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. 2021 Dec;35(23):5112-5119.
doi: 10.1080/14786419.2020.1781116. Epub 2020 Jun 19.

Apoprunellelactone (APL), an antiprotozoal lactone from the stem barks of Isolona cooperi Hutch. & Dalziel (Annonaceae)

Timothée Aboua Okpekon  1 , Faustin Aka Kabran  1   2 , Venance Martial Say  1 , Laurent Evanno  2 , Alexandre Maciuk  2 , Philippe Loiseau  3 , Pierre Champy  2 , Bruno Figadère  2
Affiliations

Apoprunellelactone (APL), an antiprotozoal lactone from the stem barks of Isolona cooperi Hutch. & Dalziel (Annonaceae)

Timothée Aboua Okpekon et al. Nat Prod Res. 2021 Dec.

Abstract

Bioassay guided fractionation of the stem barks of Isolona cooperi led to the isolation of a new lactone, apoprunellelactone (APL, 1), and two known compounds, 5-[1-hydroxyhexyl]-2H-furan-2-one (2) and oleic acid (3). Their structures were elucidated by spectral analysis including MS, UV, IR, 1D and 2D-NMR spectroscopy. Evaluated for its antiprotozoal activities, APL (1) was found to be the most active on Leishmania donovani and L. major promastigotes with EC50 values of 16.3 and 8.2 µM, respectively. Against Trypanosoma brucei brucei trypomastigote forms, the activity of APL was moderated (MEC = 38.0 µM). Its hemisynthetic ester acetic derivative (1c) was 2-42 times more active than that of the APL and reference drugs, justifying further in vivo evaluation of the two compounds (1 and 1c) on Leishmania sp and Trypanosoma brucei brucei/mice models.

Keywords: Annonaceae; Isolona cooperi; antiprotozoal activities; apoprunellelactone; lactones.

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