AUTHOR=Sevik Kilicaslan Ozlem , Cretton Sylvian , Hausmann Estelle , Quirós-Guerrero Luis , Karimou Soumana , Kaiser Marcel , Mäser Pascal , Christen Philippe , Cuendet Muriel 

TITLE=Antiprotozoal activity of natural products from Nigerien plants used in folk medicine

JOURNAL=Frontiers in Pharmacology

VOLUME=14

YEAR=2023

URL=https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2023.1190241

DOI=10.3389/fphar.2023.1190241

ISSN=1663-9812

ABSTRACT=<p>In the course of the screening of plants from Niger for antiprotozoal activity, the methanol extract of <italic>Cassia sieberiana</italic>, and the dichloromethane extracts of <italic>Ziziphus mauritiana</italic> and <italic>Sesamun alatum</italic> were found to be active against protozoan parasites, namely <italic>Trypanosoma brucei rhodesiense</italic>, <italic>Trypanosoma cruzi</italic>, <italic>Leishmania donovani</italic> and/or <italic>Plasmodium falciparum</italic>. Myricitrin (<bold>1</bold>), quercitrin (<bold>2</bold>) and 1-palmitoyl-lysolecithin (<bold>3</bold>) were isolated from <italic>C. sieberiana</italic>. From <italic>Z. mauritiana</italic>, the three triterpene derivatives <bold>13</bold>, <bold>15</bold>, and <bold>16</bold> are described here for the first time. Their chemical structures were determined by 1D and 2D NMR experiments, UV, IR and HRESIMS data. The absolute configurations were assigned via comparison of the experimental and calculated ECD spectra. In addition, eight known cyclopeptide alkaloids (<bold>4</bold>, <bold>5</bold>, <bold>7</bold>–<bold>12</bold>), and five known triterpenoids (<bold>6</bold>, <bold>14</bold>, <bold>17–19</bold>) were isolated. The antiprotozoal activity of the isolated compounds, as well as of eleven quinone derivatives (<bold>20–30</bold>) previously isolated from <italic>S. alatum</italic> was determined <italic>in vitro.</italic> The cytotoxicity in L6 rat myoblast cells was also evaluated. Compound <bold>18</bold> showed the highest antiplasmodial activity (IC<sub>50</sub> = 0.2 µm) and compound <bold>24</bold> inhibited <italic>T. b. rhodesiense</italic> with an IC<sub>50</sub> value of 0.007 <italic>µ</italic>M. However, it also displayed significant cytotoxicity in L6 cells (IC<sub>50</sub> = 0.4 µm).</p>