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.     

In vitro inactivation of corpora allata of the bugOncopeltus fasciatus by precocene II

Summary Corpora allata fromOncopeltus fasciatus incubated in vitro in medium containing 10^–5.35 M (1 g/ml) of precocene II lose their ability to secrete juvenile hormone when reimplanted into last instar larvae.Acknowledgments. We thank Mr K. Dorn, Mrs L. Dolezal, Mrs V. Nötzli-Graf, Mr K.H. Trautmann and Mr A. Schuler for technical help, Dr W. Vogel and Dr A. Dübendorfer for valuable discussions.     

Effect of dihydroergocristine infusion on tolbutamide-induced insulin secretion in man

Summary The insulinemic response to 1 g of tolbutamide i.v. is greatly enhanced (+145%) after a 60-min infusion of the -lytic dihydrogenated ergot alkaloid, dihydroergocristine (83.3 m/min, corresponding to a total dose of 5 mg) in 7 healthy subjects. No differences are observed in the glycemic responses.Acknowledgment. The authors are grateful to Mr Franco Della Sala, M.D., for his skillful technical assistance.     

Microwave measurements of the absolute values of absorption by water vapour in the atmosphere

MEASUREMENT of the absolute value of absorption by water vapour at microwave frequencies is difficult because the effect is so small. Far in the wings of the absorption lines, in the so-called 'windows' of the spectrum, it is especially difficult to achieve high accuracy in the free atmosphere. But it is in these windows that the behaviour of the absorption is important from both applied and scientific points of view. Satellite communications, remote sensing of the atmosphere, and radioastronomy, are all influenced by this behaviour. Measurements on an Earth-space path are reported here; the results indicate a nonlinear relationship between absorption and water-vapour content.     

Effects of dosage and cadmium pretreatment on the binding of cadmium in rat bile

Summary The effects of dosage and of cadmium pretreatment on the binding of cadmium in rat bile were studied. With increasing dose a higher cumulative biliary excretion of Cd was observed and a higher percentage of the Cd was excreted in a low-molecular-weight form. On the other hand, after cadmium pretreatment, a decrease in the cumulative biliary excretion of cadmium was observed but a greater percentage of that excreted into the bile was bound to high molecular weight compounds.     

Density gradient centrifugation of cells separated from multicellular tumor spheroids

Summary Cells from a murine fibrosarcoma (FSa) have been grown in vitro as multicell tumor spheroids (MTS). The growth rate of these MTS was determined. Follwing selected periods of growth, MTS were made into a single cell suspension and separated on linear density gradients of Renografin. While only 1 population of cells was separated from small spheroids (400 m diameter), at least 3 subpopulations of tumor cells were separated and isolated from large spheroids (800 m in diameter).This investigation was supported in part by grants numbered CA-18628 and CA-06294, awarded by the National Cancer Institute, DHEW.     

Multiplicity of monoamine oxidase in chick brain

Summary The substrate- and inhibitor-related characteristics of monoamine oxidase (MAO) were studied on chick brain mitochondria. It was found that neither 5-hydroxytryptamine nor -phenylethylamine is the specific substrate for type A and type B MAO in chick brain.     

Structure specificity of some immunoadjuvant synthetic glycopeptides

Summary The immunoadjuvant activity of muramyl dipeptide seems to be critically dependent on the type of substitution of the -carboxyl group of the D-isoglutamine residue. Moreover the nonapeptide L-Ala-D-isoGlu-L-Lys-D-Ala-(Gly)₅-OME also shows a definite effect.