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1.
Sci Rep ; 14(1): 308, 2024 01 03.
Artigo em Inglês | MEDLINE | ID: mdl-38172290

RESUMO

Alzheimer's disease (AD) is considered the leading cause of dementia in the elderly worldwide. It results in progressive memory loss and impairment of cognitive and motor skills, leading to a high degree of disability and dependence. The development of AD is associated with the accumulation of senile plaques in the brain, caused by the amyloidogenic pathway of the disease. Several genetic and biochemical events are linked to AD development, with oxidative stress being one of them. Due to the scarcity of drugs aimed at treating AD, antioxidant compounds are increasingly studied as therapeutic targets for the disease. In this study, we investigate the antioxidant and anti-Alzheimer potential of the Tetragonisca angustula (Jataí) pollen extract in a Drosophila melanogaster Alzheimer's model. For this purpose, we utilized a D. melanogaster AD-like model, which expresses genes related to the amyloidogenic pathway of Alzheimer's disease. We explored the floral origin of the collected pollen, conducted phytochemical prospecting, and evaluated its antioxidant capacity in vitro. In vivo experiments involved assessing the survival and climbing ability of the D. melanogaster AD-like model with various concentrations of the pollen extract. Our findings revealed that the pollen extract of Tetragonisca angustula exhibits a significant antioxidant response and high concentrations of important phytochemicals, such as flavonoids and polyphenols. Furthermore, it enhanced the survival rate of D. melanogaster, and across all concentrations tested, it improved the climbing ability of the flies after 15 days of treatment with methanolic pollen extract. Additionally, the pollen extract reduced the neurodegeneration index in histopathological analysis. Thus, our study demonstrates the potential of Tetragonisca angustula pollen as an important subject for further investigation, aiming to isolate molecules that could potentially serve as therapeutic targets for Alzheimer's disease.


Assuntos
Doença de Alzheimer , Antioxidantes , Humanos , Abelhas , Animais , Idoso , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Doença de Alzheimer/metabolismo , Drosophila melanogaster , Pólen/metabolismo , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico
2.
Pharmaceutics ; 14(6)2022 May 31.
Artigo em Inglês | MEDLINE | ID: mdl-35745755

RESUMO

Annona muricata Linn. is a common plant found in the warmest regions of South and Central America and its use in traditional medicine has been reported for the treatment of various illnesses. In the current study, we investigate the antioxidant and anti-inflammatory activities of crude extract and fractions from A. muricata L. leaves in isolated murine phagocytic immune cells as well as experimental LPS-induced acute lung injury (ALI). In a luminol-dependent chemiluminescence assay, we showed that ethyl acetate (EtOAc.f) and n-butanol (BuOH.f) fractions-both rich in polyphenols-reduced the generation of reactive oxygen species (ROS) by neutrophils stimulated with opsonized zymosan; similar results were found in culture of bone marrow-derived macrophages (BMDMs). By evaluating anti-inflammatory activity in BMDMs, EtOAc.f and BuOH.f reduced secretion of IL-6 and expression of the co-stimulatory molecule CD40. Furthermore, in LPS-induced ALI, oral administration of EtOAc.f reduced myeloperoxidase (MPO) activity in lung tissue. In addition, on a mechanism dependent on glutathione levels, the oxidative damage was also attenuated. These findings revealed direct antioxidant and anti-inflammatory activities of polyphenols-rich fractions of A. muricata L. leaves on neutrophils and macrophages. Moreover, the reduced oxidative damage and levels of inflammatory markers in experimental ALI suggest that these fractions might be explored for the development of new therapies for inflammatory conditions.

3.
J Pharm Biomed Anal ; 206: 114387, 2021 Nov 30.
Artigo em Inglês | MEDLINE | ID: mdl-34583125

RESUMO

Chronic hyperglycemia and hyperlipidemia are associated with excessive formation of reactive oxygen species and advanced glycation end-products. The present study aimed to evaluate the potential in vitro antidiabetic properties of Kielmeyera coriacea inner bark. The main phytochemical compounds were identified by UHPLC-ESI/MSn and the ethanol extract and its fractions were used to evaluate their antioxidant and anti-glycation capacities, as well as their inhibitory potential against glycoside and lipid hydrolases activities. The polar fractions, especially the n-butanol fraction, had free radical scavenging and quenching properties (ORAC and FRAP values>1800 and 1000 µmol trolox eq/g, respectively, and DPPH IC50<4 µg/mL), and inhibited ROS production (p < 0.01), lipid peroxidation (p < 0.001), glycation (IC50 ~ 10 µg/mL in the BSA-fructose assay; IC50 ~ 200 µg/mL in the BSA-methylglyoxal and arginine-methylglyoxal assays), α-amylase (IC50<0.1 µg/mL) and lipase (IC50<5 µg/mL), with no cytotoxicity. Biomolecules well-known as potent antioxidants were identified for the first time in the inner bark of K. coriacea, such as protocatechuic acid, epicatechin and procyanidins A, B and C. Together, our results support the antioxidant, anti-glycation and glycoside and lipid hydrolases inhibitory properties of the inner bark of K. coriacea, a species found in the Brazilian savanna, which makes it especially useful to combat oxidative stress and hyperglycemia and hyperlipidemia.


Assuntos
Antioxidantes , alfa-Amilases , Antioxidantes/farmacologia , Produtos Finais de Glicação Avançada , Hipoglicemiantes/farmacologia , Lipase , Extratos Vegetais/farmacologia
4.
Biomed Pharmacother ; 142: 112049, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34426250

RESUMO

Dyslipidemia is a risk factor for the pathogenesis of several diseases, such as obesity, hypertension, atherosclerosis and cardiovascular diseases. In addition to interfering with serum concentrations of cholesterol and triglycerides, hyperlipidemia is involved in oxidative stress increase and reduction of the endogenous antioxidant defenses. The fruit peel of Annona crassiflora crude extract (CEAc) and its polyphenols-rich fraction (PFAc) were investigated against hypertriglyceridemia, hypercholesterolemia and hepatic oxidative stress in Triton WR-1339-induced hyperlipidemic mice. Lipid parameters in serum, feces and liver, as well as hepatic oxidative status, and enzymatic and non-enzymatic antioxidant defense systems were analyzed. Pre-treatment with CEAc for 12 days decreased hepatic triglycerides and total cholesterol, and similar to PFAc, increased the high-density lipoprotein level. There were reductions in lipid peroxidation and protein carbonylation, as well as restoration of the glutathione defense system and total thiol content in the liver of the hyperlipidemic mice treated with PFAc. The fruit peel of A. crassiflora, a promising natural source of bioactive molecules, showed a potential lipid-lowering action and hepatoprotective activities triggered by reduction of oxidative damage and maintenance of the enzymatic and non-enzymatic antioxidant systems impaired by the hyperlipidemic state.


Assuntos
Annona/química , Antioxidantes/farmacologia , Glutationa/metabolismo , Hiperlipidemias/tratamento farmacológico , Hipolipemiantes/farmacologia , Extratos Vegetais/farmacologia , Polifenóis/farmacologia , Animais , Antioxidantes/isolamento & purificação , Antioxidantes/uso terapêutico , Colesterol/metabolismo , Frutas/química , Hiperlipidemias/induzido quimicamente , Hipolipemiantes/isolamento & purificação , Hipolipemiantes/uso terapêutico , Metabolismo dos Lipídeos/efeitos dos fármacos , Peroxidação de Lipídeos/efeitos dos fármacos , Fígado/efeitos dos fármacos , Masculino , Camundongos Endogâmicos C57BL , Estresse Oxidativo/efeitos dos fármacos , Oxirredutases/metabolismo , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/uso terapêutico , Polietilenoglicóis/toxicidade , Polifenóis/isolamento & purificação , Polifenóis/uso terapêutico , Carbonilação Proteica/efeitos dos fármacos , Triglicerídeos/metabolismo
5.
J Ethnopharmacol ; 215: 140-146, 2018 Apr 06.
Artigo em Inglês | MEDLINE | ID: mdl-29274842

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Plants preparations are used by traditional medicine in the treatment of various diseases, such as type-2 diabetes mellitus. Some medicinal plants are capable of controlling the complications of this metabolic disease at different levels, for example, providing antioxidant compounds that act against oxidative stress and protein glycation and others which are capable of inhibiting the catalysis of digestive enzymes and thus contribute to the reduction of hyperglycemia and hyperlipidemia. Our objective was to investigate the antioxidant and anti-glycation activities of some medicinal plants and their potential inhibitory against α-amylase, α-glucosidase and pancreatic lipase activities. MATERIAL AND METHODS: Based on the ethnobotanical researches carried out by academic studies conducted at the Federal University of Uberlandia, ten plants traditionally used in the treatment of type-2 diabetes mellitus were selected. Ethanol (EtOH) and hexane (Hex) extracts of specific parts of these plants were used in enzymatic assays to evaluate their inhibitory potential against α-amylase, α-glucosidase and lipase, as well as their antioxidant (DPPH, ORAC and FRAP) and anti-glycation (BSA/fructose model) capacities. RESULTS: The results indicate that EtOH extract of four of the ten analyzed plants exhibited more than 70% of antioxidant and anti-glycation capacities, and α-amylase and lipase inhibitory activities; no extract was able to inhibit more than 40% the α-glucosidase activity. The EtOH extracts of Bauhinia forficata and Syzygium. cumini inhibited α-amylase (IC50 8.17 ± 2.24 and 401.8 ± 14.7 µg/mL, respectively), whereas EtOH extracts of B. forficata, Chamomilla recutita and Echinodorus grandiflorus inhibited lipase (IC50 59.6 ± 10.8, 264.2 ± 87.2 and 115.8 ± 57.1 µg/mL, respectively). In addition, EtOH extracts of B. forficata, S. cumini, C. recutita and E. grandiflorus showed, respectively, higher antioxidant capacity (DPPH IC50 0.7 ± 0.1, 2.5 ± 0.2, 1.3 ± 0.2 and 35.3 ± 9.0 µg/mL) and anti-glycation activity (IC50 22.7 ± 4.4, 246.2 ± 81.7, 18.5 ± 2.8 and 339.0 ± 91.0 µg/mL). CONCLUSIONS: EtOH extracts of four of the ten species popularly cited for treatment of type 2 diabetes mellitus have shown promising antioxidant and anti-glycation properties, as well as the ability to inhibit the digestive enzymes α-amylase and lipase. Thus, our results open new possibilities for further studies in order to evaluate the antidiabetic potential of these medicinal plants.


Assuntos
Antioxidantes/farmacologia , Diabetes Mellitus Tipo 2 , Inibidores de Glicosídeo Hidrolases , Lipase/antagonistas & inibidores , Plantas Medicinais/química , alfa-Amilases/antagonistas & inibidores , Antioxidantes/química , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Pâncreas/enzimologia , alfa-Glucosidases
6.
J Agric Food Chem ; 65(22): 4428-4438, 2017 Jun 07.
Artigo em Inglês | MEDLINE | ID: mdl-28514152

RESUMO

A polyphenol-enriched fraction from Annona crassiflora fruit peel (Ac-Pef) containing chlorogenic acid, (epi)catechin, procyanidin B2, and caffeoyl-glucoside was investigated against hepatic oxidative and nitrosative stress in streptozotocin-induced diabetic rats. Serum biochemical parameters, hepatic oxidative and nitrosative status, glutathione defense system analysis, and in silico assessment of absorption, distribution, metabolism, excretion, and toxicity (ADMET) of the main compounds of Ac-Pef were carried out. Ac-Pef treatment during 30 days decreased serum alanine aminotransferase, aspartate aminotransferase, and alkaline phosphatase activities, as well as hepatic lipid peroxidation, protein carbonylation and nitration, inducible nitric oxide synthase level, and activities and expressions of glutathione peroxidase, superoxide dismutase, and catalase. There were increases in antioxidant capacity, glutathione reductase activity, and reduced glutathione level. ADMET predictions of Ac-Pef compounds showed favorable absorption and distribution, with no hepatotoxicity. A. crassiflora fruit peel showed hepatoprotective properties, indicating a promising natural source of bioactive molecules for prevention and therapy of diabetes complications.


Assuntos
Annona/química , Diabetes Mellitus Experimental/tratamento farmacológico , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Polifenóis/administração & dosagem , Substâncias Protetoras/administração & dosagem , Alanina Transaminase/sangue , Animais , Antioxidantes/administração & dosagem , Antioxidantes/química , Aspartato Aminotransferases/sangue , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/metabolismo , Frutas/química , Glutationa Peroxidase/sangue , Humanos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Estrutura Molecular , Extratos Vegetais/química , Polifenóis/química , Substâncias Protetoras/química , Ratos
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