Purpose: To examine the anti-leishmanial and cytotoxic effects of five naturally occurring phenolic
compounds: luteolin (1), lalioside (2), luteolin-4’-O-β-D-glucopyranoside (3), apigenin 4-O-β-D-glucopyranoside
(4) and apigenin (5) on Leishmania tropica KWH23 amastigotes .
Methods: The compounds were isolated from the leaves of
Lawsonia Inermis
via hyphenated high
performance liquid chromatography-high resolution mass spectrometry coupled with solid phase
extraction-tube transfer nuclear magnetic resonance technique. The isolated compounds were given
intraperitoneally to L. tropica KWH23 amastigotes-infected albino mice at a dose of ≥ 3 mg/kg for 5
days. Amphotericin-B was used as standard (reference) drug. Lymphocytes were used to analyze their
cytotoxicity.
Results: For compound 1, mean lesion size decreased from 0.82 ± 0.12 to 0.10 ± 0.01 after 120 days,
with 97 % cure of intracellular L. tropica amastigotes at a dose of 15 mg/kg, compared to amphotericin
B which produced 95 % cure at a dose of 30 mg/kg. Half-maximal concentration (IC
50) for compound 1
was 4.15 μg/ml against lymphocytes.
Conclusion: The results indicate that luteolin is a potent inhibitor of L. tropica amastigotes, with a
higher cytotoxic activity against lymphocytes, compared with luteolin-4’-O-β-D-glucopyranoside.
