Advances in Antimalarial Drug Evaluation and New Targets for Antimalarials

Grellier, Philippe; Deregnaucourt, Christiane; Isabelle, Florent

doi:10.5772/34075

Cited by 5 publications

(4 citation statements)

References 138 publications

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“…53 Thus, the extract of A. polystachyus may possess appetite-suppressing activity which could be attributed to flavonoids, saponins, and phenolic compounds. 45,54,55 Notably, the present finding is in agreement with the previous finding. 45 However, the finding of the current study on body weight was not consistent with previous similar studies.…”

Section: Discussionsupporting

confidence: 94%

Anti-Oxidant Potential and Antimalarial Effects of Acanthus polystachyus Delile (Acanthaceae) Against Plasmodium berghei: Evidence for in vivo Antimalarial Activity

Kifle¹,

Atnafie²

2020

JEP

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Section: Discussionsupporting

confidence: 94%

Anti-Oxidant Potential and Antimalarial Effects of Acanthus polystachyus Delile (Acanthaceae) Against Plasmodium berghei: Evidence for in vivo Antimalarial Activity

Kifle¹,

Atnafie²

2020

JEP

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“…This might indicate that the plant could have an increased anorexic effect with escalating dose. This appetite suppressing activity of the extract might be ascribed to saponins, flavonoids, and phenolic compounds [43]. Importantly, this result is consistent with previous reports on hydro methanolic extract of Calpurnia aurea (Fabaceae), Dodonaea angustifolia and other plants [11,28,50].…”

Section: Discussionsupporting

confidence: 92%

Antimalarial Activity of Crude Extract of Buddleja Polystachya Fresen (Buddlejacea) Against Plasmodium Berghei in Mice

Mohammed¹,

Abdulwuhab²,

Mohammed³

2016

IOSR

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Malaria is one of the most serious widespread diseases encountered by human and it is the second leading cause of death from infectious diseases next to HIV/AIDS in Africa. People, in several parts of the world, use different traditional medicines for treating malaria and it has been reported that the roots, leaves, and flowers of various species of Buddleja are used for the same purpose. The aim of the present study was, therefore, to evaluate in vivo and phytochemical screening of secondary metabolites, safety and antimalarial activity of the crude extractof Buddleja polystachy in mice. The animals were divided into 5 groups. The first group served as negative control and was administered with vehicle (0.2ml of distilled water). Group two (B100), three (B200) and four (B300) were administered 100, 200 and 300 mg/kg Buddleja polystachy extract, respectively. Group five served as positive control group and was administered with chloroquine (10mg/kg/day). Antimalarial activity was evaluated using 4-day suppressive assays against P. Berghei by orally administering the mice with either vehicle, various doses of the Buddleja polystachya extract or chloroquine, while safety study was performed using acute toxicity studies by administering 2000mg/kg of the Buddleja polystachya extract to non-infected mice.The effect of crude extract was was measured and analyzed using One-way ANOVA and paired t-test. The result showed that the extracts did not caused symptoms of toxicity at the given doses. Preliminary phytochemical screening of the leaves powder of the plant indicated the presence of major antimalarial secondary metabolites. The extract of Buddleja polystachya leaves exerted dose dependent parasitemia suppression, although the active responsible principles are yet to be identified, which need further studies to elucidate the antimalarial mechanism of their action. It can be concluded that crude extracts of Buddleja polystachya showed strong activities against P. berghei indicating that it contains some chemical constituents that possibly lead to antimalarial drug development

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“…The increase of multiple resistances to classical antimalarials (e.g. quinolines and antifolates derivates) is becoming a major issue for public health [3,4]. Moreover, a decrease of sensitivity to artemisinin has already been reported in Western Cambodia [5,6].…”

Section: Introductionmentioning

confidence: 99%

“…The malaria parasite is a complex cell that contains (besides the plasma membrane) several membranes delimiting organelles such as the nucleus, endoplasmic reticulum, Golgi apparatus, vestigial plastid-like apicoplast, mitochondria and food/digestive vacuole [7]. These membranes contain several transporters that are responsible for essential cellular processes such as the movement of solutes across biological membranes, the regulation of essential nutrient uptake, ion homeostasis and the disposal of toxic waste, although transporters may also be part of the regulatory pathways [3,7]. Membrane transporters such as P-type ATPases are already utilized as specific and potent drug targets in several human diseases [7][8][9], irrespective of their location on the plasma membrane or in intracellular membranes [10].…”

Section: Introductionmentioning

confidence: 99%

Antimalarial screening via large‐scale purification of Plasmodium falciparum Ca²⁺‐ATPase 6 and in vitro studies

et al. 2013

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The most severe form of human malaria is caused by the parasite Plasmodium falciparum. Despite the current need, there is no effective vaccine and parasites are becoming resistant to most of the antimalarials available. Therefore, there is an urgent need to discover new drugs from targets that have not yet suffered from drug pressure with the aim of overcoming the problem of new emerging resistance. Membrane transporters, such as P. falciparum Ca2+‐ATPase 6 (PfATP6), the P. falciparum sarcoplasmic/endoplasmic reticulum Ca2+‐ATPase (SERCA), have been proposed as potentially good antimalarial targets. The present investigation focuses on: (a) the large‐scale purification of PfATP6 for maintenance of its enzymatic activity; (b) screening for PfATP6 inhibitors from a compound library; and (c) the selection of the best inhibitors for further tests on P. falciparum growth in vitro. We managed to heterologously express in yeast and purify an active form of PfATP6 as previously described, although in larger amounts. In addition to some classical SERCA inhibitors, a chemical library of 1680 molecules was screened. From these, we selected a pool of the 20 most potent inhibitors of PfATP6, presenting half maximal inhibitory concentration values in the range 1–9 μm. From these, eight were chosen for evaluation of their effect on P. falciparum growth in vitro, and the best compound presented a half maximal inhibitory concentration of ~ 2 μm. We verified the absence of an inhibitory effect of most of the compounds on mammalian SERCA1a, representing a potential advantage in terms of human toxicity. The present study describes a multidisciplinary approach allowing the selection of promising PfATP6‐specific inhibitors with good antimalarial activity.

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Advances in Antimalarial Drug Evaluation and New Targets for Antimalarials

Cited by 5 publications

References 138 publications

<p>Anti-Oxidant Potential and Antimalarial Effects of <em>Acanthus polystachyus Delile</em> (Acanthaceae) Against <em>Plasmodium berghei</em>: Evidence for in vivo Antimalarial Activity</p>

<p>Anti-Oxidant Potential and Antimalarial Effects of <em>Acanthus polystachyus Delile</em> (Acanthaceae) Against <em>Plasmodium berghei</em>: Evidence for in vivo Antimalarial Activity</p>

Antimalarial Activity of Crude Extract of Buddleja Polystachya Fresen (Buddlejacea) Against Plasmodium Berghei in Mice

Antimalarial screening via large‐scale purification of Plasmodium falciparum Ca²⁺‐ATPase 6 and in vitro studies

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Advances in Antimalarial Drug Evaluation and New Targets for Antimalarials

Cited by 5 publications

References 138 publications

<p>Anti-Oxidant Potential and Antimalarial Effects of <em>Acanthus polystachyus Delile</em> (Acanthaceae) Against <em>Plasmodium berghei</em>: Evidence for in vivo Antimalarial Activity</p>

<p>Anti-Oxidant Potential and Antimalarial Effects of <em>Acanthus polystachyus Delile</em> (Acanthaceae) Against <em>Plasmodium berghei</em>: Evidence for in vivo Antimalarial Activity</p>

Antimalarial Activity of Crude Extract of Buddleja Polystachya Fresen (Buddlejacea) Against Plasmodium Berghei in Mice

Antimalarial screening via large‐scale purification of Plasmodium falciparum Ca2+‐ATPase 6 and in vitro studies

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Antimalarial screening via large‐scale purification of Plasmodium falciparum Ca²⁺‐ATPase 6 and in vitro studies