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Biomedical subjects

A Shulman

Publications and source records attributed to A Shulman.

At least 127 records · Page 7Linked to original sources

Action of 1,10-phenanthroline transition metal chelates and their constituents on the rat isolated diaphragm preparation.

The actions of two related series of fully co-ordinated, divalent 1,10-phenanthroline transition metal chelates have been investigated on the rat isolated diaphragm muscle-phrenic nerve preparation and, where possible, compared with those of their constituent metal ions and ligands. Each member of both series of chelates produced blockade of neuromuscular transmission, although mechanistically not of a uniform type, and several elicited varying degrees of muscle contracture. The kinetic reactivity of the metal chelate appeared to be an important factor determining the nature of the biological response and profound differences in response were observed between labile and inert chelates differing in some cases by only one electron in the 3d shell.

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Action of 1,10-phenanthroline transition metal chelates on P388 mouse lymphocyte leukaemic cells.

(1)Fully coordinated 1,10-phenanthroline and 2,2'-bipyridine chelates of Ru(II) are lethal in vitro to cultured and ascites P388 mouse lymphocytic leukaemic cells; 1,10-phenanthroline chelates are generally more potent than corresponding 2,2'-bipyridine compounds, and mixed-ligand (acetylacetonato) monovalent chelates of both series are more active than the corresponding identical-ligand divalent chelates. Lethal potency is greatest for Ru(II) chelates containing highly alkylated ligands. (2) Within two series of tetramethyl-1,10-phenanthroline chelates, the inert Ru(II) and Ni(II) members are less active against P388 cultured and ascites cells than the corresponding more labile chelates of Cu(II), Cd(II), Zn(II), Fe(II), and Co(II); for the ascites cells, the rank order of lethal potency of the chelates correlates reasonably well with their anticipated rank order of kinetic reactivity. (3) Repeated subculture of P388 cells in the presence of a mixed-ligand Ru(II) chelate has produced a cell line that shows a stable 10-fold resistance to the chelate; the resistant cell line is selectively cross-resistant to certain Ru(II) identical and mixed-ligand chelates. (4) The presence of a fluorescent Ru(II) chelate has been demonstrated at the surface and within the cytoplasm and nucleus of P388 ascites cells exposed to it either in vitro or in the mouse. (5) Ru(II) and Cu(II) chelates of tetramethyl-1,10-phenanthroline do not appear to be chemotherapeutically active against P388 ascites cells in the mouse.

Animals↗