Selective inhibition of carbonic anhydrase IX and XII by coumarin and psoralen derivatives

A small library of coumarin and their psoralen analogues EMAC10157a-b-d-g and EMAC10160a-b-d-g has been designed and synthesised to investigate the effect of structural modifications on their inhibition ability and selectivity profile towards carbonic anhydrase isoforms I, II, IX, and XII. None of the new compounds exhibited activity towards hCA I and II isozymes. Conversely, both coumarin and psoralen derivatives were active against tumour associated isoforms IX and XII in the low micromolar or nanomolar range of concentration. These data further corroborate our previous findings on analogous derivatives, confirming that both coumarins and psoralens are interesting scaffolds for the design of isozyme selective hCA inhibitors.     

Update on the presence of taste buds on the laryngeal surface of the epiglottis]

Previous investigations have ascertained, according to the results obtained by Bradley et al. (1980) in the sheep, that the laryngeal surface of the epiglottis of goat and bovine is always provided with numerous taste buds. These observations have verified in other ruminant species, as the moufflon and the buffalo, the validity of the above-named datum and have ascertained that it is always inconstant in the other animal species considered (wild boar, coypu). These taste buds show a typical structure (diameter of the outer taste pore varying from 2.7 to 4.2 micron, width of the chemoreceptors varying from 30 to 60 micron and length from 27.5 to 57.5 micron). Moreover, the normal structure of the above-named taste buds is also testified by the arrangement of their innervation and particularly by the integrity of the synaptic contacts. The results of the present research have permitted a critical and more severe examination of the probable functional role of those laryngeal receptors. In fact, in the ruminants they may protect the deep airways precluding to food particles the larynx in the phase of food regurgitation.     

Saponification of Methylated Mucosubstances at Low Temperatures

A fresh 1% solution of KOH in 70% ethanol in 2 hr at 2-4 C restores basophilia to methylated acid mucosubstances satisfactorily without detaching or damaging tissue sections. A 0.5% solution of Ba(OH)₂ under the same conditions gives results nearly as good, but NaOH and KMnO₄ are unsatisfactory.