Re- and demineralization characteristics of dentin depending on fluoride application and baseline characteristics in situ.

OBJECTIVES: The aim of this double-blinded, randomized, cross-over in situ study was to evaluate the re- and demineralization characteristics of sound dentin as well as highly and lowly demineralized dentin after the application of different fluoride concentrations. METHODS: In each of four experimental legs of four weeks 20 participants wore intraoral mandibular appliances containing two (highly demineralized [EH]) bovine enamel and four (lowly and highly demineralized [DL,DH]) bovine dentin specimens (n = 480). Each specimen included one sound (ST) and one demineralized lesion area (DT). The four randomly allocated treatments included the following dentifrices: fluoride-free, zinc-carbonate-nano-hydroxyapatite [nHA0], 0 ppm F- [negative control,NaF0], 1100 ppm F- as NaF [standard therapy,NaF1100] and 5000 ppm F- as NaF [positive control,NaF5000]. Differences in integrated mineral loss (ΔΔZ) and lesion depth (ΔLD) were calculated between values before and after the in situ period using transversal microradiography. RESULTS: After the in situ period specimens of nHA0 and NaF0 showed signs of demineralization, indicated by significantly lower ΔZ&LD values for EH and DL (only nHA0)(p ≤ 0.028), whereas specimens of NaF1100 and NaF5000 showed signs of remineralization, indicated by significantly higher ΔZ values for EH (only NaF5000), DL and DH (p ≤ 0.012). The correlation between ΔΔZDT/ΔΔZST and F- was moderate for EH(rDT = 0.497;rST = 0.463) and DL(rDT = 0.575;rST = 0.598) and strong for DH(rDH = 0.700;rST = 0.611)(p < 0.001). No significant differences for ΔΔZDT/ΔΔZST were observed between nHA0 and NaF0(p ≥ 0.333;ANCOVA). CONCLUSION: The present in situ model was capable to reveal a fluoride dose-response on sound, lowly and highly demineralized dentin and also enamel specimens. Furthermore, both fluoride-free dentifrices, one containing nanohydroxyapatite, did not hamper demineralization. CLINICAL SIGNIFICANCE: The present in situ model was capable to reveal a fluoride dose-response on dentin similar to the anticipated clinical efficacy. Highly demineralized specimens seem to be recommendable for measuring anti-caries effects on dentin in situ. Furthermore both fluoride-free dentifrices, one containing nanohydroxyapatite, did not hamper demineralization. The study was registered in the German Clinical Trials Register (DRKS-ID: DRKS00011653).

Synthesis of the porcine intestinal peptide PHI and its 24-glutamine analogue.

PHI--a new candidate hormone from porcine intestinal tract-- corresponds to a linear heptacosapeptide amide of remarkable sequence homology to the known members of the glucagon family, particularly to the vasoactive intestinal peptide (VIP) and secretin. The position 24 usually occupied by an aminodicarboxylic acid omega-amide, in the present case, however, carries a glutamic acid, thus opening the question of whether this structural feature is related to desamidation in one of the isolation and characterization steps or of whether it is significant for this peptide factor. Consequently the heptacosapeptide amides corresponding to the proposed primary structure and to its 24-glutamine analogue have been synthesized. Comparative chromatographic and biological studies on the natural and the two synthetic products have confirmed the correctness of the primary structure proposed for the isolated PHI. Since [24-glutamic acid] and [24-glutamine]PHI exhibit no significant differences in their biological potencies, the main question is still open of whether the position 24 in native PHI is occupied by the aminodicarboxylic acid omega-amide (glutamine) or by N-substituted derivatives (N-glycosyl).

[Total synthesis of somatostatin-28 (author's transl)]. / Totalsynthese von Somatostatin-28.

The total synthesis of the octacosapeptide corresponding to the proposed primary structure of porcine somatostatin-28 is described. The synthesis has been performed using a protection scheme of maximum selectivity (acid labile side chain protection based on tert-butyl alcohol and 1-adamantol derived protecting groups in combination with the S-tert-butylthio group for reversible and selective blocking of the cysteine thiol functions and the 2-nitrophenylthio group for the temporary protection of the alpha-amino functions of intermediate segments) and of carefully selected fragments. Upon assembly in sequence order of the four suitably protected fragments related to sequences 18-28, 15-17, 8-14 and 1-7, the asymmetric disulfides were reduced by exposure of the fully protected octacosapeptide to phosphines. Subsequently, the final deprotection was performed with trifluoroacetic acid and the resulting dihydrosomatostatin-28 was then converted by air oxidation into the "cyclic peptide". Gel filtration on Biogel P-6 and ion-exchange chromatography on Biogel CM-2 produced somatostatin-28 at a high degree of purity. Comparative analysis of the synthetic and natural product by means of chromatographic, immunological and biological assays confirmed the structure proposed for this putative precursor of somatostatin-14.