Ciprofloxacin Cardiotoxicity and Hepatotoxicity in Humans and Animals

Adikwu, Elias; Nelson, Barnaby

doi:10.4236/pp.2012.32028

Cited by 30 publications

(13 citation statements)

References 55 publications

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“…On the contrary, in HEK 293, the conjugate did not induce a significant level of ROS. The fact that the action of most of the synthesised conjugates results in negligible ROS generation is advantageous, suggesting low cardio-and hepatotoxicity potential, which stands in strike contrast with bare antibacterial fluoroquinolones [33][34][35].…”

Section: Ros Generationmentioning

confidence: 99%

Conjugates of Ciprofloxacin and Levofloxacin with Cell-Penetrating Peptide Exhibit Antifungal Activity and Mammalian Cytotoxicity

Ptaszyńska

Gucwa

Olkiewicz

et al. 2020

IJMS

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Seven conjugates composed of well-known fluoroquinolone antibacterial agents, ciprofloxacin (CIP) or levofloxacin (LVX), and a cell-penetrating peptide transportan 10 (TP10-NH2) were synthesised. The drugs were covalently bound to the peptide via an amide bond, methylenecarbonyl moiety, or a disulfide bridge. Conjugation of fluoroquinolones to TP10-NH2 resulted in congeners demonstrating antifungal in vitro activity against human pathogenic yeasts of the Candida genus (MICs in the 6.25–100 µM range), whereas the components were poorly active. The antibacterial in vitro activity of most of the conjugates was lower than the activity of CIP or LVX, but the antibacterial effect of CIP-S-S-TP10-NH2 was similar to the mother fluoroquinolone. Additionally, for two representative CIP and LVX conjugates, a rapid bactericidal effect was shown. Compared to fluoroquinolones, TP10-NH2 and the majority of its conjugates generated a relatively low level of reactive oxygen species (ROS) in human embryonic kidney cells (HEK293) and human myeloid leukemia cells (HL-60). The conjugates exhibited cytotoxicity against three cell lines, HEK293, HepG2 (human liver cancer cell line), and LLC-PK1 (old male pig kidney cells), with IC50 values in the 10–100 µM range and hemolytic activity. The mammalian toxicity was due to the intrinsic cytoplasmic membrane disruption activity of TP10-NH2 since fluoroquinolones themselves were not cytotoxic. Nevertheless, the selectivity index values of the conjugates, both for the bacteria and human pathogenic yeasts, remained favourable.

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Section: Ros Generationmentioning

confidence: 99%

Conjugates of Ciprofloxacin and Levofloxacin with Cell-Penetrating Peptide Exhibit Antifungal Activity and Mammalian Cytotoxicity

Ptaszyńska

Gucwa

Olkiewicz

et al. 2020

IJMS

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“…Recently, rising cases of ciprofloxacin-associated organ toxicities have been reported. 4 Ciprofloxacin is mainly excreted via the kidneys. 1 Nephrotoxic reactions to fluoroquinolones appear to be uncommon but potentially serious.…”

Section: Introductionmentioning

confidence: 99%

Beneficial effects of quercetin on renal injury and oxidative stress caused by ciprofloxacin in rats

et al. 2015

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Ciprofloxacin is a broad-spectrum quinolone antibiotic commonly used in clinical practice. Quercetin is an antioxidant belongs to flavonoid group. It inhibits the production of superoxide anion. In this study, we aimed to evaluate the effects of quercetin on renal injury and oxidative stress caused by ciprofloxacin. Twenty-eight female Wistar albino rats were divided into four groups: control, quercetin (20 mg kg−1 day−1 gavage for 21 days), ciprofloxacin (20 mg kg−1 twice a day intraperitoneally for 10 days), and ciprofloxacin + quercetin. Samples were processed for histological and biochemical evaluations. Malondialdehyde (MDA) and glutathione (GSH) levels, superoxide dismutase (SOD), and catalase (CAT) activities were measured in kidney tissue. The ciprofloxacin group showed histopathological changes such as infiltration, dilatation in tubules, tubular atrophy, reduction of Bowman’s space, congestion, hemorrhage, and necrosis. In the ciprofloxacin + quercetin group, these histopathological changes markedly reduced. MDA levels increased in the ciprofloxacin group and decreased in the ciptofloxacin + quercetin group. SOD and CAT activities and GSH levels significantly decreased in the ciprofloxacin group. On the other hand, in the ciprofloxacin + quercetin group, SOD and CAT activities and GSH levels significantly increased with regard to the ciprofloxacin group. We concluded that quercetin has antioxidative and therapeutic effects on renal injury and oxidative stress caused by ciprofloxacin in rats.

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“…SOD, GST, and LPO activities were predominantly higher in tissues of ciprofloxacin treated fish. Ciprofloxacin has the potential to cause hepatotoxic effects on both humans and animals 55 . The authors 55 also reported that the generation of free radicals might induce oxidative stress in liver tissue, resulting in organ damage.…”

Section: Discussionmentioning

confidence: 99%

“…Ciprofloxacin has the potential to cause hepatotoxic effects on both humans and animals 55 . The authors 55 also reported that the generation of free radicals might induce oxidative stress in liver tissue, resulting in organ damage. CAT activity was found to be inhibited significantly in liver tissue.…”

Section: Discussionmentioning

confidence: 99%

Responses of Cirrhinus mrigala to second‐generation fluoroquinolone (ciprofloxacin) toxicity: Assessment of antioxidants, tissue morphology, and inorganic ions

Ramesh

Sujitha

Anila

et al. 2020

Environmental Toxicology

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Ciprofloxacin drugs are a second‐generation fluoroquinolone highly prescribed medication against various bacterial infections in human and aquaculture practices. These drugs are chemically designed to persist in the body long enough to achieve target objectives. Extensive usage has resulted in ciprofloxacin becoming a ubiquitous contaminant in the environment. Unfortunately, the ecotoxicological profiles for ciprofloxacin are scanty. This study was aimed to assess the ecotoxicity of ciprofloxacin at environmentally relevant concentrations (1 μg/L, and 1.5 μg/L) to a cultivable fish Cirrhinus mrigala. Responses of antioxidant enzymes, histological anomalies, and inorganic ion levels were studied. SOD activity in gill, liver, and kidney tissues was elevated in ciprofloxacin‐exposed groups when compared with the control group. CAT activity was predominantly decreased in ciprofloxacin treated groups relative to the control group. GST activity in the ciprofloxacin treated groups was increased (except kidney tissues [Treatment I (1 μg/L)], and gill tissues fifteenth day) significantly (p < .05). The LPO level was elevated in the ciprofloxacin treatment groups throughout the study period (except Treatment II (1.5 μg/L) tenth day in kidney tissues). A series of histological anomalies were noticed in the gill, liver, and kidney tissues of the ciprofloxacin treated groups. Ciprofloxacin exposure caused a significant decrease of sodium, potassium, and chloride levels in the plasma of C. mrigala. A parallel among an imbalanced oxidative defense system, tissue structural changes, and alterations of plasma inorganic ions could be considered as a reliable biomarker for antibiotic toxicity study. This study could be a primary platform for further toxicity studies to understand the potential molecular impacts and adverse effects of ciprofloxacin on aquatic organisms.

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Ciprofloxacin Cardiotoxicity and Hepatotoxicity in Humans and Animals

Cited by 30 publications

References 55 publications

Conjugates of Ciprofloxacin and Levofloxacin with Cell-Penetrating Peptide Exhibit Antifungal Activity and Mammalian Cytotoxicity

Conjugates of Ciprofloxacin and Levofloxacin with Cell-Penetrating Peptide Exhibit Antifungal Activity and Mammalian Cytotoxicity

Beneficial effects of quercetin on renal injury and oxidative stress caused by ciprofloxacin in rats

Responses of Cirrhinus mrigala to second‐generation fluoroquinolone (ciprofloxacin) toxicity: Assessment of antioxidants, tissue morphology, and inorganic ions

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