The traditional medicine Spilanthes acmella, and the alkylamides spilanthol and undeca-2E-ene-8,10-diynoic acid isobutylamide, demonstrate in vitro and in vivo antimalarial activity.

The traditional medicine Spilanthes acmella, and the alkylamides spilanthol and undeca-2E-ene-8,10-diynoic acid isobutylamide, demonstrate in vitro and in vivo antimalarial activity.
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传统药物千日菊、烷基酰胺千日菊素和十一碳二烯-8,10-二炔酸异丁酰胺在体外和体内均表现出抗疟活性。

DOI:
10.1002/ptr.3395
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发表时间:
2011
期刊:
Phytotherapy research : PTR
影响因子:
--
通讯作者:
Grellier,Philippe
Grellier,Philippe
中科院分区:
--
文献类型:
--
作者:
Spelman,Kevin;Depoix,Delphine;McCray,Megan;Mouray,Elisabeth;Grellier,Philippe

文献摘要

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Spilanthesspp. are used as traditional herbal medicines in Africa and India to treat malaria. Yet, to date, there are no data on the active constituents or the most effective extraction methods for this indication. The isolated alkylamides, spilanthol and undeca‐2E‐ene‐8,10‐diynoic acid isobutylamide, found inS. acmellaMurr., were shown to have IC50s of 16.5 μg/mL and 41.4 μg/mL onPlasmodium falciparumstrain PFB and IC50s of 5.8 μg/mL and 16.3 μg/mL for the chloroquine resistantP. falciparumK1 strain, respectively. Further investigations revealed that at relatively low concentrations, spilanthol and the water extract ofS. acmellareduced the parasitemia 59% and 53% in mice infected withP. yoelii yoelii17XNL at 5 mg/kg and 50 mg/kg, respectively. Unexpectedly, the 95% ethanol extract ofS. acmellawas less effective (36% reduction in parasitemia) at 50 mg/kg. These results provide the first evidence supportingS. acmellaagainst malaria and demonstrating active constituents inS. acmellaagainstP. falciparum. Copyright © 2011 John Wiley & Sons, Ltd.