2008
DOI: 10.1016/j.tiv.2008.01.002
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Screening and detection of the in vitro agonistic activity of xenobiotics on the retinoic acid receptor

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Cited by 54 publications
(25 citation statements)
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“…However, results in this study do not completely exclude the possibility that 4-oxo-RAs are present in the rivers. That is, because SPE procedures applied in this study were different from those reported in the previous study Recent studies have also reported that synthetic compounds such as organochlorine pesticides, styrene dimers, monoalkylphenols and parabens show RAR agonistic activity in vitro (Nishikawa et al, 2003;Lemaire et al, 2005;Kamata et al, 2008). However, due to their low potencies, any contribution to the RARa agonistic activity of our samples should be negligible at normal environmental concentrations.…”
Section: Discussionmentioning
confidence: 72%
“…However, results in this study do not completely exclude the possibility that 4-oxo-RAs are present in the rivers. That is, because SPE procedures applied in this study were different from those reported in the previous study Recent studies have also reported that synthetic compounds such as organochlorine pesticides, styrene dimers, monoalkylphenols and parabens show RAR agonistic activity in vitro (Nishikawa et al, 2003;Lemaire et al, 2005;Kamata et al, 2008). However, due to their low potencies, any contribution to the RARa agonistic activity of our samples should be negligible at normal environmental concentrations.…”
Section: Discussionmentioning
confidence: 72%
“…However, TCMs usually comprise hundreds or thousands of components, only a few of which are responsible for the pharmaceutical and/or toxic effects. A large number of effective analysis techniques have been developed to determine the bioactive compounds of medicinal plants [3], including classic pharmacological approaches [4,5], molecular bio-chromatography [6,7], chromatographic fingerprinting [8,9], combinatorial chemistry [10], high-throughput screening [11], ultra-highthroughput screening [12], high-content screening [13] and DNA microarray technology [14]. Nevertheless, the large number of constituents in TCMs makes screening and analysis for bioactive compounds extremely difficult, even from well-documented formulations for specific diseases.…”
Section: Introductionmentioning
confidence: 99%
“…28,[41][42][43][44][45] Recent studies have also revealed that xenobiotic environmental pollutants can elicit the binding affinity to and the agonistic activity on RARs. Xenobiotic compounds including not only wellknown endocrine disrupting chemicals (EDCs) such as alkylphenols, [46][47][48] phthalate esters, 49) styrene dimers 48) and organochlorine pesticides 50) but also non-EDCs 51) have been proven to exhibit agonistic activity on one or several isotypes of RAR in vitro (Table 2). However, xenobiotic pollutants with agonistic activity at RARα are very limited as compared with those with RARβ or RARγ agonistic ability (Table 2).…”
Section: Natural and Xenobiotic Compounds That Act As Rar Agonistsmentioning
confidence: 99%
“…However, xenobiotic pollutants with agonistic activity at RARα are very limited as compared with those with RARβ or RARγ agonistic ability (Table 2). Kamata et al 48) evaluated the RARγ agonistic activity of 543 compounds including industrial chemicals, agrochemicals, natural compounds, medicines and cosmetic chemicals with a yeast two-hybrid assay, and revealed that 85 chemicals including 16 organochlorine pesticides, 14 styrene dimers, 9 alkylphenols and 6 parabens were active at RARγ (showing ≥ 20% of RARγ agonistic activity of 10 nM of atRA) at concentrations equal to 0.2-10 µM. Lemaire et al 50) also reported that organochlorine pesticides having teratogenic activities in animals (i.e., aldrin, chlordane, dieldrin, endrin and endosulfan) weakly activate RARβ and RARγ but do not activate RARα in a transactivation assay, and that among these five pesticides, endrin is the most effective at both RARβ and RARγ with 50% effective concentrations of 17.6 µM (6.7 mg/l) and 6.0 µM (2.3 mg/l), respectively.…”
Section: Natural and Xenobiotic Compounds That Act As Rar Agonistsmentioning
confidence: 99%
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