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Glycosylphosphatidylinositols (GPIs) anchored proteins are commonly localized onto lipid rafts. These extracellular proteins participate in a variety of cellular functions, including as receptors for viruses and toxins. Intracellular trafficking of World Health Organization recognized mosquito-larvicidal BinAB toxin is mediated via GPI-anchored Cqm1 receptor protein in Culex mosquitoes. We confirmed conformational change in Cqm1 dimer on interaction with BinA/BinB proteins by dynamic light scattering, modelling of hydrodynamic parameters using the atomic structures, and synchrotron Small Angle solution X-ray scattering (SAXS). A reliable model of the receptor-BinB complex was also constructed from joint SAXS/SANS refinement. We confirmed electrostatic interactions of the Cqm1 ectodomain with lipid rafts reconstituted in model membranes and report receptor-dependent impairment of model liposomes by BinA/B proteins. Liposomal disruption was toxin concentration-dependent as monitored by the release of encapsulated carboxyfluorescein dye. Interestingly, BinA alone, without BinB, showed efficient efflux of the fluorescent dye in agreement with the reported high larvicidal activity of BinA variants. The study provides insight into BinA/B toxin internalization mechanism in the membrane model that is toxin internalization is mediated via receptor-dependent pore formation mechanism. It also suggests a tangible and environmentally safe strategy for control of mosquito population. [ABSTRACT FROM AUTHOR]

Ethyl-4-[(2,4-dinitrophenyl)-hydrazonomethyl]-3,5-dimethyl-1 H-pyrrole-2-carboxylate ( 3) has been newly synthesized by the condensation of ethyl-4-formyl-3,5-dimethyl-1 H-pyrrole-2-carboxylate and 2,4-dinitrophenylhydrazine, characterized by FT-IR, H NMR, UV-Vis, DART Mass and elemental analysis. The formation of compound ( 3) and its properties have been evaluated by quantum chemical calculations. The calculated thermodynamic parameters show that the formation reaction of ( 3) is exothermic and spontaneous at room temperature. The vibrational analysis indicates that ( 3) forms dimer in the solid state by heteronuclear double hydrogen bonding (N-H···O). Topological parameters electron density ( ρ), Laplacian of electron density (∇ ρ), and total electron energy density ( H) at bond critical points (BCP) have been analyzed using 'atoms in molecules' (AIM) theory. The interaction energies of dimer formation using DFT and AIM calculations are found to be −14.6509 and −15.5308 kcal/mol, respectively. AIM ellipticity analysis confirms the presence of resonance-assisted hydrogen bonding in dimer. The global electrophilicity index (ω = 5.91 eV) shows that title molecule is a strong electrophile. The local reactivity descriptors Fukui functions ( f, f), softness ( s, s), and electrophilicity indices ( ω, ω) analyses are performed to determine the reactive sites within molecule. [ABSTRACT FROM AUTHOR]

Introduction: Papaya (Carica papaya Linn.) belongs to the family Caricaceae and is well known for its therapeutic and nutritional properties all over the world. The different parts of the papaya plant have been used since ancient times for its therapeutic applications. Herein, we aimed to review the anticancer, anti-inflammatory, antidiabetic and antiviral activities of papaya leaf. Methods: All information presented in this review article regarding the therapeutic application of Carica papaya leaf extract has been acquired by approaching various electronic databases, including Scopus, Google scholar, Web of science, and PubMed. The keywords Carica papaya, anticancer, anti-inflammatory, immunomodulatory, and phytochemicals were explored until December 2019. Results: The papaya plant, including fruit, leaf, seed, bark, latex, and their ingredients play a major role in the management of disease progression. Carica papaya leaf contains active components such as alkaloids, glycosides, tannins, saponins, and flavonoids, which are responsible for its medicinal activity. Additionally, the leaf juice of papaya increases the platelet counts in people suffering from dengue fever. Conclusion: The major findings revealed that papaya leaf extract has strong medicinal properties such as antibacterial, antiviral, antitumor, hypoglycaemic and anti-inflammatory activity. Furthermore, clinical trials are needed to explore the medicative potential of papaya leaf. [ABSTRACT FROM AUTHOR]