We have extended our studies on the structure-activity relationship in neuropeptide proctolin (Arg-Tyr-Leu-Pro-Thr) by evaluating the effects of a series of proctolin analogues modified in position 2 of the peptide chain, including: [Phe(p-Cl)2]- (1), [D-Phe(p-Cl)2]- (2), [N-Me-Tyr2]- (3), [D-Phe(p-NH2)2]- (4), [D-Phe(p-N,N-di-Me)2]- (5), [N-Me-Tyr(OMe)]- (6), [D-3-Pal2]- (7), [L-Nal2]- (8), [D-Nal2]- (9), [Lys(Nic)2]- (10), [D-Lys(Nic)2]- (11), [D-Phe-(p-NO2)2]- (12). These peptides were evaluated for myotropic activity on the heart of Tenebrio molitor and contractile activity of the foregut of Schistocerca gregaria. Analogues 1-5, 7-9, and 12 retained a weak cardiotropic activity in Tenebrio molitor while peptides 1, 8 and 12 preserved 15-25% of the locust-gut contracting activity of proctolin. Peptides 2, 4 and 7 showed weak inhibitory activity in Schistocerca gregaria foregut, whereas only peptides 4 and 7 reduced the maximum response to applied proctolin by 64% and 49% respectively, at the 10(-6) M concentration.

Animals↗

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Myotropic effects of new proctolin analogues modified in the position 5 of peptide chain in insects.

To explain the role of the Thr5 residue of proctolin (Arg-Tyr-Leu-Pro-Thr) in the myotropic activity of this insect neuropeptide, we synthesized two groups of its analogues: 1) Arg-Tyr-Leu-Pro-X-OH with X = Val (1), D-Val (2), Ile (3), D-Ile (4), Ala (5), D-Ala (6), Asn (7), Gln (8), Ser (9), Pro (10), Phe (11), Asp (12), Glu (13), Arg (14), D-Arg (15), Lys (16) and Gly (17) and 2) Arg-Tyr-Leu-Pro-R', where R' = isobutylamine (18), S-1-methyl-1-phenylmethylamine (19), R-1-methyl-1-phenylmethylamine (20), R-2-amino-1-propanol (21), S-2-amino-1-propanol (22), R-1-amino-2-propanol (23), S-2-amino-1-propanol (24), 3-amino-1-propanol (25). Decapeptide proctolylproctolin (H-Arg-Tyr-Leu-Pro-Thr-Arg-Tyr-Leu-Pro-Thr-OH) (26) was synthesized. Syntheses of these peptides were carried out by solid-phase method. All peptides were bioassayed in vitro on the semi-isolated hearts of Tenebrio molitor using a cardioexcitatory test and on the foregut of locust (Schistocerca gregaria). Peptides 1, 3, 5, 9, 13, 14, 16, 22, and 23 retained about 30-50% of the cardioexcitatory activity in T. molitor. Analogues 1 and 3 preserved about 50% and analogue 8 about 80% of the myotropic activity, whereas compound 4 and 9 showed a very weak contractile activity in S. gregaria.

Animals↗

PubMedDate not supplied

Tradimus. An end to the Project.

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Education, Nursing↗

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APHEDA, ACTU aid agency, takes union humanitarian ideals abroad.

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Altruism↗

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Relationship of difficult forceps delivery to dental arches and occlusion.

This study examined the relationship between the extensive use of forceps procedures during delivery and later occlusal characteristics. The work uses data collected in National Collaborative Perinatal Research Project (USA), in which more than 60,000 pregnancies and the children's health were followed by regular medical tests and examinations. Of these, a subsample of 2,074 children participated in dental examinations, including the production of dental casts with wax bites to register occlusion. A total of 84 children, 55 boys and 29 girls, were coded as having undergone difficult or very difficult forceps deliveries. A control group was matched by age, sex, race, and site of dental examination. The results show a significant increase in asymmetric molar occlusion (P < 0.005) and canine relations (P < 0.001) in the study group. The sagittal length of the mandibular arch was increased in the difficult forceps delivery group (P < 0.01). In conclusion, difficult forceps procedures are associated with a later asymmetric occlusion.

Birth Injuries↗

PubMedDate not supplied

New proctolin analogues and their myotropic effects on heart of yellow mealworm Tenebrio molitor L. and foregut of locust-Schistocerca gregaria L.

We have extended our work on structure/activity relationship of neuropeptide 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 (1), N-Me-Arg (2), Can (3), D-Tyr2, D-Leu3, D-Thr5]-proctolin (12). In analogues 1-9, 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 3, 5 and 6) or homo-Arg (compound 7). Analogues 1-12 were evaluated for myotropic action on in vitro heart preparation of Tenebrio molitor, whereas peptides 2, 5 and 7-12 were tested for contractile action on isolated foregut of Schistocerca gregaria. Peptides 2 and 3 retained full cardiotropic activity in Tenebrio molitor while peptides 5 and 7 preserved 40% and 15%, respectively, locust-gut contracting activity of proctolin. Peptides 11 and 12 showed antagonistic activity in Schistocerca gregaria foregut.

Animals↗