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Use of Dermatologics during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Clioquinol is an antibacterial and antifungal agent. No studies are published on the use of this drug during human or experimental animal pregnancy. Mafenide (Sulfamylon) and silver sulfadiazine (Silvadene, Thermazene, Flint SSD, Sildimac) are topical antibacterial and antifungal agents used to treat infections secondary to skin burns. No human studies of these drugs in human pregnancy and birth defects are published. No animal teratology studies of mafenide are published. According to manufacturer information, silver sulfadiazine was not teratogenic in animal studies (unpublished).
Clioquinol
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Clioquinol was formerly used widely in topical medicaments for the treatment of leg ulcers and in combination preparations with corticosteroids for the treatment of (secondarily infected) eczema. Allergic reactions were mostly seen in patients with venous leg ulcers and stasis dermatitis, who are known to be highly susceptible to contact sensitization. Because of its yellow color and the availability of more effective anti-infective agents, it is infrequently used in European countries anymore. As this inevitably resulted in low frequencies of sensitization, clioquinol, which had been part of the European baseline series for decades, was removed from it in 2019 (48).
Treatment and Prevention of Amebiasis
Published in Roberto R. Kretschmer, Amebiasis: Infection and Disease by Entamoeba histolytica, 2020
Side-effects — The most important toxic reaction, mainly observed with clioquinol, is subacute myeloptic neuropathy. This disease, first described in Japan, appears to be restricted to that country because further cases have been rare in the rest of the world. It is noteworthy that clioquinol has been quite popular as self-medication for the treatment of “tourist-diarrhea” in many countries. A task force created in Japan for the study of the side-effects of clioquinol demonstrated a clear correlation between the use of this particular drug and the appearance of subacute optic myelopathy.44,45 In consequence, treatment with clioquinol was banned. Other side-effects of oxyquinoleins are iodine toxidermatitis, anal pruritus, and occasionally nausea and intestinal colic. Nevertheless, this drug is quite effective against exclusively intestinal amebiasis, particularly in its subacute and those claimed chronic forms and of course in the treatment of E. histolytica cyst carriers.
Novel strategies for the fight of Alzheimer’s disease targeting amyloid-β protein
Published in Journal of Drug Targeting, 2022
Yang Xie, Yan Wang, Shangfei Jiang, Xiaohong Xiang, Jianhua Wang, Linhong Ning
In terms of the toxicity of Aβ aggregation state, Aβ-targeted agents have been mainly designed to restrain Aβ oligomerization or fibrillization, with plenty of such agents brought out successively (especially metal chelators and metal complexes), which have been reported as inhibitors interacting with Aβ species through various mechanisms [20,21]. For example, metal cations such as Cu2+ and Zn2+ is capable of coordinating with residues at the N-terminal of Aβ peptides, resulting in accelerated aggregation of Aβ and stabilised Aβ oligomers [22,23]. Hence, it has been proposed that metal-induced Aβ aggregation could be disaggregated by metal chelators, which is capable of capturing metal cations out of metal-Aβ aggregates and could be potential therapeutic agents of AD [24,25]. It has been reported that the chelation strategy designed to reduce amyloid pathology has plausibility in AD treatment [26]. In recent decades, improved cognition in Phase II clinical trials of the non-specific chelators (e.g. clioquinol (5-chloro-7-iodo-8-hydroxyquinoline)) encouraged a continued pursuit for therapeutic efficacy [27,28]. However, a quinoline derivative, PBT2, failed to show clinical benefit in a Phase 2a study in AD patients and was discontinued [29]. Besides, some kinds of natural compounds (e.g. gallic acid 30] and synthesised peptides [3]1 were proposed to have the ability of hampering Aβ pathologies through metal chelation and Aβ inhibition. The results of animal experiment demonstrated that a few metal chelating agents have exhibited therapeutic activities [32,33].
Developments with multi-target drugs for Alzheimer’s disease: an overview of the current discovery approaches
Published in Expert Opinion on Drug Discovery, 2019
Juan F. González, Andrés R. Alcántara, Antonio L. Doadrio, Jose María Sánchez-Montero
(5-chloro-7-iodoquinoline-8-ol, 8HQ, Figure 4) is an old drug with antifungal properties, which was withdrawn in 1983 due to its neurotoxicity at high doses. That said, topical clioquinol is still in clinical use for certain skin disorders. As already commented, the metal dyshomeostasis hypothesis postulates that an increase of the brain bioactive metals (iron, copper, and zinc) levels in the aging brain promotes amyloid plaques formation and neuroinflammation process in the pathogenesis of AD. Based on this, targeting these metal ions is an attractive challenge in the development of new leads for the future treatment of AD. Thus, clioquinol was explored as an anti-Alzheimer drug because it is a known metal-protein-attenuating compound (MPAC) [97] and several in vitro and animal model assays have concluded that MPACs possess the ability to disaggregate beta-amyloid peptide, thus promoting solubilization and clearance of beta-amyloid protein in the brain. In this context, clioquinol reached phase 2 clinical trials; but, in 2005 Prana Company terminated the development of clioquinol studies because the drug synthetic process generates a toxic contaminant. Nonetheless, several 8-hydroxyquinoline (8HQ) derivatives were investigated for their neuroprotective effect against different neurodegenerative pathologies, and, additionally, 8HQ-based scaffolds have been successfully tested as building block to the design and development of new hybrid compounds possessing both antioxidant and metal-chelating properties [98].
Anti-tumour activity of zinc ionophore pyrithione in human ovarian cancer cells through inhibition of proliferation and migration and promotion of lysosome-mitochondrial apoptosis
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2020
Mengge Chen, Yanpeng Ding, Yuan Ke, Yifei Zeng, Nuomin Liu, Yahua Zhong, Xinying Hua, Zheng Li, Yudi Xiong, Chaoyan Wu, Haijun Yu
Our previous studies have proved that clioquinol could transfer Zinc into cancer cells focussing on lysosome [17,18]. Then we further demonstrated that clioquinol combined with Zinc could inhibit NF-kB activity and leading cancer cells apoptosis [19]. The recent studies found that transferring Zinc into cells could also increase the radiosensitivity of nasopharyngeal cancer stem-like cells [20,21]. However, there were rarely studies to explore the influence of overloaded Zinc on ovarian cancer and the drug-resistant cells. Therefore, we researched the anti-cancer effects of ZPT combined with Zinc in this study. We emphasised the inhibiting effect of overloaded Zinc on the malignancy tumour behaviours and provided a considerable treatment strategy for ovarian cancer.