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At least 991 records · Page 55Linked to original sources
PubMed2004

In vitro antigenotoxic potential of acitretin in human lymphocytes treated with the antineoplastic alkylating agent ASE (NSC-71964).

Acitretin is widely used in the systemic treatment of severe forms of psoriasis and other skin disorders. ASE, namely 3beta-hydroxy-13alpha-amino-13,17-seco-5alpha-androstan-17-oic-13,17-lactam-p-bis(2-chloro-ethyl)amino phenylacetate (AzaSteroidalEster, NSC-71964), is an alkylating agent with antineoplastic activity and mutagenic properties. The aim of this study was to investigate the possible genotoxic and/or antigenotoxic effects of acitretin in human lymphocyte cultures in vitro, using sister chromatid exchange (SCE) and cytokinesis-blocked micronucleus (CBMN) assays. Micronucleus (MN) analysis was achieved in combination with fluorescence in situ hybridization (FISH), using an alpha-satellite DNA pancentromeric probe. It was found that acitretin alone demonstrated no clastogenic or aneugenic activity. However, simultaneous incubation of lymphocyte cultures with ASE and acitretin resulted in a reduction of ASE-induced SCEs. For MN analysis lymphocytes were treated with ASE and acitretin at 21 and 41 h after culture initiation, corresponding to G1 and G2 phases, respectively, and lasted until cell harvest. Acitretin caused a decrease in ASE-induced MN when treatment of cells started at 41 h, but exerted no effect on them when treatment started at 21 h. These findings suggest that acitretin exerts antigenotoxic effects in human lymphocyte cultures, the expression of which may be related to the cycle phase of the cells upon onset and duration of the treatment, at least as far as MN frequency is concerned.

Acitretin↗
PubMedDate not supplied

New carbocyclic lexitropsins with dinitromustard as N-terminal fragment. Inhibition of topoisomerases.

A series of carbocyclic lexitropsins was evaluated for their capacity to inhibit human topoisomerases I and II. The synthesized compounds were carbocyclic oligopeptides with dinitromustard as N-terminal fragment. In the topoisomerases I and II assays, the relaxation of DNA were inhibited with all four compounds. This inhibition was directly proportional to the compound concentration.

DNA Topoisomerases, Type I↗
PubMed1986

Kinetics of the intramolecular cyclization of bis(2-chlorethyl)aminoethyl esters of carboxylic acids.

Using a direct protentiometric method the kinetics of the intramolecular cyclization of 12 synthesized bis(2-chlorethyl)-aminoethyl esters of carboxylic acids has been studied. To determine the rate constants of hydrolysis (in 50% water-ethanol medium) the model of successive reactions of first order A----B----C has been used. An attempt has been made to relate the values obtained for the rate constants with the chemical structures of the compounds studied. The kinetic characteristics have been compared to the data of the antileucemic activity of the compounds against tumor models in vivo.

Animals↗
PubMed1994

Cytotoxic activity of two new lipophilic steroid nitrogen carbamates incorporated into low-density lipoprotein.

Low-density lipoprotein (LDL) is a potential drug carrier in cancer chemotherapy. Two novel cytotoxic lipophilic steroid derivatives with two nitrogen carbamate groups on a C-17 side chain were successfully incorporated into LDL using a reassembly technique. The antineoplastic activity of the new agents against T-47D breast cancer cells in culture was approximately twice that of a previously characterized compound with only one such group.

Antineoplastic Agents↗
PubMedDate not supplied

The hydrolysis of estramustine phosphate; in vitro studies.

The hydrolysis of estramustine phosphate by enzymes of blood, liver, intestines and prostate of man, dog and rat was studied by using specific analytical methods for the parent compound and some of its metabolites. Estramustine phosphate was stable in blood and plasma of different species but rapidly dephosphorylated to estramustine by liver, intestinal and prostatic enzymes. The prostate was the most active tissue. The ester bond by which nornitrogen mustard is linked to estradiol-17-phosphate was slowly cleaved by enzymes from the liver and prostate of the rat, dog and man. The dog tissues were more effective than those of the rat and man. Intestinal enzymes also exhibited the ability to hydrolyze the carbamic ester, but to a greater extent in the rat than in the dog. It is concluded that, with regard to the metabolism of estramustine, the rat is more similar to man than is the dog. Possible clinical implications of the biotransformation of estramustine phosphate are discussed.

Animals↗
PubMed1989

Induction of sister chromatid exchanges and cell division delays in human lymphocytes by the anti-tumour agent homo-aza-steroidal ester of p-bis(2-chloroethyl)aminophenoxy acetic acid.

3 beta-Hydroxy-13 alpha-amino-13,17-seco-5 alpha-androstan-17-oic-13,17-lactam-p-bis(2-chloroethyl) aminophenoxyacetate (NSC 294859) is a new modified steroidal alkylating agent. This compound was given by i.p. administration to mice bearing different types of tumour. It was found to exhibit good activity in L1210 and P388 leukaemias with maintenance of activity against advanced tumours. The treatment of colon 26 tumour and B16 melanoma resulted in positive antineoplastic activity. The drug was not shown to be active in a melphalan-resistant P388 line. In this study, NSC 294859 was found to be effective in causing statistically significant increases in sister-chromatid exchange (SCE) rates and cell division delays. The alkylating agent component, p-bis-(2-chloroethyl)aminophenoxy acetic acid, was shown to be less effective than the parent compound, while the modified steroid component, 3 beta-hydroxy-13 alpha-amino-13,17-seco-5 alpha-androstan-17-oic-13,17-lactam, showed no effect. There were no statistically significant differences among donors regarding the induction of SCEs and replication indices (RIs) for the compounds tested.

Alkylating Agents↗
PubMed1977

Effect of oral estramustine phosphate on pituitary, gonadal, and adrenal function in the green monkey (Cercopithecus aethiops sabaeus).

We studied the effects of estramustine phosphate on pituitary, gonadal, and adrenal function in the green monkey. A 2-week course of estramustine phosphate (75 mg per day) reversibly suppressed the luteinizing hormone and testosterone response to luteinizing hormone-releasing hormone but did not affect pituitary-adrenal function assessed by the 11-deoxycorticosterone response to metyrapone. Treatment with oral estramustine phosphate also resulted in a significant increase in corticosteroid-binding globulin but did not affect a series of liver enzymes nor hematology. The results are consistent with a pure estrogen effect produced by hydrolysis of the carbamate-ester bona at a site distant from estrogen target tissues and could explain most of the reported in vivo effects of this compound.

Administration, Oral↗
PubMedDate not supplied

Effect of drug-vinyl copolymer delivery composites on the rat prostate.

A radiation polymerized drug-vinyl copolymer delivery composite (0.8 mm in diameter, 3 mm long) was inserted into the right-lobe ventral prostate (I), into the right testis (II), and subcutaneously (III) into the back of male Wistar rats. The implantation was carried out over a period of 12 weeks maximum. From the relationship between the site of surgical insertion of the implant and the physiologic response (as measured by the decrease in the weight of the prostatic organs, e.g., ventral prostates, dorsolateral prostates, and seminal vesicles), it was found that in an AA560-containing composite (36 micrograms daily), the physiologic response is increased in order of (III) greater than (II) greater than (I). The same tendency was observed in the Estracyt-containing composite system (15 micrograms daily). The difference in the physiologic response owing to the site of surgical insertion of the implant was not observed in an E2-17 beta-containing composite (6 micrograms daily), although this composite showed the strongest physiologic response. No physiologic response in rats with CMA-containing composite (28 micrograms daily) was noted.

Acrylates↗