1,4-Benzoxazines are important motifs in many pharmaceuticals and can be formed by a reaction sequence involving the oxidation of -aminophenols to their corresponding quinone imine followed by an inverse electron demand Diels-Alder (IEDDA) cycloaddition with a suitable dienophile. Reported herein is the development of a reaction sequence that employs horseradish peroxidase to catalyze the oxidation of the aminophenols prior to the IEDDA as a more sustainable alternative to the use of conventional stoichiometric oxidants. The synthesis of 10 example benzoxazines is demonstrated in this "one-pot, two-step" procedure with yields between 42% and 92%.
View Article and Find Full Text PDFPoly(lactic--glycolic acid) (PLGA) is one of the preferred polymeric inactive ingredients for long-acting parenteral drug products that are constituted of complex formulations. Despite over 30 years of use, there are still many challenges faced by researchers in formulation-related aspects pertaining to drug loading and release. Until now, PLGA-based complex generic drug products have not been successfully developed.
View Article and Find Full Text PDFDrug targeting is a progressive area of research with folate receptor alpha (FRα) receiving significant attention as a biological marker in cancer drug delivery. The binding affinity of folic acid (FA) to the FRα active site provides a basis for recognition of FRα. In this study, FA was conjugated to beta-cyclodextrin (βCD) and subjected to in silico analysis (molecular docking and molecular dynamics (MD) simulation (100 ns)) to investigate the affinity and stability for the conjugated system compared to unconjugated and apo systems (ligand free).
View Article and Find Full Text PDFExtracellular signal-regulated kinases 1 and 2 (ERK1/2) play key roles in promoting cell survival and proliferation through the phosphorylation of various substrates. Remarkable antitumour activity is found in many inhibitors that act upstream of the ERK pathway. However, drug-resistant tumour cells invariably emerge after their use due to the reactivation of ERK1/2 signalling.
View Article and Find Full Text PDFFour tropical seaweeds, Gracilaria manilaensis Yamamoto & Trono, Ulva reticulata Forsskål, Kappaphycus alvarezii (Doty) L.M.Liao and Turbinaria conoides (J.
View Article and Find Full Text PDFPrenylation of aromatic natural products by membrane-bound prenyltransferases (PTs) is an important biosynthesis step of many bioactive compounds. At present, only a few plant flavonoid-related PT genes have been functionally characterized, mainly due to the difficulties of expressing these membrane proteins. Rapid and effective methods to produce functional plant membrane proteins are thus indispensable.
View Article and Find Full Text PDFDengue virus (DV) infection is one of the main public health concerns, affecting approximately 390 million people worldwide, as reported by the World Health Organization. Yet, there is no antiviral treatment for DV infection. Therefore, the development of potent and nontoxic anti-DV, as a complement for the existing treatment strategies, is urgently needed.
View Article and Find Full Text PDFA series of C4-substituted tertiary nitrogen-bearing 2'-hydroxychalcones were designed and synthesised based on a previous mixed type acetylcholinesterase inhibitor. Majority of the 2'-hydroxychalcone analogues displayed a better inhibition against acetylcholinesterase (AChE) than butyrylcholinesterase (BuChE). Among them, compound was identified as the most potent AChE inhibitor (IC: 3.
View Article and Find Full Text PDFChitosan, as a biodegradable and biocompatible polymer, is characterized by anti-microbial and anti-cancer properties. It lately has received a widespread interest for use as the pulmonary particulate backbone materials of drug carrier for the treatment of infectious disease and cancer. The success of chitosan as pulmonary particulate drug carrier is a critical interplay of their mucoadhesive, permeation enhancement and site/cell-specific attributes.
View Article and Find Full Text PDFFlavonoids and prenylated flavonoids are active components in medicinal plant extracts which exhibit beneficial effects on human health. Prenylated flavonoids consist of a flavonoid core with a prenyl group attached to it. This prenylation process is catalyzed by prenyltranferases (PTs).
View Article and Find Full Text PDFThe limitations of existing drug delivery systems (DDS) such as non-specific bio-distribution and poor selectivity have led to the exploration of a variety of carrier platforms to facilitate highly desirable and efficient drug delivery. Stimuli-responsive DDS are one of the most versatile and innovative approach to steer the compounds to the intended sites by exploiting their responsiveness to a range of various triggers. Preparation of stimuli-responsive DDS using celluloses and their derivatives offer a remarkable advantage over conventional polymer materials.
View Article and Find Full Text PDFMarine algae have been reported as important sources of biogenic volatile halocarbons that are emitted into the atmosphere. These compounds are linked to destruction of the ozone layer, thus contributing to climate change. There may be mutual interactions between the halocarbon emission and the environment.
View Article and Find Full Text PDFIn this study, we investigate the binding interactions of two synthetic antiviral peptides (DET2 and DET4) on type II dengue virus (DENV2) envelope protein domain III. These two antiviral peptides are designed based on the domain III of the DENV2 envelope protein, which has shown significant inhibition activity in previous studies and can be potentially modified further to be active against all dengue strains. Molecular docking was performed using AutoDock Vina and the best-ranked peptide-domain III complex was further explored using molecular dynamics simulations.
View Article and Find Full Text PDFDengue virus Type 2 (DENV-2) is predominant serotype causing major dengue epidemics. There are a number of studies carried out to find its effective antiviral, however to date, there is still no molecule either from peptide or small molecules released as a drug. The present study aims to identify small molecules inhibitor from National Cancer Institute database through virtual screening.
View Article and Find Full Text PDFThe high oxygen content in natural biomass resources, such as vegetable oil or biomass-pyrolysed bio oil, is the main constraint in their implementation as a full-scale biofuel for the automotive industry. In the present study, renewable fuel with petrodiesel-like properties was produced catalytic deoxygenation of oleic acid in the absence of hydrogen (H). The deoxygenation pathway of oleic acid to bio-hydrocarbon involves decarboxylation/decarbonylation of the oxygen content from the fatty acid structure in the form of carbon dioxide (CO)/carbon monoxide (CO), with the presence of a goat manure supported Ni-Al hydrotalcite (Gm/Ni-Al) catalyst.
View Article and Find Full Text PDFBackground: Dengue infection is an endemic infectious disease and it can lead to dengue fever, dengue hemorrhagic fever, and/or dengue shock syndromes. Dengue NS2B/NS3 protease complex is essential for viral replication and is a primary target for anti-dengue drug development. In this study, a NS2B/NS3 protease inhibition assay was developed using AlphaScreen beads and was used to screen compounds for their protease inhibition activities.
View Article and Find Full Text PDFExpert Opin Drug Deliv
December 2018
Introduction: Pulmonary drug delivery is organ-specific and benefits local drug action for lung cancer. The use of nanotechnology and targeting ligand enables cellular-specific drug action. Combination approaches increase therapeutic efficacy and reduce adverse effects of cancer chemotherapeutics that have narrow therapeutic index window and high cytotoxicity levels.
View Article and Find Full Text PDFCompounds with activity at serotonin (5-hydroxytryptamine) 5-HT and α adrenergic receptors have potential for the treatment of central nervous system disorders, drug addiction or overdose. Isolaureline, dicentrine and glaucine enantiomers were synthesized, and their in vitro functional activities at human 5-HT and adrenergic α receptor subtypes were evaluated. The enantiomers of isolaureline and dicentrine acted as antagonists at 5-HT and α receptors with (R)-isolaureline showing the greatest potency (pK = 8.
View Article and Find Full Text PDFIn this study, the ()-enantiomers of the aporphine alkaloids, nuciferine and roemerine, were prepared a synthetic route involving catalytic asymmetric hydrogenation and both stereoisomers were evaluated for functional activity at human 5-HT and adrenergic α receptor subtypes using a transforming growth factor-α shedding assay. Both enantiomers of each of the compounds were found to act as antagonists at 5-HT and α receptors. ()-roemerine was the most potent compound at 5-HT and 5-HT receptors (p = 7.
View Article and Find Full Text PDFStaphylococcus aureus is a major cause of nosocomial infections and secretes a diverse spectrum of virulence determinants as well as forms biofilm. The emergence of antibiotic-resistant S. aureus highlights the need for alternative forms of therapeutics other than conventional antibiotics.
View Article and Find Full Text PDFFood Addit Contam Part A Chem Anal Control Expo Risk Assess
July 2017
Adulteration of herbal health supplements with phosphodiesterase-5 (PDE-5) inhibitors and their analogues is becoming a worldwide problem. The aim of this study was to investigate herbal and food products sold in the Malaysian market for the presence of these adulterants. Sixty-two products that claim to enhance men's sexual health were sampled between April 2014 and April 2016.
View Article and Find Full Text PDFEffective novel peptide inhibitors which targeted the domain III of the dengue envelope (E) protein by blocking dengue virus (DENV) entry into target cells, were identified. The binding affinities of these peptides towards E-protein were evaluated by using a combination of docking and explicit solvent molecular dynamics (MD) simulation methods. The interactions of these complexes were further investigated by using the Molecular Mechanics-Poisson Boltzmann Surface Area (MMPBSA) and Molecular Mechanics Generalized Born Surface Area (MMGBSA) methods.
View Article and Find Full Text PDFFive tropical seaweeds, (Doty) Doty ex P.C. Silva, Hauck, Sonder ex J.
View Article and Find Full Text PDFAim: In present study, the anti-inflammatory activities of a new series of benzimidazole derivatives were studied, investigating their inhibition of secretory phospholipase A, lipoxygenase, COXs and lipopolysaccharide-induced secretion of TNF-α and IL-6 in mouse RAW264.7 macrophages.
Results: Synthesized compounds effectively inhibited proinflammatory enzymes and cytokines.
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