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1.
Drug Des Devel Ther ; 18: 3825-3839, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39219697

RESUMO

Background: The twigs and roots of Erythrina subumbrans (Hassk). Merr. Was reported to possess antidiabetic activity by reducing the activity of α-glucosidase and α-amylase. TNF-α is a pro-inflammatory cytokine in obesity and diabetes mellitus (DM). It inhibits the action of insulin, causing insulin resistance. Adiponectin is an anti-inflammatory peptide synthesized in white adipose tissue (WAT) and its high levels are linked with a decreased risk of DM. However, information about the effect of Erythrina subumbrans (Hassk). Merr. on insulin resistance are still lacking. Purpose: To obtain the effects of the ethanol extract of E. subumbrans (Hassk) Merr. leaves (EES) in improving insulin resistance conditions. Methods: The leaves were collected at Ciamis, West Java, Indonesia, and were extracted using ethanol 96%. The effects of EES were studied in fructose-induced adult male Wistar rats by performing the insulin tolerance test (ITT) and assessing blood glucose, TNF-α, adiponectin, and FFA levels. The number of WAT and BAT of the adipose tissues was also studied. The total phenols and flavonoids in EES were determined by the spectrophotometric method and the presence of quercetin in EES was analyzed using the LC-MS method. Results: EES significantly reduced % weight gain, TNF-α levels, and increased adiponectin levels in fructose-induced Wistar rats. EES significantly reduced the FFA levels of fructose-induced Wistar rats and significantly affected the formation of BAT similar to that of metformin. All rats in EES and metformin groups improved insulin resistance as proven by higher ITT values (3.01 ± 0.91 for EES 100 mg/kg BW; 3.01 ± 1.22 for EES 200 mg/kg BW; 5.86 ± 3.13 for EES 400 mg/kg BW; and 6.44 ± 2.58 for metformin) compared with the fructose-induced group without treatment (ITT = 2.62 ± 1.38). EES contains polyphenol compounds (2.7638 ± 0.0430 mg GAE/g extract), flavonoids (1.9626 ± 0.0152 mg QE/g extract), and quercetin 0.246 µg/mL at m/z 301.4744. Conclusion: Erythrina subumbrans (Hassk). Merr. extract may have the potential to be further explored for its activity in improving insulin resistance conditions. However, further studies are needed to confirm its role in alleviating metabolic disorders.


Assuntos
Erythrina , Frutose , Resistência à Insulina , Extratos Vegetais , Ratos Wistar , Animais , Ratos , Masculino , Erythrina/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Frutose/farmacologia , Tecido Adiposo/efeitos dos fármacos , Tecido Adiposo/metabolismo , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Folhas de Planta/química , Relação Dose-Resposta a Droga
2.
Drug Des Devel Ther ; 18: 3443-3459, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39109327

RESUMO

Purpose: This study aimed to isolate and characterize palmatine from Fibraurea tinctoria Lour stems, quantify its content, and determine its antioxidant and antidiabetic activities. Patients and Methods: Palmatine was isolated from the methanol extract of Fibraurea tinctoria Lour stems by silica gel column chromatography. Structural elucidation of the isolated compounds was performed using spectral data analysis and comparison with the literature. High-Performance Liquid Chromatography (HPLC) was used to quantitatively determine palmatine in the crude methanol extract and fractions. The DPPH and non-enzymatic SOD mimic methods were used to assess the antioxidant activity of the methanol extract, fractions, and isolated compounds. The antidiabetic activity was evaluated in silico by the molecular docking method of alpha-glucosidase and DPP-IV enzymes. Palmatine was used as a test ligand and was compared with berberine and its native ligand or standard compounds. Results: The isolated compound was identified as palmatine. Quantification of palmatine compound by HPLC showed that palmatine was found in the extract and all fractions. In the in vitro antioxidant activity test using the DPPH method, fraction 4 showed the highest activity, with an IC50 value of 91 ppm. In contrast, using the non-enzymatic SOD mimic method, the methanol extract, fraction 5, and isolated compound (palmatine) exhibited very strong antioxidant activity, with IC50 values of 18, 20, and 28 ppm, respectively. The in silico antidiabetic activity of palmatine is thought to have the potential to inhibit these two enzymes. Conclusion: These results showed that Fibraurea tinctoria Lour stems have potential as an antioxidant and antidiabetic agent. Further research on phytochemical and pharmacological is required to validate the use of this plant species for the treatment of various diseases, especially diabetes mellitus.


Assuntos
Antioxidantes , Alcaloides de Berberina , Hipoglicemiantes , Simulação de Acoplamento Molecular , Extratos Vegetais , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Antioxidantes/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/química , Alcaloides de Berberina/farmacologia , Alcaloides de Berberina/isolamento & purificação , Alcaloides de Berberina/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Compostos de Bifenilo/antagonistas & inibidores , Compostos de Bifenilo/química , Picratos/antagonistas & inibidores , Picratos/química , Simulação por Computador , alfa-Glucosidases/metabolismo , Relação Estrutura-Atividade
3.
Drug Des Devel Ther ; 18: 3595-3616, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39156483

RESUMO

Background: Diabetes mellitus is a complex metabolic disorder that has an enormous impact on people's quality of life and health. Although there is no doubt about the effectiveness of oral hypoglycemic agents combined with lifestyle management in controlling diabetes, no individual has ever been reported to have been completely cured of the disease. Globally, many medicinal plants have been used for the management of diabetes in various traditional systems of medicine. A deep look in the literature has revealed that the Liliaceae family have been poorly investigated for their antidiabetic activity and phytochemical studies. In this review, we summarize medicinal plants of Liliaceae utilized in the management of type II diabetes mellitus (T2DM) by inhibition of α-glucosidase enzyme and phytochemical content. Methods: The literature search was conducted using databases including PubMed, ScienceDirect, and Google Scholar to find the significant published articles about Liliaceae plants utilized in the prevention and treatment of antidiabetics. Data were filtered to the publication period from 2013 to 2023, free full text and only English articles were included. The keywords were Liliaceae OR Alliaceae OR Amaryllidaceae AND Antidiabetic OR α-glucosidase. Results: Six medicinal plants such as Allium ascalonicum, Allium cepa, Allium sativum, Aloe ferox, Anemarrhena asphodeloides, and Eremurus himalaicus are summarized. Phytochemical and α-glucosidase enzymes inhibition by in vitro, in vivo, and human studies are reported. Conclusion: Plants of Liliaceae are potential as medicine herbs to regulating PPHG and prevent the progression of T2DM and its complication. In silico study, clinical application, and toxicity evaluation are needed to be investigated in the future.


Assuntos
Diabetes Mellitus Tipo 2 , Inibidores de Glicosídeo Hidrolases , Hipoglicemiantes , Plantas Medicinais , alfa-Glucosidases , Humanos , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Plantas Medicinais/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Diabetes Mellitus Tipo 2/tratamento farmacológico , alfa-Glucosidases/metabolismo , Animais
4.
Mar Drugs ; 22(8)2024 Jul 27.
Artigo em Inglês | MEDLINE | ID: mdl-39195460

RESUMO

The subcritical water extraction of Undaria pinnatifida (blade, sporophyll, and root) was evaluated to determine its chemical properties and biological activities. The extraction was conducted at 180 °C and 3 MPa. Root extracts exhibited the highest phenolic content (43.32 ± 0.19 mg phloroglucinol/g) and flavonoid content (31.54 ± 1.63 mg quercetin/g). Sporophyll extracts had the highest total sugar, reducing sugar, and protein content, with 97.35 ± 4.23 mg glucose/g, 56.44 ± 3.10 mg glucose/g, and 84.93 ± 2.82 mg bovine serum albumin (BSA)/g, respectively. The sporophyll contained the highest fucose (41.99%) and mannose (10.37%), whereas the blade had the highest galactose (48.57%) and glucose (17.27%) content. Sporophyll had the highest sulfate content (7.76%). Key compounds included sorbitol, glycerol, L-fucose, and palmitic acid. Root extracts contained the highest antioxidant activity, with IC50 values of 1.51 mg/mL (DPPH), 3.31 mg/mL (ABTS+), and 2.23 mg/mL (FRAP). The root extract exhibited significant α-glucosidase inhibitory activity with an IC50 of 5.07 mg/mL, indicating strong antidiabetic potential. The blade extract showed notable antihypertensive activity with an IC50 of 0.62 mg/mL. Hence, subcritical water extraction to obtain bioactive compounds from U. pinnatifida, supporting their use in functional foods, cosmetics, and pharmaceuticals is highlighted. This study uniquely demonstrates the variation in bioactive compound composition and bioactivities across different parts of U. pinnatifida, providing deeper insights. Significant correlations between chemical properties and biological activities emphasize the use of U. pinnatifida extracts for chronic conditions.


Assuntos
Antioxidantes , Extratos Vegetais , Undaria , Antioxidantes/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/química , Undaria/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Água/química , Raízes de Plantas/química , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Flavonoides/química , Anti-Hipertensivos/farmacologia , Anti-Hipertensivos/isolamento & purificação , Anti-Hipertensivos/química , Fenóis/isolamento & purificação , Fenóis/farmacologia , Fenóis/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Algas Comestíveis
5.
Bioorg Chem ; 152: 107763, 2024 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-39216195

RESUMO

This manuscript describes the isolation of nine new nor-3,4-seco-dammarane triterpenoids, norqingqianliusus A-I (1-9) and one known nortriterpenoid (10) from Cyclocarya paliurus leaves. Norqingqianliusus A and B (1 and 2) possess a unique 3,4-seco-dammarane-type C26 tetranortriterpenoid skeleton. The compounds were structurally characterized through modern spectroscopic techniques. Moreover, the potential mechanism of hypoglycemic activity was further explored by studying the effects on glucosamine-induced insulin resistant HepG2 cells. In vitro hypoglycemic effects of all of the isolates were investigated using insulin resistant HepG2 cells. The glucose consumption was significantly promoted by compound 10, in a dose-dependent manner, thus alleviating damage in IR-HepG2 cells. Besides, it reduced the PEPCK and GSK3ß gene expression, involved in glucose metabolism. The anti-diabetic effects of the plant, utilized traditionally, can hence be attributed to the presence of nor-3,4-seco-dammarane triterpenoids in the leaves.


Assuntos
Damaranos , Hipoglicemiantes , Juglandaceae , Folhas de Planta , Triterpenos , Triterpenos/farmacologia , Triterpenos/química , Triterpenos/isolamento & purificação , Folhas de Planta/química , Humanos , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Juglandaceae/química , Células Hep G2 , Estrutura Molecular , Relação Estrutura-Atividade , Relação Dose-Resposta a Droga
6.
Fitoterapia ; 178: 106177, 2024 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-39122120

RESUMO

This study was conducted to determine and compare the phenolic compounds, glucosinolate contents and antidiabetic effects of the extracts obtained by ultrasonic and conventional extraction method of the leaves and flowers of the Crambe tataria. The highest antioxidant activity (12.95 mg/mL IC50 value) and total phenolic content (1313.57 mg GAE/100 g fw) were detected in the ultrasonic flower extract. In total flavonoid results, extracts obtained from the flower part of C. tataria had higher values than that of extracts obtained from the leaf part. The most abundant phenolic component in the flower extract was catechin. The highest catechin content in all samples was detected in the ultrasonic flower extract with a value of 374.37 mg/kg. Rutin was the dominant phenolic component in the leaf extract. Rutin values were 654.38 mg/kg and 757.30 mg/kg for conventional and ultrasonic extraction, respectively. In glucosinolate analysis, the highest glucoraphanin content was obtained in flower samples and by conventional extraction method (3466.84 mg/kg). The highest contents of sinigrin (689.97 mg/kg), glucotropaeolin (420.89 mg/kg), glucoerucin (357.27 mg/kg), glucoraphasatin (181.11 mg/kg) and gluconasturtin (66.07 mg/kg) were detected in ultrasonic flower extracts. The highest α-amylase and α-glucosidase enzyme inhibition effects belonged to the ultrasonic flower extract with values of 3.70 mg/mL and 4.89 mg/mL, respectively. As a result, this study determined for the first time that ultrasonic extraction of C. tataria flowers has much higher bioactive components and antidiabetic effects, revealing the potential use of this plant in the fields of medicine, pharmacology and chemistry.


Assuntos
Antioxidantes , Flores , Glucosinolatos , Hipoglicemiantes , Extratos Vegetais , Folhas de Planta , Glucosinolatos/isolamento & purificação , Glucosinolatos/análise , Flores/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/análise , Hipoglicemiantes/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Antioxidantes/análise , Fenóis/análise , Fenóis/isolamento & purificação , Fenóis/farmacologia , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/análise , Flavonoides/análise , Flavonoides/isolamento & purificação , Ultrassom
7.
Mar Drugs ; 22(8)2024 Aug 12.
Artigo em Inglês | MEDLINE | ID: mdl-39195481

RESUMO

Enhalus acoroides, a tropical seagrass, is known for its significant contribution to marine ecosystems and its potential health benefits due to bioactive compounds. This study aims to compare the carotenoid levels in E. acoroides using green extraction via ultrasound-assisted extraction (UAE) and microwave-assisted extraction (MAE) and to evaluate the biological properties of these extracts against oxidative stress, diabetes, and obesity through in silico and in vitro analyses. E. acoroides samples were collected from Manado City, Indonesia, and subjected to UAE and MAE. The extracts were analyzed using UHPLC-ESI-MS/MS to identify carotenoids, including ß-carotene, lutein, lycopene, ß-cryptoxanthin, and zeaxanthin. In silico analysis was conducted to predict the compounds' bioactivity, toxicity, and drug-likeness using WAY2DRUG PASS and molecular docking with CB-Dock2. The compounds C3, C4, and C7 demonstrated notable interactions, with key metabolic proteins and microRNAs, further validating their potential therapeutic benefits. In vitro assays evaluated antioxidant activities using DPPH and FRAP assays, antidiabetic properties through α-glucosidase and α-amylase inhibition, and antiobesity effects via lipase inhibition and MTT assay with 3T3-L1 cells. Results indicated that both UAE and MAE extracts exhibited significant antioxidant, antidiabetic, and antiobesity activities. MAE extracts showed higher carotenoid content and greater biological activity compared to UAE extracts. These findings suggest that E. acoroides, mainly when extracted using MAE, has promising potential as a source of natural bioactive compounds for developing marine-based antioxidant, antidiabetic, and antiobesity agents. This study supplements existing literature by providing insights into the efficient extraction methods and the therapeutic potential of E. acoroides carotenoids.


Assuntos
Fármacos Antiobesidade , Antioxidantes , Carotenoides , Hipoglicemiantes , Simulação de Acoplamento Molecular , Antioxidantes/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Carotenoides/farmacologia , Carotenoides/isolamento & purificação , Carotenoides/química , Fármacos Antiobesidade/farmacologia , Fármacos Antiobesidade/isolamento & purificação , Fármacos Antiobesidade/química , Camundongos , Animais , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Simulação por Computador , Obesidade/tratamento farmacológico , Células 3T3-L1 , Espectrometria de Massas em Tandem , Indonésia , Micro-Ondas , Estresse Oxidativo/efeitos dos fármacos
8.
Int J Biol Macromol ; 275(Pt 2): 133686, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38972653

RESUMO

Eucommia ulmoides Oliv. (tu-chung), as a famous nature medical and edible plant, has the effect of tonifying liver and kidney, strengthening the function of the muscles and bones, and miscarriage prevention. Accumulating evidence has demonstrated that the polysaccharides from Eucommia ulmoides Oliv. (EUPs) are a kind of vital and representative biologically active macromolecules and have various health-promoting biological activities in vivo and in vitro, such as antioxidant activity, immunomodulatory activity, hypolipidemic and hypoglycemic activities, anti-inflammatory activities, anti-tumor activity, and among others. The review aims to comprehensively and systematically collate the recent research progress on extraction and purification methods, structural characteristics, biological activities, mechanism of action, structural modification, and toxicity of EUPs to support their therapeutic potential and health-care functions. New valuable insights for future research with EUPs were also proposed in the areas of structural characterization and pharmacological activities to promoting the development of therapeutic agents and functional foods.


Assuntos
Eucommiaceae , Polissacarídeos , Polissacarídeos/química , Polissacarídeos/farmacologia , Polissacarídeos/isolamento & purificação , Eucommiaceae/química , Humanos , Antioxidantes/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Animais , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação
9.
Food Chem ; 458: 139516, 2024 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-39053391

RESUMO

The study investigates the effect of conventional and novel extraction techniques on the protein extraction yield from bitter gourd seeds (Momordica charantia). Ultrasound assisted-extraction (UAE) treatment for 30 min at 4 °C using a 20 kHz ultrasound probe resulted in the highest extraction yield of crude proteins. After purification, 9.08 ± 0.23 g of protein with 82.69 ± 0.78% purity was obtained from 100 g of M. charantia seeds on a dry basis. Mass spectrometry identified proteins with reported antidiabetic activity. Antidiabetic assays showed significantly higher antidiabetic activity for the purified protein (81.10 ± 2.64%) compared to the crude protein (32.59 ± 2.76%). In vitro cytotoxicity analysis showed minimal cytotoxicity levels at concentrations <200 µg.mL-1. Overall, UAE was effective to obtain crude protein from M. charantia seeds and a subsequent purification step enhanced antidiabetic activity. However, further research is required to demonstrate in-vivo antidiabetic activity.


Assuntos
Hipoglicemiantes , Momordica charantia , Extratos Vegetais , Proteínas de Plantas , Sementes , Momordica charantia/química , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/isolamento & purificação , Proteínas de Plantas/isolamento & purificação , Proteínas de Plantas/química , Proteínas de Plantas/farmacologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Sementes/química , Humanos , Fracionamento Químico/métodos , Animais
10.
J Ethnopharmacol ; 334: 118516, 2024 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-38971341

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Calotropis gigantea (L.) Dryand. (C. gigantea) is a traditional medicinal plant, recognized for its effectiveness in managing diabetes, along with its notable antioxidant, anti-inflammatory, and anticancer properties. Type II diabetes mellitus (T2DM) is characterized by chronic metabolic disorders associated with an elevated risk of hepatocellular carcinoma (HCC) due to hyperglycemia and impaired insulin response. The scientific validation of C. gigantea's ethnopharmacological efficacy offers advantages in alleviating cancer progression in T2DM complications, enriching existing knowledge and potentially aiding future clinical cancer treatments. AIM: This study aimed to investigate the preventive potential of the dichloromethane fraction of C. gigantea stem bark extract (CGDCM) against diethylnitrosamine (DEN)-induced HCC in T2DM rats, aiming to reduce cancer incidence associated with diabetes while validating C. gigantea's ethnopharmacological efficacy. MATERIALS AND METHODS: Spontaneously Diabetic Torii (SDT) rats were administered DEN to induce HCC (SDT-DEN-VEH), followed by treatment with CGDCM. Metformin was used as a positive control (SDT-DEN-MET). All the treatments were administered for 10 weeks after the initial DEN injection. Diabetes-related parameters, including serum levels of glucose, insulin, and glycosylated hemoglobin (HbA1c), as well as liver function enzymes (aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, and gamma-glutamyl transferase), were quantified. Serum inflammation biomarkers interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) were evaluated. Liver tissue samples were analyzed for inflammation protein expression (IL-6, TNF-α, transforming growth factor-ß1 (TGF-ß1), and α-smooth muscle actin (α-SMA)). Histopathological evaluation was performed to assess hepatic necrosis, inflammation, and fibrosis. Liver cell proliferation was determined using immunohistochemistry for Ki-67 expression. RESULTS: Rats with SDT-DEN-induced HCC treated with CGDCM exhibited reduced serum glucose levels, elevated insulin levels, and decreased HbA1c levels. CGDCM treatment also reduced elevated hepatic IL-6, TNF-α, TGF-ß1, and α-SMA levels in SDT-DEN-VEH rats. Additionally, CGDCM treatment prevented hepatocyte damage, fibrosis, and cell proliferation. No adverse effects on normal organs were observed with CGDCM treatment, suggesting its safety for the treatment of HCC complications associated with diabetes. Additionally, the absence of adverse effects in SD rats treated with CGDCM at 2.5 mg/kg further supports the notion of its safe usage. CONCLUSIONS: These findings suggest that C. gigantea stem bark extract exerts preventive effects against the development of HCC complications in patients with T2DM, expanding the potential benefits of its ethnopharmacological advantages.


Assuntos
Calotropis , Diabetes Mellitus Experimental , Dietilnitrosamina , Insulina , Cloreto de Metileno , Casca de Planta , Extratos Vegetais , Animais , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Casca de Planta/química , Masculino , Ratos , Dietilnitrosamina/toxicidade , Cloreto de Metileno/química , Insulina/sangue , Calotropis/química , Diabetes Mellitus Experimental/tratamento farmacológico , Neoplasias Hepáticas/prevenção & controle , Neoplasias Hepáticas/tratamento farmacológico , Neoplasias Hepáticas/induzido quimicamente , Neoplasias Hepáticas/patologia , Diabetes Mellitus Tipo 2/tratamento farmacológico , Hipoglicemiantes/farmacologia , Hipoglicemiantes/isolamento & purificação , Carcinoma Hepatocelular/induzido quimicamente , Carcinoma Hepatocelular/tratamento farmacológico , Carcinoma Hepatocelular/prevenção & controle , Fígado/efeitos dos fármacos , Fígado/patologia , Fígado/metabolismo , Glicemia/efeitos dos fármacos , Caules de Planta/química , Neoplasias Hepáticas Experimentais/prevenção & controle , Neoplasias Hepáticas Experimentais/induzido quimicamente , Neoplasias Hepáticas Experimentais/tratamento farmacológico , Neoplasias Hepáticas Experimentais/patologia
11.
Food Res Int ; 191: 114731, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-39059924

RESUMO

The recovery of bioactive compounds is a promising approach for obtaining rich extracts from fruit by-products. This study investigated the influence of Natural Deep Eutectic Solvents (NADES) and Ultrasound-Assisted Extraction (UAE) on the phenolic content, antioxidant capacity, and in vitro antidiabetic activity of Psidium myrtoides by-product. Among eight NADES evaluated based on choline chloride, NADES ChCl:Gly (1:2) was selected for its efficiency in extracting total phenolic compounds (TPC) with high antioxidant capacity. The optimized conditions were 61 °C, a solid-liquid ratio of 100 mg 5 mL-1, and a 60-minute extraction time. ChCl:Gly exhibited superior TPC recovery (2.6-fold greater effectiveness) compared to the 60 % hydroethanolic solution. Twenty-six phenolic compounds were identified, including significant levels of catechin (336.48 mg g-1) and isoquercetin (26.09 mg g-1). Phenolic acids, such as p-anisic acid (5.47 mg g-1) and methoxyphenylacetic acid (0.23 mg g-1), were identified for the first time in the purple araçá by-product. The ChCl:Gly extract demonstrated the highest bioactivity, showcasing antioxidant and antidiabetic capacities. This study introduces an innovative and sustainable alternative for recovering phenolic compounds from fruit by-products, offering enhanced recovery efficiency and/or selectivity compared to organic solvents.


Assuntos
Antioxidantes , Solventes Eutéticos Profundos , Frutas , Fenóis , Extratos Vegetais , Psidium , Fenóis/análise , Fenóis/isolamento & purificação , Extratos Vegetais/química , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/análise , Psidium/química , Solventes Eutéticos Profundos/química , Frutas/química , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/química , Hipoglicemiantes/análise , Ondas Ultrassônicas , Química Verde , Solventes/química
12.
Biomed Pharmacother ; 177: 117072, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38991301

RESUMO

The development of natural substances derived from nature poses a significant challenge as technologies for the extraction and characterization of active principles advance. Hispolon has received a lot of attention in recent years, ascribable to its wide range of biological activities. It is a phenolic molecule that was extracted from several mushroom species such as Phellinus igniarius, Phellinus linteus, Phellinus lonicerinus, Phellinus merrillii, and Inonotus hispidus. To provide a comprehensive overview of the pharmacological activities of hispolon, this review highlights its anticancer, anti-inflammatory, antioxidant, antibacterial, and anti-diabetic activities. Several scientific research databases, including Google Scholar, Web of Science, PubMed, SciFinder, SpringerLink, Science Direct, Scopus, and, Wiley Online were used to gather the data on hispolon until May 2024. The in vitro and in vivo studies have revealed that hispolon exhibited significant anticancer properties through modifying several signaling pathways including cell apoptosis, cycle arrest, autophagy, and inhibition of angiogenesis and metastasis. Hispolon's antimicrobial activity was proven against many bacterial, fungal, and viral pathogens, highlighting its potential use as a novel antimicrobial agent. Additionally, hispolon displayed potent anti-inflammatory activity through the suppression of key inflammatory mediators, such as inducible NO synthase (iNOS), tumor necrosis factor-α (TNF-α), and cyclooxygenases-2 (COX-2), and the modulation of mitogen-activated protein kinases (MAPK) and nuclear factor kappa B (NF-κB) signaling pathways. The antioxidant potential of hispolon was attributed to its capacity to neutralize reactive oxygen species (ROS) and to increase the activity of antioxidant enzymes, indicating a possible involvement in the prevention of oxidative stress-related illnesses. Hispolon's antidiabetic activity was associated with the inhibition of aldose reductase and α-glucosidase. Studies on hispolon emphasized its potential use as a promising scaffold for the development of novel therapeutic agents targeting various diseases, including cancer, infectious diseases, inflammatory disorders, and diabetes.


Assuntos
Anti-Inflamatórios , Antineoplásicos , Antioxidantes , Animais , Humanos , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/isolamento & purificação , Antioxidantes/farmacologia , Antioxidantes/isolamento & purificação , Antineoplásicos/farmacologia , Antineoplásicos/isolamento & purificação , Hipoglicemiantes/farmacologia , Hipoglicemiantes/isolamento & purificação , Imino Açúcares/farmacologia , Imino Açúcares/química , Transdução de Sinais/efeitos dos fármacos , Catecóis
13.
Phytochemistry ; 226: 114206, 2024 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-38972440

RESUMO

Eighteen compounds including eleven previously undescribed diterpenes were isolated from the leaves of Croton mangelong. The structures were determined by HRESIMS, IR, NMR, X-ray diffraction and ECD spectroscopic analysis. All isolates were assayed for their anti-hyperglycemic activities in insulin resistance (IR) 3T3-L1 adipocytes, and compound 4 was tested for its anti-diabetic activity in vivo. Results suggested compound 4 could effectively reduce blood glucose level in diabetic SD rats in a dose of 30 mg/kg.


Assuntos
Células 3T3-L1 , Croton , Diterpenos , Hipoglicemiantes , Folhas de Planta , Ratos Sprague-Dawley , Folhas de Planta/química , Diterpenos/farmacologia , Diterpenos/química , Diterpenos/isolamento & purificação , Croton/química , Animais , Camundongos , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Ratos , Estrutura Molecular , Diabetes Mellitus Experimental/tratamento farmacológico , Masculino , Resistência à Insulina , Glicemia/efeitos dos fármacos , Adipócitos/efeitos dos fármacos
14.
Food Chem ; 460(Pt 1): 140493, 2024 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-39053284

RESUMO

In this study, the structural characterization, physicochemical properties, antioxidant, hypolipidemic, and hypoglycemic potentials of polysaccharide components (BLP-1, BLP-2, and BLP-3) purified from blueberry leaf polysaccharides (BLP) were investigated. Ion chromatography results showed that BLP-1, BLP-2, and BLP-3 contained rhamnose, arabinose, galactose, glucose, and glucuronic acid. In contrast to BLP-1, BLP-2 and BLP-3 included galacturonic acid. The methylation analysis results indicated that the backbones of BLP-1, BLP-2, and BLP-3 were mainly composed of glycosidic linkages of arabinose, galactose, and glucose, which was consistent with the results of the previously determined monosaccharide composition. The in-vitro antioxidant results showed that BLP-1, BLP-2, and BLP-3 possessed antioxidant activity with the highest scavenging of -OH radicals. Furthermore, BLP-1, BLP-2, and BLP-3 showed high bile acid-binding activity and α-amylase inhibitory activity, suggesting that they have the potentials of hypolipidemic and hypoglycemic. This study provides a reference for the utilization of blueberry leaf resources.


Assuntos
Mirtilos Azuis (Planta) , Hipoglicemiantes , Hipolipemiantes , Extratos Vegetais , Folhas de Planta , Polissacarídeos , Mirtilos Azuis (Planta)/química , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/isolamento & purificação , Hipolipemiantes/química , Hipolipemiantes/isolamento & purificação , Hipolipemiantes/farmacologia , Folhas de Planta/química , Polissacarídeos/química , Polissacarídeos/isolamento & purificação , Polissacarídeos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Animais , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Humanos , Camundongos , Masculino , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/química
15.
Molecules ; 29(13)2024 Jun 27.
Artigo em Inglês | MEDLINE | ID: mdl-38998999

RESUMO

Phellinus is a precious perennial medicinal fungus. Its polysaccharides are important bioactive components, and their chemical composition is complex. The polysaccharides are mainly extracted from the fruiting body and mycelium. The yield of the polysaccharides is dependent on the extraction method. They have many pharmacological activities, such as antitumor, immunomodulatory, antioxidant, hypoglycemic, anti-inflammatory, etc. They are also reported to show minor toxic and side effects. Many studies have reported the anticancer activity of Phellinus polysaccharides. This review paper provides a comprehensive examination of the current methodologies for the extraction and purification of Phellinus polysaccharides. Additionally, it delves into the structural characteristics, pharmacological activities, and mechanisms of action of these polysaccharides. The primary aim of this review is to offer a valuable resource for researchers, facilitating further studies on Phellinus polysaccharides and their potential applications.


Assuntos
Polissacarídeos Fúngicos , Humanos , Polissacarídeos Fúngicos/química , Polissacarídeos Fúngicos/farmacologia , Polissacarídeos Fúngicos/isolamento & purificação , Basidiomycota/química , Polissacarídeos/química , Polissacarídeos/farmacologia , Polissacarídeos/isolamento & purificação , Antioxidantes/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Antineoplásicos/farmacologia , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Animais , Phellinus/química
16.
Molecules ; 29(13)2024 Jun 27.
Artigo em Inglês | MEDLINE | ID: mdl-38999001

RESUMO

The root of Adenophora tetraphylla (Thunb.) Fisch. is a common Chinese materia medica and the polysaccharides which have been isolated from the plant are important active components for medicinal purposes. The objective of the current study was to optimize the extraction parameters and evaluate the glucose consumption activity for Adenophorae root polysaccharides (ARPs). The optimization of ARP extraction was evaluated with preliminary experiments and using response surface methodology (RSM). The conditions investigated were 35-45 °C extraction temperature, 20-30 (v/w) water-to-solid ratio, and 3-5 h extraction time. The antidiabetic effects of ARPs for the glucose consumption activity were evaluated in HepG2 cells. The statistical analyses of the experiments indicated that temperature, water-to-solid ratio, and extraction time significantly affected ARP yield (p < 0.01). The correlation analysis revealed that the experimental data were well-aligned with a quadratic polynomial model, as evidenced by the mathematical regression model's fit. The optimal conditions for maximum ARP yield were 45 °C extraction temperature and 28.47:1 (mL/g) water-to-solid ratio with a 4.60 h extraction time. Extracts from these conditions showed significant activity of promoting cell proliferation from 11.26% (p < 0.001) to 32.47% (p < 0.001) at a dose of 50 µg/mL to 800 µg/mL and increasing glucose consumption to 75.86% (p < 0.001) at 250 µg/mL on HepG2 cells. This study provides a sustainable alternative for the industry since it allowed simplified handling and a specific quantity of ARPs. Furthermore, ARPs might directly stimulate the glucose consumption in the liver and showed no cytotoxicity; therefore, ARPs probably could be taken as a potential natural source of antidiabetic materials.


Assuntos
Glucose , Raízes de Plantas , Polissacarídeos , Água , Humanos , Células Hep G2 , Polissacarídeos/farmacologia , Polissacarídeos/química , Polissacarídeos/isolamento & purificação , Glucose/metabolismo , Raízes de Plantas/química , Água/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Solubilidade , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação
17.
Int J Biol Macromol ; 274(Pt 2): 133433, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38936581

RESUMO

Corn silk is widely used as a traditional Chinese medicine possessing multiple beneficial effects, whose active ingredient is corn silk polysaccharide (CSP). CSP is abundant in corn silk, and has a variety of bioactivities, such as antioxidant, hypoglycemic, hypolipidemic, hepatorenal-protective, antitumor, anti-fatigue, immunomodulating, and anti-ischemia-reperfusion injury effects. Moreover, CSP ameliorates diabetes, diabetes nephropathy, and hyperlipidemia. This review aimed to comprehensively and systematically summarize recent information on the extraction, purification, structural characterization, biological activity, potential mechanism, and toxicity of CSP. Thus, it could provide a reference for the further use of CSP and discuss the future prospects of CSP research and development.


Assuntos
Polissacarídeos , Zea mays , Zea mays/química , Polissacarídeos/farmacologia , Polissacarídeos/química , Polissacarídeos/isolamento & purificação , Humanos , Animais , Antioxidantes/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Medicina Tradicional Chinesa
18.
Biomed Pharmacother ; 177: 117043, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38941896

RESUMO

This study investigated the chemical constituents, antioxidant potential, and in vitro and in silico antidiabetic activity of Gymnema sylvestre. Column chromatography and spectroscopic techniques identified twelve compounds from the methanol extract, including 4 sterols (1-4), 5 triterpenoids (5-9), and 3 flavonoids (10-12). The chemophenetic significance of all compounds was also investigated. The antioxidant capacity of the extract and compounds (1-4) was evaluated using FRAP and DPPH assays. The extract exhibited strong free radical scavenging activity (IC50 = 48.34 µg/mL), while compounds (1-4) displayed varying degrees of efficacy (IC50 = 98.30-286.13 µg/mL). The FRAP assay indicated significant reducing power for both extract and compounds (58.54, 47.61, 56.61, and 49.11 mg Eq.VitC/g for extract and compounds 1 & 2, 3, and 4, respectively). The antidiabetic potential was assessed through α-amylase and α-glucosidase enzyme inhibition assays. The crude extract demonstrated the most potent inhibition (IC50 = 218.46 and 57.42 µg/mL for α-glucosidase and α-amylase respectively) suggesting its potential for managing postprandial hyperglycaemia. In silico studies employed molecular docking and dynamics simulations to elucidate the interactions between identified compounds and α-amylase/α-glucosidase enzymes. The results revealed promising binding affinities between the compounds and target enzymes, with compound 6 demonstrating the highest predicted inhibitory activity with -10 kcal/mol and -9.1 kcal/mol for α-amylase and α-glucosidase, respectively. This study highlights the presence of diverse bioactive compounds in Gymnema sylvestre. The extract exhibits antioxidant properties and inhibits carbohydrate-digesting enzymes, suggesting its potential as a complementary therapeutic approach for managing hyperglycaemia associated with type 2 diabetes.


Assuntos
Antioxidantes , Simulação por Computador , Inibidores de Glicosídeo Hidrolases , Gymnema sylvestre , Hipoglicemiantes , Simulação de Acoplamento Molecular , Extratos Vegetais , Hipoglicemiantes/farmacologia , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/química , Antioxidantes/farmacologia , Antioxidantes/isolamento & purificação , Gymnema sylvestre/química , Extratos Vegetais/farmacologia , Inibidores de Glicosídeo Hidrolases/farmacologia , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo , Metabolismo Secundário
19.
Food Chem ; 457: 140143, 2024 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-38901339

RESUMO

The Hippophae rhamnoides L. pomace was generated in the production process for juice, wine of food industry. To expand the application of pomace, the extraction process optimization, enrichment and identification of triterpene acids were performed in this study. The extraction yield was 14.87% under optimal ultrasound-assisted extraction techniques performed via response surface methodology. The extract was subsequently purified to obtain the triterpenoid acid enrichment fraction (TPF) with the content of 75.23% ± 1.45%. 13 triterpenoid acids were identified via UPLC-Triple-TOF MS/MS and further semi-quantified through comparison with triterpenoid acid standards. TPF exhibited a strong inhibitory effect on α-glucosidase with IC50 value of 5.027 ± 0.375 µg/mL, as determined via enzyme inhibition experiment and molecular docking. Additionally, the TPF significantly reduced postprandial glucose levels, as revealed via carbohydrate tolerance tests, as well as ameliorate serum lipid profiles. Therefore, pomace may be a promising resource of functional food components with therapeutic and commercial values.


Assuntos
Hippophae , Hipoglicemiantes , Extratos Vegetais , Triterpenos , Triterpenos/química , Triterpenos/farmacologia , Triterpenos/isolamento & purificação , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/isolamento & purificação , Hippophae/química , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Animais , alfa-Glucosidases/química , alfa-Glucosidases/metabolismo , Masculino , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Espectrometria de Massas em Tandem , Glicemia/metabolismo , Ratos , Humanos , Simulação de Acoplamento Molecular , Cromatografia Líquida de Alta Pressão
20.
Fitoterapia ; 177: 106099, 2024 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-38945491

RESUMO

This paper explores the potential of flavonoid alkaloids, a unique class of compounds that contain both flavonoid and alkaloid structures, as emerging targets for drug discovery. These compounds exhibit diverse biological activities, such as anti-inflammatory, anti-cancer, and anti-diabetic effects, which are attributed to the combination of different flavonoid scaffolds and alkaloid groups. Flavonoid alkaloids have attracted researchers' attention due to their diverse structures and important bio-activities. Therefore, this review summarizes recent advances in the extraction, purification, structural characterization, synthesis pathways and biological activities of flavonoid alkaloids from natural sources. Finally, the potential prospects and challenges associated with this class of compounds in pharmacological research are discussed along with details of a mechanistic investigation and future clinical applications in this research field.


Assuntos
Alcaloides , Descoberta de Drogas , Flavonoides , Alcaloides/farmacologia , Alcaloides/isolamento & purificação , Alcaloides/química , Estrutura Molecular , Flavonoides/farmacologia , Flavonoides/isolamento & purificação , Flavonoides/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/química , Humanos , Hipoglicemiantes/farmacologia , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação , Animais , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação
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