Planta Med 2011; 77 - PM48
DOI: 10.1055/s-0031-1282806

Evaluation of acute toxicity of betulin

MN Makarova 1, AN Shikov 1, OI Avdeeva 1, ON Pozharitskaya 2, IE Makarenko 1, VG Makarov 1, GI Djachuk 1
  • 1St.-Petersburg State medical Academy named after I.I. Mechnikov, 47, Piskarevsky pr., 195067, St-Petersburg, Russia
  • 2St.-Petersburg Institute of Pharmacy, 47/5, Piskarevsky pr., 195067, St-Petersburg, Russia

Betulin is a pentacyclic triterpene alcohol belonging to the lupane series of compounds. It is extracted from the outer birch bark. The birch triterpenes have known antiallergic, antiviral, antimicrobial, antitumor and hepatoprotective effects [1–3]. Although to our knowledge no reports about acute toxicity of betulin were published. Acute toxicity of betulin was studied on rats and mice.

Betulin (98%) was provided by VTT. Male and female outbreed rats and mice were administered with betulin in single dose of 1000–16000mg/kg intragastric and rats in single dose of 250–4000mg/kg intraperitoneally. No significant effect of betulin administration on body weight of animals and no lethal effect were observed during 14 days after administration in rats and mice in all doses tested. LD50 was not reached in all experiments. Skin irritation, edema or infiltration at the injection site after intraperitoneal injection was not observed. Irritation of the gastrointestinal tract of rats and mice, and peritoneum in rats at the site of drugs injection has been not fixed. The form and location of all internal organs were without pathology booth in rats and mice and there were no significant changes in mass coefficients of organs.

In result of single intragastric administration or intraperitoneal injection of betulin in rats and mice no toxic effects were observed. Results of 14 days of observation of animals and data of necropsy evidenced about safety of this substance. Betulin is non-toxic and may be classified as substance of VI class toxicity [4].

Keywords: betulin, intragastric administration, intraperitoneal injection, mice, rats

Acknowledgement: the study was done in frame of FORESTSPECS project, grant agreement 227239

References: 1. Alakurtti S et al. (2006) Eur J Pharm Sci 29: 1–13

2. Krasutsky PA (2006) Nat Prod Rep 23: 919–942

3. Shikov AN et al. (2011) Phytomedicine doi:10.1016/j.phymed.2011.01.021;

4. Gosselin RE et al. (1976) Clinical Toxicology of Commercial Products. Acute Poisoning, 4th edition. Baltimore: Williams and Wilkins.