Synthesis, conformation, and biological activity of the carbohydrate-free vespulakinin 1

Synthesis of the carbohydrate-free heptadecapeptide corresponding to the amino acid sequence of vespulakinin 1 was achieved by the continuous flow solid phase procedure on 4-hydroxymethyl-phenoxyacetyl-norleucyl derivatized Kieselguhr-supported polydimethylacrylamide resin, as well as by a combination of solid phase and solution syntheses. Preformed Fmoc-amino acid symmetrical anhydrides (Boc derivative for the N-terminal residue) were used for amine acylation in the continuous flow method. Serine and threonine were side chain protected as tert.-butyl ethers and the 4-methoxy-2, 3, 6,-trimethyl-benzenesulfonyl group was used for masking the guanidino function of arginine residues. After cleavage from the resin the final peptide was purified by ion exchange chromatography and characterized by amino acid analysis, high voltage electrophoresis, and RP-HPLC analysis. Alternatively, the protected N-terminal octapeptide, Fmoc-Thr(But)-Ala-Thr(But)-Thr(But)-Arg(Mtr)-Arg-(Mtr)-Arg(Mtr)-Gly-OH was prepared on 4-hydroxymethyl-3-methoxyphenoxyacetyl-norleucyl derivatized Kieselguhr-supported polydimethylacrylamide resin and the C-terminal nonapeptide H-Arg(NO2)-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg-(NO2)-OBzl was synthesized in solution through the fragment condensation method. The two fragments were coupled by the DCC-HOBt procedure and the resulting heptadecapeptide was deblocked and purified. The conformational features of the synthesized peptides are reported. Preliminary pharmacological experiments indicated that carbohydrate-free vespulakinin 1 is more potent than bradykinin in lowering rat blood pressure.     

The synthesis and 16S A-site rRNA recognition of carbohydrate-free aminoglycosides

The first carbohydrate-free aminoglycoside analogs bearing the 2-deoxystreptamine moiety were synthesized from asymmetrically protected 2-deoxystrepamine and subsequently demonstrated to have significant binding to the 16S A-site rRNA target and moderate functional activity.     

New ideas on the origin of bilateral animals

Comparative anatomy and embryology provide impressive evidence that the ventral side of all Bilateria (except Chordata) originates from the blastoporal surface, while the mouth and anus develop, respectively, from the anterior and posterior extremities of an elongated blastopore. From the point of view of paleontology, some Vendian multicellular animals represent transitional forms between Radiata and Bilateria. Vendian Bilateria are metameric organisms with a symmetrical or asymmetrical arrangement of segments; they can be considered as bilaterally symmetrical coelenterates crawling on the oral surface. In the recent Cnidaria, homologues of the genes “Brachyury,” “goosecoid” and “fork head” are expressed around the mouth. In the recent Bilateria these genes are expressed along the elongated blastopore and around the mouth and anus. These data corroborate the validity of the idea of amphistomy and the homology between the ventral surface in Bilateria and oral disk in coelenterates. It is supposed that the ancestors of Bilateria were crawling on the oral surface (=ventral side) and gave rise to both Fanerozoic Cnidaria and triploblastic Bilateria. This allows us to suggest the origin of Bilateria from Vendian bilaterally symmetrical coelenterates with numerous metameric pockets of the gastral cavity. Such ancestors gave rise to both Cnidaria and Bilateria. Apparently the primary Bilateria were complicated organisms having a coelom and segmentation, which allows us to explain the great diversity of highly organized organisms (arthropods, mollusks, and others) in the Cambrian era. An idea is proposed that Ctenophora are the only group of recent Eumetazoa that retain primary axial symmetry.     

Plato on kinds of animals

Some biologists and philosophers of biology have seen in Plato an especially objectionable version of essentialism or topology. Although kinds of animals are mentioned in almost all of Plato's dialogues, in none of them is there an explicity stated doctrine of animal kinds. An examination of the dialogues has, moreover, failed to reveal some implicit but consistent and unambiguous view of kinds that Plato might have held.