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.

scholarly journals Synthesis, antimalarial activity evaluation and molecular docking studies of some novel dispiro-1,2,4,5-tetraoxanes

2015 ◽  
Vol 10 (4) ◽  
pp. 917 ◽  
Author(s):  
Mukesh Kumar Kumawat ◽  
Dipak Chetia
Keyword(s):  
Plasmodium Falciparum ◽  
Molecular Docking ◽  
Resistant Strain ◽  
Antimalarial Activity ◽  
Binding Pocket ◽  
Docking Studies ◽  
Spectroscopic Techniques ◽  
Molecular Docking Studies ◽  
Activity Screening

<p class="Abstract">Seven novel dispiro-1,2,4,5-tetraoxane derivatives were synthesized and characterized by a number of analytical and spectroscopic techniques. The molecules were subsequently screened for in vitro antimalarial activity against chloroquine resistant strain of <em>Plasmodium falciparum</em> (RKL-9). At antimalarial activity screening, two compounds, namely 5d (MIC = 15.6 µg/mL or 64.5 µM) and 5f (MIC = 15.6 µg/mL or 54.6 µM) were found to be about 1.5 times more potent against chloroquine resistant strain-RKL-9 compared to chloroquine (MIC = 25.0 µg/mL or 78.3 µM). Molecular docking studies of potent ligands were also performed in cysteine protease binding pocket residues of falcipain-2 as a target protein.</p><p> </p>

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 Aktivitas Antimalaria Daun Erythrina variegata

2018 ◽  
Vol 10 (1) ◽  
pp. 36
Author(s):  
Tati Herlina ◽  
Unang Supratman ◽  
Anas Subarnas ◽  
Supriyatna Sutardjo ◽  
Noor Rain Abdullah
Keyword(s):  
Plasmodium Falciparum ◽  
Lactate Dehydrogenase ◽  
Column Chromatography ◽  
Active Compound ◽  
Resistant Strain ◽  
Methanol Extract ◽  
Antimalarial Activity ◽  
Antimalarial Agents ◽  
Erythrina Variegata

The leaves of Erythrina variegata (Leguminosae) used tradisional plant of an antimalarial. In the course of our continuing search for novel an antimalarial compound from Erythrina plants, the methanol extract of the leaves ofE. variegata showed significant antimalarial activity in vitro toward Plasmodium falciparum in vitro using the lactate dehydrogenase (LDH) method. The methanol extract of the leaves of E. variegata showed against bothstrains of parasite with IC50of 6.8 ?g/ml against K1 and > 60 ?g/ml against 3D7, respectively. The methanol extract of the leaves of E. variegata was separated by using bioassay-guide fractionation. The n-buthanol fraction yieldedthe most activity, exhibiting equipotency against both strains of parasite with IC50of 5.1 ?g/ml against K1 and 13.5 ?g/ml against 3D7, respectively. Furthermore, by using the antimalarial activity to follow separation, the n-buthanol fraction was separated by combination of column chromatography to yield an active compound. The active compound showed antimalarial activity against both strains of parasite used with IC50 of 4.3 ?g/ml against K1 and 23.5 ?g/ml against 3D7, respectively. Its inhibition of the resistant strain (K1) was also much better compared to its inhibition of the sensitive strain (3D7), indicated that the leaves of E. variegata to be potential as antimalarial agents, but its lower potency compared to artemisinin and chloroquin.

scholarly journals In Vitro Antimalarial Activity and Cytotoxity of 20 Ethanolic Crude Extracts from Thai Herbs Against Plasmodium Falciparum TM267

2017 ◽  
Vol 35 (2) ◽  
pp. 109
Author(s):  
Natharinee Horata ◽  
Sarawut Suttirat ◽  
Taweebhorn Panpanich ◽  
Anuthida Siriphor ◽  
Budsaraporn Navaprayoonvach ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Molecular Docking ◽  
Antimalarial Activity ◽  
Vero Cells ◽  
Ocimum Sanctum ◽  
Root Extract ◽  
Active Compounds ◽  
Crude Extracts ◽  
Plumbago Indica

Objective: To determine the antimalarial activity of ethanol crude extracts from 20 Thai herbs against Plasmodiumfalciparum (P. falciparum) chloroquine-resistant strain TM267. Molecular docking of the active compounds from the selected Thaiherbs were analyzed with Plasmodium falciparum dihydrofolate reductase (PfDHFR).Material and Method: An in vitro study of antimalarial activity against P. falciparum TM267 was done using a parasitelactate dehydrogenese assay, and the cytotoxic effects of extracts were tested against Vero cells using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. The 50% inhibitory concentration (IC50) and 50%cytotoxicity concentration were calculated from the dose-response curves. Molecular docking and post-dockingwere analyzed with the x-ray crystal structure of PfDHFR-thymidylate synthase complexed with pyrimethamine,nicotinamide adenine dinucleotide phosphate and deoxyuridylate.Results: Of these, the Plumbago indica L. root extract showed high antimalarial activity, with an IC50 value of 3.7μg/ml and less cytotoxicity when tested against Vero cells, followed by the Citrus hystrix DC. fruit extract, Vitex trifoliaLinn. root extract, Ocimum sanctum L. leave extract, of Allium sativum L. bulb extract and Salacia chinensis L. stem extract,respectively. All 7 active compounds reported from these herbal extracts had high docking scores against PfDHFR.The Citrusoside C from Citrus hystrix DC. had the highest docking score.Conclusion: It could be purposed that there were active compounds in Plumbago indica L., Vitex trifolia Linn. and Citrus hystrix DC. which are potential inhibitors against malaria that could bind to the active site of PfDHFR. However, the active Citrusosides from Citrus hystrix DC. should be further investigated for their effectiveness against malaria. 

scholarly journals Prenylated Isoflavanones from the Stem Bark of Erythrina poeppigiana (Leguminosae) and its Antimalarial Properties

2017 ◽  
Vol 12 (8) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Tati Herlina ◽  
Anderson Arnold Aloanis ◽  
Dikdik Kurnia ◽  
Desi Harneti ◽  
Rani Maharani ◽  
...  
Keyword(s):  
Methanol Extract ◽  
Ethyl Acetate Extract ◽  
Antimalarial Activity ◽  
Stem Bark ◽  
In Vitro Bioassay ◽  
Erythrina Poeppigiana ◽  
Antimalarial Agents ◽  
Bioassay Guided Fractionation ◽  
Promising Source

During the course of our continuous search for novel antimalarial compounds derived from the Indonesian Erythrina plants, the methanol extract of the stem bark of Erythrina poeppigiana demonstrated significant antimalarial activity against Plasmodium falciparum parasites, in vitro. Bioassay-guided fractionation of the ethyl acetate extract resulted in the isolation of three known platyisoflavanone (1), erypogein D (2), and sophoraisoflavanone A (3). Compounds 1–3 showed strong antimalarial activity against 3D7 strain of P. falciparum with IC50 values of 0.52, 0.36, and 3.65μM, respectively. This result indicates that stem bark of E. poeppigiana is a promising source of antimalarial agents, and merits further investigation.

scholarly journals Stage-dependent effect of deferoxamine on growth of Plasmodium falciparum in vitro

Blood ◽  
1990 ◽  
Vol 76 (6) ◽  
pp. 1250-1255 ◽  
Author(s):  
S Whitehead ◽  
TE Peto
Keyword(s):  
Plasmodium Falciparum ◽  
Growth Inhibition ◽  
Antimalarial Activity ◽  
Clinical Malaria ◽  
Inhibitory Effect ◽  
Parasite Development ◽  
And Control ◽  
Speed Of Onset

Abstract Deferoxamine (DF) has antimalarial activity that can be demonstrated in vitro and in vivo. This study is designed to examine the speed of onset and stage dependency of growth inhibition by DF and to determine whether its antimalarial activity is cytostatic or cytocidal. Growth inhibition was assessed by suppression of hypoxanthine incorporation and differences in morphologic appearance between treated and control parasites. Using synchronized in vitro cultures of Plasmodium falciparum, growth inhibition by DF was detected within a single parasite cycle. Ring and nonpigmented trophozoite stages were sensitive to the inhibitory effect of DF but cytostatic antimalarial activity was suggested by evidence of parasite recovery in later cycles. However, profound growth inhibition, with no evidence of subsequent recovery, occurred when pigmented trophozoites and early schizonts were exposed to DF. At this stage in parasite development, the activity of DF was cytocidal and furthermore, the critical period of exposure may be as short as 6 hours. These observations suggest that iron chelators may have a role in the treatment of clinical malaria.

scholarly journals In vitro activities of novel catecholate siderophores against Plasmodium falciparum.

1996 ◽  
Vol 40 (9) ◽  
pp. 2094-2098 ◽  
Author(s):  
B Pradines ◽  
F Ramiandrasoa ◽  
L K Basco ◽  
L Bricard ◽  
G Kunesch ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Mechanism Of Action ◽  
Ribonucleotide Reductase ◽  
Antimalarial Activity ◽  
Iron Chelators ◽  
Resistant Clone ◽  
Iron Deprivation ◽  
Level Of Activity ◽  
Susceptible Clone

The activities of novel iron chelators, alone and in combination with chloroquine, quinine, or artemether, were evaluated in vitro against susceptible and resistant clones of Plasmodium falciparum with a semimicroassay system. N4-nonyl,N1,N8-bis(2,3-dihydroxybenzoyl) spermidine hydrobromide (compound 7) demonstrated the highest level of activity: 170 nM against a chloroquine-susceptible clone and 1 microM against a chloroquine-resistant clone (50% inhibitory concentrations). Compounds 6, 8, and 10 showed antimalarial activity with 50% inhibitory concentrations of about 1 microM. Compound 7 had no effect on the activities of chloroquine, quinine, and artemether against either clone, and compound 8 did not enhance the schizontocidal action of either chloroquine or quinine against the chloroquine-resistant clone. The incubation of compound 7 with FeCI3 suppressed or decreased the in vitro antimalarial activity of compound 7, while no effect was observed with incubation of compound 7 with CuSO4 and ZnSO4. These results suggest that iron deprivation may be the main mechanism of action of compound 7 against the malarial parasites. Chelator compounds 7 and 8 primarily affected trophozoite stages, probably by influencing the activity of ribonucleotide reductase, and thus inhibiting DNA synthesis.

scholarly journals Synthesis and in Vitro Antimalarial Activity of Alkyl Esters Gallate as a Growth Inhibitors of Plasmodium Falciparum

2018 ◽  
Vol 34 (2) ◽  
pp. 655-662 ◽  
Author(s):  
Ade Arsianti ◽  
Hendry Astuti ◽  
Fadilah Fadilah ◽  
Daniel Martin Simadibrata ◽  
Zoya Marie Adyasa ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Antimalarial Activity ◽  
Growth Inhibitors ◽  
Alkyl Esters

scholarly journals Overexpression of Plasmodium falciparum M1 Aminopeptidase Promotes an Increase in Intracellular Proteolysis and Modifies the Asexual Erythrocytic Cycle Development

Pathogens ◽  
2021 ◽  
Vol 10 (11) ◽  
pp. 1452
Author(s):  
Carolina C. Hoff ◽  
Mauro F. Azevedo ◽  
Adriana B. Thurler ◽  
Sarah El Chamy Maluf ◽  
Pollyana M. S. Melo ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Antimalarial Activity ◽  
Fold Increase ◽  
Cysteine Proteases ◽  
Aminopeptidase Activity ◽  
Lower Sensitivity ◽  
Wild Type ◽  
Erythrocytic Cycle ◽  
Transgenic Parasite

Plasmodium falciparum, the most virulent of the human malaria parasite, is responsible for high mortality rates worldwide. We studied the M1 alanyl-aminopeptidase of this protozoan (PfA-M1), which is involved in the final stages of hemoglobin cleavage, an essential process for parasite survival. Aiming to help in the rational development of drugs against this target, we developed a new strain of P. falciparum overexpressing PfA-M1 without the signal peptide (overPfA-M1). The overPfA-M1 parasites showed a 2.5-fold increase in proteolytic activity toward the fluorogenic substrate alanyl-7-amido-4-methylcoumarin, in relation to the wild-type group. Inhibition studies showed that overPfA-M1 presented a lower sensitivity against the metalloaminopeptidase inhibitor bestatin and to other recombinant PfA-M1 inhibitors, in comparison with the wild-type strain, indicating that PfA-M1 is a target for the in vitro antimalarial activity of these compounds. Moreover, overPfA-M1 parasites present a decreased in vitro growth, showing a reduced number of merozoites per schizont, and also a decrease in the iRBC area occupied by the parasite in trophozoite and schizont forms when compared to the controls. Interestingly, the transgenic parasite displays an increase in the aminopeptidase activity toward Met-, Ala-, Leu- and Arg-7-amido-4-methylcoumarin. We also investigated the potential role of calmodulin and cysteine proteases in PfA-M1 activity. Taken together, our data show that the overexpression of PfA-M1 in the parasite cytosol can be a suitable tool for the screening of antimalarials in specific high-throughput assays and may be used for the identification of intracellular molecular partners that modulate their activity in P. falciparum.

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