Disruption of mitochondrial function as the basis of the trypanocidal effect of trifluoperazine onTrypanosoma cruzi

Summary The tricyclic anti-calmodulin drug trifluoperazine (TFP) inhibited growth and motility of epimastigotes ofTrypanosoma cruzi, at concentrations lower than 100 M, and motility and infectivity of the bloodstream trypomastigote form at 200 M. Electron microscopy of TFP-treated epimastigotes showed that the major effect was at the mitochondrial level, with gross swelling and disorganization. The oligomycin-sensitive, mitochondrial ATPase was completely inhibited by 20 M TFP, and the same drug concentration caused a 60% decrease in intracellular ATP content. The results suggest that the trypanocidal effect of TFP may be related more to mitochondrial damage than to the well-known anticalmodulin effect of the drug.     

Metabolism of 3β-hydroxycholest-5-en-26-oic acid in hamsters

Summary Metabolism of 26-hydroxycholesterol to 3-hydroxychol-5-en-24-oic acid and other C24-bile acids has been expected to occur by way of 3-hydroxycholest-5-en-26-oic acid in studies in vitro. 3-Hydroxycholest-5-en-26-oic acid was infused intravenously into bile fistula hamsters and the following C24-bile acids were identified: 3-hydroxychol-5-en-24-oic acid, lithocholic acid, chenodeoxycholic acid, and a small amount of cholic acid.     

Effect of feeding cereal-legume diets to rats on in vitro absorption of45Ca

Summary The in vitro absorption of calcium from the duodenum was significantly less in a group of rats fed on a wheat diet than in a group fed a wheat and Bengal gram (7030) diet.     

Dissociation of glucocorticoid effects of C-21 steroids at high concentrations in thymocytes

Summary A dissociation between inhibition of RNA synthesis and cell lysis was observed when thymocytes of adrenalectomized rats were incubated with high concentrations of pregn-4-ene-11-ol-3, 20-dione and pregna-1,4-diene-11-ol-3,20-dione. In contrast, no dissociation of these effects was found with the typical glucocorticoids cortisol and corticosterone, nor with their 1,4-diene analogs under the same conditions.Acknowledgments. This work was supported by grants from the Consejo Nacional de Investigaciones Científicas y Técnicas de la República Argentina to the Instituto de Biologia y Medicina Experimental and the Programa de Regulación Hormonal y Metabólica as well as by financial help from the Secretaría de Ciencia y Tecnología.     

A new semisynthetic ergot peptide alkaloid: DCN 203-922

Summary We report the synthesis, stereochemistry and preliminary pharmacological evaluation of DCN 203-922, a novel ergot alkaloid of the cyclol type, which contains in its peptide moiety the uncommon amino acid L-allo-isoleucine.Part of this paper was reported by this author at the Herbstversammlung der Schweizerischen Chemischen Gesellschaft, Bern, in October 1986.     

Biosynthesis of 1-aminocyclopropanecarboxylic acid: Steric course of the reaction at the C-4 position

Summary Under the action of the appropriate synthase from ripe tomatoes a 11 mixture of (3S, 4R)-[3,4-²H₂] and (3R, 4S)-[3,4-²H₂]-(2S)-adenosylmethionine is transformed into a 11 mixture of the two meso forms of [²H₂]-1-aminocyclopropanecarboxylic acid, a result which proves the operation of an inversion mechanism and which is consistent with direct nucleophilic displacement of the leaving group in the substrate.     

Molt-induced muscle atrophy decreases the zinc content of the pectoralis of the Giant Canada Goose (Branta canadensis maxima)

Summary During molt-induced atrophy of the pectoralis muscle of the Giant Canada Goose (Branta canadensis maxima), the zinc content of the muscle was significantly reduced (p0.0139), though the concentration of zinc per unit weight of muscle appeared higher (p0.0232). Zinc lost from the muscle during molt could be utilized for growth of the new flight feathers.Acknowledgments. Funds for this study were obtained from an operating grant awarded to J. C. G. by the Natural Sciences and Engineering Research Council of Canada.     

Excretion of acid hydrolases during molting inPhilosamia ricini

Summary The level of the acid hydrolases -glucuronidase (EC 3.2.3.11), acid phosphatase (EC 3.1.3.2) and acid protease (EC 3.4.4) was studied during larval growth and molting inP. ricini. The level of activity of these enzymes remained low during larval growth; however, the level increased sharply at the time of molting and declined sharply thereafter in the newly ecdysed insect. Interestingly, the diminished activity of these enzymes was almost quantitatively recovered in the cast-off cuticle. The excretion of acid hydrolases through the cast-off cuticle has hitherto not been reported in insects during molting.     

Isolation and partial characterization of cuticular collagen from the parasitic nematodeGaigeria pachyscelis

Summary The cuticle from adultGaigeria pachyscelis was isolated by solubilizing the internal tissues with sodium dodecyl sulphate (SDS) at 37°C. Cuticular protein was extracted with guanidine-HCl and -mercaptoethanol and purified by ammonium sulphate fractionation and DEAE-cellulose chromatography. SDS-polyacrylamide gel electrophoresis of purified protein revealed 2 polypeptides with apparent mol. wts of 58,000 and 74,000. As judged from their hydroxyproline content both of them are collagenous in nature. Results of gel filtration indicate that cuticular collagen exists in two forms, a non-associated form at low concentration and an associated form at high concentration.Acknowledgments. We thank Drs L.N. Singh and H.C. Tewari for providing the necessary facilities. Laboratory assistance of Mr Ram Kishore is highly appreciated.