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Iqbal M Choudhary - One of the best experts on this subject based on the ideXlab platform.
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potent Insulin Secretagogue from scoparia dulcis linn of nepalese origin
Phytotherapy Research, 2015Co-Authors: Khaga Raj Sharma, Achyut Adhikari, Rahman M Hafizur, Abdul Hameed, Sayed Ali Raza, Surya K Kalauni, Junichi Miyazaki, Iqbal M ChoudharyAbstract:Ethno-botanical inspired isolation from plant Scoparia dulcis Linn. (Sweet Broomweed) yielded six compounds, coixol (1), glutinol (2), glutinone (3), friedelin (4), betulinic acid (5), and tetratriacontan-1-ol (6). There structures were identified using mass and 1D- and 2D-NMR spectroscopy techniques. Compounds 1–6 were evaluated for their Insulin secretory activity on isolated mice islets and MIN-6 pancreatic β-cell line, and compounds 1 and 2 were found to be potent and mildly active, respectively. Compound 1 was further evaluated for Insulin secretory activity on MIN-6 cells. Compound 1 was subjected to in vitro cytotoxicity assay against MIN-6, 3T3 cell lines, and islet cells, and in vivo acute toxicity test in mice that was found to be non-toxic. The Insulin secretory activity of compounds 1 and 2 supported the ethno-botanic uses of S. dulcis as an anti-diabetic agent. Copyright © 2015 John Wiley & Sons, Ltd.
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potent Insulin Secretagogue from scoparia dulcis linn of nepalese origin
Phytotherapy Research, 2015Co-Authors: Khaga Raj Sharma, Achyut Adhikari, Rahman M Hafizur, Abdul Hameed, Sayed Ali Raza, Surya K Kalauni, Junichi Miyazaki, Iqbal M ChoudharyAbstract:Ethno-botanical inspired isolation from plant Scoparia dulcis Linn. (Sweet Broomweed) yielded six compounds, coixol (1), glutinol (2), glutinone (3), friedelin (4), betulinic acid (5), and tetratriacontan-1-ol (6). There structures were identified using mass and 1D- and 2D-NMR spectroscopy techniques. Compounds 1-6 were evaluated for their Insulin secretory activity on isolated mice islets and MIN-6 pancreatic β-cell line, and compounds 1 and 2 were found to be potent and mildly active, respectively. Compound 1 was further evaluated for Insulin secretory activity on MIN-6 cells. Compound 1 was subjected to in vitro cytotoxicity assay against MIN-6, 3T3 cell lines, and islet cells, and in vivo acute toxicity test in mice that was found to be non-toxic. The Insulin secretory activity of compounds 1 and 2 supported the ethno-botanic uses of S. dulcis as an anti-diabetic agent.
Fatima Regina Mena Barreto Silva - One of the best experts on this subject based on the ideXlab platform.
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astragalin augments basal calcium influx and Insulin secretion in rat pancreatic islets
Cell Calcium, 2019Co-Authors: Paola Miranda Sulis, Thais Fernandes, Renata Goncalves, Marisa Jadna Silva Frederico, Geison M Costa, Marcela Aragon, Luis Fernando Ospina, Fatima Regina Mena Barreto SilvaAbstract:Abstract Astragalin is a flavonol glycoside with several biological activities, including antidiabetic properties. The objective of this study was to investigate the effects of astragalin on glycaemia and Insulin secretion, in vivo, and on calcium influx and Insulin secretion in isolated rat pancreatic islets, ex vivo. Astragalin (1 and 10 mg / kg) was administered by oral gavage to fasted Wistar rats and serum glucose and plasma Insulin were measured. Isolated pancreatic islets were used to measure basal Insulin secretion and calcium influx. Astragalin (10 mg/ kg) decreased glycaemia and increased Insulin secretion significantly at 15–180 min, respectively, in the glucose tolerance test. In isolated pancreatic cells, astragalin (100 μM) stimulated calcium influx through a mechanism involving ATP-dependent potassium channels, L-type voltage-dependent calcium channels, the sarcoendoplasmic reticulum calcium transport ATPase (SERCA), PKC and PKA. These findings highlight the dietary coadjuvant, astragalin, as a potential Insulin Secretagogue that may contribute to glucose homeostasis.
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Insulin stimulus secretion coupling is triggered by a novel thiazolidinedione sulfonylurea hybrid in rat pancreatic islets
Journal of Cellular Physiology, 2019Co-Authors: Camila Pires Mendes, Marisa Jadna Silva Frederico, Allisson Jhonatan Gomes Castro, Barbara Graziela Postal, Geisel T C Oliveira, Ana Luiza Ludwig Moraes, Patricia D Neuenfeldt, Ricardo Jose Nunes, Danusa Menegaz, Fatima Regina Mena Barreto SilvaAbstract:New compounds with promising antidiabetic activity were synthesized. For the first time, a portion of the glibenclamide molecule was bound to a part of the core structure of thiazolidinedione to evaluate Insulin Secretagogue activity. Following studies in our laboratory, 4-{2-[2-(3,4-dichlorophenyl)-4-oxo-1,3-thiazolidin-3-yl]ethyl}benzene-1-sulfonamide (DTEBS) was selected to evaluate glycemia using the glucose tolerance test and Insulin Secretagogue activity by E.L.I.S.A. The mechanism of action of this compound was studied by 45 Ca2+ influx and whole-cell patch-clamp in rat pancreatic isolated islets. Furthermore, AGE formation in vitro was investigated. We herein show that this novel hybrid compound (DTEBS) exhibits an Insulinogenic index and a profile of serum Insulin secretion able to maintain glucose homeostasis. Its mechanism of action is mediated by ATP-sensitive potassium channels (KATP) and L-type voltage-dependent calcium channels (VDCC) and by activating protein kinase C and A (PKC and PKA). In addition, the stimulatory action of the compound on calcium influx and Insulin secretion indicates that the potentiation of voltage-sensitive K+ currents (Kv) is due to the repolarization phase of the action potential after Secretagogue excitation-secretion in pancreatic islets. Furthermore, under these experimental conditions, the compound did not induce toxicity and the in vitro late response of the compound to protein glycation reinforces its use to prevent complications of diabetes. DTEBS exerts an Insulin Secretagogue effect by triggering KATP, VDCC, and Kv ionic currents, possibly via PKC and PKA pathway signal transduction, in beta-cells. Furthermore, DTEBS may hold potential for delaying the late complications of diabetes.
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the potent Insulin Secretagogue effect of betulinic acid is mediated by potassium and chloride channels
Archives of Biochemistry and Biophysics, 2018Co-Authors: Allisson Jhonatan Gomes Castro, Paola Miranda Sulis, Luisa Helena Cazarolli, Moacir Geraldo Pizzolatti, Lizandra C Bretanha, Diana Patricia Rey Padilla, Diana Marcela Aragon Novoa, Betina Fernanda Dambros, Fatima Regina Mena Barreto SilvaAbstract:Betulinic acid (BA) has been described as an Insulin Secretagogue which may explain its potent antihyperglycemic effect; however, the exact role of BA as an Insulinogenic agent is not clear. The aim of this study was to investigate the mechanism of BA on calcium influx and static Insulin secretion in pancreatic islets isolated from euglycemic rats. We found that BA triggers calcium influx by a mechanism dependent on ATP-dependent potassium channels and L-type voltage-dependent calcium channels. Additionally, the voltage-dependent and calcium-dependent chloride channels are also involved in the mechanism of BA, probably due to an indirect stimulation of calcium entry and increased intracellular calcium. Additionally, the downstream activation of PKC, which is necessary for the effect of BA on calcium influx, is involved in the full stimulatory response of the triterpene. BA stimulated the static secretion of Insulin in pancreatic islets, indicating that the abrupt calcium influx may be a key step in its Secretagogue effect. As such, BA stimulates Insulin secretion through the activation of electrophysiological mechanisms, such as the closure of potassium channels and opening of calcium and chloride channels, inducing cellular depolarization associated with metabolic-biochemical effects, in turn activating PKC and ensuring the secretion of Insulin.
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the role of calcium in intracellular pathways of rutin in rat pancreatic islets potential Insulin Secretagogue effect
European Journal of Pharmacology, 2013Co-Authors: Virginia Demarchi Kappel, Marisa Jadna Silva Frederico, Luisa Helena Cazarolli, Barbara Graziela Postal, Camila Pires Mendes, Fatima Regina Mena Barreto SilvaAbstract:Rutin is a flavonol glycoside with multiple biological activities and it has been demonstrated that rutin modulates glucose homeostasis. In pancreatic β-cell, an increase in intracellular calcium concentration triggers exocytosis and thus Insulin secretion. The aim of the study reported herein was to investigate the effect of rutin associated intracellular pathways on Ca(2+) uptake in isolated rat pancreatic islets. We focused on the acute effects of rutin on in vivo Insulin secretion and the in vitro cellular signaling of pancreatic islets related to this effect. The results show that rutin significantly increased glucose-induced Insulin secretion in an in vivo treatment. Moreover, it was demonstrated that rutin stimulated Ca(2+) uptake after 10 min of incubation compared with the respective control group. The involvement of L-type voltage-dependent Ca(2+) channels (L-VDCCs) was evidenced using nifedipine, while the use of glibenclamide and diazoxide demonstrated that the ATP-sensitive potassium (KATP) channels are not involved in the rutin action in pancreatic islets. In conclusion, rutin diminish glycemia, potentiate Insulin secretion in vivo and significantly stimulates Ca(2+) uptake in rat pancreatic islets. A novel cellular mechanism of action of rutin in Ca(2+) uptake on pancreatic β-cells was elucidated. Rutin modulates Ca(2+) uptake in pancreatic islets by opening L-VDCCs, alter intracellular Ca(2+), PLC and PKC signaling pathways, characterizing KATP channel-independent pathways. These findings highlight rutin, a dietary adjuvant, as a potential Insulin Secretagogue contributing to glucose homeostasis.
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chapter 2 natural and synthetic chalcones tools for the study of targets of action Insulin Secretagogue or Insulin mimetic
Studies in natural products chemistry, 2013Co-Authors: Luisa Helena Cazarolli, Virginia Demarchi Kappel, Moacir Geraldo Pizzolatti, Ricardo Jose Nunes, Ana Paula Zanatta, Daniela Ota Hisayasu Suzuki, Rosendo A Yunes, Fatima Regina Mena Barreto SilvaAbstract:Chalcones are a group of plant-derived polyphenolic compounds that possess a wide variety of biological activities. Several lead compounds with various pharmacological properties have been developed based on the chalcone skeleton. The beneficial effect of these substances has been studied in relation to diabetes mellitus. Several studies have demonstrated that chalcones either from natural or synthetic sources can influence carbohydrate pathways, especially glucose metabolism. These studies verified the effectiveness of chalcones as antihyperglycemic and/or hypoglycemic agents through in vitro and in vivo experimental responses. In this context, these molecules are attractive substances which can enrich the current therapy options and they have become the subject of considerable interest in both academia and industry. The purpose of this review is to discuss the recent developments related to the chemistry and medicinal properties of chalcones, especially concerning their role in glucose homeostasis and carbohydrate metabolism. Also, taking into account the relevant structure–activity relationships of these compounds, the development of new approaches to study the interactions of chalcones in specific targets combining in silico (computational modeling) and in vitro pharmacological studies on β-cells represents a challenge for future perspectives aimed at characterizing molecular targets for diabetes therapy.
P Daisy - One of the best experts on this subject based on the ideXlab platform.
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Insulin Secretagogue antihyperlipidemic and other protective effects of gallic acid isolated from terminalia bellerica roxb in streptozotocin induced diabetic rats
Chemico-Biological Interactions, 2011Co-Authors: Cecily Rosemary R Latha, P DaisyAbstract:Abstract Diabetes mellitus causes derangement of carbohydrate, protein and lipid metabolism which eventually leads to a number of secondary complications. Terminalia bellerica is widely used in Indian medicine to treat various diseases including diabetes. The present study was carried out to isolate and identify the putative antidiabetic compound from the fruit rind of T. bellerica and assess its chemico-biological interaction in experimental diabetic rat models. Bioassay guided fractionation was followed to isolate the active compound, structure was elucidated using 1H and 13C NMR, IR, UV and mass spectrometry and the compound was identified as gallic acid (GA). GA isolated from T. bellerica and synthetic GA was administered to streptozotocin (STZ)-induced diabetic male Wistar rats at different doses for 28 days. Plasma glucose level was significantly (p
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Insulin Secretagogue antihyperlipidemic and other protective effects of gallic acid isolated from terminalia bellerica roxb in streptozotocin induced diabetic rats
Chemico-Biological Interactions, 2011Co-Authors: Cecily Rosemary R Latha, P DaisyAbstract:Diabetes mellitus causes derangement of carbohydrate, protein and lipid metabolism which eventually leads to a number of secondary complications. Terminalia bellerica is widely used in Indian medicine to treat various diseases including diabetes. The present study was carried out to isolate and identify the putative antidiabetic compound from the fruit rind of T. bellerica and assess its chemico-biological interaction in experimental diabetic rat models. Bioassay guided fractionation was followed to isolate the active compound, structure was elucidated using (1)H and (13)C NMR, IR, UV and mass spectrometry and the compound was identified as gallic acid (GA). GA isolated from T. bellerica and synthetic GA was administered to streptozotocin (STZ)-induced diabetic male Wistar rats at different doses for 28 days. Plasma glucose level was significantly (p<0.05) reduced in a dose-dependent manner when compared to the control.Histopathological examination of the pancreatic sections showed regeneration of β-cells of islets of GA-treated rats when compared to untreated diabetic rats. In addition, oral administration of GA (20mg/kg bw) significantly decreased serum total cholesterol, triglyceride, LDL-cholesterol, urea, uric acid, creatinine and at the same time markedly increased plasma Insulin, C-peptide and glucose tolerance level. Also GA restored the total protein, albumin and body weight of diabetic rats to near normal. Thus our findings indicate that gallic acid present in fruit rind of T. bellerica is the active principle responsible for the regeneration of β-cells and normalizing all the biochemical parameters related to the patho-biochemistry of diabetes mellitus and hence it could be used as a potent antidiabetic agent.
Khaga Raj Sharma - One of the best experts on this subject based on the ideXlab platform.
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potent Insulin Secretagogue from scoparia dulcis linn of nepalese origin
Phytotherapy Research, 2015Co-Authors: Khaga Raj Sharma, Achyut Adhikari, Rahman M Hafizur, Abdul Hameed, Sayed Ali Raza, Surya K Kalauni, Junichi Miyazaki, Iqbal M ChoudharyAbstract:Ethno-botanical inspired isolation from plant Scoparia dulcis Linn. (Sweet Broomweed) yielded six compounds, coixol (1), glutinol (2), glutinone (3), friedelin (4), betulinic acid (5), and tetratriacontan-1-ol (6). There structures were identified using mass and 1D- and 2D-NMR spectroscopy techniques. Compounds 1–6 were evaluated for their Insulin secretory activity on isolated mice islets and MIN-6 pancreatic β-cell line, and compounds 1 and 2 were found to be potent and mildly active, respectively. Compound 1 was further evaluated for Insulin secretory activity on MIN-6 cells. Compound 1 was subjected to in vitro cytotoxicity assay against MIN-6, 3T3 cell lines, and islet cells, and in vivo acute toxicity test in mice that was found to be non-toxic. The Insulin secretory activity of compounds 1 and 2 supported the ethno-botanic uses of S. dulcis as an anti-diabetic agent. Copyright © 2015 John Wiley & Sons, Ltd.
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potent Insulin Secretagogue from scoparia dulcis linn of nepalese origin
Phytotherapy Research, 2015Co-Authors: Khaga Raj Sharma, Achyut Adhikari, Rahman M Hafizur, Abdul Hameed, Sayed Ali Raza, Surya K Kalauni, Junichi Miyazaki, Iqbal M ChoudharyAbstract:Ethno-botanical inspired isolation from plant Scoparia dulcis Linn. (Sweet Broomweed) yielded six compounds, coixol (1), glutinol (2), glutinone (3), friedelin (4), betulinic acid (5), and tetratriacontan-1-ol (6). There structures were identified using mass and 1D- and 2D-NMR spectroscopy techniques. Compounds 1-6 were evaluated for their Insulin secretory activity on isolated mice islets and MIN-6 pancreatic β-cell line, and compounds 1 and 2 were found to be potent and mildly active, respectively. Compound 1 was further evaluated for Insulin secretory activity on MIN-6 cells. Compound 1 was subjected to in vitro cytotoxicity assay against MIN-6, 3T3 cell lines, and islet cells, and in vivo acute toxicity test in mice that was found to be non-toxic. The Insulin secretory activity of compounds 1 and 2 supported the ethno-botanic uses of S. dulcis as an anti-diabetic agent.
Akalpita U. Arvindekar - One of the best experts on this subject based on the ideXlab platform.
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antidiabetic activity of kalanchoe pinnata in streptozotocin induced diabetic rats by glucose independent Insulin Secretagogue action
Pharmaceutical Biology, 2013Co-Authors: Swapnil B. Patil, Madhav M. Joglekar, Vandana R Dongare, Chaitanya R Kulkarni, Akalpita U. ArvindekarAbstract:AbstractContext. Kalanchoe pinnata Lam. (Crassulaceae) is used as a traditional medicine worldwide to treat several ailments, including diabetes. However, the mechanism for the antihyperglycemic action is unknown.Objective: The present study evaluates the antihyperglycemic and Insulin Secretagogue potential of Kalanchoe pinnata and assessment of the probable mechanism of action.Materials and methods: Steam distillate of Kalanchoe pinnata leaves was subjected to solvent fractionation and antidiabetic activity was detected in dichloromethane (DCM) fraction. In the in vivo studies, rats were treated with 5 and 10 mg/kg body weight of DCM fraction for 45 days orally. Lipid profile and other biochemical parameters were estimated. The probable mechanism for Insulin Secretagogue action was evaluated through studies using diazoxide and nifedipine. The bioactive component from DCM fraction was studied using HPTLC, GCMS and IR.Results and discussion: Fasting blood glucose values were reduced to 116 mg/dl from 228 m...
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Insulinotropic and β-cell protective action of cuminaldehyde, cuminol and an inhibitor isolated from Cuminum cyminum in streptozotocin-induced diabetic rats
The British journal of nutrition, 2013Co-Authors: Swapnil B. Patil, Shreehari S. Takalikar, Madhav M. Joglekar, Vivek S. Haldavnekar, Akalpita U. ArvindekarAbstract:Cuminum cyminum, a commonly used spice, is known to have anti-diabetic action. The present study aims towards the isolation of bioactive components from C. cyminum and the evaluation of their Insulin Secretagogue potential with the probable mechanism and β-cell protective action. The anti-diabetic activity was detected in the petroleum ether (pet ether) fraction of the C. cyminum distillate and studied through in vivo and in vitro experiments. Bioactive components were identified through GC-MS, Fourier transform infrared spectroscopy and NMR analysis. The isolated components were evaluated for their Insulin Secretagogue action using rat pancreatic islets. Further, the probable mechanism of stimulation of islets was evaluated through in vitro studies using diazoxide, nifedipine and 3-isobutyl-1-methylxanthine. β-Cell protection was evaluated using the (1-(4,5-dimethylthiazol-2-yl)-3,5-diphenylformazan) (MTT) assay, the alkaline comet assay and nitrite production. The administration of the pet ether fraction for 45 d to streptozotocin-induced diabetic rats revealed an improved lipid profile. Cuminaldehyde and cuminol were identified as potent Insulinotrophic components. Cuminaldehyde and cuminol (25 μg/ml) showed 3·34- and 3·85-fold increased Insulin secretion, respectively, than the 11·8 mm-glucose control. The Insulinotrophic action of both components was glucose-dependent and due to the closure of the ATP-sensitive K (K⁺-ATP) channel and the increase in intracellular Ca²⁺ concentration. An inhibitor of Insulin secretion with potent β-cell protective action was also isolated from the same pet ether fraction. In conclusion, C. cyminum was able to lower blood glucose without causing hypoglycaemia or β-cell burn out. Hence, the commonly used spice, C. cyminum, has the potential to be used as a novel Insulinotrophic therapy for prolonged treatment of diabetes.
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Insulin Secretagogue alpha glucosidase and antioxidant activity of some selected spices in streptozotocin induced diabetic rats
Plant Foods for Human Nutrition, 2011Co-Authors: Swapnil B. Patil, Chaitanya R Kulkarni, Varsha Adhikrao Ghadyale, Shreehari Subhash Taklikar, Akalpita U. ArvindekarAbstract:Spices are extensively used to enhance the taste and flavor of foods and are known to possess several medicinal properties. Myristica fragrans, Parmelia perlata, Illicium verum, Trachyspermum copticum and Myristica malabarica, the commonly used spices in India were assessed for antidiabetic activity in streptozotocin induced diabetic rats. In the in vitro Insulin secretion studies on isolated islets of Langerhans, M. fragrans, T. copticum and M. malabarica showed dose dependent Insulin secretion. At 1 mg/ml, P. perlata showed significant in vitro alpha-glucosidase inhibitory activity with IC(50) value of 0.14 mg/ml followed by M. malabarica (0.64 mg/ml), I. verum (0.67 mg/ml), M. fragrans (0.85 mg/ml) and T. copticum (0.92 mg/ml). The DPPH free radical scavenging activity of the extracts at a concentration of 1 mg/ml was as M. malabarica (90.45%), M. fragrans (89.89%), I. verum (87.22%), P. perlata (76.70%) and T. copticum (38.14%). P. perlata showed the highest phenolic content (i.e., 118.5 mg gallic acid equivalents/g) followed by M. malabarica (84.13 mg gallic acid equivalents/g). M. malabarica showed the highest flavonoid content (i.e., 38.35 mg quercetin equivalents/g). Regular use of these spices may prevent postprandial rise in glucose levels through inhibition of intestinal alpha-glucosidase and may maintain blood glucose level through Insulin Secretagogue action.