Cytotoxic, Antiproliferative and Pro-Apoptotic Effects of 5-Hydroxyl-6,7,3′,4′,5′-Pentamethoxyflavone Isolated from Lantana ukambensis

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Cytotoxic, Antiproliferative and Pro-Apoptotic Effects of 5-Hydroxyl-6,7,3′,4′,5′-Pentamethoxyflavone Isolated from Lantana ukambensis

Authors
Type
Published Article
Journal
Nutrients
2072-6643
Publisher
MDPI AG
Publication Date
Volume
7
Issue
12
Pages
10388–10397
Identifiers
DOI: 10.3390/nu7125537
Source
LBMCC
Keywords
  • Cytotoxic
  • Lantana Ukambensis (Vatke) Verdc.
  • Polymethoxyflavones
Funders
  • Fonds National de la Recherche Luxembourg

Abstract

Lantana ukambensis (Vatke) Verdc. is an African food and medicinal plant. Its red fruits are eaten and highly appreciated by the rural population. This plant was extensively used in African folk medicinal traditions to treat chronic wounds but also as anti-leishmanial or cytotoxic remedies, especially in Burkina Faso, Tanzania, Kenya, or Ethiopia. This study investigates the in vitro bioactivity of polymethoxyflavones extracted from a L. ukambensis as anti-proliferative and pro-apoptotic agents. We isolated two known polymethoxyflavones, 5,6,7,3 1 ,4 1 ,5 1-hexamethoxyflavone (1) and 5-hydroxy-6,7,3 1 ,4 1 ,5 1-pentamethoxyflavone (2) from the whole plant of L. ukambensis. Their chemical structures were determined by spectroscopic analysis and comparison with published data. These molecules were tested for the anti-proliferative, cytotoxic and pro-apoptotic effects on human cancer cells. Among them, 5-hydroxy-6,7,3 1 ,4 1 ,5 1-pentamethoxyflavone (2) was selectively cytotoxic against monocytic lymphoma (U937), acute T cell leukemia (Jurkat), and chronic myelogenous leukemia (K562) cell lines, but not against peripheral blood mononuclear cells (PBMCs) from healthy donors, at all tested concentrations. Moreover, this compound exhibited significant anti-proliferative and pro-apoptotic effects against U937 acute myelogenous leukemia cells. This study highlights the anti-proliferative and pro-apoptotic effects of 5-hydroxy-6,7,3 1 ,4 1 ,5 1-pentamethoxyflavone (2) and provides a scientific basis of traditional use of L. ukambensis.

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