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.

Phytochemistry investigation and antioxidant activity of four edible Verbenaceae of Burkina Faso

“…Indeed, this study concluded that Vitexdoniana fruit pulp could be promoted as: carbohydrate and lipid supplements for cereal-based diets inrural communities [39]. Sawadogo et al [3] have quantified some metal ions (Na + and K + ) and showed th.eir implication in the Na + -K + -pump action.…”

“…Thus we couldn't find the derivative luteolin and rutin [1] in our extracts. Other researchers showed in the dichloromethane fractions of L. rhodesiensis, two flavonoids such as 5,6,7,3',4',5'hexamethoxyflavone and its analogue, 5-hydroxy-6,7,3',4',5'pentamethoxyflavone [3]. The most elucidated studies on L. chevalieri, L. rhodesiensis, V. diversifolia and V. donianaespecially related to their content of essential oils [1], [3], [5], [8].…”

“…). These plants are as well-known and used in traditional medicines in Burkina Faso [3], [4] [5], [6]. Phytochemistry and biological screening of these plants form integral part is our research plan.…”

Methoxy-flavones identified from Ageratum conyzoides induce capase -3 and -7 activations in Jurkat cells

“…Limited data are available on this flavone. The few studies report its isolation from Lantana ukambensis, Citrus reticulate and A. conyzoides, and its cytotoxicity against P-388 mouse lymphocytic leukemia and A549 lung carcinoma cells, and inhibition of histamine release in RBL-2HR cells (Adebayo et al, 2010;Sawadogo et al, 2015;Itoh et al, 2008).…”

A review on Lantana rhodesiensis Moldenke: traditional uses, phytochemical constituents and pharmacological activities

“…Roots are boiled in water and drunk for rheumatism and generalized body pains [4][5][6][7][8][9][10][11][12][13][14]. Especially in Burkina Faso, L. rhodesiensis is used in folk medicine to treat chronic wounds and skin diseases [15]. Accordint toTeketay et al [13], leaf ofL.…”