TY - JOUR
T1 - Antiparasitic compounds from Cornus florida L. with activities against Plasmodium falciparum and Leishmania tarentolae
AU - Graziose, Rocky
AU - Rojas-Silva, Patricio
AU - Rathinasabapathy, Thirumurugan
AU - Dekock, Carmen
AU - Grace, Mary H.
AU - Poulev, Alexander
AU - Ann Lila, Mary
AU - Smith, Peter
AU - Raskin, Ilya
N1 - Funding Information:
This work was funded by the Medicines for Malaria Venture (MMV) . R. Graziose is supported by a Ruth L. Kirschstein predoctoral training award provided by the National Center for Complementary and Alternative Medicine of the National Institutes of Health. P. Rojas-Silva is funded by a SENESCYT 2011 Scholarship provided by the Ecuadorian government. We would like to thank Dr. Lena Struwe for her help in identifying the plant material used in this project. We would also like to thank Dr. Anita Brinker for her help with LC/APPI-MS and Dr. David Ribnicky for his help with GC/EI-MS. We are grateful for the cultures of L. tarentolae, kindly provided by Dr. Larry Simpson University of California, Los Angeles.
PY - 2012/7/13
Y1 - 2012/7/13
N2 - Aim of the study: The objective of this study was to identify the antiplasmodial constituents from the bark of Cornus florida L., a plant traditionally used in North America for the treatment of malaria. Methods and materials: Dried and powdered bark was extracted with 95% ethanol. The resultant extract was subjected to in vitro antiplasmodial-guided fractionation against Plasmodium falciparum (D10 strain). Antiplasmodial IC 50 values were calculated for pure compounds. Compounds were also assayed against Leishmania tarentolae, and rat skeletal myoblast L6 cells to assess antileishmanial activity and cytotoxicity, respectively. Results: Antiplasmodial-guided fractionation afforded 8 compounds: betulinic acid (1), ursolic acid (2), β-sitosterol (3), ergosta-4,6,8,22-tetraene-3-one (4), 3β-O-acetyl betulinic acid (5), 3-epideoxyflindissol (6), 3β-O-cis-coumaroyl betulinic acid (7), 3β-O-trans-coumaroyl betulinic acid (8), of which, (6) is for the first time here isolated from a natural product and (4), (7) and (8) are reported for the first time from this genus. In vitro IC 50 values against P. falciparum for (4) (61.0 μM) (6) (128.0 μM), (7) (10.4 μM), (8) (15.3 μM) are reported for the first time. Antileishmanial IC 50 values are reported here for the first time for (4) (11.5 μM), (6) (1.8 μM), (7) (8.3 μM) and (8) (2.2 μM). Cytotoxicity against L6 cells is reported for all compounds. Conclusions: The compounds isolated in this study, while displaying moderate in vitro antiplasmodial activity, do not fully support the historical importance of C. florida as an antimalarial remedy in North America. The traditional remedy may exert its well documented effects by mechanisms unrelated to direct antiplasmodial action. While not traditionally used to treat Leishmania, this work shows that several constituents of C. florida possess promising in vitro antileishmanial activity.
AB - Aim of the study: The objective of this study was to identify the antiplasmodial constituents from the bark of Cornus florida L., a plant traditionally used in North America for the treatment of malaria. Methods and materials: Dried and powdered bark was extracted with 95% ethanol. The resultant extract was subjected to in vitro antiplasmodial-guided fractionation against Plasmodium falciparum (D10 strain). Antiplasmodial IC 50 values were calculated for pure compounds. Compounds were also assayed against Leishmania tarentolae, and rat skeletal myoblast L6 cells to assess antileishmanial activity and cytotoxicity, respectively. Results: Antiplasmodial-guided fractionation afforded 8 compounds: betulinic acid (1), ursolic acid (2), β-sitosterol (3), ergosta-4,6,8,22-tetraene-3-one (4), 3β-O-acetyl betulinic acid (5), 3-epideoxyflindissol (6), 3β-O-cis-coumaroyl betulinic acid (7), 3β-O-trans-coumaroyl betulinic acid (8), of which, (6) is for the first time here isolated from a natural product and (4), (7) and (8) are reported for the first time from this genus. In vitro IC 50 values against P. falciparum for (4) (61.0 μM) (6) (128.0 μM), (7) (10.4 μM), (8) (15.3 μM) are reported for the first time. Antileishmanial IC 50 values are reported here for the first time for (4) (11.5 μM), (6) (1.8 μM), (7) (8.3 μM) and (8) (2.2 μM). Cytotoxicity against L6 cells is reported for all compounds. Conclusions: The compounds isolated in this study, while displaying moderate in vitro antiplasmodial activity, do not fully support the historical importance of C. florida as an antimalarial remedy in North America. The traditional remedy may exert its well documented effects by mechanisms unrelated to direct antiplasmodial action. While not traditionally used to treat Leishmania, this work shows that several constituents of C. florida possess promising in vitro antileishmanial activity.
KW - Antileishmanial
KW - Antiplasmodial
KW - Betulinic acid
KW - Cornus
KW - Cytotoxicity
KW - Malaria
KW - Triterpene
UR - https://www.scopus.com/pages/publications/84862853930
U2 - 10.1016/j.jep.2012.05.017
DO - 10.1016/j.jep.2012.05.017
M3 - Artículo
C2 - 22609155
AN - SCOPUS:84862853930
SN - 0378-8741
VL - 142
SP - 456
EP - 461
JO - Journal of Ethnopharmacology
JF - Journal of Ethnopharmacology
IS - 2
ER -
SDG 3 Good Health and Well-being