Abstract
Piper amalago L. leaves were extracted with supercritical carbon dioxide and compressed propane under different conditions, and with chloroform by the conventional maceration method. These methods were compared for the pyrrolidine alkaloid content. Supercritical carbon dioxide (SFE-CO2) at 313 K and 12.55 MPa showed the highest selectivity for the main compound (600.53 mg/g of extract). A gradient high-performance liquid chromatography (HPLC) method was developed and validated to quantify the alkaloid N-[7-(3′,4′-methylenedioxyphenyl)-2(Z),4(Z)-heptadienoyl]pyrrolidine (1) in the extracts. The HPLC method showed linearity, precision and accuracy, allowing the quantitative analysis of the alkaloid in all the samples. All the extracts were tested against the promastigote and intracellular amastigote forms of Leishmania amazonensis. The antileishmanial activity was evaluated in terms of inhibitory concentration for 50% of protozoa (IC50). The cytotoxicity was also evaluated against J774A1 macrophages, and the cytotoxic concentrations for 50% of macrophages were obtained (CC50). The SFE-CO2 (313 K; 12.55 MPa) extract showed the highest antileishmanial activity with the following IC50 values of 16 and 7 µg/mL against the promastigotes and intracellular amastigotes forms, respectively. The extract showed low cytotoxicity with a CC50 value of 93 µg/mL.
Highlights
Leishmaniasis affects about 12 million people in the tropical and subtropical areas of the World, being a serious health public problem [1]
This paper has described the development and validation of a high-performance liquid chromatography (HPLC) method for quantification of the pyrrolidine alkaloid N-[7-(3′,4′-Methylenedioxyphenyl)-2(Z),4(Z)-heptadienoyl]pyrrolidine (1) in extracts of P. amalago L. leaves
CO2, compressed propane, and maceration methods were examined with respect to pyrrolidine alkaloid content, using the validated HPLC method
Summary
Leishmaniasis affects about 12 million people in the tropical and subtropical areas of the World, being a serious health public problem [1]. The urban development, migration of people to endemic areas and human immunodeficiency virus infection are the main factors for the increasing of infected individuals [2]. This disease is caused by protozoans of the genus Leishmania that lead to cutaneous, visceral, and mucosal clinical forms [3,4]. Miltefosine is a novel compound active against leishmaniasis, but it is teratogenic [5]. These facts indicate a need to discover new drugs, and plants have been considered as potential sources of new and more effective products [6]
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