Abstract
A new indole alkaloid, 12-hydroxy-N-acetyl-21(N)-dehydroplumeran-18-oic acid (13), and 11 known indole alkaloids: 3,4,5,6-tetradehydro-β-yohimbine (3), 19(E)-hunteracine (4), β-yohimbine (5), yohimbine (6), 19,20-dehydro-17-α-yohimbine (7), uleine (10), 20-epi-dasycarpidone (11), olivacine (8), 20-epi-N-nor-dasycarpidone (14), N-demethyluleine (15) and 20(E)-nor-subincanadine E (12) and a boonein δ-lactone 9, ursolic acid (1) and 1D,1O-methyl-chiro-inositol (2) were isolated from the EtOH extracts of different parts of Aspidosperma ulei Markgr. (Apocynaceae). Identification and structural elucidation were based on IR, MS, 1H- and 13C-NMR spectral data and comparison to literature data. The antiplasmodial and antimalarial activity of 1, 5, 6, 8, 10 and 15 has been previously evaluated and 1 and 10 have important in vitro and in vivo antimalarial properties according to patent and/or scientific literature. With the aim of discovering new antiplasmodial indole alkaloids, 3, 4, 11, 12 and 13 were evaluated for in vitro inhibition against the multi-drug resistant K1 strain of the human malaria parasite Plasmodium falciparum. IC50 values of 14.0 (39.9), 4.5 (16.7) and 14.5 (54.3) μg/mL (μM) were determined for 3, 11 and 12, respectively. Inhibitory activity of 3, 4, 11, 12 and 13 was evaluated against NIH3T3 murine fibroblasts. None of these compounds exhibited toxicity to fibroblasts (IC50 > 50 μg/mL). Of the five compounds screened for in vitro antiplasmodial activity, only 11 was active.
Highlights
Malaria continues to be a disease that afflicts the whole World, especially the African continent.data from 99 countries reveals that based on the overall number of deaths malaria is in decline [1]
Phytochemical investigation of the leaf, bark, trunk wood, root wood and root bark EtOH extracts of Aspidosperma ulei led to the isolation and structural elucidation of several classes of compounds (Figure 1)
This work represents a significant contribution to the knowledge of the chemical composition of
Summary
Malaria continues to be a disease that afflicts the whole World, especially the African continent.data from 99 countries reveals that based on the overall number of deaths malaria is in decline [1]. Malaria continues to be a disease that afflicts the whole World, especially the African continent. The main antimalarials available today are the quinolines that are structural mimics of the plant-derived natural product quinine and the semi-synthetic derivatives of another plant-derived natural product, artemisinin. Resistance of the malaria parasites to these drugs is an issue of concern and it is important to discover new compounds that may be developed into the generation of antimalarial drugs [2]. Aspidosperma spp. extracts exhibit antimalarial activity and remedies prepared from the bark are used in traditional medicine for the treatment of malaria [3]. Screening of bark extracts representing six Aspidosperma spp. for in vitro inhibition against chloroquine-resistant W2 and chloroquine-sensitive
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