The host targeting effect of chloroquine in malaria

Coban, Cevayir

doi:10.1016/j.coi.2020.07.005

Cited by 50 publications

(38 citation statements)

References 67 publications

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“…Currently, the treatment with artemisinin-based combination therapies, a sesquiterpene lactone firstly isolated from Artemisia annua, is the most used in almost all endemic malaria regions (WHO 2021a). However, artemisinin-based combination therapies are quickly failing across South-East Asia due to the identification of locally Plasmodium resistance strains (Pasupureddy et al 2019;Coban 2020). M. balsamina is widely used to treat fever symptoms associated with malaria in some African countries, namely Mozambique (Bandeira et al 2001).…”

Section: P-glycoprotein Modulation Activitymentioning

confidence: 99%

Momordica balsamina: phytochemistry and pharmacological potential of a gifted species

et al. 2022

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Momordica balsamina L. (Cucurbitaceae), frequently named balsam apple, southern balsam pear or African pumpkin, is a vegetable with high nutritional value, being mostly used as food in sub-Saharan Africa. It has also been largely used in traditional medicine to treat several diseases, such as malaria fevers and diabetes. As a member of the Cucurbitaceae family, the main constituents are cucurbitane-type triterpenoids, with different oxidation patterns, named cucurbitacins. This review aims at summarizing our contribution to the phytochemical study of M. balsamina and the evaluation of the isolated cucurbitacins and derivatives as multidrug resistance reversers in cancer cells and bacteria. In this way, the selective antiproliferative activity against multidrug resistant cancer cells of cucurbitacins obtained from M. balsamina, their ability as P-glycoprotein inhibitors in cancer cells overexpressing this ABC transporter, as well as efflux pump inhibitors in resistant bacteria strains are reviewed. Moreover, the in vitro antimalarial activity of cucurbitacins and acyl derivatives against the blood and liver-stages of Plasmodium strains, and the in vivo activity of selected compounds is also reviewed. Besides our work, edible and medicinal uses, and other studies mainly reporting the biological activities of M. balsamina extracts, such as antidiabetic, antibacterial, anti-inflammatory, and antioxidant properties are also addressed.

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Section: P-glycoprotein Modulation Activitymentioning

confidence: 99%

Momordica balsamina: phytochemistry and pharmacological potential of a gifted species

et al. 2022

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“…Chloroquine has been used for malaria treatment and prophylaxis (Coban, 2020). During the Severe Acute Respiratory Syndrome (SARS) pandemic in 2002-2004, chloroquine was reported to inhibit SARS coronavirus (SARS-CoV-1) (Keyaerts et al, 2004).…”

Section: Introductionmentioning

confidence: 99%

COVID-19 Drugs Chloroquine and Hydroxychloroquine, but Not Azithromycin and Remdesivir, Block hERG Potassium Channels

Szendrey

Guo

et al. 2021

J Pharmacol Exp Ther

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Abbreviations: HEK, human embryonic kidney; hERG, human ether ago go related gene; IC 50 , half maximal inhibitory concentration; I hERG , hERG current; I Kr , rapidly activating delayed rectifier potassium current; I Ks , slowly activating delayed rectifier K + current; LQTS, long QT syndrome; MEM, minimum essential medium; QT c , corrected QT interval; V 1/2 , voltage of half maximal activation. CQ, chloroquine; HCQ, hydroxychloroquine; AZ, azithromycin; RDV, remdesivir.

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“…Recently however, chloroquine was shown to exhibit not only anti-parasitic activity but also anti-inflammatory properties and thus may directly affect the host immune system [ 42 ]. The mechanism of host-mediated response due to chloroquine is however still not fully understood [ 58 ]. Immune mechanisms associated with chloroquine treatment can be different between human and animal infections.…”

Section: Discussionmentioning

confidence: 99%

Dual Anti-Malarial and GSK3β-Mediated Cytokine-Modulating Activities of Quercetin Are Requisite of Its Potential as a Plant-Derived Therapeutic in Malaria

et al. 2021

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Although death in malaria is attributed to cerebrovascular blockage and anaemia, overwhelming cytokine production can contribute to the severity of the disease. Therefore, mitigation of dysregulated inflammatory signalling may provide further benefit for malaria treatment. Quercetin (3,3′,4′,5,7-pentahydroxyflavone) is known to inhibit glycogen synthase kinase-3β (GSK3β), a potent regulator of both pro- and anti-inflammatory effects. Quercetin is therefore a potential therapeutic to modulate the imbalanced cytokine production during malarial infection. Anti-malarial effects of quercetin were evaluated in murine models of severe and cerebral malaria using Plasmodium berghei NK65 and ANKA strains, respectively. Western blotting and analysis of cytokines were carried out to determine the GSK3β-mediated cytokine-modulating effects of quercetin in infected animals. Quercetin (25 mg/kg BW) treatment in P. berghei NK65-infected animals resulted in 60.7 ± 2.4% suppression of parasitaemia and significantly decreased serum levels of TNF-α and IFN-γ, whilst levels of IL-10 and IL-4 were elevated significantly. Western analysis revealed that pGSK3β (Ser9) increased 2.7-fold in the liver of quercetin-treated NK65-infected animals. Treatment of P. berghei ANKA-infected mice with quercetin (15 mg/kg BW) increased (2.3-fold) pGSK3β (Ser9) in the brains of infected animals. Quercetin is a potential plant-derived therapeutic for malaria on the basis that it can elicit anti-malarial and GSK3β-mediated cytokine-modulating effects.

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The host targeting effect of chloroquine in malaria

Cited by 50 publications

References 67 publications

Momordica balsamina: phytochemistry and pharmacological potential of a gifted species

Momordica balsamina: phytochemistry and pharmacological potential of a gifted species

COVID-19 Drugs Chloroquine and Hydroxychloroquine, but Not Azithromycin and Remdesivir, Block hERG Potassium Channels

Dual Anti-Malarial and GSK3β-Mediated Cytokine-Modulating Activities of Quercetin Are Requisite of Its Potential as a Plant-Derived Therapeutic in Malaria

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