A tissue-selective prostaglandin E2 analog with potent antifertility effects

Summary N-methanesulfonyl 16-phenoxy--tetranor PGE₂ is a prostaglandin analog which is markedly more tissue selective than PGE₂. This compound is 10–30 times more potent than PGE₂ in animal models which are considered relevant to antifertility effects in humans. In pharmacological tests which are believed to be predictive for side effects in humans, the compound has potency either equal to or less than that of PGE₂.     

Influence of PGA1 on cartilage growth

Summary Using the Fell technique of organ culture of cartilage in a chemically defined medium, it has been shown that prostaglandin A₁ at a concentration of 25 g/ml caused chondrocyte death in chick embryonic limb rudiments. An equimolar concentration of PGE₂ was not toxic to the cells.Acknowledgments. We are grateful for the support of C. J. K. by the Medical Research Council and of D. L. G. by the Arthritis and Rheumatism Council for Research. Our thanks are due to Dame Honor Fell, F. R. S. for invaluable advice and guidance, to Dr J. Pike (Upjohn Co.) for supplies of prostaglandin A₁, and to Dr Sylvia Fitton-Jackson for the gift of culture medium.     

A new one-step synthesis of hexahydrocannabinoid analogs

Summary A one-step synthesis of hexahydrocannabinoid analogs (HHC) is described making use of the condensation of phenolic ketones and aldehydes with citronellal in the presence of pyridine.Grateful thanks are accorded to Drs L. Chopard and S. Selvavinayakam for spectral measurements and Dr I. Fleming for useful discussion.R. Mechoulam and Y. Gaoni, Recent advances in the chemistry of Hashish, in: Progress in the Chemistry of Organic natural products, vol. 25, p. 175. Ed. L. Zechmeister. Springer Verlag, Wien 1967; R. Mechoulam, Marijuana Chemistry and Pharmacology, metabolism and clinical effects. Academic Press, New York 1973; R. Mechoulam, N. K. McCallum and S. Burstein, Chem. Rev.76, 75 (1976).     

The effect of daily evening isoproterenol administration on reproductive organ growth in male rats treated neonatally with testosterone propionate

Summary Daily evening injections of isoproterenol extended the period of high pineal N-acetyltransferase activity and retarded the growth of testes, seminal vesicles and prostate in rats treated neonatally with testosterone propionate.The authors are grateful to Mrs Marie Svobodová for her skillful technical assistance.     

Proteolytic activity on endogeneous substrates in cell-free extracts ofTrypanosoma cruzi

Summary Cell-free extracts ofTrypanosoma cruzi contain proteolytic activity able to degrade endogenous substrates. The activity was maximal at pH 3 to 4, had an optimal temperature of 65°C, and was strongly inhibited by N--p-tosyl-L-lysine chloromethyl ketone.This investigation received financial support from the UNDP/World Bank/WHO Special Programme for Research and Training in Tropical Diseases, the Fundación Julio Cherny, and the Ministerio de Salud Pública y Medio Ambiente de la República Argentina. The authors gratefully acknowledge the technical assistance of Mr Esteban Bontempi.     

The free radical oxidation of the tetrahydrocannabinols

Summary The free radical oxidation of ¹ and ⁶-tetrahydrocannabinol has been examined by spin trapping techniques and intermediates that would lead to cannabinol have been trapped. The 1st step in the oxidation of ¹-THC involves the removal of 3-H, while for ⁶-THC, either 2-H or 5-H. Intermediates were isolated which could be pyrolysed to the diene and cannabinol.     

Captopril (SQ 14,225): In vitro and in vivo influence on the proliferative response of rat lymphocytes

Summary Captopril in vitro (50–500 g/ml) increased³H-TdR incorporation in unstimulated and mitogen-stimulated cultures of rat lymphocytes. Unseparated spleen and lymph node cells of rats orally treated with captopril (50 mg/kg/day×4) showed decreased basal and mitogen stimulated³H-TdR incorporation. The removal of macrophages abrogated this inhibitory effect. Leucine aminopeptidase activity of macrophages was reduced — in vivo and in vitro — by captopril.Acknowledgments. The authors thank the Squibb Institute for Medical Research for the gift of Captopril. The excellent technical assistance of Ms B. Hasselriis, Ms B. Rumler and Ms E. Greve Petersen is gratefully acknowledged.     

Identification of an acyclic diterpene alcohol in the defense secretion of soldiers ofReticulitermes lucifugus

Summary The defense secretion of soldiers ofReticulitermes lucifugus has been shown to contain, predominantly, (R)-(–)-(E,E)-geranyllinalool together with germacrene A and -farnesene.This report covers part of a collaborative study with J.-L. Clément, Lab. d'Evolution, Université P. et M. Curie, Paris, to whom we are grateful for supplies of material and discussions. We also thank Dr O.T. Jones for collections ofReticulitermes lucifugus.     

Genetic polymorphisms and intrauterine development. Evidence of decreased heterozygosity in light-for-dates human newborn babies

Summary In 2 independent samples of low-birth-weight infants the proportion of females and homozygotes for a series of polymorphic systems was higher in light-for-dates than in preterm babies. The observation seems to give support to the hypothesis that homozygosity for normal polymorphisms may decrease in general intrauterine growth rate. Since it is known that survival rate is strongly related to birth weight, a correlation between growth retardation and homozygosity may have a major role in the maintenance of such polimorphisms.We thank Prof. L. Ginzburg for helpful comments.