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 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 Glideosomal GAP50 binders that inhibit invasion and restrict malaria parasite in vitro and in vivo

2021 ◽  
Author(s):  
Prakhar Agrawal ◽  
Surekha Kumari ◽  
Upendra Sharma ◽  
Dinkar Sahal
Keyword(s):  
Mouse Model ◽  
Small Molecules ◽  
Malaria Parasite ◽  
Drug Combinations ◽  
Antiplasmodial Activity ◽  
Modern World ◽  
Anchor Protein

Abstract Malaria continues to be a killer disease even in the modern world. Vaccines and drugs have a lot to learn from the malaria parasite before they can be successful. Here, using a filter for glideosomal anchor protein PfGAP50, we have explored a plethora of small molecules to shortlist eight GAP50 binders with promising antiplasmodial activity (IC50 < 3 µM) that are also highly selective. Of these, Hayatinin, Bedaquiline, MMV688271, Curine, and Brilacidin with PfINDO IC50 ≤ 1 µM were found to stall merozoites invasion by inhibiting IMC formation besides increasing ROS levels in trophozoites. Bedaquiline loaded healthy RBCs showed prophylactic ability to prevent intraerythrocytic development of malaria parasite. Synergistic activities with ΣFIC values as low as 0.22 (Curine and Artemisinin) or 0.37 (Bedaquiline and Artemisinin) augur well for the development of drug combinations to combat malaria effectively. Interestingly, orally delivered Bedaquiline (50 mg/Kg b. wt.) showed substantial suppression of parasitemia in the mouse model of malaria.

scholarly journals In Vitro and In Vivo Antimalarial Activities and Toxicological Assessment of Pogostemon Cablin (Blanco) Benth

2020 ◽  
Vol 25 ◽  
pp. 2515690X2097838
Author(s):  
Arisara Phuwajaroanpong ◽  
Prapaporn Chaniad ◽  
Natharinee Horata ◽  
Saowanee Muangchanburee ◽  
Kantarakorn Kaewdana ◽  
...  
Keyword(s):  
Body Weight ◽  
Antimalarial Activity ◽  
Ethanolic Extract ◽  
Vero Cells ◽  
Toxicological Assessment ◽  
Pogostemon Cablin ◽  
Dehydrogenase Enzyme ◽  
Preliminary Study

The aim of this study was to investigate the antimalarial activities and toxicity of Pogostemon cablin extracts. In vitro activities against the chloroquine-resistant Plasmodium falciparum K1 strain were assessed by using the Plasmodium lactate dehydrogenase enzyme (pLDH) assay, while in vivo activity against the Plasmodium berghei ANKA strain in mice was investigated using a 4-day suppressive test. The in vitro and in vivo toxicity were determined in Vero cells and mice, respectively. The ethanolic extract possessed antimalarial activity with an IC50 of 24.49 ± 0.01 µg/ml, whereas the aqueous extract showed an IC50 of 549.30 ± 0.07 µg/ml. Cytotoxic analyses of the ethanolic and aqueous extracts revealed a nontoxic effect on Vero cells at a concentration of 80 µg/ml. Based on a preliminary study of in vitro antimalarial activity, the ethanolic extract was chosen as a potential agent for further in vivo antimalarial activity analysis in mice. The ethanolic extract, which showed no toxic effect on mice at a dose of 2000 mg/kg body weight, significantly suppressed parasitemia in mice by 38.41%, 45.12% and 89.00% at doses of 200, 400 and 600 mg/kg body weight, respectively. In conclusion, this study shows that the ethanolic P. cablin extract possesses in vitro and in vivo antimalarial activity without toxic effects.

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 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.

scholarly journals Chemical and Bioactivity Evaluation of the Bark of Neonauclea purpurea

2012 ◽  
Vol 7 (2) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Netiya Karaket ◽  
Kanyaratt Supaibulwatana ◽  
Supatsara Ounsuk ◽  
Valérie Bultel-Poncé ◽  
Van Cuong Pham ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Traditional Medicine ◽  
Resistant Strain ◽  
Antimalarial Activity ◽  
Indole Alkaloids ◽  
Vero Cells ◽  
Stem Bark ◽  
Meoh Extract ◽  
Bioassay Guided Fractionation

Bioassay-guided fractionation of the MeOH extract from the stem bark of Neonauclea purpurea used in traditional medicine, resulted in the isolation of 2 indole alkaloids, cadambine (1) and α-dihydrocadambine (2), as well as a quinolic compound, 2,6-dimethoxy-1,4-benzoquinone (3). Antimalarial activity evaluation showed that compounds 2 and 3 exhibited mild in vitro antimalarial activity against Plasmodium falciparum, the chloroquine-resistant strain K1 with IC50 values of 6.6 and 11.3 μM, respectively. Compounds 1 and 2 showed no cytotoxicity to monkey (Vero) cells, but compound 3 showed weak cytotoxicity with an IC50 value of 1.19 μM.

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 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.

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