Chloroquine to fight COVID-19: A consideration of mechanisms and adverse effects?

Zhan, Xia; Dowell, Sharon; Shen, Ying; Lee, Dexter L.

doi:10.1016/j.heliyon.2020.e04900

Cited by 16 publications

(9 citation statements)

References 96 publications

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“…Side effects: Though potentially capable of inhibiting the virus, hydroxychlorine has been reported of inducing fulminant hepatic failure and ventricular arrhythmias [150] and causes more renal toxicity than chloroquine does [151]. Both these drugs have been associated with delayed action potential in the nerves and prolonged QT interval in myocytes [152].…”

Section: Antimalarial Drugs: Chloroquine and Hydroxychloroquine -Its Mode Of Action And Possible Side Effectsmentioning

confidence: 99%

Factors for COVID-19 Infection that Govern the Severity of Illness

Ghosh¹,

Sarkar

Sepay³

et al. 2021

SciMed. J.

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Coronaviruses have been posing a serious threat to mammals and birds and a new class of SARS-CoV is creating havoc to the world after its first incidence in Wuhan City in China in December 2019. These viruses are mainly responsible for causing serious respiratory tract infections which generally appear initially as the common cold and can be lethal just like SARS-CoV. The problems seem to vary and worsen from one person to another depending on age, gender, ethnicity, blood groups, host genetics, and associated comorbidities. Complications should also arise as this virus keeps mutating and evolving. This review points out the various underlying causes behind the severity of the illness and the mechanisms associated with it. This review will help society to understand the risks and severities associated with COVID-19. Individuals with health complexities and predispositions listed in this review are the most vulnerable in terms of severity and should take every possible measure to protect themselves from getting infected. As a consequence, this will lead to a decrease in mortality rates arising from COVID-19. Doi: 10.28991/SciMedJ-2021-0302-9 Full Text: PDF

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Section: Antimalarial Drugs: Chloroquine and Hydroxychloroquine -Its Mode Of Action And Possible Side Effectsmentioning

confidence: 99%

Factors for COVID-19 Infection that Govern the Severity of Illness

Ghosh¹,

Sarkar

Sepay³

et al. 2021

SciMed. J.

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“…Chloroquine is a weak base compound, referred to as lysosomotropic drug, which accumulates in endosomes and lysosomes, and increased lysosomal pH leading to a decrease in lysosomal protease activities and, finally, prevents viral entry into host cells [69,70]. Chloroquine also inhibits viral replication due to the lack of enzyme functional activities at a high pH [71]. The elevated pH in endosomes by chloroquine could explain the in vitro activity against the omicron variant.…”

Section: Discussionmentioning

confidence: 99%

Antiviral Activity of Repurposing Ivermectin against a Panel of 30 Clinical SARS-CoV-2 Strains Belonging to 14 Variants

et al. 2022

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Over the past two years, several variants of SARS-CoV-2 have emerged and spread all over the world. However, infectivity, clinical severity, re-infection, virulence, transmissibility, vaccine responses and escape, and epidemiological aspects have differed between SARS-CoV-2 variants. Currently, very few treatments are recommended against SARS-CoV-2. Identification of effective drugs among repurposing FDA-approved drugs is a rapid, efficient and low-cost strategy against SARS-CoV-2. One of those drugs is ivermectin. Ivermectin is an antihelminthic agent that previously showed in vitro effects against a SARS-CoV-2 isolate (Australia/VI01/2020 isolate) with an IC50 of around 2 µM. We evaluated the in vitro activity of ivermectin on Vero E6 cells infected with 30 clinically isolated SARS-CoV-2 strains belonging to 14 different variants, and particularly 17 strains belonging to six variants of concern (VOC) (variants related to Wuhan, alpha, beta, gamma, delta and omicron). The in vitro activity of ivermectin was compared to those of chloroquine and remdesivir. Unlike chloroquine (EC50 from 4.3 ± 2.5 to 29.3 ± 5.2 µM) or remdesivir (EC50 from 0.4 ± 0.3 to 25.2 ± 9.4 µM), ivermectin showed a relatively homogeneous in vitro activity against SARS-CoV-2 regardless of the strains or variants (EC50 from 5.1 ± 0.5 to 6.7 ± 0.4 µM), except for one omicron strain (EC50 = 1.3 ± 0.5 µM). Ivermectin (No. EC50 = 219, mean EC50 = 5.7 ± 1.0 µM) was, overall, more potent in vitro than chloroquine (No. EC50 = 214, mean EC50 = 16.1 ± 9.0 µM) (p = 1.3 × 10−34) and remdesivir (No. EC50 = 201, mean EC50 = 11.9 ± 10.0 µM) (p = 1.6 × 10−13). These results should be interpreted with caution regarding the potential use of ivermectin in SARS-CoV-2-infected patients: it is difficult to translate in vitro study results into actual clinical treatment in patients.

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“…Hasil penambatan molekuler menunjukkan seluruh ligan uji memiliki energi pengikatan lebih besar dibandingkan dengan senyawa pembanding, yaitu chloroquine (Tabel 4). Chloroquine dan senyawa turunannya berupa hydroxychloroquine merupakan senyawa yang telah diadopsi secara luas dalam mengobati Covid-19 (Zhan et al 2020). Senyawa khas pada tanaman mangga, yakni mangiferin menghasilkan energi bebas Gibbs (ΔG) yang paling besar dengan nilai -5.0440 kkal/mol, diikuti dibutyl phthalate (-3.2040 kkal/mol), trigonelline (-2.2410 kkal/mol), D-(+)-maltose (-2.2200 kkal/mol), citroflex A-4 (-1.9840 kkal/mol), α-glucoheptitol (-1.9800 kkal/mol), bis-beta-D-fructofuranose 1,2':2,3'dianhydride (-1.7080 kkal/mol), 16heptadecyne-1,2,4-triol (-1.5580 kkal/mol), hexitol (-0.4620 kkal/mol), dan chloroquine (-0.4420 kkal/mol).…”

Section: Analisis Lc-msunclassified

Potency of Bioactive Compounds in Indramayu Mango Peel Waste to Inhibit ACE2

et al. 2021

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According to reports, mango peel contains bioactive compounds—especially phenolic—threefold higher than the flesh. This issue underlies the research that aims to identify bioactive compounds from Indramayu mango peel which have the potential as ACE2 inhibitors. The study was initiated by extracting mango peel simplicia using aquadest, then carried out with phytochemical screening, and identification of compound content by LC-MS. The extraction obtained 21.3% of yield. The results of phytochemical screening showed that secondary metabolites in the form of alkaloids, flavonoids, saponins, and tannins were identified in the mango peel. At the same time, the LC-MS fragmentation results obtained 40 compounds based on the largest sample area. The result from fragmentation were tested for Lipinski bioavailability prediction and ADMET test and obtained 10 potential compounds. Molecular docking was performed on the ACE2 receptor with 10 sample ligands and 1 comparison ligand using YASARA Structure. All of the sample ligands (from Lipinski and ADMET test) showed higher free energies than comparison ligand, chloroquine. Mangiferin is a typical mango compound identified in LC-MS, had inhibitor activity against ACE2. Two-dimensional visualization using Discovery Studio showed mangiferin interaction with the receptor via hydrogen bond, hydrogen carbon bond and phi-anion interactions at three amino acid residues (Thr371, Glu375, Glu402) on the active site of ACE2. Keywords: ACE2, bioactive compound, mango peel, mangiferin, waste

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Chloroquine to fight COVID-19: A consideration of mechanisms and adverse effects?

Cited by 16 publications

References 96 publications

Factors for COVID-19 Infection that Govern the Severity of Illness

Factors for COVID-19 Infection that Govern the Severity of Illness

Antiviral Activity of Repurposing Ivermectin against a Panel of 30 Clinical SARS-CoV-2 Strains Belonging to 14 Variants

Potency of Bioactive Compounds in Indramayu Mango Peel Waste to Inhibit ACE2

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