Hypolipidemic Activity Research Articles

In vitro study on antioxidant and lipid-lowering activities of tobacco polysaccharides

Tobacco polysaccharides were extracted by hot water extraction, and purified and separated using DEAE-52 cellulose chromatography columns, and three purified polysaccharide fractions, YCT-1, YCT-2, and YCT-3, were finally obtained. The physicochemical properties of the three fractions were analyzed by ultraviolet spectroscopy, high-performance liquid chromatography and high-performance gel chromatography. The in vitro antioxidant activity of tobacco polysaccharides was compared among different fractions by using DPPH radical, hydroxyl radical scavenging assay and potassium ferricyanide method. The in vitro hypoglycemic activity was compared using α-amylase and α-glucosidase activity inhibition assay. And the in vitro hypolipidemic activity were investigated by using pancreatic lipase activity inhibition assay and HepG-2 intracellular lipid accumulation assay. All the results showed that the constituent monosaccharides of the three tobacco polysaccharide fractions were similar, but the molar percentages of each monosaccharide were different. The average molecular weights of the three components were 27,727 Da, 27,587 Da, and 66,517 Da, respectively, and the scavenging activities on DPPH radicals and hydroxyl radicals were at a high level with good quantitative-effect relationships. The reducing power were much lower than that of the positive control VC, and the three polysaccharide fractions had a weak inhibitory ability on α-amylase activity, but showed excellent inhibitory ability on α-glucosidase and pancreatic lipase activity. In addition, the results of cellular experiments showed that all three fractions were able to inhibit lipid over-accumulation in HepG-2 cells by increasing the mRNA expression levels of PPAR-α, CPT-1A, and CYP7A1 genes, and the tobacco polysaccharide YCT-3 showed the best effect. The mechanism by which YCT-3 ameliorated the over-accumulation of intracellular lipids in HepG-2 cells was found to be related to its influence on the expression of miR-155-3p and miR-17-3p in the exosomes of HepG-2 cells.Graphical

Novel Synthesis of Phytosterol Ferulate Using Acidic Ionic Liquids as a Catalyst and Its Hypolipidemic Activity.

Phytosterol ferulate (PF) is quantitively low in rice, corn, wheat, oats, barley, and millet, but it is potentially effective in reducing plasma lipids. In this study, PF was synthesized for the first time using acidic ionic liquids as a catalyst. The product was purified, characterized using Fourier transform infrared, mass spectroscopy, and nuclear magnetic resonance, and ultimately confirmed as the desired PF compound. The conversion of phytosterol surpassed an impressive 99% within just 2 h, with a selectivity for PF exceeding 83%. Plasma lipid-lowering activity of PF was further investigated by using C57BL/6J mice fed a high-fat diet as a model. Supplementation of 0.5% PF into diet resulted in significant reductions in plasma total cholesterol, triacylglycerols, and nonhigh-density lipoprotein cholesterol by 13.7, 16.9, and 46.3%, respectively. This was accompanied by 55.8 and 36.3% reductions in hepatic cholesterol and total lipids, respectively, and a 22.9% increase in fecal cholesterol excretion. Interestingly, PF demonstrated a higher lipid-lowering activity than that of its substrates, a physical mixture of phytosterols and ferulic acid. In conclusion, an efficient synthesis of PF was achieved for the first time, and PF had the great potential to be developed as a lipid-lowering dietary supplement.

Structural characterization, rheological characterization, hypoglycemic and hypolipidemic activities of polysaccharides from Morchella importuna using acidic and alkaline deep eutectic solvents

During the preparation of polysaccharides (PSs), rheological characterization and bioactivities of PSs are affected by diverse extraction media through changing their structural properties. In this study, PSs were extracted comparatively from Morchella importuna (MIPs) with deep eutectic solvents (DESs) including an acidic deep eutectic solvent (MIP-AC) and an alkaline deep eutectic solvent (MIP-AL), respectively. The physico-chemical properties, rheological properties, and hypoglycemic and hypolipidemic activities of the MIPs were then studied. The results showed that DESs as an extraction medium could not only significantly increase the extraction yield of MIPs but also increase the contents of carbohydrates and sulfuric acid groups in MIPs. Moreover, DESs treatment could change the glycosidic linkage type and surface morphology of MIPs, reduce the molecular weight and viscosity of MIPs, and improve the system stability of MIPs, thus affecting the rheological properties and hypoglycemic and hypolipidemic activities of MIPs. It is worth noting that MIP-AL possessed stronger hypoglycemic and hypolipidemic activities, which was reflected by its roles in inhibiting the activities of α-glucosidase and α-amylase, increasing glucose consumption, and reducing triglyceride and cholesterol contents in Hep G2 cells. This research will provide a theoretical basis for the selection of DESs for extraction of specially appointed PSs.

Algae in Biomedicine.

Algae, which live in marine or freshwater, are photosynthetic organisms. They vary greatly in size, morphology, and degree of complexity of their body structures. Algae are generally divided into two main groups, microalgae, which are small in size, and macroalgae, which are larger in size. These aquatic organisms have rich and valuable compounds including sterols, polysaccharides, pigments, fatty acids, proteins, enzymes, minerals, and vitamins that could be used in different application fields due to their bioactive functions. In recent years, algae and their components have attracted interest in biomedicine and health applications as their bioactive components could show antioxidant, anticancer, anti-inflammatory, antiviral, antiangiogenic, antidiabetic, antiobesity, immunostimulatory, vaccine adjuvant, and hypolipidemic activities. In this chapter, these activities and bioactive components underlying these properties are reviewed.

The effect of Kalonji (Nigella sativa) seed oil on cardiometabolic risk factors in hyperlipidemia-induced albino rats: An experimental study

Background: India is facing a heavy burden of non-communicable diseases (NCDs) due to explosion in the epidemiological transition worldwide. In that mainly cardiometabolic risk factors like dyslipidemia play an important role in the prevalence of NCDs. According to the National Obesity Forum in Nottingham, UK, obesity itself can be the fundamental cause of numerous other illnesses and conditions, including cardiovascular disease, hypertension, stroke, hyperlipidemia, diabetes, cancers, osteoarthritis, respiratory disorders, sleep apnea, fertility problems, Alzheimer’s disease, depression, and other psychological disorders. Obesity has not historically been categorized as a disease; therefore, treatment options covered by health insurance plans have been limited. A combination of genetics, lifestyle behaviors, and comorbidities represents the lion’s share of determinants. Aims and Objectives: The effect of Kalonji (Nigella sativa) seed oil on lipid profile is seen on cardiometabolic risk factors partly, that is, dyslipidemia in high-fat diet-induced hyperlipidemic albino rats. Materials and Methods: After obtaining approval from the Animal Ethics Committee, the albino rats of weighing 120–200 g were selected and induced hyperlipidemia by giving high-fat diet for 4 weeks. The basal lipid profiles were estimated and also hyperlipidemic levels were estimated after 4 weeks of high-fat diet. Then, oral feeding started with the standard drug atorvastatin 10 mg and with extract of Kalonji seed oil of low dose 200 mg and 600 mg/kg body weight of high dose is given for a period of 1 month. Again lipid profile estimation was done on days 14 and 30. The data analyzed statistically analyzed by drawing mean and standard deviation. Results: It is observed that a high dose 600 mg/kg body weight of Kalonji showed significant hypolipidemic activity as compared to a low dose 200 mg/kg. It lowers total cholesterol and low-density lipoprotein levels significantly as that of the standard drug atorvastatin 10 mg/kg. Conclusion: Kalonji (N. sativa) has produced hypolipidemic activity significantly with a high dose 600 mg/kg significantly as that of atorvastatin 10 mg/kg. Kalonji also has not produced any toxic changes like hepatotoxicity at high doses. Hence, Kalonji as anti-dyslipidemic proves in decreasing the risk factors in the development of NCDs.

<i>Cassia auriculata</i> L.–A mini review of phytochemical compounds and their antidiabetic mechanisms

<abstract> <p><italic>Cassia auriculata</italic> is an important medicinal herb traditionally used for the treatment and management of diabetes. Scientific research has reported some bioactivities related to traditional roles that include antihyperglycemic and antihyperlipidemic, which could inhibit onset of diabetes. Our aim was twofold: To review the presence of phytochemical compounds in plant extracts and to perform an <italic>in-papyro</italic> evaluation of their antidiabetic potential. A detailed literature survey was carried out for evaluating metabolic syndrome-related medicinal bioactivities and antidiabetic activity from specific compounds of <italic>C. auriculata</italic>. We uncovered a wide range of medicinal uses of <italic>C. auriculata</italic> in Ayurveda and Sri Lankan medicinal traditions and cultures. Many of the compounds in <italic>C. auriculata</italic> extracts have already been reported for their specific antidiabetic, hypoglycemic, and hypolipidemic activities, which exhibited positive effects on neuro, renal, and liver support. In conclusion, our findings suggested that the phytocomposition of <italic>C. auriculata</italic> could be attributed to the presence of antidiabetic activity through various mechanisms.</p> </abstract>

Design and synthesis of guaiacol-based fibrate derivatives with potential hypolipidemic and liver protective actions

Hypolipidemic and hepatoprotective effectives of the newly synthesized guaiacol-based fibrate derivatives were evaluated in Triton WR-1339-induced hyperlipidemic mice. All the target compounds were preliminary screened, in which compound T5 showed significant hypolipidemic effects, decreasing triglycerides (TG) and total cholesterol (TC), which was better than the positive drug clofibrate. Furthermore, compound T5 has a dose-dependent effect on the blood lipid lowering activity of hyperlipidemia mice, and hepatic transaminases (AST and ALT) induced by hyperlipidemia have a significant improvement effect. Histological examination of the liver of hyperlipidemic mice supplemented with T5 revealed a significant amelioration in hepatic lipid accumulation when compared with the effect of the positive drug clofibrate. The mechanism of lipid-lowering showed that T5 could significantly increase the expression of PPAR-α protein in the liver of hyperlipidemic mice. In addition, T5 can also improve the lipid peroxidation process induced by hyperlipidemia, reducing the level of malondialdehyde (MDA). These findings reinforced the effects of T5 as a hypolipidemic candidate compound with liver protective activity.

Comparative Effects of the Aqueous Extracts of Gongronema Latifolium and Tetrapleura Tetraptera on Serum Liver and Kidney Markers as well as Glucose Tolerance Test of Albino Rat

The study investigated the effect of aqueous extract of G. latifolum and T. tetraplura on serum liver and kidney markers as well as glucose tolerance test of albino Rat. A total of twenty five male albino rats were randomly grouped into five groups. Group 1 served as control, Group 2 and 4 received 200 and 400mg/kg G. latifolium respectively. Animals in Group 3 and 5 received 200mg/kg and 400mg/kg T. tetraplura respectively for 28days. Result for AST was significantly (P<0.05) higher in group 5 (43.000±3.033) when compared to the control group (30.400±2.158). ALT concentration was also significantly (P<0.05) in group 5 (34.600±1.077) when compared to the control (22.400±1.326). Result for kidney function parameters showed a significant (p˂0.05) increase in urea concentration of the group 5 (26.962±0.6340) when compared to the control (24.242±1.875) From the obtained results, it could be concluded that T. tetraplura could induce hepatotoxicity and nephrotoxicity. Also, from obtained results, the spices possess hypolipidemic and antioxidant activity. These ability of the spices to carry out these activities can be attributed to it rich phytochemical constituents.

Guggulsterone phytosomes: A novel approach to alleviate hyperlipidemia in high-fat diet-fed rats

Introduction: Guggulsterone, derived from Commiphora mukul, is a potent hypolipidemic medication with low bioavailability and water insolubility. To address these challenges, the study aimed to formulate phytosomes and evaluate the efficacy of guggulsterone phytosomes (GPs) in reducing hyperlipidemia in rats on a high-fat diet. Methods: GPs were formulated by incorporating soya lecithin with a suitable solvent to enhance their efficacy against hyperlipidemia induced by a high-fat diet in rats. The optimized GPs were characterized, and in vitro drug release pattern was examined. The hypolipidemic effect of GPs (25 mg/kg body weight) was evaluated in Sprague Dawley rats over 28 days. Results: The GPs demonstrated favorable entrapment effectiveness with a particle size of 145.4 nm and a zeta potential of -17.8 mV. In terms of drug release, the GPs exhibited better stability and bioavailability, with a release of 92.07 ± 1.67% within 24 hours, compared to pure guggulsterone, which only released 28.07 ± 0.81%. GPs elevated the levels of high-density lipoprotein (HDL) and significantly (P<0.05) reduced triglycerides (TG), low-density lipoprotein (LDL) levels, and total cholesterol (TC), compared to their respective control groups. Moreover, GPs showed substantial (P<0.05) antioxidant activity, reduced steatosis, inflammatory cell, and fat cell infiltration in the liver tissue. Conclusion: GPs exhibited hypolipidemic activity in rats with high-fat diet-induced hyperlipidemia compared to pure guggulsterone. These findings emphasize the potential of GPs as an effective therapeutic intervention for managing hyperlipidemia, surpassing the conventional use of the pure compound.

Impact of Mucuna pruriens seed on lipid profiles in rats with streptozotocin-induced diabetes

Background: Mucuna pruriens (MP) is a tropical legume, widely used in the treatment of parkinsonism, erectile dysfunction, anti-venomous, and anti-diabetic properties. It contains multiple phytonutrients and is rich in soluble fibers and proteins and is used as a drug of choice in traditional medicine for different ailments. Aims and Objectives: The study aimed to study the hypolipidemic activity of alcoholic extract MP seeds in Type 2 diabetic rats with hyperlipidemia, by assessing lipid profile of rats in comparison with rats treated with a standard anti-diabetic drug. Materials and Methods: Fifty-four Wistar rat pups were made diabetic by injecting intraperitoneal injection of streptozotocin (65 mg/kg). After 12 weeks, animals with diabetic and dyslipidemia were selected and divided into three groups diabetic control, test drug group (fed with MP alcoholic extract 200 mg/kg), and standard drug group (fed with glibenclamide 0.1 mg/kg), and 18 rats of same age were kept for normal control group. Results: MP seeds exhibited a gradual and progressive change in the low-density lipoprotein levels in diabetic rats (4th week [−34.3%], 8th week [−42.24%], and 12th week [−45.30%]), serum triglycerides levels (4th week [−39.3%], 8th week [−44.49%], and 12th week [−46.65%]). Whereas serum high-density lipoprotein levels were significantly increased (39.3% increase by 4 weeks, 54.95% increase by 8 weeks, and 61.03% increase by 12 weeks). This suggests that active phytochemical compounds in the MP seeds exert hypolipidemic properties by its antioxidant and high fiber content. Conclusion: MP seeds contain phytonutrients and soluble fiber compounds, which helps in reduction of lipid levels in rats with diabetes induced hyperlipidemia.

Monascus-fermented quinoa alleviates hyperlipidemia in mice by regulating the amino acid metabolism pathway.

Monascus has the ability to produce secondary metabolites, such as monacolin K (MK), known for its physiological functions, including lipid-lowering effects. Widely utilized in industries such as health food and medicine, MK is a significant compound derived from Monascus. Quinoa, recognized by the Food and Agriculture Organization of the United Nations as "the only plant food that can meet human basic nutritional needs by itself", possesses dual advantages of high nutritional value and medicinal food homology. This study employed animal experiments to investigate the hypolipidemic activity of Monascus-fermented quinoa (MFQ) and explored the molecular mechanism underlying the lipid-lowering effect of MFQ on hyperlipidemic mice through transcriptomic and metabolomic analyses. The results demonstrated that high-dose MFQ intervention (1600 mg kg-1 d-1) effectively decreased weight gain in hyperlipidemic mice without significant changes in cardiac index, renal index, or spleen index. Moreover, hepatic steatosis in mice was significantly improved. Serum levels of total cholesterol, triglycerides, and low-density lipoprotein cholesterol were markedly reduced, demonstrating that the lipid-lowering effect of MFQ was comparable to the drug control lovastatin. Conversely, both low-dose MFQ (400 mg kg-1 d-1) and unfermented quinoa exhibited no significant lipid-lowering effect. Integrated analysis of the transcriptome and metabolome suggested that MFQ may regulate amino acid levels in hyperlipidemic mice by influencing metabolic pathways such as phenylalanine, tyrosine, and tryptophan metabolism. This regulation alleviates hyperlipidemia induced by a high-fat diet, resulting in a significant reduction in blood lipid levels in mice.

Coffee pulp simulated digestion enhances its in vitro ability to decrease emulsification and digestion of fats, and attenuates lipid accumulation in HepG2 cell model

The coffee industry produces a considerable quantity of coffee pulp (CP), a by-product with high levels of caffeine, phenolic compounds, and dietary fiber, which are reportedly involved in the lipid homeostasis regulation required to maintain human health. This work's objective was to evaluate the hypolipidemic activity of coffee pulp flour (CPF) and aqueous extract (CPE) after static simulated digestion by the assessment of their in vitro capacity to decrease emulsification and digestion of fats, and lipid-lowering capacity in HepG2 cells after the induction of intracellular fat accumulation. The CPF and CPE digested fractions displayed in vitro hypolipidemic properties by preserving the reduction of micellar cholesterol solubility (27–34%) and the secondary bile acid-binding capacity (22–30%), increasing their primary bile acid-binding ability (2.7-fold and 2.4-fold, respectively), and inhibiting the lipase and the HMGCR (77–79% and 36–85%, respectively) activities. Moreover, the hypolipidemic properties of non-digested fractions enhanced the CPF potential to decrease lipid absorption. Both ingredients (CPF and CPE) demonstrated lipid-lowering effects since they effectively counteract the accumulation of intracellular triglycerides and cholesterol triggered by palmitic acid in hepatic cells after the simulated digestion. This study suggests that phenolic compounds, caffeine, and dietary fiber may be responsible for the lipid-lowering properties exhibited by the CP ingredients and their composition differences affect the above-mentioned properties exhibited in the simulated digestion. These results contribute to demonstrating that the CPF and the CPE may act as modulators of pathways involved in hepatic lipid accumulation and could be a key element in its prevention.

Conducting biological tests in the development of self-emulsifying drug delivery systems with simvastatin

The aim of the study was to compare the hypolipidemic activity of the developed self-emulsifying drug delivery systems with simvastatin with reference samples of the substance and the finished drug product of industrial production. Materials and methods. The substance of simvastatin (India, s. DK40-2005021, 99.09 %, introduced into the composition of self-emulsifying compositions based on castor oil (Ukraine), polyethylene glycol 40 hydrogenated castor oil (India), Tween 80 (Ukraine), glycerol monostearate (Gustav Heess GmbH, Germany) or polyethylene glycol 100 stearate (ERCA, Italy). Reference samples were Simvastatin-Sandoz (Salutas Pharma, Germany, series LX5161) and simvastatin in pure form. The experimental animals were Syrian hamsters aged 2 months. Hyperlipidemia was modeled by means of an alimentary load. To assess the state of lipid metabolism in animals, the content of triacylglycerols, total cholesterol, low-density lipoprotein and high-density lipoprotein in the blood serum was determined by colorimetric enzymatic methods using the appropriate standard reagent kits "Triacylglycerols F" HP022.02, "Cholesterol F" HP026.02, "Cholesterol-LDL F" HP026.05 and "Cholesterol-HDL F" HP026.04 (LLC SPE "Filicit-Diagnostics", Ukraine) on a semi-automatic biochemical analyzer MapLab Plus (BSI, Italy). Results. The reference samples had similar dose-dependent efficacy parameters. At the same time, the test samples, also having similar dose-dependent effects, in absolute terms at the maximum concentration reduced the amount of low-density lipoprotein and total cholesterol more effectively than the reference samples. When using the test samples in their average concentration, the level of triglycerols was significantly reduced, which is rather a concomitant effect of simvastatin. Conclusions. The improvement of the overall efficacy of simvastatin when it is introduced into self-emulsifying drug delivery systems has been proved, which is associated with the modification of pharmacokinetic parameters by improving the solubility of the substance in the aqueous environment of the gastrointestinal tract

Hypolipidemic effect of dill seed (Anethum graveolens L.) essential oil on lipid profile and peroxisome proliferator-activated receptor- γ expression in hyperlipidemic male rats

Herbal medicines have been suggested for the treatment of hyperlipidemic disorders. The hypolipidemic activities of dill essential oil on lipid profile and peroxisome proliferator-activated receptor-γ (PPARγ) expression in adipose tissue were studied in male rats with hyperlipidemia. The effects were studied and compared of dill essential oil and atorvastatin on serum lipid profile and aspartate aminotransferase (AST), alanine aminotransferase (ALT) levels, histopathological damage of liver and PPARγ gene expression in the adipose tissue of male rats with hyperlipidemia. The treatment with dill decreased body weight, serum cholesterol, triglyceride, LDL-C, ALT and AST levels, histopathological damage to the liver and PPARγ expression of adipose tissue, and increased serum HDL-C levels in experimental hyperlipidemic rats compared to the hyperlipidemic control rats, both significantly. The plant and atorvastatin improved hyperlipidemia, attenuated liver tissue damage and down-regulated PPARγ expression. So, dill could be defined as an excellent candidate for treatment of hyperlipidemia.

Selection and evaluation of quality markers for the regulation of PXR-CYP3A4/FXR-LXRα by Exocarpium Citri Grandis for the treatment of hyperlipidaemia with dispelling blood stasis and removing phlegm

Hyperlipidaemia is described as "excessive phlegm" and "blood stasis" in the classic theory of traditional Chinese medicine. Exocarpium Citri Grandis has the effect of dispelling blood stasis and removing phlegm, which can better meet the treatment needs of this disease. However, there is still a lack of focus and depth in the study of the chemical composition of this medicine, and the correlation between the study of relevant medicinal substances and the efficacy of dispelling stasis and removing phlegm is insufficient. To address this issue, this study was carried out to validate the overall efficacy and identify and determine the chemical composition of Exocarpium Citri Grandis. The regulatory mechanism of the PXR-CYP3A4/FXR-LXRα pathway and its active ingredients were screened, and a pharmacokinetic study of active ingredients was performed. The obtained multidimensional data were statistically analysed and comprehensively evaluated. The quality marker of Exocarpium Citri Grandis in the treatment of hyperlipidaemia based on the PXR-CYP3A4/FXR-LXRα mechanism to exert the efficacy of dispelling blood stasis and removing phlegm was finally determined. Based on the above experiments, we identified 27 compounds from the ethanol extract of Exocarpium Citri Grandis. Among them, naringenin, meranzin hydrate, apigenin, caffeic acid phenethyl ester, anacardiin, hesperidin and naringin can significantly regulate all or part of the targets in the PXR-CYP3A4/FXR-LXRα pathway. It also has suitable content and pharmacokinetic characteristics in vivo. In conclusion, this study established quality markers to characterize the efficacy of Exocarpium Citri Grandis in dispelling blood stasis and removing phlegm, which provides a scientific basis for the targeted evaluation of the hypolipidaemic activity of this medicinal plant.

Enhancement of γ-Aminobutyric Acid and the Characteristics of Nutrition and Function in White Quinoa through Ultrasound Stress at the Pre-Germination Stage.

The global production of quinoa has been increasing in recent years. In plant-based foods, ultrasound stress has received increasing attention, owing to its ability to enhance the production of primary and secondary metabolites. We studied the effects of ultrasonic stress at the pre-germination stage on the γ-aminobutyric acid (GABA) accumulation and characteristics of nutrition and function in quinoa. The results showed that ultrasonic conditions of 100 W for 4 min promoted an increase in GABA content by 9.15-fold, to 162.47 ± 6.69 mg/100 g·DW, compared to that of untreated quinoa, through promoting a 10.2% and 71.9% increase in the water absorption and glutamate decarboxylase activity of quinoa, respectively. Meanwhile, compared to untreated quinoa, ultrasonic stress at the pre-germination stage enhanced the total phenolic, total flavonoid, and total saponin contents of quinoa by 10.2%, 33.6%, and 90.7%, to 3.29 mg GA/g·DW, 104.0 mg RE/100 g·DW, and 7.13 mg/g, respectively, without decreasing its basic nutritional quality. Ultrasonic stress caused fissures on the surface of quinoa starch particles. Additionally, germination under ultrasonic stress increased the n3 polyunsaturated fatty acids by 14.4%. Furthermore, ultrasonic stress at the pre-germination stage promoted the scavenging of 2,2-diphenyl1-picrylhydrazyl radicals and inhibitions of α-amylase, α-glucosidase, and pancreatic lipase by 14.4%, 14.9%, 24.6%, and 20.0% in vitro, compared to untreated quinoa. The results indicated that the quinoa sprouted via ultrasonic stress could represent a promising method through which to develop nutritionally balanced whole grains rich in GABA, with hypoglycemic and hypolipidemic activities, which could provide theoretical support for the development of functional whole-grain foods based on quinoa.

Ultrasonic extraction of Moringa oleifera seeds polysaccharides: Optimization, purification, and anti-inflammatory activities

Natural polysaccharides exhibit numerous beneficial properties, such as antioxidant, antitumor, hypoglycemic, and hypolipidemic activities. Moringa oleifera seeds are of high dietary and therapeutic value which drew a lot of attention. However, the regulation effect on anti-inflammatory activity of polysaccharides remains to be studied. Herein, novel bioactive polysaccharides (MOSP-1) were extracted from Moringa oleifera seeds, and the anti-inflammatory properties of MOSP-1 were uncovered. Ultrasound-assisted extraction (UAE) was used to prepare the polysaccharides with optimized conditions (70 °C, 43 min, and liquid-solid-ratio 15 mL/g). Then, DEAE-Sepharose Fast Flow columns were applied to isolate and purify MOSP-1. Rhamnose, arabinose, galactose, and glucose were identified as the monosaccharide constituents of MOSP-1, with a molecular weight of 5.697 kDa. Their proportion in molarity was 1:0.183:0.108:0.860 and 8 types of glycosidic linkages were discovered. Bioactive assays showed that MOSP-1 possessed scavenging activities against DPPH and ABTS radicals, confirming its potential antioxidation efficacy. In vitro experiments revealed that MOSP-1 could reduce the expression of inflammation-related cytokines, inhibit the activation of ERK, JNK, and p38 (the MAPK signaling pathway), and enhance phagocytic functions. This study indicates that polysaccharides (MOSP-1) from Moringa oleifera seeds with anti-inflammatory properties may be used for functional food and pharmaceutical product development.

Potential hypoglycemic and hypolipidemic bioactive constituents in Cyclocarya paliurus leaves explored by affinity ultrafiltration with α‐glucosidase and pancreatic lipase

AbstractCyclocarya paliurus has been widely applied for therapeutic feeding as a traditional Chinese medicine homologous food with high nutritional and medical value. Nevertheless, the specific bioactive compounds liable for hypoglycemic and hypolipidemic properties and underlying mechanisms remain unexplored. In the present study, the in vitro hypoglycemic and hypolipidemic effects of C. paliurus were assessed by α‐glucosidase and pancreatic lipase inhibition assays, and the results indicated that 70% ethanol extract exhibited remarkable α‐glucosidase and pancreatic lipase inhibitory activity with the IC50 value of 3.14 μg/mL and 0.98 μg/mL, respectively. A total of 18 and 15 potential ligand candidates were screened, and the chemical structures were characterized. Furthermore, the docking result showed that chlorogenic acid, quercetin, kaempferol 3‐O‐rhamnoside, and pterocaryoside A contributed to the underlying hypoglycemic and hypolipidemic effects of C. paliurus, further strengthened the bindings of the enzyme‐ligand complex and suppressed the enzyme's activity with the binding energies ranged from −4.00 to −6.31 kcal/mol. The interrelations between the specific bioactive constituents, α‐glucosidase or lipase, and hypoglycemic or hypolipidemic activities were also carified. The present study reveals substantial prospects of C. paliurus to be developed as a natural dietotherapy, disease‐prevention, and healthcare for diabetes and obesity in the near future.

Hypolipidemic Effect of Chloroform Extract of Lagenaria siceraria: Potential Inhibitory Activity of Phytochemicals Targeting the HMG-CoA Reductase Revealed by Molecular Docking and Simulation Studies

Conventional systems of medicine play a crucial role in maintaining healthcare. Herbal medicines are intact and less harmful to human beings than synthetic medicines. This study aimed to investigate the phytochemicals and in vivo hypolipidemic effect of chloroform extract of Lagenaria siceraria in Triton X-100 (100 mg/kg body weight) induced hyperlipidemic Wistar rats. The phytochemical characterization and estimation were performed on the base of the GC-MS approach. The Lagenaria siceraria extract (250 and 500 mg/kg bw) was administered orally to hyperlipidemic-induced rats for 7 days to examine its hypolipidemic activity. The experimental animals did not display any acute toxicity. Atorvastatin (10 mg/kg bw) was used as a standard drug. Administration of Lagenaria siceraria extract lowers the total cholesterol (TC), triglyceride (TG), and low-density lipoproteins-cholesterol (LDL-C) levels whereas elevating the high-density lipoproteins-cholesterol (HDL-C) level. Histological studies of the liver and heart also showed the hypolipidemic effect of the extract. On the 8th day, no inflammation of the liver, myocardial necrosis, fibrosis, or atypia was seen. Furthermore, binding affinity and plausible binding mode of stigmastan-3-ol with HMG-CoA reductase were predicted by molecular docking studies which showed the same interaction patterns as atorvastatin. Moreover, the docking results were refined by 100 ns MD simulations which revealed that stigmastan-3-ol extract formed a stable complex with protein and did not induce any conformational changes in protein structure.

Advances in Research on Marine-Derived Lipid-Lowering Active Substances and Their Molecular Mechanisms.

Hyperlipidemia (HLP) is a metabolic disorder caused by abnormal lipid metabolism. Recently, the prevalence of HLP caused by poor dietary habits in the population has been increasing year by year. In addition, lipid-lowering drugs currently in clinical use have shown significant improvement in blood lipid levels, but are accompanied by certain side effects. However, bioactive marine substances have been shown to possess a variety of physiological activities such as hypoglycemic, antioxidant, antithrombotic and effects on blood pressure. Therefore, the hypolipidemic efficacy of marine bioactive substances with complex and diverse structures has also attracted attention. This paper focuses on the therapeutic role of marine-derived polysaccharides, unsaturated fatty acids, and bioactive peptides in HLP, and briefly discusses the main mechanisms by which these substances exert their hypolipidemic activity in vivo.