Yoga in the management of Diabetes Mellitus

Diabetes mellitus is a chronic metabolic disorder in which the body is unable to make proper utilisation of glucose, resulting in the condition of hyperglycaemia. Excess glucose in the blood ultimately results in high levels of glucose being present in the urine (glycosuria). This increase the urine output, which leads to dehydration and increase thirst. India has the largest diabetic population in the world. Changes in eating habits, increasing weight and decreased physical activity are major factors leading to increased incidence of Diabetes. Lifestyle plays an important role in the development of Diabetes. Yoga offers natural and effective remedies without toxic side-effects, and with benefits that extend far beyond the physical. This system of Yoga is a simple, natural programme involving five main principles: proper exercise, proper breathing, proper relaxation, proper diet and positive thinking and meditation. It is a cost effective lifestyle intervention technique

Diet and Lifestyle Modifications in Sthoulya (Obesity)

In Process of Modernization and Rapid urbanization human beings are falling prey to various disorders. Unhealthy food habits and lifestyle play a major role in causing many ailments including Obesity. The prevalence of Obesity worldwide has dramatically increased during the last three decades. Obesity has significant effects on an individual's quality of life as well as their life expectancy. The treatment of many of these conditions which involves multi-drug regimens which can be associated with a variety of side effects. Although therapy with prescription of medication is often unavoidable lifestyle modifications can play a key role in Obesity. In Ayurveda and other alternative therapy can manage the obesity through Ahara (Diet) and Vihara (Lifestyle)

Larvicidal activities of 2-Aryl-2,3-Dihydroquinazolin -4-ones against malaria vector Anopheles arabiensis, In Silico ADMET prediction and molecular target investigation

Malaria, affecting all continents, remains one of the life-threatening diseases introduced by parasites that are transmitted to humans through the bites of infected Anopheles mosquitoes. Although insecticides are currently used to reduce malaria transmission, their safety concern for living systems, as well as the environment, is a growing problem. Therefore, the discovery of novel, less toxic, and environmentally safe molecules to effectively combat the control of these vectors is in high demand. In order to identify new potential larvicidal agents, a series of 2-aryl-1,2-dihydroquinazolin-4-one derivatives were synthesized and evaluated for their larvicidal activity against Anopheles arabiensis. The in silico absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties of the compounds were also investigated and most of the derivatives possessed a favorable ADMET profile. Computational modeling studies of the title compounds demonstrated a favorable binding interaction against the acetylcholinesterase enzyme molecular target. Thus, 2-aryl-1,2-dihydroquinazolin-4-ones were identified as a novel class of Anopheles arabiensis insecticides which can be used as lead molecules for the further development of more potent and safer larvicidal agents for treating malaria.Fil: Venugopala, K. N.. Durban University Of Technology; SudáfricaFil: Pushpalatha, R.. Reva University; IndiaFil: Tratat, C.. King Faisal University; Arabia SauditaFil: Gleiser, Raquel M.. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Instituto Multidisciplinar de Biología Vegetal (P). Grupo Vinculado Centro de Relevamiento y Evaluación de Recursos Agrícolas y Naturales; ArgentinaFil: Bhandary, S.. Indian Institute Of Science Education And Research Bhopal; IndiaFil: Chopra, D.. Indian Institute Of Science Education And Research Bhopal; IndiaFil: Morsy, M.. King Faisal University; Arabia SauditaFil: Al-Dhubiab, B. E.. King Faisal University; Arabia SauditaFil: Attimarad, M. B.. King Faisal University; Arabia SauditaFil: Nair, A.. King Faisal University; Arabia SauditaFil: Sreeharsha, N.. King Faisal University; Arabia SauditaFil: Venugopala, R.. University Of Kwazulu-natal; SudáfricaFil: Deb, P. K.. Philadelphia University; JordaniaFil: Chandrashekharappa, S.. Institute For Stem Cell Biology And Regenerative Medicine; IndiaFil: Khalil, H.. King Faisal University; Arabia SauditaFil: Alwassil, O.. King Saud Bin Abdulaziz University For Health Sciences; Arabia SauditaFil: Abed, S. N.. Philadelphia University; JordaniaFil: Bataineh, Y. A.. Philadelphia University; JordaniaFil: Palenge, R.. Reva University; IndiaFil: Haroun, M.. King Faisal University; Arabia SauditaFil: Pottathil, S.. King Faisal University; Arabia SauditaFil: Girish, M. B.. Reva University; IndiaFil: Akrawi, S. H.. King Faisal University; Arabia SauditaFil: Mohanlall, V.. Durban University Of Technology; Sudáfric

Crystallography, in silico studies, and In vitro antifungal studies of 2,4,5 trisubstituted 1,2,3-triazole analogues

A series of 2,4,5 trisubstituted-1,2,3-triazole analogues have been screened for their antifungal activity against five fungal strains, Candida parapsilosis, Candida albicans, Candida tropicalis, Aspergillus niger, and Trichophyton rubrum, via a 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) microdilution assay. Compounds GKV10, GKV11, and GKV15 emerged as promising antifungal agents against all the fungal strains used in the current study. One of the highly active antifungal compounds, GKV10, was selected for a single-crystal X-ray diffraction analysis to unequivocally establish its molecular structure, conformation, and to understand the presence of different intermolecular interactions in its crystal lattice. A cooperative synergy of the C-H···O, C-H···N, C-H···S, C-H···π, and π···π intermolecular interactions was present in the crystal structure, which contributed towards the overall stabilization of the lattice. A molecular docking study was conducted for all the test compounds against Candida albicans lanosterol-14α-demethylase (pdb = 5 tzl). The binding stability of the highly promising antifungal test compound, GKV15, from the series was then evaluated by molecular dynamics studies.</jats:p

Yoga in the management of Diabetes Mellitus

Diabetes mellitus is a chronic metabolic disorder in which the body is unable to makeproper utilisation of glucose, resulting in the condition of hyperglycaemia. Excess glucose inthe blood ultimately results in high levels of glucose being present in the urine (glycosuria). This increase the urine output, which leads to dehydration and increase thirst. India has the largest diabetic population in the world. Changes in eating habits, increasing weight and decreased physical activity are major factors leading to increased incidence of Diabetes. Lifestyle plays an important role in the development of Diabetes. Yoga offers natural and effective remedies without toxic side-effects, and with benefits that extend far beyond the physical. This system of Yoga is a simple, natural programme involving five main principles: proper exercise, proper breathing, proper relaxation, proper diet and positive thinking and meditation. It is a cost effective lifestyle intervention technique

Development of UV Spectrophotometric Procedures for Determination of Amlodipine and Celecoxib in Formulation: Use of Scaling Factor to Improve the Sensitivity

FDA has recently approved a new fixed-dose combination of amlodipine besylate (AMD) and celecoxib (COX) for the treatment of hypertension and osteoarthritis. No analytical method has been reported for analysis of these two analytes so far. Hence, to monitor the quality and quantity in the formulation of AMD and COX a simple, accurate, precise, economical, and eco-friendly spectroscopic analytical method has been established. The first method involves the determination of AMD and COX by the first derivative UV spectroscopic method with scaling factor 10. However, the second method was based on the direct measurement of UV absorbance of AMD at 364.3 nm and ratio first derivative UV spectroscopic method for COX. Both methods showed good linearity in the range of 5 to 40 μg/ml for COX, whereas AMD showed linearity in the range of 0.5 to 10 μg/ml in first derivative method with scaling factor 10 and 1 to 10 μg/ml in the second method with good correlation coefficient (R2 > 0.998). Both the methods were validated for LOD, LOQ, accuracy, precision, recovery studies, and stability as per the ICH guidelines, and the validated results were well within the acceptable range. Both the methods were successfully utilized for the determination of AMD and COX in the presence of each other in the formulation, and statistically compared between the proposed methods. Therefore, the proposed procedures can be utilized for regular quality control studies

Lipid Nanoparticles as a Promising Drug Delivery Carrier for Topical Ocular Therapy&mdash;An Overview on Recent Advances

Due to complicated anatomical and physical properties, targeted drug delivery to ocular tissues continues to be a key challenge for formulation scientists. Various attempts are currently being made to improve the in vivo performance of therapeutic molecules by encapsulating them in various nanocarrier systems or devices and administering them via invasive/non-invasive or minimally invasive drug administration methods. Biocompatible and biodegradable lipid nanoparticles have emerged as a potential alternative to conventional ocular drug delivery systems to overcome various ocular barriers. Lipid-based nanocarrier systems led to major technological advancements and therapeutic advantages during the last few decades of ocular therapy, such as high precorneal residence time, sustained drug release profile, minimum dosing frequency, decreased drug toxicity, targeted site delivery, and, therefore, an improvement in ocular bioavailability. In addition, such formulations can be given as fine dispersion in patient-friendly droppable preparation without causing blurred vision and ocular sensitivity reactions. The unique advantages of lipid nanoparticles, namely, solid lipid nanoparticles, nanostructured lipid carriers, nanoemulsions, and liposomes in intraocular targeted administration of various therapeutic drugs are extensively discussed. Ongoing and completed clinical trials of various liposome-based formulations and various characterization techniques designed for nanoemulsion in ocular delivery are tabulated. This review also describes diverse solid lipid nanoparticle preparation methods, procedures, advantages, and limitations. Functionalization approaches to overcome the drawbacks of lipid nanoparticles, as well as the exploration of new functional additives with the potential to improve the penetration of macromolecular pharmaceuticals, would quickly progress the challenging field of ocular drug delivery systems

Enhancement of Anticorrosive Performance of Cardanol Based Polyurethane Coatings by Incorporating Magnetic Hydroxyapatite Nanoparticles

The present investigation demonstrates renewable cardanol-based polyol for the formulation of nanocomposite polyurethane (PU) coatings. The functional and structural features of cardanol polyol and nanoparticles were studied using FT-IR and 1H NMR spectroscopic techniques. The magnetic hydroxyapatite nanoparticles (MHAPs) were dispersed 1&ndash;5% in PU formulations to develop nanocomposite anticorrosive coatings. An increase in the strength of MHAP increased the anticorrosive performance as examined by immersion and electrochemical methods. The nanocomposite PU coatings showed good coating properties, viz., gloss, pencil hardness, flexibility, cross-cut adhesion, and chemical resistance. Additionally, the coatings were also studied for surface morphology, wetting, and thermal properties by scanning electron microscope (SEM), contact angle, and thermogravimetric analysis (TGA), respectively. The hydrophobic nature of PU coatings increased by the addition of MHAP, and an optimum result (105&deg;) was observed in 3% loading. The developed coatings revealed its hydrophobic nature with excellent anticorrosive performance

Effective Therapeutic Delivery and Bioavailability Enhancement of Pioglitazone Using Drug in Adhesive Transdermal Patch

The administration of pioglitazone as an oral therapy is restricted due to various challenges. The aim of the current investigation was to evaluate the suitability of pioglitazone in adhesive transdermal patch as an alternative delivery system, in order to improve therapeutic delivery. Drug in adhesive pioglitazone (2% w/w) transdermal patch were optimized for drug release, suitable adhesive, and skin permeation enhancer. The selected patch was examined for drug-loading capacity and the patch with greater pioglitazone (6% w/w) was evaluated in rat models. The release of pioglitazone was influenced by the tested adhesive and was shown to be significantly higher (p &lt; 0.001) with patch, prepared using Duro-Tak 87-2516. The ex vivo permeation results substantiate the release data as a greater transdermal flux (15.67 &plusmn; 2.35 &micro;g/cm2/h) was demonstrated in patch fabricated with Duro-Tak 87-2516. Skin penetration enhancers promoted the ex vivo transdermal delivery of pioglitazone, and was ~2 folds (p &lt; 0.0001) higher with propylene glycol, as compared to patch without enhancer. The maximum solubility of pioglitazone in Duro-Tak 87-2516 was found to be 6% w/w. Increasing the drug content in patch enhanced the transdermal flux and was highest when the pioglitazone level was 6% w/w (72.68 &plusmn; 5.76 &micro;g/cm2/h). In vivo pharmacokinetic data demonstrate that the AUC0-&alpha; in transdermal application (13,506.51 &plusmn; 1649.92 ng&middot;h/mL) was ~2 times higher (p &lt; 0.0001) as compared to oral dosage form. In conclusion, the promising results observed here signifies that developed patch could be a viable alternative for oral therapy of pioglitazone

Computational, crystallographic studies, cytotoxicity and anti-tubercular activity of substituted 7-methoxy-indolizine analogues.

Indolizines are heteroaromatic compounds, and their synthetic analogues have reportedly showed promising pharmacological properties. In this study, a series of synthetic 7-methoxy-indolizine derivatives were synthesised, characterised and evaluated for in vitro whole-cell anti-tuberculosis (TB) screening against susceptible (H37Rv) and multi-drug-resistant (MDR) strains of Mycobacterium tuberculosis (MTB) using the resazurin microplate assay method. The cytotoxicity was evaluated using the MTT assay. In silico molecular-docking study was conducted for compounds 5a-j against enoyl-[acyl-carrier] protein reductase, a key enzyme of the type II fatty acid synthesis that has attracted much interest for the development of novel anti-TB compounds. Thereafter, molecular dynamic (MD) simulation was undertaken for the most active inhibitors. Compounds 5i and 5j with the methoxy functional group at the meta position of the benzoyl group, which was at the third position of the indolizine nucleus, demonstrated encouraging anti-TB activity against MDR strains of MTB at 16 μg/mL. In silico studies showed binding affinity within the range of 7.07-8.57 kcal/mol, with 5i showing the highest binding affinity. Hydrogen bonding, π-π- interactions, and electrostatic interactions were common with the active site. Most of these interactions occurred with the catalytic amino acids (Pro193, Tyr158, Phe149, and Lys165). MD simulation showed that 5j possessed the highest binding affinity toward the enzyme, according to the two calculation methods (MM/PBSA and MM/GBSA). The single-crystal X-ray studies of compounds 5c and 5d revealed that the molecular arrangements in these two structures were mostly guided by C-H···O hydrogen-bonded dimeric motifs and C-H···N hydrogen bonds, while various secondary interactions (such as π···π and C-H···F) also contributed to crystal formation. Compounds 5a, 5c, 5i, and 5j exhibited no toxicity up to 500 μg/mL. In conclusion, 5i and 5j are promising anti-TB compounds that have shown high affinity based on docking and MD simulation results