Antiplasmodial activity-aided isolation and identification of quercetin-4’-methyl ether in Chromolaena odorata leaf fraction with high activity against chloroquine-resistant Plasmodium falciparum

Abstract

The present study was undertaken to evaluate the antiplasmodial activity of Chromolaena odorata leaf extract and gradient fractions through in vivo and in vitro tests, aimed at identifying its antiplasmodial constituents. Sub-fractions obtained from the most active gradient fraction were further tested for cytotoxicity against THP-1 cells, chloroquine-sensitive (HB3) and chloroquine-resistant (FCM29) Plasmodium falciparum. Our results showed the dichloromethane gradient fraction was most effective, significantly (P < 0.05) suppressing infection by 99.46% at 100 mg/kg body weight. Amongst its 13 sub-fractions (DF1-DF13), DF11 was highly active, with IC50 of 4.8 and 6.74 μg/ml against P. falciparum HB3 and FCM29, respectively. Cytotoxicity of DF11 was estimated to be above 50 μg/ml, and its separation by column chromatography yielded a flavonoid which was characterized as 3, 5, 7, 3' tetrahydroxy-4'-methoxyflavone from its spectroscopic data. It significantly suppressed infection (65.43-81.48%) in mice at 2.5-5 mg/kg doses and compared favourably with the effects of chloroquine and artemisinin. It may therefore serve as a useful phytochemical and antiplasmodial activity marker of C. odorata leaves, which exhibit potential for development as medicine against malaria.

Antimalarial Activity of the n-Butanol Fraction of Uapaca togoensis (Pax) Stem Bark in Mice

“…41 Saponins, flavonoids and tannins have been suggested to act as primary antioxidant or free radicals scavengers that can counteract the oxidative damage induced by the malaria parasite. 42 The antimalarial activities of the n-butanol fraction observed in this study may therefore have been due to the presence of these phytochemicals exerting their activity through one or both of these mechanisms, or may be even through a yet to be identified mechanism. The chemosuppression produced by the n-butanol fraction of Uapaca togoensis in the current study was in agreement with other studies which reported that the nbutanol fraction of medicinal plants like Asparagus africanus 43 and Dodonaea angustifolia 38 possesses significant antimalarial activity compared to the other fractions studied.…”

“…21 This difference in antimalarial activity may be linked to the fact that the ethyl acetate fraction was devoid of saponins and tannins and studies have reported these phytochemicals to possess antimalarial activity. 42 Research on medicinal plants contributed to the isolation of compounds with potent antimalarial activity including artemisinin and quinine. Thus the isolation of compounds from the n-butanol fraction of U. togoensis is desirable as this may lead to the discovery of lead compounds which could be further adjusted by semi-synthetic approaches to obtain effective antimalarial agents.…”

The protective effect of Moringa oleifera leaf extract on liver damage in mice infected with Plasmodium berghei ANKA

“…Terpenoids, flavonoids, saponin, alkaloids, quercetin and kaempferol were known to have antimalarial activity and antioxidant activity which might also play antimalarial activity [24,25]. It has been reported and suggested that quercetin and kaempferol presented antimalarial activity against in vitro culture of Plasmodium falciparum and P. berghei infected mice [26,27]. In addition, antimalarial activity of these compounds was found evidently on the ring stage of the malaria parasite [28].…”

Wound healing property review of siam weed, Chromolaena odorata

“…[23] Its active phytochemical substances are as follows: (1) flavonoid aglycones (flavanones, flavonols, flavones) including acacetin, chalcones, eupatilin, luteolin, naringenin, kaempferol, quercetin, quercetagetin, and sinensetin;[2425262728293031] (2) terpenes and terpenoids;[32] (3) essential oils;[333435363738] (4) alkaloids including pyrrolizidine;[394041] (5) saponins and tannins;[23] (6) phenolic acids including ferulic acid, protocatechuic acid;[42] (7) phytoprostane compound including chromomoric acid. [43]…”

“…From review literature regarding the traditional uses, phytochemical properties of C. odorata are anti-bacterial,[27444344454647] anticancer,[2148] anticonvulsant,[49] antidiabetic,[505152] anti-diarrheal,[5354] anti-fungal,[5556] anti-inflammatory,[575859] antioxidant,[606162636465] and antiparasitic,[3040] hemostatic and wound healing,[1522236669] and hepatoprotective activities. [7071]…”