Salvia officinalis L.: Antitrypanosomal Activity and Active Constituents against Trypanosoma brucei rhodesiense.

Núria Llurba Montesino,Thomas J Schmidt,Marcel Kaiser,Pascal Mäser

doi:10.3390/molecules26113226

Abstract

As part of our studies on antiprotozoal activity of approved herbal medicinal products, we previously found that a commercial tincture from Salvia officinalis L. (common Sage, Lamiaceae) possesses high activity against Trypanosoma brucei rhodesiense (Tbr), causative agent of East African Human Trypanosomiasis. We have now investigated in detail the antitrypanosomal constituents of this preparation. A variety of fractions were tested for antitrypanosomal activity and analyzed by UHPLC/+ESI QqTOF MS. The resulting data were used to generate a partial least squares (PLS) regression model that highlighted eight particular constituents that were likely to account for the major part of the bioactivity. These compounds were then purified and identified and their activity against the pathogen tested. All identified compounds (one flavonoid and eight diterpenes) displayed significant activity against Tbr, in some cases higher than that of the total tincture. From the overall results, it can be concluded that the antitrypanosomal activity of S. officinalis L. is, for the major part, caused by abietane-type diterpenes of the rosmanol/rosmaquinone group.

Highlights

Human African Typanosomiasis (HAT or “sleeping sickness”) is one of 20 diseases currently classified by WHO as neglected tropical diseases (NTDs)
We reported on the antiprotozoal activity of 53 herbal medicinal products (HMPs) approved in Germany and commonly marketed for other ailments
We report on the identification of the main antitrypanosomal constituents from this HMP, using a multivariate statistics-guided isolation approach, and their bioactivity against the pathogen

Summary

Introduction

Human African Typanosomiasis (HAT or “sleeping sickness”) is one of 20 diseases currently classified by WHO as neglected tropical diseases (NTDs). HAT, as well as the cattle disease Nagana, are caused by the kinetoplastid parasite Trypanosoma brucei subsp. [1] and are usually lethal if untreated. The few existing medications for HAT are toxic or difficult to administer. Drugs in use against Nagana suffer from increasing parasite resistance. The identification of new active chemical entities against T. brucei is, an urgent need. The first orally active trypanocidal drug to treat late-stage HAT, fexinidazole [2], was introduced. It remains important to identify further new active compounds, against the diseases affecting humans as well as animals, possibly with new mechanisms of action, in order to develop further drugs against African trypanosomes

Methods

Results

Conclusion