The fungal meroterpenoid
biosynthetic pathways exhibit an abundance of unusual chemistries and
interesting enzyme reactions, including those of the multi-functional non-heme Fe(II)- and 2-oxoglutarate-dependent oxygenases that
perform selective C–H activation/functionalization
with unusual substrate promiscuity and catalytic versatility. Structure–function studies of these remarkable enzymes provide
an excellent platform for the development of useful biocatalysts for synthetic
biology to create novel molecules for drug discovery.
Rubbing actions are often conducted to apply
topical formulations onto the skin. However,
few studies have reported the reasons for the acceleration of drug permeation
through skin after topical application with or without rubbing. In addition, no
studies observed the effect of rubbing direction on the skin
penetration-enhancement effects. In this paper, the
authors investigated the
effects of rubbing direction on the skin permeation and disposition of a model
hydrophilic drug, caffeine. This paper provides useful
information on the effect of rubbing action and rubbing
direction on the skin permeation of topically applied drugs.
Marine dinoflagellates are well known as rich
sources of biologically active compounds possessing unique chemical structures.
This paper deals isolation and structure elucidation of two new cytotoxic 15-membered
macrolides, iriomoteolodes-14a and 14b, from the marine dinoflagellate Amphidinium
species collected off Iriomote Island, Okinawa. The structures including the
absolute stereochemistry of eight stereocenters were determined on basis of
spectroscopic data and chemical conversion method. These compounds are
analogous to known macrolides, amphidinolides O and P, and the biosynthetic
relationships for four compounds are also described.
Quantitative nuclear magnetic resonance is
a powerful tool in quantitative determination of the main component and
impurities in a drug substance or a drug product because of its high accuracy,
precision and efficiency. This method has the potential to establish
metrological traceability easily and expected to be widely utilized for some compendial guidelines and official
standards. In this study, the authors conducted
an inter-laboratory comparison for qNMR methodology and confirmed that statistically
qNMR has the competence to obtain the same quantification performance and
accuracy as the conventional reliable methods.
generation plays a major role in hemin/peroxide-induced oxidative stress. The authors developed a
method for trapping tyrosyl radicals using a derivative of N-methyl
luminol, a tyrosine labeling reagent. The
derivative selectively forms a covalent bond with tyrosine residue (tyrosine
click reaction) under single-electron oxidation conditions. This reaction
labels oxidative stress hotspots not only at the protein level but also at the
level of tyrosine residues undergoing oxidation. The cover picture depicts
an image of tyrosine click reaction to aid in the visualization of
hemin/peroxide-induced oxidative stress generated in blood vessels.
Synthesis of Hydroxybenzofuranyl-pyrazolyl and Hydroxyphenyl-pyrazolyl Chalcones and Their Corresponding Pyrazoline Derivatives as COX Inhibitors, Anti-inflammatory and Gastroprotective Agents
Released: August 01, 2020 | Volume 68 Issue 8 Pages 742-752
Fatma Abd El-Fattah Ragab, Enas Ibrahim Mohammed, Gehad A. Abdel Jaleel, Ahmed Abbass Mohamed Abd El-Rahman Selim, Yassin Mohammed Nissan