1. Antimalarial and cytotoxic activities of pregnene-type steroidal alkaloids from Holarrhena pubescens roots.
- Author
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Cheenpracha S, Boapun P, Limtharakul Née Ritthiwigrom T, Laphookhieo S, and Pyne SG
- Subjects
- Alkaloids isolation & purification, Antimalarials isolation & purification, Antineoplastic Agents, Phytogenic isolation & purification, Cell Line, Tumor, Humans, Magnetic Resonance Spectroscopy, Molecular Structure, Phytochemicals isolation & purification, Phytochemicals pharmacology, Plant Roots chemistry, Plasmodium falciparum drug effects, Pregnenes isolation & purification, Steroids isolation & purification, Thailand, Alkaloids pharmacology, Antimalarials pharmacology, Antineoplastic Agents, Phytogenic pharmacology, Holarrhena chemistry, Pregnenes pharmacology, Steroids pharmacology
- 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 IC
50 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.- Published
- 2019
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