Lipase Inhibitory Activity Research Articles

Isolation, Identification and Pharmacological Effects of Mandragora autumnalis Fruit Flavonoids Fraction.

Since ancient times, Mandragora autumnalis has been used as a traditional medicinal plant for the treatment of numerous ailments. In light of this, the current study was designed to isolate and identify the chemical constituents of the flavonoids fraction from M. autumnalis ripe fruit (FFM), and evaluate its DPPH scavenging, anti-lipase, cytotoxicity, antimicrobial and antidiabetic effects. An ethyl acetate extract of M. autumnalis was subjected to a sequence of silica gel column chromatography using different eluents with various polarities. The chemical structures of the isolated compounds were identified using different spectral techniques, including 1H NMR and 13C NMR. FFM’s anti-diabetic activity was assessed using a glucose transporter-4 (GLUT4) translocation assay, as well as an inhibition against α-amylase and α-glucosidase using standard biochemical assays. The FFM anti-lipase effect against porcine pancreatic lipase was also evaluated. Moreover, FFM free radical scavenging activity using the DPPH test and antimicrobial properties against eight microbial strains using the micro-dilution method were also assessed. Four flavonoid aglycones were separated from FFM and their chemical structures were identified. The structures of the isolated compounds were established as kaempferol 1, luteolin 2, myricetin 3 and (+)-taxifolin 4, based on NMR spectroscopic analyses. The cytotoxicity test results showed high cell viability (at least 90%) for up to 1 mg/mL concentration of FFM, which is considered to be safe. A dose-dependent increase in GLUT4 translocation was significantly shown (p < 0.05) when the muscle cells were treated with FFM up to 0.5 mg/mL. Moreover, FFM revealed potent α-amylase, α-glucosidase, DPPH scavenging and porcine pancreatic lipase inhibitory activities compared with the positive controls, with IC50 values of 72.44 ± 0.89, 39.81 ± 0.74, 5.37 ± 0.41 and 39.81 ± 1.23 µg/mL, respectively. In addition, FFM inhibited the growth of all of the tested bacterial and fungal strains and showed the greatest antibacterial activity against the K. pneumoniae strain with a MIC value of 0.135 µg/mL. The four flavonoid molecules that constitute the FFM have been shown to have medicinal promise. Further in vivo testing and formulation design are needed to corroborate these findings, which are integral to the pharmaceutical and food supplement industries.

Binary ethanol-water solvents affect betalain contents and health-promoting properties of red Celosia argentea inflorescence extracts

The present work aimed to compare the betalain profiles and contents in the red inflorescence of Celosia argentea extract obtained using different ethanol-water ratios. The impact of betalain content on the health-promoting properties was also evaluated. Freeze-dried inflorescence powder was extracted three times with aqueous-ethanol (0, 20, 40, 60, and 80% (v/v) ethanol). The highest total betacyanin content was found in the 40 and 60% aqueous-ethanolic extracts. Total phenolic content and antioxidant activities of the extracts increased with increasing ethanol concentration. The antioxidant activities measured by oxygen radical absorbance capacity (ORAC) assay of the 60 and 80% aqueous-ethanolic extracts were significantly higher than that of ascorbic acid. The IC50 of α-glucosidase inhibitory activities of all extracts were comparable to that of acarbose. Phenolics were the major responsible compounds for antioxidant (r = 0.975, p &lt; 0.01 by ORAC assay), α-amylase (r = -0.725, p &lt; 0.01), and lipase (r = 0.607, p &lt; 0.05) inhibitory activities, whilst betacyanins corresponded to α-glucosidase inhibitory activities (r = 0.627, p &lt; 0.05). The 60% aqueous-ethanolic extract was superior to the others in terms of colour, phytochemical contents, and health-promoting activities. These extracts can be utilised as natural food colorant, functional ingredients, and nutraceuticals.

In vitro inhibitory potential of Amaranthus lividus L. against therapeutic target enzymes

Background and Aims: The search for new enzyme inhibitors in plants is attractive because they can be used as drugs in the treatment of various diseases. Amaranthus spp. (Amaranthaceae) includes about 70 different species, some of which are edible and some of which are used in traditional medicine to treat various ailments. Amaranthus lividus L. is a vegetable whose stems and leaves are used for human consumption in Turkey. Methods: In this study, the in vitro enzyme inhibition potential of A. lividus on α-amylase, α-glucosidase, acetylcholinesterase (AChE), elastase, lipase, neuraminidase and tyrosinase was investigated for the first time. For this purpose, water extract of A. lividus was prepared. The tests of enzyme inhibitory activity were carried out by spectrophotometric and fluorometric methods. Results: The water extract showed significant α-glucosidase and α-amylase inhibitory activities. Also, it displayed good elastase, lipase and tyrosinase inhibitory activities. However, it exhibited low inhibitory activity on AChE and neuraminidase. Conclusion: The plant and its active constituents may be used as an antidiabetic enzyme inhibitor with future phytochemical constituent analysis.

Antioxidative-, Antimicrobial-, Enzyme Inhibition-, and Cytotoxicity-Based Fractionation and Isolation of Active Components from Monotheca buxifolia (Falc.) A. DC. Stem Extracts.

The current study elaborates the pharmacological potential of the methanolic extract and its fractions of the stems of Monotheca buxifolia based on thin-layer chromatography and column chromatography analyses, exploiting biological and phytochemical assays. The results suggest that bioassay-guided isolation and fractionation led to the accumulation of biologically active components in the most active fractions that resulted in the isolation of different compounds. Structural elucidation of the purified compounds was accomplished using spectroscopic one-dimensional (1H, 13C) and two-dimensional NMR (heteronuclear multiple quantum coherence, heteronuclear multiple bond coherence, and correlation spectroscopy) and spectrometric (electron ionization mass spectrometry and high-resolution electron ionization mass spectrometry) techniques. The n-hexane, CHCl3, and EtAOc fractions led to the isolation of lupeol from different fractions. 1-Triacontanol was also isolated from the n-hexane fraction, while benzoic acid, methyl benzoate, ursolic acid, and 3-hydroxybenzoic acid were obtained from the EtOAc fraction. The compounds depicted good-to-moderate total antioxidative potential and total reducing power activity and significant free-radical scavenging activity. All the compounds showed significant urease and lipase inhibitory activity with poor-to-moderate amylase inhibition. Significant zone of inhibition was observed against different bacterial strains by the isolated compounds. This work therefore states that bioassay-guided isolation plays a vital role in the isolation of biologically active constituents that can be exploited for drug development.

Potential of phenolic compounds in Ligustrum robustum (Rxob.) Blume as antioxidant and lipase inhibitors: Multi-spectroscopic methods and molecular docking.

Ligustrum robustum (Rxob.) Blume is traditionally served as a functional tea in China. In this work, the antioxidant activities of L. robustum (Rxob.) Blume extract (LRE) were evaluated and its inhibitory effect and mechanism on pancreatic lipase were further investigated. With the high contents of phenols (139.70± 1.41mg gallic acid equivalent/g extract) and flavonoids (326.46± 7.36mg rutin equivalent/g extract), LRE showed significant antioxidant activities (p<0.05) for scavenging free radicals and hydrogen peroxide, inhibiting lipid peroxidation and providing strong reducing power. Meanwhile, LRE displayed remarkable inhibitory activity on pancreatic lipase with a low half-effective inhibitory concentration (IC50 ) of 2.469± 0.005mg/ml which was further determined as non-competitive inhibition. The spectroscopic results showed that LRE inhibited the activity of pancreatic lipase by modifying the tertiary and secondary structures of lipase. Moreover, four phenolic compounds (acteoside, lipedoside A, oleuropein and ligurobustoside C) were identified from LRE by the high performance liquid chromatography-quadrupole- time of flight-mass spectrometry. In addition, according to molecular docking analysis, the four phenols could interact with pancreatic lipase by hydrogen bonds, so as to change the spatial structure of pancreatic lipase and inhibit its catalytic activity. The present results suggest that LRE not only exhibits strong antioxidant capacity but possesses effectively inhibitory activity on pancreatic lipase, which might have the potential to be developed as functional food and nutraceuticals for the prevention of metabolic diseases. PRACTICAL APPLICATION: Ligustrum robustum (Rxob.) Blume extract has been confirmed to possess antioxidant activity and lipase inhibitory activity, which indicates that the L. robustum extract has the potential to prevent oxidative stress and regulate fat metabolism. This work suggests that L. robustum extract can be served as a novel resource to prepare nutraceuticals and functional food in food industries.

First report of fatty acids in Mimosadiplotricha bee pollen with in vitro lipase inhibitory activity.

Bee pollen (BP) is full of nutrients and phytochemicals, and so it is widely used as a health food and alternative medicine. Its composition and bioactivity mainly depend on the floral pollens. In this work, BP collected by Apis mellifera with different monoculture flowering crops (BP1-6) were used. The types of floral pollen in each BP were initially identified by morphology, and subsequently confirmed using molecular phylogenetic analysis. Data from both approaches were consistent and revealed each BP to be monofloral and derived from the flowers of Camellia sinensis L., Helianthus annuus L., Mimosa diplotricha, Nelumbo nucifera, Xyris complanata, and Ageratum conyzoides for BP1 to BP6, respectively. The crude extracts of all six BPs were prepared by sequential partition with methanol, dichloromethane (DCM), and hexane. The crude extracts were then tested for the in vitro (i) α-amylase inhibitory, (ii) acetylcholinesterase inhibitory (AChEI), and (iii) porcine pancreatic lipase inhibitory (PPLI) activities in terms of the percentage enzyme inhibition and half maximum inhibitory concentration (IC50). The DCM partitioned extract of X. complanata BP (DCMXBP) had the highest active α-amylase inhibitory activity with an IC50 value of 1,792.48 ± 50.56 µg/mL. The DCM partitioned extracts of C. sinensis L. BP (DCMCBP) and M. diplotricha BP (DCMMBP) had the highest PPLI activities with an IC50 value of 458.5 ± 13.4 and 500.8 ± 24.8 µg/mL, respectively), while no crude extract showed any marked AChEI activity. Here, the in vitro PPLI activity was focused on. Unlike C. sinensis L. BP, there has been no previous report of M. diplotricha BP having PPLI activity. Hence, DCMMBP was further fractionated by silica gel 60 column chromatography, pooling fractions with the same thin layer chromatography profile. The pooled fraction of DCMMBP2-1 was found to be the most active (IC50 of 52.6 ± 3.5 µg/mL), while nuclear magnetic resonance analysis revealed the presence of unsaturated free fatty acids. Gas chromatography with flame-ionization detection analysis revealed the major fatty acids included one saturated acid (palmitic acid) and two polyunsaturated acids (linoleic and linolenic acids). In contrast, the pooled fraction of DCMMBP2-2 was inactive but pure, and was identified as naringenin, which has previously been reported to be present in M. pigra L. Thus, it can be concluded that naringenin was compound marker for Mimosa BP. The fatty acids in BP are nutritional and pose potent PPLI activity.

Solvents effect on phenolics, iridoids, antioxidant activity, antibacterial activity, and pancreatic lipase inhibition activity of noni (Morinda citrifolia L.) fruit extract

This study focused on the relationship between content levels of phytochemicals and the biological activities of noni (Morinda Citrifolia L.) fruit extracts (NFEs) prepared with traditional solvents and deep eutectic solvents (DESs). The results indicated the total phenolic content in Bet-Gly (Betaine: Glycerol) extracts (11.89 mg GAE/g DW) and total iridoid content in 70% ethanol extracts (26.38 mg CE/g DW) were the highest. A total of 17 compounds were identified and quantified in NFEs. Traditional solvent extracts, except ethyl acetate, exhibited higher antioxidant activities than DESs. Three DES extracts showed higher activities against pancreatic lipase than traditional solvent extracts. Multivariate analysis revealed that the type of extraction solvent exerts a significant influence on the phytochemical compositions and biological activities of NFEs. This study provided valuable information on the efficient extraction of phytochemicals from noni fruits and DESs are promising green solvent for the extraction of bioactive compounds from noni fruits.

THE INHIBITORY ON LIPASE ACTIVITY AND LD50 DETERMINATION OF HERBAL FORTIFIED GREEN TEA (GAMBOENG TEA)

A randomized controlled trial was conducted on three formulas of an herbal drink containing green “gamboeng” tea fortified with bay leaf and cinnamon bark at various concentrations. One gram of mixed formula was brewed in hot water at 700 C-90 0C for 10–15 minutes, and the yield of each plant was determined. We also determined the phenolic content and lipase inhibition activity of each formula. We obtained a yield of each plant with green “gamboeng” tea (66.2 %), bay leaves (10.7 %), and cinnamon bark (44.8 %). Green “gamboeng” tea has the highest percentage of phenolic compound 30.25 ± 1.201 %. Inhibition lipase activity was calculated using an Elisa reader at  =405 nm. We have three formulas with the highest lipase inhibition activity. For the three formulas, a mixture of green “gamboeng” tea, bay leaf, and cinnamon bark was F-3.2 (80.598%), F-4.1(74.306), and F-5.2 (80.299%). We also conducted acute toxicity for the formulas above using rats as an animal model. We observed the body weight, organ weight, motoric, and mortality of rats during 14 days of observation, after using the formula with the concentration of 3.75, 7.5, and 15 g/kg body weight. We also used a control group of rats in this experiment. The results of acute toxicity showed no mortality of rats from the lowest to the highest doses. We concluded that LD50 of the three formulas was &gt; 15 g/kg body weight. Between the treated groups and the control groups for organ weight and motoric activity showed no significant difference. Our conclusion is that this herbal formula drink has an activity for lipase inhibition, and is also safe for consumption by humans that suffer from obesity.

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

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

Enzyme kinetics, molecular docking, and in silico characterization of canary seed (Phalaris canariensis L.) peptides with ACE and pancreatic lipase inhibitory activity

The bioactivity of canary seed peptides (CSP) towards metabolism-regulating enzymes was evaluated. Peptides with angiotensin-converting enzyme (ACE), dipeptidyl peptidase IV (DPP-IV), and pancreatic lipase activity remained stable (p < 0.05) to simulated gastrointestinal digestion (SGD). CSP-SGD were transported efficiently (>10%) through the Caco-2 monolayer, indicating absorption through the intestinal epithelium. Lineweaver-Burk plots demonstrated that CSP-SGD act as mixed-type inhibitors for DPP-IV and α-glucosidase. Furthermore, CSP-SGD were potent as antihypertensive and antiobesity agents. Molecular docking and in silico analyses were targeted to understand CSP-SGD interactions with ACE and pancreatic lipase. ACE-inhibitory peptides (LHPQ, QTPHQ, KPVPR, and ELHPQ) acted as non-competitive inhibitors by destabilization of the transition state and Zn(II) coordination in ACE. The uncompetitive inhibition of pancreatic lipase by peptides (VPPR, LADR, LSPR, and TVGPR) destabilized the open-lid conformation of pancreatic lipase. The results of this study showed that canary seed proteins could serve as a source of biologically active peptides.

Optimization of Extraction of Polyphenols and Flavonoids from Papaya Peel and Its Anti-tyrosinase and Anti-pancreatic Lipase

The extract process of polyphenols and flavonoids from papaya peel were optimized and their antioxidant activity, anti-tyrosinase and anti-pancreatic lipase were evaluated. On the basis of single factor experiment, orthogonal experiment was used to study the influence of ultrasonic temperature, ultrasonic time, ethanol concentration and solid-liquid ratio on the contents of polyphenols, flavonoids from papaya peel. The scavenging ability of papaya peel on DPPH free radicals and ABTS free radicals and its inhibitory activity on tyrosinase and pancreatic lipase were measured. The optimal extraction conditions were obtained: Ultrasonic temperature 40 ℃, ultrasonic time 60 min, 60% ethanol, solid-liquid ratio 1:25 g/mL. Under the optimal conditions, the contents of polyphenols and flavonoids from papaya peel reached (82.00±0.65) mg/g and (162.76±2.82) mg/g, respectively. The scavenging rates of papaya peel on DPPH free radicals and ABTS free radicals reached (94.79%±0.10%), (96.94%±0.23%), respectively. The inhibition rate of papaya peel on tyrosinase with L-Tyr and L-Dopa as the substrate reached (83.33%±6.80%), (67.12%±0.32%), respectively. The inhibition rate of papaya peel on pancreatic lipase reached (82.78%±1.28%), indicating that papaya peel had strong antioxidant capacity, tyrosinase and pancreatic lipase inhibitory activity.

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

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

Increasing RG-I content and lipase inhibitory activity of pectic polysaccharides extracted from goji berry and raspberry by high-pressure processing

The impact of high-pressure processing (HPP) extraction on the structural, rheological, and functional properties of goji berry and raspberry pectic polysaccharides were investigated under acidic and alkaline conditions. These properties were compared with those of pectic polysaccharides extracted by conventional hot-acid and cold-alkali methods. Extraction yield, molecular weight, rheological behavior, and antioxidant activity of pectic extracts depended on the source materials of extraction. The solvent pH was the driving factor for the degree of esterification, as revealed by NMR and FTIR analysis. Monosaccharide composition was the primary variable between the extracts. The hot-acid extraction led to the highest galacturonic acid (GalA) contents, 46.9% for goji berry and 65.2% for raspberry, indicating the prevalence of homogalacturonans (HG) regions. HPP-assisted acidic/alkaline extractions gave rise to higher rhamnogalacturonan-I (RG-I) regions, pointing to the prevalence of hairy regions. The antioxidant activity of raspberry extracts was significantly (P ≤ 0.05) higher than goji berry extracts. The higher amount of RG-I may determine the higher antioxidant activity of raspberry pectic polysaccharides. The correlation between structural parameters and the lipase inhibitory activity also revealed that the higher lipase inhibitory activity of pectic polysaccharides is mostly correlated with the higher content of RG-I (r = 0.9259, P = 0.00033). Thus, HPP-assisted extraction may intensify the lipase inhibitory activity of pectic polysaccharides by increasing their RG-I content.

Influence of Elicitation and Drying Methods on Anti-Metabolic Syndrome, and Antimicrobial Properties of Extracts and Hydrolysates Obtained from Elicited Lovage (Levisticum officinale Koch)

This research aims to investigate the influence of elicitation and drying methods (natural, convection, microwave, and freeze-drying), with jasmonic acid (JA) and yeast extract (YE) on the biological activity of extracts and hydrolysates from lovage (Levisticum officinale Koch) leaves. The results indicate that the highest TPC was determined for hydrolysates obtained from JA-elicited microwave-dried lovage (24.96 mg/gDW). The highest ACE and lipase inhibitory activity was noted for PBS extract obtained from JA-elicited lovage after microwave drying (EC50 = 0.16 and 0.12 mg/mL, respectively). Ethanolic extract from JA-elicited lovage after freeze-drying was characterized by the highest α-amylase inhibitory activity (EC50 = 3.92 mg/mL) and the highest α-glucosidase inhibitory activity (EC50 = 1.43 mg/mL) was noted for hydrolysates from control plants subjected to freeze-drying. The highest antimicrobial activity towards C. albicans yeasts was observed for microwave ethanolic extracts with minimal inhibition (MIC) and lethal (MLC) concentrations of 0.625 and 1.25 mg/mL, respectively.

Identification and characterization of cholesterol esterase and lipase inhibitory peptides from amaranth protein hydrolysates

Human diet is undergoing a shift towards plant-based diet as a sustainable source of protein compared to animal-derived protein. In this study, cholesterol esterase (CEase) and pancreatic lipase (PL) inhibitory activities of amaranth protein hydrolysates (APHs) were studied. Bromelain, chymotrypsin, and actinase E were used for generating APHs at 2, 4 & 6 h of hydrolysis. Higher PL inhibiting potential were observed in bromelain-derived APHs (IC50 = 0.38–0.66 mg/mL) in comparison to intact amaranth proteins (IC50 = 3.93 mg/mL). Bromelain-4 h hydrolysates (AB4) demonstrated significant inhibitory potential for both CEase (IC50 = 0.47 mg/mL) and PL (IC50 = 0.48 mg/mL) activity. Peptide identification in AB-4 hydrolysate revealed that among 17 bioactive peptides, three peptides (FPFPPTLGY, FGAPR, and FPFVPAPT) were predicted as potential PL inhibitors and only one peptide (FPFVPAPT) was predicted as CEase inhibitor based on the number of substrate binding sites on active site of the enzymes. This is the first study providing insights into amaranth protein derived bioactive peptide possessing CEase and LIP inhibitory potential.

Ephedra alata extracts exerts anti-obesity, anti-hyperglycemia, anti-antipyretic and analgesic effects

PurposeThis study paper aims to evaluate the Phytochemical Composition, anti-obesity, anti-antipyretic and analgesic effect of Ephedra alata (Ea) extracts.Design/methodology/approachObesity was induced in male Wistar rats through a high-fat/fructose diet (HF/FD). Control rats received a standard diet.FindingsResults of this study showed that the Ea methanol extract (MEEa) exhibited a prominent selective inhibitory effect against lipase activity (IC50 = 1.29 mg/ml) as compared to water and ethyl acetate extracts (with IC50 = 1.63 and 1.89, respectively). Also, MEEa exert antipyretic and analgesic activities. In high-fat-high-fructose diet rats, the administration of MEEa inhibited lipase activity in the intestine, pancreas and serum by 53%, 40% and 53%, respectively. It was found to significantly decrease body weight by 20% (p = 0.09) and delay the absorption of triglycerides (TG), total cholesterol (TC), LDL-cholesterol (LDL-C) and increase HDL-cholesterol (HDL-C). In addition, MEEa efficiently decreased a-amylase activity in the intestine, pancreas and serum by 43%, 26% and 46%, respectively, and blood glucose level by 35% (p = 0.06).Originality/valueTo the best of the authors’ knowledge, this study demonstrates for the first time that MEEa are efficient in preventing obesity and hyperglycemia, pain and fever.

Based on Multi-Activity Integrated Strategy to Screening, Characterization and Quantification of Bioactive Compounds from Red Wine.

According to French Paradox, red wine was famous for the potential effects on coronary heart disease (CHD), but the specific compounds against CHD were unclear. Therefore, screening and characterization of bioactive compounds from red wine was extremely necessary. In this paper, the multi-activity integrated strategy was developed and validated to screen, identify and quantify active compounds from red wine by using ultra high performance liquid chromatography-fraction collector (UHPLC-FC), ultra fast liquid chromatography-quadrupole-time-of-flight/mass spectrometry (UFLC-Q-TOF/MS) and bioactive analysis. UHPLC-FC was employed to separate and collect the components from red wine, which was further identified by UFLC-Q-TOF/MS to acquire their structural information. Furthermore, the active fractions were tested for antioxidant activity, inhibitory activity against thrombin and lipase activities in vitro by the activity screening kit. As the results, there were 37 fractions had antioxidant activity, 22 fractions had thrombin inhibitory activity and 28 fractions had lipase inhibitory activity. Finally, 77 active components from red wine were screened and 12 ingredients out of them were selected for quantification based on the integration of multi-activity. Collectively, the multi-activity integrated strategy was helpful for the rapid and effective discovery of bioactive components, which provided reference for exploring the health care function of food.

Physicochemical and Functional Characterization of Newly Designed Biopolymeric-Based Encapsulates with Probiotic Culture and Charantin.

The identification of novel sources of synbiotic agents with desirable functionality is an emerging concept. In the present study, novel encapsulates containing probiotic L. acidophilus LA-05® (LA) and Charantin (CT) were produced by freeze-drying technique using pure Whey Protein Isolate (WPI), pure Maltodextrin (MD), and their combination (WPI + MD) in 1:1 core ratio, respectively. The obtained microparticles, namely WPI + LA + CT, MD + LA + CT, and WPI + MD + LA + CT were tested for their physicochemical properties. Among all formulations, combined carriers (WPI + MD) exhibited the highest encapsulation yields for LA (98%) and CT (75%). Microparticles showed a mean d (4, 3) ranging from 50.393 ± 1.26 to 68.412 ± 3.22 μm. The Scanning Electron Microscopy revealed uniformly amorphous and glass-like structures, with a noticeably reduced porosity when materials were combined. In addition, Fourier Transform Infrared spectroscopy highlighted the formation of strong hydrogen bonds supporting the interactions between the carrier materials (WPI and MD) and CT. In addition, the thermal stability of the combined WPI + MD was superior to that of pure WPI and pure MD, as depicted by the Thermogravimetric and Differential Scanning Calorimetry analysis. More interestingly, co-encapsulation with CT enhanced LA viability (8.91 ± 0.3 log CFU/g) and Cells Surface Hydrophobicity (82%) in vitro, in a prebiotic-like manner. Correspondingly, CT content was heightened when co-encapsulated with LA. Besides, WPI + MD + LA + CT microparticles exhibited higher antioxidant activity (79%), α-amylase inhibitory activity (83%), and lipase inhibitory activity (68%) than single carrier ones. Furthermore, LA viable count (7.95 ± 0.1 log CFU/g) and CT content (78%) were the highest in the blended carrier materials after 30 days of storage at 4 °C. Synbiotic microparticle WPI + MD + LA + CT represents an effective and promising approach for the co-delivery of probiotic culture and bioactive compounds in the digestive tract, with enhanced functionality and storage properties.

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

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

Citrinin and α-pyrone derivatives with pancreatic lipase inhibitory activities from Penicillium sp. SCSIO 41302

One new citrinin monomer derivative (1), and two new natural products α-pyrone analogues (2a and 2b), were isolated from the sponge derived fungus Penicillium sp. SCSIO 41302. Their structures were determined by extensive spectroscopic analysis, chiral-phase HPLC analysis, modified Mosher’s method, ECD calculations, and X-ray single-crystal diffraction. Bioactivity screening showed that compounds 2b and 8 exhibited obvious inhibitory activities against pancreatic lipase and acetyl cholinesterase with IC50 values of 48.5 and 4.8 μM, respectively, which indicated that different chiral center between enantiomers (2a and 2b) might result in different biological activities (IC50 value against PL for 2a >100 μg/ml).