[Effect of the segregation and accumulation of chloroquine and daunorubicin by L cells (LSM subline) on the activity of lysosomal hydrolases]. / Vliianie segregatsii i akkumuliatsii khlorokhina i daunorubitsina kletkami L (sublinii LSM) na aktivnost' lizosomnykh gidrolaz.

Kinetics of chloroquine and daunorubicin (DNR) uptake by cultured L cells (subline LSM) has been studied. With their constant concentrations in the medium the uptake of both chloroquine and DNR was characterized as a two phase process. Within 1.5-2 hours, these cells accumulated as much as 90 per cent of the total chloroquine and DNR amounts taken up during the whole incubation period. The segregation and accumulation of these substances took place in lysosomes. Chloroquine and DNR concentrations within lysosomes exceed those in the medium by 1100 and 5000 times, respectively. The chloroquine and DNR accumulation in lysosomes inhibited activities of some lysosomal hydrolases tested: cathepsins B and D, N-acetyl-beta, D-glucosaminidase and acid phosphatase. Unlike, the activity of acid lipase was not affected by chloroquine, and was sufficiently stimulated (by 55%) by DNR. The mechanism of inhibition of lysosomal enzymes by chloroquine and DNR is not yet known, although some suggestions are made. Possible consequences of lysosomal activity inhibition for cell metabolism are discussed in addition to a possible role of lysosomotropic agents as regulators of lysosomal functional activity.

[Lysosomotropic agents as regulators of the activity of lysosomal hydrolases]. / Lizosomotropnye agenty kak reguliatory aktivnosti lizosomnykh gidrolaz.

Activities of lysosomal enzymes acid phosphatase, N-acetyl-beta-D-glucosaminidase, beta-galactosidase, acid lipase and cathepsins B and D were studied after accumulation of neutral red, acridine orange chloroquine and daunorubicin in lysosomes of fibroblasts of the LSM substrain. All the drugs studied proved to be inhibitors of these enzymes except of daunorubicin, which stimulated acid lipase activity. Lysosomotropic drugs are considered as possible regulators of the activity of lysosomes.

[Effect of the segregation of neutral red, acridine orange and ammonium chloride by L cells (subline LSM) on lysosomal hydrolase activity]. / Vliianie segregatsii neitral'nogo krasnogo, akridinovogo oranzhevogo i khloristogo ammoniia kletkami L (sublinii LSM) na aktivnost' lizosomal'nykh gidrolaz.

Kinetics of Neutral red (NR) and Acridine orange (AO) uptake by cultured L cells (subline LSM) has been studied. It was found that the uptake of both NR and AO, with their constant concentrations in the medium was characterized as a two-phase process. During 2 hours, these cells concentrated as much as 90% of the total amount of NR and AO taken up during the whole incubation period. The segregation and accumulation of NR, AO as well as NH4Cl took place in lysosomes. NR and AO concentrations within the cells exceed by 600 and 400 times, respectively, those in the medium. NR, AO and NH4+ accumulation in cells resulted in inhibition of the activity of the following lysosomal hydrolases: cathepsins B and D, acid lipase, N-acetyl-beta,D-glucosaminidase, beta-galactosidase, acid phosphatase and galactosyltransferase, the latter being a marker of Golgi apparatus. The effect of lysosomal enzyme activity inhibition on the cell economy, and a possible role of lysosomotropic agents as regulators of the lysosomal apparatus functional activity are discussed.

[Cytophotometric study of the granules formed in frog erythrocytes incubated in solutions of acridine orange, chloroquine and daunorubicin]. / Tsitofotometricheskoe issledovanie granul, obrazuiushchikhsia v éritrotsitakh liagushki pri inkubatsii ikh v rastvorakh akridinovogo oranzhevogo, khlorokhina i daunorubitsina.

Granules arising in the cytoplasm of Rana temporaria erythrocytes incubated in either solution containing acridine orange, chloroquine or antibiotic daunorubicine were studied cytophotometrically. The stuff concentrations in the granules were estimated under various conditions of incubation. The stuff concentrations in the granules appeared to be 1000-fold higher than in the incubation solutions. The average concentration in the granules did not depend on either the initial concentration of the stuff solution or the incubation time. The stuff concentration in the granules decreases with the increase of the granule size. Mechanisms of cation-acid segregation and accumulation by living cell are discussed.