Exposure to Electromagnetic Fields from Mobile Phones and Fructose consumption Coalesce to Perturb Metabolic Regulators AMPK/SIRT1-UCP2/FOXO1 in Growing Rats.

Objective: In this study, the combined effect of two stressors, namely, electromagnetic fields (EMFs) from mobile phones and fructose consumption, on hypothalamic and hepatic master metabolic regulators of the AMPK/SIRT1-UCP2/FOXO1 pathway were elucidated to delineate the underlying molecular mechanisms of insulin resistance.

Methods: Weaned Wistar rats (28 days old) were divided into 4 groups: Normal, Exposure Only (ExpO), Fructose Only (FruO), and Exposure and Fructose (EF). Each group was provided standard laboratory chow for 8 weeks Additionally, the control groups, namely, the Normal and FruO groups, had unrestricted access to drinking water and fructose solution (15%), respectively.

Characterizing (un)binding mechanism of USP7 inhibitors to unravel the cause of enhanced binding potencies at allosteric checkpoint.

The ability to predict the intricate mechanistic behavior of ligands and associated structural determinants during protein-ligand (un)binding is of great practical importance in drug discovery. Ubiquitin specific protease-7 (USP7) is a newly emerging attractive cancer therapeutic target with bound allosteric inhibitors. However, none of the inhibitors have reached clinical trials, allowing opportunities to examine every aspect of allosteric modulation.

Guava Leaf Extract Suppresses Fructose Mediated Non-Alcoholic Fatty Liver Disease in Growing Rats.

Purpose: Fructose is highly lipogenic, and its unhindered ingestion by children and adolescents is understood to induce hypertriglyceridemia and non-alcoholic fatty liver disease (ped-NAFLD) that is till date managed symptomatically or surgically. The aim of the present study was to investigate the potential of hydroethanolic extract of leaves of Guava (PG-HM) to suppress the alterations in the hepatic molecular signals due to unrestricted fructose (15%) drinking by growing rats.

Methods: Weaned rats (4 weeks old) in control groups had access to fructose drinking solution (15%) for four (4FDR) or eight (8FDR) weeks, ie, till puberty or early adulthood, respectively, while treatment groups (4PGR, 8PGR) additionally received PG-HM (500 mg/kg, po).

Simultaneous exposure to electromagnetic field from mobile phone and unimpeded fructose drinking during pre-, peri-, and post-pubertal stages perturbs the hypothalamic and hepatic regulation of energy homeostasis by early adulthood: experimental evidence.

The present-day children-adolescents ubiquitously use the mobile phones and unrestrictedly consume fructose-laden diet. Unfortunately, a rise in the incidence of insulin resistance and fatty liver syndrome in young adults has also been recorded. To delineate a possible correlate, the effect of exposure to electromagnetic field (EMF) from the mobile phone and unrestricted fructose intake during pre-, peri-, and post-pubertal stages of development on orexigenic and anorexigenic signals arising from the hypothalamus and liver of rats is investigated here.

Molecular and Metabolic Markers of Fructose Induced Hepatic Insulin Resistance in Developing and Adult Rats are Distinct and Aegle marmelos is an Effective Modulator.

The time course of pathogenesis of fructose mediated hepatic insulin resistance (HepIR) is not well-delineated and we chronicle it here from post-weaning to adulthood stages. Weaned rats were provided for either 4 or 8 weeks, i.e.

Molecular dynamics simulation reveals the possible druggable of USP7.

The plasticity in Ubiquitin Specific Proteases (USP7) inducing conformational changes at important areas has highlighted an intricate mechanism, by which USP7 is regulated. Given the importance of USP7 in oncogenic pathways and immune-oncology, identification of USP7 inhibitors has attracted considerable interest. Despite substantial efforts, the discovery of deubiquitinases (DUBs) inhibitors, knowledge of their binding site and understanding the possible mechanism of action has proven particularly challenging.

Synthesis, biological evaluation and docking study of N-(2-(3,4,5-trimethoxybenzyl)benzoxazole-5-yl) benzamide derivatives as selective COX-2 inhibitor and anti-inflammatory agents.

A series of N-(2-(3,4,5-trimethoxybenzyl)-benzoxazole-5-yl)benzamide derivatives (3a-3n) was synthesized and evaluated for its in vitro inhibitory activity against COX-1 and COX-2. The compounds with considerable in vitro activity (IC < 1 µM), were evaluated in vivo for their anti-inflammatory and ulcerogenic potential. Out of the fourteen newly synthesized compounds; 3b, 3d, 3e, 3h, 3l and 3m were found to be most potent COX-2 inhibitors in in vitro enzymatic assay with IC in the range of 0.

Development and validation of High-performance Thin-layer Chromatography Method for Simultaneous Determination of Polyphenolic Compounds in Medicinal Plants.

Context: Quantitative standardization of plant-based products is challenging albeit essential to maintain their quality.

Aims: This study aims to develop and validate high-performance thin-layer chromatography (HPTLC) method for the simultaneous determination of rutin (Ru), quercetin (Qu), and gallic acid (Ga) from Linn. (PG) and (L.

Aegle marmelos impedes onset of insulin resistance syndrome in rats provided with drinking fructose from weaning to adulthood stages of development - a mechanistic study.

In this study, we explored the effect of aqueous extract of leaves of Aegle marmelos (AM) on hepatic carbohydrate metabolism and insulin downstream signalling in rats given fructose (15%) in drinking water from weaning to adulthood. Wistar albino rats (4 weeks old) were randomly divided into normal control (NC), fructose control (FC), and treatment (AMT) groups and were fed for a period of 8 weeks the following diets: chow + water, chow + fructose (15%), and chow + fructose (15%) + AM (500 mg/kg per day, p.o.

Investigation of anti-asthmatic potential of Kanakasava in ovalbumin-induced bronchial asthma and airway inflammation in rats.

Ethno-pharmacological Relevance: Kanakasava is an Indian traditional Ayurvedic formulation containing Datura (Datura metel), Vasaca (Adhatoda vasica), Dhataki (Woodfordia fruticosa) and Grape (Vitis vinifera) extracts as major constituents and used to treat pulmonary diseases including coughing, breathing difficulty and asthma. The present study was designed to assess the safety and therapeutic efficacy of Kanakasava against ovalbumin-induced bronchial asthma and related airway inflammation in rats due to lack of evidence based therapeutic efficacy data.

Material And Methods: Male wistar rats were sensitized with allergen (ovalbumin, 40mg/rat+aluminum hydroxide, 2.

Cardioprotective effects of rutin via alteration in TNF-α, CRP, and BNP levels coupled with antioxidant effect in STZ-induced diabetic rats.

Diabetic cardiomyopathy (DCM) is a dreadful complication of diabetes responsible for 80 % mortality in diabetic patients, but unfortunately its pharmacotherapy is still incomplete. Rutin is a naturally occurring flavonoid having a long history of use in nutritional supplements for its action against oxidative stress, inflammation, and hyperglycemia, the key players involved in the progression of DCM, but remains unexplored for its role in DCM. This study was conducted to address this lacuna.

Zingiber officinale attenuates retinal microvascular changes in diabetic rats via anti-inflammatory and antiangiogenic mechanisms.

Purpose: Diabetic retinopathy is a common microvascular complication of long-standing diabetes. Several complex interconnecting biochemical pathways are activated in response to hyperglycemia. These pathways culminate into proinflammatory and angiogenic effects that bring about structural and functional damage to the retinal vasculature.

Pharmacodynamic Study of Interaction of Aqueous Leaf Extract of Psidium Guajava Linn. (Myrtaceae) with Receptor Systems Using Isolated Tissue Preparations.

The present study investigates the interaction of aqueous leaf extract of Psidium guajava with muscarinic, serotonergic and adrenergic receptor system using isolated rat ileum, gastric fundus and trachea, respectively. The concentration-dependent contractile response of aqueous leaf extract of Psidium guajava was parallel and rightward of standard agonists, ACh and 5-HT indicating agonistic activity on muscarinic and serotonergic receptor systems. The inhibition of aqueous leaf extract of Psidium guajava mediated contractions in presence of atropine (10(-7) M) and ketanserin (10(-6) M) confirmed the activity.

Genistein ameliorates cardiac inflammation and oxidative stress in streptozotocin-induced diabetic cardiomyopathy in rats.

The present study was undertaken to evaluate the protective effects of genistein against cardiac inflammation and oxidative stress in streptozotocin (STZ) (45 mg/kg body weight)-induced diabetic rats. genistein (300 mg/kg/day) was administered orally for 24 weeks to STZ-induced diabetic rats. The effects of genistein on blood glucose, % glycosylated hemoglobin (HbA1c), C-reactive protein, tumor necrosis factor (TNF- α), transforming growth factor (TGF-β1), and total antioxidant were studied.

Interaction of aqueous leaf extract of Aegle marmelos (L.) Corr. with cholinergic, serotonergic and adrenergic receptors: an ex vivo study.

Objectives: The aim was to study interaction of aqueous leaf extract of Aegle marmelos (AM) with cholinergic, serotonergic, and adrenergic receptor systems using appropriate rat tissues-ileum, fundus and tracheal chain, respectively.

Materials And Methods: Cumulative concentration-response curves (CRC) were constructed at various doses on each tissue for AM and respective standard agonist. The CRC was again plotted in presence and absence of respective standard antagonist to confirm the interaction of receptor system and AM.

Qualitative and quantitative assessment of four marketed formulations of brahmi.

This study was conducted with the aim to compare two batches each of four popular commercial formulations of Bacopa monnieri (Brahmi), and report, if any, inter-batch variations. The formulations were procured from local market and analyzed for label specifications, uniformity of weight of capsule, identity, purity and strength parameters (total ash content test, acid insoluble ash content, water soluble extractive, alcohol soluble extractive, loss on drying). Bacoside A, one of the pharmacologically active saponin present in B.

Evaluation of wound healing potential of topical formulation of leaf juice of tridax procumbens L. In mice.

Tridax procumbens L. (Compositae) is a common weed that grows in the rice fields of India. Traditionally the juice from leaves of Tridax procumbens has been used for healing dermal wound.

Calotropis procera root extracts block VEGF-induced angiogenesis: quantitative analysis.

Angiogenesis is controlled by number of growth factors, including vascular endothelial growth factor (VEGF). Plant derived anti-angiogenic molecules acting via VEGF are being investigated for curtailing angiogenesis dependent diseases. In this study, methanolic (CM), n-hexane (CH), ethylacetate (CE) and water (CW) extracts of the roots of Calotropis procera were tested for anti-angiogenic activity.

Boswellic acid inhibits inflammatory angiogenesis in a murine sponge model.

The aim of the present study was to investigate the effects of boswellic acid (BA) on key components of inflammatory angiogenesis in the murine cannulated sponge implant angiogenesis model. Polyester-polyurethane sponges, used as a framework for fibrovascular tissue growth, were implanted in Swiss albino mice and BA (12.5 or 25mg/kg/day) was given through installed cannulas for nine days.

Cytotoxic and antitumor effects of brucine on Ehrlich ascites tumor and human cancer cell line.

Aims: Brucine (BRU), a natural plant alkaloid is reported to possess cytotoxic and antiproliferative activities. In this study we aimed to investigate its in vitro and in vivo antitumor and antiangiogenic effects.

Main Methods: Cell proliferation and viability was assessed using microculture tetrazolium tests (MTT).

Antitumor properties of Boswellic acid against Ehrlich ascites cells bearing mouse.

Boswellic acid (BA), a triterpene, isolated from Boswellia serrata (Burseraceae) has been found to possess potent anti-inflammatory and anti-cancer activity. The present study aimed at exploring the possible role of BA on ascites and solid Ehrlich tumor. Ascitic tumor development was evaluated 14 d after tumor implantation by quantification of the ascitic fluid volume whereas solid tumor was evaluated after 30 d tumor implantation by H&E and IHC.

2-Buten-4-Olide (2-B4O) suppresses feeding in neonate and developing rat pups.

The factors that control the satiety behavior and consequently the milk intake in neonates are complex. Mechanical stimulus of gastric filling and emptying are understood to be critical players, though not exclusive. Recently, sugar acid namely, 2-Buten-4-Olide (2-B4O) has been suggested as an endogenous satiety substance in studies conducted on adult rats and monkeys.

Anti-tumor studies with extracts of Calotropis procera (Ait.) R.Br. root employing Hep2 cells and their possible mechanism of action.

Anti-tumor potential of root extracts of Calotropis procera: methanolic extract (CM), hexane extract (CH), aqueous extract (CW) and ethylacetate extract (CE) and its possible mechanism against Hep2 cancer cells has been investigated. Cellular proliferation activities were assayed by tetrazolium bromide (MTT) colorimetry. Morphological changes of cancer cells were observed under inverted microscope and cell cycle parameters were determined by flow cytometry following propidium iodide staining.

Therapeutic potential of green tea: a new horizon in drug discovery.

Worldwide, tea is one of the most widely consumed beverages. Green tea consumption is especially popular in China, Japan and other Asian countries. It has been found to be rich in polyphenolic compounds, of which catechins are the major constituents.

Evaluation of the effect of Withania somnifera root extracts on cell cycle and angiogenesis.

In the Indian System of Medicine, the medicinal plant, Withania somnifera Dunal (Solanaceae) finds application for numerous ailments including cancer. This study explores the mechanism(s) underlying this property. The hydroalcoholic extract of the roots (WS) was partitioned between chloroform (WS-chloroform) and water (WS-water).