Antimalarials: unapproved uses or indications

Wolf, Ronni; Wolf, Danny; Ruocco, Vincenzo

doi:10.1016/s0738-081x(99)00092-9

Cited by 45 publications

(40 citation statements)

References 216 publications

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“…Because our CQ was co-administered with injury in the early stage of liver fibrosis, we hypothesized that the ability of CQ to neutralize inflammation, which is a well-known indication used in a clinic, 26 might counteract the AAF/CCL 4 -induced toxicity and, as a result, hinder the induction of autophagy. The mechanism by which CQ suppresses AAF/CCL 4induced fibrosis remains to be further clarified.…”

Section: Inhibited Autophagy Alleviated Aaf/ccl 4 -Induced Liver Fibrmentioning

confidence: 99%

Increased Autophagy Markers Are Associated with Ductular Reaction during the Development of Cirrhosis

Hung

Yuan

Chen

et al. 2015

The American Journal of Pathology

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Autophagy is a regulatory pathway in liver fibrosis. We investigated the roles of autophagy in human cirrhotic livers. Cirrhotic and noncirrhotic liver tissues were obtained from patients with hepatocellular carcinoma, and liver tissues from live donors served as control. Patients with cirrhotic livers had significantly increased levels of various essential autophagy-related genes compared with noncirrhotic livers. In addition, colocalization of autophagy marker microtubule-associated protein 1 light chain 3B (LC3B) with lysosome-associated membrane protein-1, increased levels of lysosome-associated membrane protein-2, and increased maturation of lysosomal cathepsin D were observed in cirrhotic livers. By using dual-immunofluorescence staining, we demonstrated that increased LC3B was located mainly in the cytokeratin 19-labeled ductular reaction (DR) in human cirrhotic livers and in an experimental cirrhosis induced by 2-acetylaminofluorene (AAF) with carbon tetrachloride (CCl4), indicating a conserved response to chronic liver damage. Furthermore, an AAF/CCl4-mediated increase in DR and fibrosis were attenuated after chloroquine treatment, suggesting that the autophagy-lysosome pathway was essential for AAF/CCl4-induced DR-fibrosis. In conclusion, we demonstrated that increased autophagy marker positively correlated with DR during the development of cirrhosis. Therefore, targeting autophagy may hold therapeutic value for liver cirrhosis.

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Section: Inhibited Autophagy Alleviated Aaf/ccl 4 -Induced Liver Fibrmentioning

confidence: 99%

Increased Autophagy Markers Are Associated with Ductular Reaction during the Development of Cirrhosis

Hung

Yuan

Chen

et al. 2015

The American Journal of Pathology

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“…Hydroxychloroquine (HCQ) is used in the treatment of rheumatoid arthritis and systemic lupus erythematosus and as an antimalarial [1]. Like other antimalarial drugs, such as (±)-chloroquine, (±)-primaquine and (±)-mefloquine [2], HCQ is administered as a racemic mixture [rac-HCQ] of two enantiomers, R(−)-HCQ and S(+)-HCQ.…”

Section: Introductionmentioning

confidence: 99%

Enantioselective analysis of the metabolites of hydroxychloroquine and application to an in vitro metabolic study

Cardoso¹,

Bonato

2005

Journal of Pharmaceutical and Biomedical Analysis

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“…It has also been used as an antimalarial drug [2]. HCQ is administered as a racemic mixture of (1)-(S)-HCQ and (2)-(R)-HCQ and its hepatic metabolism generates three active metabolites, desethylchloroquine (DCQ), desethylhydroxychloroquine (DHCQ), and bisdesethylchloroquine (BDCQ), which are also chiral molecules [3] (Fig.…”

Section: Introductionmentioning

confidence: 99%

Capillary electrophoretic chiral separation of hydroxychloroquine and its metabolites in the microsomal fraction of liver homogenates

2006

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A rapid, selective, and low-cost chiral capillary electrophoretic method was developed for the simultaneous analysis of hydroxychloroquine (HCQ) and its three chiral metabolites: desethylchloroquine (DCQ), desethylhydroxychloroquine (DHCQ), and bisdesethylchloroquine (BDCQ) in the microsomal fraction of liver homogenates. After liquid-liquid extraction using toluene as extracting solvent, the drug and metabolites were resolved on a fused-silica capillary (50 microm ID, 50 cm total length, and 42 cm effective length), using 100 mmol/L of Tris/phosphate buffer, pH 9.0 containing 1% w/v sulfated-beta-CD and 30 mg/mL hydroxypropyl-beta-CD. Detection was carried out at 220 nm. The extraction procedure was efficient in removing endogenous interferents, and low values (

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Antimalarials: unapproved uses or indications

Cited by 45 publications

References 216 publications

Increased Autophagy Markers Are Associated with Ductular Reaction during the Development of Cirrhosis

Increased Autophagy Markers Are Associated with Ductular Reaction during the Development of Cirrhosis

Enantioselective analysis of the metabolites of hydroxychloroquine and application to an in vitro metabolic study

Capillary electrophoretic chiral separation of hydroxychloroquine and its metabolites in the microsomal fraction of liver homogenates

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