@article{fdi:010067604,
  title = {{W}ayanin and guaijaverin, two active metabolites found in a {P}sidium acutangulum {M}art. ex {DC} (syn. {P}. persoonii {M}c{V}augh) ({M}yrtaceae) antimalarial decoction from the {W}ayana {A}merindians},
  author = {{H}ouel, {E}. and {N}ardella, {F}. and {J}ullian, {V}al{\'e}rie and {V}alentin, {A}. and {V}onthron-{S}enecheau, {C}. and {V}illa, {P}. and {O}brecht, {A}. and {K}aiser, {M}. and {B}ourreau, {E}. and {O}donne, {G}. and {F}leury, {M}arie and {B}ourdy, {G}enevi{\`e}ve and {E}parvier, {V}. and {D}eharo, {E}ric and {S}tien, {D}.},
  editor = {},
  language = {{ENG}},
  abstract = {{E}thnopharmacological relevance: {P}sidium acutangulum {M}art. ex {DC} is a small tree used by the {W}ayana {A}merindians from the {U}pper-{M}aroni in {F}rench {G}uiana for the treatment of malaria. {A}im of the study: {I}n a previous study, we highlighted the in vitro antiplasmodial, antioxidant and anti-inflammatory potential of the traditional decoction of {P}. acutangulum aerial parts. {O}ur goal was then to investigate on the origin of the biological activity of the traditional remedy, and eventually characterize active constituents. {M}aterials and methods: {L}iquid-liquid extractions were performed on the decoction, and the antiplasmodial activity evaluated against chloroquine-resistant {F}c{B}1 ([{H}-3]-hypoxanthine bioassay) and 7{G}8 (p{LDH} bioassay) {P}. falciparum strains, and on a chloroquine sensitive {NF}54 ([{H}-3]-hypoxanthine bioassay) {P}. falciparum strain. {T}he ethyl acetate fraction ({D}) was active and underwent bioguided fractionation. {A}ll the isolated compounds were tested on {P}. falciparum {F}c{B}1 strain. {I}n vitro anti-inflammatory activity ({IL}-1 beta, {IL}-6, {IL}-8, {TNF} alpha) of the ethyl acetate fraction and of an anti-{P}lasmodium active compound, was concurrently assessed on {LPS}-stimulated human {PBMC} and {NO} secretion inhibition was measured on {LPS} stimulated {RAW} murine macrophages. {C}ytotoxicity of the fractions and pure compounds was measured on {VERO} cells, {L}6 mammalian cells, {PBMC}s, and {RAW} cells. {R}esults: {F}ractionation of the ethyl acetate soluble fraction ({IC}50 ranging from 3.4 to < 1 mu g/m{L} depending on the parasite strain) led to the isolation of six pure compounds: catechin and five glycosylated quercetin derivatives. {T}hese compounds have never been isolated from this plant species. {T}wo of these compounds (wayanin and guaijaverin) were found to be moderately active against {P}. falciparum {F}c{B}1 in vitro ({IC}50 5.5 and 6.9 mu {M} respectively). {W}e proposed the name wayanin during public meetings organized in {J}une 2015 in the {U}pper-{M}aroni villages, in homage to the medicinal knowledge of the {W}ayana population. {A}t 50 mu g/m{L}, the ethyl acetate fraction ({D}) significantly inhibited {IL}-1 beta secretion (-46%) and {NO} production (21%), as previously observed for the decoction. {T}he effects of {D} and guiajaverin (4) on the secretion of other cytokines or {NO} production were not significant. {C}onclusions: {T}he confirmed antiplasmodial activity of the ethyl acetate soluble fraction of the decoction and of the isolated compounds support the previous results obtained on the {P}. acutangulum decoction. {T}he antiplasmodial activity might be due to a mixture of moderately active non-toxic flavonoids. {T}he anti-inflammatory activities were less marked for ethyl acetate fraction ({D}) than for the decoction.},
  keywords = {{P}sidium acutangulum ; {T}raditional remedy ; {C}ytokines ; {A}ntimalarial ; {G}lycosylated flavonols ; {F}rench guiana ; {GUYANE} {FRANCAISE}},
  booktitle = {},
  journal = {{J}ournal of {E}thnopharmacology},
  volume = {187},
  numero = {},
  pages = {241--248},
  ISSN = {0378-8741},
  year = {2016},
  DOI = {10.1016/j.jep.2016.04.053},
  URL = {https://www.documentation.ird.fr/hor/fdi:010067604},
}