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1.
Int J Mol Sci ; 25(13)2024 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-39000039

RESUMO

Tauroursodeoxycholic acid (TUDCA) is approved for the treatment of liver diseases. However, the antihyperglycemic effects/mechanisms of TUDCA are still less clear. The present study aimed to evaluate the antidiabetic action of TUDCA in streptozotocin (STZ)-induced type 2 diabetes mellitus (T2DM) in rats. Fifteen adult Wistar albino male rats were randomly divided into three groups (n = five in each): control, diabetic (STZ), and STZ+TUDCA. The results showed that TUDCA treatment significantly reduced blood glucose, HbA1c%, and HOMA-IR as well as elevated the insulin levels in diabetic rats. TUDCA therapy increased the incretin GLP-1 concentrations, decreased serum ceramide synthase (CS), improved the serum lipid profile, and restored the glycogen content in the liver and skeletal muscles. Furthermore, serum inflammatory parameters (such as TNF-α, IL-6, IL-1ß, and PGE-2) were substantially reduced with TUDCA treatment. In the pancreas, STZ+TUDCA-treated rats underwent an obvious enhancement of enzymatic (CAT and SOD) and non-enzymatic (GSH) antioxidant defense systems and a marked decrease in markers of the lipid peroxidation rate (MDA) and nitrosative stress (NO) compared to STZ-alone. At the molecular level, TUDCA decreased the pancreatic mRNA levels of iNOS and apoptotic-related factors (p53 and caspase-3). In conclusion, TUDCA may be useful for diabetes management and could be able to counteract diabetic disorders via anti-hyperlipidemic, antioxidant, anti-inflammatory, and anti-apoptotic actions.


Assuntos
Apoptose , Diabetes Mellitus Experimental , Inflamação , Estresse Oxidativo , Ratos Wistar , Ácido Tauroquenodesoxicólico , Animais , Ácido Tauroquenodesoxicólico/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/metabolismo , Apoptose/efeitos dos fármacos , Ratos , Masculino , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Estreptozocina , Glicemia/metabolismo , Glicemia/efeitos dos fármacos , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Fígado/metabolismo , Fígado/efeitos dos fármacos , Fígado/patologia
2.
J Pharm Biomed Anal ; 249: 116337, 2024 Jul 04.
Artigo em Inglês | MEDLINE | ID: mdl-38986347

RESUMO

This study aimed to identify and quantify the primary components in lotus leaf and to explore the hypolipidemic components through spectral-effect relationships and chemometric methods. Utilizing a data-dependent acquisition-diagnostic fragment ion/characteristic neutral loss screening strategy (DFI-NLS), a reliable HPLC-Q-TOF-MS analysis was conducted, identifying 77 compounds, including 36 flavonoids, 21 alkaloids, 3 terpenoids, 11 organic acids, 4 phenols, 1 lignin and 1 unsaturated hydrocarbon. A straightforward HPLC-DAD method was developed for the simultaneous determination of seven major components in lotus leaf, and quercetin-3-O-glucuronide (Q3GA) was identified as the most abundant component. The HPLC fingerprints of 36 lotus leaf sample batches were assessed using chemometric approaches such as principal component analysis and hierarchical cluster analysis. The hypolipidemic effect of these samples was analyzed by measuring total cholesterol (TC) and total triglycerides (TG) levels in palmitic acid (PA) and oleic acid (OA)-induced lipid modeling in HepG-2 cells, employing partial least squares regression and grey relation analysis to investigate the spectral-effect relationship of the lotus leaf. The in vivo hypolipidemic effect of these compounds was assessed using an egg yolk powder-induced high-fat zebrafish model. The findings indicated that peak No.11 (Q3GA) in the chemical fingerprint was significantly associated with hypolipidemic activity, suggesting it as a potential hypolipidemic compound in lotus leaf. In summary, this study facilitates the exploration of the phytochemical compounds and their bioactive properties in the lotus leaf.

3.
Nutrients ; 16(11)2024 May 27.
Artigo em Inglês | MEDLINE | ID: mdl-38892571

RESUMO

Pistacia lentiscus L. (P. lentiscus) is an evergreen shrub (Anacardiaceae family) primarily found in the Mediterranean region. The plant has been thoroughly characterized, resulting in a high concentration of bioactive compounds as flavonoids and phenolics. Moreover, P. lentiscus was revealed to possess a great nutritional and industrial importance because of its variety of biological activities, including antibacterial, anti-inflammatory, anti-atherogenic and antioxidant properties. Many of its beneficial health properties and applications date back to antiquity, and the European Medicines Agency officially acknowledged it as an herbal medicinal product. Indeed, it is widely employed in conventional medicine to treat several diseases, including type 2 diabetes (T2D). On this basis, this review aims to summarize and describe the chemical composition of different parts of the plant and highlight the potential of P. lentiscus, focusing on its antidiabetic activities. The plant kingdom is drawing increasing attention because of its complexity of natural molecules in the research of novel bioactive compounds for drug development. In this context, P. lentiscus demonstrated several in vitro and in vivo antidiabetic effects, acting upon many therapeutic T2D targets. Therefore, the information available in this review highlighted the multitarget effects of P. lentiscus and its great potential in T2D treatment.


Assuntos
Diabetes Mellitus Tipo 2 , Hipoglicemiantes , Pistacia , Extratos Vegetais , Pistacia/química , Hipoglicemiantes/farmacologia , Humanos , Diabetes Mellitus Tipo 2/tratamento farmacológico , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/análise , Fitoterapia , Animais
4.
Medicina (Kaunas) ; 60(6)2024 May 31.
Artigo em Inglês | MEDLINE | ID: mdl-38929535

RESUMO

Introduction: The ongoing concern of the medical profession regarding chronic medication is related to increasing patient adherence and compliance to treatment and reducing medication side effects. In this respect, drugs represented by fixed-dose combinations of active substances within the same tablet have emerged. Such a principle can be extrapolated by following the potential beneficial effects that a chronic medication can have on chronic pathologies affecting different systems. Materials and Methods: The study included 48 female Albino Wistar rats, aged 16-18 months, which were divided into two groups: ovariectomized and non-ovariectomized rats. One batch of 12 non-ovariectomized rats received no treatment, becoming a control batch (NOVX-M). The ovariectomized (OVX) group was divided into 3 batches of 12 rats each: no treatment, control (OVX-M), fenofibrate-treated (OVX-F) and statin-treated (OVX-S) rats. At 12 weeks after ovariectomy, a femoral fracture occurred in the right hind limb of all animals included in the experiment To reveal the changes, at intervals of 2, 4, 6 and 8 weeks post-fracture, the proximal part of the femur was evaluated by NMR diffusiometry, which allows random motion of proton molecules expressed by self-diffusion coefficients, D, thus allowing analysis of the size and complexity of microscopic order cavities within biological structures, such as pores inside bones. Results: The effects of hypolipidemic medication in the absence of estrogen were evidenced, proving the beneficial effect that fenofibrate can have in preserving healthy tissue exposed to osteoporotic risk during the menopausal period. The effects of lipid-lowering medication are also influenced by the duration of administration. Conclusions: Osteoporosis and heart disease are two chronic pathologies that affect mainly female population in the second half of life, and proving the dual therapeutic potential of lipid-lowering medication may also have positive effects by increasing adherence and compliance to treatment.


Assuntos
Hipolipemiantes , Ovariectomia , Ratos Wistar , Animais , Feminino , Ratos , Hipolipemiantes/farmacologia , Hipolipemiantes/uso terapêutico , Hipolipemiantes/administração & dosagem , Espectroscopia de Ressonância Magnética/métodos , Fenofibrato/farmacologia , Fenofibrato/uso terapêutico , Modelos Animais de Doenças , Fêmur/efeitos dos fármacos , Osso e Ossos/efeitos dos fármacos
5.
J Clin Lipidol ; 2024 Apr 05.
Artigo em Inglês | MEDLINE | ID: mdl-38908967

RESUMO

BACKGROUND: Cardiovascular (CV) risk scores identify individuals at higher long-term risk of CV events that may benefit from more aggressive preventive interventions. OBJECTIVE: To assess the association of CV-risk categories and criteria with long-term CV events. METHODS: Observational cohort study between 2000-2019 on patients aged 40-80 years, followed by 14 primary care centers assisted by 1 hospital in Portugal. Follow-up began when electronic health records data allowed for CV-risk classification and dynamic reassessment per 2019 ESC/EAS Guidelines. Inclusion criteria required at least one appointment with a primary care physician within three years before follow-up initiation. We assessed the 10-year adjusted hazard-ratio of combined CV death and non-fatal Atherosclerotic Cardiovascular Disease (ASCVD) hospitalization, across SCORE risk categories and criteria, using Cox proportional hazards models adjusted for sex, age, competing comorbidities, and medication. RESULTS: The study included 161 681 observations from 87 035 unique patients. During the observation period, 71 787 patients were classified as low/moderate, 51 476 as high and 38 418 as very-high CV-risk categories. In the very-high group, prevalent comorbidities were hypertension (69%), hypercholesterolemia (69%) and type 2 diabetes (61%), and 13% were hospitalized for ASCVD. The adjusted 10-year hazard ratio of the composite of CV death or ASCVD hospitalization was 2.10 (95% CI: 1.91-2.32) for high-risk and 3.56 (95% CI: 3.21-3.96) for very-high-risk patients (low-risk as reference). CONCLUSION: Our study reinforces the prognostic relevance of CV-risk stratification for long-term prediction of CV death and ASCVD hospitalization in an unselected cohort, independently of sex, age, competing comorbidities and medication.

6.
Antioxidants (Basel) ; 13(6)2024 May 28.
Artigo em Inglês | MEDLINE | ID: mdl-38929101

RESUMO

Camellia polyodonta flowers are rich sources of phenolics and less attention has been paid to their potential biological activity. This study aims to explore the crude extracts and resulting purified fractions (CPFP-I, II, III, and IV) through compositional analysis and antioxidant and hypolipidemic activities in vitro and in vivo. Among four fractions, CPFP-II contained the highest total phenolic content and flavonoid content, while CPFP-III exhibited the greatest total proanthocyanidin content. Among the 14 phenolic compounds, CPFP-II displayed the highest content of procyanidin B2, B4, and C1, whereas CPFP-III contained the highest amount of 1,2,3,6-tetragalloylglucose. The DPPH, ABTS, and FRAP assessments demonstrated a consistent trend: CPFP-II > CPFP-III > CPFP-I > CPFP-IV. In vivo experiments showed that that all four fractions significantly reduced lipid levels in hyperlipidemic C. elegans (p < 0.05), with CPFP-II exhibiting the most potent effect. Furthermore, CPFP-II effectively bound to bile acids and inhibited the enzymatic activity of pancreatic lipase in vitro. Consequently, CPFP-II should be prioritized as a promising fraction for further exploration and should provide substantial support for the feasibility of the C. polyodonta flower as a natural alternative.

7.
Antioxidants (Basel) ; 13(6)2024 Jun 05.
Artigo em Inglês | MEDLINE | ID: mdl-38929133

RESUMO

In the light of growing concerns faced by Western societies due to aging, natality decline, and epidemic of cardio-metabolic diseases, both preventable and treatable, new and effective strategical interventions are urgently needed in order to decrease their socio-economical encumbrance. The recent focus of research has been redirected towards investigating the potential of haskap (Lonicera caerulea L.) as a novel functional food or superfruit. Therefore, our present review aims to highlight the latest scientific proofs regarding the potential of Lonicera caerulea L. (LC), a perennial fruit-bearing plant rich in polyphenols, in reversing cardio-metabolic dysfunctions. In this regard, a systematic search on two databases (PubMed and Google Scholar) from 1 January 2016 to 1 December 2023 was performed, the keyword combination being Lonicera caerulea L. AND the searched pharmacological action, with the inclusion criteria consisting of in extenso original articles, written in English. The health-enhancing characteristics of haskap berries have been examined through in vitro and in vivo studies from the 35 included original papers. Positive effects regarding cardiovascular diseases and metabolic syndrome have been assigned to the antioxidant activity, hypolipidemic and hypoglycemic effects, as well as to the hepatoprotective and vasoprotective potential. Latest advances regarding LCF mechanisms of action are detailed within this review as well. All these cutting-edge data suggest that this vegetal product would be a good candidate for further clinical studies.

8.
J Med Food ; 27(7): 589-600, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38770678

RESUMO

Momordica charantia (MC), a member of the Cucurbitaceae family, is well known for its pharmacological activities that exhibit hypoglycemic and hypolipidemic properties. These properties are largely because of its abundant bioactive compounds and phytochemicals. Over the years, numerous studies have confirmed the regulatory effects of MC extract on glycolipid metabolism. However, there is a lack of comprehensive reviews on newly discovered MC-related components, such as insulin receptor-binding protein-19, adMc1, and MC protein-30 and triterpenoids 3ß,7ß,25-trihydroxycucurbita-5,23(E)-dien-19-al, and the role of MC in gut microbiota and bitter taste receptors. This review offers an up-to-date overview of the recently reported chemical compositions of MC, including polysaccharides, saponins, polyphenolics, peptides, and their beneficial effects. It also provides the latest updates on the role of MC in the regulation of gut microbiota and bitter taste receptor signaling pathways. As a result, this review will serve as a theoretical basis for potential applications in the creation or modification of MC-based nutrient supplements.


Assuntos
Microbioma Gastrointestinal , Hipoglicemiantes , Hipolipemiantes , Momordica charantia , Extratos Vegetais , Momordica charantia/química , Humanos , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Microbioma Gastrointestinal/efeitos dos fármacos , Hipolipemiantes/farmacologia , Hipolipemiantes/química , Animais , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/química
9.
Food Sci Nutr ; 12(4): 2833-2845, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38628208

RESUMO

Hyperlipidemia is a multifaceted metabolic disease, which is the major risk factor for atherosclerosis and cardiovascular diseases. Traditional Chinese medicine provides valuable therapeutic strategies in the treatment of hyperlipidemia. Inonotus obliquus has been used in traditional medicine to treat numerous diseases for a long time. To screen and isolate the fractions of I. obliquus polysaccharides (IOP) that can reduce blood lipid in the hyperlipemia animals and cell models, and investigate its mechanisms. The active component IOP-A2 was isolated, purified, and identified. In vivo, rats were randomly divided into blank control group (NG), the high-fat treatment group (MG), lovastatin group (PG), and IOP-A group. Compared with MG, the hyperlipidemic rats treated with IOP-A2 had decreased body weight and organ indexes, with the level of serum total cholesterol (TC), triglyceride (TG), and low-density lipoprotein cholesterol (LDL-C) significantly decreased (p < .05), and level of serum high-density lipoprotein cholesterol (HDL-C) significantly increased (p < .05). Hepatocyte steatosis in hepatic lobules was significantly reduced. In vitro, the accumulation of lipid droplets in the model of fatty degeneration of HepG2 cells was significantly alleviated, and cellular TC and TG content was significantly decreased (p < .01). Moreover, the expression of recombinant cytochrome P450 7A1 (CYP7A1) and Liver X Receptor α (LXRα) were up-regulated (p < .05) both in vivo and in vitro. The results showed that IOP-A2 may exert its hypolipidemic activity by promoting cholesterol metabolism and regulating the expression of the cholesterol metabolism-related proteins CYP7A1, LXRα, SR-B1, and ABCA1.

10.
Phytomedicine ; 128: 155528, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38555774

RESUMO

BACKGROUND: Obesity and hyperlipidemia can induce a variety of diseases, and have become major health problems worldwide. How to effectively prevent and control obesity has become one of the hot-spots of contemporary research. Mulberry leaf is the dried leaf of Morus alba L., which is approved by the Ministry of Health as a "homology of medicine and food", rich in diverse active constituents and with a variety of health effects including anti-obesity and anti-hyperlipidemia activities. PURPOSE: The review attempts to summarize and provide the molecular basis, mechanism, safety and products for further exploration and application of mulberry leaf on the treatment on the control of weight gain and obesity. METHODS: This review is conducted by using ScienceDirect, PubMed, CNKI and Web of Science databases following Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA). RESULTS: Based on the research progress of domestic and foreign scholars, the effective phytochemicals, molecular mechanisms and product applications of mulberry leaf in the prevention and treatment of obesity and related metabolic diseases were summarized. CONCLUSION: Mulberry leaf has excellent medicinal and health care value in obesity treatment. However, its pharmacodynamic substance basis and molecular mechanisms need to be further studied.


Assuntos
Fármacos Antiobesidade , Morus , Obesidade , Compostos Fitoquímicos , Folhas de Planta , Morus/química , Folhas de Planta/química , Obesidade/tratamento farmacológico , Humanos , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/química , Fármacos Antiobesidade/farmacologia , Fármacos Antiobesidade/química , Animais , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Fitoterapia
11.
Nat Prod Res ; : 1-7, 2024 Mar 27.
Artigo em Inglês | MEDLINE | ID: mdl-38534130

RESUMO

Five trichothecenes including a new one, together with two previously undescribed benzene derivatives were isolated from the solid culture of Trichothecium sp. Their structures were established by 1D and 2D NMR data in conjunction with HR-ESI-MS analysis. Compounds 1-5 exhibited cytotoxicity against MCF-7 cell lines at various levels ranging from IC50 of 7.23 to 16.95 µM. Compound 6 decreased the concentration of blood lipids in zebra fish at the concentration of 20 µM.

12.
Heliyon ; 10(4): e25880, 2024 Feb 29.
Artigo em Inglês | MEDLINE | ID: mdl-38384579

RESUMO

The current study assessed the hypolipidemic effect and modulation of hepatic enzymes by different edible oils in obese Wistar rats. In order to conduct this study, 36 Wistar rats that were collected at 5 weeks of age and weighed an average of 70 g were split into two groups: 28 of them were fed a high-fat diet (HFD) and 8 of them were fed a control diet. After 5 weeks of feeding, rats from the HFD (obese, n = 4) and the control diet group (n = 4) were sacrificed. Subsequently, the rest of obese rats (n = 24) were separated into six groups, including the continuing high-fat (CHF) diet group, rice bran oil (RBO) diet group, olive oil (OO) diet group, soybean oil (SO) diet group, cod liver oil (CLO) diet group, and sunflower oil (SFO) diet group, and the continuing control diet group (n = 4). Rats from each group were sacrificed following an additional 5 weeks, and all analytical tests were carried out. The results found that the interventions of RBO, CLO, and SFO in obese rats reduced their body weight non-significantly when compared with CHF. It was also observed that a non-significant reduction in weight of the heart, AAT, and EAT occurred by RBO, OO, SO, and CLO, while SFO reduced the AAT level significantly (p < 0.05). Besides, RBO, OO, SO, CLO, and SFO decreased IBAT and liver fat significantly compared to CHF. Similarly, the administration of RBO, OO, SO, and CLO reduced ALT significantly. RBO reduced GGT (p < 0.05) significantly, but other oils did not. The given oil has the efficiency to reduce TC, TAG, and LDL-C but increase HDL-C significantly. These findings suggest that different edible oils can ameliorate obesity, regulate lipid profiles, and modulate hepatic enzymes.

13.
Molecules ; 29(4)2024 Feb 08.
Artigo em Inglês | MEDLINE | ID: mdl-38398534

RESUMO

Vaccinium dunalianum leaf buds make one of the most commonly used herbal teas of the Yi people in China, which is used to treat articular rheumatism, relax tendons, and stimulates blood circulation in the body. In addition, 6'-O-caffeoylarbutin (CA) is a standardized extract of V. dunalianum, which has been found in dried leaf buds, reaching levels of up to 31.76%. Because of the uncommon phenomenon, it is suggested that CA may have a potential therapeutic role in hyperlipidemia and thrombosis. This study was designed to study the efficacy of CA on treating hyperlipidemia and thrombosis and the possible mechanisms behind these effects. Hyperlipidemia and thrombosis zebrafish models were treated with CA to observe variations of the integrated optical density within the vessels and the intensity of erythrocyte staining within the hearts. The possible mechanisms were explored using network pharmacology and molecular docking. The results demonstrate that CA exhibits an excellent hypolipidemic effect on zebrafish at concentrations ranging from 3.0 to 30.0 µg/mL and shows thrombosis inhibitory activity in zebrafish at a concentration of 30.0 µg/mL, with an inhibition rate of 44%. Moreover, network pharmacological research shows that MMP9, RELA, MMP2, PRKCA, HSP90AA1, and APP are major targets of CA for therapy of hyperlipidemia and thrombosis, and may relate to pathways in cancer, chemical carcinogenesis-receptor activation, estrogen signaling pathway, and the AGE-RAGE signaling pathway in diabetic complications.


Assuntos
Arbutina , Ácidos Cafeicos , Medicamentos de Ervas Chinesas , Hiperlipidemias , Trombose , Animais , Arbutina/análogos & derivados , Fibrinolíticos/farmacologia , Hiperlipidemias/tratamento farmacológico , Simulação de Acoplamento Molecular , Farmacologia em Rede , Trombose/tratamento farmacológico , Peixe-Zebra
14.
AAPS PharmSciTech ; 25(2): 34, 2024 Feb 08.
Artigo em Inglês | MEDLINE | ID: mdl-38332233

RESUMO

Pravastatin sodium (PVS) is a hypolipidemic drug with poor oral bioavailability due to the first-pass effect. Therefore, this study aims to formulate and evaluate transdermal patches containing PVS-loaded nanoemulsions (PVS-NEs) to increase PVS's hypolipidemic and hepatoprotective activities. PVS-NEs were prepared using the aqueous titration method, where oleic acid was chosen as an oil phase, and span 80 and tween 80 were used as surfactant and cosurfactant respectively. Droplet size (DS), polydispersity index (PDI), zeta potential (ZP), clarity, and thermodynamic stability of NEs were all characterized. Also, PVS-NEs (NE2) with 50% oil phase, 40% SC mix 2:1, and 10% water were selected as an optimum formula based on the results of DS (251 ± 16), PDI (0.4 ± 0.16), and ZP (-70 ± 10.4) to be incorporated into a transdermal patch, and PVS-NE2 loaded transdermal patches (PVS-NE2-TDPs) were prepared by solvent evaporation method. F1 patch with HPMC E15 and PVP K30 in a ratio of 3:1 represented satisfactory patch properties with good drug-excipients compatibility. Thus, it was selected as an optimum patch formula. The optimized F1 patch was characterized for thickness, moisture content, weight variation, and drug-excipients incompatibility. Therefore, it was subjected to ex vivo skin permeation and finally pharmacodynamic studies. Ex vivo permeation studies of F1 revealed that the cumulative amount of PVS permeated across rat skin was 271.66 ± 19 µg/cm2 in 72 h, and the pharmacodynamic studies demonstrated that the F1 patch was more effective in treating hyperlipidemia than PVS-TDP (control patch) based on both blood analysis and histopathological examination. .


Assuntos
Hiperlipidemias , Pravastatina , Ratos , Animais , Administração Cutânea , Excipientes , Adesivo Transdérmico , Hiperlipidemias/tratamento farmacológico , Ratos Wistar
15.
Plant Foods Hum Nutr ; 79(1): 209-218, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38340238

RESUMO

The active ingredient group is a prominent feature reflecting the inherent characteristics of plant-based functional foods. Chinese hawthorn leaf (CHL), a tea substitute possessing intrinsic nutritional properties in anti-hyperlipidemia, was first found to be adulterated with Malus doumeri leaf (MDL) owing to similar commercial labels. In this context, the above-mentioned two contrasting species were explored through phytochemical profiling and activity assessment. The amelioration effect of CHL on free fatty acids-elicited lipid deposition in HepG2 cells was significantly better than that of MDL. Molecular networking-based metabolic profiles identified 68 and 67 components in CHL and MDL, with 33 shared components. Extreme gradient boosting (XGBoost) algorithm with outstanding performance was selected to screen candidate components contributing to hypolipidemic activity, and the output was later interpreted by Shapley additive explanations (SHAP) method. Twelve and eight components were separately screened as hyperlipidemic inhibitors in CHL and MDL, while only four constituents were shared. The bioactivity evaluation of selected ingredients and combinations further confirmed their anti-hyperlipidemia capacity. These findings emphasized the feasibility of filtering bioactivity-related compounds using interpretable machine learning approaches and illustrated that related species may contain different hypolipidemic contributors, even if shared constituents existed.


Assuntos
Crataegus , Malus , Alimento Funcional , Folhas de Planta , China
16.
Cureus ; 16(1): e51433, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38298275

RESUMO

Background and objective The hypolipidemic statins have been associated with various side effects, and in some cases, adverse reactions in humans and experimental animals, such as myotoxicity, neurobehavioral toxicity, as well as liver and kidney injuries. The purpose of the present study was to examine the possibility of the induction of oxidative stress in the brain and plasma of mice dosed with single or repetitive doses of three statins (atorvastatin, simvastatin, and rosuvastatin). Methods Male Swiss-origin mice were dosed orally with single doses of each of the three statins at 500 or 1000 mg/kg of body weight. Other groups of mice were dosed orally with repeated daily doses of each of the statins at 200 mg/kg of body weight/day for 14 or 28 consecutive days. These doses of statins were chosen to not produce overt toxicity in mice within the time frame allocated for each experiment. Brain and plasma glutathione (GSH) and malondialdehyde (MDA) levels, as well as liver enzymes activities alanine transaminase (ALT) and aspartate transaminase (AST), were determined using commercial kits. Results Single-dose treatments of the mice with the statins at either 500 or 1000 mg/kg significantly and dose-dependently (p < 0.05) reduced the GSH level in the plasma and the whole brain when compared with respective control values. Atorvastatin was the least effective statin, as only the high dose achieved a significant reduction in brain GSH level in comparison with the respective control value. Repetitive administration of the three statins at 200 mg/kg of body weight/day for 14 or 28 consecutive days significantly and time-dependently reduced plasma and brain GSH levels in comparison with respective control values. The oxidative stress biomarker MDA level significantly increased in the plasma and brain of mice following single or repetitive treatments with the three statins, and the most effective one was rosuvastatin. In association with these changes, activities of the liver enzymes ALT and AST were also increased in the plasma with single and repetitive statin treatments, and the most effective one was rosuvastatin. Conclusion The data suggest an association of high doses of three statins (atorvastatin, simvastatin, and rosuvastatin) with the induction of oxidative stress manifested as GSH reduction and MDA elevation as adverse effects in the brain and plasma of mice, which suffered from the additional burden of liver injury. These effects could be the basis of an in-depth exploration of statin adverse effects in experimental animals and to find an animal model, probably the mice, for the induction of adverse effects of statins that target the brain, as well as to shed light on potential statin intolerance outcomes following single-dose treatments in this species.

17.
Food Res Int ; 176: 113813, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38163717

RESUMO

The proteins were mainly derived from Protaetia brevitarsis larval extracts obtained using two empty intestine methods (traditional static method: TSM or salt immersion stress method: SISM) and extraction solvents (water: W or 50 % water-ethanol: W:E), and the proteins were used as objects to investigate the effect of emptying intestine methods on hypolipidemic peptides. The results revealed that the F-2 fractions of protein hydrolysate had stronger in vitro hypolipidemic activity, with the peptides obtained by SISM possessing a stronger cholesterol micelle solubility inhibition rate, especially in SISM-W:E-P. Moreover, a total of 106 peptides were tentatively identified, among which SISM identified more peptides with an amino acid number < 8. Meanwhile, five novel peptides (YPPFH, YPGFGK, KYPF, SPLPGPR and VPPP) exhibited good hypolipidemic activity in vitro and in vivo, among which YPPFH, VPPP and KYPF had strong inhibitory activities on pancreatic lipase (PL) and cholesteryl esterase (CE), and KYPF, SPLPGPR and VPPP could significantly reduce the TG content in Caenorhabditis elegans. Thus, P. brevitarsis can be developed as a naturally derived hypolipidemic component for the development and application in functional foods.


Assuntos
Besouros , Hidrolisados de Proteína , Animais , Larva/química , Hidrolisados de Proteína/farmacologia , Hidrolisados de Proteína/metabolismo , Besouros/química , Peptídeos/farmacologia , Peptídeos/metabolismo , Água/metabolismo , Proteínas de Insetos/farmacologia , Proteínas de Insetos/metabolismo
18.
Foods ; 13(1)2024 Jan 02.
Artigo em Inglês | MEDLINE | ID: mdl-38201186

RESUMO

Chlorella oil nanoliposomes (CO-NLP) were synthesized through ultrasonic injection with ethanol, and their physicochemical properties and hypolipidemic efficacy were systematically investigated. The results revealed that the mean particle size of CO-NLP was 86.90 nm and the encapsulation efficiency (EE) was 92.84%. Storage conditions at 4 °C were conducive to the stability of CO-NLP, maintaining an EE of approximately 90% even after 10 days of storage. The release profile of CO-NLP adhered more closely to the first-order kinetic model during in vitro assessments, exhibiting a slower release rate compared to free microalgae oil. In simulated in vitro digestion experiments, lipolytic reactions of CO-NLP were observed during intestinal digestion subsequent to nanoliposome administration. Notably, the inhibitory effect of CO-NLP on cholesterol esterase activity was measured at 85.42%. Additionally, the average fluorescence intensity of nematodes in the CO-NLP group was 52.17% lower than in the control group at a CO-NLP concentration of 500 µg/mL, which suggests a pronounced lipid-lowering effect of CO-NLP. Therefore, the CO-NLP exhibited characteristics of small and uniform particle size, elevated storage stability, gradual release during intestinal digestion, and a noteworthy hypolipidemic effect. These findings designate CO-NLP as a novel lipid-lowering active product, demonstrating potential for the development of functional foods.

19.
Int J Health Sci (Qassim) ; 18(1): 4-9, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38188896

RESUMO

Objectives: This study examines the metabolic consequences of saponin and flavonoid extracts of Gongronema latifolium leaves in rat offspring whose mothers consumed sucrose during breastfeeding. Methods: Thirty-two female albino Wistar rats were randomly assigned to control group, given water only: sucrose group, given sucrose solution only; flavonoid groups, given sucrose solution and 100 mg/kg b.w. and 200 mg/kg b.w. of flavonoid and saponin groups, given sucrose solution and 100 mg/kg b.w. and 200 mg/kg b.w. of saponin extracts, for 3 weeks during lactation. Then the body, hepatic and pancreatic weights, food intake, glucose tolerance, lipid profile, insulin, and leptin levels of their offspring were measured. Results: There was a significant decrease in the body weight (BW), food intake, and glucose level among the flavonoid and saponin groups compared to the control group. However, when compared to the sucrose group, there was a significant decrease in food intake, blood glucose level, triglyceride, and very low-density lipoprotein cholesterol levels and a significant increase in the BW. There was no significant difference in insulin and leptin levels, hepatic, and pancreatic weights among groups. Conclusion: This study shows that G. lactifolium consumption among lactating rats maintains metabolic homeostatic as it protects against elevated blood glucose level and dyslipidemia in offspring post-weaning. It also suggests that the hypoglycemic and hypolipidemic properties of G. latifolium maybe as a result of saponin and flavonoids inherent in the plant.

20.
Clin Cardiol ; 47(1): e24183, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-37933175

RESUMO

AIM: This study aims to characterize sociodemographic and clinical characteristics, use of lipid-lowering therapies (LLTs), and low-density lipoprotein cholesterol (LDL-C) control in a population with increased cardiovascular (CV) risk. METHODS: A cross-sectional observational study that uses electronic health records of patients from one hospital and across 14 primary care health centers in the North of Portugal, spanning from 2000 to 2020 (index date). Patients presented at least (i) 1 year of clinical data before inclusion, (ii) one primary care appointment 3 years before the index date, and (iii) sufficient data for CV risk classification. Patients were divided into three cohorts: high CV risk; atherosclerotic cardiovascular disease (ASCVD) risk equivalents without established ASCVD; evidence of ASCVD. CV risk and LDL-C control were defined by the 2019 and 2016 European Society of Cardiology (ESC)/European Atherosclerosis Society (EAS) dyslipidemia guidelines. RESULTS: A total of 51 609 patients were included, with 23 457 patients classified as high CV risk, 19 864 with ASCVD equivalents, and 8288 with evidence of ASCVD. LDL-C control with 2016 ESC/EAS guidelines was 32%, 10%, and 18% for each group, respectively. Considering the ESC/EAS 2019 guidelines control level was even lower: 7%, 3%, and 7% for the same cohorts, respectively. Patients without any LLT prescribed ranged from 37% in the high CV risk group to 15% in patients with evidence of ASCVD. CONCLUSION: We found that LDL-C control was very low in patients at higher risk of CV events. An alarming gap between guidelines on dyslipidemia management and clinical implementation persists, even in those at very high risk or with established ASCVD.


Assuntos
Aterosclerose , Doenças Cardiovasculares , Dislipidemias , Inibidores de Hidroximetilglutaril-CoA Redutases , Humanos , LDL-Colesterol , Inibidores de Hidroximetilglutaril-CoA Redutases/uso terapêutico , Doenças Cardiovasculares/diagnóstico , Doenças Cardiovasculares/epidemiologia , Doenças Cardiovasculares/prevenção & controle , Estudos Transversais , Fatores de Risco , Dislipidemias/diagnóstico , Dislipidemias/tratamento farmacológico , Dislipidemias/epidemiologia , Aterosclerose/epidemiologia , Aterosclerose/tratamento farmacológico , Fatores de Risco de Doenças Cardíacas
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