Nirma University Journals
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IN-SILICO PREDICTION OF THE NEUROINFLAMMATION MECHANISM OF CAPPARIS SEPIARIA
Full text linkNeuroinflammation or neural dysfunction is a major risk factor that can initiate multiple intracellular signaling cascades to release different proinflammatory cytokines, chemokines and various reactive oxygen species leading to multiple neurodegenerative diseases, such as Alzheimer’s disease, Parkinson’s disease, and Huntington’s disease. The adverse effects associated with the long-term use of conventional non-steroidal anti-inflammatory drugs is attracting herbal medicines as potential therapeutic candidates worldwide. Capparis sepiaria L (C. sepiaria) belonging to Capparaeae is therapeutic medicinal plant used to relieve various ailments including skin diseases, tumours, blood purification, toxaemia, snakebite and disease of the muscles. The objective of this study is to determine the pharmacokinetic and pharmacodynamic properties of C.sepiaria phyto-constituents as therapeutic molecules against neuro inflammation by using in-silico docking analysis and drug disposition. Six phyto- constituents identified from the leaves of C. sepiaria were docked against six pro-inflammatory markers of neuroinflammation followed by the prediction of their safety and bioavailability using GOLD 5.2, admetSAR softwareS respectively. The docking scores obtained were comparable and even better than the five standard marketed drugs. β-amyrin and quercetine present in the leaves of C.sepiaria showed highest fitness score with P38 MAP kinase, NF-kB, mTOR, TACE AChE, BChE markers which are also the targets of the drugs like Galantamine, Donepazil and Rivastigmine. To our understanding this is the first study investgating the inhibitory effect of C. sepiaria in the neuroinflammation. Thus, Capparis sepiaria may prove to be a potential antineuroinflammatory agent and may be further explored as a potential therapeutic candidate for the management of neurodegenerative diseases.
 
DOCKING STUDY OF MARKETED ANTIMALARIALS ON PLASMODIUM FALCIPARUM DIHYDROFOLATE REDUCTASE (Pf DHFR)
Full text linkMalaria is one of the most pivotal parasitic diseases in humans and the malarial parasite transmission in above 100 countries of a population of five million people. In this study, we selected marketed antimalarial drugs hydroxychloroquine, artemisinin and primaquine and performed docking study using Auto Dock on Plasmodium falciparum dihydrofolate reductase (PfDHFR). Docking study suggested about the binding of the drugs at the active site. Docking study also demonstrated about the potency of the drug and their binding affinity with the target. Different binding modes of marketed drugs were observed with different amino acid interactions with different features like hydrophobic, hydrogen bonding, and van der Waals interactions. The least binding energy interaction structures were selected to observe the dock pose of drugs at the active site of PfDHFR
CONDUCTING CLINICAL RESEARCH DURING PANDEMIC ERA: PROBLEMS AND PROSPECTS
Full text linkThe COVID-19 pandemic has significantly affected ongoing clinical research, as conducting clinical research is often seen as secondary to addressing the immediate health needs of patients by healthcare providers. Pandemics create operational challenges and raise scientific and ethical issues for clinical research activities. The benefit of clinical research in terms of opportunities for patients suffering from various diseases, and ability to investigate new therapies to address pandemics cannot be overlooked. This review summarizes the challenges that arise during a pandemic while conducting clinical research along with solutions for addressing these challenges
POTENTIAL IMPORTANCE OF JUGLANS REGIA LINN: NUTRITIONAL PROFILE AND HEALTH BENEFITS
Full text linkFood containing good amount of nutritional value is the most important parameter for maintaining human health and complete physical well-being. Number of plants are available with good source of vitamins and minerals and having other nutritional composition. Juglans regia Linn. (Family-Juglandaceae), commonly known as walnut has substantial benefits as dietary supplement. It possesses remarkable edible and nutritive values, with ease of processing and food manufacturing. It is widely spread and cultivated in various parts of world because of its valuable kernels. Dietician and other health workers of developing countries should give due attention in promoting the research work and projects for studying the medicinal importance, processing of walnut fruit and shell, manufacturing, improvement in nutritive values and potential health benefits of the walnut fruit to promote their utilization as food in respective countries. Many researchers have proved the therapeutic potential of the Juglans regia. It is one of the most important non-timber forest products. The nutritional importance of walnut is related to its seed or kernel. The aim of the present review is to provide the benefits of the walnut with respect to its nutritional profile and therapeutic as well as pharmacological importance as an antioxidant, hypolipidemic, antidiabetic, antimicrobial, antihypertensive and hepatoprotective activity
NANOTECHNOLOGY IN BATTLE AGAINST CORONAVIRUS: AN OVERVIEW
Full text linkThe COVID-19 is an infectious disease and SARS-CoV-2 virus is the causative agent. The nanoparticles rages from 0.2nm to the 1000nm. The particle having less than 200nm shows greater effective application as drug delivery system. As the particle size decreases the surface area will increase hence the nano size material/ drug and formulation has advantage over the conventional dosage forms in the treatment of COVID-19. Along with this the nano medicines easily cross the different cellular membranes, cross the epithelial wall, permeate through the lung tissues and helps to target the lungs. The nanotechnology based diagnostic kits and therapeutics might lead us to stop this COVID-19. The nanotechnology-based formulation has ability to give promising vaccines because they are small in size and it will be act against viruses. So in future the nanotechnology has important role in fight against of COVID 19
SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF SUBSTITUTED 1,3,4- THIADIAZOLE DERIVATIVES AS ANTICONVULSANT AGENTS: `
Full text linkEpilepsy is considered as a brain disorder which involves repeated and spontaneous seizures. Seizures (convulsions) are defined as episodes of disturbed brain functions causing changes in attention or behavior. They are caused by abnormally excited electrical signals in the brain. Comprehensive literature assessment revealed that amongst the compounds studied for anticonvulsant activity; 1,3,4-thiadiazole nucleus showed potent anticonvulsant activity. Acetazolamide and methazolamide are the examples of 2,5-disubstituted-1,3,4- thiadiazole analogues. Hydrazine hydrate and isothiocyanate are used for formation of intermediate and reacted further with substituted aromatic aldehydes in the presence of thiourea to give final derivatives, substituted 1,3,4-thiadiazole. This title compound in step-1 was prepared by stirring of hydrazine hydrate with isothiocyanate whereas in step-2, substituted benzaldehyde was used in presence of thiourea. All synthesized compounds were characterized by physical and spectral characteristics. Structure elucidation of the synthesized compounds was carried out by spectral analysis, FTIR and Mass analysis. PTZ model was used to determine anticonvulsant activity of the final synthesized compounds using Carbamazepine as a standard drug. All synthesized compounds of showed no sedation side effect as compared to reference standard (carbamazepine). The present study indicated that 4-fluoro substituted compound (6b) showed significant protection against pentylenetetrazole induced convulsions as well as mortality within 24 h in mice. It also decreased number of convulsions (P<0.01) and increased onset time for clonic convulsion (P<0.05) which was statistically significant in comparison to control. Study could further be investigated to design & identify lead compound
THERAPEUTIC TARGET OF PHOSPHOTIDYL INOSITOL 3 KINASE IN VARIOUS DISEASE AND DISORDERS
Full text linkThe Phosphogtidyl Inositol 3 kinase belongs to the lipid kinase family. Its major role is in phosphorylation of various cell functions. PI3Ks has three different classes with different activities. Major classes are class I, class II and class III. PI3K has multiple cell functions like growth, proliferation, differentiation, motility and survival. PI3 kinase has a major role in breast cancer, viral infection, thyroid cancer, inflammation, alzheimer disease, and parkinson disease. In breast cancer and most of other cancer\u27s, isoform p110α is mutated. This mutation causes the kinase to be active. Both upstream and downstream PI3 kinase pathway has a potential target for drug development in cancer. Phosphatidylinositide 3- kinases (PI3-K) phosphorylate the third hydroxyl position of the inositide head of phosphoinositide lipids, phosphatidylinositide (PtdIns), phosphatidylinositol (3)-phosphate (Ptdlns(4) P) and phosphatidylinositol (4,5)- bisphosphate (Ptdlns(4,5) P2). Different examples of PI3 kinase inhibitors are wortmannin, quercetin, LY-294002, BKM 120, GDC- 0941 of which many are in the phase 1 clinical trials. It also plays an important role in viral infection. Porcine circovirus type 2 infections are the main reason for the apoptosis both in vitro as well as in vivo and inhibition of PI3K can be useful treatment for that
DEVELOPMENT AND VALIDATION OF HIGH PRESSURE LIQUID CHROMATOGRAPHY ANALYTICAL METHOD FOR RELATED SUBSTANCE OF ACETYLCYSTEINE EFFERVESCENT TABLET
Full text linkThe HPLC method was developed specially for the related substances of n-acetyl-l-cysteine (NAC) effervescent tablet formulation where the issue of merging of impurities peaks was observed during the development of the method. So, development was triggered with an aim of separation of all the known possible impurities peaks from that of principal peak of acetylcysteine as well as each four known impurities. Finally the analytical method for related substance of acetylcysteine with a gradient program on HPLC was developed and validated with the mandatory experiments. The related substance method was efficient to separate the co-eluting peaks of impurities and its individual known impurities from the principal peaks specifically for the effervescent formulation. The method was specific, selective and reproducible. Recovery and linearity was also found within the acceptance criteria. Solution stability was also established and evaluated during the method validation. Method was successfully evaluated for robustness using various alterations in the method parameters for its functionalities
PHOTOPROTECTIVE ACTIVITY OF FLAVONOIDS: A REVIEW
Full text linkIn the recent years, there has been a high rise in the magnitude of ultraviolet light reaching the earth surface due to the fact that stratospheric ozone is being depleted at a fast rate, which in turn has led to increased cases of skin cancer and other skin disorders. UVC radiation is extremely detrimental to the skin even in a small amount but fortunately it is absorbed by the molecular oxygen and the ozone layer. UVB radiation makes 4-5% of the UV light and is 1000 times more capable of causing sunburn than UVA. UVA can cause instant tanning effect and chronic exposure to UVA can cause detrimental effects to the underlying structures of the skin and cause premature photo-aging. Flavonoids are natural secondary plant phenolics which are sub-divided into 6 sub-classes. They possess antioxidant and chelating properties. The biochemical activities of flavonoids and their metabolites depend on their chemical structure and the relative orientation of various moieties on the molecule. Natural flavonoids are one of the many candidates as a defence barrier against the UV damage due to their UV absorbing properties, chelating properties, anti-oxidant properties and their ability to modulate several signalling pathways. However these substances must denote their safety in inclusion to its efficacy as a photoprotective agent