Abstract

An antiplasmodial activity-guided isolation was carried out on the dichloromethane extract of Tithonia diversifolia dried leaves. A total of five germacranolide type sesquiterpene lactones and a new flavonol, 3,6-dihydroxy-2-(4′-hydroxyphenyl)-7-methoxy-4H-chromen-4-one, were isolated. The flavonol reported an IC50 above 6.00 µM against the chloroquine sensitive strain, NF54. The antimalarial activity of the Tithonia diversifolia dichloromethane leaf extract was attributed to orizabin and tagitinin C.

Highlights

  • An ethnobotanical survey indicated that Tithonia diversifolia is used as one of the traditional antimalarial remedies in Zimbabwe [1]

  • Phytochemical studies revealed that T. diversifolia contains large amounts of sesquiterpene lactones, which constitute up to 3% dry weight of some Asteraceae species, e.g., Helenium amarum [11], flavonoids, diterpenoids [12,13], chromene, and flavones [14], among other minority compounds

  • Antiplasmodial activity of DCM crude extract of T. diversifolia leaves is mainly due to orizabin and tagitinin C

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Summary

Introduction

An ethnobotanical survey indicated that Tithonia diversifolia is used as one of the traditional antimalarial remedies in Zimbabwe [1]. Phytochemical studies revealed that T. diversifolia contains large amounts of sesquiterpene lactones, which constitute up to 3% dry weight of some Asteraceae species, e.g., Helenium amarum [11], flavonoids, diterpenoids [12,13], chromene, and flavones [14], among other minority compounds. These phytochemicals are most significantly concentrated in the leaves, followed by the roots and lowest in the stems [15,16]. Flavonoids consist of a large group of polyphenolic compounds having a benzo-γpyrone structure, most commonly known as the C6-C3-C6 skeleton They are synthesized by the phenyl propanoid pathway [17]. AAwweebb-b-basaesdedsesaerachrchretrreietrvieedvendo nmoamtchaitncghirnegsproensspeosnfsoersthfoerfltahveofnloalv.onItos ls.cIitesns- cientifi tnifiacmneamcoeuclodubldebdeeddeudcuecdedasas77-m-meetthhooxxyy--33,,44′,,66--ttrrihihyyddrorxoyxflyafvlaovnoenoer 3o,r6-3d,i6h-yddihroyxdyr-o2-x(y4--2-(4-hy hdyrdorxoyxpyhpehnenyyl)l-)7-7--mmeetthhooxxyy--44HH--cchhrorommene-n4--4o-noen. e

Materials and Methods
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