Synthesis and Antiplasmodial Activity of 4-Alkylidene(arylidene)hydrazono-1,3-oxazinan-2-ones and 3-Hydroxy-N'-alkylidene(arylidene)propanehydrazonamides

2010 ◽  
Vol 63 (10) ◽  
pp. 1430 ◽  
Author(s):  
Mehdi Khankischpur ◽  
Rolf D. Walter ◽  
Thomas Kurz
Keyword(s):  
Plasmodium Falciparum ◽  
Sensitive Strain ◽  
Antiplasmodial Activity ◽  
Ic50 Value

Previously unreported 6-substituted 4-alkylidene(arylidene)hydrazono-1,3-oxazinan-2-ones and a series of open-chained 3-hydroxy-N′-alkylidene(arylidene)propanehydrazonamides were synthesized and evaluated for their in vitro antiplasmodial activity. The most active 3-hydroxy-N′-alkylidene(arylidene)propanehydrazonamide exhibits potent in vitro antiplasmodial activity against the chloroquine-sensitive strain 3D7 of Plasmodium falciparum and demonstrates an IC50 value of 0.2 µM.

scholarly journals THE EFFECT OF MALACCA LEAVES (Phyllantus emblica) ETHANOLIC EXTRACT ON Plasmodium falciparum GROWTH IN VITRO

2018 ◽  
Vol 12 (4) ◽  
Author(s):  
Nuzul Asmilia ◽  
T Armansyah TR ◽  
Dwinna Aliza ◽  
Juli Melia ◽  
Erdiansyah Rahmi ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Ethanolic Extract ◽  
Negative Control Group ◽  
Positive Control ◽  
Negative Control ◽  
Probit Analysis ◽  
Antiplasmodial Activity ◽  
Control Group ◽  
Ic50 Value

The aim of this research was to find out in vitro antiplasmodium activity of Malacca leaves (Phyllantus emblica) ethanolic extract against Plasmodium falciparum growth. In this study, Plasmodium culture contained 5% parasitemia in ring stage was cultured using candle jar method and antiplasmodial activity test was carried out using microculture. The treatments were divided into 7 groups with four repetitions. K1 as negative control group was given Roswell Park Memorial Institute (RPMI), while K2 as positive control group was given artesdiaquine. Groups K3, K4, K5, K6, and K7 group was added with 100 µg/mL, 75 µg/mL, 50 µg/mL, 25 µg/mL, and 5 µg/mL of Malacca leaves ethanolic extract, respectively. Antiplasmodial activity was determined by inhibition concentration of 50% parasite growth (IC50). The data were analyzed using ANOVA and followed by Duncan test. The average of parasitemia level in group K1, K2, K3, K4, K5, K6, and K7 were 55.25±15.62, 8.50±2.52, 8.50±3.00, 9.25±0.95, 9.00±2.70, 9.79±2.06, and 10.75±2.22, respectively. The average of inhibition percentage in group K1, K2; K3; K4; K5; K6; and K7 were 0.00±0.00%, 84.62±4.55%; 84.62±5.43%; 83.26±1.73%; 83.71±4,90%; 82.35±3,73%; and 80.54±6.83%, respectively (P0.01). The results showed that the administration of malacca leaves ethanolic extract significantly affect (P0.01) the inhibition of Plasmodium growth as compared to group K1 (negative control). Probit analysis reveals the IC50 value was 3.889 µg/mL. In conclusion, all doses of malacca leaves ethanolic extract used in this study was able to inhibit Plasmodium falciparum growth with IC50 value was 3.889 µg/mL.

Fucoxanthin, Tetraprenylated Toluquinone and Toluhydroquinone Metabolites from Sargassum heterophyllum Inhibit the in vitro Growth of the Malaria Parasite Plasmodium falciparum

2008 ◽  
Vol 63 (11-12) ◽  
pp. 848-852 ◽  
Author(s):  
Anthonia F. Afolayan ◽  
John J. Bolton ◽  
Carmen A. Lategan ◽  
Peter J. Smith ◽  
Denzil R. Beukes
Keyword(s):  
Plasmodium Falciparum ◽  
South African ◽  
Malaria Parasite ◽  
Marine Algae ◽  
Sensitive Strain ◽  
Antiplasmodial Activity ◽  
In Vitro Growth ◽  
Parasite Plasmodium ◽  
Parasite Plasmodium Falciparum

Abstract In the course of our search for antimalarial leads from marine algae, four metabolites, sargaquinoic acid, sargahydroquinoic acid, sargaquinal and fucoxanthin, were isolated from the South African alga Sargassum heterophyllum. Fucoxanthin and sargaquinal showed good antiplasmodial activity toward a chloroquine-sensitive strain (D10) of Plasmodium falciparum (IC50 1.5 and 2.0 μm, respectively), while sargaquinoic acid and sargahydroquinoic acid were only moderately active (IC50 12.0 and 15.2 μm, respectively).

scholarly journals In vitro Assessment of Antiplasmodial Activity and Acute Oral Toxicity of Dissotis rotundifolia Extracts and Fractions on Plasmodium falciparum Strains

2020 ◽  
pp. 8-19
Author(s):  
Rock Djehoue ◽  
Rafiou Adamou ◽  
Abdou Madjid O. Amoussa ◽  
Adande A. Medjigbodo ◽  
Anatole Laleye ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Acute Toxicity ◽  
Ethanolic Extract ◽  
Antiplasmodial Activity ◽  
Oral Toxicity ◽  
Aqueous Fraction ◽  
Vector Borne Diseases ◽  
Natural Substances ◽  
Study Laboratory

Aim: Dissotis rotundifolia were selected after an ethnopharmacological survey conducted on plants used traditionally for malaria treatment in South Benin, with the aim of discovering new natural active extracts against malaria parasites. Place and Duration of Study: Laboratory of Biochemistry and Bioactive Natural Substances, University of Abomey-Calavi (Benin)/ Laboratory of Infectious Vector Borne Diseases, Regional Institute of Public Health (Benin)/ Laboratoire d’Histologie, de Cytogénétique et d’Embryologie, Faculté des Sciences de la Santé (Benin). The study was conduct from October 2018 to June 2019 in Benin. Methodology: The antiplasmodial activity of the plant extracts was evaluated using the parasite lactate dehydrogenase (pLDH) immunodetection assay. The extract with the best antiplasmodial activity were used on Wistar rats for acute toxicity. Results: Ethanolic extract of Dissotis rotundifolia showed promising activity (Isolate: IC50 = 22.58 ± 1.12 µg/mL; 3D7: IC50 = 6.81 ± 0.85 µg/mL) on Plasmodium falciparum compared to the aqueous extract (Isolate: IC50 > 100 µg/mL; 3D7: IC50> 100 µg/mL). The aqueous fraction of D. rotundifolia exhibit highly potent activity against P. falciparum strain (Isolate: IC50 > 100 µg/mL μg/mL; 3D7: IC50 = 4.05 ± 0.72 μg/mL). Haemolytic effect of actives extracts and fractions is less than 5%. Ethanolic extract of D. rotundifolia revealed no obvious acute toxicity in rat up to the highest dose administered (2000 mg/kg). Conclusion: This study justifies traditional uses of D. rotundifolia against malaria. A bioguided fractionation of these extracts would identify molecules responsible for their antiplasmodial activity. Moreover, these results could lead to the design of improved traditional medicines in the basis of this plant.

scholarly journals Boromycin has Rapid-Onset Antibiotic Activity Against Asexual and Sexual Blood Stages of Plasmodium falciparum

2022 ◽  
Vol 11 ◽  
Author(s):  
Laís Pessanha de Carvalho ◽  
Sara Groeger-Otero ◽  
Andrea Kreidenweiss ◽  
Peter G. Kremsner ◽  
Benjamin Mordmüller ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Plasmodium Knowlesi ◽  
Rapid Onset ◽  
Multidrug Resistant ◽  
Antiplasmodial Activity ◽  
Onset Of Action ◽  
Streptomyces Antibioticus ◽  
Life Cycle Stages ◽  
Almost All

Boromycin is a boron-containing macrolide antibiotic produced by Streptomyces antibioticus with potent activity against certain viruses, Gram-positive bacteria and protozoan parasites. Most antimalarial antibiotics affect plasmodial organelles of prokaryotic origin and have a relatively slow onset of action. They are used for malaria prophylaxis and for the treatment of malaria when combined to a fast-acting drug. Despite the success of artemisinin combination therapies, the current gold standard treatment, new alternatives are constantly needed due to the ability of malaria parasites to become resistant to almost all drugs that are in heavy clinical use. In vitro antiplasmodial activity screens of tetracyclines (omadacycline, sarecycline, methacycline, demeclocycline, lymecycline, meclocycline), macrolides (oleandomycin, boromycin, josamycin, troleandomycin), and control drugs (chloroquine, clindamycin, doxycycline, minocycline, eravacycline) revealed boromycin as highly potent against Plasmodium falciparum and the zoonotic Plasmodium knowlesi. In contrast to tetracyclines, boromycin rapidly killed asexual stages of both Plasmodium species already at low concentrations (~ 1 nM) including multidrug resistant P. falciparum strains (Dd2, K1, 7G8). In addition, boromycin was active against P. falciparum stage V gametocytes at a low nanomolar range (IC50: 8.5 ± 3.6 nM). Assessment of the mode of action excluded the apicoplast as the main target. Although there was an ionophoric activity on potassium channels, the effect was too low to explain the drug´s antiplasmodial activity. Boromycin is a promising antimalarial candidate with activity against multiple life cycle stages of the parasite.

scholarly journals In vitro antiplasmodial activity of Phyllanthus amarus against Plasmodium falciparum and evaluation of its acute toxicity effect in mouse model

2021 ◽  
Vol 11 (1) ◽  
pp. 31
Author(s):  
Yusuf Mohammed ◽  
Karimatu Aliyu ◽  
IdrisNasir Abdullahi ◽  
AminaAbdullahi Umar ◽  
Fatima Bashir ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Acute Toxicity ◽  
Mouse Model ◽  
Antiplasmodial Activity ◽  
Phyllanthus Amarus ◽  
Toxicity Effect

scholarly journals In Vitro Assessment of Antiplasmodial Activity and Cytotoxicity of Polyalthia longifolia Leaf Extracts on Plasmodium falciparum Strain NF54

2019 ◽  
Vol 2019 ◽  
pp. 1-9 ◽  
Author(s):  
Bethel Kwansa-Bentum ◽  
Kojo Agyeman ◽  
Jeffrey Larbi-Akor ◽  
Claudia Anyigba ◽  
Regina Appiah-Opong
Keyword(s):  
Plasmodium Falciparum ◽  
Ethyl Acetate ◽  
Red Blood Cells ◽  
Blood Cells ◽  
Radical Scavenging ◽  
Antimalarial Drugs ◽  
Antiplasmodial Activity ◽  
Leaf Extracts ◽  
Polyalthia Longifolia

Background. Malaria is one of the most important life-threatening infectious diseases in the tropics. In spite of the effectiveness of artemisinin-based combination therapy, reports on reduced sensitivity of the parasite to artemisinin in Cambodia and Thailand warrants screening for new potential antimalarial drugs for future use. Ghanaian herbalists claim that Polyalthia longifolia has antimalarial activity. Therefore, antiplasmodial activity, cytotoxic effects, and antioxidant and phytochemical properties of P. longifolia leaf extract were investigated in this study. Methodology/Principal Findings. Aqueous, 70% hydroethanolic and ethyl acetate leaf extracts were prepared using standard procedures. Antiplasmodial activity was assessed in vitro by using chloroquine-sensitive malaria parasite strain NF54. The SYBR® Green and tetrazolium-based calorimetric assays were used to measure parasite growth inhibition and cytotoxicity, respectively, after extract treatment. Total antioxidant activity was evaluated using a free radical scavenging assay. Results obtained showed that extracts protected red blood cells against Plasmodium falciparum mediated damage. Fifty percent inhibitory concentration (IC50) values were 24.0±1.08 μg/ml, 22.5±0.12 μg/ml, and 9.5±0.69 μg/ml for aqueous, hydroethanolic, and ethyl acetate extracts, respectively. Flavonoids, tannins, and saponins were present in the hydroethanolic extract, whereas only the latter was observed in the aqueous extract. Aqueous and hydroethanolic extracts showed stronger antioxidant activities compared to the ethyl acetate extract. Conclusions/Significance. The extracts of P. longifolia have antiplasmodial properties and low toxicities to human red blood cells. The extracts could be developed as useful alternatives to antimalarial drugs. These results support claims of the herbalists that decoctions of P. longifolia are useful antimalarial agents.

In vitro antiplasmodial activity of aqueous extracts of Ochna schweinfurthiana leaf on Plasmodium falciparum

2018 ◽  
Vol 14 (2) ◽  
pp. 269
Author(s):  
Babasoji P. Omoniwa ◽  
Titilayo O. Johnson ◽  
Omolola Soji-Omoniwa ◽  
Istifanus Gurumtet ◽  
Ruth A. Manzah
Keyword(s):  
Plasmodium Falciparum ◽  
Antiplasmodial Activity ◽  
Aqueous Extracts

Antiplasmodial activity of short peptide-based compounds

RSC Advances ◽  
2015 ◽  
Vol 5 (29) ◽  
pp. 22674-22684 ◽  
Author(s):  
Amit Mahindra ◽  
Rahul P. Gangwal ◽  
Sunil Bansal ◽  
Nathan E. Goldfarb ◽  
Ben M. Dunn ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Antiplasmodial Activity ◽  
Short Peptide

Three series of short peptide-based compounds were synthesized, which upon evaluation against chloroquine-sensitive (D6) and chloroquine-resistant (W2) strains ofPlasmodium falciparum in vitro, produced IC50values ranging between 1.4–4.7 μg mL−1.

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