In vitro cytotoxic, antifungal, trypanocidal and leishmanicidal activities of acetogenins isolated from Annona cornifolia A. St. -Hil. (Annonaceae)

Luciana A.R.S Lima,Patrícia S Cisalpino,Policarpo A Sales Júnior,Lúcia P.S Pimenta,Maria Amélia D Boaventura,Carlos L Zani,Tânia M.A Alves,Susana Johann,Alvaro J Romanha

doi:10.1590/0001-3765201420130048

Abstract

Annona cornifolia A. St. -Hil. is a small annual perennial tree found in the Brazilian savannah; their green fruit is popularly used in the treatment of ulcers. The acetogenins isolated from the seeds of Annona cornifolia previously showed to possess antioxidant activity. In continuation of our investigations on the biological activities of acetogenins, four binary mixtures and ten pure adjacent bis-tetrahydrofuran annonaceous acetogenins were evaluated: the cytotoxic (against three human tumor cell lines), antifungal (against Paracoccidioides brasiliensis), trypanocidal (against Trypanosoma cruzi) and leishmanicidal (against Leishmania amazonensis) activities. Acetogenins presented cytotoxic activity confirming their potential use in anti-cancer therapy. Regarding leishmanicidal and trypanocidal activities, an inhibition of 87% of L. amazonensis amastigotes and 100% of T. cruzi amastigotes and trypomastigotes was observed, when tested at the concentration of 20 µg mL-1. Moreover, six acetogenins showed more activity against all the three tested isolates of P. brasiliensis than trimethoprim-sulfamethoxazole, a drug used for treating paracoccidioidomycosis. Thus, acetogenins may be an alternative in treating a number of diseases that have a huge impact on millions of people worldwide. This paper reports for the first time the antifungal, leishmanicidal and trypanocidal activities for these acetogenins.

Highlights

Several Annona species of the Annonaceae family produce edible fruits that are widely consumed in Brazil, such as Annona squamosa and Annona muricata
Six acetogenins showed more activity against all the three tested isolates of P. brasiliensis than trimethoprim-sulfamethoxazole, a drug used for treating paracoccidioidomycosis
This paper reports for the first time the antifungal, leishmanicidal and trypanocidal activities for these acetogenins

Summary

Introduction

Several Annona species of the Annonaceae family produce edible fruits that are widely consumed in Brazil, such as Annona squamosa and Annona muricata. -Hil., with orange fruits, is a small annual perennial tree cornifolia (Santos et al 2006, 2007, Lima et al 2009, 2010), as well as from the leaves of Rollinia laurifolia (Pimenta et al 2001, 2003, 2005). There are no reports on the study of other parts of Annona cornifolia, including the phytochemical studies of the fruit. The fruits of several Annona species are an important source of proteins, carbohydrates and amino acids (Correa 1984). Further research may shed light on the use of fruit of A. cornifolia in future dietary supplementation

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