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1.
An Acad Bras Cienc ; 94(4): e20201909, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36102390

RESUMO

Hederagenin, a natural compound distributed in many medicinal plants, has a variety of pharmacological properties including anti-bacteria, anti-inflammation, anti-oxidation, and anti- apoptosis.. The aim of this study was to evaluate the effects of hederagenin on decreasing blood lipid and anti-oxidative stress in oleic acid-induced HepG2 cells and hyperlipidemic rats, and explore underlying mechanisms. In vitro, TG was used as the index to verify the lipid-lowering effect of hederagenin in oleic acid-induced HepG2 cells. In vivo, TC, TG, LDL-C, and HDL-C were used as direct indicators to study the antilipemic effect of hederagenin in hyperlipidemic rats. MDA, SOD, and GSH-PX were measured to analyze the anti-oxidative effect of hederagenin. The signaling pathways of anti-oxidation were evaluated using Western blot. Our results showed that hederagenin (250µmol/L) increased significantly TG clearance rate. In addition, treatment with hederagenin, XZK and simvastatin reduced effectively TC, TG, LDL-C and MDA content, and increased HDL-C, SOD and GSH-PX in HFD rats. Moreover, the phosphorylation level of p38 MAPK was inhibited after administration of hederagenin, XZK and simvastatin. Our results revealed that hederagenin possessed beneficial potentials for hypolipidemic effects, especially in TG clearance. The mechanism might be associated with inhibition of lipid absorption, reduction of lipid oxidation, and down-regulation of p38MAPK phosphorylation.


Assuntos
Hipolipemiantes , Ácido Oleico , Animais , LDL-Colesterol , Células Hep G2 , Humanos , Hipolipemiantes/farmacologia , Hipolipemiantes/uso terapêutico , Ácido Oleanólico/análogos & derivados , Ratos , Sinvastatina/farmacologia , Sinvastatina/uso terapêutico , Superóxido Dismutase , Proteínas Quinases p38 Ativadas por Mitógeno
2.
J Agric Food Chem ; 70(32): 9877-9887, 2022 Aug 17.
Artigo em Inglês | MEDLINE | ID: mdl-35917452

RESUMO

This study aimed to evaluate the food processing properties of bovine bone gelatin-derived peptides (BGPs) and their effects and mechanisms on hypertension and hypertension complications in spontaneously hypertensive rats (SHRs). BGPs had good acid, high temperature, and NaCl resistance abilities in vitro. Additionally, Maillard reaction of BGPs with low-dose reducing sugar (≤15%) exhibited a free radical scavenging effect. BGPs significantly reduced the blood pressure, triglyceride levels, and the low-density lipoprotein cholesterol/high-density lipoprotein cholesterol ratio in SHRs through downregulated angiotensin converting enzyme (ACE), angiotensin II (Ang II), and Ang II type 1 receptor (AT1R) levels and the upregulated Ang II type 2 receptor (AT2R) level. In brief, BGP could alleviate hypertension and dyslipidemia in SHRs by inhibiting ACE/Ang II/AT1R and activating the Ang II/AT2R signaling pathway. Our study suggests that BGP has good food processing properties and could be a potential nutraceutical for antihypertensive and antihyperlipidemic issues.


Assuntos
Anti-Hipertensivos , Hipertensão , Angiotensina II/metabolismo , Animais , Anti-Hipertensivos/farmacologia , Pressão Sanguínea , Bovinos , Colesterol/farmacologia , Manipulação de Alimentos , Gelatina/farmacologia , Hipolipemiantes/farmacologia , Peptídeos/farmacologia , Ratos , Ratos Endogâmicos SHR , Receptor Tipo 1 de Angiotensina/metabolismo
3.
Front Biosci (Landmark Ed) ; 27(7): 206, 2022 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-35866393

RESUMO

INTRODUCTION: Boesenbergia rotunda is a famous culinary/medicinal herb native to Southeast Asia region and it is traditionally used in the treatment of several diseases. This study investigated the anti-diabetic properties of Boesenbergia rotunda polyphenol extract (BRE) in high fructose/streptozotocin-induced diabetic rats. METHOD: The in vitro antioxidant activity was evaluated using DPPH and ABST colorimetric assays, while the Folin-Ciocalteu method was used for the total phenolic content of BRE. For diabetes induction, a combination of high fructose solution and streptozotocin was administered to the rats and diabetic rats were orally administrated with BRE (100 and 400 mg/kg) for 5 weeks. The fasting blood glucose, body weight gain, food and water consumption were determined during the treatment period. RESULTS: BRE showed excellent in vitro DPPH and ABTS scavenging activity with high phenolic content. BRE significantly lowered fasting blood glucose level, HbA1c, lipid profile, hepatorenal biochemical parameters and ameliorated the IPGTT in diabetic rats. Additionally, BRE reversed body weight loss, attenuated food and water intake, serum insulin level, pancreatic ß-cell function and pancreatic cell morphology. Furthermore, fructose 1,6 biphosphatase, glucose-6-phosphatase, malondialdehyde (MDA) and proinflammatory cytokines levels were also ameliorated in the BRE-treated diabetic rats, while pancreatic antioxidant enzymes activities (GSH, SOD and CAT) were significantly increased in the treated rats. CONCLUSIONS: In conclusion, the results showed that BRE effectively displayed antidiabetic effects and has possible value for antidiabetic oral medication.


Assuntos
Diabetes Mellitus Experimental , Zingiberaceae , Animais , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Antioxidantes/uso terapêutico , Glicemia/metabolismo , Metabolismo dos Carboidratos , Frutose , Hipoglicemiantes/farmacologia , Hipolipemiantes/farmacologia , Fenóis/efeitos adversos , Polifenóis/farmacologia , Ratos , Estreptozocina/efeitos adversos , Zingiberaceae/metabolismo
4.
Chin J Physiol ; 65(3): 125-135, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35775531

RESUMO

Cajanus cajan (L.) Millsp., known as pigeon pea, is one of the major grain legume crops of the tropical world. It recognizes as an ethnomedicine to possess various functions, such as helping in healing wound and cancer therapy. We investigated whether 95% ethanol extracts from C. cajan root (EECR) protect against methylglyoxal (MGO)-induced insulin resistance (IR) and hyperlipidemia in male Wistar rats and explored its possible mechanisms. The hypoglycemic potential of EECR was evaluated using α-amylase, α-glucosidase activities, and advanced glycation end products (AGEs) formation. For in vivo study, the rats were divided into six groups and orally supplemented with MGO except for Group 1 (controls). Group 2 was supplemented with MGO only, Group 3: MGO + metformin, Group 4: MGO + Low dose-EECR (L-EECR; 10 mg/kg bw), Group 5: MGO + Middle dose-EECR (M-EECR; 50 mg/kg bw), and Group 6: MGO + High dose-EECR (H-EECR; 100 mg/kg bw). EECR possessed good inhibition of α-glucosidase, α-amylase activities, and AGEs formation (IC50 = 0.12, 0.32, and 0.50 mg/mL), respectively. MGO significantly increased serum levels of blood glucose (GLU), glycosylated hemoglobin, homeostasis model assessment of IR, AGEs, lipid biochemical values, and atherogenic index, whereas EECR decreased these levels in a dose-dependent manner. EECR can also act as an insulin sensitizer, which significantly decreased (47%, P < 0.05) the blood GLU levels after intraperitoneal injection of insulin in the insulin tolerance tests. The hypoglycemic and antihyperlipidemic mechanisms of EECR are likely through several possible pathways including the inhibition of carbohydrate-hydrolyzing enzymes (α-glucosidase and α-amylase) and the enhancement of MGO-trapping effects on inhibition of AGEs formation.


Assuntos
Cajanus , Diabetes Mellitus Experimental , Animais , Cajanus/metabolismo , Diabetes Mellitus Experimental/tratamento farmacológico , Produtos Finais de Glicação Avançada/metabolismo , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Hipolipemiantes/farmacologia , Hipolipemiantes/uso terapêutico , Insulina , Óxido de Magnésio , Masculino , Aldeído Pirúvico/metabolismo , Aldeído Pirúvico/farmacologia , Ratos , Ratos Wistar , alfa-Amilases , alfa-Glucosidases
5.
J Food Drug Anal ; 30(1): 77-87, 2022 03 15.
Artigo em Inglês | MEDLINE | ID: mdl-35647727

RESUMO

Since the combinatorial components responsible for the antihyperlipidemic activity of Citrus reticulata 'Chachi' (CRC) peels remains unclear, we herein developed a bioactive equivalence oriented feedback screening method to discover the bioactive equivalent combinatorial components (BECCs) from CRC peels. Using palmitic acid (PA)-stimulated hepatocyte model, a combination of 5 polymethoxyflavones (PMFs) including tangeretin, sinensetin, nobiletin, 5,7,8,4'-tetramethoxyflavone and 3,5,6,7,8,3',4'-heptamethoxyflavone was identified to be responsible for the antihyperlipidemic effect of CRC peels. Via evaluation of combination effect by combination index (CI), these 5 PMFs were found to take effect via a synergistic mode. Our data indicated that the antihyperlipidemic mechanism of PMF combination was associated with the inhibition of fatty acid and cholesterol synthesis, and inflammation. Also, the PMF combination exhibited robust antihyperlipidemic effects in HFD-fed rats in vivo. Our study offers evidence-based data to uncover the pharmacological effect of CRC peels.


Assuntos
Citrus , Animais , Hipolipemiantes/farmacologia , Extratos Vegetais/farmacologia , Ratos
6.
Int J Mol Sci ; 23(11)2022 May 25.
Artigo em Inglês | MEDLINE | ID: mdl-35682613

RESUMO

Bile acid metabolism, involved with the digestion and absorption of nutrients in the gut, is linked to the gut microbiota community, greatly impacting the host's metabolism. We examined the hypothesis that the modulation of bile acid metabolism by dietary fat contents, gallbladder removal (GBX; cholecystectomy), and bile acid sequestrant (BAS; cholestyramine) treatment could alter energy, glucose, and lipid metabolism through the changes in the gut microbiota. Mice were randomly assigned to the following six groups: (1) Sham GBX surgery (Sham) + low fat/high carbohydrate diet (LFD), (2) Sham + high fat diet (HFD), (3) Sham + HFD + BAS, (4) GBX + LFD, (5) GBX + HFD, and (6) GBX + HFD + BAS. BAS groups received 2% cholestyramine. After an 8-week intervention, energy, glucose, and lipid metabolism, and the gut microbiota community were measured. HFD groups exhibited higher body weight gain than LFD, and GBX increased the weight gain comped to Sham groups regardless of BAS in HFD (p < 0.05). Homeostatic model assessment for insulin resistance (HOMA-IR) was higher in HFD than LFD, and GBX increased it regardless of BAS. Serum lipid profiles were worsened in GBX + HFD compared to Sham + LFD, whereas BAS alleviated them, except for serum HDL cholesterol. Hepatic tumor-necrosis-factor-α (TNF-α) mRNA expression and lipid peroxide contents increased with GBX and BAS treatment compared to Sham and no BAS treatment (p < 0.05). Hepatic mRNA expression of sterol regulatory element-binding transcription factor 1c (SREBP1c) and peroxisome proliferator-activated receptor gamma (PPAR-γ) exhibited the same trend as that of tumor necrosis factor-α (TNF-α). The α-diversity of gut bacteria decreased in GBX + HFD and increased in GBX + HFD + BAS. Akkermentia, Dehalobacterium, SMB53, and Megamonas were high in the Sham + LFD, and Veillonella and Streptococcus were rich in the Sham + HFD, while Oscillospira and Olsenella were high in Sham + HFD + BAS (p < 0.05). GBX + LFD increased Lactobacillus and Sutterella while GBX + HFD + BAS elevated Clostridium, Alistipes, Blautia, Eubacterium, and Coprobacillus (p < 0.05). In conclusion, the modulation of bile acid metabolism influences energy, glucose, and lipid metabolisms, and it might be linked to changes in the gut microbiota by bile acid metabolism modulation.


Assuntos
Gorduras na Dieta , Microbioma Gastrointestinal , Animais , Ácidos e Sais Biliares/metabolismo , Colecistectomia , Resina de Colestiramina/metabolismo , Resina de Colestiramina/farmacologia , Dieta Hiperlipídica/efeitos adversos , Gorduras na Dieta/farmacologia , Glucose/metabolismo , Hipolipemiantes/farmacologia , Metabolismo dos Lipídeos , Fígado/metabolismo , Camundongos , Camundongos Endogâmicos C57BL , RNA Mensageiro/metabolismo , Fator de Necrose Tumoral alfa/metabolismo , Aumento de Peso
7.
Artigo em Inglês | MEDLINE | ID: mdl-35690118

RESUMO

Dysregulated inflammatory responses and blood-brain barrier (BBB) dysfunction are recognized as central factors in the development of psychiatric disorders. The present study was designed to evaluate the effect of niacin on BBB integrity in ketamine-induced model of psychosis. Meanwhile, mepenzolate bromide (MPN), a GPR109A receptor blocker, was used to investigate the role of this receptor on the observed niacin's effect. Male Wistar rats received ketamine (30 mg/kg/day, i.p) for 5 consecutive days and then niacin (40 mg/kg/day, p.o), with or without MPN (5 mg/kg/day, i.p), was given for the subsequent 15 days. Three days before the end of experiment, rats were behaviorally tested using open field, novel object recognition, social interaction, and forced swimming tests. Niacin significantly ameliorated ketamine-induced behavioral deficits, amended gamma aminobutyric acid and glutamate concentration, decreased tumor necrosis factor-α and matrix metallopeptidase 9 levels, and increased netrin-1 contents in the hippocampus of rats. Niacin also augmented the hippocampal expression of ZO-1, occludin, and claudin-5 proteins, indicating the ability of niacin to restore the BBB integrity. Moreover, the histopathologic changes in hippocampal neurons were alleviated. Since all the beneficial effects of niacin in the present investigation were partially abolished by the co-administration of MPN; GPR109A receptor was proven to partially mediate the observed antipsychotic effects of niacin. These data revealed that GPR109A-mediated signaling pathways might represent potential targets for therapeutic interventions to prevent or slow the progression of psychosis.


Assuntos
Barreira Hematoencefálica , Encefalite , Hipolipemiantes , Niacina , Transtornos Psicóticos , Animais , Barreira Hematoencefálica/efeitos dos fármacos , Modelos Animais de Doenças , Encefalite/induzido quimicamente , Encefalite/tratamento farmacológico , Hipolipemiantes/farmacologia , Hipolipemiantes/uso terapêutico , Ketamina/farmacologia , Masculino , Niacina/farmacologia , Niacina/uso terapêutico , Transtornos Psicóticos/tratamento farmacológico , Ratos , Ratos Wistar , Receptores Acoplados a Proteínas G/metabolismo , Receptores Nicotínicos/metabolismo , Proteínas de Junções Íntimas/metabolismo
8.
PLoS One ; 17(6): e0269953, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35737711

RESUMO

BACKGROUND: Individuals with hyperlipidemia are two times more likely to develop atherosclerotic cardiovascular disease (ASCVD) as opposed to those with controlled serum total cholesterol (TC) levels. Considering the documented adverse events of the current lipid-lowering medications which ultimately affect patient's compliance, substantial efforts have been made to develop new therapeutic strategies. Probiotics, on the other hand, are reported to have lipid-lowering activity with the added benefit of being generally well-tolerated making it an appealing adjuvant therapy. METHODS: A total of fifty Lactic acid bacteria (LAB) were isolated from raw milk (human and animal) and dairy products. Isolates demonstrating promising in vitro cholesterol removal capabilities were morphologically and biochemically characterized. Lastly, two bacterial candidates were selected for evaluation of their potential hypolipidemic activity using a laboratory animal model. Statistical differences between the means were analyzed by one-way analysis of variance (ANOVA) followed by Tukey's post-hoc test. A p-value < 0.05 was considered statistically significant. RESULTS: Most of the isolates demonstrated an in vitro cholesterol removal activity. The six LAB isolates showing the highest cholesterol removal activity (36.5-55.6%) were morphologically and biochemically identified as Lactobacillus, Pediococcus, and Lactococcus species. The results demonstrated two promising antihyperlipidemic candidates, a Lactococcus lactis ssp. lactis with an in vivo significant reduction of serum triglycerides (TG) levels by 34.3%, and a Pediococcus sp. that was able to significantly reduce both the serum TC and TG levels by 17.3% and 47.0%, respectively, as compared to the diet-induced hyperlipidemic animal group. CONCLUSION: This study further supports the growing evidence regarding the antihyperlipidemic activity among probiotics, presenting them as a promising therapeutic approach for the management of hyperlipidemia.


Assuntos
Hiperlipidemias , Lactobacillales , Lactococcus lactis , Probióticos , Animais , Colesterol , Hiperlipidemias/tratamento farmacológico , Hipolipemiantes/farmacologia , Hipolipemiantes/uso terapêutico , Pediococcus , Probióticos/uso terapêutico
9.
J Agric Food Chem ; 70(21): 6429-6443, 2022 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-35587527

RESUMO

Hyperlipidemia is intricately associated with the dysregulation of gut microbiota and host metabolomes. This study explored the antihyperlipidemic function of oryzanol and investigated whether the function of oryzanol affected the gut microbiome and its related metabolites. Hamsters were fed a standard diet (Control) and a high fat and cholesterol (HFCD) diet with or without oryzanol, separately. Our results showed that oryzanol significantly decreased HFCD-induced fat accumulation, serum total cholesterol, low-density lipoprotein cholesterol (LDL-c), LDL-c/HDL-c ratio, triglyceride, and liver steatohepatitis, attenuated HFCD-induced gut microbiota alterations, and altered amino acid concentrations in feces and the liver. We investigated the role of the gut microbiota in the observed beneficial effects; the protective effects of oryzanol were partly diminished by suppressing the gut bacteria of hamsters after using antibiotics. A fecal microbiota transplantation experiment was carried out by transplanting the feces from HFCD group hamsters or hamsters given oryzanol supplementation (as a donor hamster). Our results showed that administering the fecal liquid from oryzanol-treated hamsters attenuated HFCD-induced hyperlipidemia, significantly decreased the abundance of norank_f__Erysipelotrichaceae, norank_f__Eubacteriaceae, and norank_f__Oscillospiraceae and the concentration of tyrosine. These outcomes are significantly positively correlated with serum lipid concentration. This study illustrated that gut microbiota is the target of oryzanol in the antihyperlipidemic effect.


Assuntos
Microbioma Gastrointestinal , Hiperlipidemias , Doenças Metabólicas , Aminoácidos/metabolismo , Animais , Colesterol/metabolismo , LDL-Colesterol/metabolismo , Cricetinae , Dieta Hiperlipídica/efeitos adversos , Hiperlipidemias/tratamento farmacológico , Hiperlipidemias/etiologia , Hipolipemiantes/farmacologia , Metabolismo dos Lipídeos , Fígado/metabolismo , Doenças Metabólicas/metabolismo , Fenilpropionatos
10.
Biomed Pharmacother ; 151: 113153, 2022 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-35598372

RESUMO

Solanum anomalum is a plant used ethnomedically for the treatment of diabetes. The study was aimed to validate ethnomedical claims in rat model and identify the likely antidiabetic compounds. Leaf extract (70-210 mg/kg/day) and fractions (140 mg/kg/day) of S. anomalum were evaluated in hyperglycaemic rats induced using alloxan for effects on blood glucose, lipids and pancreas histology. Phytochemical characterisation of isolated compounds and their identification were performed using mass spectrometry and NMR spectroscopy. Bioinformatics tool was used to predict the possible protein targets of the identified bioactive compounds. The leaf extract/fractions on administration to diabetic rats caused significant lowering of fasting blood glucose of the diabetic rats during single dose study and on repeated administration of the extract. The hydroethanolic leaf extracts also enhanced glucose utilization capacity of the diabetic rats and caused significant lowering of glycosylated hemoglobin levels and elevation of insulin levels in the serum. Furthermore, triglycerides, LDL-cholesterol, and VLDL-cholesterol levels were lowered significantly, while HDL-cholesterol levels were also elevated in the treated diabetic rats. There was absence or few pathological signs in the treated hyperglycaemic rat pancreas compared to that present in the pancreas of control group. Diosgenin, 25(R)-diosgenin-3-O-α-L-rhamnopyranosyl-(1→4)-ß-D-glucopyranoside, uracil, thymine, 1-octacosanol, and octacosane were isolated and identified. Protein phosphatases along with secreted proteins are predicted to be the major targets of diosgenin and the diosgenin glycoside. These results suggest that the leaf extract/fractions of S. anomalum possess antidiabetic and antihyperlipidemic properties, offer protection to the pancreas and stimulate insulin secretion, which can be attributable to the activities of its phytochemical constituents.


Assuntos
Diabetes Mellitus Experimental , Diosgenina , Hiperglicemia , Solanum , Animais , Glicemia , Colesterol , Diabetes Mellitus Experimental/metabolismo , Diosgenina/uso terapêutico , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Hipolipemiantes/química , Hipolipemiantes/farmacologia , Hipolipemiantes/uso terapêutico , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Ratos
11.
Int J Mol Sci ; 23(10)2022 May 17.
Artigo em Inglês | MEDLINE | ID: mdl-35628426

RESUMO

Disorders of lipoprotein metabolism are among the major risk factors for cardiovascular disease (CVD) development. Single nucleotide polymorphisms (SNPs) have been associated with the individual variability in blood lipid profile and response to lipid-lowering treatments. Here, we genotyped 34 selected SNPs located in coding genes related to lipid metabolism, inflammation, coagulation, and a polymorphism in the MIR499 gene-a microRNA previously linked to CVD-to evaluate the association with lipid trait in subjects with moderate dyslipidemia not on lipid-lowering treatment (Treatment-naïve (TN) cohort, n = 125) and in patients treated with statins (STAT cohort, n = 302). We also explored the association between SNPs and the effect of a novel phytochemical lipid-lowering treatment in the TN cohort. We found that 6 SNPs (in the MIR499, TNFA, CETP, SOD2, and VEGFA genes) were associated with lipid traits in the TN cohort, while no association was found with the response to twelve-week phytochemical treatment. In the STAT cohort, nine SNPs (in the MIR499, CETP, CYP2C9, IL6, ABCC2, PON1, IL10, and VEGFA genes) were associated with lipid traits, three of which were in common with the TN cohort. Interestingly, in both cohorts, the presence of the rs3746444 MIR499 SNP was associated with a more favorable blood lipid profile. Our findings could add information to better understand the individual genetic variability in maintaining a low atherogenic lipid profile and the response to different lipid-lowering therapies.


Assuntos
Doenças Cardiovasculares , Dislipidemias , Hipolipemiantes , MicroRNAs , Arildialquilfosfatase/genética , Doenças Cardiovasculares/tratamento farmacológico , Doenças Cardiovasculares/genética , Doenças Cardiovasculares/metabolismo , Dislipidemias/tratamento farmacológico , Dislipidemias/genética , Dislipidemias/metabolismo , Humanos , Hipolipemiantes/farmacologia , Metabolismo dos Lipídeos/efeitos dos fármacos , MicroRNAs/genética , Compostos Fitoquímicos/farmacologia , Polimorfismo de Nucleotídeo Único
12.
Molecules ; 27(7)2022 Mar 31.
Artigo em Inglês | MEDLINE | ID: mdl-35408659

RESUMO

BACKGROUND: So far, no articles have discussed the hypolipidemic effect of wheat germ protein in in vivo experiments. OBJECTIVE: In this study, we investigated the effects of wheat germ protein (WGP, 300 mg/kg/day) and wheat germ (WG, 300 mg/kg/day) on cholesterol metabolism, antioxidant activities, and serum and hepatic lipids in rats fed a high-fat diet through gavage. METHODOLOGY: We used 4-week-old male Wistar 20 rats in our animal experiment. Biochemical indicators of fecal, serum and liver were tested by kits or chemical methods. We also conducted the cholesterol micellar solubility experiment in vitro. RESULTS: After 28 days of treatment, our results showed that WGP significantly reduced the serum levels of total cholesterol (p < 0.05) and nonhigh-density lipoprotein cholesterol (p < 0.05), improved the enzymatic activities of cholesterol 7-α hydroxylase (p < 0.01) and low-density lipoprotein receptor (p < 0.01) and increased bile acid excretion in feces (p < 0.05). CONCLUSION: WG did not significantly increase bile acid excretion in feces or decrease serum levels of total cholesterol. Moreover, WGP and WG both presented significant antioxidant activity in vivo (p < 0.05) and caused a significant reduction in cholesterol micellar solubility in vitro (p < 0.001). Therefore, WGP may effectively prevent hyperlipidemia and its complications as WGP treatment enhanced antioxidant activity, decreased the concentration of serum lipids and improved the activity of enzymes involved in cholesterol metabolism.


Assuntos
Antioxidantes , Dieta Hiperlipídica , Animais , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Ácidos e Sais Biliares/metabolismo , Colesterol/metabolismo , Dieta Hiperlipídica/efeitos adversos , Fezes , Hipolipemiantes/farmacologia , Fígado , Masculino , Ratos , Ratos Wistar , Triticum/metabolismo
13.
Environ Sci Pollut Res Int ; 29(40): 61049-61064, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-35435548

RESUMO

This study aimed to investigate the microencapsulation of novel condensed tannins isolated from Periploca angustifolia roots, using ß-cyclodextrin macrocyclic oligosaccharides, in order to enhance their antioxidant and antihyperlipidemic potentials. Scanning electron microscopy and Fourier transform infrared spectroscopy results revealed that tannin fraction was successfully included into ß-cyclodextrin cavities proved with an encapsulation efficacy of 70%. Our in vitro findings highlighted that both pure and encapsulated tannins have efficient inhibition capacities of pancreatic lipase activity. However, the inclusion complex has the greatest, in vivo, antioxidant, and antihyperlipidemic effects. In fact, results showed that complexed tannins had markedly restored serum lipid biomarkers, lipid peroxidation, protein carbonyl oxidation, and antioxidant enzyme defense. These findings were additionally confirmed by aortic and myocardial muscle sections of histological examination. Consequently, ß-cyclodextrin microencapsulation may be considered as an effective and promising technique for tannin delivery with improved antioxidant and antihyperlipidemic activities.


Assuntos
Periploca , Proantocianidinas , beta-Ciclodextrinas , Animais , Antioxidantes/metabolismo , Hipolipemiantes/farmacologia , Estresse Oxidativo , Periploca/química , Periploca/metabolismo , Proantocianidinas/farmacologia , Ratos , Espectroscopia de Infravermelho com Transformada de Fourier , Taninos/farmacologia , beta-Ciclodextrinas/química
14.
Mar Drugs ; 20(4)2022 Apr 07.
Artigo em Inglês | MEDLINE | ID: mdl-35447932

RESUMO

Six new aromatic acids (1-6) and three new leucine derivatives containing an unusual oxime moiety (7-9) were isolated and identified from the deep-sea-derived actinomycetes strain Streptomyces chumphonensis SCSIO15079, together with two known compounds (10-11). The structures of 1-9 including absolute configurations were determined by detailed NMR, MS, and experimental and calculated electronic circular dichroism spectroscopic analyses. Compounds 1-9 were evaluated for their antimicrobial and cytotoxicity activities, as well as their effects on intracellular lipid accumulation in HepG2 cells. Compounds 3 and 4, with the most potent inhibitory activity on intracellular lipid accumulation at 10 µM, were revealed with potential antihyperlipidemic effects, although the mechanism needs to be further studied.


Assuntos
Actinobacteria , Actinomyces , Dicroísmo Circular , Hipolipemiantes/farmacologia , Leucina , Lipídeos , Estrutura Molecular
15.
Biomed Res Int ; 2022: 3811036, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35445134

RESUMO

This study focused on the optimization of ultrasound-assisted compound enzyme extraction for polysaccharides (RTPs) from Radix trichosanthis by orthogonal experiment and response surface methodology, and then its extraction kinetics model and antihyperlipidemic activities were studied. The optimum extraction process was as follows: cellulase-1.0%, papain-1.0%, pectase-0.5%, pH-5, extraction temperature-50°C, and liquid-to-solid ratio-30 mL/g; prediction value of RTPs was 7.54%; the experimental yield of RTPs was 7.22%, while 50 minutes was optimized in Weibull kinetics model. Then high-dose groups of RTP extract could reduce the TC, TG, and LDL-C levels and increase the level of HDL-C in high-fat mice, with the ability to lower the MDA content and enhance SOD level.


Assuntos
Celulase , Medicamentos de Ervas Chinesas , Animais , Antioxidantes , Hipolipemiantes/farmacologia , Camundongos , Polissacarídeos/farmacologia , Temperatura
16.
Molecules ; 27(6)2022 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-35335266

RESUMO

Hyperlipidemia is a chronic metabolic disease caused by the abnormal metabolism of lipoproteins in the human body. Its main hazard is to accelerate systemic atherosclerosis, which causes cerebrovascular diseases such as coronary heart disease and thrombosis. At the same time, although the current hypolipidemic drugs have a certain therapeutic effect, they have side effects such as liver damage and digestive tract discomfort. Many kinds of polysaccharides from natural resources possess therapeutic effects on hyperlipidemia but still lack a comprehensive understanding. In this paper, the research progress of natural polysaccharides on reducing blood lipids in recent years is reviewed. The pharmacological mechanisms and targets of natural polysaccharides are mainly introduced. The relationship between structure and hypolipidemic activity is also discussed in detail. This review will help to understand the value of polysaccharides in lowering blood lipids and provide guidance for the development and clinical application of new hypolipidemic drugs.


Assuntos
Hiperlipidemias , Hipolipemiantes , Humanos , Hiperlipidemias/tratamento farmacológico , Hipolipemiantes/química , Hipolipemiantes/farmacologia , Hipolipemiantes/uso terapêutico , Recursos Naturais , Polissacarídeos/química , Polissacarídeos/farmacologia , Polissacarídeos/uso terapêutico
17.
Bioorg Chem ; 121: 105665, 2022 04.
Artigo em Inglês | MEDLINE | ID: mdl-35152138

RESUMO

Berberine is a quaternary isoquinoline alkaloid that exhibits potent hypoglycemic and hypolipidemic activity. Many medicinal chemists are currently working on structural modifications around the parent scaffold of berberine, expecting to further enhance its hypolipidemic activity and reducing its cytotoxicity. In this study, a focused berberine-like compound library containing 12,600 molecules was built via the introduction of various "drug-like" fragments at the C8 and C9 positions of berberine. Sixteen comopounds were hit by using the in-house QSAR models previously reported by our group. Considering synthesis feasibility and the cost of building-blocks, only four berberine analogs (library ID: 2028, 3847, 6033, and 12456) were selected and synthesized for investigating their lipid-lowering activities. Preliminary lipid-lowering study showed that compound 12456 with the phenylsulfonyl group at the C9 position had potent cholesterol inhibitory activity in HepG2 cells, superior to that of the parent compound berberine. Subsequently, a total of twenty-five 9-O-phenylsulfonyl-berberines (1a-1y) and twenty-four 9-O-phenylsulfonyl-tetrahydroberberine (2a-2x) were designed, synthesized, and evaluated by lipid-lowering experiments. The results displayed that most compounds exhibited more lipid-lowering activities than berberine. Among them, compound 1m inhibited cholesterol production close to 50% in both cell models when compared with the blank control; the inhibition of triglycerides exceeded 70%. Moreover, 1m also had significant pharmacological effects on the inhibition of LDLC and promotion of HDLC production, especially in the HepG2 cell model, in which the inhibitory rate against LDLC was close to 70% and the increase rate of HDLC was more than 75%. The hypolipidemic experiment of SD rats demonstrated that after 40 days of administration (1m, 15 mg/kg/d), blood cholesterol was reduced by 19.6%, triglycerides reduced by 34.52%, and LDLC reduced by 41.49%, when compared with the high-fat diet model (HFD). In addition, after 80 days of administration, the three indexes of 1m were still better than that of berberine. Oil Red O staining and H&E staining results showed that 1m exhibited potent lipid scavenging activity. All in all, 1m was discovered and identified as a potent lipid-lowering agent and a new berberine-like candidate, being evaluated by subsequent studies.


Assuntos
Berberina , Animais , Berberina/química , Berberina/farmacologia , Colesterol , Hipolipemiantes/química , Hipolipemiantes/farmacologia , Ratos , Ratos Sprague-Dawley , Triglicerídeos
18.
Food Funct ; 13(5): 2729-2742, 2022 Mar 07.
Artigo em Inglês | MEDLINE | ID: mdl-35170606

RESUMO

Grifola frondosa (GF), also known as maitake (a type of mushroom), has been widely used as a food item and it exhibits various health-beneficial hypoglycemic activities. Rats fed with a fat/high-sucrose-based diet were used to determine the hypoglycemic activity of 95% and 55% GF ethanol extracts (labeled as GF95 and GF55, respectively). The activity was determined by monitoring the fasting blood glucose level. Oral glucose tolerance tests were conducted, and the levels of alanine aminotransferase and aspartate aminotransferase were studied to study the hypoglycemic activity. The HPLC-ESI-TOF-MS technique was used to analyze the samples, and the results revealed that alkaloids were present in abundance in GF95 and GF55. It was also observed that GF55 contained some organic acids and GF95 contained extra small amounts of phenoloid. The levels of intestinal microbiota were analyzed, and the results from transcriptome analysis indicated that GF55 reduced the relative abundance of Romboutsia and affected RT-Db1, thereby improving the extent of glucose metabolism achieved. GF95 downregulated the mRNA level of Socs1 by increasing the levels of Oscillibacter, Butyricimonas, Barnesiella, Turicibacter, Methanosphaera, Asaccharobacter, Globicatella, Bifidobacterium, Allobaculum, and Romboutsia. The expression of Pik3rl was upregulated when the levels of Ruminococcus and Saccharibacteria increased. The hypoglycemic activity was induced under these conditions. The obtained data indicated that the efficiency of GF95 to control glucose levels was higher than the efficiency of GF55. This suggested that GF95 can be potentially used to protect against hyperglycemia.


Assuntos
Grifola , Hipolipemiantes/farmacologia , Animais , Glicemia/metabolismo , Dieta Hiperlipídica , Modelos Animais de Doenças , Microbioma Gastrointestinal/efeitos dos fármacos , Homeostase/efeitos dos fármacos , Hiperglicemia/prevenção & controle , Hipolipemiantes/química , Hipolipemiantes/uso terapêutico , Masculino , Ratos , Ratos Wistar
19.
Food Funct ; 13(6): 3110-3132, 2022 Mar 21.
Artigo em Inglês | MEDLINE | ID: mdl-35212344

RESUMO

Spearmint belongs to the genus Mentha in the family Labiatae (Lamiaceae), which is cultivated worldwide for its remarkable aroma and commercial value. The aromatic molecules of spearmint essential oil, including carvone, carveol, dihydrocarvone, dihydrocarveol and dihydrocarvyl acetate, have been widely used in the flavors and fragrances industry. Besides their traditional use, these aromatic molecules have attracted great interest in other application fields (e.g., medicine, agriculture, food, and beverages) especially due to their antimicrobial, antioxidant, insecticidal, antitumor, anti-inflammatory and antidiabetic activities. This review presents the sources, properties, synthesis and application of spearmint aromatic molecules. Furthermore, this review focuses on the biological properties so far described for these compounds, their therapeutic effect on some diseases, and future directions of research. This review will, therefore, contribute to the rational and economic exploration of spearmint aromatic molecules as natural and safe alternative therapeutics.


Assuntos
Monoterpenos Cicloexânicos/farmacologia , Mentha spicata/química , Óleos Voláteis/química , Animais , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/química , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Vias Biossintéticas , Fármacos do Sistema Nervoso Central/química , Fármacos do Sistema Nervoso Central/farmacologia , Monoterpenos Cicloexânicos/química , Monoterpenos Cicloexânicos/metabolismo , Monoterpenos Cicloexânicos/toxicidade , Humanos , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Hipolipemiantes/química , Hipolipemiantes/farmacologia , Inseticidas , Substâncias Protetoras/química , Substâncias Protetoras/farmacologia
20.
J Diabetes Res ; 2022: 3250016, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35224106

RESUMO

This study investigates the effects of the water-soluble and organic-soluble Trichosanthes extracts on the hyperglycemic condition in streptozotocin- (STZ-) induced diabetic rats. The blood glucose levels, body weights, water intake, and urine volumes of rats in different experimental groups were monitored throughout the experiment, and the results obtained indicate that the two extracts can effectively reduce blood sugar levels, increase body weights, and improve water intake and urine volumes in diabetic rats. Based on blood biochemical analyses, the two extracts play an important role in regulating the diabetes-induced lipid metabolism disorder, increasing the levels of insulin and C-peptide, and alleviating the symptoms of diabetes. The variation in the liver glycogen contents of the water-soluble fraction and ethanol fraction groups suggests that the mechanisms underlying the hypoglycemic effects of the two extracts are different. Indeed, the water-soluble fraction alleviates diabetes symptoms in rats mainly by antioxidative activity, unlike the ethanol fraction.


Assuntos
Diabetes Mellitus Tipo 1/tratamento farmacológico , Extratos Vegetais/metabolismo , Trichosanthes/metabolismo , Animais , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Glicemia/metabolismo , Diabetes Mellitus Tipo 1/fisiopatologia , Modelos Animais de Doenças , Hipolipemiantes/metabolismo , Hipolipemiantes/farmacologia , Hipolipemiantes/uso terapêutico , Insulina/sangue , Insulina/metabolismo , Insulina/uso terapêutico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Ratos
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