The hemolytic activity of heterocyclic N-alkyl amine oxides

Summary The N-alkyl derivatives of morpholine-, pyrrolidine-, piperidine- and perhydroasepine-N-oxides caused the rapid, temperature-dependent, hemolysis of human red blood cells. The most hemolytic were the amine oxides with alkyl groups having 14–18 carbon atoms.     

Correlation of physicochemical parameters and biological activity in steroids 9α-substituted cortisol derivatives

Resumen Por primera vez se han analizado las relaciones estructura-función de diez derivados del 9-cortisol substituido usando técnicas de regresión de parámetros múltiples. Se concluye que los factores electrónicos y estéricos son de mayor importancia al determinar el efecto del substituyente, y que la unión hidrofóbica también es de importante consideración. Se discute el significado de estos resultados.

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This investigation was supported in part by Public Health Service Research Grants No. AM-14824 (to M.E.W.) and No. GM 07492 (to C.H.) from the National Institutes of Arthritis and Metabolic Diseases, and General Medical Sciences, U.S. Public Health Service.     

Effects of ovarian steroids on superoxide dismutase activity in the rat brain

The levels of manganese superoxide dismutase (MnSOD) and copper-zinc superoxide dismutase (CuZnSOD) were determined in appropriate subcellular fractions prepared from whole brain homogenates of cycling and long-term (3 week) ovariectomized (OVX) Wistar rats, and were compared to the levels found in corresponding samples prepared from OVX rats treated with progesterone (P) or estradiol 17B-benzoate (EB). The activity of both SODs was steady during the estrous cycle, except at proestrus, when MnSOD activity was elevated significantly. Bilateral ovariectomy resulted three weeks later in an increase of the MnSOD activity even higher than that recorded at proestrus. High post-castration MnSOD activity was lowered profoundly by exogenous P (2 mg) or EB (0.5 g), given s.c. to OVX animals 2 h or 24 h before sacrifice. Neither removal of the ovaries nor the hormone treatments affected the activity of CuZnSOD. These results suggest suppressive effects of ovarian steroids on MnSOD activity in the rat brain.     

Discovery of novel avermectins with unprecedented insecticidal activity

Summary A new class of insecticidal and antiparasitic agents, 4-amino-4-deoxy avermectins, has been developed by chemical modification of avermectin B₁. The most effective of these compounds are 1500-fold more potent than avermectin B₁ (abamectin) against the beet armywormSpodoptera exigua and show similar potency against other lepidopteran larvae.     

Thyroid activity in response to some gonadal steroids in methallibure-treatedHeteropneustes fossilis (Bloch)

Summary Methallibure treatment is as effective as hypophysectomy in reducing thyroid activity inH. fossilis. Sex steroids (TP and EB) administration restored thyroid activity in methallibure-treated females to normal level, but failed to elicit any response in males. This drug seems to block TSH secretion and thyroid hormone synthesis inH. fossilis.Financial assistance in the form of SRF from ICAR, New Delhi to one of us (R.B.R.), gift of methallibure from ICI Ltd., UK and TSH from NIH, USA, to T.P.S. are gratefully acknowledged.     

Maintenance of thyroid activity with some steroids in hypophysectomized and gonadectomized catfish,Mystus vittatus (Bloch)

Zusammenfassung Beim amerikanischen WelsMystus vittatus (Bloch) wurde festgestellt, dass die Radiojodaufnahme der Schilddrüse nach Hypophysektomie durch Cortison und Sexualhormone wieder normalisiert werden kann.     

Thyroid activity in response to some gonadal steroids in methallibure-treated Heteropneustes fossilis (Bloch).

Methallibure treatment is as effective as hypophysectomy in reducing thyroid activity in H. fossilis. Sex steroids (TP and EB) administration restored thyroid activity in methallibure-treated females to normal level, but failed to elicit any response in males. This drug seems to block TSH secretion and thyroid hormone synthesis in H. fossilis.     

Effect of nitrate esters of androgen steroids on the succinate oxidase and NADH-Cytochrome C reductase activity of isolated rat liver mitochondria

Résumé Le testostérone et la 5-androstane-17-ol-3-one stimulent l'activité de la succinoxydase des mitochondries intactes et l'activité de la NADH-cytochrome-c-réductase des mitochondries à membranes lésées, extraites du foie du rat blanc. Les nitrates-esters des mÊmes stéroÏdes réduisent l'activité des deux enzymes.     

Conversion of steroids by microorganisms

Zusammenfassung Die methodischen Grundlagen der Umwandlung von Steroiden durch Mikroorganismen werden diskutiert, insbesondere die apparativen Erfordernisse, die Kulturbedingungen sowie der Nachweis und die Isolierung der Reaktionsprodukte. Die Umsetzungen mit Enzymen aus Mikroorganismen werden denjenigen mit Nebennieren-Enzymen gegenübergestellt.Von mikrobiologischen Reaktionen stehen Hydrierungen, Dehydrierungen und besonders Hydroxylierungen an verschiedenen Stellen der Steroidmolekel im Vordergrund. Im weiteren wurde auch Abbau der Seitenkette von Pregnanderivaten, der mit Ringspaltung und/oder mit Dehydrierung in 1-Stellung einhergehen kann, festgestellt. Die Einführung dieser Doppelbindung wird speziell besprochen.

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From a lecture at the 128^th National Meeting of the American Chemical Society, Minneapolis, Minn.; Symposium on Metabolic Conversions of Steroids; September 16, 1955. Communication No. 136 On Steroids. No. 135 compareE. Vischer, J. Schmidlin, andA. Wettstein, Exper. (in press).     

Anticonvulsant activity of farnesylacetone epoxide--a novel marine natural product.

A marine natural product, farnesylacetone epoxide, which is chemically related to juvenile hormone, has anticonvulsant properties at nonsedative doses in mice.     

Cytotoxic and antitumor activity of a new series of heterocyclic compounds: dipyrido (4,3-b) (3,4-f) indoles]

Among newly synthesized compounds derived from the dipyrido [4,3-b] [3,4-f] indole nucleus, two have proved to be particularly active in vitro and in vivo. Their cytotoxic effects on cultured cells have been determined. At non toxic doses, they displayed a pronounced inhibitory effect on experimental L1210 Leukemia. These compounds have a strong affinity for DNA molecules.     

On the interaction of glucocorticoids and anabolic steroids

Zusammenfassung Der durch Hydrokortison (zehntätige Zufuhr) erhöhte Spiegel der gesamten Lipämie im Serum und der löslichen und unlöslichen Glykogenfraktion in der Leber der Ratte wurde mittels gleichzeitiger 19-Nortestosteron-phenylpropionatzugabe erniedrigt, während 19-Nortestosteron-phenylpropionat allein die verfolgten Parameter nicht beeinflusste.     

Sexual steroids and monoamine metabolism during gestation

Summary The experiments show influence of progesterone and estradiol on regulation of enzymes of monoamine metabolism, MAO and COMT during pregnancy. Both the hormones inhibit enzymes MAO and COMT in the adrenals when determined at 0 h parturition. Estradiol has stronger inhibitory effect than progesterone. The results provide evidence for important endocrine implication during pregnancy for processes of monoamine regulation.The generous help of Dr.Raynaud of CEA, France is gratefully acknowledged. A.R.B. is pre-doctoral fellow of Paris University.