Anti-leishmanial activity of betulin derivatives

Sami Alakurtti, N. Sacerdoti-Sierra, C. L. Jaffe, Salme Koskimies, Jari Yli-Kauhaluoma

    Research output: Contribution to journalArticleScientificpeer-review


    Betulin (lup-20(29)-ene-3ß,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. Betulin and its derivatives such as betulinic acid have many interesting pharmacological properties, such as cytotoxic activity against many tumour cell lines and anti-HIV activity with a new mechanism of action. Several synthetic betulin derivatives that have been chemically modified at the positions C-3 and C-28 of the lupane skeleton were produced, and the anti-leishmanial inhibition activity of compounds was evaluated at 50 µM against Leishmania donovani and Leishmania tropica. Betulonic acid had the best anti-leishmanial activity with remarkable 98% inhibition at 50 µM giving a GI50 value of 14.6 µM. In conclusion, carbonyl or carboxyl groups seem to have beneficial effect in anti-leishmanial inhibition activity, and these compounds represent important leads for further optimization.
    Original languageEnglish
    Pages (from-to)S37-S37
    JournalEuropean Journal of Pharmaceutical Sciences
    Issue number1, Supplement
    Publication statusPublished - 2008
    MoE publication typeA1 Journal article-refereed
    Event19th Helsinki Drug Research 2008 - Helsinki, Finland
    Duration: 9 Jun 200811 Jun 2008


    • betulin
    • betulin derivatives
    • betulinic acid
    • cytotoxic
    • tumours
    • anti-leishmanial
    • Leishmania donovani
    • Leishmania tropica


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