Saffron (Crocus sativus L.) has been widely used in traditional or phytomedicine as a treatment of neurological disorders. The saffron is showing great potential to treat various neurological diseases without any apparent side effects. As there are very limited drugs available for the treatment of neurological diseases, saffron provides hope to treat the brain disorders and conditions such as anxiety, depression, Alzheimer’s disease, and Parkinson’s disease. This brief review deals with medicinal applications of saffron plant towards neurological diseases
Five member heterocyclic 1,3,4-oxadiazole derivatives were synthesized and evaluated for their anticancer activity. Compounds containing 1,3,4-oxadiazole ring in their structure are characterised by multidirectional biological activity. The important mechanism behind tumor suppression by 1,3,4-Oxadiazole is related with the inhibition of different growth factors, enzymes and kinases etc. The 1,3,4-Oxadiazole scaffold is a five member heterocyclic ring having versatile activities and created interest for synthetic organic and medicinal chemists for the designing of novel compounds having anti- cancer activity. There are great potential in the development of the simple and small 1,3,4-oxadiazole nucleus which is present in various compounds that possess considerable pharmcological properties such as anticancer and aimed to evaluate new products. The main aim of this review article is to highlight the targeted activity of 1,3,4-Oxadiazole derivatives and their structure activity relationship to generate potential anticancer agents.
Type 2 diabetes mellitus (T2DM) is a chronic metabolic syndrome, which occurs due to increased glucose levels in the human body. There has been lot of work in developing novel approaches to tackle this disease. GLP-1 receptor (GLP-1R), one of the class-B G-protein-coupled receptors (GPCR), is a budding molecular target to design drugs for treating type 2 diabetes. In this review, authors have summarized the physiological actions of Glucagon-like peptide-1 receptor (GLP-1R) and current available drugs based on GLP-1 RAs. Some of the exemplary studies in this area have been examined in detail. Authors conclude that development of degradation-resistant, long-acting GLP-1 receptor agonists is a promising area of research and lot of work needs to be done to understand its mechanism of action.
Allium cepa has phytochemical characteristics well known to be used in our gastronomy. Due to its particle size, low systemic bioavailability is the major disadvantage associated that pose major hurdle for its use for medicinal purpose. These limitations can be overcome by converting the bulk size particles to nanosized particles. The present study was to prepare the nano-particles of Allium cepa with improved aqueous solubility, and to investigate their in-vitro efficacy against Entamoeba gingivalis, a protozoan associated with poor oral hygiene leading to advanced periodontal disease. Allium cepa nanoparticles of the size ranging 85–95 nm with the aqueous solubility of upto 3 mg/mL were prepared, and the anti-amoebic activities were tested in-vitro against Entamoeba gingivalis (ATCC 30927). The trophozoites of Entamoeba gingivalis were cultured in the presence of Alliumcepa’s Bulk/nano- particles or metronidazole, the inhibition caused by each particles type at various concentrations was calculated by counting the viable trophozoites under the inverted microscope. Alliumcepa nanoparticles showed inhibitory results of more than 80%, which is comparable with that of standard drug Metronidazole against E. gingivalis demonstrating its use as a potential anti-parasitic herbal drug.
Oxidative stress (OS) is involved in pathophysiological events of different diseases. Antioxidants mitigate and suppress the adverse effect of OS in the body. Due to lesser side effects and cost effectiveness natural antioxidant is a choice of people nowadays. The present study was designed to characterize/analyze phytochemicals and antioxidant potential in Parthenium hysterophorus (Asteraceae) stem (PHS) sequentially extracted fractions. Chemical characterization of PHS samples was carried out using Gas Chromatography-Mass Spectrometry (GC-MS) and Spectrophotometric techniques. Comparative antioxidant potential in PHS fractions was studied using in vitro antioxidant models. Thin layer chromatography (TLC) was performed to show a differential occurrence of phytochemicals in test fractions and related radical scavenging potential. PHS fractions showed differential presence of compounds. Appreciable radical scavenging, reducing power, and metal ion chelation potential was found in PHS fractions. In conclusion, P. hysterophorus stem may be considered a good source of natural antioxidant compounds.
Novel series of 5-nitroindoline-2-ones was synthesized starting from 5-nitroindoline-2,3-dione 2 and 2-(5-nitro-2-oxoindolin-3-ylidene)hydrazine-1 carbothioamide 3. Compounds were evaluated for their antimicrobial activities. The data showed that compounds 2 and 6b have excellent antimicrobial activities against the two tested strains of G+ve bacteria Staphylococcus aureus and Streptococcus and E. coli when compared with the standards. Furthermore, in-vitro enzyme assay and molecular docking studies were performed for the compounds 2 and 6b against E. coli DNA gyrase B. Prediction of ADMET properties and QSAR study of compounds was carried out respectively.
In an attempt to further explore the role of substituted carboxylic acid derivatives as antidiabetic agent, a series of alkoxyimino-substituted carboxylic acid derivatives (101-206) were designed, synthesized and evaluated for their inhibitory potential against a-amylase and a-glucosidase enzyme. Among all the tested compounds, 102 & 105 has displayed the most potent activity against a-glucosidase with the IC50 of 142.21±1.8 mM and 182.83±2.43 mM respectively, as compared to the standard drug acarbose (136.89±1.67 mM). Based on the inhibition percentage, the inhibition activity of 102 and 105 on a-glucosidase had higher potential than a-amylase. The mode of binding interactions between the a-glucosidase enzyme and the compound 102 was established to be uncompetitive using kinetic analysis. The predicted drug-likeness properties (Lipinski parameters and in silico ADME properties) of the compounds revealed their suitability as potential drug candidate.
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The present study investigated the effect of monocrotophos, a commonly used organophosphate pesticide exposure in the kidney tissues of the swiss albino mice. Monocrotophos was administered at the sub-lethal doses of 1.25mg/kg, 2.5 mg/kg and 5.0 mg/kg body weight for 24 hr. Monocrotophos toxicity generated oxidative stress in the mice as evidenced by significant decrease in the activities of glutathione, superoxide dismutase and catalase enzymes. The exposure increased the lipid peroxidation and protein oxidation in a dose dependent manner. Oxidative stress generation also elicited cytotoxic effects on the mice kidney which were supported by the histopathological changes like degeneration in glomerulus, bowmen’s capsule and tubules, hemorrhage, mononuclear cell infiltration, tubular cast and congested blood vessels in a dose-dependent manner. In conclusion, the study indicated that monocrotophos exposure at various doses induces significant deleterious health effects in mice kidney tissues via oxidative stress generation.
Cite as: Devi, S., Singh, J., Kumar, V., & Malik, V. (2019). Monocrotophos induced Biochemical and Histopathological alterations in the Kidney tissues of Mice. Chemical Biology Letters, 6(2), 39-45.
