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Malaria caused by plasmodium parasite is at the moment the highest killer disease in the tropics, killing mostly pregnant women and children under the age of five years. Efforts are on to developing more potent antimalarials from plants' sources that will be cheaper, without adverse effects, readily available and will be able to replace existing an...
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... extract showed a significant chemosuppression of up to 85.05 % (Table 1) following a 4 day treatment with 800 mg/kg extract compared with the infected untreated group. This chemosuppressive effect was in a dose dependent order. ...
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... In addition, the chloroquine standard drug inhibited P. berghei parasite growth more (P < 0.05) than that of the extracttreated and infected control groups. The lower efficiency of crude extracts might be related to impurities, poor separation, low selectivity, slow-acting absorption, low bioavailability, or other pharmacokinetic and pharmacodynamic parameters [74]. ...
The emergence and spread of antimalarial drug resistance have become a significant problem worldwide. The search for natural products to develop novel antimalarial drugs is challenging. Therefore, this study aimed to assess the antimalarial and toxicological effects of Chan-Ta-Lee-La (CTLL) and Pra-Sa-Chan-Dang (PSCD) formulations and their plant ingredients. The crude extracts of CTLL and PSCD formulations and their plant ingredients were evaluated for in vitro antimalarial activity using Plasmodium lactate dehydrogenase enzyme and toxicity to Vero and HepG2 cells using the tetrazolium salt method. An extract from the CTLL and PSCD formulations exhibiting the highest selectivity index value was selected for further investigation using Peter’s 4-day suppressive test, curative test, prophylactic test, and acute oral toxicity in mice. The phytochemical constituents were characterized using gas chromatography-mass spectrometry (GC-MS). Results showed that ethanolic extracts of CTLL and PSCD formulations possessed high antimalarial activity (half maximal inhibitory concentration = 4.88, and 4.19 g/mL, respectively) with low cytotoxicity. Ethanolic extracts of the CTLL and PSCD formulations demonstrated a significant dose-dependent decrease in parasitemia in mice. The ethanolic CTLL extract showed the greatest suppressive effect after 4 days of suppressive (89.80%) and curative (35.94%) testing at a dose of 600 mg/kg. Moreover, ethanolic PSCD extract showed the highest suppressive effect in the prophylactic test (65.82%) at a dose of 600 mg/kg. There was no acute toxicity in mice treated with ethanolic CTLL and PSCD extracts at 2,000 mg/kg bodyweight. GC-MS analysis revealed that the most abundant compounds in the ethanolic CTLL extract were linderol, isoborneol, eudesmol, linoleic acid, and oleic acid, whereas ethyl 4-methoxycinnamate was the most commonly found compound in the ethanolic PSCD extract, followed by 3-hydroxy-2-(4-hydroxy-3-methoxyphenyl)-4H-chromen-4-one, flamenol, oleic acid amide, linoleic acid, and oleic acid. In conclusions, ethanolic CTLL and PSCD extracts exhibited high antimalarial efficacy in vitro . The ethanolic CTLL extract at a dose of 600 mg/kg exhibited the highest antimalarial activity in the 4-day suppressive and curative tests, whereas the ethanolic PSCD extract at a dose of 600 mg/kg showed the highest antimalarial activity in the prophylactic test.
... This might be due to the low concentration of active phytochemical constituent associated with the unpurified or nature of extract, low selectivity, low absorption, poor bioavailability, and other pharmacodynamics and pharmacokinetics properties of the 80% methanol extract and activity may not be detected in lower doses [19,33] [35]. Moreover, the prolonged survival time of mice treated with 400mg/kg of the 80% methanol extract is a strong indicator of the ability of the extract to reduce the overall pathogenic effect of the parasite [36]. ...
Ethnopharmacological relevance:
Malaria is still a known health threat, especially in parts of sub-Saharan Africa. It is one of the frequently mentioned issues with hospital admission and outpatient care in Ethiopia. Cucumis ficifolius A. Rich roots are historically used in Ethiopia to treat meningitis, inflammation, and malaria. However, the antimalarial activity of this plant has not been scientifically studied so far.
Aim of the study:
This study aimed to determine the in vivo antimalarial activity of 80% methanol extract and solvent fractions of the roots of Cucumis ficifolius against Plasmodium berghei infection in mice.
Methods:
The in vivo antimalarial activity of the 80% methanol extract and solvent fractions of Cucumis ficifolius A. Rich was evaluated by standard chemo suppressive, curative and repository tests using Plasmodium berghei (ANKA strain) in Swiss albino mice at doses of 100, 200 and 400 mg/kg/day. The level of parasitemia, survival time, variation in weight, rectal temperature, and packed cell volume of mice were determined to establish the activity of the extracts.
Result:
The 80% methanol extract of Cucumis ficifolius A. Rich roots had a promising suppression of parasitemia at 400 mg/kg with a chemosuppression value of 65.21 ± 1.20%. Among the solvent fractions, the chloroform fraction showed the highest antimalarial activity in the four-day suppressive test with a chemosuppression value of 55.9 ± 0.28%, followed by the n-butanol (42.9 ± 0.24%), and aqueous (40.57 ± 0.52%) fractions at a dose of 400 mg/kg. The highest survival times were observed with crude extract (15.4 ± 0.24 days) at 400 mg/kg, and chloroform fraction (13.4 + 0.24 days), though all extracts increased survival time.
Conclusion:
The findings of the present study collectively indicate the root extract of Cucumis ficifolius has a promising antiplasmodial activity which substantiates the traditional claim of the plant.
... Untreated control group received only vehicle (10% DMSO solution). Chloroquine (standard) was used as positive control at the dose of 5 mg/kg for 4 days [52]. Thin smear for each animal was prepared, fixed with methanol and then strained with giemsa. ...
A novel series of pyrazolyl chalcones containing quinoline scaffold, 5 a-v has been synthesized by Claisen Schimdt condensation of aromatic acetophenone with 1-(4-methylquinolin-2-yl)-3-aryl-1H-pyrazole-4-carbaldehyde in quantitative yield. The compounds were characterized using IR, NMR, MS and elemental analysis. An E-configuration about CC ethylenic bond was determined using 1H NMR spectroscopy. These compounds exhibited significant antimalarial potential against CQ-sensitive and CQ-resistant strain of Plasmodium falciparum. Structure activity relationship has also been established based on outcomes of in vitro schizont inhibition assay. Compound 5u, (Z)-3-(1-(4-methylquinolin-2-yl)-3-p-tolyl-1H-pyrazol-4-yl)-1-p-tolylprop-2-en-1-one, was found to be the most potent among the series of synthetic analogues. In vivo, it demonstrated significant parasitemia suppression of 78.01% at a dose of 200mg/kg against P. berghei in infected mice without any mortality in 7 days. In silico molecular docking study revealed that this compound 5u bound to the active site of cysteine protease falcipain-2 enzyme. Furthermore, in silico ADME studies, were also performed and physicochemical qualifications of the title compounds were determined. The biological outcomes of newer heterocyclic compounds may pave the new paths for researchers in development of potential antimalarial agents.
... This finding agrees with other studies in which the percentage of parasitemia in the suppressive and curative tests was lower than in the prophylactic test [24]. In general, the models showed a dose-dependent decrease in parasitemia levels as observed in the reports of Unekwuojo et al. [25], Muluye et al. [26], Habte et al. [27], and Orabueze et al. [28]. ...
... (Makinde, Obih, 1985;Oko et al., 2012;Unekwuojo, Omale, Aminu, 2011;Umar et al., 2013;Memvanga et al., 2015;Adebayo, Adewole, Krettli, 2017). The leaves of Morinda lucida are frequently used in the Congolese traditional medicine for the treatment of malaria and febrile diseases. ...
Morinda lucida leaves are largely used by Congolese traditional healers for the treatment of uncomplicated malaria. The antimalarial activity of their ethanolic extract has been confirmed both in vitro and in vivo. However, the development of relevant formulations for potential
clinical application is hampered since the active ingredients contained in this extract exhibit
poor water solubility and low oral bioavailability. Hence, this work aims not only to develop
self-nanoemulsifying drug delivery systems (SNEDDSs) for oral delivery of the ethanolic
extract of Morinda lucida (ML) but also to evaluate its oral antimalarial activity alone and in
combination with other Congolese ethanolic plant extracts (Alstonia congensis, Garcinia kola,
Lantana camara, Morinda morindoides or Newbouldia laevis). Based on the solubility of these
different extracts in various excipients, SNEDDS preconcentrates were prepared, and 200 mg/g
of each plant extract were suspended in these formulations. The 4-day suppressive Peter’s test
revealed a significant parasite growth inhibiting effect for all the extract-based SNEDDS (from
55.0 to 82.4 %) at 200 mg/kg. These activities were higher than those of their corresponding
ethanolic suspensions given orally at the same dose (p<0.05). The combination therapy of MLSNEDDS with other extract-based SNEDDS exhibited remarkable chemosuppression, ranging
from 74.3 % to 95.8 % (for 100 + 100 mg/kg) and 86.7 % to 95.5 % (for 200 + 200 mg/kg/day).
In regard to these findings, SNEDDS suspension may constitute a promising approach for oral
delivery of ML alone or in combination with other antimalarial plants
... Aqueous leaf extract of M. lucida has been previously shown to possess flavonoids, among other bioactive components (Unekwuojo et al., 2011). Flavonoids are known for their antioxidant and anti-inflammatory properties. ...
Increasing drug resistance is a great threat to malaria control. Therefore, a continuous investigation into alternative therapy to mitigate malaria-associated damages is important. In this study, we investigated the anti-hypoglycaemic and anti-hyperlipidaemic effects of aqueous extract of Morinda lucida leaf in Plasmodium berghei-infected mice. Twenty-five mice were randomly grouped into five: Uninfected, infected-untreated, chloroquine (20 mg/kg, per oral), and extract-treated (400 mg/kg and 800 mg/kg, respectively, per oral) groups. Fasting blood glucose was measured before parasite inoculation and after the last treatment. Blood was collected for lipid profile assay at the end of the 4-day treatment. Our results revealed that both chloroquine and the extract lowered parasite growth (p <0.05), while chloroquine and 400 mg/kg of the extract improved blood glucose in Plasmodium berghei-infection. More so, all the treated groups showed attenuated Plasmodium berghei-induced dyslipidaemia, with 400 mg/kg of the extract exhibiting better efficacy. Therefore, this study suggests that Morinda lucida leaf extract can be harnessed as a therapeutic regimen for improved malaria treatments and associated complications. Further study is recommended to elucidate the mechanism of anti-hypoglycaemic and anti-hyperlipidaemic activities of the extract and the possible bioactive compound(s) involved.
... is finding is consistent with other studies in which the inhibitory effect of prophylactic tests was lower than the 4-day suppressive test [27,28]. However, the overall ethanolic leaf extract of S. androgynus significantly reduced parasitemia in prophylactic and suppressive models of P. berghei-infected mice confirming the antimalarial potential of this extract. ...
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.
... P. berghei, a rodent parasite was chosen for the in vivo chemosuppressive activity in the four-day antimalarial test (Peters, 1965). This method was also used by Ebiloma et al., 2011 in the investigation of the antimalarial activity of Morinda lucida (Benth) against erythrocytic stage of mice infected with chloroquine sensitive Plasmodium berghei NK-65. ...
... Also, previous works have shown the anti-malarial activity of chemical constituents like alkaloids and flavonoids isolated from plants (Okokon et al., 2006;Balogun et al., 2009). Also the antimalarial activity observed in this study could be due to single or combined effect of these compounds (Ebiloma et al., 2011). Although numerous bioactive agents have been isolated from the roots, stem bark and leaves of Artocarpus communis, few antimalarial studies have been reported to date (Boyom, et al., 2009). ...
Background: The potential of Artocarpus altilis stem bark as a safe antimalarial agent, and the identification of its antimalarial constituents was explored. Materials and Methods:The air-dried stem bark was extracted with 70% ethanol, filtered and concentrated in vacuo to obtain the extract (EE). The extract was successively partitioned to give n-hexane (AAH),dichloromethane (AAD), ethyl acetate (AAE)n-butanol (AAB)and aqueous (AAQ)fractions respectively after determining the acute toxicity using Lorke’s method. These were each evaluated for chemosuppressive antimalarial activities (0-200mg/kg) against chloroquine-sensitive Plasmodium berghei-berghei-infected albino mice. Normal saline and chloroquine, 10 mg/kg were negative and positive control respectively.The survival times and percentage survivors of the mice in both experiments were determined after observation for twenty-eight days post-drug administration. The five (5) column chromatographic (CC) fractions, AAH1, AAH2, AAH3, AAH4andAAH5 obtained from the most active AAH, were also evaluated for antimalarial activities (0-50mg/kg). Further column purification and repeated PTLC of AAH5 yielded three bands, which were finally subjected to GC-MS analysis. Results:EE gave ED50 and LD50 values of 227.17and >5000 mg/kg while its partitioned fractions gave ED50 values as follows: AAH, 79.14; AAD, 215.59;AAE, 160.46,AAB,81.42; and AAQ, 90.85 mg/kg respectively. The primary CC fractions also gave ED50 values as follows:AAH1 21.95;AAH2, 26.96;AAH3,21.30; AAH4, 20.92 andAAH5, 20.75 mg/kg respectively to identify AAH5 as the putative fraction. GC-MS analysis revealed eleven major compounds (1–11) in the three PTLC bands as the antiplasmodial constituents of the plant. Conclusion:The stem bark of A. altilis is a potential agent in malaria control which is safe for oral use.
... P. berghei, a rodent parasite was chosen for the in vivo chemosuppressive activity in the four-day antimalarial test (Peters, 1965). This method was also used by Ebiloma et al., 2011 in the investigation of the antimalarial activity of Morinda lucida (Benth) against erythrocytic stage of mice infected with chloroquine sensitive Plasmodium berghei NK-65. ...
... Also, previous works have shown the anti-malarial activity of chemical constituents like alkaloids and flavonoids isolated from plants (Okokon et al., 2006;Balogun et al., 2009). Also the antimalarial activity observed in this study could be due to single or combined effect of these compounds (Ebiloma et al., 2011). Although numerous bioactive agents have been isolated from the roots, stem bark and leaves of Artocarpus communis, few antimalarial studies have been reported to date (Boyom, et al., 2009). ...
Background:
The potential of Artocarpus altilis stem bark as a safe antimalarial agent, and the identification of its antimalarial constituents was explored.
Materials and methods:
The air-dried stem bark was extracted with 70% ethanol, filtered and concentrated in vacuo to obtain the extract (EE). The extract was successively partitioned to give n-hexane (AAH), dichloromethane (AAD), ethyl acetate (AAE) n-butanol (AAB) and aqueous (AAQ) fractions respectively after determining the acute toxicity using Lorke's method. These were each evaluated for chemosuppressive antimalarial activities (0-200mg/kg) against chloroquine-sensitive Plasmodium berghei-berghei-infected albino mice. Normal saline and chloroquine, 10 mg/kg were negative and positive control respectively.The survival times and percentage survivors of the mice in both experiments were determined after observation for twenty-eight days post-drug administration. The five (5) column chromatographic (CC) fractions, AAH1, AAH2, AAH3, AAH4 and AAH5 obtained from the most active AAH, were also evaluated for antimalarial activities (0-50mg/kg). Further column purification and repeated PTLC of AAH5 yielded three bands, which were finally subjected to GC-MS analysis.
Results:
EE gave ED50 and LD50 values of 227.17and >5000 mg/kg while its partitioned fractions gave ED50 values as follows: AAH, 79.14; AAD, 215.59; AAE, 160.46, AAB, .42; and AAQ, 90.85 mg/kg respectively. The primary CC fractions also gave ED 50 values as follows: AAH1 21.95; AAH2, 26.96; AAH3, 21.30; AAH4, 20.92 and AAH5, 20.75 mg/kg respectively to identify AAH5 as the putative fraction. GC-MS analysis revealed eleven major compounds (1-11) in the three PTLC bands as the antiplasmodial constituents of the plant.
Conclusion:
The stem bark of A. altilis is a potential agent in malaria control which is safe for oral use.
... P. berghei, a rodent parasite was chosen for the in vivo chemosuppressive activity in the four-day antimalarial test (Peters, 1965). This method was also used by Ebiloma et al., 2011 in the investigation of the antimalarial activity of Morinda lucida (Benth) against erythrocytic stage of mice infected with chloroquine sensitive Plasmodium berghei NK-65. ...
... Also, previous works have shown the anti-malarial activity of chemical constituents like alkaloids and flavonoids isolated from plants (Okokon et al., 2006;Balogun et al., 2009). Also the antimalarial activity observed in this study could be due to single or combined effect of these compounds (Ebiloma et al., 2011). Although numerous bioactive agents have been isolated from the roots, stem bark and leaves of Artocarpus communis, few antimalarial studies have been reported to date (Boyom, et al., 2009). ...
Background: The potential of Artocarpus altilis stem bark as a safe antimalarial agent, and the identification of its antimalarial constituents was explored. Materials and Methods:The air-dried stem bark was extracted with 70% ethanol, filtered and concentrated in vacuo to obtain the extract (EE). The extract was successively partitioned to give n-hexane (AAH), dichloromethane (AAD), ethyl acetate (AAE) n-butanol (AAB) and aqueous (AAQ) fractions respectively after determining the acute toxicity using Lorke's method. These were each evaluated for chemosuppressive antimalarial activities (0-200mg/kg) against chloroquine-sensitive Plasmodium berghei-berghei-infected albino mice. Normal saline and chloroquine, 10 mg/kg were negative and positive control respectively.The survival times and percentage survivors of the mice in both experiments were determined after observation for twenty-eight days post-drug administration. The five (5) column chromatographic (CC) fractions, AAH1, AAH2, AAH3, AAH4 and AAH5 obtained from the most active AAH, were also evaluated for antimalarial activities (0-50mg/kg). Further column purification and repeated PTLC of AAH5 yielded three bands, which were finally subjected to GC-MS analysis. Results: EE gave ED50 and LD50 values of 227.17and >5000 mg/kg while its partitioned fractions gave ED50 values as follows: AAH, 79.14; AAD, 215.59; AAE, 160.46, AAB, .42; and AAQ, 90.85 mg/kg respectively. The primary CC fractions also gave ED50 values as follows: AAH1 21.95; AAH2, 26.96; AAH3, 21.30; AAH4, 20.92 and AAH5, 20.75 mg/kg respectively to identify AAH5 as the putative fraction. GC-MS analysis revealed eleven major compounds (1-11) in the three PTLC bands as the antiplasmodial constituents of the plant. Conclusion: The stem bark of A. altilis is a potential agent in malaria control which is safe for oral use.
