The discovery of the natural compound Boeravinone-C as a potential antiobesity drug candidate targeting pancreatic lipase using chemo-informatics-based approaches.

Obesity is a metabolic disorder distinguished by excess fat deposition in fatty tissues. Pancreatic lipase is one of the promising drug targets for treating obesity due to its critical role in the hydrolysis of triglycerides into mono-glycerides and free fatty acids. Due to unsatisfactory results and severe side effects of the current drugs available for treating obesity, there is an urgent need to identify novel therapeutic options. Boerhaavia diffusa is one of the widely known species of flowering plant commonly known as Punamava. Extracts from Punamava plants have been widely used in treating countless ailments in traditional medicine. Recently, multiple reports demonstrated the potential antiobesity activity of B. diffusa plant extracts. In this scenario, we have evaluated numerous reported B. diffusa against pancreatic lipase drug targets to identify which reported phytochemicals to have the most promising potential to act as an inhibitor for pancreatic lipase using computational approaches. All the twenty-four phytochemicals from Boerhaavia diffusa were identified as significantly strong binders with a range of binding energies between -6.0 to -8.0 Kcal/mol inside the pancreatic lipase active binding site. On the other hand, we calculated 2D Quantitative Structure-Activity Relationship (QSAR) molecular descriptor properties adhered to Lipinski's rule of five. Between twenty-four phytochemicals evaluated, Boeravinone-C, with a range binding energy of -8.0 Kcal/mol, was discovered as the best lead-like molecule, compared to marketed Orlistat, which has shown -5.6 Kcal/mol of binding energy. Conclusively, Boeravinone-C from B. diffusa extract showed promising inhibitory potential against pancreatic lipase worth further evaluation.

Development of Dapagliflozin Solid Lipid Nanoparticles as a Novel Carrier for Oral Delivery: Statistical Design, Optimization, In-Vitro and In-Vivo Characterization, and Evaluation.

Controlling hyperglycemia and avoiding glucose reabsorption are significant goals in type 2 diabetes treatments. Among the numerous modes of medication administration, the oral route is the most common. Introduction: Dapagliflozin is an oral hypoglycemic agent and a powerful, competitive, reversible, highly selective, and orally active human SGLT2 inhibitor. Dapagliflozin-loaded solid lipid nanoparticles (SLNs) are the focus of our present investigation. Controlled-release lipid nanocarriers were formulated by integrating them into lipid nanocarriers. The nanoparticle size and lipid utilized for formulation help to regulate the release of pharmaceuticals over some time. Dapagliflozin-loaded nanoparticles were formulated by hot homogenization followed by ultra-sonication. The morphology and physicochemical properties of dapagliflozin-SLNs have been characterized using various techniques. The optimized dapagliflozin-SLNs have a particle size ranging from 100.13 ± 7.2 to 399.08 ± 2.4 nm with 68.26 ± 0.2 to 94.46 ± 0.7% entrapment efficiency (%EE). Dapagliflozin-SLNs were optimized using a three-factor, three-level Box-Behnken design (BBD). Polymer concentration (X1), surfactant concentration (X2), and stirring duration (X3) were chosen as independent factors, whereas %EE, cumulative drug release (%CDR), and particle size were selected as dependent variables. Interactions between drug substances and polymers were studied using Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM). Differential scanning calorimetry (DSC), X-ray diffraction (XRD), and atomic force microscopy (AFM) analysis indicated the crystalline change from the drug to the amorphous crystal. Electron microscope studies revealed that the SLNs' structure is nearly perfectly round. It is evident from the findings that dapagliflozin-SLNs could lower elevated blood glucose levels to normal in STZ-induced diabetic rats, demonstrating a better hypoglycemic impact on type 2 diabetic patients. The in vivo pharmacokinetic parameters of SLNs exhibited a significant rise in Cmax (1258.37 ± 1.21 mcg/mL), AUC (5247.04 mcg/mL), and oral absorption (2-fold) of the drug compared to the marketed formulation in the Sprague Dawley rats.

Calcifying Epithelial Odontogenic Cyst of Maxilla: A Clinical and Histological Rarity with Literature Review.

A cyst is defined as a pathological cavity which may or may not have an epithelial lining and which has a fluid, semi-fluid, or gaseous contents and is not formed by the accumulation of pus. The calcifying epithelial odontogenic cyst (CEOC) was first reported by Gorlin et al. in 1962. At that time, it was classified as a cyst related to the odontogenic apparatus. It was later renamed as calcifying cystic odontogenic tumor (CCOT) in the World Health Organization classification devised in 2005 due to its histological complexity, morphological diversity, and aggressive proliferation. CCOT was later recognized by numerous names including Gorlin cyst, calcifying ghost cell odontogenic cyst and/or dentogenic ghost cell tumor. It has a peak incidence during the second and third decades of life and does not demonstrate any gender predilection. Radiographically, CEOC may appear as a unilocular or multilocular radiolucent lesion with either well-circumscribed or poorly-defined margins and may also be observed in association with unerupted teeth. Calcification is an important radiographic feature for the interpretation of CEOC/CCOT. The typical histopathological features of CEOC include a fibrous wall and lining of the odontogenic epithelium with either columnar or cuboidal basal cells resembling ameloblasts. The treatment of choice for CEOC is conservative surgical enucleation; however, recurrence is also not found to be uncommon. Herein, we are reporting a case of the same in a 21-year-old female which was a great dilemma during the diagnostic workup.

Sensitivity and Specificity of Magnetic Resonance Imaging in Prediction of Cervical Lymph Node Metastasis in Oral Squamous Cell Carcinomas.

Background: The inaccuracies in clinical examination have been well-documented while advanced imaging modalities including computed tomography (CT) and magnetic resonance imaging (MRI) have been shown to have superior diagnostic accuracy in detecting occult and nodal metastasis. The aim of the present study was to identify as well as evaluate the inaccuracies in clinical examination and of clinical diagnostic criteria in known cases of oral squamous cell carcinomas (OSCCs) with the help of MRI. Methodology: A total of 24 patients attending as outpatients were included in the study while clinically diagnosed and histopathologically proven cases of OSCC were examined clinically and then, subjected to advanced imaging with the help of MRI. Statistical Analysis Used: Statistical analysis was done using Statistical Package for Social Sciences (SPSS) version 17.0 (SPSS Inc., Chicago, IL, USA) while paired t-test was performed for evaluating size of tumor and lymph node recorded on clinical and imaging findings. p<0.05 was considered statistically significant. Results: Detection of tumor size and lymph node metastasis were found to be higher in case of MRI than when accomplished by clinical staging alone while paired t-test values for difference in results were found to be statistically significant (p<0.05). Conclusions: The present study showed that clinical diagnostic criteria alone were not sufficient and reliable for detecting metastatic lymphadenopathy highlighting the significance of advanced imaging modalities like MRI for an efficient pre-operative diagnostic work-up as well as, as a tool for planning treatment in patients with OSCCs.