Chemotherapeutic effects of 4-isothiocyanato-4′-nitrodiphenylamine (C9333-Go/CGP 4540) on infections withNematospiroides dubius,Hymenolepis diminuta,Hymenolepis nana andSpirometra mansonoides

Summary 4-Isothiocyanato-4-nitrodiphenylamine possessed anthelmintic activity againstNippostrongylus dubius andHymenolepis nana in mice andH. diminuta in rats as determined by both egg counts and recovery of parasites at autopsy. No activity was detected against the cestode,Spirometra mansonoides, in cats.This investigation was supported in part by grants AI-10512 and AI-09483 from the National Institutes of Health. The authors are indebted to Dr P.P. Weinstein for providing animals infected withSpirometra mansonoides.     

Production and detection of antibody against estradiol receptor in the calf uterus. Interaction with the estrogen receptor from the hen oviduct]

The antibodies against estrogen receptor were obtained after injecting Rabbits with a cytoplasmic receptor fraction isolated from Calf uterus. The estrogen receptor was partially proteolysed by the action of trypsin and subsequently purified by affinity chromatography (purification 4,000 to 10,000 fold, to a purity of 5-20%). The affinity of the antibody for the proteolysed receptor is KD approximately 1 nM and serum titres have reached values of approximately 50 nM. The values remained constant after the third injection. Preliminary results indicate that the antibody has approximately the same affinity for "native" cytoplasmic estrogen receptor from Calf uterus, as well as for the "trypsinized" forms of estrogen receptor isolated from Calf uterine cytosol and Hen oviduct nuclei.     

Effects of several preoperative medications on fat cell lipolysis, and activity of adipose tissue cyclic AMP phosphodiesterase.

Effects were examined of atropine, diazepam, pethidene, promethazine, scopolamine, omnopon and papaverine on basal and noradrenaline-stimulated lipolysis in rat isolated fat cells and on rat adipose tissue cyclic AMP phosphodiesterase activity. Papaverine at high concentration (1 mM) inhibited both basal and hormone-stimulated lipolysis, whereas diazepam enhanced basal lipolysis. At a 'clinical dose', omnopon increased both basal and noradrenaline-stimulated lipolysis. Adipose tissue cAMP phosphodiesterase activity was strongly inhibited by 1 mM diazepam, papaverine, promethazine and omnopon (280 microgram ml-1). Lack of enhancement of lipolysis by the established cAMP phosphodiesterase antagonist papaverine, is compatible with simultaneous inhibition also of adipose adenyl cyclase. Diazepam-stimulated lipolysis is compatible with its phosphodiesterase inhibitory activity. It is proposed that papaverine-containing omnopon may offer some survival advantages during surgical stress by facilitating a caloric supply.     

Impaired amylase release from the parotid gland of rats treated with reserpine.

Using an automated system for the analysis of amylase, the release of this enzyme was compared in superfused parotid gland segments from control and reserpine treated rats. Stimulant-evoked amylase release was delayed and of smaller magnitude in the glands of the treated animals and a reduction of the transmembrane K+ gradient caused a smaller and short lasting reduction in Ach-evoked release of amylase in the glands from these animals.     

Affinity chromatography of human serum proteins using matrix bound lectin fromViscum album L.

Summary The D-galactose specific lectin fromViscum album L. reacts with serum proteins that contain the corresponding D-galactopyranosyl residues. By affinity chromatography of human serum on lectin-sepharose IgM, ₂-macroglobulin, haptoglobin and -lipoprotein were quantitatively retained. Only parts of IgA, IgG and transferrin were retarded. The other serum proteins are unbounded as albumin, ₁A– and ₁C.     

(−)-Maalian-5-ol,a new enantiomeric sesquiterpenoid from the liverwortPlagiochila ovalifolia

Summary A new enantiomeric sesquiterpene alcohol named (–)-maalian-5-ol was isolated from the liverwort, and the structure and absolute configuration was determined to be the stereostructureI by chemical and spectral evidence.The authors express their gratitude to Dr H. Inoue, National Science Museum, for identification of the liverwort, and Prof. T. Tokoroyama, Osaka City University, for sending of the data of (–)--maaliene and (+)-selina-5,11-diene. Thanks are also due to the Ministry of Education for financial support of this work.     

The effect of acidic polysaccharides and prostaglandin-like substances isolated from Propionibacterium acnes on granulocyte chemotaxis.

Three acidic polysaccharide (AP) fractions and the prostaglandin-like substances (PLS) isolated from P. acnes were investigated regarding their chemotactic activities on polymorphonuclear leukocytes. Both AP's and PLS induced a significant chemotatic response, which suggests their involvement in inflammatory acne vulgaris.     

Effect of insulin on immunological phagocytosis by macrophages.

It was shown that, in physiological concentrations, insulin enhances, in vitro, the immunological phagocytosis of sensitized sheep erythrocytes by cultured mouse peritoneal macrophages. Insulin seems to stimulate macrophage phagocytosis as a cholinomimetic agonist by increasing the intracellular levels of cyclic GMP.     

Increase in Na+, K+ -ATPase enzyme units in liver and kidneys from essential fatty acid deficient rats.

(3H)-Ouabain binding to liver and kidney preparations was utilized to estimate the number of Na+, K+-ATPase enzyme units in livers and kidneys from rats fed 2% corn oil supplemented or fat-free diets. The specific (3H)-ouabain binding in liver and kidney preparations from fatty acid deficient rats was increased approximately 40%, but the affinity of the binding sites for ouabain (Kd-value) remained unchanged. The increased concentration of Na+, K+-ATPase enzyme units observed in the essential fatty acid deficient rats may contribute to the reduced body fat accumulation and elevated heat production observed in these animals.     

The structure of amoorastatone and the cytotoxic limonoid 12-hydroxyamoorastatin

Summary 2 new limonoid-type terpenes have been isolated from an aqueous extract of seeds produced by the Eastern Himalayan (India) plantAphanamixis grandifolia Bl. By interpreting principally mass spectral and nuclear magnetic resonance data, the structures of 12-hydroxyamoorastatin (2b) and amoorastatone (3) were elucidated. Unequivocal evidence for the 12-hydroxyamoorastatin structural assignment was obtained by chemical conversion to sendanin (4). Amoorastatin derivative2b was found to significantly inhibit growth of the murine P388 lymphocytic leukemia cell lines but amoorastatone in the same system was inactive. In a comparative biological study, sendanin (4) and anthothecol (7) were also found significantly to inhibit growth of the P388 cell line, while rohitukin (8) and limonin (9) were found to be inactive.Part 63 of the series Antineoplastic Agents. For the previous contribution refer to G.R. Pettit, T.S. Krupa and R.M. Reynolds, Int. J. Peptide Protein Res., in preparation. The present investigation was supported in part by Public Health Research Grant No. CA-16049-05 from the National Cancer Institute, the Fannie E. Rippel Foundation, Mrs Mary Dell Pritzlaff, the Spencer T. and Ann W. Olin Foundation, Mr John F. Schmidt, and the Phoenix Coca-Cola Bottling Company.