@article{fdi:010064808,
  title = {{E}valuation of antiplasmodial and antileishmanial activities of herbal medicine {P}seudelephantopus spiralis ({L}ess.) {C}ronquist and isolated hirsutinolide-type sesquiterpenoids},
  author = {{G}irardi, {C}. and {F}abre, {N}icolas and {P}aloque, {L}. and {R}amadani, {A}. {P}. and {B}enoit-{V}ical, {F}. and {G}onzalez-{A}spajo, {G}. and {H}addad, {M}ohamed and {R}engifo, {E}. and {J}ullian, {V}al{\'e}rie},
  editor = {},
  language = {{ENG}},
  abstract = {{E}thnopharmacological relevance: {P}seudelephantopus spiralis ({L}ess.) {C}ronquist is distributed in the {C}aribbean, {M}esoamerica and {L}atin {A}merica. {P}reparations of the plant are traditionally used in {L}atin {A}merica for the treatment of various diseases including fever, malaria, and spleen or liver inflammations. {M}aterials and methods: {A}erial parts of {P}. spiralis were extracted with either ethanol or distilled water. {S}even hirsutinolide-type sesquiterpenoids were isolated: 8-acetyl-13-ethoxypiptocarphol (1), diacetylpiptocarphol (2), piptocarphins {A} (3), {F} (4) and {D} (5), (1{S}*,4{R}*,8{S}*,10{R}*)-1,4-epoxy-13-ethoxy-1,8,10-trihydroxygermacra-5{E},7(11)-dien-6,12-olide (6), and piptocarphol (7). {E}xtracts and isolated compounds (2, 3, 5-7) were screened for their in vitro antiplasmodial activity against the chloroquine-resistant {P}lasmodium falciparum strain {F}c{M}29-{C}ameroon and antileishmanial activity against three stages of {L}eishmania infantum. {T}heir cytotoxicities were also evaluated against healthy {VERO} cell lines and {J}774{A}.1 macrophages, the host cells of the {L}eishmania parasites in humans. {R}esults: {A}queous extracts showed a greater inhibitory effect than alcoholic extracts, with {IC}50 on {P}. falciparum of 3.0 mu z/m{L} versus 211 mu g/m{L}, and on {L} infantum of 13.4 mu g/m{L} versus >50 mu g/m{L}. {B}oth extracts were found to be cytotoxic to {VERO} cells ({CC}50 < 3 mu g/m{L}). {S}esquiterpene lactones 2 and 3 showed the best activity against both parasites but failed in selectivity. {C}arbon 8 hydroxylated hirsutinolides 5-7 presented the particularity of exhibiting two conformers observed in solution during extensive {NMR} analyses in {CD}3{OD} and {UHPLC}-{MS}. {T}he presence of a hydroxyl function at {C}-8 decreased the activity of 5-7 on the two parasites and also on {VERO} cells. {C}onclusion: {T}he antiplasmodial activity displayed by the aqueous extract explains the traditional use of {P}. spiralis in the treatment of malaria. {T}his activity seems to be attributable to the presence of sesquiterpene lactones 2 and 3, the most active against {P}. falciparum. {A}queous extract and compounds 2, 3 and 6 were also active against {L} infantum but lacked in selectivity due to their cytotoxicity towards macrophages. {E}xploring the safety and antiplasmodial efficacy of this traditional remedy will require further toxicological and in vivo studies in the light of the cytotoxicity towards healthy cell lines displayed by the aqueous extract and compounds 2 and 3.},
  keywords = {{P}seudelephantopus spiralis ; {S}esquiterpene lactones ; {H}irsutinolides ; {M}alaria ; {L}eishmaniasis ; {AMERIQUE} {LATINE} ; {PEROU}},
  booktitle = {},
  journal = {{J}ournal of {E}thnopharmacology},
  volume = {170},
  numero = {},
  pages = {167--174},
  ISSN = {0378-8741},
  year = {2015},
  DOI = {10.1016/j.jep.2015.05.014},
  URL = {https://www.documentation.ird.fr/hor/fdi:010064808},
}