Research Progress in the Promissing Natural Product-Betulin

Yuri, Shanko; Kaur, Kulvinder Kochar

doi:10.26717/bjstr.2018.08.001619

BJSTR

2018

DOI: 10.26717/bjstr.2018.08.001619

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Research Progress in the Promissing Natural Product-Betulin

Shanko Yuri

Kulvinder Kochar Kaur

Abstract: Betulin is a pentacyclic triterpene alcohol with a lupane skeleton and is known to possess a broad range of biological activities, including antiinflammatory, anti-viral and anti-cancer actions. Betulin contains primary and secondary hydroxyls that are situated in different steric environments and shows different activities. The literature concerning the pharmacological properties, the resource and isolation of betulin, the chemical synthesis of betulin and its derivatives, the biotransformation of betulin was… Show more

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Cited by 2 publications

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Betulin Derivatives. Biological Activity and Solubility Improvement

Александровна¹,

Сергеевна²,

Владимировна³

et al. 2019

JCPRM

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In the review the biological properties (antitumor, antiviral, hypolipidemic, anti-inflammatory, etc.) and bioavailability of betulin and betulinic acid derivatives were discussed. These compounds are isolated from various natural sources, including birch bark (Betula, Betulaceae). The structure-activity correlation was considered for well-known betulinic acid derivatives. The perspectivity of this compounds as active pharmaceutical ingredients was demonstrated by in vitro, in vivo, and ex vivo experiments. The type of antitumor actions, generally, depends on substituents at the C-3 and C-28 carbon atoms of the lupane skeleton. It is very important that the carboxyl group of betulinic acid in the C-28 position was present. In this case, the cytotoxicity of C-3 modified derivatives is extremely high for all tested cell lines. The use of these compounds in the medical practice is complicated because they have low bioavailability and poor water solubility (from 1 to 100 µg*l-1). The main chemical syntheses for solubility improvement of betulin derivatives by grafting of hydrophilic groups were discussed. Moreover, the colloid-chemical approaches for the bioavailability improving of triterpenoids include: 1) including of these compounds in liposomes, vesicles and other nanoparticles; 2) obtaining of micelles with high-molecular compounds; 3) colloid-chemical dissolution due to physico-mechanical action; 4) inclusion complexes formation; 5) using of polymers for triterpenoids grafting. Chemical modification of betulin and betulinic acid by polar groups, such as phosphate/phosphonate, sulfate, amino acids, etc. has been shown for bioavailability improving.

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Betulin Derivatives. Biological Activity and Solubility Improvement

Александровна¹,

Сергеевна²,

Владимировна³

et al. 2019

JCPRM

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Antioxidant Activity of New Copolymer Conjugates of Methoxyoligo(Ethylene Glycol)Methacrylate and Betulin Methacrylate with Cerium Oxide Nanoparticles In Vitro

et al. 2022

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The synthesis of two new copolymer conjugates of methoxyoligo(ethylene glycol)methacrylate MPEGMA and betulin methacrylate BM was developed via RAFT polymerization. The molar content of BM units was equal to 9–10 and 13–16 mol%, respectively (HPLC, 1H and 13C NMR); molar weights were equal to 75000–115000. CeO2 NPs as a component of the hybrid material were synthesized for the preparation of the composition with copolymer conjugates of MPEGMA and BM. We showed a significant increase in G6PDH and GR activities by 21–51% and 9–132%, respectively, which was due to the increase in NADPH concentration under the action of copolymers in vitro. The actions of copolymers and CeO2 NPs combination were stronger than those of the individual components: the SOD activity increased by more than 30%, the catalase activity increased dose-dependently from 13 to 45%, and the GR activity increased to 49%. The maximum increase in enzyme activity was observed for the G6PDH from 54% to 151%. The MDA level dose-dependently increased by 3–15% under the action of copolymers compared with the control, and dose-dependently decreased by 3–12% in samples containing CeO2 NPs only. CeO2 NP–copolymer compositions can be used for the design of new biomimetic medical products with controlled antioxidant properties.

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Research Progress in the Promissing Natural Product-Betulin

Cited by 2 publications

References 36 publications

Betulin Derivatives. Biological Activity and Solubility Improvement

Betulin Derivatives. Biological Activity and Solubility Improvement

Antioxidant Activity of New Copolymer Conjugates of Methoxyoligo(Ethylene Glycol)Methacrylate and Betulin Methacrylate with Cerium Oxide Nanoparticles In Vitro

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