Resveratrol-loaded nanoemulsion gel system to ameliorate UV-induced oxidative skin damage: from in vitro to in vivo investigation of antioxidant activity enhancement.

In the present study resveratrol nanoemulsion gel was developed and optimized with the aim of enhancing the permeability and antioxidant activity against ultraviolet (UV)-induced oxidative skin damage. Droplet size, polydispersity index, drug permeation flux, permeability coefficient and drug deposition in skin of resveratrol-loaded nanoemulsion were found to be 65.00 ± 5.

Dynamics of Prolyl Hydroxylases Levels During Disease Progression in Experimental Colitis.

Hypoxia inducible factor (HIF)-prolyl hydroxylase (PHD) inhibitors are shown to be protective in several models of inflammatory bowel disease (IBD). However, these non-selective inhibitors are known to inhibit all the three isoforms of PHD, i.e.

Dichotomy of bisphenol A-induced expression of peroxisome proliferator-activated receptors in hepatic and testicular tissues in mice.

Environmental and dietary exposure to bisphenol A (BPA) and its toxicological consequences are extensively reported. BPA has multiple cellular targets. One of the mechanisms of action of BPA involves interaction with and activation of nuclear receptors (NRs) including peroxisome proliferator activated-receptors (PPARs).

Fenofibrate ameliorates neural, mechanical, chemical, and electrical alterations in the murine model of heart failure.

Heart failure (HF) is a leading cause of hospitalization across the world and is known to cause ill-health and heavy economic losses. In the present study, a rat model of isoproterenol (ISO, 85 mg/kg subcutaneously for two subsequent days) induced HF was developed. ISO induces HF by its direct effect, that is, rise in left ventricular end-diastolic pressure (mechanical) and indirectly by altering the baroreflex (neural), electrocardiography (electrical), and development of oxidative stress and hyperlipidemia (chemical).

Strategizing biodegradable polymeric nanoparticles to cross the biological barriers for cancer targeting.

The biological barriers in the body have been fabricated by nature to protect the body from foreign molecules. The successful delivery of drugs is limited and being challenged by these biological barriers including the gastrointestinal tract, brain, skin, lungs, nose, mouth mucosa, and immune system. In this review article, we envisage to understand the functionalities of these barriers and revealing various drug-loaded biodegradable polymeric nanoparticles to overcome these barriers and deliver the entrapped drugs to cancer targeted site.

Cinnamomum cassia exhibits antileishmanial activity against Leishmania donovani infection in vitro and in vivo.

Background: There is a pressing need for drug discovery against visceral leishmaniasis, a life-threatening protozoal infection, as the available chemotherapy is antiquated and not bereft of side effects. Plants as alternate drug resources has rewarded mankind in the past and aimed in this direction, we investigated the antileishmanial potential of Cinnamomum cassia.

Methodology: Dichloromethane, ethanolic and aqueous fractions of C.

Anti-inflammatory role of tempol (4-hydroxy-2,2,6,6-tetramethylpiperidin-1-oxyl) in nephroprotection.

Inflammation is one of the mechanisms involved in the acute kidney injury (AKI) caused by cisplatin (CP)-induced nephrotoxicity. Tempol (4-hydroxy-2,2,6,6-tetramethylpiperidin-1-oxyl) has powerful antioxidant activity. We investigated its potential nephroprotective effects and the underlying mechanisms that may add further benefits to its clinical usefulness in a CP-induced AKI model.

Recent Advances Towards Treatment of HIV: Synthesis and SAR Studies.

In the present study, authors want to encourage the research exertions through structureactivity relationship for the identification of effective molecules for the treatment of Human immunodeficiency virus because nowadays AIDS is considered as one of the main causes of death in human beings. A diversity of biological resources has been searched and developed for the treatment of HIV but unfortunately, until now, no medicine is found to be fully effective and safe for the cure of patients. Human immunodeficiency virus is a type of lentivirus which causes the infection of HIV and once it enters the human body, it stays for a longer period of time triggering immunodeficiency syndrome.

Valproic Acid Induced Neurotoxicological Manifestations and its Mitigation by Melatonin in Rat Brain Synaptosomes.

Background And Aims: A short branched chain fatty acid, valproic acid (VPA), has been used worldwide for decades in the intervention of seizure disorders, neuropathic pain and migraine. However, several adverse effects of VPA have been reported over the years. The aim of our investigation was to evaluate the adverse effects of VPA on synaptic functions by using synaptosomal preparation of rat brain as an in vitro model and the possible protective role of melatonin against VPA induced neurotoxicity.

Chemical constituents with antimicrobial and antioxidant activity from the aerial parts of (Sm.) Sweet.

(Sm.) Sweet grows all over the world and used to treat cough and bronchitis. The air-dried powder of the aerial parts was exhaustively extracted with methanol and the concentrated extract was adsorbed on silica gel for preparation of slurry.

Isolation and Characterization of Nuciferoic Acid, a Novel Keto Fatty Acid with Hyaluronidase Inhibitory Activity from Cocos nucifera Linn. Endocarp.

Background: Inflammation and oxidative stress are very closely related to pathophysiological processes and linked to multiple chronic diseases. Traditionally, the coconut fruits were used in Guatemala for treatment of dermatitis and inflammation. Isolation of the anti-inflammatory agent from the hard shell of the coconut fruit was targeted in the current study.

Synthesis, ADME, docking studies and in vivo anti-hyperglycaemic potential estimation of novel Schiff base derivatives from octadec-9-enoic acid.

A new series of octadec-9-enoic acid schiff base entities (S1-S30) were designed and synthesized targeting peroxisome proliferator activated receptor-gamma for agonist action. Molinspiration software (online) was used to estimate drug like molecular properties of the metabolites. Docking disquisition on co-crystallized protein of PPAR-γ (PDB ID 1FM9) was carried out which showed S21, S10 and S7 as best situated in the vital sites of receptor having docking scores -9.

Guggulsterone, a farnesoid X receptor antagonist lowers plasma trimethylamine--oxide levels: An evidence from in vitro and in vivo studies.

The current study investigated the role of guggulsterone (GS), a farnesoid X receptor antagonist, in the choline metabolism and its trimethylamine (TMA)/flavin monooxygenases/trimethylamine--oxide (TMAO) inhibiting potential in a series of in vitro and in vivo studies as determined by high-performance liquid chromatography (HPLC), mass spectroscopy (MS), and liquid chromatography (LC)-MS techniques. Atherosclerosis (AS) was successfully induced in a group of experimental animals fed with 2% choline diet for 6 weeks. Serum lipid profiles such as total cholesterol, triglycerides, low-density lipoprotein cholesterol, high-density lipoprotein cholesterol, and very low-density lipoprotein cholesterol were measured.

Serotonergic mechanisms in the 6-Hz psychomotor seizures in mice.

Serotonin (5-hydroxytrytamine (5-HT)) plays an important role in experimental seizures. Recently, we reported the depletion of 5-HT by parachlorophynylalanine (PCPA) in whole brain to enhance 6-Hz psychomotor seizures in mice. In the present work, we investigated the effect of 5-HT depletion in cortex and hippocampus, brain regions relevant for epilepsy, on behavioral and ultra-structural changes following 6-Hz psychomotor seizures in mice.

Cardioprotective Efficacy of (L.) Seed Extract in Heart Failure Rats Through Modulation of Endothelin Receptors and Antioxidant Potential.

The present study aimed to evaluate the therapeutic and prophylactic potential of extract in isoproterenol-induced heart failure (HF) in Wistar rats. Two weeks after the isoproterenol administration, rats developed severe impairment in left ventricular functions, reduced baroreflex sensitivity, and significant alteration in hemodynamic parameters and lipid profile. HF rats also exhibited enhanced lipid peroxidation and increased expression of endothelin receptors (ET and ET).

Unfolding the pleiotropic facades of rosuvastatin in therapeutic intervention of myriads of neurodegenerative disorders.

Rosuvastatin, a 3-hydroxy-3-methylglutaryl-coenzyme (HMG-CoA) reductase inhibitor, and one of the most popular antihyperlipidemic medications have been found to possess pharmacodynamic activities much different from its usual indication. Recent research studies have revealed the efficacy of rosuvastatin in attenuating neuroinflammation, reducing the progression of Alzheimer's disease, providing protection against cerebral ischaemia and spinal cord injury as well as ameliorating epilepsy. Mechanisms behind the neuroprotective potential of rosuvastatin can be attributed to its pleiotropic effects, independent of its ability to inhibit HMG-CoA reductase.

Glycyrrhizic acid suppresses 1,2-dimethylhydrazine-induced colon tumorigenesis in Wistar rats: Alleviation of inflammatory, proliferation, angiogenic, and apoptotic markers.

Objectives: Colon cancer is the major health disease related with high mortality. Glycyrrhizic acid (GA) is an active constituent of licorice with anti-inflammatory and anticarcinogenesis effects. We investigated the chemopreventive potential of GA against 1,2-dimethylhydrazine (DMH)-induced colon tumorigenesis in Wistar rats.

Generation of three spinocerebellar ataxia type-12 patients derived induced pluripotent stem cell lines (IGIBi002-A, IGIBi003-A and IGIBi004-A).

Spinocerebellar ataxia type-12 (SCA12) is a neurological disorder caused due to triplet (CAG) repeat expansion in 5' UTR of PPP2R2B. It is one of the most prominent SCA-subtype in Indian population and till date no patient specific models have been described. Human-induced-pluripotent-stem cell (HiPSC) based disease modelling has become the next generation tool for studying various human pathologies.

Ursolic acid loaded intra nasal nano lipid vesicles for brain tumour: Formulation, optimization, in-vivo brain/plasma distribution study and histopathological assessment.

The aim was to formulate an optimized ursolic acid (UA) loaded lipid vesicle using formulation by design approach (FbD) for improving the drug targeting by nasal route for brain tumor. Three factors were evaluated at three different levels using anethole (terpene) (A), ethanol (B) and phospholipid90 G (C) as independent variables and their individual and combined effects were observed for PDI (Y), vesicle size (Y) and encapsulation efficiency (Y) to select an optimal system (UALVopt). The optimized formulation was further converted into gel and evaluated for drug release, nasal permeation study, brain/plasma uptake and histopathology study.

Anti-carcinogenic effect of hesperidin against renal cell carcinoma by targeting COX-2/PGE2 pathway in Wistar rats.

The present study was designed to evaluate the protective effects of hesperidin, a flavonoid on DEN initiated and Fe-NTA promoted renal carcinogenesis in Wistar rats. Renal cancer was initiated by a single i.p.

Bisphosphonates: Future perspective for neurological disorders.

Neurodegenerative disorders and osteoporosis share some common underlying pathological features including calcium overload, accumulation of toxic chemicals, inflammation and impaired protein prenylation by isoprenoids (farnesyl pyrophosphate and geranylgeranyl pyrophosphate) appear later stage of life. Substantial number of pre-clinical and clinical reports as well as in vitro data univocally acknowledged the negative impact of altered post-translational modification (prenylation) of proteins like small GTPases (Rffhes, Rho, Rac etc.) and cholesterol levels in both serum and brain on CNS integrity.

Rosuvastatin alleviates high-salt and cholesterol diet-induced cognitive impairment in rats via Nrf2-ARE pathway.

Objective: The objectives of our study were to investigate the possible effect of rosuvastatin in ameliorating high salt and cholesterol diet (HSCD)-induced cognitive impairment and to also investigate its possible action via the Nrf2-ARE pathway.

Methods: In silico studies were performed to check the theoretical binding of rosuvastatin to the Nrf2 target. HSCD was used to induce cognitive impairment in rats and neurobehavioral studies were performed to evaluate the efficacy of rosuvastatin in enhancing cognition.

S-allyl cysteine ameliorates cyclophosphamide-induced downregulation of urothelial uroplakin IIIa with a concomitant effect on expression and release of CCL11and TNF-α in mice.

Background: The aim of this study was to evaluate the modulatory effect of S-allyl cysteine against cyclophosphamide-induced changes in uroplakin IIIa, CCL11 and TNF-α.

Methods: Mice were treated with cyclophosphamide (200mg/kg×7 d, ip). S-allyl cysteine (150mg/kg×7d, ip), and comparator compound mesna (40mg/kg×7d, ip) were administered 1h before and 4h after each cyclophosphamide dose.

In silico molecular interaction of bisphenol analogues with human nuclear receptors reveals their stronger affinity vs. classical bisphenol A.

Background: Bisphenol A (BPA) is known for endocrine disrupting activity. In order to replace BPA, a number of bisphenol analogues have been designed. However, their activity profile is poorly described and little information exists about their endocrine disrupting potential and interactions with nuclear receptors.