Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 20 de 1.514
Filter
1.
J Oleo Sci ; 73(5): 717-727, 2024.
Article in English | MEDLINE | ID: mdl-38692894

ABSTRACT

The anti-diabetic effect of Ficus carica (Fig) seed oil was investigated. 4 groups with 6 rats in each group were used in the experiment as control, diabetes (45 mg/kg streptozotocin), fig seed oil (FSO) (6 mL/ kg/day/rat by gavage) and diabetes+FSO groups. Glucose, urea, creatinine, ALT, AST, GSH, AOPP and MDA analyses were done. Pancreatic tissues were examined histopathologically. When fig seed oil was given to the diabetic group, the blood glucose level decreased. In the diabetes+FSO group, serum urea, creatinine, AOPP, MDA levels and ALT and AST activities decreased statistically significantly compared to the diabetes group, while GSH levels increased significantly, histopathological, immunohistochemical, and immunofluorescent improvements were observed. It has been shown for the first time that FSO has positive effects on blood glucose level and pancreatic health. It can be said that the protective effect of fig seed oil on tissues may be due to its antioxidant activity.


Subject(s)
Antioxidants , Blood Glucose , Diabetes Mellitus, Experimental , Ficus , Hypoglycemic Agents , Pancreas , Plant Oils , Seeds , Streptozocin , Animals , Ficus/chemistry , Diabetes Mellitus, Experimental/drug therapy , Plant Oils/pharmacology , Plant Oils/isolation & purification , Seeds/chemistry , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/isolation & purification , Blood Glucose/metabolism , Male , Pancreas/drug effects , Pancreas/pathology , Pancreas/metabolism , Antioxidants/pharmacology , Rats , Rats, Wistar , Creatinine/blood
2.
Pak J Pharm Sci ; 37(1): 71-78, 2024 Jan.
Article in English | MEDLINE | ID: mdl-38741402

ABSTRACT

Diabetes mellitus, recognized by elevated glucose level in the body fluids is commonly caused by less insulin production or its action. To overcome the complications of diabetes, chemical drugs are never preferred over herbal medicines. Present study was designed to find out the anti-diabetic and health-promoting effects of ethanolic leaf extracts of Cucumis melo and Citrullus lanatus in induced-diabetic albino rats. Thirty male albino rats were bought from the animal house of the university and divided randomly into five feeding groups (n=6). Diabetes was induced in rats of groups A, B, C & D by a single dose of intra-peritoneal injection of streptozotocin (55 mg/Kg), whereas, the rats of group E were considered as control. The rats of groups A, B & C were fed basal diet supplemented with plant extracts (150mg/Kg body weight), whereas; only basal diet was offered to rats of groups D & E. After 28 days of the experiment, blood was collected for biochemical analysis. Results revealed that body weight, glucose, AST, ALB, GGT, HDL, cholesterol, triglyceride, urea and creatinine level differed significantly among treatment groups. It was therefore concluded that ethanolic leaf extracts of Cucumis melo and Citrullus lanatus can be used separately or in combination for the management of diabetes.


Subject(s)
Blood Glucose , Citrullus , Cucumis melo , Diabetes Mellitus, Experimental , Hypoglycemic Agents , Lipids , Plant Extracts , Animals , Diabetes Mellitus, Experimental/drug therapy , Diabetes Mellitus, Experimental/blood , Plant Extracts/pharmacology , Cucumis melo/chemistry , Male , Blood Glucose/drug effects , Blood Glucose/metabolism , Citrullus/chemistry , Rats , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/isolation & purification , Lipids/blood , Plant Leaves/chemistry , Kidney/drug effects , Kidney/metabolism , Liver/drug effects , Liver/metabolism , Streptozocin
3.
Pak J Pharm Sci ; 37(1): 163-171, 2024 Jan.
Article in English | MEDLINE | ID: mdl-38741413

ABSTRACT

Medicinal plants contain a wide variety of bioactive phytoconstituents which can serve as new therapeutic agents for several diseases. This study examines the antidiabetic potential of Aitchisonia rosea in alloxan-induced diabetic rats and identifies its bioactive phytoconstituents using GC-MS. In vitro, antidiabetic potential was established using the α-amylase inhibition assay. In vivo, antidiabetic potential was investigated by employing the oral glucose tolerance test (OGTT). GC-MS analysis was used to identify the bioactive phytoconstituents. The in vitro and in vivo tests showed that the aqueous extract of A. rosea possesses better antidiabetic potential. The α-amylase inhibition assay highlighted an IC50 value of 134.87µg/ml. In an oral glucose tolerance test, rats given an aqueous A. rosea extract significantly lowered their blood sugar levels significant reduction in the blood glucose concentration was observed in the oral glucose tolerance test in rats treated with the aqueous A. rosea extract. GC-MS investigation revealed many phytoconstituents, with serverogenin acetate and cycloheptasiloxane tetradecamethyl being important antidiabetic agents. This study found anti-diabetic properties in A. rosea extract. The phytochemical and GC-MS investigation also found serverogenin acetate and cycloheptasiloxane tetradecamethyl, which could be used to develop new antidiabetic drugs.


Subject(s)
Blood Glucose , Diabetes Mellitus, Experimental , Gas Chromatography-Mass Spectrometry , Hypoglycemic Agents , Plant Components, Aerial , Plant Extracts , Animals , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/isolation & purification , Hypoglycemic Agents/chemistry , Plant Extracts/pharmacology , Plant Extracts/chemistry , Diabetes Mellitus, Experimental/drug therapy , Diabetes Mellitus, Experimental/blood , Diabetes Mellitus, Experimental/chemically induced , Plant Components, Aerial/chemistry , Male , Blood Glucose/drug effects , Rats , Glucose Tolerance Test , alpha-Amylases/antagonists & inhibitors , alpha-Amylases/metabolism , Rats, Wistar , Phytochemicals/pharmacology , Phytochemicals/analysis , Alloxan
4.
Pak J Pharm Sci ; 37(2): 315-320, 2024 Mar.
Article in English | MEDLINE | ID: mdl-38767098

ABSTRACT

The present study was designed to assess Tradescantia spathacea's antidiabetic ability, as well as the antiulcer activity of the entire plant extract. The diabetic condition was evaluated using Streptozotocin's oral glucose tolerance test, diabetes-alloxan and diabetes-models. Antiulcer activities were observed in rats where gastric ulcers were either caused by oral administration of ethanol, or pyloric ligation. Standards include ranitidine, glibenclamide and sucralfate. In all models, the blood glucose levels of animals treated with the test extract were found to be significantly lower compared to diabetic care. Similarly, in all models, the ulcer index in the animals treated with the test extract was found to be significantly lower relative to the animals under vehicle supervision. Our findings say T. Spathacea extract has essential anti-diabetic properties, as well as antiulcer properties.


Subject(s)
Anti-Ulcer Agents , Blood Glucose , Diabetes Mellitus, Experimental , Hypoglycemic Agents , Plant Extracts , Rats, Wistar , Stomach Ulcer , Animals , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/isolation & purification , Plant Extracts/pharmacology , Plant Extracts/isolation & purification , Anti-Ulcer Agents/pharmacology , Anti-Ulcer Agents/isolation & purification , Diabetes Mellitus, Experimental/drug therapy , Stomach Ulcer/drug therapy , Stomach Ulcer/prevention & control , Stomach Ulcer/pathology , Stomach Ulcer/chemically induced , Male , Rats , Blood Glucose/drug effects , Blood Glucose/metabolism , Methanol/chemistry , Glucose Tolerance Test , Solvents/chemistry , Phytotherapy
5.
Pak J Pharm Sci ; 37(2): 307-314, 2024 Mar.
Article in English | MEDLINE | ID: mdl-38767097

ABSTRACT

Long-lasting hyperglycemia can potentially cause damage to organs such as the kidneys, liver and pancreas. Glimepiride (GLIM), as a drug of choice in the treatment of diabetes mellitus (DM), has the risk of decreasing the functioning of organs such as the kidneys, liver and pancreas. Black rice bran ethanol extract (EEBRB) with antioxidant content has been shown to protect the kidney, liver and pancreas organs. The aim of this study was to establish the effect of EEBRB on lowering fasting blood glucose (FBG) and protecting several organs after GLIM administration in alloxan (ALX)-induced hyperglycemic rats. A total of 20 rats were divided into 4 groups and treated for 21 days treatments using following preparations: normal control (NC), diabetic group (DC), GLIM 1 mg/ kgBW and combination of glimepiride 1mg/kgBW and EEBRB 50 mg/KgBW (GLBR). The results showed that the GLBR was able to lower blood glucose levels back to normal (<126 mg/dL) and protect kidney, liver and pancreas cells by increasing the amount in normal cells.


Subject(s)
Blood Glucose , Diabetes Mellitus, Experimental , Hypoglycemic Agents , Kidney , Liver , Oryza , Pancreas , Plant Extracts , Sulfonylurea Compounds , Animals , Sulfonylurea Compounds/pharmacology , Plant Extracts/pharmacology , Plant Extracts/isolation & purification , Kidney/drug effects , Kidney/metabolism , Blood Glucose/drug effects , Blood Glucose/metabolism , Oryza/chemistry , Liver/drug effects , Liver/metabolism , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/isolation & purification , Diabetes Mellitus, Experimental/drug therapy , Diabetes Mellitus, Experimental/blood , Diabetes Mellitus, Experimental/chemically induced , Pancreas/drug effects , Pancreas/metabolism , Pancreas/pathology , Male , Rats , Ethanol/chemistry , Rats, Wistar
6.
Int J Biol Macromol ; 269(Pt 2): 132225, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38729460

ABSTRACT

The macroalgae are a sustainable bioresource that can be harnessed for their functional food and nutraceutical applications. This study characterized the biochemical composition and bioactive potential of natural biological macromolecules, such as macroalgal polysaccharides extracted using a green, aqueous extraction process. The in-vitro antioxidant and antiglycemic activity of these polysaccharides were evaluated using model, free radical and antiglycemic compounds. The prebiotic potential of macroalgal polysaccharides were analysed based on their ability to promote the growth of two potential probiotic bacteria Lactobacillus acidophilus and L. bulgaricus and suppress the growth of enteric bacteria, Escherichia coli. Among the polysaccharides studied, the brown algal polysaccharide MPS8 MPS9 and MPS10 exhibited good antioxidant, antiglycemic and prebiotic activity. Based on infrared spectroscopy, the functional groups sulfation and carboxylation were identified in potential polysaccharides. The monosaccharide composition in the bioactive polysaccharides was determined using High Performance Anion Exchange Chromatography Pulse Amperometric detector (HPAEC-PAD). These bioactive polysaccharides were fractionated using ion exchange chromatography to purify it and further characterized using gel permeation chromatography and NMR spectroscopy. The results these polysaccharides are mainly composed of fucose and glucose which is due to the fucoidan and laminarin, respectively. Such macromolecules with high dietary fiber content and bioactivity are in global demand as functional food, nutraceutical and pharmaceutical formulations.


Subject(s)
Antioxidants , Dietary Fiber , Polysaccharides , Prebiotics , Seaweed , Seaweed/chemistry , Polysaccharides/chemistry , Polysaccharides/isolation & purification , Polysaccharides/pharmacology , Antioxidants/pharmacology , Antioxidants/chemistry , Antioxidants/isolation & purification , Dietary Fiber/analysis , India , Monosaccharides/analysis , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/isolation & purification , Escherichia coli/drug effects
7.
Front Biosci (Landmark Ed) ; 29(5): 183, 2024 May 11.
Article in English | MEDLINE | ID: mdl-38812295

ABSTRACT

BACKGROUND: The present study aimed to investigate the in-vitro anti-diabetic, anti-cholinesterase, and anti-inflammatory potential of extracts from different parts of Ficus benghalensis, including leaves, stem, and roots, as well as isolated column fractions (F-B-1 C, F-B-2 C, F-B-3 C, and F-B-4 C). METHODS: The extracts and subsequent fractions were evaluated for their inhibitory activity against key enzymes involved in diabetes [α-glucosidase and α-amylase], neurodegenerative diseases [acetylcholinesterase and butyrylcholinesterase], and inflammation (cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX)). RESULTS: The results showed that F. benghalensis leaf extract exhibited the highest α-glucosidase inhibitory activity (73.84%) and α-amylase inhibitory activity (76.29%) at 1000 µg/mL. The stem extract (65.50%) and F-B-2 C fraction (69.67%) also demonstrated significant α-glucosidase inhibitory activity. In terms of anti-cholinesterase activity, the extracts of roots, leaves, and stem showed promising inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with half maximal inhibitory concentration (IC50) values ranging from 50.50 to 474.83 µg/mL. The derived fractions (F-B-1 C, F-B-2 C, F-B-3 C, and F-B-4 C) also exhibited notable inhibition of AChE and BChE, with IC50 values from 91.85 to 337.94 µg/mL. Moreover, the F-B-3 C fraction demonstrated the highest COX-2 inhibitory potential (85.72%), followed by F-B-1 C (83.13%), the stem extract (80.85%), and the leaves extract (79.00%). The F-B-1 C fraction showed the highest 5-LOX inhibitory activity (87.63%), while the root extract exhibited the lowest inhibition (73.39%). CONCLUSIONS: The results demonstrated promising bioactivity, suggesting the potential of F. benghalensis as a source of natural compounds with therapeutic applications. Further studies are required to identify and isolate the active components responsible for these effects and to evaluate their in-vivo efficacy and safety.


Subject(s)
Anti-Inflammatory Agents , Cholinesterase Inhibitors , Ficus , Hypoglycemic Agents , Plant Extracts , Ficus/chemistry , Plant Extracts/pharmacology , Plant Extracts/chemistry , Cholinesterase Inhibitors/pharmacology , Cholinesterase Inhibitors/isolation & purification , Cholinesterase Inhibitors/chemistry , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/isolation & purification , Anti-Inflammatory Agents/chemistry , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/isolation & purification , Plant Leaves/chemistry , Butyrylcholinesterase/metabolism , Glycoside Hydrolase Inhibitors/pharmacology , Glycoside Hydrolase Inhibitors/isolation & purification , alpha-Amylases/antagonists & inhibitors , Lipoxygenase Inhibitors/pharmacology , Lipoxygenase Inhibitors/isolation & purification , Acetylcholinesterase/metabolism , Arachidonate 5-Lipoxygenase/metabolism , Plant Roots/chemistry
8.
Comput Biol Chem ; 110: 108087, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38718496

ABSTRACT

INTRODUCTION: Diabetes Mellitus is the metabolic disorder most prevalent globally, accounting for a substantial morbidity rate. The conventional drugs available for the management of diabetes are either expensive or lack the required efficacy. The purpose of this research is to isolate and characterize an active phytoconstituent from Coccinia grandis and assess its anti-diabetic properties. METHODS AND MATERIALS: Stems of Coccinia grandis are subjected to successive extraction and isolation. The isolated compound by column chromatography was characterized by FTIR (fourier-transform infrared), 1 H NMR (proton nuclear magnetic resonance), and Mass spectroscopy. The antidiabetic potential of the isolated compound was evaluated by in-vitro alpha-amylase inhibitory activity. Further, the compound was subjected to molecular docking studies to study its interaction with the human pancreatic alpha-amylase (Molegro Virtual Docker) as well to determine the pharmacokinetic and toxicity profile using computational techniques (OSIRIS property explorer, Swiss ADME, pkCSM, and PreADMET). RESULTS: The characterization of the compound suggests the structure to be 2,4-ditertiary butyl phenol. The in-vitro alpha-amylase inhibitory study indicated a concentration-dependent inhibition and the IC50 (median lethal dose) value of the isolated compound was found to be 64.36 µg/ml. The docking study with the A chain of receptor 5EMY yielded a favorable docking score of -81.48 Kcal mol-1, suggesting that the compound binds to the receptor with high affinity through electrostatic, hydrophobic, and hydrogen bonds. Furthermore, the silico ADME analysis of the compound revealed improved metabolism, a skin permeability of -3.87 cm/s, gastrointestinal absorption of 95.48 %, and a total clearance of 0.984 log ml min-1 kg-1. In silico toxicity analysis also predicted cutaneous irritations but no carcinogenicity, mutagenicity, or hepatotoxicity. CONCLUSION: The data suggested that the isolated compound (2, 4-tertiary butyl phenol) has the potential to inhibit the alpha-amylase activity and possess optimal ADME properties as well as tolerable side effects.


Subject(s)
Molecular Docking Simulation , Phenols , alpha-Amylases , Humans , alpha-Amylases/antagonists & inhibitors , alpha-Amylases/metabolism , Phenols/chemistry , Phenols/pharmacology , Phenols/isolation & purification , Cucurbitaceae/chemistry , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , Enzyme Inhibitors/isolation & purification , Molecular Structure , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/isolation & purification
9.
J Ethnopharmacol ; 331: 118300, 2024 Sep 15.
Article in English | MEDLINE | ID: mdl-38718889

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Schisandra sphenanthera (Schisandra sphenanthera Rehd. et Wils.) is the dried mature fruit of Schisandra sphenanthera, a plant in the Magnoliaceae family. It was used in the treatment of diabetes mellitus in the Jade Fluid Decoction and the Xiaoke pills, which were recorded in ancient books. However, its mechanism of action in the treatment of type 2 diabetes mellitus (T2DM) was unclear and needs further study. AIM OF THE STUDY: This research aimed to investigate the chemical composition and lignan content of Schisandra sphenanthera petroleum ether parts (SPEP) and to evaluate the effects of SPEP on sweet taste receptors (STRs) and intestinal flora in rats on a high-fat diet (HFD). Additionally, the relationships between SPEP and hyperglycemia and insulin resistance were examined. MATERIALS AND METHODS: GC-MS was used to determine the chemical composition of SPEP, and HPLC was used to determine the lignin content. A combination of the HFD and the administration of streptozotocin (STZ) was employed to generate a rat model of T2DM. Petroleum ether extracts from Schisandra sphenanthera were used as the focus of the research to evaluate the effects of these extracts on the glucolipid metabolism of T2DM rats, as well as the underlying mechanisms. RESULTS: Analysis of the GC-MS spectrum of SESP revealed a total of 58 compounds. HPLC analysis revealed that SPEP had the highest concentration of Schisandrin A and the lowest concentration of Schisandrol A. The drug administration intervention resulted in a significant decrease in body weight and pancreatic weight of diabetic rats compared to the Normal group. When compared to the Model group, the body weight of rats in the drug administration group and the Metformin group had a more moderate decrease, while the pancreatic weight and pancreatic-to-body ratio increased. The Model group shown significant increases in FBG, OGTT, GHb, TC, TG, LDL-C, ALT, AST, MDA, FINS, and NEFA, as well as significant decreases in HDL-C and SOD, when compared to the Normal group (P < 0.05). The administration of each group was found to be significantly effective in decreasing FBG, OGTT, GHb, TC, TG, LDL-C, ALT, AST, MDA, FINS, NEFA, while increasing HDL-C and SOD when compared to the Model group. The application of SPEP had a positive impact on hepatocyte swelling, hepatocyte degeneration, and necrosis, as well as the morphological structure of pancreatic islet cells. Furthermore, the protein expression levels of T1R2, TRPM5 and GLP-1 in the small intestine of the Model group were reduced. After a period of six weeks, the protein expression levels began to align more closely with those of the Normal group of rats. Analysis of 16S rRNA sequencing revealed that the intestinal microbiota of diabetic rats was significantly disrupted, with a decrease in the abundance of the Firmicutes phylum and an increase in the abundance of the Bacteroidetes phylum. Furthermore, the composition of the dominant genus was distinct from that of the control group. After the drug intervention, the microbiota of diabetic rats was significantly altered, exhibiting a higher abundance and diversity, as well as a significant enrichment of the community. The SPEP treatment resulted in a significant increase in acetic acid, propionic acid, and butyric acid. CONCLUSIONS: The findings of this research indicated that SPEP could be effective in treating T2DM through the regulation of STRs, the adjustment of disturbed metabolite levels, and the alteration of intestinal flora.


Subject(s)
Alkanes , Diabetes Mellitus, Experimental , Diabetes Mellitus, Type 2 , Gastrointestinal Microbiome , Hyperglycemia , Insulin Resistance , Plant Extracts , Rats, Sprague-Dawley , Schisandra , Animals , Schisandra/chemistry , Gastrointestinal Microbiome/drug effects , Male , Diabetes Mellitus, Experimental/drug therapy , Plant Extracts/pharmacology , Plant Extracts/chemistry , Plant Extracts/administration & dosage , Diabetes Mellitus, Type 2/drug therapy , Hyperglycemia/drug therapy , Rats , Alkanes/chemistry , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/isolation & purification , Diet, High-Fat/adverse effects , Blood Glucose/drug effects , Blood Glucose/metabolism , Streptozocin , Receptors, G-Protein-Coupled/metabolism , Lignans/pharmacology , Lignans/isolation & purification
10.
Int J Biol Macromol ; 267(Pt 2): 131376, 2024 May.
Article in English | MEDLINE | ID: mdl-38608981

ABSTRACT

Diabetes is a chronic, metabolic disease characterized by hyperglycemia resulting from either insufficient insulin production or impaired cellular response to insulin. Exopolysaccharides (EPS) produced by Lactobacillus spp. demonstrated promising therapeutic potential in terms of their anti-diabetic properties. Extraction and purification of EPS produced by Lactobacillus acidophilus and Limosilactobacillus reuteri were performed using ethanol precipitation, followed by alcohol/salt based aqueous two-phase system (ATPS). The purification process involved ethanol precipitation followed by an alcohol/salt-based ATPS. The study systematically investigated various purification parameters in ATPS, including ethanol concentration, type and concentration of ionic liquid, type and concentration of salt and pH of salt. Purified EPS contents from L. acidophilus (63.30 µg/mL) and L. reuteri (146.48 µg/mL) were obtained under optimum conditions of ATPS which consisted of 30 % (w/w) ethanol, 25 % (w/w) dipotassium hydrogen phosphate at pH 10 and 2 % (w/w) 1-butyl-3-methylimidazolium octyl sulfate. The extracted EPS content was determined using phenol sulphuric acid method. In α-amylase inhibition tests, the inhibitory rate was found to be 92.52 % (L. reuteri) and 90.64 % (L. acidophilus), while in α-glucosidase inhibition tests, the inhibitory rate was 73.58 % (L. reuteri) and 68.77 % (L. acidophilus), based on the optimized parameters selected in ATPS. These results suggest that the purified EPS derived from the postbiotics of Lactobacillus spp. hold promise as potential antidiabetic agents.


Subject(s)
Hypoglycemic Agents , Ionic Liquids , Lactobacillus , Polysaccharides, Bacterial , Ionic Liquids/chemistry , Polysaccharides, Bacterial/chemistry , Polysaccharides, Bacterial/pharmacology , Polysaccharides, Bacterial/isolation & purification , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/isolation & purification , Hydrogen-Ion Concentration , Ethanol/chemistry , alpha-Amylases/antagonists & inhibitors , Lactobacillus acidophilus , Salts/chemistry
11.
J Ethnopharmacol ; 330: 118252, 2024 Aug 10.
Article in English | MEDLINE | ID: mdl-38663782

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Atractylis aristata batt., as an endemic plant from the Asteraceae family, holds a significant position in the Ahaggar region of southern Algeria's traditional medicine. The aerial parts of Atractylis aristata was used to cure inflammation, fever, and stomach disorders. AIM OF THE STUDY: The objective of the present investigation was to ascertain the overall bioactive components and phytochemical components and examine the antioxidant, antidiabetic, anti-inflammatory, acute toxicity, and sedative properties of the crude extract obtained from the aerial portions of Atractylis aristata (AaME). MATERIALS AND METHODS: The AaME's antioxidant activity was assessed by the use of pyrogallol autoxidation, (1,1 diphenyl-2-picrylhydrazyl) (DPPH), 2,2'-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid (ABTS), and reducing power (RP) techniques. 1 mg/mL of AaME was used to evaluate the antidiabetic activity by applying the enzyme α-amylase inhibitory power test. At the same time, the bovine serum albumin (BSA) denaturation method was employed to quantify the in vitro anti-inflammatory activity at different concentrations (1.5625, 0.78125, 0.390625, 0.1953125 and 0.09765625 mg/mL). In contrast, following the Organization for Economic Co-operation and Development (OECD) guideline No. 423, which covers acute oral toxicity testing protocols, the limit dosage test was employed to assess in vivo acute toxicity. At the dose of 0.08 mg/mL, the carrageenan-induced paw edema approach was used to assess the anti-inflammatory efficacy in vivo, and the sedative activity was carried out at the dose of 0.08 mg/mL using the measurement of the locomotor method. Different bioactive compounds were identified within AaME using LC-MS/MS and HPLC-UV analysis. RESULTS: The acute toxicity study showed no fatalities or noticeable neurobehavioral consequences at the limit test; this led to their classification in Globally Harmonized System (GHS) category Five, as the OECD guideline No 423 recommended. At a concentration of 0.08 mg/mL (2000 mg/kg), AaME showed apparent inhibition of paw edema and a significant (p = 0.01227) reduction in locomotor activity compared to the control animals. Our findings showed that AaME exhibited considerable antioxidant (IC50 = 0.040 ± 0.003 mg/mL (DPPH), IC50 = 0.005 ± 5.77 × 10-5 mg/mL (ABTS), AEAC = 91.15 ± 3.921 mg (RP) and IR% = 23.81 ± 4.276 (Inhibition rate of pyrogallol) and rebuts antidiabetic activities (I% = 57.6241% ± 2.81772). Our findings revealed that the maximum percentage of BSA inhibition (70.84 ± 0.10%) was obtained at 1.562.5 mg/mL. Thus, the AaME phytochemical profile performed using phytochemical screening, HPLC-UV, and LC-MS/MS analysis demonstrated that A. aristata can be a valuable source of chemicals with biological activity for pharmaceutical manufacturers. CONCLUSION: The phytochemical profiling, determined through HPLC-UV and LC-MS/MS applications, reveals this plant's therapeutic value. The aerial parts of Atractylis aristata contain bioactive molecules such as gallic acid, ascorbic acid, and quercetin, contributing to its significant antioxidant capabilities. Furthermore, identifying alizarin, the active compound responsible for its anti-inflammatory properties, could provide evidence supporting the anti-inflammatory capabilities of this subspecies.


Subject(s)
Anti-Inflammatory Agents , Antioxidants , Hypnotics and Sedatives , Hypoglycemic Agents , Phenols , Plant Extracts , Animals , Antioxidants/pharmacology , Antioxidants/isolation & purification , Antioxidants/chemistry , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/isolation & purification , Hypoglycemic Agents/chemistry , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/isolation & purification , Anti-Inflammatory Agents/chemistry , Plant Extracts/pharmacology , Plant Extracts/chemistry , Plant Extracts/toxicity , Male , Phenols/pharmacology , Phenols/analysis , Phenols/isolation & purification , Hypnotics and Sedatives/pharmacology , Hypnotics and Sedatives/isolation & purification , Hypnotics and Sedatives/toxicity , Mice , Asteraceae/chemistry , Rats, Wistar , Rats , Edema/drug therapy , Edema/chemically induced , Female , Plant Components, Aerial/chemistry
12.
Food Chem ; 451: 139467, 2024 Sep 01.
Article in English | MEDLINE | ID: mdl-38678661

ABSTRACT

Betacyanins have garnered escalating research interest for their promising bioactivities. However, substantial challenges in purification and separation have impeded a holistic comprehension of the distinct bioactivities of individual betacyanins and their underlying mechanisms. Herein, betanin and phyllocactin monomers with purity exceeding 95% were successfully obtained from Hylocereus polyrhizus peel using a feasible protocol. These monomers were subsequently employed for comparative bioactivity assessments to uncover underlying mechanisms and illuminate structure-activity relationships. Interestingly, phyllocactin exhibited superior antioxidant activities and 36.1% stronger inhibitory activity on α-glucosidase compared to betanin. Mechanistic studies have revealed that they function as mixed-type inhibitors of α-amylase and competitive inhibitors of α-glucosidase, with interactions predominantly driven by hydrogen bonding. Notably, phyllocactin demonstrated a greater binding affinity with enzymes than betanin, thereby substantiating its heightened inhibitory activity. Overall, our results highlight novel bioactivities of betacyanin monomers and provide profound insights into the intricate interplay between structures and properties.


Subject(s)
Antioxidants , Betacyanins , Cactaceae , Hypoglycemic Agents , Plant Extracts , Antioxidants/chemistry , Antioxidants/pharmacology , Antioxidants/isolation & purification , Betacyanins/chemistry , Betacyanins/pharmacology , Betacyanins/isolation & purification , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/isolation & purification , Cactaceae/chemistry , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Extracts/isolation & purification , alpha-Glucosidases/chemistry , alpha-Glucosidases/metabolism , alpha-Amylases/antagonists & inhibitors , alpha-Amylases/chemistry , Structure-Activity Relationship
13.
J Ethnopharmacol ; 329: 118133, 2024 Jul 15.
Article in English | MEDLINE | ID: mdl-38580187

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Angelica roots are a significant source of traditional medicines for various cultures around the northern hemisphere, from indigenous communities in North America to Japan. Among its many applications, the roots are used to treat type 2 diabetes mellitus; however, this application is not mentioned often. Ethnopharmacological studies have reported the use of A. japonica var. hirsutiflora, A. furcijuga, A. shikokiana, and A. keiskei to treat diabetes symptoms, and further reports have demonstrated the three angelica roots, i.e., A. japonica var. hirsutiflora, A. reflexa, and A. dahurica, exhibit insulin secretagogue activity. AIM OF THE STUDY: This study aimed to phytochemically characterize and compare angelica roots monographed in the European Pharmacopeia 11th, isolate major plant metabolites, and assess extracts and isolates' capability to modulate pancreatic ß-cell function. MATERIALS AND METHODS: Root extracts of Angelica archangelica, Angelica dahurica, Angelica biserrata, and Angelica sinensis were phytochemically profiled using liquid chromatography method coupled with mass spectrometry. Based on this analysis, simple and furanocoumarins were isolated using chromatography techniques. Extracts (1.6-50 µg/mL) and isolated compounds (5-40 µmol/L) were studied for their ability to modulate insulin secretion in the rat insulinoma INS-1 pancreatic ß-cell model. Insulin was quantified by the homogeneous time-resolved fluorescence method. RESULTS: Forty-one secondary metabolites, mostly coumarins, were identified in angelica root extracts. A. archangelica, A. dahurica, and A. biserrata root extracts at concentration of 12.5-50 µg/mL potentiated glucose-induced insulin secretion, which correlated with their high coumarin content. Subsequently, 23 coumarins were isolated from these roots and screened using the same protocol. Coumarins substituted with the isoprenyl group were found to be responsible for the extracts' insulinotropic effect. CONCLUSIONS: Insulinotropic effects of three pharmacopeial angelica roots were found, the metabolite profiles and pharmacological activities of the roots were correlated, and key structures responsible for the modulation of pancreatic ß-cell function were identified. These findings may have implications for the traditional use of angelica roots in treating diabetes. Active plant metabolites may also become lead structures in the search for new antidiabetic treatments.


Subject(s)
Angelica , Insulin-Secreting Cells , Phytochemicals , Plant Extracts , Plant Roots , Angelica/chemistry , Insulin-Secreting Cells/drug effects , Insulin-Secreting Cells/metabolism , Plant Extracts/pharmacology , Plant Extracts/chemistry , Animals , Phytochemicals/pharmacology , Phytochemicals/isolation & purification , Phytochemicals/analysis , Rats , Insulin/metabolism , Insulin Secretion/drug effects , Coumarins/pharmacology , Coumarins/isolation & purification , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/isolation & purification , Hypoglycemic Agents/chemistry
14.
Food Funct ; 15(8): 3939-3958, 2024 Apr 22.
Article in English | MEDLINE | ID: mdl-38536669

ABSTRACT

The mulberry plant is a member of the Moraceae family and belongs to the Morus genus. Its entire body is a treasure, with mulberries, mulberry leaves, and mulberry branches all suitable for medicinal use. The main active ingredient in mulberries is mulberry polysaccharide. Studies have shown that polysaccharides from different parts of mulberry exhibit antioxidant, antidiabetic, antibacterial, anti-inflammatory, and blood pressure-lowering properties. There are more studies on the biological activities, extraction methods, and structural characterization of polysaccharides from different parts of mulberry. However, the structural characterization of mulberry polysaccharides is mostly confined to the types and proportions of monosaccharides and the molecular weights of polysaccharides, and there are fewer systematic studies on polysaccharides from different parts of mulberry. In order to better understand the bioactive structure of mulberry polysaccharides, this article discusses the recent research progress in the extraction, separation, purification, bioactivity, structural modification, and application of polysaccharides from different parts of mulberry (mulberry leaves, mulberry fruits, and mulberry branches). It also delves into the pharmacological mechanisms of action of mulberry polysaccharides to provide a theoretical basis for further research on mulberry polysaccharides with a view to their deeper application in the fields of feed and nutraceuticals.


Subject(s)
Fruit , Morus , Plant Extracts , Plant Leaves , Polysaccharides , Morus/chemistry , Polysaccharides/chemistry , Polysaccharides/pharmacology , Polysaccharides/isolation & purification , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Leaves/chemistry , Fruit/chemistry , Humans , Antioxidants/pharmacology , Antioxidants/chemistry , Antioxidants/isolation & purification , Animals , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/isolation & purification
15.
Chem Biodivers ; 21(5): e202400245, 2024 May.
Article in English | MEDLINE | ID: mdl-38436134

ABSTRACT

Despite Aloe's traditional use, Aloe juvenna Brandham & S.Carter is poorly characterized. Other Aloes are known for their antidiabetic activity. This study describes the antidiabetic potentials and phytoconstituents of the A. juvenna leaves methanolic extract (AJME). Twenty-six phytoconstituents of AJME were described using HPLC/MS-MS. Lupeol and vitexin were isolated using column chromatography. The antidiabetic activity of AJME was investigated using an in vivo high-fat diet/streptozotocin-induced diabetic rat model and in vitro α-glucosidase and α-amylase inhibitory activity assays. AJME demonstrated its α-amylase inhibitory activity (IC50=313±39.9 ppm) with no effect on α-glucosidase. In vivo, AJME dose-dependently improved hyperglycaemia in a high-fat diet/streptozotocin-induced diabetic rat model. Notably, the higher dose (1600 mg/kg) of AJME significantly downregulated serum interleukin-6, tumor necrosis factor-α, and matrix metalloproteinase-1 genes, suggesting its anti-inflammatory effect. These findings indicate AJME's potential as a significant antidiabetic agent through its α-amylase inhibition, hypoglycaemic, and anti-inflammatory properties.


Subject(s)
Aloe , Anti-Inflammatory Agents , Diabetes Mellitus, Experimental , Hypoglycemic Agents , Plant Extracts , Plant Leaves , Streptozocin , alpha-Amylases , Animals , Aloe/chemistry , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/isolation & purification , alpha-Amylases/antagonists & inhibitors , alpha-Amylases/metabolism , Diabetes Mellitus, Experimental/drug therapy , Diabetes Mellitus, Experimental/chemically induced , Rats , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/isolation & purification , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Extracts/isolation & purification , Plant Leaves/chemistry , Male , Diet, High-Fat , Glycoside Hydrolase Inhibitors/pharmacology , Glycoside Hydrolase Inhibitors/chemistry , Glycoside Hydrolase Inhibitors/isolation & purification , Dose-Response Relationship, Drug , Rats, Sprague-Dawley
16.
Chem Biodivers ; 21(5): e202301788, 2024 May.
Article in English | MEDLINE | ID: mdl-38484132

ABSTRACT

Curcuma angustifolia Roxb. is a plant with medicinal potential, traditionally used to treat different diseases. The present study aimed to determine the antidiabetic activity of C. angustifolia rhizome in vitro and in silico. The methanolic extract of C. angustifolia rhizome was analyzed by FTIR and GC-MS to determine the phytochemicals present. The antidiabetic potential of the extract was evaluated by different assays in vitro. The extract inhibited both α-amylase and α-glucosidase enzymes and the glucose diffusion through the dialysis membrane in a concentration-dependent manner with IC50 values of 530.39±0.09, 293.75±0.11, and 551.74±0.3 µg/ml respectively. The methanolic extract also improved yeast cell's ability to take up glucose across plasma membranes and the adsorption of glucose. The findings were supported by molecular docking studies. The results showed that the methanol extract of C. angustifolia rhizome has significant antidiabetic activity and thus can be also studied to isolate the potential compound with antidiabetic activities.


Subject(s)
Curcuma , Hypoglycemic Agents , Methanol , Molecular Docking Simulation , Plant Extracts , Rhizome , alpha-Amylases , alpha-Glucosidases , Curcuma/chemistry , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/isolation & purification , Rhizome/chemistry , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Extracts/isolation & purification , alpha-Amylases/antagonists & inhibitors , alpha-Amylases/metabolism , alpha-Glucosidases/metabolism , Methanol/chemistry , Phytochemicals/pharmacology , Phytochemicals/chemistry , Phytochemicals/isolation & purification , Glycoside Hydrolase Inhibitors/pharmacology , Glycoside Hydrolase Inhibitors/chemistry , Glycoside Hydrolase Inhibitors/isolation & purification , Dose-Response Relationship, Drug , Glucose/metabolism
17.
Chem Pharm Bull (Tokyo) ; 71(10): 756-765, 2023.
Article in English | MEDLINE | ID: mdl-37779077

ABSTRACT

In this review, our resent pharmaceutical food science research for bio-functional molecules obtained from natural resources that contribute to i) suppression of postprandial blood glucose elevation and/or improvement of glucose tolerance and ii) reduction of visceral fat accumulation and improvement of lipid metabolism were summarized. Based on studies using MONOTORI science, salacinol (1), neokotalanol (4), and trans-tiliroside (20) have been approved or notified by the Consumer Affairs Agency in Japan as functional substances in food with health claims, Food for Specified Health Use and Food with Functional Claims.


Subject(s)
Biological Products , Blood Glucose , Food Technology , Functional Food , Hypoglycemic Agents , Hypolipidemic Agents , Lipid Metabolism , Food Technology/trends , Japan , Intra-Abdominal Fat/drug effects , Lipid Metabolism/drug effects , Blood Glucose/drug effects , Humans , Biological Products/chemistry , Biological Products/isolation & purification , Biological Products/pharmacology , Hypolipidemic Agents/chemistry , Hypolipidemic Agents/isolation & purification , Hypolipidemic Agents/pharmacology , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/isolation & purification , Hypoglycemic Agents/pharmacology
18.
Int J Med Mushrooms ; 25(8): 19-31, 2023.
Article in English | MEDLINE | ID: mdl-37560887

ABSTRACT

Polysaccharides serve as promising ingredients for health-beneficial functional foods, while there were no investigations into the structural characterizations and bioactivities of an edible mushroom Cantharellus yunnanensis. In the study, crude polysaccharides from this mushroom were extracted by hot water and isolated by ethanol precipitation. Then, a neutral polysaccharide (named CY-1) was purified from the crude polysaccharide by deproteinization with Sevag reagent, decolorization with a kind of macroporous adsorption resin SP-825, DEAE-52 cellulose column chromatography and dialysis. The physicochemical properties of CY-1 were characterized by UV, IR, SEM, NMR, and HPLC analyses. Structural characterizations revealed that CY-1 is a homogeneous heteropolysaccharide with an average molecular weight of 3.06 × 104 Da. CY-1 exhibited a honeycomb structure with an irregular branching shape, and it was composed of mannose, glucose, fucose, xylose, arabinose, galactose, rhamnose, and glucuronic acid, with molar fractions of 54.83%, 25.11%, 10.28% 4.53%, 2.12%, 1.64%, 0.83%, and 0.64%, respectively. In vitro hypoglycemic tests showed that CY-1 had an inhibitory effect on α-glucosidase. In addition, CY-1 of 160 µg/mL promoted glucose consumption in normal HepG2 cells. These results suggested that CY-1 may be a potential hypoglycemic agent.


Subject(s)
Agaricales , Hypoglycemic Agents , Polysaccharides , Agaricales/chemistry , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/isolation & purification , Polysaccharides/chemistry , Polysaccharides/isolation & purification
19.
Molecules ; 27(4)2022 Feb 16.
Article in English | MEDLINE | ID: mdl-35209111

ABSTRACT

The recent study investigated the in vitro anti-diabetic impact of the crude extract (MeOH) and subfractions ethyl acetate (EtOAc); chloroform; n-butanol; n-hexane; and aqueous fraction of S. edelbergii and processed the active EtOAc fraction for the identification of chemical constituents for the first time via ESI-LC-MS analysis through positive ionization mode (PIM) and negative ionization mode (NIM); the identified compounds were further validated through computational analysis via standard approaches. The crude extract and subfractions presented appreciable activity against the α-glucosidase inhibitory assay. However, the EtOAc fraction with IC50 = 0.14 ± 0.06 µg/mL revealed the maximum potential among the fractions used, followed by the MeOH and n-hexane extract with IC50 = 1.47 ± 0.14 and 2.18 ± 0.30 µg/mL, respectively. Moreover, the acarbose showed an IC50 = 377.26 ± 1.20 µg/ mL whereas the least inhibition was observed for the chloroform fraction, with an IC50 = 23.97 ± 0.14 µg/mL. Due to the significance of the EtOAc fraction, when profiled for its chemical constituents, it presented 16 compounds among which the flavonoid class was dominant, and offered eight compounds, of which six were identified in NIM, and two compounds in PIM. Moreover, five terpenoids were identified-three and two in NIM and PIM, respectively-as well as two alkaloids, both of which were detected in PIM. The EtOAc fraction also contained one phenol that was noticed in PIM. The detected flavonoids, terpenoids, alkaloids, and phenols are well-known for their diverse biomedical applications. The potent EtOAc fraction was submitted to computational analysis for further validation of α-glucosidase significance to profile the responsible compounds. The pharmacokinetic estimations and protein-ligand molecular docking results with the support of molecular dynamic simulation trajectories at 100 ns suggested that two bioactive compounds-dihydrocatalpol and leucosceptoside A-from the EtOAc fraction presented excellent drug-like properties and stable conformations; hence, these bioactive compounds could be potential inhibitors of alpha-glucosidase enzyme based on intermolecular interactions with significant residues, docking score, and binding free energy estimation. The stated findings reflect that S. edelbergii is a rich source of bioactive compounds offering potential cures for diabetes mellitus; in particular, dihydrocatalpol and leucosceptoside A could be excellent therapeutic options for the progress of novel drugs to overcome diabetes mellitus.


Subject(s)
Drug Discovery , Glycoside Hydrolase Inhibitors/chemistry , Glycoside Hydrolase Inhibitors/pharmacology , Models, Molecular , Plant Extracts/chemistry , Plant Extracts/pharmacology , Scutellaria/chemistry , Chemical Fractionation , Chromatography, Liquid , Drug Discovery/methods , Enzyme Activation/drug effects , Glycoside Hydrolase Inhibitors/isolation & purification , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/isolation & purification , Hypoglycemic Agents/pharmacology , Ligands , Molecular Docking Simulation , Molecular Dynamics Simulation , Molecular Structure , Plant Extracts/isolation & purification , Spectrometry, Mass, Electrospray Ionization , Structure-Activity Relationship , Tandem Mass Spectrometry
20.
Food Funct ; 13(6): 3343-3352, 2022 Mar 21.
Article in English | MEDLINE | ID: mdl-35212690

ABSTRACT

Douchi is a popular soy-fermented food that originated in China with documented hypoglycemic effects. However, the responsible molecules and the mechanism underlying their beneficial effects remain unclear. Therefore, in this study, we aimed to identify the responsible peptide(s) in douchi. A peptide extract of douchi was isolated step-wise by the C18 Sep-Pak technique, size exclusion chromatography, and semi-preparative liquid chromatography, and then the peptides were sequenced by UPLC-MS/MS. A total of 21 peptides were identified, of which three peptides, P3 (HPFR), P5 (VY), and P7 (SFLLR), were shown to improve glucose uptake in L6 cells. Both P5 and P7 increased glucose transporter 4 (GLUT4) translocation via the activation of AMPK and MAPK signaling pathways, but not the insulin-signaling pathway; adding an AMPK or an MAPK inhibitor prevented P5 or P7-induced glucose uptake as well as AMPK and MAPK activation. Our study showed that P5 and P7 could promote glucose uptake via AMPK and MAPK signaling pathways. In this study, two hypoglycemic peptides from douchi have been characterized for the first time.


Subject(s)
Fermented Foods , Glucose/metabolism , Hypoglycemic Agents/isolation & purification , Myoblasts/metabolism , Peptides/isolation & purification , AMP-Activated Protein Kinases/metabolism , Amino Acid Sequence , Animals , Cell Line , Glucose Transporter Type 4/metabolism , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/pharmacology , Insulin/metabolism , MAP Kinase Signaling System , Muscle Fibers, Skeletal/drug effects , Muscle Fibers, Skeletal/metabolism , Myoblasts/drug effects , Peptides/chemistry , Peptides/pharmacology , Rats , Signal Transduction
SELECTION OF CITATIONS
SEARCH DETAIL
...