Extraction, isolation and characterization of Andrographis paniculata (A.p.) products were developed. Three natural diterpenes compounds were obtained and one was used for chemical modifications. Evaluation of their inhibition of TNFα induced NFκB transcriptional activity. A rapid analytical method for the determination and quantitation of three diterpenoid lactones (andrographolide 1, didehydroandrographolide 2, neoandrographiside 3) found in A. paniculata extracts was investigated. After some optimizations on column type and injection solvent, the separation was achieved in 9 min on a monolithic Chromolith Performance RP18e column (100 mm × 4.6 mm ID, 2 µm), with a gradient solvent system of water and methanol, UV detection at 220 nm and ELSD detection. The method was proved to be suitable for the quantitation of these three diterpenes in four different commercial Andrographis dietary supplements. The anti-inflammatory activities of a mixture of known composition have been evaluated showing differences in activity depending on the relative ratio of various diterpenes and also a possible synergic activity for some of them.
We report here the use of eucalyptol as a bio-based solvent for Hiyama coupling, cyanation, and multicomponent reactions on O,S,N-heterocycles. These heterocycles were chosen as targets or as starting materials given their biological potential; they play an important role in therapeutically active compounds. Once again, eucalyptol proved to be a credible and sustainable alternative to common solvents.
Pyrazine-fused 1,2,6,6a-tetrazapentalenes
(PyTeAP) are zwitterionic
tricyclic compounds exhibiting an original pattern with four consecutive
nitrogen atoms. They were obtained by a challenging cyclization through
the formation of a N–N bond under thermolytic conditions. Ten
derivatives were synthesized, and the original scaffold of PyTeAP
was confirmed by single-crystal X-ray diffraction analysis of one
derivative. Examination of their photophysical properties in solution
revealed blue fluorescence with λem = 416–426
nm. Theoretical investigations of the aromaticity in these compounds
through magnetic criteria evidenced the presence of a dominant 14-electron
circuit at the periphery.
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