The in vitro antiprotozoal and cytotoxic activity of the aqueous extract, the 80% methanol extract, and its different soluble fractions and subfractions from Brucea sumatrana seeds were assessed against two Trypanosom...The in vitro antiprotozoal and cytotoxic activity of the aqueous extract, the 80% methanol extract, and its different soluble fractions and subfractions from Brucea sumatrana seeds were assessed against two Trypanosoma (T. cruzi and T. brucei brucei), Leishmania infantum and chloroquine and pyrimethanine-resistant K1strain of P. falciparum and against MRC-5 cell-lines respectively. Results indicated that the 80% methanol extract showed a cytotoxic effect against MRC-5 cell lines with CC50 value of 0.54 μg/ml. It however exhibited pronounced and non selective activity against T. cruzi (IC50 = 1.52 μg/ml, SI = 0.03) and L. infantum (IC50 = 2.41 μg/ml, SI = 0.22). It however displayed pronounced and selective effect against T. brucei brucei (IC50 2.16) and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum (IC50 2.16). All soluble fractions and subfractions from the partition of the 80% methanol extract were found to exhibit an antiprotozoal activity with IC50 values ranging from T .cruzi, T. b. brucei, L. infantum and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values of 0.33, 81, 81 and >81 respectively. The chloroform soluble fraction rich in alkaloid was cytotoxic against MRC-5 cell lines (CC50 = 27.09 μg/ml) and showed good activity against T. b. brucei (IC50 = 8.36 and SI = 3.24) and moderate activity against T. cruzi, L. infantum and chloroquine-pyrimethane-resistant K1 strain of P. falciparum (20 50 50 = 1.55 and 0.43 μg/ml respectively), they however displayed pronounced antiprotozoal activity against T. cruzi, T. b. brucei and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values ranging from P. falciparum (SI = >6.2 and >1.72 respectively). These extracts however showed good and low activity respectively against L. infantum (IC50 = 24.05 and 6.82 μg/ml respectively).展开更多
Objective:To investigate the leishmanicidal effect of the Bixa orellana crude seed extract and its fractions against Leishmania amazonensis.Methods:Four main fractions(BO-A,BO-B,BO-C and BO-D)were obtained by exhausti...Objective:To investigate the leishmanicidal effect of the Bixa orellana crude seed extract and its fractions against Leishmania amazonensis.Methods:Four main fractions(BO-A,BO-B,BO-C and BO-D)were obtained by exhaustion with solvent with increased polarity from the Bixa orellana crude seed extract and 28 sub-fractions.The antileishmanial activity was evaluated in intracellular amastigotes and the cytotoxicity was assessed in murine intraperitoneal macrophages.Results:The BO-A and BO-B fractions showed a good antileishmanial activity with IC50 values of(12.9±4.1)and(12.4±0.3)μg/mL,respectively.The sub-fractions BO-B1(IC_(50)=(11.8±3.8)μg/mL)and BO-B3[IC_(50)=(13.6±4.7)μg/mL]also proved to have a good leishmanicidal effect.In general,the sub-fractions showed a lower toxicity than the crude extract.A selectivity index of 9 indicated a moderate selectivity of the BO-A,BO-B and BO-C fractions and BO-B1 sub-fraction.Conclusions:Potential of this plant against cutaneous leishmaniasis should be further investigated.展开更多
文摘The in vitro antiprotozoal and cytotoxic activity of the aqueous extract, the 80% methanol extract, and its different soluble fractions and subfractions from Brucea sumatrana seeds were assessed against two Trypanosoma (T. cruzi and T. brucei brucei), Leishmania infantum and chloroquine and pyrimethanine-resistant K1strain of P. falciparum and against MRC-5 cell-lines respectively. Results indicated that the 80% methanol extract showed a cytotoxic effect against MRC-5 cell lines with CC50 value of 0.54 μg/ml. It however exhibited pronounced and non selective activity against T. cruzi (IC50 = 1.52 μg/ml, SI = 0.03) and L. infantum (IC50 = 2.41 μg/ml, SI = 0.22). It however displayed pronounced and selective effect against T. brucei brucei (IC50 2.16) and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum (IC50 2.16). All soluble fractions and subfractions from the partition of the 80% methanol extract were found to exhibit an antiprotozoal activity with IC50 values ranging from T .cruzi, T. b. brucei, L. infantum and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values of 0.33, 81, 81 and >81 respectively. The chloroform soluble fraction rich in alkaloid was cytotoxic against MRC-5 cell lines (CC50 = 27.09 μg/ml) and showed good activity against T. b. brucei (IC50 = 8.36 and SI = 3.24) and moderate activity against T. cruzi, L. infantum and chloroquine-pyrimethane-resistant K1 strain of P. falciparum (20 50 50 = 1.55 and 0.43 μg/ml respectively), they however displayed pronounced antiprotozoal activity against T. cruzi, T. b. brucei and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values ranging from P. falciparum (SI = >6.2 and >1.72 respectively). These extracts however showed good and low activity respectively against L. infantum (IC50 = 24.05 and 6.82 μg/ml respectively).
基金Supported by the Ministry of Public Health and Ministry of Science,Technology and Enviroment of Cuba(Grant No.1003021/2010).
文摘Objective:To investigate the leishmanicidal effect of the Bixa orellana crude seed extract and its fractions against Leishmania amazonensis.Methods:Four main fractions(BO-A,BO-B,BO-C and BO-D)were obtained by exhaustion with solvent with increased polarity from the Bixa orellana crude seed extract and 28 sub-fractions.The antileishmanial activity was evaluated in intracellular amastigotes and the cytotoxicity was assessed in murine intraperitoneal macrophages.Results:The BO-A and BO-B fractions showed a good antileishmanial activity with IC50 values of(12.9±4.1)and(12.4±0.3)μg/mL,respectively.The sub-fractions BO-B1(IC_(50)=(11.8±3.8)μg/mL)and BO-B3[IC_(50)=(13.6±4.7)μg/mL]also proved to have a good leishmanicidal effect.In general,the sub-fractions showed a lower toxicity than the crude extract.A selectivity index of 9 indicated a moderate selectivity of the BO-A,BO-B and BO-C fractions and BO-B1 sub-fraction.Conclusions:Potential of this plant against cutaneous leishmaniasis should be further investigated.
