Krishna R Gupta

Three-dimensional protein structure prediction from amino acid sequence has been a thought-provoking task for decades, but it of pivotal importance as it provides a better understanding of its function. In recent years, the methods for prediction of protein structures have advanced considerably. Computational techniques and increase in protein sequence and structure databases have influence the laborious protein structure determination process. Still there is no single method which can predict all the protein structures. In this review, we describe the four stages of protein structure determination. We have also explored the currenttechniques used to uncover the protein structure and highpoint best suitable method for a given protein. Keywords: Protein, Structure, X­ray, NMR, Mass spectroscopy, Rosette

The blood brain barrier (BBB) segregates the central nervous system from the systemic circulation nevertheless also retard the effective treatment of central nervous system diseases. Intrinsically, the BBB prevents contagions and pathogens by invade the brain, but also restraint the brain uptake of therapeutic molecules. The potentiality to treat central nervous system disorders is strongly limited by the poor access of many therapeutic agent to the target tissues, formed by a complex interplay of endothelial cells, astrocyte and pericytes and the cells are connected by tight junctions which express a variety of receptors, transporters, and pores which allow the penetration of specific substances from the blood into the CNS through which only selected molecules can passively diffuse to reach the brain. Nonetheless, under certain pathological conditions, the BBB is interrupted by allowing direct interaction between blood components and consequently, it plays a pivotal role in minimizing CNS toxin exposure, controlling immune–CNS communication, maintaining a low protein CNS environment, separating peripheral and CNS neuro- signals, and importantly, regulating ion homeostasis. At present, along with the structural and mechanistic manifestation of the BBB under physiological and pathological conditions it is feasible to design drug delivery systems that could cross the BBB adequately. This review focuses on strategies that influence such BBB disruption for delivering nano-carriers to the central nervous system with wider implementations and broader prospection the treatment of brain targeted therapy, nano-medicines have turn out to be more potent, more distinct and less toxic than traditional drug therapy. Keywords: Nanocarriers CNS diseases, Blood brain barrier Interruption in BBB Nanoneurology.

Aim: The aim of present study was to develop and validate a dissolution test method for Cyclobenzaprine HCL in its formulation using RP-HPLC method. Design: Optimization of chromatographic parameters, development of the dissolution test method using RP-HPLC and to validate the developed methods as per ICH guidelines. Materials and Methods: The optimized dissolution parameters includes USP apparatus II at a paddle rotation rate of 50 rpm and 900 ml of 1.2 pH 0.1N HCL buffer at 37?C0.5?C. Under these conditions, the in vitro release profiles of cyclobenzaprine HCL showed good results. The drug release was estimated by RP-HPLC using column Shodex C18-4E (250×4.6mm×5mm), detection wavelength 289.4 nm having the flow rate 1.0 mL/min using Acetonitrile : phosphate buffer (3.0 pH) in the proportion of 65:35%v/v. Results: The percent drug amount released estimated by proposed method was found to be 99.04%, The method was found to be linear with correlation coefficient was found to be 0.9991 in the concentration range was 2-10 mg/mL. The mean % recovery of Cyclobenzaprine was found to be 100.04.Precision values observed less than 2.All the validation parameters were within the acceptance range. Conclusion: The results obtained by proposed dissolution method for tablet formulation containing Cyclobenzaprine HCL are reliable, precise and accurate. Hence it was routinely adopted for dissolution analysis of the said drugs in the formulation. Keywords: Cyclobenzaprine HCL, Dissolution test, RPHPLC, Validation.

In 2015, around 44 million people throughout the world, Dementia caused due to Alzheimer’s disease (AD) is associated with a progressive neurodegenerative disorder and this figure is estimated to double by the year 2050. Accumulation of b amyloid triggers the progression of AD through overproduction and aggregation which actively induce synaptic dysfunction leading to disease expression. The generation of Amyloid b -protein (Ab), occurs through sequential cleavage of b - and g -secretases while its removal is dependent on the proteolysis and lysosomal degradation system. The present review is focused on the treatments and strategies based on therapies being developed for treating AD which targets b - amyloid protein. These prospects include agents acting on (Ab ), blocking Tau oligomerization, acetylcholinesterase Inhibitors, N-Methyl-D-Aspartate Receptor (NMDA) antagonist. Targeting Amyloid b -protein (Ab ) (Anti- Amyloid Approach), targeting amyloid aggregation, amyloid based vaccination therapy, Inhibition of Tau Phosphorylation, targeting amyloid clearance and cholesterol lowering drug. Keywords: Alzheimer’s disease, Amyloid peptide, Amyloid precursor protein, Biogenesis, Therapeutic β targets.

The present paper describes the synthesis and antibacterial as well as antioxidant activity of new chalcone derivatives derived from p-chloroacetopheneone. In the present work the reaction of p-chloroacetophenone with different substituted aromatic aldehyde. The newly synthesized chalcones (A-D) were analysed by their spectral data TLC, IR, UV and melting point. These newly synthesized compounds were evaluated for in-vitro antioxidant activity by Diphenyl Picryl Hydrazine (DPPH) model using ascorbic acid as standard and for antimicrobial activity by Cup Plate method on gram positive and gram negative bacterial strain using amoxicillin as standard. Keywords: Chalcone, Antimicrobial, Antioxidant, P-chloroacetophenone, Aromatic aldehyde

Nowadays various drugs synthesized by various computational drug designs as well as various drugs have complex structure. Due to their complex structure, higher molecular weight which will increases solubility issues. Solubility is the most important and challenging task for researchers. Bioavailability and absorption of a drug depends on solubility of drug and thus we achieve pharmacological response. But poor aqueous solubility is a rate limiting step in bioavailability which made drug development more difficult. Drugs having low bioavailability require to be administered at a higher dose to achieve desired drug concentration in the systemic circulation and reach the target site. Thus, instead of getting desired effects drug produces side effects in the gastrointestinal tract. Hence, with the advancement of chemical science, the need of development of pharmaceutical technologies is also increasing. New techniques have been developed with a focus on enhancement of the solubility and oral bioavailability of poorly water-soluble drugs. The present review focuses on new technologies which are being used to resolve solubility issue of poorly soluble drugs which is the rate limiting step in bioavailability. Keywords: Solubility, Need of solubility, Techniques of solubility enhancement

The marine is the primary source of uniquely structured natural materials, which are primarily found in living things. Marine algae have long been utilised as food and medicine and are crucial to the ecology. Marine creatures have the potential to be abundant sources of highly bioactive secondary metabolites that could serve as valuable starting points for the creation of novel pharmaceuticals. The sea is regarded as the largest remaining pool of natural molecules to be assessed for therapeutic activity and provides a tremendous resource for novel compounds due to the fact that marine animals make up around half of all species in the world. It is a real fact that the importance of marine organisms as a source of new substances is growing. Algae can be divided into two primary categories: macroalgae (seaweeds), which includes green, brown, and red algae, and microalgae, which includes blue-green algae, dinoflagellates, bacillariophyta (diatoms), etc. The natural bioactive compounds found in marine algae have been demonstrated to be a rich source of anti-diabetic, anti-inflammatory, antiviral, antifungal, hypolipidemic, antioxidant, anti-hypercholesterolemia, antibacterial, and antineoplastic activities. They generate fresh secondary metabolites with potential for use as pharmaceuticals because of their biological activity. The potential pharmacological, therapeutic, and research applications of these substances have been covered in this review. Keywords: Marine, Extraction, Chemical Compound, Therapeutic Effects, Medicinal value