9-Hydroxyellipticine: inhibitory effect on skin carcinogenesis induced in Swiss mice by 7,12-dimethylbenz[a]anthracene

9-Hydroxyellipticine (9-hydroxy-5,11-dimethyl-6-H-pyrido[4,3b]carbazole), a potent inhibitor of monooxygenases, strongly inhibits the initiation of skin tumors by 7,12-dimethylbenz[a]anthracene (DMBA) in male NMRI Swiss mice. 9-Hydroxyellipticine has not effect on promotion step.     

Carnitine transport in submitochondrial particles and reconstituted proteoliposomes.

Influx and efflux measurements of carnitine with submitochondrial particles lead to the conclusion that carnitine can cross the inner mitochondrial membrane by either facilitated diffusion or more rapidly by a carnitine-carnitine exchange. Both, the facilitated diffusion and the exchange are inhibited by N-ethylmaleimide or mersalyl at low concentrations. Reconstituted particles prepared from liposomes and either submitochondrial particles or an octyl β-glucoside-solubilized preparation were active in catalyzing carnitine-carnitine exchange.     

Inhibition of modulation of thymus-leukemia antigens by concanavalin A.

When incubated at 37 °C in medium containing antibodies specific for thymus-leukemia (TL) antigens, viable cells bearing these antigens become resistant to the cytolytic effects of guinea pig complement, a process termed antigenic modulation. Antibody-induced membrane redistribution of the TL antigens, detected by indirect immunofluorescence, occurs with a similar pace. When high concentrations of concanavalin A (Con A) were included with antibodies in the incubation medium, TL antigenic modulation as well as antigen patching and capping were markedly inhibited, similar to effects of Con A on membrane immunoglobulin redistribution with murine spleen cells. Colchicine antagonized the inhibition by Con A suggesting the involvement of microtubules. In parallel experiments high concentrations of Con A failed to alter the quantity of TL antigen expression or its rate of change with time during incubation in cognate antisera. These results support the hypotheses that (a) generalized alterations in membrane receptor mobility may be induced by ligand binding to the cell membrane, and (b) under certain conditions stable interactions occur between normally independent cell surface antigens.     

Role of β-carotene in the reaction centres of Photosystems I and II of spinach chloroplasts prepared in non-polar solvents

Spinach chloroplasts have been prepared nonaqueously using non-polar solvents (n-hexane, CCl₄, n-heptane) and the β-carotene content extracted in a controlled manner. This procedure is reproducible and does not result in large structural or spectral changes of the chloroplasts. The organisation of the chlorophyll-proteins is unaltered, as fragmentation with digitonin results in the appearance of the same fractions as found previously for aqueously-prepared chloroplasts, including the pink zone containing cytochromes f and b₆ in the ratio 1:2. The chloroplasts possess both Photosystem I activity (P-700 photo-bleaching, and NADP⁺ photoreduction) and Photosystem II activity (parabenzoquinone reduction with Mn²⁺ as electron donor, and chlorophyll fluorescence induction). Use of moderate intensity red illumination has allowed a study of the role of β-carotene in photochemistry separate from its roles in energy transfer and photoprotection.Removal of the fraction of β-carotene closely associated with the Photo-system I reaction centre caused the rate of NADP⁺ photoreduction to fall to a low, but significantly non-zero level. Thus, in the complete absence of β-carotene, photochemistry can still be observed, however the specific association of β-carotene with the reaction centre is required for maximal rates. We propose that β-carotene bound at the reaction centre decreases the rate of transfer of excitation energy away from the reaction centre, and increases the rate of photochemistry. It is possible that this occurs via formation of an exciplex between ground state β-carotene and chlorophyll in the first excited state.     

Early hCG-induced desensitization in Leydig cells.

The early mechanism of hCG induced down regulation of its own receptor as well as steroidogenesis refractoriness of rat Leydig cells to gonadotropin stimulation have been investigated. A single injection of 5, 12, 25, 50 and 100 IU of hCG in rats induced within 8 hours, Leydig cells desensitization. However, apparent receptor loss was significantly lower only in the rats who received 50 and 100 IU of hCG. Cycloheximide inhibits hCG-induced receptors loss but had no effect on hCG-induced desensitization. The most likely explanation for desensitization in the presence of binding sites and a normal adenylate cyclase, is a defective coupling between the receptor sites and the catalytic subunit.     

Antimetabolic activities of 2-fluoro-L-histidine.

2-Fluoro-L-Histidine inhibits protein synthesis in various cell cultures, as measured by ³H-leucine incorporation. This histidine analog also inhibits the cytopathogenicity of a number of RNA and DNA viruses in primary and continuous cell cultures; it blocks the transformation of normal mouse (MO) cells by murine sarcoma virus, and partially suppresses the release of murine leukemia virus by a continuously infected mouse cell line (JLSV5). In human skin fibroblasts, it reduces the interferon-inducing capacity of poly(I)·poly(C). Inhibition of cell protein synthesis may be the common cause of the various effects. 4-Fluoro-L-histidine is essentially inert in all of the test systems examined.