Plants as Sources of Antimalarial Drugs, Part 4: Activity of Brucea javanica Fruits Against Chloroquine-Resistant Plasmodium falciparum in vitro and Against Plasmodium berghei in vivo

Abstract

Extracts of Brucea javanica fruit have been prepared and monitored for their in vitro and in vivo antiplasmodial activities. The antimalarial activity of the fruit was found to be attributable to its quassinoid constituents. Nine of the quassinoids possessed in vitro IC50 values between 0.046-0.0008 microgram/ml against the chloroquine resistant Plasmodium falciparum strain (Kl) tested. The two quassinoid glycosides tested were considerably less active in vitro than the aglycones. Four quassinoids were found to possess activity in vivo against Plasmodium berghei infections in mice after oral dosing. All five quassinoids tested in vivo showed some toxicity.

Use of microdilution to assess in vitro antiamoebic activities of Brucea javanica fruits, Simarouba amara stem, and a number of quassinoids

“…These quassinoids were highly active against amoebae and account for the high potency of the chloroform extract ( Table 2). The polar fractions 3, 5, and 6 are devoid of the quassinoids listed above, but they do contain other more polar quassinoids, including quassinoid glycosides (9). One of the nonglycosides from the polar fractions, bruceine D, had antiamoebic activity comparable to that of bruceines B and C, whereas the glucoside, yadanzioside F, was much less active.…”

“…Similarly, the chloroform extract of S. amara was highly active, but the activity of fractions 5 and 6 favored fraction 5, the butanol phase. When the extraction procedure described above is followed, the major quassinoid constituents present in these species are concentrated in the chloroform extract (9). B. javanica contains the quassinoids bruceines A, B, and C, which pass into the chloroform extract together with the minor constituent, bruceantin.…”

“…Quassinoids of both types are potent antiamoebic agents, and both types have antimalarial (10) and antileukemic (2) activities. The antiamoebic activities of the compounds are shown in Table 2, and for comparison their in vitro antimalarial activities against a multidrug-resistant strain (Ki) of Plasmodium falciparum (5,(9)(10)(11) are also given.…”

“…These Glaucarubinone, 2'-acetylglaucarubinone, ailanthinone, and holacanthone were available from previous extractions of S. amara fruits (11). All quassinoids have been identified previously by their spectroscopic characteristics (9,11).…”

Study of Antiparasitic and Cytotoxicity of the Aqueous, the 80% Methanol Extract and Its Fractions, and the Acute Toxicity of the Aqueous Extract of <i>Brucea sumatrana</i> (Simaroubaceae) Leaves Collected in Mai-Ndombe, Democratic Republic of Congo

“…Several phytomolecules in the tested samples including flavonoids, alkaloids, steroids, terpenes and phenolic compounds isolated from other medicinal plants have been previously reported as potent antiprotozoal agents [41]- [50]. The presence these secondary metabolites identified in the studied plant extracts and fractions may be contributed to the observed antiprotozoal activity, particularly, different terpenes belonging to the quassinoids groups mainly isolated from the seeds of B. javanica growing in Asian regions are known as active principles for various evaluated biological activities already men-tioned above [1]- [10]. However, the observed antiprotozoal activity of the aqueous and 80% methanol extracts of B. sumatrana leaves might be attributed to either the individual class of compounds present in respective extract or to the synergistic action that each class of compounds exert to give the observed biological activity as also previously reported by [51].…”