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At least 955 records · Page 53Linked to original sources
PubMed1988

Investigations on the anti-HIV activity of 2',3'-dideoxyadenosine analogues with modifications in either the pentose or purine moiety. Potent and selective anti-HIV activity of 2,6-diaminopurine 2',3'-dideoxyriboside.

Several 2',3'-dideoxyadenosine analogues with modifications in either the ribose or purine moiety were evaluated for their inhibitory effects on the replication of human immunodeficiency virus (HIV) in MT-4 cell cultures. The 2',3'-dideoxyriboside of 2,6-diaminopurine (ddDAPR) inhibited HIV antigen expression and HIV-induced cytopathogenicity at a 50% effective dose of 2.4-3.8 microM, as compared to 3-6 microM for 2',3'-dideoxyadenosine (ddAdo), whereas 50% inhibition of MT-4 cell viability was noted only at a concentration of 477 and 889 microM, respectively. Both ddDAPR and ddAdo were only weakly inhibitory to the proliferation of a number of T-lymphoblast and T-lymphocyte cell lines, pointing to the selectivity of these compounds as anti-HIV agents. In contrast to ddAdo, ddDAPR was found to be a poor substrate for adenosine deaminase, which may be advantageous from a chemotherapeutic viewpoint. Substitution of an azido or fluoro group at the 2' and 3'-position of the ribose moiety in either "up" or "down" configurations resulted in a decrease of the anti-HIV potency and selectivity of ddAdo. In addition to ddDAPR other purine-modified ddAdo analogues, i.e. several pyrrolo[2,3-d]pyrimidine 2',3'-dideoxynucleosides, were investigated for their anti-HIV activity, but none of these derivatives proved as potent or selective as ddDAPR.

Adenosine Deaminase↗
PubMed1984

In vitro effect of n-hexane and its metabolites on selected enzymes in glycolysis, pentose phosphate pathway and citric acid cycle.

The effect of n-hexane, 2-hexanol, 5-hydroxy-2-hexanone, 2,5-hexanediol, methyl n-butyl ketone ( MnBK ) and 2,5-hexanedione (2,5-HD) has been studied in vitro on crystalline glyceraldehyde-3-phosphate dehydrogenase (GAPDH), DL-glyceraldehyde-3-phosphate: NAD oxidoreductase (phosphorylating) EC. 1.2.1.12 and phosphofructokinase (PFK) ATP: D-fructose-6-phosphate-1-phosphotransferase; EC. 2.7.1.11 and lactic dehydrogenase (LDH) L-lactate: NAD+ oxidoreductase, EC. 1.1.1.27. MnBK and 2,5-HD both inhibited GAPDH and PFK activities selectively. n-Hexane and 2-hexanol had no effect on GAPDH and PFK activities; 5-hydroxy-2-hexanone and 2,5-hexanediol exhibited a slight inhibitory effect on these enzymes. Neither metabolites of n-hexane have any effect on LDH activity. 2,5-Hexanedione did not inhibit transketolase (D-sedoheptulose-7-phosphate: D-glyceraldehyde-3-phosphate glycolaldehyde transferase, EC. 2.2.1.1) and succinate dehydrogenase (succinate: 2,6-dichlorophenol-indophenol oxidoreductase, EC. 1.3.99.1) activities. The levels of ATP were reduced in 2,5-HD-treated cat sciatic nerves and returned to normal levels by exposing the nerve to sodium pyruvate.

Adenosine Triphosphate↗