Pharmacological properties of the ubiquitous natural product betulin

Sami Alakurtti, Taru Mäkelä, Salme Koskimies, Jari Yli-Kauhaluoma (Corresponding Author)

    Research output: Contribution to journalReview ArticleScientificpeer-review

    473 Citations (Scopus)

    Abstract

    Betulin (lup-20(29)-ene-3β,28-diol) is an abundant naturally occurring triterpene and it is found predominantly in bushes and trees forming the principal extractive (up to 30% of dry weight) of the bark of birch trees. Presently, there is no significant use for this easily isolable compound, which makes it a potentially important raw material for polymers and a precursor of biologically active compounds. Betulin can be easily converted to betulinic acid, which possesses a wide spectrum of biological and pharmacological activities. Betulinic acid has antimalarial and anti-inflammatory activities. Betulinic acid and its derivatives have especially shown anti-HIV activity and cytotoxicity against a variety of tumor cell lines comparable to some clinically used drugs. A new mechanism of action has been confirmed for some of the most promising anti-HIV derivatives, which makes them potentially useful additives to the current anti-HIV therapy. Betulinic acid is specifically cytotoxic to several tumor cell lines by inducing apoptosis in cells. Moreover, it is non-toxic up to 500 mg/kg body weight in mice. The literature concerning derivatization of betulin for structure–activity relationship (SAR) studies and its pharmacological properties is reviewed.

    Original languageEnglish
    Pages (from-to)1-13
    Number of pages13
    JournalEuropean Journal of Pharmaceutical Sciences
    Volume29
    Issue number1
    DOIs
    Publication statusPublished - 2006
    MoE publication typeA2 Review article in a scientific journal

    Keywords

    • betulin
    • betulinic acid
    • birch bark
    • betulin derivatives
    • natural products
    • betula sp.
    • medicinal chemistry
    • health
    • Health-effects
    • bark
    • cytotoxic

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