Isoprostanes are produced by the non-enzymatic, free radical peroxidation of phospholipid-esterified arachidonic acid. They have been used as biomarkers of oxidative stress, but they also have been found to have potent biological activity. ent-8-iso-15(S)-Prostaglandin F2α (ent-8-iso-15(S)-PGF2α) is a potent vasoconstrictor of porcine retinal and brain microvessels with EC50 values of 15 and 24 nM, respectively. This isoprostane is about ten-fold more potent than 8-iso-PGF2α in a whole blood platelet aggregation inhibition assay.
Enzymatically-derived prostaglandin E2 (PGE2) is an optically pure compound whereas PGE2 derived from the free radical-catalyzed peroxidation of arachidonate is a racemic mixture. Ent-PGE2 is the opposite enantiomer of PGE2. Significant amounts of racemic PGE2 (rac-PGE2) are generated in vitro and in vivo in settings of oxidative stress via the isoprostane pathway. A proposed mechanism for the formation of rac-PGE2 involves the base catalyzed equilibration from 15-E2t-isoprostane (8-iso-PGE2), generated from the 15-H2t-isoprostane endoperoxide.
ent-Entecavir is an enantiomeric impurity of the antiviral drug Entecavir. Entecavir is an oral antiviral drug used in the treatment of hepatitis B virus (HBV) infection. Entecavir is a reverse transcriptase inhibitor. It prevents the hepatitis B virus from multiplying and reduces the amount of virus in the body. More specifically, it is a deoxyguanosine analogue belonging to a class of carbocyclic nucleosides, that inhibits reverse transcription, DNA replication and transcription in the viral replication process.
ent-Abacavir is an enatiomer of Abacavir. Abacavir is a carbocyclic 2'-deoxyguanosine nucleoside reverse transcriptase inhibitor and an anti-HIV drug used to treat HIV infection. Intracellular enzymes convert Abacavir to its active form, carbovir-triphosphate (CBV-TP), which then selectively inhibits HIV reverse transcriptase by incorporating into viral DNA. Abacavir is metabolized in the liver by uridine diphosphate glucuronyltransferase and alcohol dehydrogenase resulting in inactive glucuronide and carboxylate metabolites, respectively.
ent-(+)-verticilide is an effective and specific inhibitor of cardiac ryanodine receptor (RyR2) calcium release channels, demonstrating antiarrhythmic properties. It suppresses RyR2-mediated diastolic Ca2+ leak and shows greater potency and a unique action mechanism compared to Dantrolene and Tetracaine. ent-(+)-verticilide serves as a valuable tool for exploring the therapeutic potential of addressing RyR2 hyperactivity in cardiac and neurological conditions [1].
16beta,17-Dihydroxy-ent-kaurane-19-oic acid as an anti-HIV principle, it showed significant activity against HIV replication in H9 lymphocyte cells with an EC50 value of 0.8 microgram mL. It also possesses the activities of decompression and blood viscosi
Ent-11alpha-Hydroxy-15-oxokaur-16-en-19-oic acid has anti-cancer activity, it induces apoptosis of human malignant cancer cells, it also inhibits hepatocellular carcinoma in vitro and in vivo via stabilizing IkBα.
ent-11alpha-Hydroxyabieta-8(14),13(15)-dien-16,12alpha-olide shows significant cytotoxic activity against ANA-1 and Jurkat cells with IC50 values 7.12 x 10(-3) and 1.79 x 10(-2) microM.