New Proctolin Analogues: Synthesis and Biological Investigation in Insects

We have extended our work on structure/activity relationship studies of the neuropeptiden proctolin (H-Arg-Tyr-Leu-Pro-Thr-OH) by evaluating the effects of the following proctolin analogues: H-X¹-Tyr-Leu-Pro-Thr-OH, where X¹ = D-Arg (I), N-Me-Arg (II), Can (III), Orn(di-Me) (IV), Orn(iPr) (V), Lys(N, N-di-Me) (VI), Lys(iPr) (VII), Lys(Nic) (VIII) and D-Lys(Nic) (IX). In analogues I–IX, the N-terminal Arg residue was replaced by basic amino acid derivatives with peptides containing amino acid residues with an isosteric system on the back side chain relative to Arg (compounds III, V and VI) or homo-Arg (compound VII). Analogues I–IX were evaluated for myotropic activity on the in vitro heart preparation of Tenebrio molitor, whereas peptides II, V, and VII–IX were tested for contractile activity on the isolated foregut of locust Schistocerca gregaria. Peptide II and III showed full cardiotropic activity in T. molitor while peptides V and VII showed 40% and 15%, respectively, locust-gut contracting activity of proctolin.     

Kinematics of soft-bodied, legged locomotion in Manduca sexta larvae

Caterpillar crawling is distinct from that of worms and molluscs; it consists of a series of steps in different body segments that can be compared to walking and running in animals with stiff skeletons. Using a three-dimensional kinematic analysis of horizontal crawling in Manduca sexta, the tobacco hornworm, we found that the phase of vertical displacement in the posterior segments substantially led changes in horizontal velocity and the segments appeared to pivot around the attached claspers. Both of the motions occur during vertebrate walking. In contrast, vertical displacement and horizontal velocity in the anterior proleg-bearing segments were in phase, as expected for running gaits coupled by elastic storage. We propose that this kinematic similarity to running results from the muscular compression and release of elastic tissues. As evidence in support of this proposal, the compression and extension of each segment were similar to harmonic oscillations in a spring, although changes in velocity were 70 degrees out of phase with displacement, suggesting that the spring was damped. Measurements of segment length within, and across, intersegmental boundaries show that some of these movements were caused by folding of the body wall between segments. These findings demonstrate that caterpillar crawling is not simply the forward progression of a peristaltic wave but has kinetic components that vary between segments. Although these movements can be compared to legged locomotion in animals with stiff skeletons, the underlying mechanisms of caterpillar propulsion, and in particular the contribution of elastic tissues, remain to be discovered.     

New Proctolin Analogues: Synthesis and Biological Investigation in Insects

Summary We have extended our work on structure/activity relationship studies of the neuropeptiden proctolin (H-Arg-Tyr-Leu-Pro-Thr-OH) by evaluating the effects of the following proctolin analogues: H-X¹-Tyr-Leu-Pro-Thr-OH, where X¹=d-Arg(I),N-Me-Arg (II), Can (III), Orn(di-Me) (IV), Orn (iPr) (V), Lys(N, N-di-Me) (VI), Lys(iPr) (VII), Lys(Nic) (VIII) andd-Lys(Nic) (IX). In analogues I–IX, the N-terminal Arg residue was replaced by basic amino acid derivatives with peptides containing amino acid residues with an isosteric system on the back side chain relative to Arg (compounds III, V and VI) orhomo-Arg (compound VII). Analogues I–IX were evaluated for myotropic activity on thein vitro heart preparation ofTenebrio molitor, whereas peptides II, V, and VII–IX were tested for contractile activity on the isolated foregut of locustSchistocerca gregaria. Peptide II and III showed full cardiotropic activity inT. molitor while peptides V and VII showed 40% and 15%, respectively, locust-gut contracting activity of proctolin.