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1.
J Ethnopharmacol ; 328: 118065, 2024 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-38508432

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Cornel iridoid glycosides (CIG) are extracted from Corni fructus, a herbal medicine used in traditional Chinese medicine to treat diabetes. However, the antidiabetic effects of CIG and the underlying metabolic mechanisms require further exploration. AIM OF THE STUDY: This study aimed to assess the antidiabetic effects and metabolic mechanism of CIG by performing metabolomic analyses of serum and urine samples of rats. MATERIALS AND METHODS: A rat model of type 2 diabetes mellitus (T2DM) was established by administering a low dose of streptozotocin (30 mg/kg) intraperitoneally after 4 weeks of feeding a high-fat diet. The model was evaluated based on several parameters, including fasting blood glucose (FBG), random blood glucose (RBG), urine volume, liver index, body weight, histopathological sections, and serum biochemical parameters. Subsequently, serum and urine metabolomics were analyzed using ultra-high-pressure liquid chromatography coupled with linear ion trap-Orbitrap tandem mass spectrometry (UHPLC-LTQ-Orbitrap-MS). Data were analyzed using unsupervised principal component analysis (PCA) and supervised orthogonal partial least squares discriminant analysis (OPLS-DA). Differential metabolites were examined by the Kyoto Encyclopedia of Genes and Genomes (KEGG) metabolic pathways to explore the underlying mechanisms. RESULTS: After 4 weeks of treatment with different doses of CIG, varying degrees of antidiabetic effects were observed, along with reduced liver and pancreatic injury, and improved oxidative stress levels. Compared with the T2DM group, 19 and 23 differential metabolites were detected in the serum and urine of the CIG treatment group, respectively. The key metabolites involved in pathway regulation include taurine, chenodeoxycholic acid, glycocholic acid, and L-tyrosine in the serum and glycine, hippuric acid, phenylacetylglycine, citric acid, and D-glucuronic acid in the urine, which are related to lipid, amino acid, energy, and carbohydrate metabolism. CONCLUSIONS: This study confirmed the antidiabetic effects of CIG and revealed that CIG effectively controlled metabolic disorders in T2DM rats. This seems to be meaningful for the clinical application of CIG, and can benefit further studies on CIG mechanism.


Assuntos
Diabetes Mellitus Tipo 2 , Medicamentos de Ervas Chinesas , Ratos , Animais , Diabetes Mellitus Tipo 2/tratamento farmacológico , Diabetes Mellitus Tipo 2/metabolismo , Glicosídeos Iridoides/farmacologia , Glicosídeos Iridoides/uso terapêutico , Glicemia , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Hipoglicemiantes/análise , Cromatografia Líquida de Alta Pressão/métodos , Medicamentos de Ervas Chinesas/uso terapêutico , Metabolômica/métodos
2.
J Ethnopharmacol ; 328: 118094, 2024 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-38521433

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Hodgsonia heteroclita has been known as an important traditionally consumed medicinal plant of North-East India known to have antidiabetic properties. This study aims to investigate the effects of the ethanolic fruit extract of Hodgsonia heteroclita against hyperglycemia and hyperlipidemia by using streptozotocin (STZ) treated diabetic mice. MATERIALS AND METHODS: The fruits of H. heteroclita were collected from the various parts of Kokrajhar district, Assam India (Geographic coordinates: 26°24'3.85″ N 90°16'22.30″ E). Basic morphological evaluations were carried out by the Botanical Survey of India, Eastern circle, Shillong, who also certified and identified the plant. Hexane, chloroform, and ethanolic extracts of the fruit of H. heteroclita were investigated for α-amylase inhibition assay as a rapid screening tool for examining anti-diabetic activity. The efficacy of ethanolic extract at a dose of 100, 200, and 300 mg/kg body weight was tested for 21 days in STZ-induced diabetic mice. The body weight, fasting plasma glucose and serum lipids, and hepatic glycogen levels were measured in experimental animals to examine the antihyperglycemic and antihyperlipidemic efficacy of the extract. Both HPTLC and LC-MS analysis was performed to examine the phyotochemicals present in the ethanolic extract of H. heteroclita. RESULTS: It has been observed that treatment with the ethanolic extract dose-dependently reduced the plasma glucose levels, total cholesterol, low density lipoprotein-cholesterol, very low-density lipoprotein-cholesterol, triglyceride, and increased the body weight, liver glycogens and high-density lipoprotein-cholesterol in STZ treated diabetic mice. HPTLC demonstrated the presence of triterpene compounds and LC-MS analysis revealed the presence Cucurbitacin I, Cucurbitacin E, and Kuguacin G as the triterpene phytoconstituents. CONCLUSION: The present study demonstrated that ethanolic fruit extract of H. heteroclita improved both glycemic and lipid parameters in mice model of diabetes.


Assuntos
Cucurbitaceae , Diabetes Mellitus Experimental , Triterpenos , Camundongos , Animais , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Hipoglicemiantes/análise , Hipolipemiantes/farmacologia , Hipolipemiantes/uso terapêutico , Hipolipemiantes/análise , Glicemia , Frutas/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Extratos Vegetais/química , Diabetes Mellitus Experimental/tratamento farmacológico , Etanol/química , Glicogênio Hepático , Colesterol/farmacologia , Peso Corporal , Triterpenos/farmacologia , Estreptozocina/farmacologia
3.
Spectrochim Acta A Mol Biomol Spectrosc ; 309: 123844, 2024 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-38198995

RESUMO

Metformin is considered as type 2 diabetes first line treatment according to American Diabetes Association and European Association. But, in some cases, di- or tri - therapy should be prescribed for glycemic management, prevention of the maximum dose side effects and induced effectiveness. Co-administration of Linagliptin with metformin has many benefits on diabetic patients such as decrease the possibility of hypoglycemia. For the first time, novel and reliable techniques were developed and verified for the concurrent quantification of metformin hydrochloride and linagliptin, while accounting for the existence of metformin toxic impurity 1-cyanoguanidine in their pure and dosage forms. Method (A) utilizes the zero-order spectrophotometric approach to quantitatively determine the concentration of linagliptin. The measurements are performed at a wavelength of 295 nm. The double divisor derivative ratio spectrophotometric method is used in Method (B) to measure the amounts of metformin and cyanoguanidine at 252 nm and 219 nm wavelengths, respectively. The spectrophotometric method (C) for determining metformin and cyanoguanidine at 252 nm and 223 nm, respectively, is based on the single divisor derivative ratio-zero crossing technique. The obtained findings were subjected to statistical comparison with the reported method, revealing no statistically significant differences. The Green Analytical Procedure Index (GAPI) and Analytical GREEnness Metric approach (AGREE) determined that these approaches had a high degree of environmental friendliness. Additionally, the proposed strategy was deemed to be practical according to the Blue Applicability Grade Index (BAGI) assessment tool.


Assuntos
Diabetes Mellitus Tipo 2 , Guanidinas , Metformina , Humanos , Metformina/análise , Linagliptina/análise , Hipoglicemiantes/análise , Diabetes Mellitus Tipo 2/tratamento farmacológico
4.
J AOAC Int ; 107(1): 40-45, 2024 Jan 04.
Artigo em Inglês | MEDLINE | ID: mdl-37824214

RESUMO

BACKGROUND: In 2019, the U.S. Food and Drug Administration approved a brand-new combination of linagliptin and empagliflozin in a formulation called Glyxambi® tablets for managing type 2 diabetes mellitus. Nowadays, spectrophotometric techniques occupy the first place among their peers in terms of ease of application, friendliness to the environment, and low costs. OBJECTIVE: This research discusses the development of two very simple spectrophotometric protocols based on zero-order spectra for the determination of linagliptin and empagliflozin. METHODS: The developed protocols were the induced dual-wavelength and absorption correction protocols. Linagliptin could be determined directly at 305 nm, at which the empagliflozin spectrum was zero-crossing. Empagliflozin was determined using the two developed protocols. The induced dual-wavelength technique was developed by calculating the equality factor of linagliptin to cancel its interference. The absorption correction technique was developed by measuring the correction absorption factor. RESULTS: The concentration ranges of linagliptin and empagliflozin were 1-10 µg/mL and 3-30 µg/mL, respectively. Excellent recovery results were found in bulk, dosage form, and synthetic mixtures. Low LOD and LOQ values were obtained, indicating the high sensitivity of the protocols. The statistical Student's t-test was performed to compare the results of the applied and reported protocols, indicating no difference between them. CONCLUSION: The proposed protocols have the advantages of being straightforward, affordable, and requiring no sophisticated manipulations, just simple mathematical calculations. The proposed protocols are acceptable for routine usage in QC laboratories and in future research applications. HIGHLIGHTS: Two novel univariate methods were developed for quantitative analysis of linagliptin and empagliflozin in their pharmaceutical and laboratory mixtures, and produced satisfactory results.


Assuntos
Diabetes Mellitus Tipo 2 , Hipoglicemiantes , Humanos , Hipoglicemiantes/análise , Linagliptina/análise , Diabetes Mellitus Tipo 2/tratamento farmacológico , Glucosídeos/análise , Compostos Benzidrílicos/análise
5.
Molecules ; 28(22)2023 Nov 13.
Artigo em Inglês | MEDLINE | ID: mdl-38005279

RESUMO

Salix babylonica L. is a species of willow tree that is widely cultivated worldwide as an ornamental plant, but its medicinal resources have not yet been reasonably developed or utilized. Herein, we extracted and purified the total flavonoids from willow buds (PTFW) for component analysis in order to evaluate their in vitro anti-tumor and hypoglycemic activities. Through Q-Orbitrap LC-MS/MS analysis, a total of 10 flavonoid compounds were identified (including flavones, flavan-3-ols, and flavonols). The inhibitory effects of PTFW on the proliferation of cervical cancer HeLa cells, colon cancer HT-29 cells, and breast cancer MCF7 cells were evaluated using an MTT assay. Moreover, the hypoglycemic activity of PTFW was determined by investigating the inhibitory effects of PTFW on α-amylase and α-glucosidase. The results indicated that PTFW significantly suppressed the proliferation of HeLa cells, HT-29 cells, and MCF7 cells, with IC50 values of 1.432, 0.3476, and 2.297 mg/mL, respectively. PTFW, at different concentrations, had certain inhibitory effects on α-amylase and α-glucosidase, with IC50 values of 2.94 mg/mL and 1.87 mg/mL, respectively. In conclusion, PTFW at different doses exhibits anti-proliferation effects on all three types of cancer cells, particularly on HT-29 cells, and also shows significant hypoglycemic effects. Willow buds have the potential to be used in functional food and pharmaceutical industries.


Assuntos
Flavonoides , Salix , Humanos , Flavonoides/farmacologia , Flavonoides/análise , Hipoglicemiantes/farmacologia , Hipoglicemiantes/análise , Extratos Vegetais/farmacologia , Extratos Vegetais/análise , Cromatografia Líquida , Células HeLa , alfa-Glucosidases , Espectrometria de Massas em Tandem , alfa-Amilases
6.
PLoS One ; 18(11): e0287894, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37917721

RESUMO

Polygonatum cyrtonema is a perennial plant, and it has long been used in traditional Chinese medicine for food and medicine. The medicinal part of P.cyrtonema is the rhizome; however, the aerial part has not been studied. To understand the effect of the topping of aerial parts on the yield and chemical components of rhizomes, as well as the chemical constituents, antioxidant, and in vitro hypoglycemic activities of the aerial stem, leave, and flower parts of P.cyrtonema, the present study was conducted. The results showed that compared to the control (CK) treatment, the topping of the aerial part increased rhizome weight gain coefficient (3.43) and the total saponin content (37.60 mg/g) significantly (P<0.01) than the CK treatment. The contents of total phenols and total flavonoids in PCL and PCF were significantly (P<0.01) higher than those in rhizomes; however, the polysaccharide content (10.47%) in PCR (whole rhizome) was higher than that in PCS (3.65%), PCL (5.99%), and PCF (4.76%) content. The protein and amino acid contents in PCS, PCL, and PCF were higher than those in rhizomes. The protein and amino acid contents in PCS, PCL, and PCF were higher than those in rhizomes. PCS, PCL, and PCF showed strong antioxidant activity (DPPH, ·OH, ABTS, and FRAP), which were better than traditional medicinal parts (the rhizome).In vitro hypoglycemic results showed that PCS, PCL, and PCF had certain inhibitory activities on α-amylase and α-glucosidase (66.25% and 52.81%), which were close to the hypoglycemic activity of rhizomes (67.96% and 52.22%). The leaf extracts also showed better inhibitory activity. To sum up, the topping measures can improve yield and total saponin content of the rhizomes from P.cyrtonema, which can be applied to improve production. The stems, leaves, and flowers had a much stronger antioxidant and hypoglycemic activities and higher the total polyphenols, flavonoids, proteins, and amino acid content. Therefore, stems, leaves, and flowers of Polygonatum can be fully developed according to different needs. they are typically used in animal feed, food storage and cosmetics.


Assuntos
Polygonatum , Saponinas , Antioxidantes/farmacologia , alfa-Glucosidases , Rizoma/química , alfa-Amilases , Aminoácidos/análise , Flavonoides/análise , Saponinas/análise , Hipoglicemiantes/farmacologia , Hipoglicemiantes/análise
7.
J Sep Sci ; 46(19): e2300267, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-37485588

RESUMO

Molecular modeling is the science of representing molecular structures numerically and simulating their behavior with the equations of quantum and classical physics. Coupling molecular modeling and simulation with chromatographic resolution for pharmaceutical products constitutes a new technique in pharmaceutical analysis. An innovative high-performance liquid chromatographic (HPLC) methodology was developed for the quantification of metformin hydrochloride (MET), empagliflozin (EMP), and canagliflozin (CAN) in bulk, laboratory-developed combinations, pharmaceutical tablets, and in the presence of melamine. Chromatographic separation was accomplished using a Symmetry column with 0.03 M potassium dihydrogen phosphate buffer and 0.02 M heptane sulphonic acid: acetonitrile as the mobile phase. Molecular modeling using molecular operating environment software was applied to properly select the stationary phase suitable for the developed HPLC method. Additionally, molecular modeling estimates and validates binding between the studied analytes and the stationary phase to clarify and explain the chromatographic separation and elution order. In accordance with the International Conference of Harmonization recommendations, the method was validated in terms of linearity, accuracy, precision, and selectivity. The linearity ranges (µg/ml) were 200-1500 (MET), 2-15 (EMP), and 20-150 (CAN) and the limit of detection values were in the ranges of 0.17-54.58 µg/ml. Analysis of pharmaceutical tablets using the suggested approach yielded satisfactory outcomes. As a result, it might be used in quality control laboratories to analyze the aforementioned medications.


Assuntos
Metformina , Inibidores do Transportador 2 de Sódio-Glicose , Hipoglicemiantes/análise , Metformina/análise , Cromatografia Líquida de Alta Pressão/métodos , Comprimidos , Canagliflozina
8.
Environ Toxicol Chem ; 42(8): 1709-1720, 2023 08.
Artigo em Inglês | MEDLINE | ID: mdl-37283207

RESUMO

Metformin, used to treat Type 2 diabetes, is the active ingredient of one of the most prescribed drugs in the world, with over 120 million yearly prescriptions globally. In wastewater-treatment plants (WWTPs), metformin can undergo microbial transformation to form the product guanylurea, which could have toxicological relevance in the environment. Surface water samples from 2018 to 2020 and sediment samples from 2020 were collected from six mixed-use watersheds in Quebec and Ontario, Canada, and analyzed to determine the metformin and guanylurea concentrations at each site. Metformin and guanylurea were present above their limits of quantification in 51.0% and 50.7% of all water samples and in 64% and 21% of all sediment samples, respectively. In surface water, guanylurea was often present at higher concentrations than metformin, while the inverse was true in sediment, with metformin frequently detected at higher concentrations than guanylurea. In addition, at all sites influenced solely by agriculture, concentrations of metformin and guanylurea were <1 µg/L in surface water, suggesting that agriculture is not a significant source of these compounds in the investigated watersheds. These data suggest that WWTPs and potentially septic system leaks are the most likely sources of the compounds in the environment. Guanylurea was detected at many of these sites above environmental concentrations of concern, where critical processes in fish may be affected. Due to the scarcity of available ecotoxicological data and the prominence of guanylurea across all sample sites, there is a need to perform more toxicological investigations of this transformation product and revisit regulations. The present study will help provide toxicologists with environmentally relevant concentration ranges in Canada. Environ Toxicol Chem 2023;42:1709-1720. © 2023 His Majesty the King in Right of Canada and The Authors. Environmental Toxicology and Chemistry published by Wiley Periodicals LLC on behalf of SETAC. Reproduced with the permission of the Minister of Agriculture and Agri-Food Canada.


Assuntos
Diabetes Mellitus Tipo 2 , Metformina , Poluentes Químicos da Água , Animais , Metformina/química , Hipoglicemiantes/análise , Quebeque , Água , Ontário , Poluentes Químicos da Água/análise
9.
Molecules ; 28(9)2023 May 04.
Artigo em Inglês | MEDLINE | ID: mdl-37175290

RESUMO

Ultrasound-microwave combined extraction (UMCE), gradient ethanol precipitation, chemical characterization, and antioxidant and hypoglycemic activities of Lycium barbarum leaf polysaccharides (LLP) were systematically studied. The optimal conditions for UMCE of LLP achieved by response surface method (RSM) were as follows: microwave time of 16 min, ultrasonic time of 20 min, particle size of 100 mesh, and ratio of liquid to solid of 55:1. Three novel polysaccharide fractions (LLP30, LLP50, LLP70) with different molecular weights were obtained by gradient ethanol precipitation. Polysaccharide samples exhibited scavenging capacities against ABTS and DPPH radicals and inhibitory activities against α-glucosidase and α-amylase. Among the three fractions, LLP30 possessed relatively high antioxidant and hypoglycemic activities in vitro, which showed a potential for becoming a nutraceutical or a phytopharmaceutical for prevention and treatment of hyperglycemia or diabetes.


Assuntos
Antioxidantes , Lycium , Antioxidantes/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/análise , Lycium/química , Micro-Ondas , Polissacarídeos/química , Folhas de Planta/química , Etanol/análise
10.
Int J Mol Sci ; 24(10)2023 May 16.
Artigo em Inglês | MEDLINE | ID: mdl-37240175

RESUMO

Prunus lusitanica L. is a shrub belonging to the genus Prunus L. (Rosaceae family) that produces small fruits with none known application. Thus, the aim of this study was to determine the phenolic profile and some health-promoting activities of hydroethanolic (HE) extracts obtained from P. lusitanica fruits, harvested from three different locations. Qualitative and quantitative analysis of extracts was performed using HPLC/DAD-ESI-MS and antioxidant activity was assessed by in vitro methods. Antiproliferative/cytotoxic activity was determined on Caco-2, HepG2, and RAW 264.7 cells, anti-inflammatory activity was assessed using lipopolysaccharide (LPS)-stimulated RAW 264.7 cells, and the antidiabetic, antiaging, and neurobiological action of extracts was determined in vitro by assessing their inhibitory effect against the activity of α-amylase, α-glucosidase, elastase, tyrosinase, and acetylcholinesterase (AChE). Results showed that P. lusitanica fruit HE extracts from the three different locations showed identical phytochemical profile and bioactivities, although small differences were observed regarding the quantities of some compounds. Extracts of P. lusitanica fruits contain high levels in total phenolic compounds, namely, hydroxycinnamic acids, as well as flavan-3-ols and anthocyanins, primarily cyanidin-3-(6-trans-p-coumaroyl)glucoside. P. lusitanica fruit extracts have a low cytotoxic/antiproliferative effect, with the lowest IC50 value obtained in HepG2 cells (352.6 ± 10.0 µg/mL, at 48 h exposure), but high anti-inflammatory activity (50-60% NO release inhibition, at 100 µg/mL extract) and neuroprotective potential (35-39% AChE inhibition, at 1 mg/mL), and moderate antiaging (9-15% tyrosinase inhibition, at 1 mg/mL) and antidiabetic (9-15% α-glucosidase inhibition, at 1 mg/mL) effects. The bioactive molecules present in the fruits of P. lusitanica deserve to be further explored for the development of new drugs of interest to the pharmaceutical and cosmetic industry.


Assuntos
Diabetes Mellitus , Doenças Neurodegenerativas , Prunus , Humanos , Prunus/química , Frutas/química , Antocianinas/análise , Monofenol Mono-Oxigenase , Doenças Neurodegenerativas/tratamento farmacológico , Acetilcolinesterase , Células CACO-2 , alfa-Glucosidases , Extratos Vegetais/química , Antioxidantes/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/análise , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/análise , Fenóis/farmacologia , Inflamação/tratamento farmacológico
11.
Food Chem ; 422: 136198, 2023 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-37121210

RESUMO

Isoflavones are important chemical components in Pueraria species with various biological activities. This study proposed an integrated strategy combining feature-based molecular networking (FBMN), chemometrics and activity evaluation for isoflavone analysis in the roots of P. lobate (PLR) and P. thomsonii (PTR). Based on the strategy, a total of 68 isoflavones were annotated in the two Pueraria species, and 11 significant difference isoflavones between PLR and PTR were identified by chemometric methods. Additionally, the correlation coefficient between the characteristic isoflavones and hypoglycemic activity were calculated, and 7 isoflavones were further confirmed as bioactive marker compounds. This approach provided guidance for the discovery of active markers among different products.


Assuntos
Isoflavonas , Pueraria , Isoflavonas/análise , Pueraria/química , Hipoglicemiantes/análise , Raízes de Plantas/química
12.
Molecules ; 28(8)2023 Apr 08.
Artigo em Inglês | MEDLINE | ID: mdl-37110550

RESUMO

Marigolds (Tagetes spp.) are major sources of bioactive compounds. The flowers are used to treat a variety of illnesses and have both antioxidant and antidiabetic effects. However, marigolds exhibit a wide range of genetic variations. Because of this, both the bioactive compounds and biological activities of the plants differ between cultivars. In the present study, nine marigold cultivars grown in Thailand were evaluated for their bioactive compound content, as well as for their antioxidant and antidiabetic activities, using spectrophotometric methods. The results showed that the Sara Orange cultivar possessed the highest total carotenoid content (431.63 mg/100 g). However, Nata 001 (NT1) had the highest amount of total phenolic compounds (161.17 mg GAE/g), flavonoids (20.05 mg QE/g), and lutein (7.83 mg/g), respectively. NT1 exhibited strong activities against the DPPH radical and ABTS radical cation, and had the highest FRAP value as well. Moreover, NT1 demonstrated the most significant (p < 0.05) α-amylase and α-glucosidase inhibitory effects (IC50 values of 2.57 and 3.12 mg/mL, respectively). The nine marigold cultivars had reasonable correlations between lutein content and the capacity to inhibit α-amylase and α-glucosidase activities. Hence, NT1 may be a good source of lutein; it may also be beneficial in both functional food production and medical applications.


Assuntos
Calendula , Tagetes , Antioxidantes/química , Luteína/química , Tagetes/química , alfa-Glucosidases , alfa-Amilases , Extratos Vegetais/química , Hipoglicemiantes/análise , Flores/química
13.
Food Res Int ; 164: 112382, 2023 02.
Artigo em Inglês | MEDLINE | ID: mdl-36737967

RESUMO

The by-product of Chinese rubing cheese is rich in whey protein. Whey hydrolysates exhibit good hypoglycemic activity, but which specific peptide components are responsible for this effect have not yet been investigated. Herein, the α-glucosidase inhibitory activity of the ultrafiltered fraction (<3 kDa) of rubing cheese whey hydrolysates was evaluated with the inhibition rate of 37.89 %. In addition, peptide identification was conducted using LC-MS/MS, and three peptides YPVEPF, VPYPQ, and LPYPY were identified. Among these, YPVEPF had higher α-glucosidase inhibitory activity (IC50 = 3.52 mg/mL) and interacted with α-glucosidase via hydrogen bonding and hydrophobic forces. YPVEPF was characterized as an amphipathic peptide rich in antiparallel (50.50 %) and random coil (35.20 %) structures, as well as showed good tolerance to gastrointestinal digestion and incubation under the temperature range of 20-80 °C. Notably, YPVEPF activity increased in the presence of Al3+ and Fe3+, as well as within the pH range of 2.0-6.0. Furthermore, YPVEPF had negligible hemolytic activity at a concentration of 1.0 mg/mL, no toxicity at concentrations below 0.5 mg/mL, and significantly promoted glucose consumption in HepG2 cells (p < 0.0001). Collectively, these findings indicate the potential of YPVEPF to be used as a novel hypoglycemic peptide in functional foods.


Assuntos
Queijo , Soro do Leite , Proteínas do Soro do Leite/química , Soro do Leite/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/análise , alfa-Glucosidases/metabolismo , Queijo/análise , Cromatografia Líquida , Espectrometria de Massas em Tandem , Peptídeos/química
14.
Nat Prod Res ; 37(24): 4251-4255, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36775581

RESUMO

Antidiabetic activity of methanolic extract, petroleum ether, ethyl acetate and n-butanol fractions of Ipomoea cairica (L.) Sweet leaves was performed in-vitro using α-glucosidase and α-amylase inhibition methods. Phytochemical study of the ethyl acetate fraction which possessed the highest antidiabetic activity led to isolation of five flavonoids for the first time from this plant, including two rare flavonoid sulphates, ombuin-3-sulphate [1] and rhamnetin-3-sulphate [2] and three flavonoid glycosides, kaempferol 7-O-α-L-rhamnopyranoside [3], kaempferol 3,7-di-O-α-L-rhamnopyranoside [4] and quercetin 3-O-α-L-arabinopyranoside [5]. The 1H and 13C NMR of 1 and 13C NMR of 2, were reported here for the first time. Compounds [1-4] showed a concentration-dependent in-vitro inhibitory activity against α-glucosidase and α-amylase. Furthermore, in-silico study predicted that compounds (1-5) showed good interactions with α-glucosidase, α-amylase, and protein tyrosine phosphatase 1b.


Assuntos
Flavonoides , Ipomoea , Flavonoides/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/análise , Quempferóis/farmacologia , Quempferóis/análise , Ipomoea/química , alfa-Glucosidases , Glicosídeos/química , Folhas de Planta/química , Extratos Vegetais/química , Sulfatos , alfa-Amilases/análise
15.
Food Chem ; 411: 135423, 2023 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-36652884

RESUMO

Psidium guajava L. is one of the most pivotal members belong to the Myrtaceae family, and it is an important tropical fruit with highly nutritional, healthy, and pharmacological values prevailing in worldwide for decades. The polysaccharides of P. guajava (PGPs) are served as one of the most active constituents, which possess a variety of biofunctionalities including anti-inflammatory, antidiarrheic, antihypertension, and antidiabetic properties. Hence, a systematic review aimed to comprehensively summarize the recent research advances of PGPs is necessary for facilitating their better understanding. The present review discussed current research progress on the PGPs, including extraction and purification methods, structural features, biological activities, and potential pharmacological mechanism. In addition, this review may also provide some valuable insights for further development and potential value in affording functionally useful agents in food industry or therapeutically effective medicine in the fields of P. guajava polysaccharides.


Assuntos
Myrtaceae , Psidium , Psidium/química , Extratos Vegetais/farmacologia , Extratos Vegetais/análise , Hipoglicemiantes/análise , Folhas de Planta/química , Polissacarídeos/farmacologia , Polissacarídeos/análise
16.
Nat Prod Res ; 37(4): 608-612, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-35428410

RESUMO

In this study, phytochemical profiling, and antidiabetic, antitumoral and cytotoxic potential of aqueous extracts of leaves of red variety of Psidium cattleianum Afzel. ex Sabine were investigated. The extracts were obtained using a cellulase complex. The total phenolic compounds (TPC) were determined, and the individual phenolic compounds were quantified by HPLC-ESI-MS/MS. For the TPC, the amounts varied from 85.91 to 106.33 mg EAG g-1. Eighteen compounds have been identified. The compounds with the highest concentrations were gallic acid, quercetin and protocatechuic acid. Antidiabetic activity was obtained through α-amylase and α-glucosidase inhibition tests. The extract inhibited 17.94% of α-amylase activity and 73.34% of α-glucosidase activity. The antitumoral activity in cells of cutaneous melanoma (SK-MEL-28) and the cytotoxic activity was determined in peripheral blood mononuclear cells (PBMC). The cellular migration was determined for cells SK-MEL-28. Antitumoral effects on cells SK-MEL-28 were observed and the absence of cytotoxicity on the PBMCs.


Assuntos
Antineoplásicos , Melanoma , Psidium , Neoplasias Cutâneas , Antioxidantes/farmacologia , Psidium/química , Leucócitos Mononucleares , Melanoma/tratamento farmacológico , Espectrometria de Massas em Tandem , Hipoglicemiantes/farmacologia , Hipoglicemiantes/análise , alfa-Glucosidases , Fenóis/análise , Antineoplásicos/farmacologia , Antineoplásicos/análise , Extratos Vegetais/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/análise , Folhas de Planta/química , alfa-Amilases/análise
17.
Crit Rev Food Sci Nutr ; 63(23): 6344-6378, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-35144492

RESUMO

Artocarpus heterophyllus Lam. (Family Moraceae), is a tropical tree, native to India and common in Asia, Africa, and several regions in South America. The fruit is commonly known as jackfruit which is one of the largest edible fruits in the world. Jackfruits comprises a wide range of nutrients, including minerals, carbohydrates, volatile compounds, proteins, and vitamins. The fruit, bark, leaves, and roots are endowed with therapeutic attributes and are utilized in the many traditional medicinal systems for the management of various ailments. Fruit and seeds are commonly used to prepare various food items, including sauce, ice creams, jams, jellies, and marmalades. Due to unique texture, jackfruit is becoming a popular meat substitute. Based on preclinical studies, jackfruit exhibits antimicrobial, antioxidant, anti-melanin, antidiabetic, anti-inflammatory, immunomodulatory, antiviral, anthelmintic, wound-healing, and antineoplastic activities. Clinical studies reveal that the leaves possess antidiabetic action in healthy and insulin-independent diabetic individuals. Despite numerous health benefits, regrettably, jackfruit has not been properly utilized in a marketable scale in areas where it is produced. This review delivers an updated, comprehensive, and critical evaluation on the nutritional value, phytochemical profiling, pharmacological attributes and underlying mechanisms of action to explore the full potential of jackfruit in health and disease.


Assuntos
Artocarpus , Humanos , Artocarpus/química , Frutas/química , Sementes , Antioxidantes/análise , Hipoglicemiantes/análise
18.
Nat Prod Res ; 37(4): 681-686, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-35608174

RESUMO

In this contribution, ethanolic extracts of Cuminum cyminum (C. cyminum) seeds were evaluated in terms of phytochemical content, total phenol and flavonoid contents. As far as the analytical techniques are concerned, UV-Vis, FTIR, HPLC, NMR (1H and 13C) and ESI-MS were performed. The binding capacity of five different antidiabetic enzymes was tested by in silico molecular docking studies. The HPLC, UV-Vis, FTIR, NMR and ESI-MS data highlighted the presence of seven biologically active molecules e.g. α-pinene, ß-pinene, Δ3-carene, ρ-cymene, α-terpineol, cuminaldehyde and linalool. The results coming from the in silico molecular docking studies showed that such phytochemicals present in the cumin seed extracts play an important role in the activity of key enzymes involved in carbohydrate metabolism. Therefore, C. cyminum is proven to be useful for the treatment of diabetes mellitus and its major secondary complications.


Assuntos
Cuminum , Hipoglicemiantes , Hipoglicemiantes/farmacologia , Hipoglicemiantes/análise , Cuminum/química , Simulação de Acoplamento Molecular , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/análise , Extratos Vegetais/química , Sementes/química
19.
Nat Prod Res ; 37(6): 1002-1005, 2023 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-35793448

RESUMO

Dracocephalum heterophyllum Benth (Lamiaceae) is a wild herb that possesses a number of biologically active phytomolecules. The aim of this study was to investigate comparative essential oils (EOs) composition and biological (antimicrobial and anti-diabetic) activities of D. heterophyllum from higher altitudes. Gas chromatography-mass spectrometry (GC/MS) and gas chromatography-flame ionisation detector (GC-FID) were carried out for the identification and quantification of EOs components. The hydrodistillation of fresh aerial part of D. heterophyllum gave (0.1-0.8) % w/v EOs yield. Altogether, twenty-seven constituents were identified in the among samples representing (91.0-98.2) % of the EOs composition. The ß-citronellol (31.5-83.7) % contributes major constituent in all samples. The in vitro antimicrobial potential of EOs was examined against six human pathogenic bacterial and two phytopathogens fungal strains. Anti-diabetic activity exhibits excellent α-amylase and better α-glucosidase enzymes inhibitor properties.


Assuntos
Anti-Infecciosos , Lamiaceae , Óleos Voláteis , Humanos , Óleos Voláteis/química , Cromatografia Gasosa-Espectrometria de Massas , Hipoglicemiantes/farmacologia , Hipoglicemiantes/análise , Lamiaceae/química , Anti-Infecciosos/química
20.
J Chromatogr Sci ; 61(8): 705-716, 2023 Oct 03.
Artigo em Inglês | MEDLINE | ID: mdl-35876214

RESUMO

In patients with Type 2 diabetes, a combination of Alogliptin and Pioglitazone medications, together with diet and physical activity, are used to improve glycemic control. Eco-friendly, cost-effective, and precise stability-indicating RP-HPLC method was developed and validated for the identification and quantification of Alogliptin and Pioglitazone in their tablet dosage form, as well as implementation to in vitro dissolution studies and uniformity of dosage unit. Isocratic separation is conducted at ambient temperature on the InertSustain C18 Analytical Column (150 × 4.6 mm, 5 µm) using mobile phase comprising 50 mM of ammonium dihydrogen phosphate and 5.0 mM of heptane sulfonic acid:acetonitrile (45:55, v/v) at a flow rate of 1.3 mL/minute. Calibration curves are conducted in the linearity range of 1-40 µg/mL of Alogliptin and 2.5-75 µg/mL of Pioglitazone with a correlation value >0.9995 and satisfactory recovery findings between 99 and 100%. The degraded samples are analyzed under relevant stress conditions as acidity, alkalinity, thermal and oxidation. The active components in finished products were subjected to a content uniformity test, which showed that they achieved the declared claim's acceptance standards (85-115%). Comparative in vitro dissolution studies are performed for generic products Inhibazone 12.5/30 mg FCT and Inhibazone 25/15 mg FCT against innovator products Oseni 12.5/30 mg FCT and Oseni 25/15 mg FCT at suitable FDA dissolution medium and different USP dissolution media and the results are similar. The metrics of the designed method were assessed according to ICH requirements, and all metrics, such as system suitability, linearity, recovery, robustness, LOD, LOQ, specificity and precision, were found to be within required tolerances and no overlapping was found for degradation peaks. Thence, the method can be used in quality control for the analysis of raw material, bulk, finish and stability.


Assuntos
Diabetes Mellitus Tipo 2 , Hipoglicemiantes , Humanos , Estabilidade de Medicamentos , Hipoglicemiantes/análise , Pioglitazona , Solubilidade , Comprimidos
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