Antiviral activities of anthraquinones,bianthrones and hypericin derivatives from lichens

The antiviral activities of some naturally occurring anthraquinones bianthrones, and hypericin derivatives were compared by the end-point CPE (viral cytopathic effects) method and plaque assays. Under optimal conditions of exposure to light, hypericin, 7,7-dichlorohypericin and 5,7-dichloroemodin exhibited strong inhibitory activity against HSV-1 (herpes simplex virus type 1) in both assays. Partial inactivation of the virus was shown by emodin, 7-chloroemodin and 7-chloro-1-O-methylemodin; the bianthrones and other anthraquinones were found to be inactive. Antiviral activity appeared to be, positively correlated with increasing substitution of chlorine in the anthraquinone structure. In the absence of light, only hypericin and 7,7-dichlorohypericin displayed detectable activity.     

Tumour inhibitory effects of a new class of cytotoxic agents: Methylhydrazine derivatives

Zusammenfassung Die tumorhemmende Wirkung einer neuen Klasse von Cytostatica (Methylhydrazinderivate) wird beschrieben. Das Wachstum des Ehrlich-Carcinoms in solider und ascitischer Form, des Crocker Sarkoms S 180, des Walker-Carcinosarkoms 256 und des Uterus-Epithelioms T 8 wird deutlich gehemmt. 1-Methyl-2-p-(isopropylcarbamoyl)benzyl-hydrazin-hydrochlorid (I) und 1-Methyl-2-p-allophanoylbenzyl-hydrazin-hydrobromid (II) zeichnen sich durch besonders starke cytostatische Aktivität aus.     

Dependence on the lipophilicity of maleimide derivatives in their inhibitory action upon chemotaxis in neutrophils

Summary Modification of polymorphonuclear neutrophils by a series of maleimide derivatives with various degrees of lipophilicity and hydrophilicity indicated that hydrophilic reagents had little effect on chemotaxis, whereas the degree of the inhibitory effect of lipophilic reagents on the chemotaxis was parallel to the degree of their lipophilicity.This work was supported in part by a grant-in-aid for Scientific Research (No.267043) from the Ministry of Education, Science and Culture, Japan, awarded to T.Y.     

Dependence on the lipophilicity of maleimide derivatives in their inhibitory action upon chemotaxis in neutrophils.

Modification of polymorphonuclear neutrophils by a series of maleimide derivatives with various degrees of lipophilicity and hydrophilicity indicated that hydrophilic reagents had little effect on chemotaxis, whereas the degree of the inhibitory effect of lipophilic reagents on the chemotaxis was parallel to the degree of their lipophilicity.     

Hyperventilation and inhibitory synapses

Summary Injection of a subconvulsive dose of strychnine (which blocked the inhibitory synapses) increases respiratory muscle activity evoked by stimulation of the sciatic nerve as well as by inhalation of hypercapnic gas mixture. Thus the inhibitory synapses prevent an excessive hyperventilation.     

Acetylcholinesterase in erythrocytes and lymphocytes: Its contribution to cell membrane structure and function

Summary Based on biochemical, histochemical and immunofluorescent studies on erythrocytes and lymphocytes, we propose an active function for acetylcholinesterase in membrane structure.This study was supported by a research grant from the Canadian Heart Foundation. Part of this work was presented at the 9th Meeting of Fedn. Eur. Biochem. Soc. at Budapest, 1974 and at the 3rd Meeting of Indian Immunol. Soc. at New Delhi, 1975. We thankOlivia Chiu, Barbara Pyne andBing Au for providing technical help.     

Laminar Acetylcholinesterase localization in the optic tectum of five seawater teleosts.

The histochemical localization of acetylcholinesterase in the optic tectum of seawater teleosts shows a characteristic laminar distribution which parallels the histological structure of the nervous centre. Significant differences have been observed between Gobius and the other 4 species of teleosts examined. It seems likely that cholinergic mechanisms play an important role in the function of teleost optic tectum.     

The deamino derivatives of [4-threonine]-oxytocin and [4-threonine]-mesotocin; Analogs possessing a surprising spectrum of diminished pharmacological activities

Zusammenfassung Synthese (Merrifield-Methode) und pharmakologische Eigenschaften der Desamino-Derivate von (4-Threonin)-Oxytocin und (4-Threonin)-Mesoxytocin werden beschrieben.

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This work was supported in part by the Medical College of Ohio, a Contract (No. 69-2193) from the Center for Population Research of the National Institute of Child Health and Human Development, Research Grants from the National Science Foundation (No. GB-4932), the National Institute of Arthritis and Metabolic Diseases (No. AM-01940) and a General Research Support Grant to Columbia University from the National Institutes of Health. The authors wish to thank Mrs.Sara Crumm for performing the amino acid analyses and Mrs.Margot Acosta for performing the bioassays. An abstract of part of this work was presented at the 2nd American Peptide Symposium, Cleveland, Ohio, August 1970;M. Manning andW. H. Sawyer,Peptides (Ed.Saul Lande, Gordon and Breach, New York 1971), in press.     

Evaluation of fragmented antibody inhibitory potency

Zusammenfassung Das Hemmpotential der Antikörperfragmente bei Kaninchen wird mit neuer Methode demonstriert.     

Acetylcholinesterase,acid phosphatase,and succinic dehydrogenase in the hypothalamic magnocellular nuclei after chlorpromazine administration

Zusammenfassung Der Einfluss des Chlorpromazins auf die Acetylcholinesterase, saure Phosphatase- und Bernsteinsäuredehydrogenaseaktivität des Nucleus supraopticus und Nucleus paraventricularis wurde histochemisch untersucht. Es wurde festgestellt, dass Chlorpromazin bei sämtlichen Enzymen eine mässige Herabsetzung der Aktivität bewirkt. Die Vermutung wird ausgesprochen, dass mit der Sedativwirkung des Chlorpromazins eine Verminderung der Enzymaktivität verknüpft ist.

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Aided by a grant from the Sigrid Jusélius Stiftelse.     

Acetylcholinesterase,acid phosphatase,and succinic dehydrogenase in the hypothalamic magnocellular nuclei after serotonin administration

Zusammenfassung Es wurde histochemisch festgestellt, dass Serotonin eine mässige Steigerung der Acetylcholinesterase- und sauren Phosphataseaktivität des Nucleus supraopticus und Nucleus paraventricularis bewirkt. Es wird an eine Aktivierung des N. supraopticus und N. paraventricularis durch Serotonin gedacht.

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Aided by a grant from the Sigrid Jusèlius Stiftelse.     

Effect of drugs on excitatory and inhibitory potentials inHelix aspersa

Résumé Des produits chimiques furent injectés à l'escargotHelix aspersa. Leur effet fut enregistré en potentiels postsynaptiques. L'hemicholinium réduit l'amplitude d'un potentiel postsynaptique d'excitation cholinergique. L'-Methyl-5-HTP et lep-chlorophenylalanine ou résperpine font décroître l'amplitude d'un potentiel postsynaptique d'exication 5-HT, le 6-Hydroxydopamine diminue celle d'un potentiel postsynaptique d'inhibition dopamine tandis que le DOPA l'augmente.     

Metabolism and signaling activities of nuclear lipids

Apart from the lipids present in the nuclear envelope, the nucleus also contains lipids which are located further inside and are resistant to treatment with nonionic detergents. Evidence is being accumulated on the importance of internal nuclear lipid metabolism. Nuclear lipid metabolism gives rise to several lipid second messengers that function within the nucleus. Moreover, it is beginning to emerge that nuclear lipids not only act as precursors of bioactive second messengers but may be directly involved in regulation of nuclear structure and gene expression. Over the last 10years, especially the role of the inositol lipid cycle in nuclear signal transduction has been extensively studied. This cycle is activated following a variety of stimuli and is regulated independently from the inositide cycle located at the plasma membrane. However, the nucleus contain other lipids, such as phosphatidylcholine, sphingomyelin, fatty acids and eicosanoids. There are numerous reports which suggest that these classes of nuclear lipids may play roles in the nucleus as important as those of phosphoinositides. This review aims at highlighting the most important aspects regarding the metabolism and signaling activities of nuclear phosphatidylcholine, sphingomyelin, fatty acids and eicosanoids.Received 7 November 2003; received after revision 18 December 2003; accepted 29 December 2003