<i>In Vitro</i> Antiprotozoal and Cytotoxic Activity of the Aqueous Extract, the 80% Methanol Extract and Its Fractions from the Seeds of <i>Brucea sumatrana</i> Roxb. (Simaroubaceae) Growing in Democratic Republic of Congo

Abstract

The <i>in vitro</i> antiprotozoal and cytotoxic activity of the aqueous extract, the 80% methanol extract, and its different soluble fractions and subfractions from <i>Brucea sumatrana</i> seeds were assessed against two Trypanosoma (<i>T. cruzi</i> and <i>T. brucei brucei</i>), <i>Leishmania infantum</i> and chloroquine and pyrimethanine-resistant K1strain of <i>P. falciparum</i> and against MRC-5 cell-lines respectively. Results indicated that the 80% methanol extract showed a cytotoxic effect against MRC-5 cell lines with CC<sub>50</sub> value of 0.54 µg/ml. It however exhibited pronounced and non selective activity against <i>T. cruzi</i> (IC<sub>50</sub> = 1.52 µg/ml, SI = 0.03) and <i><i>L. infantum</i></i> (IC<sub>50</sub> = 2.41 µg/ml, SI = 0.22). It however displayed pronounced and selective effect against T. brucei brucei (IC<sub>50</sub> < 0.25, SI > 2.16) and chloroquine and pyrimethamine-resistant K1 strain of <i>P. falciparum</i> (IC<sub>50</sub> < 0.25 µg/ml, SI > 2.16). All soluble fractions and subfractions from the partition of the 80% methanol extract were found to exhibit an antiprotozoal activity with IC<sub>50</sub> values ranging from <0.25 to 30 µg/ml. The most active was the alkaline aqueous soluble fraction exhibiting pronounced antiprotozoal activity against <i>T .cruzi</i>, <i>T. b. brucei</i>, <i>L. infantum</i> and chloroquine and pyrimethamine-resistant K1 strain of <i>P. falciparum</i> with IC<sub>50</sub> values of 0.33, <0.25, 0.25, <0.25 µg/ml respectively resulting in high selective index values of 61.36, > 81, 81 and >81 respectively. The chloroform soluble fraction rich in alkaloid was cytotoxic against MRC-5 cell lines (CC<sub>50</sub> = 27.09 µg/ml) and showed good activity against T. b. brucei (IC<sub>50</sub> = 8.36 and SI = 3.24) and moderate activity against <i>T. cruzi</i>, <i>L. infantum</i> and chloroquine-pyrimethane-resistant K1 strain of <i>P. falciparum</i> (20 < IC<sub>50</sub> < 30 µg/ml). Although the aqueous extract (decoction) and the total alkaloids extract showed a cytotoxic effect against MRC-5 cell lines (CC<sub>50</sub> = 1.55 and 0.43 µg/ml respectively), they however displayed pronounced antiprotozoal activity against <i>T. cruzi</i>, T. b. brucei and chloroquine and pyrimethamine-resistant K1 strain of <i>P. falciparum</i> with IC<sub>50</sub> values ranging from < 0.25 to 0.6 µg/ml with only a selective action against chloroquine and pyrimethamine-resistant K1 strain of <i>P. falciparum</i> (SI = >6.2 and >1.72 respectively). These extracts however showed good and low activity respectively against <i>L. infantum</i> (IC...

In vitro Anti-Leishmanial Activities of Methanol Extract of Brucea antidysenterica J.F. Mill Seeds and Its Solvent Fractions

“…The level of in vitro activities of the reference drugs, crude extract and its solvent fractions were appreciated based on the following criteria: IC 50 ≤ 5 μg/mL pronounced activity; 5 < IC 50 ≤ 20 μg/mL good activity; 20 < IC 50 ≤ 30 μg/mL moderate activity; 30 < IC 50 ≤ 64 μg/mL low activity; and IC 50 > 64 μg/mL inactive. 38 Accordingly, the crude extract, n-hexane fraction and n-butanol fraction possessed moderate, good and low anti-promastigote activity, respectively, against both L. aethiopica and L. donovani isolates. The ethyl acetate fraction demonstrated good anti-leishmanial activity against L. aethiopica and pronounced activity against L. donovani, while aqueous fraction was found to be inactive against both L. donovani and L. aethiopica promastigotes (Table 1).…”

Anti-plasmodial effect of plant extracts from Picrolemma huberi and Picramnia latifolia

“…Numerous compounds have been isolated from this family, such as quassinoids, alkaloids, triterpenes, steroids, coumarins, anthraquinones, flavonoids and other metabolites [ 55 – 58 ]. Most of the studies reported for the Simaroubaceae family show antiplasmodial activity for the quassinoids extracted from these plants [ 35 , 38 – 40 , 42 , 44 ], with characteristics of highly active compounds [ 20 ]. Quassinoids such as isobrucein B and sergolides isolated from P. huberi extracts have only been evaluated in a melanoma cell line, and in colon and lung cell lines, with sergolide having a higher cytotoxicity CC 50 in a range of 10 −7 –10 −8 M [ 45 ].…”

Simaroubaceae family: botany, chemical composition and biological activities

“…Species of the genus Ailanthus display antiasthmatic and antiallergenic activities ; hypotensive activity, mediated by Angiotensin Conversion Enzyme (ACE) inhibition by flavonoids (Loizzo et al, 2007); and, in the genus Castela, plant growth inhibitory activity (Lin et al, 1995). Species from Brucea genus have been shown to have antiprotozoal activity, against two Trypanosoma species (T. cruzi and T.brucei) and Leishmania infantum (Ehata et al, 2012), and quassinoids have been attributed to hypoglycemic activity (Noorshahida et al, 2009).…”

“…Anti asthmatic Anti allergenic Kumar et al, 2011 Cytotoxic (carcinoma and mammary adeno-carcinoma, melanoma and prostate cancer) Lavhale et al, 2009 Hypotensor: Angiotensin conversion enzyme inhibition Loizzo et al, 2007 Anti plasmodial Okunade et al, 2003 Brucea Cytotoxic Antiprotozoa (against Trypanossoma cruzi and T. brucei, Leishmania infantum, Plasmodium falciparum) Ehata et al, 2012Hypoglycaemic Noorshahida et al, 2009 Antiprotozoa (Trypanossoma evansi) Bawn et al, 2008 Eurycoma Increase in spermatogenesis and fertility Low et al, 2013 Picrolemma Anthelmintic Nunomura et al, 2006 Larvacide (against Aedes aegypti) Antimalarial (against P. falciparum) Silva et al, 2009a Quassia Antimalarial (Plasmodium berghei, Plasmodium falciparum resistant to chloroquine) Ajaiyeoba et al, 1999Bertani et al, 2006Cachet et al, 2009 Antiulcerogenic García-Barrantes and Badilla, 2011 Toma et al, 2002Antidiabetic Hussain et al, 2011Antifertilizer Raji and Bolarinwa, 1997 Sedating and anticonceptive Toma et al, 2003 Cytotoxic (against lymphocytic leukaemia, human nasopharynx carcinoma and human mammary adenocarcinoma) Kupchan andStreelman, 1976 Houël et al, 2009 Antifeeding (Bemisia, tabaci and Hypsipyla grandella) Flores et al, 2008Mancebo et al, 2000 Insecticide ( Chart 2 Biological activities of the main genera of Simaroubaceae family.…”