scholarly journals In VitroandIn VivoAntimalarial Activity Assays of Seeds fromBalanites aegyptiaca: Compounds of the Extract Show Growth Inhibition and Activity against Plasmodial Aminopeptidase

2011 ◽  
Vol 2011 ◽  
pp. 1-9 ◽  
Author(s):  
Peter Kusch ◽  
Susanne Deininger ◽  
Sabine Specht ◽  
Rudeka Maniako ◽  
Stefanie Haubrich ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Antiplasmodial Activity ◽  
Gas Chromatography Mass Spectrometry ◽  
Desert Plant ◽  
Compound A ◽  
Crude Plant Extract ◽  
Butyl Phenol ◽  
Dose Dependent

Balanites aegyptiaca(Balanitaceae) is a widely grown desert plant with multiuse potential. In the present paper, a crude extract fromB. aegyptiacaseeds equivalent to a ratio of 1 : 2000 seeds to the extract was screened for antiplasmodial activity. The determined IC50value for the chloroquine-susceptiblePlasmodium falciparumNF54 strain was 68.26 . Analysis of the extract by gas chromatography-mass spectrometry detected 6-phenyl-2(H)-1,2,4-triazin-5-one oxime, an inhibitor of the parasitic M18 Aspartyl Aminopeptidase as one of the compounds which is responsible for thein vitroantiplasmodial activity. The crude plant extract had a of 2.35  and showed a dose-dependent response. After depletion of the compound, a significantly lower inhibition was determined with a of 4.8 . Moreover, two phenolic compounds, that is, 2,6-di-tert-butyl-phenol and 2,4-di-tert-butyl-phenol, with determined IC50values of 50.29  and 47.82 , respectively, were detected. These compounds may contribute to thein vitroantimalarial activity due to their antioxidative properties. In anin vivoexperiment, treatment of BALB/c mice with the aqueousBalaniteextract did not lead to eradication of the parasites, although a reduced parasitemia at day 12 p.i. was observed.

scholarly journals In vivo efficacy and metabolism of the antimalarial cycleanine and improved in vitro antiplasmodial activity of novel semisynthetic analogues

2020 ◽  
Author(s):  
Fidelia Ijeoma Uche ◽  
Xiaozhen Guo ◽  
Jude Okokon ◽  
Imran Ullah ◽  
Paul Horrocks ◽  
...  
Keyword(s):  
Metabolic Pathways ◽  
High Performance ◽  
Antimalarial Activity ◽  
Biological Activities ◽  
Antiplasmodial Activity ◽  
Survival Times ◽  
Antiproliferative Effects ◽  
Future Evaluation

Bisbenzylisoquinoline (BBIQ) alkaloids are a diverse group of natural products that demonstrate a range of biological activities. In this study, the in vitro antiplasmodial activity of three BBIQ alkaloids (cycleanine (1), isochondodendrine (2) and 2′-norcocsuline (3)) isolated from the Triclisia subcordata Oliv. medicinal plant traditionally used for the treatment of malaria in Nigeria are studied alongside two semi-synthetic analogues (4 and 5) of cycleanine. The antiproliferative effects against a chloroquine-resistant Plasmodium falciparum strain were determined using a SYBR Green 1 fluorescence assay. The in vivo antimalarial activity of cycleanine (1) is then investigated in suppressive, prophylactic and curative murine malaria models after infection with a chloroquine-sensitive Plasmodium berghei strain. BBIQ alkaloids (1–5) exerted in vitro antiplasmodial activities with IC50 at low micromolar concentrations with the two semi-synthetic cycleanine analogues showing an improved potency and selectivity than cycleanine. At oral doses of 25 and 50mg/kg body weight of infected mice, cycleanine suppressed the levels of parasitaemia, and increased mean survival times significantly compared to the control groups. The metabolites and metabolic pathways of cycleanine (1) were also studied using high performance liquid chromatography electrospray ionization tandem mass spectrometry. Twelve novel metabolites were detected in rats after intragastic administration of cycleanine. The metabolic pathways of cycleanine were demonstrated to involve hydroxylation, dehydrogenation, and demethylation. Overall, these in vitro and in vivo results provide a basis for the future evaluation of cycleanine and its analogues as leads for further development.

scholarly journals Antiplasmodial and Cytotoxic Cytochalasins from an Endophytic Fungus, Nemania sp. UM10M, Isolated from a Diseased Torreya taxifolia Leaf

Molecules ◽  
2019 ◽  
Vol 24 (4) ◽  
pp. 777 ◽  
Author(s):  
Mallika Kumarihamy ◽  
Daneel Ferreira ◽  
Edward Croom ◽  
Rajnish Sahu ◽  
Babu Tekwani ◽  
...  
Keyword(s):  
Mouse Model ◽  
Solid Tumor ◽  
Endophytic Fungus ◽  
Antimalarial Activity ◽  
Vero Cells ◽  
Antiplasmodial Activity ◽  
Etoac Extract ◽  
Bioassay Guided Fractionation

Bioassay-guided fractionation of an EtOAc extract of the broth of the endophytic fungus Nemania sp. UM10M (Xylariaceae) isolated from a diseased Torreya taxifolia leaf afforded three known cytochalasins, 19,20-epoxycytochalasins C (1) and D (2), and 18-deoxy-19,20-epoxy-cytochalasin C (3). All three compounds showed potent in vitro antiplasmodial activity and phytotoxicity with no cytotoxicity to Vero cells. These compounds exhibited moderate to weak cytotoxicity to some of the cell lines of a panel of solid tumor (SK-MEL, KB, BT-549, and SK-OV-3) and kidney epithelial cells (LLC-PK11). Evaluation of in vivo antimalarial activity of 19,20-epoxycytochalasin C (1) in a mouse model at 100 mg/kg dose showed that this compound had weak suppressive antiplasmodial activity and was toxic to animals.

scholarly journals Evaluation of in vitro and in vivo Antiplasmodial Activity of the Leaf Latex of Aloe Weloensis (Aloaceae)

2020 ◽  
Author(s):  
Gedefaw Getnet Amare ◽  
Tadesse Awgichew ◽  
Solomon Ahmed ◽  
Zemene Demelash Kifle
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Activities ◽  
Antimalarial Activity ◽  
Potential Effect ◽  
Pack Cell Volume ◽  
Curative Effect ◽  
Parasitemia Level ◽  
Dose Dependent

Abstract Background: Nature has gifted a variety of plants having potential effect against plasmodium parasites. The present study was aimed to determine in vitro and in vivo antimalarial activity of the leaf latex of Aloe weloensis.Methods: In vitro antimalarial activity of the leaf latex of A. weloensis was determined against 3D7 strain of P. falciparum. Antimalarial activity of the three doses the latex was evaluated in 4 day-suppressive and curative models against P. berghei infected mice. Antioxidant activity of the leaf latex of A. weloensis was assessed in 2,2- diphenyl 1- picrylhydrazine assay model. Results: Antioxidant activity of the latex was concentration dependent; the strongest inhibition was measured at 400 μg/mL (73.54%). The leaf latex of A. weloensis was demonstrated inhibitory activity against 3D7 malarial strain (IC50 = 9.14 μg/ml). Suppressive and curative effect of the latex was found to be dose dependent. Parasitemia reduction was significant (200 mg/kg, p<0.01, 400 and ,600 mg/kg, p<0.001) in 4-day suppressive test compared to vehicle control. Parasitemia level of the mice treated with 200, 400 and 600 mg/kg doses of the latex significantly (p<0.001) reduced with suppression of 36%, 58% and 64% respectively in curative test. Administration of the leaf latex of A. weloensis significantly (p<0.01) improved mean survival time, pack cell volume, rectal temperature and body weight of P. berghei infected mice. Conclusion: The finding showed that the leaf latex of Aloe weloensis endowed prominent antimalarial and antioxidant activities. The result can serve as a step towards the development of safe and effective herbal therapy against plasmodium parasites.

scholarly journals Andrographolide: A Novel Antimalarial Diterpene Lactone Compound fromAndrographis paniculataand Its Interaction with Curcumin and Artesunate

2011 ◽  
Vol 2011 ◽  
pp. 1-6 ◽  
Author(s):  
Kirti Mishra ◽  
Aditya P. Dash ◽  
Nrisingha Dey
Keyword(s):  
Plasmodium Falciparum ◽  
Life Span ◽  
Plasmodium Berghei ◽  
Antimalarial Activity ◽  
Andrographis Paniculata ◽  
Antiplasmodial Activity ◽  
Template Molecule

Andrographolide (AND), the diterpene lactone compound, was purified by HPLC from the methanolic fraction of the plantAndrographis paniculata. The compound was found to have potent antiplasmodial activity when tested in isolation and in combination with curcumin and artesunate against the erythrocytic stages ofPlasmodium falciparum in vitroandPlasmodium bergheiANKAin vivo. IC50s for artesunate (AS), andrographolide (AND), and curcumin (CUR) were found to be 0.05, 9.1 and 17.4 μM, respectively. The compound (AND) was found synergistic with curcumin (CUR) and addictively interactive with artesunate (AS).In vivo, andrographolide-curcumin exhibited better antimalarial activity, not only by reducing parasitemia (29%), compared to the control (81%), but also by extending the life span by 2-3 folds. Being nontoxic to thein vivosystem this agent can be used as template molecule for designing new derivatives with improved antimalarial properties.

scholarly journals In Vivo Antiplasmodial Activity of Terminalia mantaly Stem Bark Aqueous Extract in Mice Infected by Plasmodium berghei

2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
Mariscal Brice Tchatat Tali ◽  
Cedric Derick Jiatsa Mbouna ◽  
Lauve Rachel Yamthe Tchokouaha ◽  
Patrick Valere Tsouh Fokou ◽  
Jaures Marius Tsakem Nangap ◽  
...  
Keyword(s):  
Acute Toxicity ◽  
Aqueous Extract ◽  
Plasmodium Berghei ◽  
Antimalarial Activity ◽  
Lethal Dose ◽  
Stem Bark ◽  
Antiplasmodial Activity ◽  
Bark Extract

Background. Terminalia mantaly is used in Cameroon traditional medicine to treat malaria and related symptoms. However, its antiplasmodial efficacy is still to be established. Objectives. The present study is aimed at evaluating the in vitro and in vivo antiplasmodial activity and the oral acute toxicity of the Terminalia mantaly extracts. Materials and Methods. Extracts were prepared from leaves and stem bark of T. mantaly, by maceration in distilled water, methanol, ethanol, dichloromethane (DCM), and hexane. All extracts were initially screened in vitro against the chloroquine-resistant strain W2 of P. falciparum to confirm its in vitro activity, and the most potent one was assessed in malaria mouse model at three concentrations (100, 200, and 400 mg/kg/bw). Biochemical, hematological, and histological parameters were also determined. Results. Overall, 7 extracts showed in vitro antiplasmodial activity with IC50 ranging from 0.809 μg/mL to 5.886 μg/mL. The aqueous extract from the stem bark of T. mantaly (Tmsbw) was the most potent (IC50=0.809 μg/mL) and was further assessed for acute toxicity and efficacy in Plasmodium berghei-infected mice. Tmsbw was safe in mice with a median lethal dose (LD50) higher than 2000 mg/kg of body weight. It also exerted a good antimalarial efficacy in vivo with ED50 of 69.50 mg/kg and had no significant effect on biochemical, hematological, and histological parameters. Conclusion. The results suggest that the stem bark extract of T. mantaly possesses antimalarial activity.

scholarly journals Novel Antimalarial Aminoquinolines: Heme Binding and Effects on Normal or Plasmodium falciparum-Parasitized Human Erythrocytes

2009 ◽  
Vol 53 (10) ◽  
pp. 4339-4344 ◽  
Author(s):  
Fausta Omodeo-Salè ◽  
Lucia Cortelezzi ◽  
Nicoletta Basilico ◽  
Manolo Casagrande ◽  
Anna Sparatore ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Antimalarial Activity ◽  
Heme Binding ◽  
Human Red Blood Cells ◽  
Rbc Membrane ◽  
Alkyl Derivatives ◽  
Resistant Strains ◽  
Dose Dependent

ABSTRACT Two new quinolizidinyl-alkyl derivatives of 7-chloro-4-aminoquinoline, named AM-1 and AP4b, which are highly effective in vitro against both the D10 (chloroquine [CQ] susceptible) and W2 (CQ resistant) strains of Plasmodium falciparum and in vivo in the rodent malaria model, have been studied for their ability to bind to and be internalized by normal or parasitized human red blood cells (RBC) and for their effects on RBC membrane stability. In addition, an analysis of the heme binding properties of these compounds and of their ability to inhibit beta-hematin formation in vitro has been performed. Binding of AM1 or AP4b to RBC is rapid, dose dependent, and linearly related to RBC density. Their accumulation in parasitized RBC (pRBC) is increased twofold compared to levels in normal RBC. Binding of AM1 or AP4b to both normal and pRBC is higher than that of CQ, in agreement with the lower pKa and higher lipophilicity of the compounds. AM1 or AP4b is not hemolytic per se and is less hemolytic than CQ when hemolysis is accelerated (induced) by hematin. Moreover, AM-1 and AP4b bind heme with a stoichiometry of interaction similar to that of CQ (about 1:1.7) but with a lower affinity. They both inhibit dose dependently the formation of beta-hematin in vitro with a 50% inhibitory concentration comparable to that of CQ. Taken together, these results suggest that the antimalarial activity of AM1 or AP4b is likely due to inhibition of hemozoin formation and that the efficacy of these compounds against the CQ-resistant strains can be ascribed to their hydrophobicity and capacity to accumulate in the vacuolar lipid (elevated lipid accumulation ratios).

scholarly journals Evaluating Antiplasmodial and Antimalarial Activities of Soybean (Glycine max) Seed Extracts on P. falciparum Parasite Cultures and P. berghei-Infected Mice

2020 ◽  
Vol 2020 ◽  
pp. 1-8
Author(s):  
Kevin Nyandwaro ◽  
Job Oyweri ◽  
Francis Kimani ◽  
Amos Mbugua
Keyword(s):  
Therapeutic Potential ◽  
Antimalarial Activity ◽  
Antioxidant Properties ◽  
Antiplasmodial Activity ◽  
Methanol Extracts ◽  
Lead Compounds ◽  
High Parasite ◽  
Seed Extracts

Background. Plasmodium parasite resistance to artemisinin-based combination therapies (ACTs) calls for development of new, affordable, safe, and effective antimalarial drugs. Studies conducted previously on soybean extracts have established that they possess antimicrobial, anti-inflammatory, anticancerous, and antioxidant properties. The activity of such extracts on Plasmodium parasites has not been potentially exploited. Objectives. The aim of this study was to determine the antiplasmodial activity of soybean extracts using Plasmodium falciparum cultures, followed by an in vivo evaluation of safety and antimalarial activity of the extracts in Plasmodium berghei ANKA strain-infected mice. Method. Aqueous, methanol, and peptide extracts of soybean seeds were prepared. An in vitro evaluation of the extracts for antiplasmodial activity was carried out using two P. falciparum strains: D6, a chloroquine-sensitive Sierra Leone 1 strain and W2, a chloroquine-resistant Indochina 1 strain. Following the in vitro assessment, two active extracts (peptide and methanol) were selected for in vivo assay with mice infected with P. berghei ANKA strain. The two extracts were tested for their therapeutic potential (curative test). The peptide extract was further assessed to determine whether it could prevent the establishment of a P. berghei infection (prophylactic test). For the curative tests, methanol and peptide extracts were separately administered orally to three groups of five P. berghei-infected Swiss albino mice for four days, at three dosage levels: 800, 400, and 200 mg/kg/day. In the prophylactic test, the similar dosage regimen was applied at baseline to 3 groups of uninfected mice using the peptide extract which was administered orally for 4 days. Results. Peptide and methanol extracts showed good activity with IC50 of 19.97 ± 2.57 μg/ml and 10.14 ± 9.04 μg/ml, respectively, against the D6 strain. The IC50 values for the peptide and methanol extracts were 28.61 ± 1.32 μg/ml and 14.87 ± 3.43 μg/ml, respectively, against the W2 strain. Methanol and peptide extracts exhibited high parasite-suppressive (therapeutic) activity of 72.9% and 71.9%, respectively, using the 800 mg/kg dose. In the prophylactic test, the peptide extract exhibited suppressive activity of 64.7% upon use of 800 mg/kg. Notably, there was a significant decrease (P<0.001) in suppression with lower doses. Conclusion. The results show the presence of antimalarial properties in soybean extracts with higher curative activity when compared to the prophylactic activity. However, more research needs to be conducted on this plant to possibly establish lead compounds.

scholarly journals Antiplasmodial Potential of Indonesian Medicinal Plants

2020 ◽  
Author(s):  
Nurhayati Bialangi ◽  
Mohamad Adam Mustapa ◽  
Yuszda K Salimi ◽  
Weny J.A Musa ◽  
Ari Widiyantoro ◽  
...  
Keyword(s):  
Medicinal Plants ◽  
Mouse Model ◽  
Traditional Medicine ◽  
Post Infection ◽  
High Ratio ◽  
Antiplasmodial Activity ◽  
Dependent Manner ◽  
Dose Dependent

Abstract Background: Species A. paniculata (Burm. f.) Nees known as″ Sambiloto ″ and P. pellucida L. Kunth known as″ Suruhan ″ are mainly distributed in Indonesia and their combination was used as a traditional medicine for treating malaria diseases. However, no information appears to have evaluated the antiplasmodial potential of the two plants. This research aimed to evaluate the antiplasmodial activity of the two plants and the species P. pellucida L. Kunth alone as a source of antiplasmodial agent. Methods: In vitro test of the AP-PP and PP extracts against Pf D-10 (chloroquine-sensitive) were performed as described by Desjardins et al. An in vivo test of the PP extract in mice infected with Pb ANKA was performed using Peters´ 4-day suppressive test. Parasitemia, growth and inhibition rates were determined via Giemsa-stained smear of blood and analyzed microscopically. Survival was followed up until day 21 post-infection.Results: The increased ratio of the PP extract (20:80) exhibited significant antiplasmodial in contrast to the high ratio of the AP extract (IC50, 62.01 mg/mL). Further evaluation of the PP extract alone displayed better antiplasmodial activity with an IC50 value of 4.0 mg/mL. Furthermore, an in vivo test of the PP extract in BALB/c albino mice infected with Pb ANKA exhibited a significant chemosuppressive effect in a dose-dependent manner.Conclusion: The increased ratio of the PP extract exhibited a major contribution for their activity. The PP extract alone showed better antiplasmodial activity than the AP extract and their combination. An in vivo test confirmed the efficacy of the PP extract in mouse model.

GC-MS Characterization of Phyto-Components in the Ethanolic and Hydroalcoholic Extracts of Cocos nucifera Endocarp and Evaluation of their Antimalarial Potential

2019 ◽  
Vol 9 (4) ◽  
pp. 289-294
Author(s):  
Babita Aggarwal ◽  
Pankaj Sharma ◽  
Hardarshan Singh Lamba
Keyword(s):  
Antimalarial Activity ◽  
Cocos Nucifera ◽  
Antiplasmodial Activity ◽  
Bioactive Components ◽  
Traditional Use ◽  
Standard Drug ◽  
Ic50 Values

Background: Plants are rich and cheap source of active phytoconstituents. Present study was performed in order to authenticate the traditional use of Cocos nucifera in malaria treatment as well as to search an alternative for drug resistant parasites. Objective: In the present investigation, ethanolic (ACN) and hydroalcoholic (HACN) extracts of Cocos nucifera endocarp were evaluated for antimalarial potential as well as subjected to GC-MS analysis to characterize the bioactive components. Methods: In vitro antiplasmodial activity of ACN and HACN was assessed against P. falciparum strains MRC-02 (CQ sensitive) and RKL-09 (CQ resistant) and percentage schizont maturation inhibition was determined. To confirm the antimalarial potential, in vivo Peter’s 4-Day suppressive test using P. berghei strain was performed at a dose of 25 and 50 mg/kg/day for 4 consecutive days. Bioactive components were characterized by the application of Gas chromatography and Mass spectrometric technique to the extracts. Results: Promising in vitro antiplasmodial activity was exhibited by both alcoholic (ACN) and hydroalcoholic (HACN) extracts against P. falciparum strains MRC-02 (CQ sensitive) with IC50 values < 5 µg/mL. HACN (% Suppression = 75.43 ± 0.18; MST=19.21 days) and ACN (% Suppression = 34.65 ± 0.11; MST=10.11 days) showed moderate in vivo antimalarial activity (p < 0.05) at dose 50 mg/Kg while standard drug chloroquine (8mg/kg) suppressed 100% parasitaemia. Twenty compounds have been identified and characterized by GC-MS studies.

scholarly journals Assessment of Antiplasmodial Activity and Toxicity of Crude Extracts and Isolated Compounds from Oncoba spinosa (Flacourtiaceae)

2019 ◽  
pp. 1-14
Author(s):  
Kodi Philip ◽  
Peter Kiplagat Cheplogoi ◽  
Mwangi Muthoni Elizabeth ◽  
M. Akala Hoseah ◽  
Moses K. Langat
Keyword(s):  
Acute Toxicity ◽  
Ethyl Acetate ◽  
Crude Extract ◽  
Antimalarial Activity ◽  
Local Communities ◽  
Antiplasmodial Activity ◽  
Isolation And Purification ◽  
Crude Extracts

Aims: The medicinal plant Oncoba spinosa is used by the local communities in Butebo County in Eastern Uganda for treatment of malaria and other diseases. In vitro antiplasmodial activities of the crude extracts and isolated compounds were screened against chloroquine sensitive 3D7 and resistant Dd2 strains. In vivo acute toxicity of the extracts and structure elucidation were also determined in the study. Experimental: Crude extracts of: n-hexane, dichloromethane, ethyl acetate and methanol were prepared. Isolation and purification of these extracts were done using chromatographic techniques which consisted of column and thin layer chromatography. The structures were elucidated on the basis of spectroscopic evidence. In vitro antiplasmodial activity was performed on chloroquine sensitive 3D7 and resistant Dd2 strains of Plasmodium falciparum using SYBR Green 1 assay technique. Lorke’s method of acute toxicity was used to determine the in vivo acute toxicity of the crude extracts in mice. Results: The root ethyl acetate crude extract had highest antiplasmodial activity of IC50:4.69 ± 0.01 µg/mL and 3.52 ± 0.02 µg/mL against 3D7 and Dd2 strains respectively while the remaining three were inactive against both strains of Plasmodium. Isolation resulted in the identification of three known compounds which included: β-sitosterol, benzoic acid and chaulmoogric acid. Among the tested compounds β-sitosterol showed the highest activity of IC50 3D7: 5.51 µM. Dichloromethane and hexane extracts were non-toxic with LD50 > 5000 mg/kg while the EtOAc and MeOH extracts were slightly toxic with LD50 of 547.72 mg/kg. Statistically significance existed between the antiplasmodial activity of the crude extracts and compounds when compared with the controls at (p < 0.05). Extracts and compounds exerted a significant (P < 0.05) decrease in antiplasmodial activity compared to the positive controls. Conclusion: The findings confirm the ethnobotanical use of O. spinosa by the local communities in Butebo County for the treatment of malaria. The results also suggest that the crude extract of this plant is safe and possesses antimalarial activity which can be used as a basis for in vivo and clinical studies to be done. Therefore the plant can offer a potential drug lead for developing a safe, effective and affordable antimalarial.

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