title: New composites of betulin esters with arabinogalactan as highly potent anti-cancer agents.
abstract: Betulin and its esters are the natural compounds with high in vitro cytotoxicity toward many cancer cells. However, the poor water solubility of these compounds has limited their applications. We prepared new composites of betulin esters using two methods, namely ball-milling of the mixtures of betulin esters with arabinogalactan and preparation of thin films of these mixtures by evaporating the aqueous solutions. These composites revealed higher water solubility as compared with the initial substances without losing the structural integrity and functionality. As a result, the new composites have shown much higher inhibitory effects against different cancer cell lines such as Ehrlich ascites carcinoma cells and lung carcinoma cells (A549) in comparison with the initial substances. The cell viability studies based on Annexin V and Propidium iodide probes have confirmed the high proapoptotic effect of betulin ester derivatives against cancer cells.
authors.affiliation: a SB RAS , Institute of Solid State Chemistry and Mechanochemistry , Novosibirsk , Russia.|b Novosibirsk State University , Novosibirsk , Russia.
authors.forename: T P
authors.initials: TP
authors.lastname: Shakhtshneider
authors.affiliation: c SB RAS , Institute of Chemistry and Chemical Technology , Krasnoyarsk , Russia.|d Siberian Federal University , Krasnoyarsk , Russia.
authors.forename: S A
authors.initials: SA
authors.lastname: Kuznetsova
authors.affiliation: c SB RAS , Institute of Chemistry and Chemical Technology , Krasnoyarsk , Russia.|e Research Institute of Molecular Medicine and Pathobiochemistry, Krasnoyarsk State Medical University , Krasnoyarsk , Russia.
authors.forename: A S
authors.initials: AS
authors.lastname: Zamay
authors.affiliation: e Research Institute of Molecular Medicine and Pathobiochemistry, Krasnoyarsk State Medical University , Krasnoyarsk , Russia.
authors.forename: T N
authors.initials: TN
authors.lastname: Zamay
authors.affiliation: e Research Institute of Molecular Medicine and Pathobiochemistry, Krasnoyarsk State Medical University , Krasnoyarsk , Russia.
authors.forename: E A
authors.initials: EA
authors.lastname: Spivak
authors.affiliation: a SB RAS , Institute of Solid State Chemistry and Mechanochemistry , Novosibirsk , Russia.
authors.forename: M A
authors.initials: MA
authors.lastname: Mikhailenko
authors.affiliation: c SB RAS , Institute of Chemistry and Chemical Technology , Krasnoyarsk , Russia.
authors.forename: Yu N
authors.initials: YN
authors.lastname: Malyar
authors.affiliation: c SB RAS , Institute of Chemistry and Chemical Technology , Krasnoyarsk , Russia.|d Siberian Federal University , Krasnoyarsk , Russia.
authors.forename: B N
authors.initials: BN
authors.lastname: Kuznetsov
authors.affiliation: c SB RAS , Institute of Chemistry and Chemical Technology , Krasnoyarsk , Russia.|d Siberian Federal University , Krasnoyarsk , Russia.
authors.forename: N V
authors.initials: NV
authors.lastname: Chesnokov
authors.affiliation: a SB RAS , Institute of Solid State Chemistry and Mechanochemistry , Novosibirsk , Russia.|b Novosibirsk State University , Novosibirsk , Russia.
authors.forename: V V
authors.initials: VV
authors.lastname: Boldyrev
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D004952:Esters / Q000737:chemistry; D005685:Galactans / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy / Q000473:pathology; D008855:Microscopy, Electron, Scanning; D012995:Solubility; D014315:Triterpenes / Q000737:chemistry* / Q000494:pharmacology; D000094062:Betulinic Acid
chemical_list: D000970:Antineoplastic Agents; D004952:Esters; D005685:Galactans; D014315:Triterpenes; C002503:betulin; D000094062:Betulinic Acid; C005653:arabinogalactan
keywords: anticancer activity; arabinogalactan; betulin diacetate; betulin dipropionate; composites; solubility