Abstract
The effects of the Securinega alkaloid (+)-phyllanthidine on Leishmania (L.) amazonensis and the first chemical investigation of Margaritaria nobilis L.f. (Phyllanthaceae) are described. Treating the parasites with this alkaloid caused a dose-dependent reduction in promastigote growth of 67.68% (IC50 82.37 μg/mL or 353 µM) and in amastigote growth of 83.96% (IC50 49.11 μg/mL or 210 µM), together with ultrastructural alterations in the promastigotes. No cytotoxic effect was detected in mammalian cells (CC50 1727.48 µg/mL or CC50 5268 µM). Classical chromatographic techniques and spectral methods led to the isolation and identification of betulinic acid, kaempferol, corilagin, gallic acid and its methyl ester, besides (+)-phyllanthidine from M. nobilis leaves and stems. Margaritaria nobilis is another source of the small group of Securinega alkaloids, together with other Phyllanthaceae (Euphorbiaceae s.l.) species. The low toxicity to macrophages and the effects against promastigotes and amastigotes are suggestive that (+)-phyllanthidine could be a promising antileishmanial agent for treating cutaneous leishmaniasis.
Highlights
Leishmaniasis is an anthropozoonotic and neglected disease, and it is considered a major health problem worldwide [1]
The analysis showed the typical morphology of untreated promastigotes (Figure 6A) and alterations in the flagellum and cellular body of promastigote forms after they were treated with the alkaloid
M—MitoScohmoendauritaho(r*s) hacaivdeoschaolwcisnocmhaensg. eSscainleLbeiasrhsm=an2iaμkmin.etoplasts after using natural products, such as the alkaloid julocrotine [36] and the oil from Ocimum gratissimum [45]. This organelle is present only in trypanosomatids, and it is a major target for drug action because of its unique structure and Somfuenacutiothno[4r4s,4h6a].ve shown changes in Leishmania kinetoplasts after using natural products, such as the alkalo(i+d)-Pjuhlyollcarnothtiindiene[3a6ls]oacnadusethdeanoiilncfrreoamse Oinctihmeunmumgbreartiosfsiamciudmoca[l4c5is]o.mTe-hliikseosrtrguacntuerlelse iins present promastigotes treated with 100 μg/mL of (+)-phyllanthidine (Figure 6E,F)
Summary
Leishmaniasis is an anthropozoonotic and neglected disease, and it is considered a major health problem worldwide [1]. This disease is caused by parasites belonging to the genus Leishmania, and it affects approximately 12 million people worldwide [2,3,4]. It is an endemic disease in 98 countries, with most cases reported in tropical and subtropical countries [5]. Molecules 2015, 20, 22157–22169 chemical composition of M. nobilis and the effect of the alkaloid (+)-phyllanthidine on the protozoan ML.ol(eLcu.)leasm20a1z5o, n20e,npsaisg.e–page
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