Study of the betulin enriched birch bark extracts effects on human carcinoma cells and ear inflammation

Cristina A Dehelean,Atena Gǎluşcan,Ionuţ Ledeţi,Melania Munteanu,Mihaela Aluaş,Istvan Zupko,Simona Cinta-Pinzaru,Codruţa Şoica

doi:10.1186/1752-153x-6-137

Abstract

BackgroundPentacyclic triterpenes, mainly betulin and betulinic acid, are valuable anticancer agents found in the bark of birch tree. This study evaluates birch bark extracts for the active principles composition.ResultsNew improved extraction methods were applied on the bark of Betula pendula in order to reach the maximum content in active principles. Extracts were analyzed by HPLC-MS, Raman, SERS and 13C NMR spectroscopy which revealed a very high yield of betulin (over 90%). Growth inhibiting effects were measured in vitro on four malignant human cell lines: A431 (skin epidermoid carcinoma), A2780 (ovarian carcinoma), HeLa (cervix adenocarcinoma) and MCF7 (breast adenocarcinoma), by means of MTT assay. All of the prepared bark extracts exerted a pronounced antiproliferative effect against human cancer cell lines. In vivo studies involved the anti-inflammatory effect of birch extracts on TPA-induced model of inflammation in mice.ConclusionsThe research revealed the efficacy of the extraction procedures as well as the antiproliferative and anti-inflammatory effects of birch extracts.

Highlights

Pentacyclic triterpenes, mainly betulin and betulinic acid, are valuable anticancer agents found in the bark of birch tree
We improved in a unique manner the extraction procedure of betulin and betulinic acid from birch bark, by obtaining a higher amount of active compound than previous studies
We enriched the knowledge on birch bark extract regarding its antitumor properties by analyzing its activity on a new cell line (A2780)

Summary

Introduction

Pentacyclic triterpenes, mainly betulin and betulinic acid, are valuable anticancer agents found in the bark of birch tree. Pentacyclic triterpenes are a class of compounds extensively studied as future anticancer agents. One of the most studied substances within this class is betulinic acid (BA) whose antineoplasic effectiveness is diminished by its poor water solubility [1]. Betulinic acid (Figure 1a) can be found in many plants, especially Betula sp.; it can be obtained by chemical synthesis from its precursor, betulin (Figure 1b), which is present in the same specie [1]. The percentage of active substances in the birch bark differs from one species to another; few studies have been made on Betula. By oxidation of the C-28 hydroxylic group to carboxyl, betulin can be rapidly converted to its more active derivate, betulinic acid, with a a b

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