Abstract:
acid (XA), the major constituent of the fruit of Xylopia aethiopica has
shown several pharmacological properties. Consequently, the fruit is being used
in the preparation of food. Traditionally, the plant is used to treat several
diseases and it has been formulated into a nasal drop despite the lack of
information about its safety, food-drug interaction, and other pharmacokinetic
properties. Therefore, this study investigated the antiplasmodial effect of XA on
P. falciparum, and its effect on rat liver CYP enzymes in vivo and in vitro. To
establish the effect of XA on P. falciparum, the parasite strain Dd2 was cultured
and treated with XA. Pentobarbitone-induced sleeping time was used to
investigate the effect of XA on rat liver enzymes. Inhibition or induction of
some isoforms of CYP450, CYP 1A1/1A2, 1A2, 2B1/2B2, 3A4, 2D6 and 2C9
was investigated using microsomal fractions of rat liver. The in vitro inhibition
of selected CYP (1A2, 3A4) was assessed by treating rat liver microsomes XA.
Results obtained showed that Xylopic acid exhibited negligible antiplasmodial
activity. The IC50 of XA > 20 μM. Xylopic acid induced CYP 1A1/1A2, 1A2,
2D6, 2C9, and inhibited CYP3A4, 2B1/2B2. The findings would help mitigate
toxicity and therapeutic failure especially in cases of co-administration of
medications with food containing XA, with metabolism altered by the latter
