In vitro anti-Leishmania activity of tetracyclic iridoids from Morinda lucida, benth

Michael Amoa-Bosompem, Mitsuko Ohashi, Mba-Tihssommah Mosore, Jeffrey Agyapong, Nguyen Huu Tung, Kofi D. Kwofie, Frederick Ayertey, Kofi Baffuor-Awuah Owusu, Isaac Tuffour, Philip Atchoglo, Georgina I. Djameh, Faustus A. Azerigyik, Senyo K. Botchie, William K. Anyan, Regina Appiah-Opong, Takuhiro Uto, Osamu Morinaga, Alfred. A. Appiah, Irene Ayi, Yukihiro Shoyama, Daniel A Boakye, Nobuo Ohta

Leishmaniasis is an infectious disease transmitted by the sand fly. It is caused by over 20 different species of Leishmania and has affected over 14 million people worldwide. One of the main forms of control of leishmaniasis is chemotherapy, but this is limited by the high cost and/or toxicity of available drugs. We previously found three novel compounds with an iridoid tetracyclic skeleton to have activity against trypanosome parasites. In this study, we determined the activity of the three anti-trypanosome compounds against Leishmania using field strain, 010, and the lab strain Leishmania hertigi. The minimum inhibitory concentration (MIC) of the compounds against 010 was determined by microscopy while the IC50 of compounds against L. hertigi was determined by fluorescence-activated cell sorting with Guava viacount analysis. We found two of the three compounds, molucidin and ML-F52, to have anti-Leishmania activity against both strains. The fluor-microscope observation with DAPI stain revealed that both Molucidin and ML-F52 induced abnormal parasites with two sets of nucleus and kinetoplast in a cell, suggesting that compounds might inhibit cytokinesis in Leishmania parasites. Molucidin and ML-F52 might be good lead compounds for the development of new anti-Leishmania chemotherapy.