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

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',4',5'-hexamethoxyflavone (1) and 5-hydroxy-6,7,3',4',5'-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',4',5'-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',4',5'-pentamethoxyflavone (2) and provides a scientific basis of traditional use of L. ukambensis.

• Authors: Wamtinga Richard Sawadogo, Claudia Cerella, Ali Al-Mourabit, Céline Moriou, Marie-Hélène Teiten, Innocent Pierre Guissou, Mario Dicato, Marc Diederich
• Journal: Nutrients (Nutrients) Vol. 7 Issue 12 Pg. 10388-97 (Dec 10 2015) ISSN: 2072-6643 [Electronic] Switzerland
• PMID: 26690473 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Flavones
• Flavonoids
• Plant Extracts
• umuhengerin
• nobiletin
• tangeretin

Topics

• Apoptosis (drug effects)
• Cell Proliferation (drug effects)
• Cell Survival (drug effects)
• Flavones (chemistry, pharmacology)
• Flavonoids (chemistry, pharmacology)
• Humans
• Jurkat Cells
• K562 Cells
• Lantana (chemistry)
• Leukocytes, Mononuclear (drug effects)
• Plant Extracts (chemistry, pharmacology)
• Plants, Medicinal (chemistry)
• U937 Cells