Unraveling the regulatory landscape of Parkinson disease: A molecular symphony of miRNAs, transcription factors, and high-risk genes.

MicroRNAs (miRNAs) have emerged as critical regulators of post-transcriptional gene expression, impacting various biological processes (development, differentiation, and progression). In medicine, miRNAs are promising diagnostic biomarkers for neurodegenerative diseases, including Parkinson's disease (PD). The current study aims at exploring the role of miRNAs and transcription factors (TFs) in regulating genes-associated with PD. Deploying bioinformatics tools, the study identifies specific miRNAs and TFs involved in PD and their potential connections to the organ-disease junction. Notably, certain miRNAs are found to be highly expressed in brain, than compared to blood. Furthermore, the study explores the expression patterns of PD-related genes in different regions of the brain and attempts to construct complex network of interactions contributing to PD pathogenesis. Additionally, the regulatory relationship of two miRNAs namely hsa-miR-375-3p and hsa-miR-423-3p with TFs are well examined. Overall, the study provides a comprehensive moon-shot view of the molecular aspects of PD and their potential therapeutic targets which could be further used as diagnostic biomarkers in early detection, drug design and development attributing towards precision medicine.

Targeting Imd pathway receptor in Drosophila melanogaster and repurposing of phyto-inhibitors: structural modulation and molecular dynamics.

Dysbiosis is a major cause of disease in an individual, generally initiated in the gastrointestinal tract. The gut, also known as the second brain, constitutes a major role in immune signaling. To study the immunity cascade, the Drosophila model was considered targeting the Imd pathway receptor (2F2L) located in the midgut. This receptor further initiates the immune signaling mechanism influenced by bacteria. To inhibit the Imd pathway, the crystal structure of Imd with PDB: 2F2L was considered for the screening of suitable ligand/inhibitor. In light of our previous studies, repurposing of anti-diabetic ligands from the banana plant namely lupeol (LUP), stigmasterol (STI), ß-sitosterol (BST) and umbelliferone (UMB) were screened. This study identifies the potential inhibitor along with the tracheal toxin (TCT), a major peptidoglycan constituent of microbes. The molecular docking and molecular dynamics simulation of complexes 2F2L-MLD, 2F2L- CAP, 2F2L-LUP, 2F2L-BST, 2F2L-STI and 2F2L-UMB elucidates the intermolecular interaction into the inhibitory property of ligands. The results of this study infer LUP and UMB as better ligands with high stability and functionality among the screened candidates. This study provides insights into the dysbiosis and its amelioration by plant-derived molecules. The identified drugs (LUP & UMB) will probably act as an inhibitor against microbial dysbiosis and other related pathogenesis (diabetes and diabetic neuropathy). Further, this study will widen avenues in fly biology research and which could be used as a therapeutic model in the rapid, reliable and reproducible screening of phytobiologics in complementary and alternative medicine for various lifestyle associated complications.

In vitro and in vivo inhibitory effects of Tabernaemontana alternifolia against Naja naja venom.

BACKGROUND: Tabernaemontana alternifolia root is traditionally used and practiced among few Indian tribes as an antidote for snakebites. OBJECTIVE: To combat and neutralize Naja naja venom using methanolic root extract of Tabernaemontana alternifolia and to explore its efficacy on venom biomarkers in search of newer herbal antidote or first-aid-point of care for therapeutics.Materialization.Pharmacological activities such as fibrinogenolytic, direct and indirect hemolytic activities for the neutralization of the venom were evaluated. Lethal toxicity annulation studies were performed using the murine model by pre-incubation and post-treatment protocols. Further, the neutralization of edema and myotoxicity were also evaluated. RESULTS: Electrophoretic analysis revealed that the complete neutralization of fibrinogen degradation was observed at 1:10 (w/w) (venom to extract). T. alternifolia exhibited an effective dose (ED50) value of 87.20 µg/mL for venom-induced hemolysis. Venom at 2 µg concentration produced 11 mm of hemolytic radiance and was neutralized at 1:20 (w/w) venom to extract concentration. The survival time and the neurotoxic symptoms in mice were concluded to be delayed by both the methods of lethal toxicity inhibition using methanol extract. The edema ratio reduced the venom to extract ratio of 1:20 (w/w) from 173 ± 45% to 133.61% when subjected to 5 µg of venom concentration. The plant extract significantly neutralized the myotoxic activity. CONCLUSION: T. alternifolia methanolic root extract could be a potent contributor in the effective treatment of N. naja venom-induced toxicity.

Bungarus caeruleus venom neutralization activity of Azima tetracantha Lam. Extract.

Azima tetracantha Lam. is native to Africa and India. The plant and its parts are used for treating various ailments including snake bites. The different concentrations of ethyl acetate leaf extract of A. tetracantha were used to neutralize the toxic effect of venom through dose dependent enzyme studies and in vivo studies. The extract was able to neutralize the 5' nucleotidase, phospholipase A2, Phosphodiesterae, phosphomonoesterase, acetylcholinesterase and hyaluronidase in a dose dependent manner with concentrations ranging from 43.98 -340.1 µg/mL of extract. The extract could retain the lysis of fibrinogen at the concentration of 1:10 (venom: extract, w/w) and also the lysis of lecithin was reduced at a concentration of 1:25 (venom: extract, w/w). The extract was able to neutralize the LD50 of venom in both mice and embryo and also reduce the myotoxic and edema properties of the venom in mice models. The venom did not show any procoagulant and hemorrhagic effect. The leaf extract possess adequate compounds/phytochemicals that could neutralize the toxic properties/activity of the B. caeruleus venom.

Acrylamide Induced Toxicity and the Propensity of Phytochemicals in Amelioration: A Review.

Acrylamide is widely found in baked and fried foods, produced in large amount in industries and is a prime component in toxicity. This review highlights various toxicities that are induced due to acrylamide, its proposed mode of action including oxidative stress cascades and ameliorative mechanisms using phytochemicals. Acrylamide formation, the mechanism of toxicity and the studies on the role of oxidative stress and mitochondrial dysfunctions are elaborated in this paper. The various types of toxicities caused by Acrylamide and the modulation studies using phytochemicals that are carried out on various type of toxicity like neurotoxicity, hepatotoxicity, cardiotoxicity, immune system, and skeletal system, as well as embryos have been explored. Lacunae of studies include the need to explore methods for reducing the formation of acrylamide in food while cooking and also better modulators for alleviating the toxicity and associated dysfunctions along with identifying its molecular mechanisms.

Phyto anti-biofilm elicitors as potential inhibitors of Helicobacter pylori.

Helicobacter pylori (H. pylori) infection is a global public health concern. Due to its high adaptability in various adverse environments (temperature, pH, adhesion, phenotypic forms), targeting the bacterium is quite challenging. Moreover, due to its high persistence, decreased patience compliance and emerging antibiotic resistance, researchers have been forced to search for novel candidates with lesser or no side effects. Hence, in the current study, phytobioactives have been screened for its anti-biofilm attributes against H.pylori. Gastric biopsy samples have been screened using confirmatory techniques (microbiological, biochemical and molecular) for their virulent and non-virulent biomarkers. Physico-nutritive parameters were standardized. H. pylori biofilms were assessed using microtitre plate assay. Biofilms' biomass and exopolysaccharide have been evaluated using crystal violet and ruthenium red staining, respectively. Anti-biofilm screening was performed using potent aqueous phytochemicals namely Acorus calamus, Colocasia esculenta and Vitex trifolia. The results indicated the confluent growth of the H. pylori biofilms confirmed through genotyping and grew best at 37 °C for 72 h at a pH of 7.5 on polystyrene plates. Further, among the phytochemicals tested, Acorus calamus exhibited the highest H. pylori anti-biofilm activity via a dose-dependent pattern. The overall observations of the study will pave way for newer approaches to understand and combat bacterial pathogenesis and will contribute towards better health and hygiene.

Adsorption of ethidium bromide from aqueous solution onto nutraceutical industrial fennel seed spent: Kinetics and thermodynamics modeling studies.

Dye pollutants from research laboratories are one of the major sources for environmental contamination. In the present study, a nutraceutical industrial fennel seed spent (NIFSS) was explored as potential adsorbent for removal of ethidium bromide (EtBr) from aqueous solution. The adsorbent was characterized by scanning electron microscopy (SEM) and Fourier transform infrared spectroscopy (FTIR). Through batch experiments, the operating variables like initial dye concentration, adsorbent dosage, temperature, contact time, and pH were optimized. Equilibrium data were analyzed using three number of two-parameter and six number of three-parameter isotherm models. The adsorption kinetics was studied using pseudo-first order and pseudo-second order. The diffusion effects were studied by film diffusion, Webber-Morris, and Dumwald-Wagner diffusion models. The thermodynamic parameters; change in enthalpy (ΔHº), entropy (ΔSº), and Gibbs free energy (ΔGº) of adsorption system were also determined and evaluated.

Investigation of Antihyperglycaemic Activity of Banana (Musa sp. Var. Nanjangud rasa bale) Flower in Normal and Diabetic Rats.

BACKGROUND: The vital enzymes of starch digestion and absorption are intestinal α-glucosidases and their inhibition improves postprandial hyperglycaemia, constituting an effective mode of therapy in diabetes. OBJECTIVES: The present study was designed to assess the inhibitory potential of ethanol extract of banana flower (EF) on mammalian α-glucosidases and its pharmacological effects on postprandial hyperglycaemia in normal and alloxan-induced diabetic rats. MATERIALS AND METHODS: EF was evaluated for its inhibitory potential and mode of inhibition on mammalian α-glucosidases. Further, the role of EF and its constituents Umbelliferone (C1) and Lupeol (C2) on glucose uptake using isolated rat hemi-diaphragm and insulinotropic activity using RINm5F (rat insulinoma) cell lines were determined. The phytocomponents in EF were also evaluated using GC-MS. RESULTS: EF illustrated a dose-dependent inhibition for rat intestinal sucrase, maltase and p-nitrophenyl-α-D-glucopyranoside (pNPG) hydrolysis (IC50 values: 18.76±0.22, 25.54±0.10 and 76.42±1.12 µg/ml, respectively) and the mode of inhibition was non-competitive with low Ki values. Oral administration (100-200 mg/kg b.wt.) of EF significantly improved the maltose/glucose-induced postprandial hyperglycaemia in normal and alloxan-induced diabetic rats. EF, C1 and C2 exhibited stimulation of glucose uptake and a dose-dependent glucose-induced insulin secretion at both 4.5 and 16.7 mM glucose concentrations. Further, GC-MS analysis revealed significant levels of steroids (25.61%), diazoprogesterone (21.31%), sesquiterpene (11.78%) and other phytocomponents. CONCLUSION: EF inhibited α-glucosidases besides promoting glucose uptake and insulin secretion, resulting in antihyperglycaemic effect determining EF as a potent anti-diabetic agent.Abbreviations used: mg/dl: milligramsper deciliter, mM: millimolar, b.wt.: body weight.

Assessment of Nutritional Quality and Global Antioxidant Response of Banana (Musa sp. CV. Nanjangud Rasa Bale) Pseudostem and Flower.

BACKGROUND: The assessment of the nutritional composition and phytochemical screening of banana pseudostem (PB) and flower (FB) advocate this nonconventional food source for routine consumption, considering its various health benefits. OBJECTIVES: The aim is to assess the proximate nutrient composition, fatty acids, minerals, amino acid profile, and global antioxidant response (GAR) of PB and FB. METHODS: Standard analytical procedures were used to determine the nutritional quality and GAR of PB and FB. RESULTS: The chemical analysis illustrated that functional profile (water holding capacity, oil holding capacity, swelling power, and solubility), and proximate (ash, moisture, protein, fat, dietary fiber, and carbohydrate) contents were substantially high in FB than PB. With a well-proportionate amino acid profile, PB (0.56) and FB (0.54) comprised of a high ratio of essential to nonessential amino acids than those of FAO/WHO requirement (0.38). The mineral analysis revealed that PB and FB were rich in macro and micro minerals in the order K > Ca > Mg > P > Na and K > Mg > Na > Ca > P, respectively. Linoleic acid was found to be the major component in PB and FB. Besides, total antioxidant activity conducted for PB and FB by GAR method, measuring both bio-accessible and insoluble fractions, revealed that the soluble fraction fared better than the chemical extracts. CONCLUSION: The results revealed high nutritional qualities of the byproducts of banana and the low cost of its production promotes their use as a prospective nonconventional food resource with high nutraceutical value. SUMMARY: AOAC: Association of Analytical CommunitiesFAO/WHO: Food and Agriculture Organization of the United Nations/World health organization Abbreviations Used: Banana flower was more potent than banana pseudostem in terms of its nutritional quality and total antioxidant capacity affirming their usefulness (of both the secondary products) in the pharmaceutical sector as a nutritional supplement due to the health-related properties of dietary fibre and associated bioactive compounds.

The effect of a plant extract enriched in stigmasterol and ß-sitosterol on glycaemic status and glucose metabolism in alloxan-induced diabetic rats.

Banana is an extensively cultivated plant worldwide, mainly for its fruit, while its ancillary product, the banana pseudostem, is consumed as a vegetable and is highly recommended for diabetics in the traditional Indian medicine system. The present study was aimed at elucidating the mechanism of antihyperglycaemia exerted by the ethanol extract of banana pseudostem (EE) and its isolated compounds viz., stigmasterol (C1) and ß-sitosterol (C2), in an alloxan-induced diabetic rat model. Diabetic rats which were administered with C1, C2 and EE (100 and 200 mg per kg b. wt.) for 4 weeks showed reduced levels of fasting blood glucose and reversal of abnormalities in serum/urine protein, urea and creatinine in diabetic rats compared to the diabetic control group of rats. Diabetic symptoms such as polyphagia, polydipsia, polyuria, urine glucose and reduced body weight were ameliorated in the diabetic group of rats fed with EE, C1 and C2 (100 mg per kg b. wt., once daily) for 28 days. The levels of insulin and Hb were also increased, while the HbA1c level was reduced. The altered activities of hepatic marker enzymes viz., aspartate transaminase (AST), alanine transaminase (ALT) and alkaline phosphatase (ALP); glycolytic enzyme (hexokinase); shunt enzyme (glucose-6-phosphate dehydrogenase); gluconeogenic enzymes (glucose-6-phosphatase, fructose-1,6-bisphosphatase and lactate dehydrogenase) and pyruvate kinase were significantly reverted to normal levels by the administration of EE, C1 and C2. In addition, increased levels of hepatic glycogen and glycogen synthase and the corresponding decrease of glycogen phosphorylase activity in diabetic rats illustrated the antihyperglycaemic potential of EE and its components. The histological observations revealed a marked regeneration of the ß-cells in the drug treated diabetic rats. These findings suggest that EE might exert its antidiabetic potential in the presence of C1 and C2, attributable to the enhanced glycolytic activity, besides increasing the hepatic glucose utilization in diabetic rats by stimulating insulin secretion from the remnant ß-cells.

Correction: Assessment of In Vivo Antidiabetic Properties of Umbelliferone and Lupeol Constituents of Banana (Musa sp. var. Nanjangud Rasa Bale) Flower in Hyperglycaemic Rodent Model.

[This corrects the article DOI: 10.1371/journal.pone.0151135.].

Evaluation of adhesive and anti-adhesive properties of Pseudomonas aeruginosa biofilms and their inhibition by herbal plants.

BACKGROUND AND OBJECTIVES: Adhesion and colonization are prerequisites for the establishment of bacterial pathogenesis. The biofilm development of Pseudomonas aeruginosa was assessed on adhesive surfaces like dialysis membrane, stainless steel, glass and polystyrene. MATERIALS AND METHODS: Microtiter plate biofilm assay was performed to assess the effect of nutrient medium and growth parameters of P. aeruginosa. Further, its growth on adhesive surfaces namely hydrophilic (dialysis membrane) and hydrophobic (polystyrene plate, square glass and stainless steel coupon) was assessed. The exopolysaccharide (EPS) was quantified using ruthenium red microplate assay and microscopic analysis was used to observe P. aeruginosa biofilm architecture. The anti-biofilm activity of herbal extracts on mature P. aeruginosa was performed. RESULTS: The formation of large scale biofilms on dialysis membrane for 72 h was proved to be the best surface. In microscopic studies, very few exopolysaccaride fibrils, indicating a rather loose matrix was observed at 48 h. Further, thick exopolysaccaride, indicated higher adhesive properties at 72 h which is evident from ruthenium red staining. Among the plant extract used, Justicia wynaadensis leaf and Aristolochia indica (Eswari) root extract showed significant reduction of anti-biofilm activity of 0.178 OD and 0.192 OD in inhibiting mature biofilms at 0.225 OD respectively, suggesting the possible use of these extracts as efficient anti-adhesive and biofilm-disrupting agents with potential applications in controlling biofilms on surfaces. CONCLUSION: Our study facilitates better understanding in the development of P. aeruginosa biofilms on different food processing and clinical surfaces ultimately taking care of food safety and hygiene.

Therapeutic Potentials of Triterpenes in Diabetes and its Associated Complications.

Diabetes is a major chronic metabolic disorder globally and around of 285 million people are affected by the disease and the number is expected to double in the next two decades. The major focus of anti-diabetic therapies is to enhance insulin production, sensitivity and/or reduce the blood glucose level. Although several synthetic drugs have been developed as antidiabetic agents but their utility has been hampered due to their side effects and poor efficacy. In this scenario, research on natural products has been gained importance due their safety profile in toxicity studies. Terpenoids belong to an important class of natural products and several terpenoids have been reported as antidiabetic agents. Some of them are under various stages of pre-clinical and clinical evaluation to develop them as antidiabetic agents. These agents can inhibit enzymes responsible for the development of insulin resistance, normalization of plasma glucose and insulin levels and glucose metabolism. Triterpenes can act as promising agents in the treatment of diabetic retinopathy, neuropathy and nephropathy or in impaired wound healing by inhibiting several pathways involved in the diabetes and associated complications. However, efforts in understanding the biological actions and clinical studies involving the applications of triterpenes in treating diabetes are very limited. Hence, special attention is imperative to explore the therapeutic potential of these compounds and provide new information to the scientific community. This review aims to provide the recent advances in triterpenes chemistry, its derivatives, biological interventions and its therapeutic applications with special emphasis on diabetes and its associated disorders.

Assessment of In Vivo Antidiabetic Properties of Umbelliferone and Lupeol Constituents of Banana (Musa sp. var. Nanjangud Rasa Bale) Flower in Hyperglycaemic Rodent Model.

Banana is an extensively cultivated plant worldwide, mainly for its fruit, while its ancillary product, the banana flower is consumed as a vegetable and is highly recommended for diabetics in the traditional Indian medicine system. This study is based on an investigation of the in vivo antihyperglycaemic activity of Umbelliferone (C1) and Lupeol (C2) isolated from the ethanol extract of banana flower (EF) in alloxan induced diabetic rat model. Diabetic rats which were administered with C1, C2 and EF (100 and 200 mg/kg b. wt.) for 4 weeks showed deterioration in fasting hyperglycaemia and reversal of abnormalities in serum/urine protein, urea and creatinine, when compared to the diabetic control group of rats. The diabetic group of rats fed with EF, C1 and C2 (100 mg/kg b. wt.) once daily, for a period of 28 days resulted in a significant reduction of diabetic symptoms viz., polyphagia, polydipsia, polyuria and urine sugar together with an improved body weight. HbA1c extent was reduced whereas levels of insulin and Hb were increased. Both the extract and compounds wielded positive impacts in diabetic rats by reversal of altered activities of hepatic marker enzymes viz., aspartate transaminase (AST), alanine transaminase (ALT), alkaline phosphatase (ALP); glycolytic enzyme (hexokinase); shunt enzyme (glucose-6-phosphate dehydrogenase); gluconeogenic enzymes (glucose-6-phosphatase, fructose-1,6-bisphosphatase, lactate dehydrogenase) and pyruvate kinase. The characteristic diabetic complications such as hypercholesterolemia and hypertriacylglycerolemia also significantly reverted to normal in the serum/liver of diabetic rats. Besides these, the treatment increased the activities of enzymatic and non-enzymatic antioxidants in the serum and liver. The histological observations revealed a marked regeneration of the ß-cells in the drug treated diabetic rats. In conclusion, the present study illustrates that EF, C1 and C2 enhances the glycolytic activities, besides increasing the hepatic glucose utilization in diabetic rats by stimulating insulin secretion from the remnant ß-cells along with potential enzymatic and non-enzymatic antioxidant activities.

3,5-Disubstituted Isoxazole Derivatives: Potential Inhibitors of Inflammation and Cancer.

The products of arachidonic acid metabolism by lipoxygenase (LOX) and cyclooxygenase (COX) significantly contribute to inflammation and carcinogenesis. Particularly, overproduction of leukotrienes and prostaglandins contribute to tumor growth by inducing formation of new blood vessels that sustain tumor cell viability and growth. Hence, search for novel anticancer drug via inhibition of LOX and COX enzymes constitutes an impressive strategy till date. In this context, a series of isoxazole derivatives were synthesized and screened for their anti-inflammatory activity via LOX and COX inhibition. Among these, 3-(3-methylthiophen-2-yl)-5-(3,4,5-trimethoxyphenyl)isoxazole (2b) showed significant inhibitory activity toward LOX and COX-2. Additionally, 2b showed a good inhibition of tumor growth, peritoneal angiogenesis, and ascite formation in Ehrlich ascites carcinoma (EAC) cell mouse model. Further, the in silico molecular studies also revealed that the compound 2b binds to the catalytic domain of LOX and COX-1 and COX-2 strongly with high atomic contact energy (ACE) score compared to standard drug. These initial pharmacological data support the fact that the compound 2b serves as the basis in developing anti-inflammatory and anticancer agents.

Evaluating the inhibitory potential of Withania somnifera on platelet aggregation and inflammation enzymes: An in vitro and in silico study.

Context Withania somnifera (L.) Dunal is traditionally used for treating various ailments, but lacks scientific evaluation. Objective This study evaluates Withania somnifera (WS) for its effect on platelet activity and inflammatory enzymes. Materials and methods Aqueous and ethanolic (1:1) leaf extracts were subjected to in vitro indirect haemolytic activity using Naja naja venom, human platelet aggregation was quantified for lipid peroxidation using arachidonic acid (AA) as agonist and 5-lipoxygenase (5-LOX) levels were determined using standard spectrometric assays. Further, molecular docking was performed by the ligand fit method using molegro software package (Molegro ApS, Aarhus, Denmark). Results The study found that aqueous and ethanol extracts have very negligible effect (15%) with an IC50 value of 13.8 mg/mL on PLA2 from Naja naja venom. Further, extracts of WS also had very little effect (18%) with an IC50 value of 16.6 mg/mL on malondialdehyde (MDA) formation. However, a 65% inhibition of 5-LOX with an IC50 value of 0.92 mg/mL was observed in 1:1 ethanol extracts. The same was evident from SAR model with the active ingredient withaferin A binding predominantly on Phe 77, Tyr 98, Arg 99, Asp 164, Leu 168, Ser 382, Arg 395, Tyr 396 and Tyr 614 with an atomic contact energy value of -128.96 compared to standard phenidone (-103.61). Thus, the current study validates the application of WS for inflammatory diseases. Conclusion This study reveals the inhibitory potential of W. somnifera on inflammatory enzymes and platelet aggregation. Thus, WS can serve as a newer, safer and affordable medicine for inflammatory diseases.

Anti-Cancer Activity of 2,4-Disubstituted Thiophene Derivatives: Dual Inhibitors of Lipoxygenase and Cyclooxygenase.

2,4-Disubstituted thiophene derivatives were synthesized and assessed for antiinflammatory and anti-cancer activities by targeting two important enzymes of the arachidonic acid metabolism. Both lipoxygenase and cyclooxygenase enzymes play vital role in chronic inflammation and carcinogenesis. Previous studies have proved that COX-2 and 5-LOX are highly activated in various types of cancers; hence inhibition of these clinically important enzymes constitutes the essential criterion for the suppression of tumor progression and metastasis. Among the tested derivatives, 2d and 2g compounds emerged as potent inhibitors of lipoxygenase and cyclooxygenase enzymes. The potent inhibitor of cyclooxygenase was further tested for in vitro cytotoxicity on cervical cancer (HeLa) cells and in vivo tumor model studies using EAT bearing mice where 2-(3,4,5- trimethoxyphenyl)-4-(N-methylindol-3-yl) thiophene (2g) showed eloquent activity. Further, in silico modeling results confirmed the active catalytic ligand binding pockets, which is evident from higher atomic contact energy values of 2d and 2g than compared to standard drug. Thus, 2g may find better application in management of inflammation and in proapoptotic therapeutic engineering.

Investigation of antihyperglycaemic activity of banana (Musa sp. var. Nanjangud rasa bale) pseudostem in normal and diabetic rats.

BACKGROUND: Postprandial hyperglycaemia in diabetes could be ameliorated by inhibiting intestinal α-glucosidases, responsible for starch hydrolysis and its absorption. Different parts of banana have been in use in conventional medicinal formulations since ancient times. Its role as an antihyperglycaemic agent has also been studied. This study was aimed at explaining the mechanism of hypoglycaemic effect by ethanol extract of banana pseudostem (EE). Additionally, studies on the active components involved in the effect have also been attempted. RESULTS: EE significantly inhibited mammalian intestinal α-glucosidases and yeast α-glucosidase (IC50 , 8.11 ± 0.10 µg mL(-1) ). The kinetic studies showed that EE inhibited sucrase, maltase and and p-nitrophenyl-α-d-glucopyranoside hydrolysis by mixed-type inhibition. Further, in vivo studies identified that the oral administration (100-200 mg kg(-1) body weight) of EE significantly suppressed the maltose/glucose-induced postprandial plasma glucose elevation and wielded an antihyperglycaemic effect in normal and alloxan-induced diabetic rats. GC-MS analysis of EE revealed high levels of ß-sitosterol (29.62%), stigmasterol (21.91%), campesterol (10.85%) and other compounds. CONCLUSION: These findings suggest that EE might exert an anti-diabetic effect by inhibition of α-glucosidases from the intestine, in turn suppressing the carbohydrate absorption into the bloodstream. Hence the results extend a foundation to the future prospects of the food-derived enzyme inhibitors in treatment of diabetes.

Synthesis, xanthine oxidase inhibition, and antioxidant screening of benzophenone tagged thiazolidinone analogs.

A series of novel 2-(diaryl methanone)-N-(4-oxo-2-phenyl-thiazolidin-3-yl)-acetamides were synthesized by various Schiff bases of (4-benzoyl-phenoxy)-aceto hydrazide with thioglycolic acid. The structures of the newly synthesized compounds were confirmed by IR, (1) H NMR, mass spectra, and C, H, N analysis. Further, all the synthesized compounds 9a-n were evaluated for xanthine oxidase (XO) inhibition and antioxidant properties. Among all the tested compounds, 9f, 9m, and 9n demonstrated potent XO inhibition of 52, 76, and 26%, respectively, compared to the standard drug allopurinol, which is evident from in vitro and in silico analysis. On the other hand, compounds 9c, 9d, and 9k exhibit potent antioxidant properties.

Synthesis, antioxidant, and xanthine oxidase inhibitory activities of 5-[4-[2-(5-ethyl-2-pyridinyl)ethoxy]phenyl]methyl]-2,4-thiazolidinedione derivatives.

Xanthine oxidase (XO) is a complex metalloflavoprotein, the overproduction of which usually leads to a pathological condition called gout. The XO inhibitors may prove to be promising antigout agents. The XO generates superoxide anions and H2O2 for the self-defense system of the organism. Abnormal production of this superoxide (reactive oxygen species) is responsible for a number of complications including inflammation, metabolic disorder, cellular aging, reperfusion damage, atherosclerosis, and carcinogenesis. In this paper, we report the synthesis of N-substituted analogs of thiazolidinedione derivatives as effective and new class of XO inhibitors and also as antioxidant agents. Among all the compounds in the series, compound 2i produced relatively better activity against human milk XO (72% inhibition), which was also supported by docking studies.