Current Bioactive Compounds - Volume 14, Issue 4, 2018

Background: The phophatidylinositol 3-kinase (PI3K) pathway is critical in regulating diverse cellular functions and its deregulation is associated to one third of human cancers. Therefore, several PI3K inhibitors have been developed with many of these entering preclinical and early clinical assessments. Structure based design has led to the development of broad array of agents including dual inhibitors of PI3K and mTOR, p Read More

Background: Chitosan is a natural polymer which has limited solubility. Chitosan is capable of being modified using multiple alternatives for chitosan chemical modifications that provide different desirable properties. Method: N-methyl chitosan was successfully prepared and characterized. N-methyl chitosan was characterized by the FTIR, XRD, SEM, TEM, solubility, water content, and specific surface area. Antifungal activity a Read More

Background: The combretastatin-A4(1) is a phenolic cis-stilbene, natural product, and was isolated from the stem wood of the South African tree Combretum caffrum in the 1980. Combretastatin A-4 (CA - 4) has received special attention in the last few years. It showed strong antitumor activity by inhibiting tubulin polymerization and interacting with the colchicine binding site on tubulin. CA-4 also acts as Vascular Disrupti Read More

Background: Using Multi-Walled Carbon Nanotubes (MWCNTs) as a drug delivery system, can avoid the need for solvents and preventing drug precipitation in aqueous solution. Soyasapogenol B (SSB) acts as an important therapeutic agent owing to its numerous reported biological activities. Hence, this work deals with preparation and characterization of SBB loaded onto functionalized MWCNTs with tetraethyl orthos Read More

Background: The identification and quantification of quercetin in tropical fruits could be an incentive to consume these fruits as health promoters. The purpose of this study was to identify and quantify the levels of quercetin in tropical fruits extracts, and then select the extract with the highest levels of quercetin, in order to synthesize nanoparticles using cashew gum as core material. Method: The detection and quantification of Read More

Background: Interest in novel sources of edible and vegetable oils have been growing due to the growing population and its accompanying energy needs. The present study investigates the physicochemical characteristics, the antioxidant property and antibacterial activity of the vegetable oil extracted from Alocasia fornicata collected from Mizoram, India. This vegetable oil could potentially serve as a highly valuable and cost- Read More

Background: Rhizosphere is rich in microbial flora. Actinomycetes are a diverse group of organisms which are reported to produce antibiotics, vitamins, enzymes and plant growth promoting substances. Aim: The main objective of this study was to screen actinomycetes from the soil samples for the production of various enzymes that could be used for industrial applications. Method: Rhizosphere soils samples were co Read More

Background: The use of antimicrobial agents affecting several biological targets at a time is one of the promising ways to fight multidrug-resistant bacterial strains, and hence it may serve to increase the efficiency of chemotherapy. Among the potential antimicrobial agents acting in this manner are redox-active complexes of transition metals with sterically hindered diphenols. Method: We synthesized the redox-active co Read More

Background: The present manuscript describes the synthesis of 3,3-diphenyl propionic acid derivatives. The key intermediate 3,3-diphenylpropionyl chloride was synthesized by the reaction of 3,3-diphenyl propionic acid and thionyl chloride. The 3,3-diphenylpropionyl chloride was further subjected to reaction with various aromatic secondary amines in the presence of potassium carbonate in acetone. Method: After synthe Read More

Background: Salvia verbenaca is a Mediterranean plant currently belonging to the Lamiaceae family. The plant is widely distributed in Morocco and is widely used in Moroccan traditional folk medicine as a cholagogue, antiseptic, diuretic and astringent. The crushed or chopped fresh leaves are also applied in poultices on wounds and emptied abscesses to facilitate their healing. The aim of this study was to assess the effect of th Read More

Background: The benzofused six membered ring lactams is the part of the core structure of various pharmaceuticals, natural products, agrochemicals and active components of various dyes. The failure to control the microbial infections and the rise in the rate of resistant to antimicrobial agents, there is a strong need to develop new antimicrobial agents. In the current study, we synthesized some benzofused Read More

Background: The synthesis of novel Mannich bases of nitro alkanes utilizing mono- and diamino sugar is abundant in the literatures. The new bases have been successfully synthesized and fully characterized. Biological investigations, particularly cytotoxic activity of our novel compounds were made against some cancer cell lines. With an attempt to improve the anticancer activity we decide to include the indole moieties (well k Read More

Background: Cancer is one of the major health and socio-economic problems of the world even though extensive progress has been made in terms of early diagnosis and cure. The research for new anticancer drug development with more effective treatment is a field of utmost importance in current drug discovery. Method: Molecular Hybridization (MH) strategy has been adapted for the rational design of new ligands, where p Read More

Background: Tuberoinfundibular Peptide of 39 (TIP39) is a neuroendocrine hormone, potentially acting through parathyroid hormone receptor 2 receptor (PTH2R) abundantly expressed in brain. Objective: This study aimed to evaluate the neuroendocrine role of TIP39 in chronic unpredictable mild stress (CUMS) induced depression and to elucidate its underlying mechanism. Method: The depression was induced in rats by CUMS Read More

Background: DNA polymerases and topoisomerases are proteins that play a vital part in DNA metabolism such as replication, transcription, recombination, and chromosome segregation during mitosis. For this reason, these enzymes are appreciated targets for the development of cancer chemotherapeutic drugs. Method: All compounds evaluated in this work were obtained under the conditions and using the reage Read More