Lipase Inhibitor Research Articles

Unraveling the metabolic pattern of angiopoietin-like 3 knock-out mouse models under fasting and fed conditions

Abstract Funding Acknowledgements Type of funding sources: Public Institution(s). Main funding source(s): University of Milan Background Angiopoietin-like 3 (ANGPTL3) is a hepatokine and a regulator of lipid and lipoprotein metabolism through lipoprotein lipase and endothelial lipase inhibition, preventing the hydrolyzation of lipoprotein-derived triglycerides. A lack of ANGPTL3 results into a hypolipidemic phenotype, with a lower profile of lipids and lipoproteins, and this is evident in humans carrying a loss of function mutation, or in cellular or in vivo models. ANGPTL3 action, from the liver, is finely regulated between oxidative and storage tissues in the fasting and postprandial phases; from the current pharmacological treatments a possible ANGPTL3 intrahepatic role besides the lipases’ inhibition is emerging, thus possibly affecting the systemic metabolism with different implications. Purpose An axis between ANGPTL3 and other Angiopoietin-like proteins is known to regulate the triglyceride partitioning after a meal or during fasting, however the effect on tissues and the following metabolic and pathologic implications are still not known. Therefore, we aim to describe the impact of ANGPTL3 deficiency in fasting or in a postprandial state, and in different compartments of the organism. Methods As models, we utilized Angptl3 Knock-out (KO) mice (C57BL6/J background) and their littermate controls (wild-type, WT) fed a chow diet for 16 weeks. We assessed the metabolic phenotype with indirect calorimetry and with lipids, glucose, and insulin tolerance tests; we evaluated changes in plasma lipids under fast, fed, and fast-refeed settings and we investigated the histology of key metabolic organs. Results ANGPTL3 KO mice fed ad libitum a chow diet are hypolipidemic (plasma triglycerides levels: 42,42±8,80 mg/dL in ANGPTL3 KO mice vs. 122,02±55,09 mg/dL in WT mice; plasma cholesterol levels: 44,00±9,11 mg/dL in ANGPTL3 KO mice vs. 76,51±15,87 mg/dL in WT mice). The oral charge lipid challenge suggests that KO mice have lower lipid levels at all time points. Conclusions This preliminary profiling of ANGPTL3 KO mice under fasting and fed conditions highlights the hypolipidemia of these models, and the potentially beneficial impact of ANGPTL3 deficiency on their metabolism compared to controls.

Fabrication of natural microcapsule with intrinsic core–shell structure as building blocks for achieving source control of obesity

Regulating oil absorption at the intestinal absorption site is a safe and effective strategy for controlling obesity. Nevertheless, all patients may experience adverse effects from medication, including lipase inhibitors. Herein, we report the preparation of natural core–shell sporopollenin microcapsules with the ultimate goal of solidifying lipids post-lipase inhibition, thus exploring a safe and effective strategy for controlling lipid absorption in obesity. Naturally occurring micro/nanoparticles provide an incredible array of potential sources for fabricating pharmaceutical microcapsule carriers. Natural pine pollen was treated with phosphoric acid to yield intact, clean, and monodisperse microcapsules. Their intrinsic core–shell structures can be harnessed as potential carriers for pharmaceutical microcapsules, ensuring their viability for large-scale production. This study proposes an innovative strategy for complementary source control of obesity utilizing natural core–shell sporopollenin microcapsules and lipase inhibitors. Natural pine pollen microcapsule carriers exhibit natural core–shell structures, tunable wetting properties, and excellent liquid absorption capabilities. Interestingly, as-prepared hydrophobic pine pollen microcapsules can be utilized for the solidification of liquid drugs. Moreover, their strong oil adsorption capability can solidify lipids in complex oil–water systems post-oral lipase inhibition. Derived from pine pollen, these natural microcapsule carriers can be produced on a large scale and boast the safety of being food-derived, making them promising candidates for essential components in obesity source control.

Chemical composition and antioxidant, enzyme inhibition and cytoprotective activity of two Antarctic lichens of the genus Psoroma (Pannariaceae)

Lichens contain different types of chemical compounds with multiple biological activities that demonstrate their potential pharmacological use. This research aims to report the metabolomic identification of the ethanolic extracts of P. antarcticum and P. hypnorum, their antioxidant, enzyme inhibitory, and their cytoprotection activity. Sixteen metabolites were identified in P. antarcticum and twelve in P. hypnorum; the extracts reported variable antioxidant activity with IC50 >350 µg/mL in DPPH·, values >18 µmol Trolox/g in ORAC and >40 µmol Trolox/g in FRAP and a phenolic compound content >10 mg GAE/g, as well as significant results in cholinesterases, α-glucosidase, pancreatic lipase, α-amylase, and tyrosinase enzyme inhibition activities with IC50 ranging from 18 to 510 µg/mL, and which were complemented by molecular docking experiments. Both extracts showed improved cytoprotection at the concentrations of 0.5 to 1.0 μg/mL. This study contributes to the knowledge of the chemical diversity of Antarctic lichen extracts and their effectiveness in the evaluation of biological activities related to neurodegenerative diseases and metabolic syndrome.

Flavonoids with lipase inhibitory activity from lemon squeezing waste: isolation, multispectroscopic and in silico studies.

Obesity is recognized as a lifestyle-related disease and the main risk factor for a series of pathological conditions, including cardiovascular diseases, hypertension and type 2 diabetes. Citrus limon is an important medicinal plant, and its fruits are rich in flavonoids investigated for their potential in managing obesity. In the present work, a green extraction applied to lemon squeezing waste (LSW) was optimized to recover pancreatic lipase (PL) inhibitors. The microwave-assisted procedure yielded an extract with higher lipase inhibitory activity than those obtained by maceration and ultrasound. The main compounds present in the extract were identified by high-performance liquid chromatographic-mass spectrometric analysis, and hesperidin, eriocitrin and 4'-methyllucenin II were isolated. The three compounds were evaluated for in vitro PL inhibitory activity, and 4'-methyllucenin II resulted in the most promising inhibitor (IC50 = 12.1 μmol L-1; Ki = 62.2 μmol L-1). Multispectroscopic approaches suggested the three flavonoids act as competitive inhibitors and the binding studies indicated a greater interaction between PL and 4'-methyllucenin II. Docking analysis indicated the significant interactions of the three flavonoids with the PL catalytic site. The present work highlights flavonoid glycosides as promising PL inhibitors and proposes LSW as a safe ingredient for the preparation of food supplements for managing obesity. © 2024 Society of Chemical Industry.

Lemon basil seed-derived peptide: Hydrolysis, purification, and its role as a pancreatic lipase inhibitor that reduces adipogenesis by downregulating SREBP-1c and PPAR-γ in 3T3-L1 adipocytes.

The purpose of this study is to assess the bioactive peptides derived from the defatted lemon basil seeds hydrolysate (DLSH) for their ability to inhibit pancreatic lipase, decrease intracellular lipid accumulation, and reduce adipogenesis. Response surface methodology (RSM) was employed to optimize trypsin hydrolysis conditions for maximizing lipase inhibitory activity (LI). A hydrolysis time of 387.06 min, a temperature of 49.03°C, and an enzyme concentration of 1.61% w/v, resulted in the highest LI with an IC50 of 368.07 μg/mL. The ultrafiltration of the protein hydrolysate revealed that the fraction below 0.65kDa exhibited the greatest LI potential. Further purification via RP-HPLC identified the Gly-Arg-Ser-Pro-Asp-Thr-His-Ser-Gly (GRSPDTHSG) peptide in the HPLC fraction F1 using mass spectrometry. The peptide was synthesized and demonstrated LI with an IC50 of 0.255 mM through a non-competitive mechanism, with a constant (Ki) of 0.61 mM. Docking studies revealed its binding site with the pancreatic lipase-colipase complex. Additionally, GRSPDTHSG inhibited lipid accumulation in 3T3-L1 cells in a dose-dependent manner without cytotoxic effects. Western blot analysis indicated downregulation of PPAR-γ and SREBP-1c levels under GRSPDTHSG treatment, while an increase in AMPK-α phosphorylation was observed, suggesting a role in regulating cellular lipid metabolism. Overall, GRSPDTHSG demonstrates potential in attenuating lipid absorption and adipogenesis, suggesting a prospective application in functional foods and nutraceuticals.

Enhancing efficiency of ultrasound-assisted biodiesel production catalyzed by Eversa® Transform 2.0 at low lipase concentration: Enzyme characterization and process optimization

This study focused on the ultrasound-assisted transesterification of simulated low-quality feedstocks using a low-cost liquid lipase Eversa® Transform 2.0 (ET2). Enzyme characterization was also performed to investigate the effect of ultrasound parameters on enzyme structure. The optimal ultrasound parameters, 40 % amplitude, and 5 % duty cycle effectively enhanced the reaction rate compared to the conventional stirring method while retaining 95 % of the enzyme activity. Analysis of circular dichroism (CD) spectra revealed the preservation of the secondary structure of ET2 under the optimal ultrasound intensities, while fluorescence spectra indicated a slight change in its tertiary structure. The implementation of a two-stage methanol dosing strategy in the ultrasound-assisted reaction effectively mitigated lipase inhibition, yielding a remarkable fatty acid methyl ester (FAME) content of 92.2 % achieved within a 12-h reaction time. Notable, this high FAME content was achieved with only a 4:1 methanol-to-oil molar ratio and a 0.5 wt% enzyme concentration. Under these optimized conditions, the ultrasound-assisted reaction also demonstrated a 15 % improvement in the final FAME content compared to the conventional stirring method. These promising results hold significant potential for advancing the field of biodiesel production via ultrasound technology, contributing substantively to sustainable energy sources.

Functional properties and structure of soluble dietary fiber obtained from rice bran with steam explosion treatment

Rice bran was modified by steam explosion (SE) treatment to investigate the effect of different steam pressure (0.4, 0.8, 1.2, 1.6, and 2.0 MPa) with rice bran through 60 mesh and rice bran pulverization (60, 80, and 100 mesh) with the steam pressure of 1.2 MPa on the functional properties and structure of soluble dietary fiber (SDF) from SE-treated rice bran. SE pretreatment enhanced glucose and cholesterol adsorption capacity, water-holding capacity, oil-holding capacity, lipase inhibition capacity and anti-oxidation properties of SDF. However, functional properties of SDF were adversely affected when steam pressure was 2.0 MPa or crushing degree of rice bran was 100 mesh. The results showed that some glycosidic and hydrogen bonds were broken, resulting in a porous honeycomb structure and decreased polymerization degree of the crystalline regions and relative crystallinity in SDF from SE-treated rice bran. In general, the optimum condition for obtaining better properties of SDF was treated for rice bran at the steam pressure of 1.2 MPa and sieve size of 60 mesh. This finding emphasizes essential information on SE treatment of rice bran in modifying the properties of SDF, which is helpful to the development and utilization of SDF from SE-treated rice bran.

Hypocholesterolemic potential of Bacillus amyloliquefaciens KAVK1 modulates lipid accumulation on 3T3-L1 adipose cells and high fat diet-induced obese rat model.

The significance of microorganisms occurring in foods is predominantly targeted due to their application for identifying a novel range of the bacterial spectrum. Diverse microbial species are capable of exhibiting potential pharmacological activities like antimicrobial and anticancer. Microbial strains capable of reducing obesity-related syndromes have also been reported. In the present study, the hypocholesterolemic efficacy of Bacillus amyloliquefaciens isolated from dairy products was scrutinised by in vitro (3T3-L1 adipose cells) and in vivo (high-fat diet-induced obese Wistar albino rats) methods. Potential cholesterol-lowering isolates were screened using a plate assay method and optimised by physical parameters. Molecular identification of the topmost five cholesterol-lowering isolates was acquired by amplification of the 16S rRNA gene region. Bacillus amyloliquefaciens strain KAVK1, followed by strains KAVK2, KAVK3, KAVK4, and KAVK5 were molecularly determined. Further, cholesterol-lowering strains degraded the spectral patterns determined by the side chain of a cholesterol molecule. The anti-lipase activity was demonstrated using the porcine pancreatic lipase inhibitory method and compared with the reference compound Atorvastatin. Lyophilised strain KAVK1 revealed maximum pancreatic lipase inhibition. Strain KAVK1 attenuated lipid accumulation in 3T3-L1 adipose cell line predicted by Oil Red O staining method. Significant reduction of body weight and change in lipid profile was recognised after the supplement of KAVK1 to obese rats. Histopathological changes in organs were predominantly marked. The result of this study implies that the cholesterol-lowering B. amyloliquefaciens KAVK1 strain was used to treat hypercholesterolemia.

Nutritional composition, bioactive compounds, and pharmacological activities of tossa jute sprout (Corchorus olitorius L.): A potential functional food

This study investigated the food properties, phytochemical profiles, and pharmacological activities of tossa jute sprout, underscoring the exploration of its potential as a functional food. Tossa jute sprout is rich in protein, carbohydrate, fiber, total soluble solids, color content, total energy, vitamins, and minerals, with a lower fat and sugar content. Bioactive compound profiling found that it contains a significant quantity of total phenolics and flavonoids. The HPLC-DAD polyphenol profile detected ten compounds, with 3,4 dihydroxybenzoic acid being the most abundant compound, followed by (−) epicatechin, rosmarinic acid, kaempferol, catechin hydrate, caffeic acid, myricetin, catechol, trans-ferulic acid, and rutin hydrate. It has strong radical scavenging, reducing power, metal chelating power, and total antioxidant power, suggesting this sprout's ability to repair cellular oxidative damage or restore impaired cellular oxidative homeostasis. It also possesses strong α-glucosidase and pancreatic lipase inhibition activities, but mild α-amylase, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) inhibition activities support the sprout's ability to lower blood sugar, suppress postprandial hyperglycemia, downregulate fat metabolism, and maintain or restore acetylcholine. Overall findings established tossa jute sprout's high potential as a functional food in eliminating malnutrition, maintaining quality health, and eradicating or moderating ailments, including diabetes, obesity, and Alzheimer's.

Medical treatment of pediatric obesity

Background: The increasing prevalence of pediatric obesity over the past few decades has become a serious public health concern. Quarantine measures during the coronavirus disease pandemic have led to an increase in childhood obesity rates. Children with obesity are at greater risk for type 2 diabetes, hypertension, dyslipidemia, polycystic ovary syndrome, obstructive sleep apnea, and adult obesity. Lifestyle modification therapy is the firstline treatment for pediatric obesity. Pharmacotherapy is the next logical treatment option in patients in whom lifestyle modifications alone are ineffective.Current Concepts: Anti-obesity medications for pediatric obesity include metformin, orlistat, glucagon-like peptide-1 agonists, phentermine, and phentermine/topiramate combination. Metformin, a medication used for type 2 diabetes has not been approved for treatment of pediatric obesity. Orlistat, a lipase inhibitor, prevents fat absorption from the human diet. Liraglutide, a glucagon-like peptide-1 agonist, is associated with decreased gastric emptying, increased satiety, and appetite suppression. Phentermine, a norepinephrine reuptake inhibitor, is approved by the Food and Drug Administration for short-term treatment of patients aged >16 years. Phentermine/topiramate is a combination of the conventional anti-obesity medication, phentermine and an antiepileptic agent, topiramate that is commonly associated with weight loss as an adverse effect.Discussion and Conclusion: Anti-obesity treatment may serve as the next logical therapeutic option for pediatric obesity. However, sufficient lifestyle modification therapy should be attempted before considering medication, and anti-obesity medications should preferably be used in combination with lifestyle modifications. Monitoring growth and pubertal development during anti-obesity treatment is essential to ensure healthy development of children and adolescents.

Novel Functional Food Properties of Forest Onion (Eleutherine bulbosa Merr.) Phytochemicals for Treating Metabolic Syndrome: New Insights from a Combined Computational and In Vitro Approach.

Metabolic syndrome is a global health problem. The use of functional foods as dietary components has been increasing. One food of interest is forest onion extract (FOE). This study aimed to investigate the effect of FOE on lipid and glucose metabolism in silico and in vitro using the 3T3-L1 mouse cell line. This was a comprehensive study that used a multi-modal computational network pharmacology analysis and molecular docking in silico and 3T3-L1 mouse cells in vitro. The phytochemical components of FOE were analyzed using untargeted ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS). Next, an in silico analysis was performed to determine FOE's bioactive compounds, and a toxicity analysis, protein target identification, network pharmacology, and molecular docking were carried out. FOE's effect on pancreatic lipase, α-glucosidase, and α-amylase inhibition was determined. Finally, we determined its effect on lipid accumulation and MAPK8, PPARG, HMGCR, CPT-1, and GLP1 expression in the preadipocyte 3T3-L1 mouse cell line. We showed that the potential metabolites targeted glucose and lipid metabolism in silico and that FOE inhibited pancreatic lipase levels, α-glucosidase, and α-amylase in vitro. Furthermore, FOE significantly (p < 0.05) inhibits targeted protein expressions of MAPK8, PPARG, HMGCR, CPT-1, and GLP-1 in vitro in 3T3-L1 mouse cells in a dose-dependent manner. FOE contains several metabolites that reduce pancreatic lipase levels, α-glucosidase, α-amylase, and targeted proteins associated with lipid and glucose metabolism in vitro.

Biomedical and therapeutic potential of marine-derived Pseudomonas sp. strain AHG22 exopolysaccharide: A novel bioactive microbial metabolite

Abstract Microbial exopolysaccharides (EPSs) are gaining interest as alternatives to chemical antioxidants and pharmaceuticals. This study mines the promising biomedical and antimicrobial potential of a marine bacterium, a prolific EPS producer, isolated from the Red Sea. Pseudomonas sp. strain AHG22 generated an EPS weighing 6.98 g·L−1, coded EPSF8, subjected to FT-IR and HPLC chemical analysis. EPSF8 was then investigated for antioxidant assessment by 2,2-diphenyl-1-picrylhydrazyl (DPPH), H2O2, ABTS˙ + , nitric oxide, total antioxidant capacity (TAC), and ferric reducing antioxidant power (FRAP). EPSF8 had an IC50 of 46.99 μg·mL−1 in the DPPH antioxidant assay and antioxidant capacities of 219.45 μg·mg−1 ascorbic acid equivalent (AAE) in the TAC assay and 54.15 μg·mg−1 AAE in the FRAP assay. The in vitro anti-inflammatory effect of EPSF8 was tested against 5-lipoxygenase (5-LOX) and cyclooxygenase-2 (COX-2) enzymes and compared with the drugs ibuprofen and celecoxib used as controls. The IC50 values of 5-LOX, COX-2, ibuprofen, and celecoxib were found to be 14.82, 15.49, 1.5, and 0.28 μg·mL−1, respectively. Additionally, EPSF8 revealed antidiabetic activity toward α-amylase and α-glucosidase, and the IC50 values were 93.1 and 127.28 μg·mL−1, compared to those of acarbose (50.93 and 4.13 μg·mL−1, respectively). Anti-obesity activity of EPSF8 by lipase inhibition revealed IC50 = 56.12 μg·mL−1 compared to orlistat (IC50 = 20.08 μg·mL−1) as a control. EPSF8 displayed antibiofilm and bactericidal activity against Gram-positive (G +ve) and Gram-negative (G −ve) ATCC pathogenic bacterial strains. It had a minimum bactericidal concentration/minimum inhibitory concentration ratio ≤2, indicating a broad bactericidal spectrum. Furthermore, EPSF8 is evidenced to have a promising anti-butyrylcholinesterase activity for the control of Alzheimer’s disease. The findings of the present analysis suggest that the isolated Pseudomonas sp. strain AHG22 EPS can potentially be explored as a promising green therapeutic compound.

Effects of matcha supplementation on in vitro digestibility and sensory acceptance of soy milk

Obesity is a major non-communicable disease that has a strong correlation to other chronic diseases such as hypertension therefore the requirement of functional foods elevates throughout the year. Matcha is known for its anti-obesity properties due to its catechin content. Soymilk is also known for its bioactive compounds for health. This research’s aim is to understand the effect between matcha concentration towards inhibition ability of digestive enzymes. Sensory evaluation is carried out with home-use-test. Results show that matcha is a strong inhibitor of lipase and a weak inhibitor of amylase which may be due to the presence of tea polyphenols. Addition of 2.4% and 1.2% matcha shows 79.176% and 45.702% lipase inhibition respectively. In contrast, trypsin and pancreatin activity is enhanced. Whereas results show no inhibition of α-amylase activity. Sample 1.2% matcha shows protease inhibition and α- amylase inhibition value -15.670% and 3.216%. The addition of 1.2% matcha is likable amongst all which makes it the best formulation for functionality and acceptance.

LARS1 is a Prognostic Biomarker and Exhibits a Correlation with Immune Infiltrates in Hepatocellular Carcinoma.

To study the relationship between LARS1 expression and immune infiltration and prognosis in hepatocellular carcinoma (HCC). The clinical characteristics together with LARS1 expression levels were obtained from the TCGA database. Immunohistochemistry confirmed LARS1 expression levels in paraneoplastic and tumor tissues. To investigate LARS1-related downstream molecules, a network of protein-protein interactions (PPIs) and the Gene Ontology (GO)/Kyoto Encyclopedia of Genes and Genomes (KEGG) were built. Furthermore, gene set enrichment analysis (GSEA) was used to analyze the pathways associated with LARS1 expression, whereas Single-sample GSEA (ssGSEA) was applied to perform an association study between immune infiltration and LARS1 gene expression. The TISCH Database and the TISIDB database were used to compare the difference of LARS1 expression in hepatocellular carcinoma and immunomodulators. In comparison to that in normal tissues, the LARS1 expression level was elevated in tumor tissues. LARS1 expression exhibited substantial correlation with AFP, Histologic grade, pathologic stage, Residual tumor, and Vascular invasion in HCC. Higher LARS1 expression in HCC was linked to lower progression-free survival (PFS), disease-specific survival (DSS), and overall survival (OS). According to the GO/KEGG study, the important biological process (neutral lipid metabolic process), cellular component (triglyceride-rich plasma lipoprotein), molecular functions (lipase inhibitor activity), and KEGG pathway (cholesterol metabolism) could be a probable function mechanism in promoting HCC. Various pathways as per GSEA revealed that they were enriched in samples with elevated LARS1 expression. The expression level of LARS1 in malignant tumor cells after immunotherapy was significantly higher than that before immunotherapy. LARS1 was also remarkably linked to the infiltration level and the immunomodulators. LARS1 can be used as a biomarker of HCC, which is associated to immune infiltration of HCC.

Inquiry lipaseoring the mechanism of pancreatic lipase inhibition by isovitexin based on multispectral method and enzyme inhibition assay.

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.

Peptidomics-based identification of antihypertensive and antidiabetic peptides from sheep milk fermented using Limosilactobacillus fermentum KGL4 MTCC 25515 with anti-inflammatory activity: in silico, in vitro, and molecular docking studies.

This study investigated the synthesis of bioactive peptides from sheep milk through fermentation with Limosilactobacillus fermentum KGL4 MTCC 25515 strain and assessed lipase inhibition, ACE inhibition, α-glucosidase inhibition, and α-amylase inhibition activities during the fermentation process. The study observed the highest activities, reaching 74.82%, 70.02%, 72.19%, and 67.08% (lipase inhibition, ACE inhibition, α-glucosidase inhibition, and α-amylase inhibition) after 48h at 37°C, respectively. Growth optimization experiments revealed that a 2.5% inoculation rate after 48h of fermentation time resulted in the highest proteolytic activity at 9.88mg/mL. Additionally, fractions with less than 3kDa of molecular weight exhibited superior ACE-inhibition and anti-diabetic activities compared to other fractions. Fermentation of sheep milk with KGL4 led to a significant reduction in the excessive production of NO, TNF-α, IL-6, and IL-1β produced in RAW 267.4 cells upon treatment with LPS. Peptides were purified utilizing SDS-PAGE and electrophoresis on 2D gels, identifying a maximum number of proteins bands ranging 10-70kDa. Peptide sequences were cross-referenced with AHTPDB and BIOPEP databases, confirming potential antihypertensive and antidiabetic properties. Notably, the peptide (GPFPILV) exhibited the highest HPEPDOCK score against both α-amylase and ACE.

Definition of the metabolic pattern of ANGPTL3 deficient mice on a chow diet and under dysmetabolic conditions

Aim: ANGPTL3 controls lipid and lipoprotein metabolism through lipoprotein lipase and endothelial lipase inhibition and the prevention of lipoprotein-derived triglycerides hydrolyzation. Here we present the metabolic profile of ANGPTL3 deficient mice in physiology and during the development of metabolic disorders. Methods: Angptl3 KO mice (C57BL6/J background) and their littermate controls (wild-type, WT) were fed a chow and a High Fat Diet (HFD, 60%kcal from lipids) for 16 weeks. During the diet protocol, changes in lipids and lipoprotein profile, under fast, fed, and fast-refeed setting were assessed. The metabolic phenotype was assessed, with a Glucose Tolerance Test (GTT) and an Insulin Tolerance Test (ITT); the lipids absorption profile was assessed with an Oral Lipid Tolerance Test (OLTT). Results: ANGPTL3 KO mice fed ad libitum a chow diet are hypolipidemic (plasma triglycerides levels: 42,42±8,80 mg/dL in ANGPTL3 KO mice compared to 122,02±55,09 mg/dL in WT mice; plasma cholesterol levels: 44,00±9,11 mg/dL in ANGPTL3 KO mice compared to 76,51±15,87 mg/dL in WT mice). After 16h fasting, ANGPTL3 KO mice on a chow diet are hypolipidemic and display small lipoproteins less rich in cholesterol and triglycerides, as established in humans, and the same holds true for mice fed a HFD diet. On HFD, ANGPTL3 KO mice gain less body weight, suggesting an improved metabolic profile compared to WT animals. The hypolipidemia is conserved during all the timepoints of OLTT, both in mice on chow or HFD, suggesting a different lipid management; in spite, no significant differences in the circulating glycaemia has been proved with a GTT after 16h of fasting; likewise, a similar sensitivity to insulin has been outlined with an ITT after 4h of fasting. Conclusions: This metabolic profiling of ANGPTL3 KO mice on chow diet or HFD highlights that these mice are hypolipidemic and may have beneficial metabolic features compared to controls.

IN VITRO ANTIOBESITY ACTIVITY OF SOME PLANTS THROUGH A MODIFIED LIPASE INHIBITION ASSAY

The objective of the present study was to evaluate the antiobesity potential of various plant (leaves or seed) extracts through a modified in vitro lipase inhibitory activity assay. Dimethyl sulphoxide (DMSO, negative control or solvent) extracts as cold infusion of leaves and seeds of some plants were studied for lipase inhibitory potential using porcine pancreatic lipase enzyme, p- nitro phenyl acetate and orlistat (as positive control or standard inhibitor). Among the leaves, the Urtica dioica showed the best pancreatic lipase inhibition activity (52.0 %). On the other hand, among the seeds, Trachyspermum ammi showed the highest per cent lipase inhibition (91.68 %). Among six leaves’ and seven seeds’ extract, it was evident that the seeds showed better pancreatic lipase inhibition activity over the leaves in the study. The lipase inhibition was found to be in the range of 34.43 to 91.68 % for the plants in study. DMSO extract of the plants under the study showed significant pancreatic lipase inhibitory activity indicating strong antiobesity activity. Therefore, the plants can be further investigated for the identification and isolation of chief bioactive constituents for developing the lead molecules for obesity treatment.

Total Content and Composition of Phenolic Compounds from Filipendula Genus Plants and Their Potential Health-Promoting Properties.

This current article was dedicated to the determination of the composition of phenolic compounds in extracts of four species of the genus Filipendula in order to establish a connection between the composition of polyphenols and biological effects. A chemical analysis revealed that the composition of the extracts studied depended both on the plant species and its part (leaf or flower) and on the extractant used. All four species of Filipendula were rich sources of phenolic compounds and contained hydrolyzable tannins, condensed tannins, phenolic acids and their derivatives, and flavonoids. The activities included data on those that are most important for creating functional foods with Filipendula plant components: the influence on blood coagulation measured by prothrombin and activated partial thromboplastin time, and on the activity of the digestive enzymes (pancreatic amylase and lipase). It was established that plant species, their parts, and extraction methods contribute meaningfully to biological activity. The most prominent result is as follows: the plant organ determines the selective inhibition of either amylase or lipase; thus, the anticoagulant activities of F. camtschatica and F. stepposa hold promise for health-promoting food formulations associated with general metabolic disorders.

The proteomic landscape of fall armyworm oral secretion reveals its role in plant adaptation.

The fall armyworm (FAW, Spodoptera frugiperda (J.E. Smith)) is a polyphagous agricultural pest with rapidly evolving adaptations to host plants. We found the oral secretion (OS) of FAW from different plants influences plant defense response differentially, suggesting its role in adapting to host plants. However, the protein expression profile of FAW OS respond to different plants is largely unknown. Here, from the mass spectrometry assay, we identified a total of 256 proteins in the OS of FAW fed on cotton (Gossypium hirsutum L.), tobacco (Nicotiana benthamiana Domin), maize (Zea mays L.) and artificial diet. The FAW OS primarily comprise of 60 proteases, 32 esterases and 92 non-enzymatic proteins. It displays high plasticity across different diets. We found that more than half of the esterases are lipases which have been reported as insect elicitors to enhance plant defense response. The lipase accumulation in cotton-fed larvae was the highest, followed by maize-fed larvae. In the presence of lipase inhibitors, the enhanced induction on defense genes in wounded leaves by OS was attenuated. However, the putative effectors were most highly accumulated in the OS from FAW larvae fed on maize compared to those fed on other diets. We identified that one of them (VRLP4) reduces the OS-mediated induction on defense genes in wounded leaves. Together, our investigation presents the proteomic landscape of the OS of FAW influenced by different diets and reveals diet-mediated plasticity of OS is involved in FAW adaptation to host plants. © 2024 Society of Chemical Industry.