram- bacteria, as well as fungi, using both disc-diffusion and broth-microdilution techniques. The results showed significant antimicrobial effects against all tested microorganisms, with inhibition zones ranging from 28.33 ± 1.66 mm to 9.0 ± 0.0 mm for bacteria and from 22.5 ± 1.7 mm to 14.0 ± 0.3 mm for fungi. Moreover, minimum inhibitory concentrations (MIC), minimum bactericidal concentrations (MBC), and minimum fungicidal concentrations (MFC) were determined, with values ranging from 0.0625% to 2.0% (v/v) for bacteria and from 2.0% to 8.0% (v/v) for fungi. The MBC/MIC and MFC/MIC ratios indicated bactericidal and fungicidal mechanisms. This study underscores the prominent attributes of EoVZ, particularly its antimicrobial and antidiabetic properties, suggesting its potential as a natural and effective agent ensuring high safety standards for public health. [ABSTRACT FROM AUTHOR]

Obesity is a disease of epidemic proportions with a concerning increasing trend. Regarded as one of the main sources of energy, lipids can also represent a big part of an unnecessary intake of calories and be, therefore, directly related to the problem of obesity. Pancreatic lipase is an enzyme that is essential in the absorption and digestion of dietary fats and has been explored as an alternative for the reduction of fat absorption and consequent weigh loss. Literature describes a great variability of methodologies and experimental conditions used in research to evaluate the in vitro inhibitory activity of compounds against pancreatic lipase. However, in an attempt to choose the best approach, it is necessary to know all the reaction conditions and understand how these can affect the enzymatic assay. The objective of this review is to understand and summarize the methodologies and respective experimental conditions that are mainly used to evaluate pancreatic lipase catalytic activity. 156 studies were included in this work and a detailed description of the most commonly used UV/Vis spectrophotometric and fluorimetric instrumental techniques are presented, including a discussion regarding the differences found in the parameters used in both techniques, namely enzyme, substrate, buffer solutions, kinetics conditions, temperature and pH. This works shows that both UV/Vis spectrophotometry and fluorimetry are useful instrumental techniques for the evaluation of pancreatic lipase catalytic activity, presenting several advantages and limitations, which make the choice of parameters and experimental conditions a crucial decision to obtain the most reliable results. [ABSTRACT FROM AUTHOR]

Copyright of Food & Fermentation Industries is the property of Food & Fermentation Industries and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Science & Technology of Food Industry is the property of Science & Technology of Food Industry Editorial Office and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Background: With the increasing global prevalence of type 2 diabetes (T2D) and obesity, there is a pressing need for novel therapeutic interventions. Lavandula stoechas, a medicinal plant traditionally used for various ailments, holds promise as a potential agent for T2D management, particularly in Morocco, where it is commonly used to treat diabetes. This study aims to evaluate the pharmacological potential of L. stoechas aqueous extract (AqLs) by assessing its lipase inhibition antioxidant and anti-inflammatory activities, identifying phenolic compounds, and examining its efficacy in reducing diabetic complications. Methods: The pharmacological potential of L. stoechas aqueous extract was investigated using in vitro assays. The inhibitory effect on pancreatic lipase, antioxidant power (FRAP), and anti-inflammatory activity (albumin denaturation method) was assessed. High-performance liquid chromatography (HPLC) analysis identified phenolic compounds. Additionally, albumin glycation was evaluated by estimating fructosamine, carbonyl groups, and amyloid β-structures to assess efficacy in mitigating diabetic complications. Results: The extract demonstrated concentration-dependent inhibition of pancreatic lipase (IC50 = 0.132 ± 0.006 mg/mL), potent antioxidant activity (IC50 = 604.99 ± 1.01 μg/mL), and dose-dependent anti-inflammatory effects (IC50 = 207.01 ± 34.94 mg/mL). HPLC analysis revealed phenolic compounds: naringin (38.28%), syringic acid (25.72%), and cinnamic acid (15.88%) were the most abundant, with 4-hydroxybenzoic acid, hydrated catechin, and catechin ranging from 9.60% to 5.24%, and p-coumaric acid (1.73%). Furthermore, the extract inhibited albumin glycation and fructosamine production, suggesting efficacy in mitigating diabetic complications. Conclusion: These findings highlight the multifaceted pharmacological potential of L. stoechas aqueous extract in T2D management, suggesting that this plant can be highly beneficial for diabetic individuals. [ABSTRACT FROM AUTHOR]

In order to clarify the inhibition of total flavonoids purified extract (TFSE) of sea buckthorn peel residue on pancreatic lipase, this research optimized the purification condition of total flavonoids crude extract (TFCE) of sea buckthorn peel residue using AB-8 macroporous resin by means of static and dynamic adsorption and desorption experiment. Ultra-performance liquid chromatography-high resolution mass spectrometry (UPLC-Q-MS) was used to analyze the component of TFSE. In addition, the inhibitory effect and types of TFSE on pancreatic lipase were explored through the method of nitrophenyl butyrate combined with enzymatic reaction kinetics. The results showed that the optimal purification conditions for AB-8 macroporous resin were a sample concentration of 2.2 mg/mL, a sample pH of 5.0, a sample volume of 140 mL, and a sample flow rate of 1.0 mL/min. The volume fraction of ethanol was 75% with the eluent being 120 mL and the elution flow rate being 1.5 mL/min. After separation and purification under these conditions, the purity of TFSE increased from 9.786% to 50.204%. The total of 39 phenolic compounds were identified from TFSE with flavonoids like rutin, catechins, and quercetin-3-O-glucoside being the main compounds. TFSE had a strong inhibition on pancreatic lipase with the IC50 being 12.46 mg/mL. In addition, the inhibition type was determined to be non-competitive inhibition by using double reciprocal plot method of Lineweaver-Burk with an inhibition constant Ki being 10.21 mg/mL. TFSE has better inhibitory activity on pancreatic lipase, which is of great significance for improving the added value of sea buckthorn peel residue products. [ABSTRACT FROM AUTHOR]

The rising prevalence of obesity has become a significant concern in both high income and low income countries. Addressing obesity has challenges due to the limitations in current treatment options. Dietary modifications have become a common approach in managing obesity and its associated risks. The study was aimed atinvestigating the anti-obesity effects of the methanol extract of Shorea tumbuggaia, focusing specifically on its ability to inhibit pancreatic lipase activity. Shorea tumbuggaia stem bark methanolic preparation was screened for total phenolic content and subjected to phytochemical tests for presence of secondary metabolites. The pancreas of a chicken was used to extract the lipase enzyme. Lipase inhibitory activity of various methanol extract concentrations was assessed using olive oil as the substrate. Additional docking investigations of Shorea tumbuggaia components were made to investigate the role in regulating obesity and its associated issues. The study revealed that the extract has exhibited concentration dependent inhibition of pancreatic lipase activity. The study findings on Shorea tumbuggaia lipase inhibitory activity are encouraging which may be due to the existence of secondary metabolites causing the inhibitory action. [ABSTRACT FROM AUTHOR]

Vetiveria zizanioides, known as vetiver grass, is renowned for its ecological significance in soil erosion control and the restoration of lands polluted by heavy metals. Additionally, this plant is extensively harvested for vetiver oil, widely utilized in both medicine and perfumery. The study was designed to investigate the phytochemicals, antilipase, hemoglobin antiglycation, antihyperglycemic, antifungal, and antibacterial properties of V. zizanioides. The GC-MS analysis revealed the presence of various volatile compounds, among which the most predominant ones, which are, 4,6,6-Trimethyl-2-(3-methylbuta-1,3-dienyl) −3-oxatricyclo [5.1.0.0(2,4)] octane, Cycloisolongifolene (8,9-dehydro-), and 9 H-Cycloisolongifolene (8-oxo-). It is noteworthy that this essential oil has shown significant inhibitory activity against α-amylase, α-glucosidase, pancreatic lipase, and glycation, with respective IC50 values of 0.47 ± 0.01, 0.42 ± 0.004, 0.58 ± 0.008, and 0.49 ± 0.005 mg/mL. Additionally, the antimicrobial activity of EoVZ was assessed against a diverse spectrum of Gram+ and Gram- bacteria, as well as fungi, using both disc-diffusion and broth-microdilution techniques. The results showed significant antimicrobial effects against all tested microorganisms, with inhibition zones ranging from 28.33 ± 1.66 mm to 9.0 ± 0.0 mm for bacteria and from 22.5 ± 1.7 mm to 14.0 ± 0.3 mm for fungi. Moreover, minimum inhibitory concentrations (MIC), minimum bactericidal concentrations (MBC), and minimum fungicidal concentrations (MFC) were determined, with values ranging from 0.0625% to 2.0% (v/v) for bacteria and from 2.0% to 8.0% (v/v) for fungi. The MBC/MIC and MFC/MIC ratios indicated bactericidal and fungicidal mechanisms. This study underscores the prominent attributes of EoVZ, particularly its antimicrobial and antidiabetic properties, suggesting its potential as a natural and effective agent ensuring high safety standards for public health.

Objective: To optimize the preparation process of polysaccharides from Lycium ruthenicum, analyze the monosaccharide composition and evaluate its pancreatic lipase inhibitory activity in vitro. Methods: Ultrasound-assisted aqueous two-phase extraction method was employed. Taking the overall evaluation value of polysaccharide recovery and extraction rate as the evaluation index, on the basis of single factor experiment, response surface analysis was conducted to optimize the extraction process. The composition of monosaccharides was studied by high performance liquid chromatography with pre-column derivatization. The pancreatic lipase inhibitory activity of Lycium ruthenicum polysaccharides was evaluated by p-nitrophenyl palmitate method. Results: The optimum extraction conditions: Ethanol-ammonium sulfate system, ethanol concentration 30.89%, ammonium sulfate concentration 17.00%, extraction temperature 49.05 ℃, extraction time 81.85 min, liquid to material ratio 29.80 g/g. At this time, the predicted total evaluation value was 0.9242, and the extraction and recovery rates were 104.76 mg/g and 96.96%, respectively. Lycium ruthenicum polysaccharides were composed of monosaccharides such as mannose, ribose, rhamnose, glucuronic acid, galacturonic acid, glucose, galactose and arabinose, with the relative molar ratios of 4.92:0.29:4.80:0.40:9.69:44.79:17.04:18.06, respectively. The IC50 value of Lycium ruthenicum polysaccharides inhibiting pancreatic lipase was 1.51 mg/mL. Conclusion: The preparation process of Lycium ruthenicum polysaccharides optimized by response surface methodology was stable. The detection method of monosaccharide composition was accurate and reliable. Lycium ruthenicum polysaccharides had good pancreatic lipase inhibitory activity in vitro. The results would provide a basis for the further development and utilization of Lycium ruthenicum polysaccharides.

In order to clarify the inhibition of total flavonoids purified extract (TFSE) of sea buckthorn peel residue on pancreatic lipase, this research optimized the purification condition of total flavonoids crude extract (TFCE) of sea buckthorn peel residue using AB-8 macroporous resin by means of static and dynamic adsorption and desorption experiment. Ultra-performance liquid chromatography-high resolution mass spectrometry (UPLC-Q-MS) was used to analyze the component of TFSE. In addition, the inhibitory effect and types of TFSE on pancreatic lipase were explored through the method of nitrophenyl butyrate combined with enzymatic reaction kinetics. The results showed that the optimal purification conditions for AB-8 macroporous resin were a sample concentration of 2.2 mg/mL, a sample pH of 5.0, a sample volume of 140 mL, and a sample flow rate of 1.0 mL/min. The volume fraction of ethanol was 75% with the eluent being 120 mL and the elution flow rate being 1.5 mL/min. After separation and purification under these conditions, the purity of TFSE increased from 9.786% to 50.204%. The total of 39 phenolic compounds were identified from TFSE with flavonoids like rutin, catechins, and quercetin-3-O-glucoside being the main compounds. TFSE had a strong inhibition on pancreatic lipase with the IC50 being 12.46 mg/mL. In addition, the inhibition type was determined to be non-competitive inhibition by using double reciprocal plot method of Lineweaver-Burk with an inhibition constant Ki being 10.21 mg/mL. TFSE has better inhibitory activity on pancreatic lipase, which is of great significance for improving the added value of sea buckthorn peel residue products.

Pistacia species (P. spp) have been used as a treatment for various diseases, including diabetes and inflammation. This study aimed to identify the main components of flavonoids in Pistacia species and evaluate the effect of aqueous extracts of P. spp on pancreatic enzymes and on cancer cells associated with obesity in colon and rectum. HPLC was used to identify the major components of flavonoids. The potent inhibitory effect of Pistacia species against pancreatic α-amylase, α-glucosidase and lipase was examined. The antiproliferative efficacy of the plant extract against several colorectal cancer cell lines were then measured. The main flavonoids component found in Pistacia species are quercetin-3-β-D-glucoside, rutin, kaempferol and vitexin. The starch blockade IC50 (µg/mL) of Pistacia species in a descending order were: P. lentiscus leaves: 1.09±0.01; P. atlantica leaves: 0.96±0.09 and P. atlantica fruits: 0.48±0.02. Pistacia species exerted promising inhibition effect for pancreatic lipase (PL). Besides the aglycones of P. atlantica leaves, all the tested aqueous extracts exerted appreciably novel antiproliferative activity against the tested colorectal cancer cell lines. This study provides useful indication for the Pistacia species as a potential novel therapeutic agent against diabesity and cancer.

Copyright of Journal of Molecular Science is the property of Journal of Molecular Science Editorial Office and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Food & Machinery is the property of Food & Machinery Editorial Office and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Researchers are increasingly interested in discovering new pancreatic lipase inhibitors as anti-obesity ingredients. Medicine-and-food homology plants contain a diverse set of natural bioactive compounds with promising development potential. This study screened and identified potent pancreatic lipase inhibitors from 20 commonly consumed medicine-and-food homology plants using affinity ultrafiltration combined with spectroscopy and docking simulations. The results showed that turmeric exhibited the highest pancreatic lipase-inhibitory activity, and curcumin, demethoxycurcumin, and bisdemethoxycurcumin were discovered to be potent pancreatic lipase inhibitors within the turmeric extract, with IC50 values of 0.52 ± 0.04, 1.12 ± 0.05, and 3.30 ± 0.08 mg/mL, respectively. In addition, the enzymatic kinetics analyses demonstrated that the inhibition type of the three curcuminoids was the reversible competitive model, and curcumin exhibited a higher binding affinity and greater impact on the secondary structure of pancreatic lipase than found with demethoxycurcumin or bisdemethoxycurcumin, as observed through fluorescence spectroscopy and circular dichroism. Furthermore, docking simulations supported the above experimental findings, and revealed that the three curcuminoids might interact with amino acid residues in the binding pocket of pancreatic lipase through non-covalent actions, such as hydrogen bonding and π-π stacking, thereby inhibiting the pancreatic lipase. Collectively, these findings suggest that the bioactive compounds of turmeric, in particular curcumin, can be promising dietary pancreatic lipase inhibitors for the prevention and management of obesity. [ABSTRACT FROM AUTHOR]

The rising prevalence of diabetes and the high cost of treatment necessitate the search for natural, safe, and effective treatment methods. This study examined the in vitro and in silico pancreatic lipase inhibitory activity as well as the hypoglycemic effect of the ethanol extract of Tapinanthus cordifolius (TC) leaves in mice. TC leaves were extracted with ethanol by Soxhlet extraction technique. The pancreatic lipase inhibitory activity of TC extract at various concentrations (50, 100, 200, 400, 800, and 1600 µg/mL) was evaluated using spectrophotometric method. The effect of bioactive compounds from TC extract on pancreatic lipase was assessed in silico using molecular docking approach. The hypoglycaemic effect of TC extract was evaluated in vivo by an oral glucose tolerance test (OGTT) in normoglycaemic mice. Glibenclamide (5 mg/kg) was used as the positive control. TC extract showed significant pancreatic lipase (PL) inhibitory activity with IC50 value of 294.30 ± 0.67 µg/mL, which was comparable to that of orlistat (IC50 = 195.70 ± 4.60 µg/mL). In silico studies identified campesterol, heptadecafluorononanoic acid, α-tocopherol-β-d-mannoside, clionasterol, and β-tocopherol as potent pancreatic lipase inhibitors. TC extract (200, 400, and 800 mg/kg) significantly reduced hyperglycemia in glucose-challenged mice. It exhibited a significant (p<0.05) increase in glucose absorption, similar to glibenclamide, with the most notable effect at 60 minutes post-glucose load. These findings suggest that Tapinanthus cordifolius leaf can effectively inhibit pancreatic lipase and reduce blood glucose levels, and may serve as a natural treatment alternative for diabetes mellitus. [ABSTRACT FROM AUTHOR]

Background: Coffee leaves are a major source of bioactive components and are used as ethnomedicine. However, despite their traditional medicinal use, information about their effects on antihyperlipidemia remains limited. Methods: The aims of this study were to evaluate the main components of leaf extracts from Arabica and Robusta coffees and to examine the potential of these coffee leaves in reducing lipid digestion and absorption in vitro. Results: Coffee leaf extracts from Arabica coffee contain a high amount of caffeine, whereas extracts from Robusta coffee contain high amounts of chlorogenic acid (CGA) and caffeine. Additionally, leaf extracts from Arabica and Robusta coffee demonstrated the inhibition of pancreatic lipase, decreased micellar cholesterol solubility, and reduced bile acid binding. Furthermore, these extracts resulted in a reduction in cholesterol uptake in Caco-2 cells. Molecular docking experiments supported this discovery, showing CGA and caffeine binding to Niemann–Pick C1-like 1 (NPC1L1), a key protein in cholesterol absorption. The results indicated that CGA and caffeine can competitively bind to NPC1L1 at the cholesterol binding pocket, reducing its cholesterol binding rate. These findings suggest that coffee leaves might help suppress lipid absorption and digestion, highlighting their potential use in preventing and treating hyperlipidemia. [ABSTRACT FROM AUTHOR]

Accumulation of excessive fat in the body is an indication of obesity, which is becoming an alarming health concern around the world. Pancreatic lipase has been found to have a promising role in the digestion of dietary fats thereby inhibition of pancreatic lipase can be a therapeutic strategy for the management of obesity. Literature showed the anti‐pancreatic lipase potential of thiazolidinediones thereby the current study is designed to identify substituted thiazolidinedione‐based molecules as pancreatic lipase inhibitors. A 3D QSAR model with R2 value of 0.7283 and Stability of 0.843 was generated to determine the nature of substitution necessary for the inhibitory activity. Based on the generated 3D QSAR, the activity of 352 novel‐designed molecules was predicted and further screened through pharmacokinetic parameters. These compounds were docked into the binding site of the pancreatic lipase which led to the identification of 14 hit molecules with dock score between −9.523 to −7.604 kcal/mol. The molecular simulation studies and free energy calculation of the hit compounds i. e. 87 and 80 revealed good stability and binding in the active site of pancreatic lipase. The current study provides 14 hit molecules, which can be synthesized and further evaluated to explore their anti‐pancreatic lipase inhibitory activity. [ABSTRACT FROM AUTHOR]

Obesity is acknowledged as a significant risk factor for various metabolic diseases, and the inhibition of human pancreatic lipase (hPL) can impede lipid digestion and absorption, thereby offering potential benefits for obesity treatment. Anthraquinones is a kind of natural and synthetic compounds with wide application. In this study, the inhibitory effects of 31 anthraquinones on hPL were evaluated. The data shows that AQ7, AQ26, and AQ27 demonstrated significant inhibitory activity against hPL, and exhibited selectivity towards other known serine hydrolases. Then the structure-activity relationship between anthraquinones and hPL was further analysed. AQ7 was found to be a mixed inhibition of hPL through inhibition kinetics, while AQ26 and AQ27 were effective non-competitive inhibition of hPL. Molecular docking data revealed that AQ7, AQ26, and AQ27 all could associate with the site of hPL. Developing hPL inhibitors for obesity prevention and treatment could be simplified with this novel and promising lead compound.

ABSTRACTThe aim of this study was to investigate acid hydrolysis-bound phenols from Rosa roxburghii Tratt and their biological activities in vitro. The optimal extraction parameters were as follows: HCl concentration of 7 mol/L, extraction time of 10 h and material-liquid ratio of 1:40 g/mL. The highest yield of bound polyphenols was 495.64 ± 11.66 mg GAE/100 g DW. There were 24 phenolic compounds and 14 flavonoids released by acid hydrolysis. The antioxidant study showed that the RRT-BPs had a certain scavenging ability of free radicals in a dose-dependent manner. RRT-BPs showed good inhibitory activity against α-glucosidase and pancreatic lipase, respectively, and RRT-PBs acted as anticompetitive and mixed inhibitors against α-glucosidase and pancreatic lipase, respectively. Our study suggests that acid-hydrolysed bound phenols have good prebiotic properties and can be used as a supplement to existing alkaline-hydrolysed bound phenols to prevent chronic diseases such as diabetes and obesity.

BackgroundWith the increasing global prevalence of type 2 diabetes (T2D) and obesity, there is a pressing need for novel therapeutic interventions. Lavandula stoechas, a medicinal plant traditionally used for various ailments, holds promise as a potential agent for T2D management, particularly in Morocco, where it is commonly used to treat diabetes. This study aims to evaluate the pharmacological potential of L. stoechas aqueous extract (AqLs) by assessing its lipase inhibition antioxidant and anti-inflammatory activities, identifying phenolic compounds, and examining its efficacy in reducing diabetic complications.MethodsThe pharmacological potential of L. stoechas aqueous extract was investigated using in vitro assays. The inhibitory effect on pancreatic lipase, antioxidant power (FRAP), and anti-inflammatory activity (albumin denaturation method) was assessed. High-performance liquid chromatography (HPLC) analysis identified phenolic compounds. Additionally, albumin glycation was evaluated by estimating fructosamine, carbonyl groups, and amyloid β-structures to assess efficacy in mitigating diabetic complications.ResultsThe extract demonstrated concentration-dependent inhibition of pancreatic lipase (IC50 = 0.132 ± 0.006 mg/mL), potent antioxidant activity (IC50 = 604.99 ± 1.01 μg/mL), and dose-dependent anti-inflammatory effects (IC50 = 207.01 ± 34.94 mg/mL). HPLC analysis revealed phenolic compounds: naringin (38.28%), syringic acid (25.72%), and cinnamic acid (15.88%) were the most abundant, with 4-hydroxybenzoic acid, hydrated catechin, and catechin ranging from 9.60% to 5.24%, and p-coumaric acid (1.73%). Furthermore, the extract inhibited albumin glycation and fructosamine production, suggesting efficacy in mitigating diabetic complications.ConclusionThese findings highlight the multifaceted pharmacological potential of L. stoechas aqueous extract in T2D management, suggesting that this plant can be highly beneficial for diabetic individuals.

To understand the effects of natural fermentation on the changes of phenolic substances in Citrus microcarpa and the inhibition of digestive enzymes, the changes of soluble total phenol, total flavone, α-amylase, α-glucosidase, and pancreatic lipase inhibition rates before and after fermentation were measured. The types of phenolic substances before and after fermentation were identified by UPLC-Q Exactive Orbitrap-MS, and the differential metabolites and their enrichment pathways were screened. Finally, the correlation relationships between the different phenolic metabolites and the inhibitory activities of the above digestion-related enzymes were analyzed based on the correlation coefficient. The results showed that natural fermentation could increase the contents of soluble total phenol and total flavone by 9.20% and 23.68%, respectively, and increase the inhibition rates of α-amylase, α-glucosidase and pancreatic lipase from 11.90% to 28.50%. A total of 52 phenolic substances were detected in Citrus microcarpa. Fermentation did not change the types of phenolic substances, but it significantly increased nine phenolic substances such as nobiletin, caffeic acid, and vitexin, and significantly decreased methoxsarin (P

Copyright of Food Research & Development is the property of Food Research & Development Editorial Department and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

BACKGROUND: Fucoidan has an anti‐obesity effect. However, there are few studies on its mechanism. In this study, we investigated the in vitro and in silico inhibitory properties of fucoidan against pancreatic lipase for the first time. We examined the changes in composition, structure, and pancreatic lipase inhibition of fucoidan during in vitro digestion. RESULTS: Simulated saliva‐gastrointestinal digestion resulted in a slight decrease in the molecular weight of fucoidan but no significant changes in the monosaccharide composition, sulfate content, and functional groups. Moreover, the digestion process significantly increased the inhibition of pancreatic lipase by fucoidan. The study on the type of inhibition showed that the inhibition of pancreatic lipase by fucoidan belonged to mixed inhibition with competitive inhibition. Molecular docking analysis showed that fucoidan could bind to the active site of pancreatic lipase. CONCLUSION: This study indicates that fucoidan can be a potential functional food for anti‐obesity. © 2024 Society of Chemical Industry. [ABSTRACT FROM AUTHOR]

Isovitexin is a main natural flavonoid component in various plants. Currently, the inhibitory effect of isovitexin on pancreatic lipase (PL) and its mechanism have not been elucidated yet. In the present study, we investigated the inhibitory effect of isovitexin on PL, as well as its interaction mechanism, using enzyme inhibition methods, spectroscopic analysis, and molecular simulations. Results showed that isovitexin possessed significant PL inhibitory activity, with IC50 values of 0.26 ± 0.02 mM. The interaction between isovitexin and PL was dominated by static quenching, and mainly through hydrogen bonding and hydrophobic interaction forces. Analysis of fluorescence spectroscopy confirmed that isovitexin binding altered the conformation of the PL. Circular dichroism (CD) spectrum indicated that isovitexin altered the secondary structure of PL by decreasing the α‐helix content and increasing the β‐fold content. Molecular simulations further characterize the conformational changes produced by the interaction between isovitexin with PL. The performed study may provide a new insight into the inhibitory mechanism of isovitexin as a novel PL inhibitor. [ABSTRACT FROM AUTHOR]

Raspberry (Rubus idaeus L.) is a fruit of great interest due to its aroma, nutritional properties, and the presence of many bioactive compounds. However, differences among cultivation systems can affect its composition and, consequently, its potential bioactivity. Herein, for the first time, raspberries grown in an aeroponic system were investigated for their chemical profile and antioxidant and anti-inflammatory activity, as well as their enzyme (α-glucosidase and pancreatic lipase) inhibitory properties in comparison to wild and conventionally cultivated fruits. High-performance liquid chromatography coupled with diode array detection (HPLC-DAD) analyses revealed the presence of gallic acid, caffeic acid, chlorogenic acid, p-coumaric acid, ferulic acid, rutin, and catechin in all the samples. The extracts exhibited in vitro anti-inflammatory activity (inhibition of nitric oxide production) regardless of the cultivation method. Of particular interest is the ability of raspberries to inhibit pancreatic lipase. With the exception of the β-carotene bleaching test, the raspberries grown in conventional and aeroponic systems were more active in terms of antioxidants than wild fruits, as evidenced by the ABTS (IC50 in the range 1.6–3.4 μg/mL), DPPH (IC50 in the range 8.9–28.3 μg/mL), and FRAP tests (24.6–44.9 μM Fe(II)/g). The raspberries from aeroponic cultivation were generally able to exert the same bioactivity as those obtained from both conventionally cultivated and wild fruits, supporting the consideration that in the future, this technology could reshape agriculture by mitigating resource constraints, fostering sustainable practices and increasing yields. [ABSTRACT FROM AUTHOR]

The novel chalcone‐sulfonate derivatives bearing thiophene motif were synthesized and characterized using 1H NMR, 13C NMR, and HRMS analysis. The evaluation of in vitro and in silico potential pancreatic lipase inhibition activity of the novel chalcone‐sulfonate derivatives bearing thiophene motif was scanned. IC50 values of compounds 5 i (28.76±2.11 μM) and 5 f (30.58±0.45 μM) were determined to be more effective pancreatic lipase inhibitors for in vitro studies. The best potential inhibitor for pancreatic lipase binding affinity was found as compound 5 f (−9.8 kcal mol−1) for in silico studies. Although compounds 5 f and 5 i were identified as the best pancreatic lipase inhibitor candidates in vitro and molecular docking studies, compounds 5 f and 5 i were predicted mutagenic and carcinogenic properties in mice according to ADMET studies. Deeply, compound 5 h was a more effective pancreatic lipase inhibitor according to enzyme inhibition, molecular docking, and ADMET studies. It can be said that compound 5 h may be a more efficient drug candidate than orlistat in the treatment of obesity. [ABSTRACT FROM AUTHOR]

Natural products are being investigated to obtain potential agents that could be used to prevent and ameliorate obesity and oxidative stress, which are two important factors that cause many metabolic disorders in the body. This study aimed to isolate and quantify the major compounds, to determine total flavonoid content, and to evaluate biological activities (antioxidant and pancreatic lipase (PL) inhibitory activity) of the methanol extract and the chloroform, ethyl acetate and the remaining aqueous subextracts of Alcea biennis Winterl. The major compound isolated from the ethyl acetate subextract was determined as tiliroside (kaempferol 3-O-β-(6″-O-trans-p-coumaroyl-glucopyranoside) using 1D-NMR and 2DNMR spectral methods. The quantification of tiliroside in the extracts was specified by the newly validated high-performance liquid chromatography (HPLC) method. Ferric-reducing antioxidant power (FRAP) assay was performed to determine the antioxidant activity and the total flavonoid content was determined. The ethyl acetate subextract was found to have the highest tiliroside (75.4263 mg/g) and total flavonoid content (189 mg QE/g) and showed the highest FRAP value (259 ± 5.1316 μM TE/g). The methanol extract had a higher PL inhibitory activity (IC50 = 100.891 ± 5.160 μg/mL) compared to the other extracts. Tiliroside exhibited higher activity (IC50 = 86.203 ± 6.323 μg/mL) than the extracts. It has been demonstrated that A. biennis may be a promising plant for treatment of obesity, and further studies should be conducted to evaluate it as a therapeutic agent. [ABSTRACT FROM AUTHOR]

By the optimization of previously established pancreatic lipase (PL) inhibitory lead, we have developed novel chromone‐containing analogues with embedded acrylate fragment as potential PL inhibitors. The analogues were designed by considering the structural features required for binding at the active site of PL enzyme with the utilization of molecular docking study. An optimized synthetic scheme was utilized for the synthesis of designed analogues of prototypes 1&2. Through in vitro PL inhibitory screening, three analogues namely, 5fj, 5gj and 9a were identified as potent PL inhibitory leads with IC50 values of 4.92, 4.23 and 3.32 μM, respectively. The protein binding of analogue 9a was analysed by fluorescence quenching study and it was found to bind at one binding site with a binding constant of 1.93 × 105 L mol−1. Analogue 9a also exhibited a competitive inhibitory mechanism with Ki value of 1.601 μM. In future, the potent lead 9a can be optimized to get a comparable or more potential PL inhibitory activity than marketed drugs. [ABSTRACT FROM AUTHOR]

Edible refined oils, which are utilized as raw materials in biodiesel production, have been replaced by by‐products (acid oil, fatty acid, deodorized distillate, and soapstock distillates) obtained from the vegetable oil refining industry, in recent years. This study aims to investigate the production of high quality biodiesel fuel in accordance with the standards (TS EN and ASTM) from sunflower soapstock acid oil. This feedstock was donated by an oil factory in the Thrace region, Turkey. Esterification reaction was performed by immobilized enzyme. For this, immobilization was carried out by covalent binding of pancreatic lipase in glutaraldehyde activated chitosan and optimum immobilization conditions were determined. The activity of the immobilized lipase and the retained activity were found to be 65.69 U/μg and 61.8%, respectively (pH: 7.5, 37°C). The Km (Michealis constant) and Vmax (maximum velocity of an enzymatically catalyzed reaction) values of the immobilized enzyme were found to be 5.1 mmol/L and 48.6 U/min/mg protein, respectively. The immobilized enzyme was employed as a biocatalyst for esterification of sunflower soapstock acid oil. Notably, an impressive yield of 75.6% was attained under the conditions of a 1:5 molar ratio of soapstock acid oil to methanol, with 10 wt% immobilized lipase as the catalyst, and a reaction temperature of 45°C for 36 h. The resulting biodiesel exhibits fuel characteristics that meet the standards outlined in TS EN 14214:2012 + A2 and ASTM D6751‐02. [ABSTRACT FROM AUTHOR]

Introduction: Obesity can lead to death with associated high-risk diseases such as cardiovascular disease, diabetes, hypertension, stroke and cancer. Obesity results from an excessive dietary fat intake. Pancreatic lipase (PL) is an enzyme that plays a major role in hydrolyzing fats into monoacylglycerol and fatty acids that can be absorbed into the small intestine. One of the strategies to treat obesity is by reducing fat absorption via PL inhibition. This study aims to search for potential PL inhibitors from selected Malaysian plants capable of reducing fat absorption. Methods: Potential PL inhibitors were virtually screened using AutoDock Vina against reported phytochemical compounds from the peels, fruits and leaves of five selected citrus plants namely Citrus aurantifolia (C. aurantifolia), C. grandis, C. medica, C. hystrix and C. microcarpa. Results: The results were classified based on the free energy of binding into three groups: high, moderate, and low inhibition. Eight compounds exhibited high activity against PL. Citrus grandis contributed the highest number of compounds, followed by C. medica, C. microcarpa, C. aurantifolia, and C. hystrix. To validate these findings, 15 methanolic extracts from various parts of these citrus plants were subjected to in vitro bioassays. Notably, the fruit extract of C. medica demonstrated the most potent PL inhibition at 62.59%, possibly due to the presence of diosmetin-6-C-glucoside. Conclusions: In conclusion, virtual screening of small molecules derived from selected citrus plants offers valuable insights into molecular docking and C. medica emerges as a potential anti-obesity plant. [ABSTRACT FROM AUTHOR]

Obesity is the imbalance between calories burned and calories expended which leads to increased consumption of energy-dense foods and physical inactivity. Obesity disorder comprises underlying causes and etiological relationships. Overweight or obese individuals can be assessed by Body mass index (BMI) measurement. Metabolic treatments and supplements are often used to prevent or reduce obesity. Lipid absorption by hydrolysis occurs by the Pancreatic lipase enzyme. So inhibition of pancreatic lipase can be suggested as an effective therapy in the treatment of obesity. The benzophenone scaffold is considered a unique structure, because of its presence in several natural and synthetic derivatives having a variety of biological activities, like anticancer, antimicrobial, and antiviral. Researchers are interested in Benzophenone motifs as they are present in pharmacologically relevant natural products. A molecular modeling technique was used to investigate the capacity of morpholino-linked benzophenone derivatives to inhibit human pancreatic lipase. An efficient method for developing novel compounds that inhibit pancreatic lipase is demonstrated by in silico docking studies and MM-GBSA binding free energy calculations. ADME investigations confirmed the similar qualities of drugs. [ABSTRACT FROM AUTHOR]

Forsythia suspensa (Thunb.) Vahl (FS) is an important plant with high edible and medicinal values. The edible fruit of FS is a common traditional medicine in China, Japan and Korea. Compared to the research on the phytochemistry and pharmacology of the fruits, study on the other parts of FS, such as leaves and flowers is still limited. In this study, an integrated strategy based on ultra-performance liquid chromatography quadrupole time of flight mass spectrometry (UPLC-QTOF-MS/MS), plant metabolomics and correlation analysis was established for comprehensively chemical characterization of fruits, leaves and flowers of FS, and discovery of α-glucosidase and pancreatic lipase inhibitory metabolites. The plant metabolic profiling of fruits, leaves and flowers of FS was performed by UPLC-QTOF-MS/MS, and a total of 74 secondary metabolites, including 15 phenylethanoid glycosides, 20 lignans, 10 cyclohexanol derivatives, 11 organic acids, 9 flavonoids, 3 triterpenes, and 10 other compounds were identified. Then, 29 differential secondary metabolites that responsible to distinguish the fruits, leaves and flowers of FS were further screened out by multivariate statistical analysis. Meanwhile, the α-glucosidase and pancreatic lipase inhibition of different parts of FS were evaluated and compared by in vitro experiments. The results demonstrated that the leaves of FS showed the highest inhibition on α-glucosidase and pancreatic lipase with IC50 of 0.17 ± 0.04 mg/mL and 0.56 ± 0.33 mg/mL, respectively. Then, the correlation between differential metabolites and enzyme inhibitory activities were investigated by Pearson correlation analysis, and 12 potential α-glucosidase and pancreatic lipase inhibitors were screen out. Additionally, the α-glucosidase and pancreatic lipase inhibitory activities of five potential enzyme inhibitory components, including quercitrin, rutin, kaempferol-3-O-rutinoside, pinoresinol-4-O-glucoside and phillyrin were further validated by in vitro assays and molecular docking analysis. The results showed that all the five potential inhibitors showed good inhibitory effects on α-glucosidase and pancreatic lipase, and the binding of the five inhibitors to enzymes mainly through hydrogen bonding, hydrophobic force, and ionic bonding. This study provided a feasible strategy for comparison and discrimination of different parts of medicinal plant and discovery of bioactive components, and also provided useful information for future utilization of different parts of FS.

Obesity is a global pandemic, thus novel developments that reduce the absorption of fats is of interest. We have evaluated the effect of graphene oxide (GO) on the lipase catalyzed hydrolysis of fats (tributyrin, sunflower and olive oil) under simulated duodenal conditions. Results indicate that the presence of GO in the digestion mixture can inhibit lipase activity up to a 90% of the initial reaction rate, and this inhibition lasts even during 2 h of digestion. The inhibition mechanism seems non competitive and could be opposite to the effect of bile salts, although the direct interaction between GO and the enzyme cannot be discarded. The inhibition is found also in alimentary fats suggesting that GO could be a strong inhibitor for fat hydrolysis.

ABSTRACTTo effectively utilize the by-products of skipjack tuna (Katsuwonus Pelamis) for the preparation of peptides with lipid-lowering activity, alkaline proteinase was selected from six commercial proteases to hydrolyze dark muscle. An L16 (54) orthogonal design was employed to optimize the hydrolysis conditions, resulting in the production of a high-peptide-content hydrolyzate named KPHs-AL. This hydrolyzate exhibited the ability to significantly reduce TG content. KPHs-AL also showed higher persuasive pancreatic lipase (PL) and cholesterol esterase (CEase) inhibitory potential than various molecular weight (Mw) fractions and other enzymatic hydrolyzates, with IC50 values of 5.14 and 8.51 mg/mL, respectively. Furthermore, KPHs-AL exerted a combined effect of regulating lipid accumulation in FAA-induced steatosis HepG2 cells, leading to decreased total cholesterol (TC) and total triglyceride (TG). Based on the high binding likelihood and interaction with specific binding sites predicted by Pepsite2, 38 peptide sequences were identified as potential PL and CEase inhibitors. Hence, KPHs-AL holds promise as a beneficial component of functional food and exhibits the potential for anti-obesity effects through the alleviation of lipid accumulation

In this study, the inhibitory effect of rape bee pollen polyphenols on pancreatic lipase was measured by enzyme kinetics method, and the interaction between pancreatic lipase and rape bee pollen polyphenol extracts was analyzed by the ultravilolet, fluorescence spectra and synchronous fluorescence spectra. The results showed that rape bee pollen polyphenols had a certain inhibitory effect on the activity of pancreatic lipase, and the half maximal inhibitory concentration (IC50) was 1.670±0.045 mg/mL. The inhibitory type was a mixed inhibition of reversible inhibition. Fluorescence spectra showed that the maximal fluorescence intensity of pancreatic lipase gradually decreased with the increasing of rape bee pollen polyphenols concentration, and the maximal fluorescence peak had a redshift from 341 nm to 349 nm. Synchronous fluorescence spectra showed that the hydrophobicity inside the enzyme decreased and the stretch of the peptide chain increased when polyphenols bind to pancreatic lipase. The fluorescence quenching mechanism showed that the quenching constant decreased from 0.1000 to 0.0743 with increasing temperature, and the binding process was static quenching with about one binding site. In conclusion, the rape bee pollen polyphenols could inhibit the pancreatic lipase activity by changing the enzyme conformation, which provided a certain theoretical basis for the mechanism of bee pollen lipid reduction.

Background: Coffee leaves are a major source of bioactive components and are used as ethnomedicine. However, despite their traditional medicinal use, information about their effects on antihyperlipidemia remains limited. Methods: The aims of this study were to evaluate the main components of leaf extracts from Arabica and Robusta coffees and to examine the potential of these coffee leaves in reducing lipid digestion and absorption in vitro. Results: Coffee leaf extracts from Arabica coffee contain a high amount of caffeine, whereas extracts from Robusta coffee contain high amounts of chlorogenic acid (CGA) and caffeine. Additionally, leaf extracts from Arabica and Robusta coffee demonstrated the inhibition of pancreatic lipase, decreased micellar cholesterol solubility, and reduced bile acid binding. Furthermore, these extracts resulted in a reduction in cholesterol uptake in Caco-2 cells. Molecular docking experiments supported this discovery, showing CGA and caffeine binding to Niemann–Pick C1-like 1 (NPC1L1), a key protein in cholesterol absorption. The results indicated that CGA and caffeine can competitively bind to NPC1L1 at the cholesterol binding pocket, reducing its cholesterol binding rate. These findings suggest that coffee leaves might help suppress lipid absorption and digestion, highlighting their potential use in preventing and treating hyperlipidemia.

Lilium brownii var. viridulum is one of the main traditional edible and medicinal lily in China. This study aimed to explore the extraction technology, physicochemical properties and functional activity of polysaccharide from Lilium brownii var. viridulum, used Lilium brownii var. viridulum scales as materials, polysaccharide yield as the index, solid-liquid ratio, extraction time and extraction temperature as factors to optimize the extraction process of lily polysaccharide. Then the polysaccharide was purified through removing protein. The physicochemical properties of the polysaccharides were analyzed, and the antioxidant and lipid-lowering abilities were measured in vitro. The results showed that the optimal extraction conditions were the material to liquid ratio 1:20 g/mL, extraction time 20 min, extraction temperature 75℃, and polysaccharide yield was 11.98%. The contents of total sugar, uronic acid and protein of crude polysaccharide were 58.46%, 8.06% and 10.85%, respectively. After deproteinization, the contents of total sugar and uronic acid of polysaccharide were increased to 84.78% and 15.41%, respectively, and the content of protein was reduced to 4.73%. The scavenging rates of 10 mg/mL deproteinized polysaccharide for DPPH and ABTS+ free radicals were 8.75% and 38.59%, respectively, which were lower than those of control VC. The inhibition rate of deproteinized polysaccharide for pancreatic lipase was 85.78%, which was higher than that of the control orlistat, indicating good inhibit pancreatic lipase effect in vitro. These results would provide a basis for further study on the structure-activity relationship and development of potential functional food, and provide theoretical reference for the application of lily.

Obesity is a major public health problem that is associated with many metabolic disorders including diabetes, hypertension, and cardiovascular diseases. Anthophycus longifolius is a brown seaweed that have been shown to possess antioxidant, antibacterial and anti-inflammatory activities. The present study investigated the anti-diabetic, anti-obesity and oxidative stress ameliorating properties of cold water (CW) and ethanolic (EtOH) extracts of A. longifolius using in vitro and ex vivo experimental models. The extracts significantly inhibited the activities of carbohydrate and lipid digestive enzymes α - glucosidase (IC50 = CW: 176.9±2.1 µg/ml; EtOH: 179.8±1.9 µg/ml); α-amylase (IC50 = CW: 86.1±1.7 µg/ml; EtOH: 77.8±1.9 µg/ml); and pancreatic lipase (IC50 = CW: 184.3±1.7 µg/ml; EtOH: 534.1±2.3 µg/ml), and stimulated adipose glucose uptake (CW: 10- 50.5 mg/g adipose tissue; EtOH: 9 - 79 mg/g adipose tissue). Incubation of adipose tissues with FeSO4 significantly depleted reduced glutathione (GSH) level, super oxide dismutase (SOD) and catalase activities, while concomitantly elevated malondialdehyde (MDA) level. These changes were significantly reversed following the treatment of A. longifolius extracts. Liquid chromatography-mass spectrometry (LC-MS) analysis of the extracts revealed the presence of rhodomycinone, salsolinol, 5-hydroxyconiferyl alcohol, 2-caffeoylisocitrate and demethylalangiside in the cold water extract, while petromyzonol 24-sulfate, atractyloside, abyssinone VI and podecdysone B in the ethanolic extract. Molecular docking analysis revealed potent interactions of the phytochemicals with GLUT4 and leptin. These results indicate the possible antidiabetic, antiobesity and oxidative stress ameliorating potentials of A. longifolius extracts at in vitro and ex vivo experimental models. The identified compounds may be responsible for the observed biological activities.

Nattokinase is an alkaline serine protease secreted by natto during fermentation. Despite its good thrombolytic effect, it is intolerant to gastrointestinal conditions and is easily digested and degraded into polypeptides, oligopeptides, and amino acids. However, whether these peptides inhibit fat-digesting enzymes and other biological activities remains unknown. To explore the bioactivity of peptides produced through nattokinase degradation, nattokinase was subjected to simulated digestion in the gastrointestinal tract, and 41 small peptides were obtained through the enzymolysis of gastric enzymes, pancreases, and chymotrypsin. Four pancreatic lipase (PL) inhibitory peptides (SW, ASF, GAY, and PGGTY) were selected based on their activity scores, water solubility, and toxicity predictions. The molecular docking results revealed that hydrogen bonds and electrostatic interactions were the main forces for inhibiting PL activity. The results of enzyme activity verification revealed that all four peptides inhibited PL activity. Among them, GAY exhibited the strongest inhibitory effect, with an inhibitory rate of 10.93 % at a concentration of 1 mg/mL. Molecular dynamics simulations confirmed that the GAY–1ETH complex demonstrated good stability. Natto foods containing nattokinase own the activity of inhibiting fat-digesting enzymes and show antiobesity potentials.

Plant-based therapies are widely utilized for treating diseases in approximately 80% of the global population, including Colombia's Chocó Department. This study aimed to identify and evaluate plants with significant therapeutic value for obesity and diabetes in Chocó. The inhibitory effects of these plants on pancreatic lipase (PL), α-glucosidase (AG), and α-amylase (AA) were assessed, and the most promising species were selected to isolate and identify bioactive components. Artocarpus altilis, Momordica balsamina, Bauhinia picta, Neurolaena lobata, and Vismia macrophylla emerged as key species based on their traditional usage among the Chocó population. Notably, the extract derived from Vismia macrophylla demonstrated the most encouraging outcomes as a digestive enzyme inhibitor, exhibiting IC50 values of 0.99 ± 0.21 μg/mL, 5.61 ± 0.82 mg/mL, and 28.91 ± 2.10 μg/mL for AG, AA, and PL, respectively. Further chemical analysis led to the isolation of three bioactive compounds: 5′-demethoxycadensin G 1, para-hydroxybenzoic acid methyl ester 2, and para-hydroxybenzoic acid butyl ester 3. Compound 1 displayed the highest activity against AG (IC50 = 164.30 ± 0.11 μM), while compounds 2 (IC50 = 28.50 ± 4.07 μM) and 3 (IC50 = 10.15 ± 3.42 μM) exhibited potent inhibitory effects on PL. Molecular docking and enzymatic kinetics studies indicate that these bioactive compounds primarily act as mixed inhibitors of AG and non-competitive inhibitors of PL. These findings underscore the potential of V. macrophylla and its compounds as effective inhibitors of digestive enzymes associated with obesity and type 2 diabetes. [ABSTRACT FROM AUTHOR]

Studies of a rare homozygous missense mutation identified in two brothers diagnosed with congenital pancreatic lipase deficiency (CPLD) provided the first definitive evidence linking CPLD with missense mutations in the gene of PNLIP. Herein, we investigated the molecular basis for the loss-of-function in the three novel PNLIP variants (c.305G > A, p.(W102∗); c.562C > T, p.(R188C); and c.1257G > A, p.(W419∗)) associated with CPLD. We characterized three novel PNLIP variants in transfected cells by assessing their secretion, intracellular distribution, and markers of endoplasmic reticulum (ER) stress. All three variants had secretion defects. Notably, the p.R188C and p.W419∗ variants induced misfolding of PNLIP and accumulated as detergent-insoluble aggregates resulting in elevated BiP at both protein and mRNA levels indicating increased ER stress. All three novel PNLIP variants cause a loss-of-function through impaired secretion. Additionally, the p.R188C and p.W419∗ variants may induce proteotoxicity through misfolding and potentially increase the risk for pancreatic acinar cell injury. [ABSTRACT FROM AUTHOR]

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This paper provides a comprehensive account of the synthesis and assessment of newly developed aryl sulfonate derivatives based on benzothiazole as enzyme inhibitors, specifically focusing on their ability to target tyrosinase, amylase, and pancreatic lipase. The assessments were performed utilizing experimental (in vitro) and computational (in silico) methodologies. For this aim, nine different aryl sulfonate derivatives were synthesized. The synthesized compounds were subjected to structural characterizations by utilizing Nuclear Magnetic Resonance (1H NMR, 13C NMR) and High‐Resolution Mass Spectrometry (HRMS) studies, which provided confirmation of their structural properties. The inhibitory efficiency of the compounds was determined by measuring their 50 % inhibitory concentration (IC50) values and comparing them with the standard inhibitory compounds. According to the in vitro amylase activity, benzo[d]thiazol‐2‐yl 4‐methylbenzenesulfonate showed the best inhibition with the lowest IC50 value (43.31±4.3 μM) which was calculated to be at a close level to the IC50 value of standard acarbose (38.50±3.8 μM). Also, benzo[d]thiazol‐2‐yl 4‐bromobenzenesulfonate (22.73±4.15 μM) and benzo[d]thiazol‐2‐yl 4‐chlorobenzenesulfonate (25.28±1.95 μM) were calculated to have the lowest IC50 values and the most effective inhibition capacities against pancreatic lipase. Benzo[d]thiazol‐2‐yl 4‐fluorobenzenesulfonate and benzo[d]thiazol‐2‐yl 4‐methylbenzenesulfonate significantly exhibited superior tyrosinase inhibition compared to other derivatives and conventional kojic acid. In silico molecular docking affirmed that benzo[d]thiazol‐2‐yl naphthalene‐2‐sulfonate presented the highest binding affinities to the studied enzymes, with values of −7.8 kcal/mol for tyrosinase, −10.7 kcal/mol for pancreatic lipase, and −9.4 kcal/mol for α‐amylase. The pharmacokinetic characteristics and drug‐likeness of the synthesized sulfonate derivatives were also evaluated using absorption, distribution, metabolism, excretion, and toxicity (ADMET) prediction. Density Functional Theory (DFT) calculations were employed at the DFT/B3LYP/6‐311 g(d,p) level of theory to investigate the electronic characteristics of the compounds, therefore facilitating the comprehension of the reported enzyme inhibitory actions. In summary, our research highlights the potential of benzothiazole aryl sulfonate derivatives as effective enzyme inhibitors that hold promise for therapeutic applications. [ABSTRACT FROM AUTHOR]

The coral-derived fungus Aspergillus austwickii SCSIO41227 from Beibu Gulf yielded four previously uncharacterized compounds, namely asperpentenones B–E (1–4), along with twelve known compounds (5–16). Their structures were elucidated using HRESIMS and NMR (1H and 13C NMR, HSQC, HMBC), among which the stereo-structure of compounds 1–3 was determined by calculated ECD. Furthermore, compounds 1–16 were evaluated in terms of their enzyme (acetylcholinesterase (AChE), pancreatic lipase (PL), and neuraminidase (NA)) inhibitory activities. These bioassay results revealed that compounds 2 and 14 exerted noticeable NA inhibitory effects, with IC50 values of 31.28 and 73.64 μM, respectively. In addition, compound 3 exhibited a weak inhibitory effect against PL. Furthermore, these compounds showed the potential of inhibiting enzymes in silico docking analysis to demonstrate the interactions between compounds and proteins. [ABSTRACT FROM AUTHOR]

A new furanone analog, (E)-2-(8,9-dihydroxy-6,8-dimethyldec-4-en-2-yl)-met-hylfuran-3(2H)-one (1), together with six known compounds, including two diterpenoids (2 and 3), one butyrolactone (4) and three isocoumarins (5–7), were isolated from a deep-sea fungus, Purpureocillium sp. SCSIO 06693. Among them, compound 1 existed as two tautomeric forms (1a and 1b) differing in configuration of the furan ring. The chemical structures were elucidated by the basis of spectroscopic evidences, including HRESIMS, NMR and optical rotation. Isolated compounds were evaluated for their cytotoxic, antiviral, antibacterial, antioxidant, acetyl cholinesterase (AChE) and pancreatic lipase (PL) enzyme inhibitory activities. Biological evaluation results revealed that compound 4 showed modest antioxidant activity against DPPH with IC50 value of 72.03 μM. In addition, compounds 1–4 exhibited PL enzyme inhibitory activities. [ABSTRACT FROM AUTHOR]

Pouteria cambodiana is a perennial plant that has a wide distribution in tropical regions. It is commonly referred to as 'Nom-nang' in the northern region of Thailand. The bark of this plant has been used for the purpose of promoting lactation among breastfeeding mothers. Moreover, P. cambodiana bark has a high nutraceutical potential due to the presence of saponins, which are secondary metabolites. The purpose of this study was to determine the optimal conditions for ultrasound-assisted extraction (UAE) of saponins from the bark of P. cambodiana and to assess the in vitro inhibitory activities of saponin-rich extracts. The most effective extraction conditions involved a temperature of 50 °C and a 50% concentration level of ethanol as the solvent, which allowed the extraction of saponin at a concentration of 36.04 mg/g. Saponin-rich extracts and their hydrolysates from P. cambodiana bark were evaluated for their ability to inhibit α-glucosidase and pancreatic lipase. The IC50 values for saponin- and sapogenin-rich extracts inhibiting α-glucosidase were 0.10 and 2.98 mg/mL, respectively. Non-hydrolysed extracts also had a stronger inhibitory effect than acarbose. In the case of pancreatic lipase, only the hydrolysed extracts exhibited inhibitory effects on pancreatic lipase (IC50 of 7.60 mg/mL). Thus, P. cambodiana bark may be an applicable natural resource for preparing ingredients for functional products with inhibitory activity against α-glucosidase and pancreatic lipase. The phenolic contents, saponin contents, and antioxidant activities of the dried extract stored at a low temperature of 25 °C for 2 months showed the best stability, with more than 90% retention. [ABSTRACT FROM AUTHOR]

Regulation of diacylglycerol acyltransferase (DGAT) and pancreatic lipase (PL) activities is important in the treatment of triacylglycerol (TG)-related metabolic diseases. Garcinia mangostana, also known as mangosteen, is a traditional medicine ingredient used in the treatment of inflammation in Southeast Asia. In this study, the ethanolic extract of G. mangostana peel inhibited human recombinant DGAT1 and DGAT2, and PL enzyme activities in vitro. The inhibitory activity of DGAT1 and DGAT2 enzymes of four representative bioactive substances in mangosteen was confirmed. In addition, G. mangostana was confirmed to suppress the serum TG levels in C57 mice by inhibiting the absorption and synthesis of TG in the gastrointestinal tract. Through this study, it was revealed that G. mangostana extract could be useful for the prevention and amelioration of TG-related metabolic diseases such as obesity and fatty liver. [ABSTRACT FROM AUTHOR]

This review highlights the importance of controlling the digestion process of orally administered lipid-based delivery systems (LBDS) and their performance. Oral LBDS are prone to digestion via pancreatic lipase in the small intestine. Rapid or uncontrolled digestion may cause the loss of delivery system integrity, its structural changes, reduced solubilization capacity and physical stability issues. All these events can lead to uncontrolled drug release from the digested LBDS into the gastrointestinal environment, exposing the incorporated drug to precipitation or degradation by luminal proteases. To prevent this, the digestion rate of orally administered LBDS can be estimated by appropriate choice of the formulation type, excipient combinations and their ratios. In addition, in vitro digestion models like pH-stat are useful tools to evaluate the formulation digestion rate. Controlling digestion can be achieved by conventional lipase inhibitors like orlistat, sterically hindering of lipase adsorption on the delivery system surface with polyethylene glycol (PEG) chains, lipase desorption or saturation of the interface with surfactants as well as formulating LBDS with ester-free excipients. Recent in vivo studies demonstrated that digestion inhibition lead to altered pharmacokinetic profiles, where C max and T max were reduced in spite of same AUC compared to control or even improved oral bioavailability. [Display omitted] [ABSTRACT FROM AUTHOR]

Agaricus bisporus is well known as a source of polysaccharides that could improve human health. The objective of this study was to explore the anti-obesity effect of A. bisporus extract (ABE), abundant in polysaccharides, and its underlying mechanism. Pancreatic lipase inhibitory activity in vitro was determined after treatment with ABE and chitosan. Treatment with ABE and chitosan significantly decreased pancreatic lipase activity. Five-week-old male SD rats were randomly divided into three groups for acute feeding with vehicle, ABE at 80 mg/kg body weight (BW)/day, and ABE at 160 mg/kg BW/day. ABE dose-dependently increased plasma lipid clearance in an oral lipid tolerance test. Five-week-old male C57BL/6N mice were fed a control diet (CD), a high-fat diet (HFD), an HFD with ABE at 80 mg/kg BW/day, ABE at 160 mg/kg BW/day, or chitosan at 160 mg/kg BW/day for eight weeks. HFD-fed mice showed significant increases in body weight, fat mass, white adipose tissue, average lipid droplet size, and serum levels of glucose, triglyceride, ALT, and AST compared to those in the CD group. However, ABE or chitosan administration ameliorated these increases. ABE or chitosan significantly reduced dietary efficiency and increased fecal excretion levels of lipids, triglycerides, and total cholesterol. These in vitro and in vivo findings suggest that ABE might act as an anti-obesity agent by inhibiting pancreatic lipase-mediated lipid absorption, at least in part. [ABSTRACT FROM AUTHOR]