Tachia sp. are used as antimalarials in the Amazon Region and
in vivo antimalarial activity of a Tachia sp. has been
previously reported. Tachia grandiflora Maguire and Weaver is
an Amazonian antimalarial plant and herein its cytotoxicity and antimalarial
activity were investigated. Spectral analysis of the tetraoxygenated xanthone
decussatin and the iridoid aglyone amplexine isolated, respectively, from the
chloroform fractions of root methanol and leaf ethanol extracts was performed.
In vitro inhibition of the growth of Plasmodium falciparum
Welch was evaluated using optical microscopy on blood smears. Crude extracts of
leaves and roots were inactive in vitro. However, chloroform fractions of the
root and leaf extracts [half-maximal inhibitory concentration (IC50) = 10.5 and
35.8 µg/mL, respectively] and amplexine (IC50= 7.1 µg/mL) were active in vitro.
Extracts and fractions were not toxic to type MRC-5 human fibroblasts (IC50>
50 µg/mL). Water extracts of the roots of T. grandiflora
administered by mouth were the most active extracts in the Peters 4-day
suppression test in Plasmodium berghei-infected mice. At 500
mg/kg/day, these extracts exhibited 45-59% inhibition five to seven days after
infection. T. grandiflora infusions, fractions and isolated
substance have potential as antimalarials.