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1.
Peptides ; 41: 107-12, 2013 Mar.
Article in English | MEDLINE | ID: mdl-23246802

ABSTRACT

The insect sulfakinins (SKs) constitute a family of neuropeptides that display both structural and functional similarities to the mammalian hormones gastrin and cholecystokinin (CCK). As a multifunctional neuropeptide, SKs are involved in muscle contractions as well as food intake regulation in many insects. In the red flour beetle Tribolium castaneum, the action on food intake by a series of synthetic SK analogs and one putative antagonist was investigated by injection in beetle adults. The most remarkable result was that both sulfated and non-sulfated SKs [FDDY(SO3H)GHMRFamide] inhibited food intake by about 70%. Strong activity observed for SK analogs featuring a residue that mimics the acidic nature of Tyr(SO3H) but lack the phenyl ring of Tyr, indicate that aromaticity is not a critical characteristic for this position of the peptide. SK demonstrated considerable tolerance to Ser and Ala substitution in position 8 (basic Arg), as analogs featuring these uncharged substitutions retained almost all of the food intake inhibitory activity. Also, the Phe in position 1 could be replaced by Ser without complete loss of activity. Conversely, substitution of Met by Nle in position 7 led to inactive compounds. Finally, the Caenorhabditis elegans sulfated neuropeptide-like protein-12 (NLP-12), that shares some sequence similarities with the SKs but features a Gln-Phe-amide rather than an Arg-Phe-amide at the C-terminus, elicited increased food intake in T. castaneum, which may indicate an antagonist activity. Co-injection of NLP-12 with nsSK blocked the food intake inhibitory effects of nsSK.


Subject(s)
Caenorhabditis elegans Proteins/pharmacology , Energy Intake/drug effects , Insect Proteins/pharmacology , Neuropeptides/pharmacology , Tribolium/drug effects , Amino Acid Sequence , Animals , Caenorhabditis elegans Proteins/chemistry , Eating , Insect Proteins/chemistry , Neuropeptides/chemistry , Structure-Activity Relationship , Tribolium/physiology
2.
Nat Prod Commun ; 4(9): 1287-90, 2009 Sep.
Article in English | MEDLINE | ID: mdl-19831046

ABSTRACT

Essential oils extracted from leaves of Aloysia polystachya and A. citriodora (Verbenaceae) and from leaves and fruits of Schinus molle var. areira (Anacardiaceae) were tested for their repellent and toxic activities against adults of Rhizopertha dominica (Coleoptera: Bostrichidae). Topical application and filter paper assays were employed for contact toxicity studies; filter paper impregnation was also used for fumigant and repellent assays. In topical tests A. polystachya was as effective as S. molle leaves. In the case of repellent assays, A. citriodora was the most effective oil based on the class scale. A. polystachya was the most toxic plant on contact toxicity by filter paper assay (LC50 26.6 mg/cm2). Fumigant toxicity was only evaluated with fruits and leaves of S. molle, and no significant differences were found between them. Published data are included to compare the fumigant toxicity of S. molle with that of A. citridora and A. polystachya.


Subject(s)
Anacardiaceae/chemistry , Insect Repellents/isolation & purification , Plant Oils/chemistry , Terpenes/isolation & purification , Verbenaceae/chemistry , Animals , Biological Assay , Female , Fruit/chemistry , Gas Chromatography-Mass Spectrometry , Insect Repellents/chemistry , Insecta , Male , Oils, Volatile/chemistry , Plant Leaves/chemistry , Terpenes/chemistry
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