TY - JOUR
T1 - Antileishmanial activity and mechanism of action from a purified fraction of Zingiber officinalis Roscoe against Leishmania amazonensis
AU - Duarte, Mariana C.
AU - Tavares, Grasiele S.V.
AU - Valadares, Diogo G.
AU - Lage, Daniela P.
AU - Ribeiro, Tatiana G.
AU - Lage, Letícia M.R.
AU - Rodrigues, Marcella R.
AU - Faraco, André A.G.
AU - Soto, Manuel
AU - da Silva, Eduardo S.
AU - Chávez Fumagalli, Miguel A.
AU - Tavares, Carlos A.P.
AU - Leite, João Paulo V.
AU - Oliveira, Jamil S.
AU - Castilho, Rachel O.
AU - Coelho, Eduardo A.F.
N1 - Publisher Copyright:
© 2016 Elsevier Inc.
PY - 2016/7/1
Y1 - 2016/7/1
N2 - In recent years, considerable attention has been given to identify new antileishmanial products derived from medicinal plants, although, to date, no new effective compound has been recently applied to treat leishmaniasis. In the present study, the antileishmanial activity of a water extract from Zingiber officinalis Roscoe (ginger) was investigated and a purified fraction, named F10, was identified as responsible by this biological activity. The chemical characterization performed for this fraction showed that it is mainly composed by flavonoids and saponins. The water extract and the F10 fraction presented IC50 values of 125.5 and 49.8 μg/mL, respectively. Their selectivity indexes (SI) were calculated and values were seven and 40 times higher, respectively, in relation to the value found for amphotericin B, which was used as a control. Additional studies were performed to evaluate the toxicity of these compounds in human red blood cells, besides of the production of nitrite, as an indicator of nitric oxide (NO), in treated and infected macrophages. The results showed that both F10 fraction and water extract were not toxic to human cells, and they were able to stimulate the nitrite production, with values of 13.6 and 5.4 μM, respectively, suggesting that their biological activity could be due to macrophages activation via NO production. In conclusion, the present study shows that a purified fraction from ginger could be evaluated in future works as a therapeutic alternative, on its own or in association with other drugs, to treat disease caused by L. amazonensis.
AB - In recent years, considerable attention has been given to identify new antileishmanial products derived from medicinal plants, although, to date, no new effective compound has been recently applied to treat leishmaniasis. In the present study, the antileishmanial activity of a water extract from Zingiber officinalis Roscoe (ginger) was investigated and a purified fraction, named F10, was identified as responsible by this biological activity. The chemical characterization performed for this fraction showed that it is mainly composed by flavonoids and saponins. The water extract and the F10 fraction presented IC50 values of 125.5 and 49.8 μg/mL, respectively. Their selectivity indexes (SI) were calculated and values were seven and 40 times higher, respectively, in relation to the value found for amphotericin B, which was used as a control. Additional studies were performed to evaluate the toxicity of these compounds in human red blood cells, besides of the production of nitrite, as an indicator of nitric oxide (NO), in treated and infected macrophages. The results showed that both F10 fraction and water extract were not toxic to human cells, and they were able to stimulate the nitrite production, with values of 13.6 and 5.4 μM, respectively, suggesting that their biological activity could be due to macrophages activation via NO production. In conclusion, the present study shows that a purified fraction from ginger could be evaluated in future works as a therapeutic alternative, on its own or in association with other drugs, to treat disease caused by L. amazonensis.
KW - Antileishmanial activity
KW - Leishmania amazonensis
KW - Nitric oxide
KW - Purified compounds
KW - Treatment
KW - Zingiber officinalis Roscoe
UR - http://www.scopus.com/inward/record.url?scp=84961710667&partnerID=8YFLogxK
U2 - 10.1016/j.exppara.2016.03.026
DO - 10.1016/j.exppara.2016.03.026
M3 - Article
C2 - 27013260
AN - SCOPUS:84961710667
SN - 0014-4894
VL - 166
SP - 21
EP - 28
JO - Experimental Parasitology
JF - Experimental Parasitology
ER -