Antimalarial and cytotoxic activities of pregnene-type steroidal alkaloids from Holarrhena pubescens roots |
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| Authors: | Sarot Cheenpracha Pannakorn Boapun Thunwadee Limtharakul Surat Laphookhieo Stephen G Pyne |
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| Institution: | 1. Division of Chemistry, School of Science, University of Phayao , Muang Phayao, Thailand;2. Faculty of Science, Department of Chemistry and Center of Excellence for Innovation in Chemistry, Chiang Mai University , Chiang Mai, Thailand;3. Research Center on Chemistry for Development of Health Promoting Products from Northern Resources, Chiang Mai University , Chiang Mai, Thailand;4. Center of Chemical Innovation for Sustainability (CIS), Mae Fah Luang University , Muang, Thailand;5. School of Science, Mae Fah Luang University , Muang, Thailand;6. School of Chemistry, University of Wollongong , Wollongong, Australia |
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| Abstract: | The phytochemical investigation of an alkaloidal extract of Holarrhena pubescens roots led to the isolation and identification of a new pregnene-type alkaloid, mokluangin D (1), together with nine known steroidal alkaloids (2–10). The structure of the new metabolite was determined on the basis of spectroscopic analyses including 1D- and 2D-NMR spectroscopy and mass spectrometry. Compounds 3 and 4 showed potent antimalarial activity against Plasmodium falciparum K1 stain with IC50 values of 1.2 and 2.0 μM, respectively, and showed weak cytotoxic activity against the NCI-H187 cell line with IC50 values of 27.7 and 30.6 μM, respectively. The substituent groups at C-3 and the carbonyl group at C-18 are important for the activity against the P. falciparum K1 stain. |
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| Keywords: | Holarrhena pubescens pregnene-type steroidal alkaloids cytotoxicity antimalarial activity |
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