Abstract:Introduction: This research main goal is to study the antiplasmodial activity of Macaranga gigantea leaf ethanolic extract and its major components on malaria parasites using ex vivo model. Methods: This study was conducted by extraction of M. gigantea leaves using ethanol and isolation of its major constituent. The extract and isolate were tested ex vivo on Balb-C mice's blood after i.p. administration of Plasmodium berghei strain ANKA. Antiplasmodial activity was observed from mice blood treated by various c… Show more
“…Amiri and collaborators [ 42 ] also demonstrated that apigenin significantly suppressed P. berghei parasiteamia by 69.74, 50.3, and 49.23% at concentrations of 70, 35 and 15 mg/kg/day, respectively in a murine malaria model. Muhaimin and collaborators [ 43 ] identified apigenin as major constituent in the ethanolic extract of Macaranga gigantea (Rchb. f. & Zoll.)…”
Background
Endodesmia calophylloides and Hymenostegia afzelii belong to the Guttiferae and Caesalpiniaceae plant families with known uses in African ethno-medicine to treat malaria and several other diseases. This study aimed at identifying antiplasmodial natural products from selected crude extracts from H. afzelii and E. calophylloides and to assess their cytotoxicity.
Methods
The extracts from H. afzelii and E. calophylloides were subjected to bioassay-guided fractionation to identify antiplasmodial compounds. The hydroethanol and methanol stem bark crude extracts, fractions and isolated compounds were assessed for antiplasmodial activity against the chloroquine-sensitive 3D7 and multi-drug resistant Dd2 strains of Plasmodium falciparum using the SYBR green I fluorescence-based microdilution assay. Cytotoxicity of active extracts, fractions and compounds was determined on African green monkey normal kidney Vero and murine macrophage Raw 264.7 cell lines using the Resazurin-based viability assay.
Results
The hydroethanolic extract of H. afzelii stem bark (HasbHE) and the methanolic extract of E. calophylloides stem bark (EcsbM) exhibited the highest potency against both Pf3D7 (EC50 values of 3.32 ± 0.15 μg/mL and 7.40 ± 0.19 μg/mL, respectively) and PfDd2 (EC50 of 3.08 ± 0.21 μg/mL and 7.48 ± 0.07 μg/mL, respectively) strains. Both extracts showed high selectivity toward Plasmodium parasites (SI > 13). The biological activity-guided fractionation led to the identification of five compounds (Compounds 1–5) from HasbHE and one compound (Compound 6) from EcsbM. Of these, Compound 1 corresponding to apigenin (EC50Pf3D7, of 19.01 ± 0.72 μM and EC50PfDd2 of 16.39 ± 0.52 μM), and Compound 6 corresponding to 3,3′-O-dimethylellagic acid (EC50Pf3D7 of 4.27 ± 0.05 μM and EC50PfDd2 of 1.36 ± 0.47 μM) displayed the highest antiplasmodial activities. Interestingly, both compounds exhibited negligible cytotoxicity against both Vero and Raw 264.7 cell lines with selectivity indices greater than 9.
Conclusions
This study led to the identification of two potent antiplasmodial natural compounds, 3,3′-O-dimethylellagic acid and apigenin that could serve as starting points for further antimalarial drug discovery.
“…Amiri and collaborators [ 42 ] also demonstrated that apigenin significantly suppressed P. berghei parasiteamia by 69.74, 50.3, and 49.23% at concentrations of 70, 35 and 15 mg/kg/day, respectively in a murine malaria model. Muhaimin and collaborators [ 43 ] identified apigenin as major constituent in the ethanolic extract of Macaranga gigantea (Rchb. f. & Zoll.)…”
Background
Endodesmia calophylloides and Hymenostegia afzelii belong to the Guttiferae and Caesalpiniaceae plant families with known uses in African ethno-medicine to treat malaria and several other diseases. This study aimed at identifying antiplasmodial natural products from selected crude extracts from H. afzelii and E. calophylloides and to assess their cytotoxicity.
Methods
The extracts from H. afzelii and E. calophylloides were subjected to bioassay-guided fractionation to identify antiplasmodial compounds. The hydroethanol and methanol stem bark crude extracts, fractions and isolated compounds were assessed for antiplasmodial activity against the chloroquine-sensitive 3D7 and multi-drug resistant Dd2 strains of Plasmodium falciparum using the SYBR green I fluorescence-based microdilution assay. Cytotoxicity of active extracts, fractions and compounds was determined on African green monkey normal kidney Vero and murine macrophage Raw 264.7 cell lines using the Resazurin-based viability assay.
Results
The hydroethanolic extract of H. afzelii stem bark (HasbHE) and the methanolic extract of E. calophylloides stem bark (EcsbM) exhibited the highest potency against both Pf3D7 (EC50 values of 3.32 ± 0.15 μg/mL and 7.40 ± 0.19 μg/mL, respectively) and PfDd2 (EC50 of 3.08 ± 0.21 μg/mL and 7.48 ± 0.07 μg/mL, respectively) strains. Both extracts showed high selectivity toward Plasmodium parasites (SI > 13). The biological activity-guided fractionation led to the identification of five compounds (Compounds 1–5) from HasbHE and one compound (Compound 6) from EcsbM. Of these, Compound 1 corresponding to apigenin (EC50Pf3D7, of 19.01 ± 0.72 μM and EC50PfDd2 of 16.39 ± 0.52 μM), and Compound 6 corresponding to 3,3′-O-dimethylellagic acid (EC50Pf3D7 of 4.27 ± 0.05 μM and EC50PfDd2 of 1.36 ± 0.47 μM) displayed the highest antiplasmodial activities. Interestingly, both compounds exhibited negligible cytotoxicity against both Vero and Raw 264.7 cell lines with selectivity indices greater than 9.
Conclusions
This study led to the identification of two potent antiplasmodial natural compounds, 3,3′-O-dimethylellagic acid and apigenin that could serve as starting points for further antimalarial drug discovery.
“…Several secondary metabolites from plants such as alkaloids, flavonoids, and triterpenoids have been reported to have antimalarial activity [31][32][33]. Terpenoids have an important role as antimalarial agents by inhibiting the Plasmodium parasites' growth from ring forms to trophozoites, and can inhibit nutrient uptake by inhibiting the permeation pathway [34,35]. Some antimalarial terpenoids isolated from other Euphorbiaceae plants have been reported, such as betulinic acid from Uapaca nitida Müll-Arg [36]; 8, 9secokaurane diterpenes from Croton kongensis Gagnep [37]; geranylgeraniol from Croton lobatus L. [38]; poly-O-acylated jatrophane diterpenes from Pedilanthus tithymaloides (L.) Poit [39]; steenkrotin A from Croton steenkampianus Gerstner [40]; 2α-hydroxyjatropholone from Jatropha integerrima Jacq [41]; jatrophone diterpenes from Jatropha isabelli Müll.…”
Sauropus androgynus (L.) Merr., in the Indonesian local name known as “Katuk,” is a tropical shrub plant of the family Euphorbiaceae. Based on genus and chemotaxonomic approaches, as well as in vitro testing of Plasmodium falciparum, leaves of S. androgynus are presumed to have an active compound content as an antimalarial. The current study aims to investigate the antimalarial activity of 96% ethanol extract and fractions of S. androgynus leaves. The ethanolic extract was fractionated using the vacuum liquid chromatography (VLC) method with three solvents of different polarities (n-hexane, chloroform, and 96% ethanol). The fraction obtained was then evaluated for antimalarial activity against P. falciparum 3D7 strain. The ethanolic extract was evaluated for antimalarial suppressive and prophylactic activity against P. berghei-infected mice, as well as inhibitory activity against the heme detoxification process in vitro. Fractionation of ethanolic extract resulted in seven combined fractions, with the most active fraction being FV (50% inhibitory concentration (IC50) = 2.042 µg/mL). The ethanolic extract showed good parasitic suppressive (therapeutic) activity with a median effective dose (ED50) value of 15.35 mg/kg body weight. In a prophylactic test, ethanolic extract showed parasite growth inhibitory activity of 67.74 ± 9.21% after the administration of 400 mg/kg body weight for 4 days before infection, and 65.30 ± 10.44% after the administration of 200 mg/kg body weight for 8 consecutive days (4 days before and after infection). The ethanolic extract also showed an effect in inhibiting the formation of β-hematin of about 26.87–79.36% at a concentration of 0.1–4 mg/mL and an IC50 value of 0.479 mg/mL. The S. androgynus leaves were shown to have antimalarial activity in vitro and in vivo, where ethanolic extract were more active compared with the fraction obtained. The antimalarial properties of the extract showed a higher suppressive activity than prophylactic activity.
“…[15][16][17][18][19][20] The plant is also known to have active phytochemicals constituents, especially on its leaves. 7,21 Solvent evaporation method has been widely and extensively used to prepare polymeric microparticles containing different drugs and in the development of modified release systems. 22,23 It is a rapid process that does not involve severe heat treatment; therefore, it is a suitable method to preserve biological products, including temperature sensitive products, without their degradation; it also allows for storage at room temperature.…”
Macaranga is a genus of the family Euphorbiaceae which comprises of about three hundred species. It is present in some parts of the world which include Indonesia, some parts of Africa, Madagascar, Asia, the east coast of Australia and the Pacific islands. 7-15 The Macaranga gigantea plants are known to be in the form of shrubs or trees and grow in places with optimum sunlight, secondary forests or forests that have been destroyed. Macaranga gigantea plants show several bioactivity which include antitumor, anticancer, antimalaria, antimicrobes, ABSTRACT Introduction: The aim of this research was to formulate the microcapsules of Macaranga gigantea leaves extract with solvent evaporation method using Ethocel 10 cP and Eudragit E100 as matrix. Methods: M. gigantea leaves were extracted using ethanol 96%. This extract was dried by rotary evaporator. The microencapsulation process of M. gigantea leaves extract was conducted by solvent evaporation method (O/W: oil in water). The formula of M. gigantea leaves extract microcapsules were designed into six formulas (Eudragit E100: FA 1 , FA 2 , FA 3 and Ethocel 10 cP: FB 1 , FB 2 , FB 3). Microcapsules of M. gigantea leaves extract were characterized for particle size, in terms of surface morphology by scanning electron microscope (SEM) and encapsulation efficiency. Antioxidant activity of the formulation have been evaluated by DPPH method. Physical characterization on microparticles were performed by conducting entrapment efficiency and SEM picture. Results: In this research, the micoparticles containing M. gigantea extract has been developed by using ethyl cellulose (Ethocel 10 cP) and eudragit (Eudragit E100) as polymer matrix. The results showed that high concentration of polymer (Ethocel 10 cP and Eudragit E100) used in microencapsulation resulted in better M. gigantea leaves extract microcapsules in terms of physical characteristics. Particle size of microcapsules containing M. gigantea leaves extract were in the range of 3.564 to 5.887 μm. Encapsulation efficiency (% EE) was categorized as good because the value were ≥ 80% to which 85.978% (FA 3) and 88.992% (FB 3). SEM picture of FA 3 (Eudragit E100) revealed that the surface of microcapsule were rough and porous. When Ethocel 10 cP used as polymer, a smoother surface and less visible pores of microcapsule were obtained. The antioxidant ability of M. gigantea leaves extract microcapsule showed that IC 50 values was 64.51 ppm. Conclusion: It can be concluded that microcapsules of M. gigantea leaves extract can be prepared by solvent evaporation method by using Eudragit E100 and Ethocel 10 cP as polymer matrix. M. gigantea leaves has potent antioxidant activity either as extract or after formulated into microcapsules.
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