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chloroquine

In Vivo Efficacy and Metabolism of the Antimalarial Cycleanine and Improved In Vitro Antiplasmodial Activity of Semisynthetic Analogues

October 30, 2021 - 12:39 -- Open Access
Author(s): 
Uche FI, Guo X, Okokon J, Ullah I, Horrocks P, Boateng J, Huang C, Li WW
Reference: 
Antimicrob Agents Chemother. 2021 Jan 20;65(2):e01995-20

Bisbenzylisoquinoline (BBIQ) alkaloids are a diverse group of natural products that demonstrate a range of biological activities. In this study, the in vitro antiplasmodial activity of three BBIQ alkaloids (cycleanine [compound 1], isochondodendrine [compound 2], and 2'-norcocsuline [compound 3]) isolated from the Triclisia subcordata Oliv. medicinal plant traditionally used for the treatment of malaria in Nigeria are studied alongside two semisynthetic analogues (compounds 4 and 5) of cycleanine. The antiproliferative effects against a chloroquine-resistant Plasmodium falciparum strain were determined using a SYBR green 1 fluorescence assay.

NOT Open Access | The return of chloroquine-sensitive Plasmodium falciparum parasites in Jazan region, southwestern Saudi Arabia over a decade after the adoption of artemisinin-based combination therapy: analysis of genetic mutations in the pfcrt gene

September 30, 2021 - 11:08 -- NOT Open Access
Author(s): 
Madkhali AM, Abdulhaq AA, Atroosh WM, Ghzwani AH, Zain KA, Ghailan KY, Hamali HA, Mobarki AA, Eisa ZM, Lau YL, Al-Mekhlafi HM
Reference: 
Parasitol Res. 2021 Sep 25

This study investigated the polymorphism in the P. falciparum chloroquine resistance transporter (pfcrt) gene 11 years after chloroquine (CQ) cessation in Jazan region, southwestern Saudi Arabia. Two hundred and thirty-five P. falciparum isolates were amplified to detect mutations in the pfcrt gene. The pfcrt 76 T molecular marker for CQ resistance was detected in 66.4% (156/235) of the isolates, while the K76 CQ-sensitive wild type was detected in 33.6%. The pfcrt 74I and pfcrt 75E point mutations were each found to be present in 56.2% of isolates, while only four isolates (1.7%) were found to carry the pfcrt 72S mutation.

NOT Open Access | Chloroquine and hydroxychloroquine ototoxicity; potential implications for SARS-CoV-2 treatment. A brief review of the literature

September 1, 2021 - 17:38 -- NOT Open Access
Author(s): 
De Luca P, Scarpa A, De Bonis E, Cavaliere M, Viola P, Gioacchini FM, Ralli M, Ettore C, Claudia C
Reference: 
Am J Otolaryngol. 2021 Sep-Oct;42(5):102640

Current clinical evidences do not support any specific treatment against SARS-CoV-2. Chloroquine (CQ) and hydroxychloroquine (HCQ) are typically used in the treatment of rheumatoid arthritis, systemic lupus erythematosus and malaria; they have been considered for off-label and compassionate use in several countries against moderate to severe cases of COVID-19 and there's actually a massive demand of these two drugs. The aim of this paper is to briefly review the published literature, summarizing evidences about audiological implications after CQ and HCQ treatment.

NOT Open Access Antiplasmodial Effect of Nano Dendrimer G2 Loaded with Chloroquine in Mice Infected with Plasmodium berghei

August 17, 2021 - 14:26 -- NOT Open Access
Author(s): 
Elmi T, Ardestani MS, Motevalian M, Hesari AK, Hamzeh MS, Zamani Z, Tabatabaie F
Reference: 
Acta Parasitol. 2021 Aug 16

Malaria is a parasitic lethal disease caused by Plasmodium protozoa. The resistance and drugs’ side effects have led to numerous researches for alternative suitable drugs with better efficiency and lower toxicity.

NOT Open Access | Current and emerging strategies to combat antimalarial resistance

August 10, 2021 - 18:03 -- NOT Open Access
Author(s): 
Rasmussen C, Alonso P, Ringwald P
Reference: 
Expert Rev Anti Infect Ther. 2021 Aug 5

Since the spread of chloroquine resistance in Plasmodium falciparum in the 1960s, recommendations have been made on how to respond to antimalarial resistance. Only with the advent of artemisinin partial resistance were large scale efforts made in the Greater Mekong Subregion to carry out recommendations in a coordinated and well-funded manner. Independent emergence of parasites partially resistant to artemisinins has now been reported in Rwanda.

NOT Open Access | The Metabolomic Profiles of Sera of Mice Infected with Plasmodium berghei and Treated by Effective Fraction of Naja naja oxiana Using (1)H Nuclear Magnetic Resonance Spectroscopy

August 10, 2021 - 17:19 -- NOT Open Access
Author(s): 
Hajialiani F, Shahbazzadeh D, Maleki F, Elmi T, Tabatabaie F, Zamani Z
Reference: 
Acta Parasitol. 2021 Aug 6

The use of venom fractions from the Iranian cobra could be useful adjunct treatments of malaria with chloroquine. A metabolomic investigation with 1HNMR spectroscopy was conducted on an effective fraction tested earlier using Plasmodium berghei as an experimental murine model.

NOT Open Access | An in vitro study on the differentiated metabolic mechanism of chloroquine-resistant Plasmodium falciparum using high-resolution metabolomics

August 4, 2021 - 12:20 -- NOT Open Access
Author(s): 
Na J, Zhang J, Choe YL, Lim CS, Park YH
Reference: 
J Toxicol Environ Health A. 2021 Aug 1:1-16

Chloroquine (CQ) is an important drug used therapeutically for treatment of malaria. However, due to limited number of studies on metabolic targets of chloroquine (CQ), it is difficult to attribute mechanisms underlying resistance associated with usage of this drug. The present study aimed to investigate the metabolic signatures of CQ-resistant Plasmodium falciparum (PfDd2) compared to CQ-sensitive Plasmodium falciparum (Pf3D7).

NOT Open Access | Microwave-assisted synthesis of hybrid PABA-1,3,5-triazine derivatives as an antimalarial agent

July 28, 2021 - 14:09 -- NOT Open Access
Author(s): 
Kashyap A, Choudhury AAK, Saha A, Adhikari N, Ghosh SK, Shakya A, Patgiri SJ, Bhattacharyya DR, Singh UP, Bhat HR
Reference: 
J Biochem Mol Toxicol. 2021 Jul 27:e22860

The present manuscript deals with the development of novel p-aminobenzoic acid (PABA) associated 1,3,5-triazine derivatives as antimalarial agents. The molecules were developed via microwave-assisted synthesis and structures of compounds were ascertained via numerous analytical and spectroscopic techniques. The synthesized compounds were also subjected to ADMET analysis.

NOT Open Access | Chloroquine inhibits pro-inflammatory effects of heme on macrophages and invivo

July 28, 2021 - 14:06 -- NOT Open Access
Author(s): 
Silva RCMC, Tan L, Rodrigues DA, Prestes EB, Gomes CP, Gama AM, Oliveira PL, Paiva CN, Manoury B, Bozza MT
Reference: 
Free Radic Biol Med. 2021 Jul 22;173:104-116

Chloroquine has been used successfully to treat Malaria, including by chloroquine-resistant Plasmodium sp., indicating that it has effects on disease itself. Since heme has inflammatory effects and contributes to the pathogenesis of hemolytic diseases, we hypothesize that the anti-inflammatory effect of chloroquine is partially due to its inhibitory effect on heme-induced macrophage activation and on inflammatory tissue damage.

Effect of α-tocopheryloxy acetic acid, a vitamin E derivative mitocan, on the experimental infection of mice with Plasmodium yoelii

June 30, 2021 - 12:17 -- Open Access
Author(s): 
Kasumi Kawamura, Aiko Kume, Rika Umemiya-Shirafuji, Shunji Kasai and Hiroshi Suzuki
Reference: 
Malaria Journal 2021 20:280, 24 June 2021

Malaria parasites are known to be vulnerable to oxidative stress. In this study, the effects of the administration of α-tocopheryloxy acetic acid (α-TEA), which is a vitamin E analogue mitocan, on Plasmodium yoelii infection in mice were examined.

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