Journal
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
Volume 29, Issue 1, Pages 1-13Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejps.2006.04.006
Keywords
betulin; betulinic acid; birch bark; betulin derivatives; natural products; Betula sp.; medicinal chemistry
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Betulin (lup-20(29)-ene-beta 3,28-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. (c) 2006 Elsevier B.V. All rights reserved.
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