Abstract
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-Dglucopyranoside (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 (IC50) 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.Keywords: Leishmania tropica, Luteolin, Lalioside, Luteolin-4’-O-β-D-glucopyranoside, Apigenin 4-O- β-D-glucopyranoside, Apigenin
Highlights
Leishmaniasis, caused by parasites belonging to the genus Leishmania (Family Trypanosomatidae), is a major public health problem in tropical and sub-tropical regions
Cutaneous leishmaniasis is caused by different Leishmania species, e.g. Leishmania tropica, Leishmania major, Leishmania amazonensis, and Leishmania brazillensis
In Pakistan, L. tropica and L. major are the main causes of cutaneous leishmaniasis [4,5]
Summary
Leishmaniasis, caused by parasites belonging to the genus Leishmania (Family Trypanosomatidae), is a major public health problem in tropical and sub-tropical regions. The World Health Organization, WHO has reported that people from 98 countries in 5 continents, are at high risk of leishmaniasis, and it is estimated that approximately 12 million people are currently infected [1,2,3]. Cutaneous leishmaniasis is caused by different Leishmania species, e.g. Leishmania tropica, Leishmania major, Leishmania amazonensis, and Leishmania brazillensis. In Pakistan, L. tropica and L. major are the main causes of cutaneous leishmaniasis [4,5]. First line therapy for cutaneous leishmaniasis in Europe, Asia and Africa is pentavalent antimonials, i.e., sodium stibogluconate and meglumine antimoniate [2]. There is an urgent need for new chemical entities for non-toxic and effective treatment of leishmaniasis [2,4]
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