Disease relevance of AIDS-107272

• Thiocoraline, a new anticancer agent derived from the marine actinomycete Micromonospora marina, was found to induce profound perturbations of the cell cycle [1].
• Deciphering the biosynthesis pathway of the antitumor thiocoraline from a marine actinomycete and its expression in two streptomyces species [2].
• Thiocoraline is a thiodepsipeptide antitumor compound produced by two actinomycetes Micromonospora sp. ACM2-092 and Micromonospora sp. ML1, isolated from two marine invertebrates (a soft coral and a mollusc) found of the Indian Ocean coast of Mozambique [2].

High impact information on AIDS-107272

• Only minor glucuronidation was observed for thiocoraline by UGT1A1 and UGT1A9 and no glucuronidation was observed in human liver S9 fraction [3].
• In contrast to the CYP metabolism observed in supersomes, no effect could be observed from the CYP3A4 inhibitors on the cytotoxicity of thiocoraline in Hep G2 cells [3].
• In vitro characterization of the biotransformation of thiocoraline, a novel marine anti-cancer drug [3].
• In addition, no glucosidation and sulfation were observed for thiocoraline in human liver cytosol and S9 fraction [3].
• The cell cycle effects observed after exposure to thiocoraline appear related to the inhibition of DNA replication [1].

Chemical compound and disease context of AIDS-107272

• Thiocoraline, a novel depsipeptide with antitumor activity produced by a marine Micromonospora. II. Physico-chemical properties and structure determination [4].

Biological context of AIDS-107272

• Surprisingly, the identified gene cluster contains more NRPS modules than expected on the basis of the number of amino acids of thiocoraline [2].
• Heterologous expression of a region of about 53 kbp, containing 26 of the ORFs, in Streptomyces albus and S. lividans led to the production of thiocoraline in these streptomycetes [2].
• Plasma samples can be stored for at least 4 months at -80 degrees C. Finally, the usefulness of this method for pharmacological research was shown in a pilot study of the pharmacokinetics of thiocoraline in rats [5].

Anatomical context of AIDS-107272

• Thiocoraline showed a potent cytotoxic activity against P-388, A-549 and MEL-28 cell lines, and also a strong antimicrobial activity against Gram-positive microorganisms [6].

Associations of AIDS-107272 with other chemical compounds

• Bioanalysis of thiocoraline, a new marine antitumoral depsipeptide, in plasma by high-performance liquid chromatography and fluorescence detection [5].

Gene context of AIDS-107272

• These studies indicate that the new anticancer drug thiocoraline probably acts by inhibiting DNA polymerase alpha activity [1].
• Thiocoraline does not inhibit DNA-topoisomerase II enzymes in vitro, nor does it induce DNA breakage in cells exposed to effective drug concentrations [1].

References