In Vitro Antiplasmodial Activity of Extracts ofTristaniopsisSpecies and Identification of the Active Constituents:  Ellagic Acid and 3,4,5-Trimethoxyphenyl-(6‘-O-galloyl)-O-β-d-glucopyranoside

2001 ◽  
Vol 64 (5) ◽  
pp. 603-607 ◽  
Author(s):  
Luisella Verotta ◽  
Mario Dell'Agli ◽  
Andrea Giolito ◽  
Marco Guerrini ◽  
Pierre Cabalion ◽  
...  
Keyword(s):  
Ellagic Acid ◽  
Antiplasmodial Activity ◽  
Active Constituents

scholarly journals Ellagic Acid Derivatives from Syzygium cumini Stem Bark: Investigation of their Antiplasmodial Activity

2009 ◽  
Vol 4 (10) ◽  
pp. 1934578X0900401 ◽  
Author(s):  
Claudia A. Simões-Pires ◽  
Sandra Vargas ◽  
Andrew Marston ◽  
Jean-Robert Ioset ◽  
Marçal Q. Paulo ◽  
...  
Keyword(s):  
Mechanism Of Action ◽  
Ellagic Acid ◽  
Stem Bark ◽  
Antimalarial Drugs ◽  
Antiplasmodial Activity ◽  
Hydroxyl Groups ◽  
Syzygium Cumini ◽  
Free Hydroxyl ◽  
Ellagic Acid Derivatives

Bioguided fractionation of Syzygium cumini (Myrtaceae) bark decoction for antiplasmodial activity was performed, leading to the isolation of three known ellagic acid derivatives (ellagic acid, ellagic acid 4-O-α-L-2″-acetylrhamnopyranoside, 3-O-methylellagic acid 3′-O-α-L-rhamnopyranoside), as well as the new derivative 3-O-methylellagic acid 3′-O-β-D-glucopyranoside. Activity investigation was based on the reduction of P. falciparum (PfK1) parasitaemia in vitro and the inhibition of β-hematin formation, a known mechanism of action of some antimalarial drugs. Among the investigated ellagic acid derivatives, only ellagic acid was able to reduce P. falciparum parasitaemia in vitro and inhibit β-hematin formation, suggesting that free hydroxyl groups are necessary for activity within this class of compounds.

scholarly journals Compounds Structurally Related to Ellagic Acid Show Improved Antiplasmodial Activity

2008 ◽  
Vol 53 (2) ◽  
pp. 622-630 ◽  
Author(s):  
Nicole Sturm ◽  
Ying Hu ◽  
Herbert Zimmermann ◽  
Karin Fritz-Wolf ◽  
Sergio Wittlin ◽  
...  
Keyword(s):  
Ellagic Acid ◽  
A549 Cells ◽  
Antiplasmodial Activity ◽  
In Vivo Studies ◽  
Hydroxyl Groups ◽  
Redox Enzymes ◽  
Trophozoite Stage ◽  
Antioxidant Genes ◽  
Nanomolar Range

ABSTRACT The cancer chemopreventive agent ellagic acid (EA) is a known inhibitor of glutathione S-transferases (GSTs) and possesses antiplasmodial activities in the upper-nanomolar range. In the recent drug development approach, the properties of the active site of Plasmodium falciparum GST were exploited for inhibitor design by introducing one or two additional hydroxyl groups into EA, yielding flavellagic acid (FEA) and coruleoellagic acid (CEA), respectively. Indeed, the inhibition of P. falciparum GST was improved with the increasing hydrophilicity of the planar polyaromatic ring system. Studying the effects of the two compounds on the central redox enzymes of Plasmodium revealed that glutathione reductase and thioredoxin reductase also are inhibited in the lower-micromolar range. Both compounds had strong antiplasmodial activity in the lower-nanomolar range and were particularly effective against chloroquine (CQ)-resistant P. falciparum strains. Neither FEA nor CEA showed cytotoxic effects on human cells. This was supported by negligible changes in transcript levels and enzyme activities of redox enzymes in human A549 cells upon treatment with the compounds. In Plasmodium, however, CEA treatment resulted in a marked downregulation of most antioxidant genes studied and impaired mainly the trophozoite stage of the parasites. In addition, EA, CEA, and FEA were found to strongly inhibit in vitro heme aggregation. In vitro and preliminary in vivo studies indicated that, compared to CQ, CEA is a slowly acting compound and is able to significantly improve the survival of Plasmodium berghei-infected mice. We conclude that FEA and CEA are promising antimalarial compounds that deserve to be studied further.

In vitro antiplasmodial activity of extracts of Alchornea cordifolia and identification of an active constituent: ellagic acid

2002 ◽  
Vol 81 (3) ◽  
pp. 399-401 ◽  
Author(s):  
J.-T Banzouzi ◽  
R Prado ◽  
H Menan ◽  
A Valentin ◽  
C Roumestan ◽  
...  
Keyword(s):  
Ellagic Acid ◽  
Antiplasmodial Activity ◽  
Active Constituent

Synthesis of Novel 1,2,3-Triazole Derivatives of Isocoumarins and 3,4-Dihydroisocoumarin with Potential Antiplasmodial Activity In Vitro

2020 ◽  
Vol 16 ◽  
Author(s):  
Lucas da Silva Santos ◽  
Matheus Fillipe Langanke de Carvalho ◽  
Ana Claudia de Souza Pinto ◽  
Amanda Luisa da Fonseca ◽  
Julio César Dias Lopes ◽  
...  
Keyword(s):  
Triazole Ring ◽  
Antiplasmodial Activity ◽  
World Health ◽  
Dipolar Cycloaddition ◽  
Terminal Alkynes ◽  
The World ◽  
Ic50 Values ◽  
Derivatives Of ◽  
Active Substances

Background: Malaria greatly affects the world health, having caused more than 228 million cases only in 2018. The emergence of drug resistance is one of the main problems in its treatment, demonstrating the urge for the development of new antimalarial drugs. Objective: Synthesis and in vitro antiplasmodial evaluation of triazole compounds derived from isocoumarins and a 3,4- dihydroisocoumarin. Method: The compounds were synthesized in 4 to 6-step reactions with the formation of the triazole ring via the Copper(I)-catalyzed 1,3-dipolar cycloaddition between isocoumarin or 3,4-dihydroisocoumarin azides and terminal alkynes. This key reaction provided compounds with an unprecedented connection of isocoumarin or 3,4-dihydroisocoumarin and the 1,2,3-triazole ring. The products were tested for their antiplasmodial activity against a Plasmodium falciparum chloroquine resistant and sensitive strains (W2 and 3D7, respectively). Results: Thirty-one substances were efficiently obtained by the proposed routes with an overall yield of 25-53%. The active substances in the antiplasmodial test displayed IC50 values ranging from 0.68-2.89 μM and 0.85-2.07 μM against W2 and 3D7 strains, respectively.

In vitro and in vivo antiplasmodial activity of novel quinoline derivative compounds by molecular hybridization

2021 ◽  
Vol 215 ◽  
pp. 113271
Author(s):  
Juliane Aparecida Marinho ◽  
Daniel Silqueira Martins Guimarães ◽  
Nícolas Glanzmann ◽  
Giovana de Almeida Pimentel ◽  
Izabelle Karine da Costa Nunes ◽  
...  
Keyword(s):  
Quinoline Derivative ◽  
Antiplasmodial Activity ◽  
Molecular Hybridization

scholarly journals Identification of the Active Ingredient and Beneficial Effects of Vitex rotundifolia Fruits on Menopausal Symptoms in Ovariectomized Rats

Biomolecules ◽  
2021 ◽  
Vol 11 (7) ◽  
pp. 1033
Author(s):  
Ji Hwan Lee ◽  
Sullim Lee ◽  
Quynh Nhu Nguyen ◽  
Hung Manh Phung ◽  
Myoung-Sook Shin ◽  
...  
Keyword(s):  
Weight Gain ◽  
Body Weight Gain ◽  
Animal Experiments ◽  
Ovariectomized Rats ◽  
Biological Functions ◽  
Menopausal Syndrome ◽  
Active Constituents ◽  
Mcf 7

Estrogen replacement therapy is a treatment to relieve the symptoms of menopause. Many studies suggest that natural bioactive ingredients from plants resemble estrogen in structure and biological functions and can relieve symptoms of menopause. The fruit of V. rotundifolia, called “Man HyungJa” in Korean, is a traditional medicine used to treat headache, migraine, eye pain, neuralgia, and premenstrual syndrome in Korea and China. The aim of the present study was to confirm that V. rotundifolia fruit extract (VFE) exerts biological functions similar to those of estrogen in menopausal syndrome. We investigated its in vitro effects on MCF-7 cells and in vivo estrogen-like effects on weight gain and uterine contraction in ovariectomized rats. Using the polar extract, the active constituents of VFE (artemetin, vitexicarpin, hesperidin, luteolin, vitexin, and vanillic acid) with estrogen-like activity were identified in MCF-7 cells. In animal experiments, the efficacy of VFE in ameliorating body weight gain was similar to that of estrogen, as evidenced from improvements in uterine atrophy. Vitexin and vitexicarpin are suggested as the active constituents of V. rotundifolia fruits.

scholarly journals Assessment of Antimalarial Activity againstPlasmodium falciparumand Phytochemical Screening of Some Yemeni Medicinal Plants

2009 ◽  
Vol 6 (4) ◽  
pp. 453-456 ◽  
Author(s):  
Mohammed A. Alshawsh ◽  
Ramzi A. Mothana ◽  
Hassan A. Al-shamahy ◽  
Salah F. Alsllami ◽  
Ulrike Lindequist
Keyword(s):  
Medicinal Plants ◽  
Antimalarial Activity ◽  
Traditional Healers ◽  
Antiplasmodial Activity ◽  
World Health ◽  
Moderate Activity ◽  
Phytochemical Screening ◽  
Cissus Rotundifolia ◽  
Health Organization

Developing countries, where malaria is one of the most prevalent diseases, still rely on traditional medicine as a source for the treatment of this disease. In the present study, six selected plants (Acalypha fruticosa,Azadirachta indica,Cissus rotundifolia,Echium rauwalfii,Dendrosicyos socotranaandBoswellia elongata) commonly used in Yemen by traditional healers for the treatment of malaria as well as other diseases, were collected from different localities of Yemen, dried and extracted with methanol and water successfully. The antiplasmodial activity of the extracts was evaluated against fresh clinical isolates ofPlasmodium falciparum. The selectivity parameters to evaluate the efficacy of these medicinal plants were measured byin vitromicro test (Mark III) according to World Health Organization (WHO) 1996 & WHO 2001 protocols of antimalarial drug tests. Among the investigated 12 extracts, three were found to have significant antiplasmodial activity with IC50values less than 4 µg/ml, namely the water extracts ofA. fruticosa,A. indicaandD. socotrana. Six extracts showed moderate activity with IC50values ranging from 10 to 30 µg/ml and three appeared to be inactive with IC50values more than 30 µg/ml. In addition, preliminary phytochemical screening of the methanolic and aqueous extracts indicated the presence of saponins, tannins, flavonoids, terpenoids, polysaccharides and peptides.

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