Endocrine disrupting activities and immunomodulatory effects in lymphoblastoid cell lines of diclofenac, 4-hydroxydiclofenac and paracetamol

Klopčič, Ivana; Markovič, Tijana; Mlinarič-Raščan, Irena; Dolenc, Marija Sollner

doi:10.1016/j.toxlet.2018.05.022

Cited by 24 publications

(17 citation statements)

References 60 publications

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“…The observations are in agreement with the fact that many xenoestrogens demonstrate antiandrogenic activity (Sohoni and Sumpter 1998). DCF and some of its metabolites were regarded as estrogenic and antiandrogenic compounds (Klopčič et al 2018). In this work estrogenic activity of EE2 and DCF was primarily reported.…”

Section: Antiestrogenic and Antiandrogenic Activitiessupporting

confidence: 84%

Endocrine disrupting potency and toxicity of novel sophorolipid quaternary ammonium salts

2021

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A new class of biosurfactants, namely quaternary ammonium sophorolipids (SQAS), suitable for pharmaceutical applications, was tested for the evaluation of their (anti)estrogenic and (anti)androgenic potency with the help of YES/YAS assays. Also their toxicity towards yeasts (Saccharomyces cerevisiae) and bacteria (Escherichia coli) was checked. The results achieved for SQAS, which can be regarded as potential micropollutants, were compared with those obtained for two well-known micropollutants diclofenac and 17α-ethinylestradiol subjected to the same testing procedures. This work demonstrated that acetylation of the hydroxyl group of the carbohydrate head of SQAS decreased the toxicity of this class of biosurfactants towards Saccharomyces cerevisiae. Furthermore, it contributed to the decrease of their endocrine disrupting potency. None of the SQAS studied showed clear agonist activity for female or male hormones. SQAS1 and SQAS2 revealed weak antiestrogenic and antiandrogenic potency. All of these properties were weaker, not only to the potency of the appropriate positive control in the antagonists bioassays, but also compared to the potency of other tested compounds, i.e. DCF and EE2. SQAS3 possessed most probably inhibitory activity towards male hormones. Moreover, cytotoxicity of two out of four studied SQAS at the highest concentrations towards the strains of Saccharomyces cerevisiae interfered with the endocrine disruption activity. It would be also worth studying it with the use of another endocrine activity test.

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Section: Antiestrogenic and Antiandrogenic Activitiessupporting

confidence: 84%

Endocrine disrupting potency and toxicity of novel sophorolipid quaternary ammonium salts

2021

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“…Most of these chemicals with the exception of diclofenac have log Kow of <4.5 indicating a relatively water soluble nature (Table 1). On the other hand, diclofenac has a log Kow of 4.51 indicating a lipophilic nature, which explain the estrogenicity exhibited by diclofenac as demonstrated by Klopcic et al 34 Interestingly, diclofenac log Kow lies in the range of log Kow that has been demonstrated to belong to estrogenic compounds. 58 Some other studies investigated mutagenicity, aryl hydrocarbon receptor activation in detecting dioxin-like activities, glucocorticogenicity and genotoxicity.…”

Section: Major Mode Of Actions and Endpointsmentioning

confidence: 95%

“…On the contrary, there are also studies reporting bioeffect of individual and cocktail mixture of pharmaceuticals using reconstituted analytical grade samples of the pharmaceuticals in specic matrices such as water. [32][33][34][35][36][37]…”

Section: Workflow For Moa Determinationmentioning

confidence: 99%

“…Investigation of its anti-estrogenic, androgenic and antiandrogenic effects, toxic effects of plant growth, mortality and DNA damaging effect on different aquatic organisms have been carried out. [32][33][34]37,160 Interestingly, there are some pharmaceuticals found to have benecial effects, such as venlafaxine and carbamazepine that were found to reduce abnormal embryo development in zebrash at an environmentally-relevant concentration of 0.5 mg L À1 . 36 This is in line with the report of a previous study that documented the highest carbamazepine concentration of 5 mg L À1 in a German wastewater.…”

Section: Endpoints On Individually Targeted Analytesmentioning

confidence: 99%

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Monitoring of emerging contaminants of concern in the aquatic environment: a review of studies showing the application of effect-based measures

et al. 2021

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“…In vivo, in vitro and ex vivo studies have shown that APAP directly perturbs hormone-dependent processes, including inhibition of androgen production and increased oestrogen production, disruption of steroidogenesis, depletion of sulfated sex hormones, perturbation of immune function, induction of oxidative stress and indirect activation of the endocannabinoid system 1,2,[61][62][63][64][65] . Independently of APAP, these processes have been implicated as mechanisms related to the development of neurodevelopmental [66][67][68][69][70][71][72][73][74][75][76] and reproductive disorders 2 .…”

Section: Nature Reviews | Endocrinologymentioning

confidence: 99%

Paracetamol use during pregnancy — a call for precautionary action

Bauer¹,

Swan

Kriebel³

et al. 2021

Nat Rev Endocrinol

123

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Paracetamol (N-acetyl-p-aminophenol (APAP), otherwise known as acetaminophen) is the active ingredient in more than 600 medications used to relieve mild to moderate pain and reduce fever. APAP is widely used by pregnant women as governmental agencies, including the FDA and EMA, have long considered APAP appropriate for use during pregnancy when used as directed. However, increasing experimental and epidemiological research suggests that prenatal exposure to APAP might alter fetal development, which could increase the risks of some neurodevelopmental, reproductive and urogenital disorders. Here we summarize this evidence and call for precautionary action through a focused research effort and by increasing awareness among health professionals and pregnant women. APAP is an important medication and alternatives for treatment of high fever and severe pain are limited. We recommend that pregnant women should be cautioned at the beginning of pregnancy to: forego APAP unless its use is medically indicated; consult with a physician or pharmacist if they are uncertain whether use is indicated and before using on a long-term basis; and minimize exposure by using the lowest effective dose for the shortest possible time. We suggest specific actions to implement these recommendations. This Consensus Statement reflects our concerns and is currently supported by 91 scientists, clinicians and public health professionals from across the globe.

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Endocrine disrupting activities and immunomodulatory effects in lymphoblastoid cell lines of diclofenac, 4-hydroxydiclofenac and paracetamol

Cited by 24 publications

References 60 publications

Endocrine disrupting potency and toxicity of novel sophorolipid quaternary ammonium salts

Endocrine disrupting potency and toxicity of novel sophorolipid quaternary ammonium salts

Monitoring of emerging contaminants of concern in the aquatic environment: a review of studies showing the application of effect-based measures

Paracetamol use during pregnancy — a call for precautionary action

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