hER-MIP is a molecularly imprinted polymer (MIP) that has been shown to selectively collect human estrogen receptor (hER) binding active substances. However, environmental samples contain various ...chemicals depending on the location and regional differences, and the hER binding activity depends on the sample type. Thus, the general applicability of hER-MIP to actual environmental samples must be elucidated. In this study, 48 environmental samples were collected and screened with hER-MIP, and a yeast assay was performed to evaluate the adsorption characteristics of the samples according to the adsorption and elution fractions. The results showed that hER-MIP collects hER binding active substances almost selectively but does not collect constitutive androstane receptor (CAR) binding active substances selectively. CAR binding activity was detected in the adsorbed fraction because several hER binding active substances also demonstrate CAR binding activity.
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EMUNI, FIS, FZAB, GEOZS, GIS, IJS, IMTLJ, KILJ, KISLJ, MFDPS, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, SBMB, SBNM, UKNU, UL, UM, UPUK, VKSCE, ZAGLJ
Pralatrexate has been approved for the treatment of relapsed/refractory peripheral T cell lymphomas. Studies in the U.S. also support the clinical efficacy of pralatrexate to treat advanced‐stage ...cutaneous T‐cell lymphomas, but outcomes in Japanese patients have not yet been reported. We herein describe two Japanese patients with heavily‐pretreated relapsed/refractory mycosis fungoides that were successfully controlled by pralatrexate.
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FZAB, GIS, IJS, KILJ, NLZOH, NUK, OILJ, SAZU, SBCE, SBMB, UL, UM, UPUK
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•Choline and geranate (CAGE) ionic liquid showed promise in treating subgingival infection.•Periodontal pathogens were killed by CAGE-induced cell membrane disruption.•CAGE overcame ...extracellular matrix, a physical barrier of biofilms that attenuates drug diffusion.•Subgingival biofilms were neutralized and eventually destroyed by CAGE treatment.
Periodontitis is a chronic inflammatory disease that causes destruction of the periodontium and eventual tooth loss. The priority in the periodontal treatment is to remove the subgingival biofilm. Chemical removal of biofilms using antimicrobial agents has been applied in clinical practice. However, their clinical effect is still limited because the agents must overcome biofilm’s significant drug tolerance, which is primarily caused by the extracellular matrix, a physical barrier that attenuates drug diffusion. This study aimed to study the use of ionic liquids (ILs), a new class of biocompatible materials, for controlling subgingival biofilms because of their excellent permeability. Choline and geranate (CAGE) IL was tested for its highly potent antiseptic behavior and permeability. Antibacterial tests revealed that the significant efficacy of CAGE against periodontopathic microorganisms was derived from their ability to destroy cell membrane, as demonstrated by membrane permeability assay and transmission electron microscopy imaging. Antibiofilm tests using two pathogenic biofilm models revealed that CAGE exerted efficacy against the biofilm-embedded bacteria, conspicuously neutralized the biofilms, and eventually destroyed the biofilm structure. Furthermore, the penetration of CAGE into the biofilm was visually confirmed using confocal laser scanning microscopy. This study highlighted the potential of CAGE as a powerful antibiofilm therapeutic.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
Molecular imprinting technology has been widely studied as a technique to obtain molecular recognition by artificial means. Selecting functional monomers or polymerization conditions plays a key role ...to optimize molecularly imprinted polymer (MIP) synthesis. To date, there have been few reports well exploiting the effect of crosslinkers. Here, in this study, we synthesized the MIPs using poly(ethyleneglycol) dimethacrylate with different units of ethylene oxide (
n
= 1 to 23) as crosslinkers to observe the molecular recognition abilities. The MIPs were attached to the surface of mono-dispersed polymer beads. The obtained spherical MIPs and non-imprinted polymers were filled in a column for high performance liquid chromatography. Then the retention selectivity toward TR active substances was evaluated. The result revealed that the recognition ability did not improve regardless of the amount of ethylene oxide. With the crosslinker (
n
= 9), extremely high retention selectivity was observed, which provides at most around ten times as large imprinting factors in comparison with other MIPs. Interestingly, we obtained the highest recognition ability at around polymerization temperature from the evaluation of the recognition ability toward temperature shift using the MIP (
n
= 9). In general, hydrogen bonding based on MIPs provides high recognition ability at low temperature, whereas, this study indicates that the use of flexible crosslinkers may enable the synthesis of MIPs that precisely memorize the conditions of polymerization. Lastly, we simultaneously analyzed the TR active substances using the column filled with MIPs (
n
= 9). The result showed relatively linear correlation between the retention strength of each substance and phycological activity toward TR obtained by yeast assay. Therefore, we can conclude that an induced fit like the receptor emerged by constructing the flexible molecular recognition field.
We report the effects of the crosslinker length on the molecular recognition for the preparation of molecularly imprinted polymers.
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IJS, KILJ, NUK, UL, UM, UPUK
We report an efficient screening procedure for the selective detection of compounds that are actively bound to estrogen receptor (ER) from environmental water samples using a receptor-mimic adsorbent ...prepared by a molecularly imprinted polymer (MIP). To mimic the recognition ability of ER, we improved the typical MIP preparation procedure using a hydrophilic matrix with a polyethylene glycol (PEG)-based crosslinker and a hydrophobic monomer to imitate the hydrophobic pocket of ER. An optimized MIP prepared with methacrylic acid as an additional functional monomer and estriol (E3), an analogue of 17β-estradiol (E2), exhibited highly selective adsorption for ER-active compounds such as E2 and E3, with significant suppression of non-specific hydrophobic adsorption. The prepared MIP was then applied to the screening of ER-active compounds in sewage samples. The fraction concentrated by the MIP was evaluated by in vitro bioassay using the yeast two-hybrid (Y2H) method and liquid chromatography–quadrupole time-of-flight mass spectrometry (LC–Q-TOFMS). Compared to an authentic adsorbent, styrene–divinylbenzene (SDB)-based resin, the fraction concentrated by the MIP had 120% ER activity in the Y2H assay, and only 25% peak volume was detected in LC–Q-TOFMS. Furthermore, a few ER-active compounds were identified only from the fraction concentrated by the MIP, although they could not be determined in the fraction concentrated by the SDB-based resin due to ion suppression along with high levels of hydrophobic compounds. These results indicated that the newly developed MIP effectively captured ER-active compounds and while allowing most non–ER-active compounds to pass through.
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•Estrogen receptor (ER) mimic adsorbents were prepared by the modified molecular imprinting.•Hydrophilic matrix with a polyethylene glycol suppressed non-selective adsorption.•The adsorbent captured ER-active compounds and while allowing most non–ER-active compounds to pass through.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
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A case of psoriasiform drug eruption caused by temozolomide Oguro, Tokuko; Nakajima, Kimiko; Aoki, Natsuko ...
Journal of cutaneous immunology and allergy,
October 2022, 2022-10-00, 20221001, 2022-10-01, Volume:
5, Issue:
5
Journal Article
Peer reviewed
Open access
Psoriasiform drug eruption is defined as condition similar to psoriasis triggered by drug administration, including de novo development of psoriasis or exacerbation of pre‐existing psoriasis. Herein, ...we describe a 52‐year‐old Japanese woman, who developed disseminated psoriasiform lesions following administration of temozolomide, a remedy for glioblastoma, although cutaneous adverse events by this drug was very rare. In addition, we assume that altered inflammatory signals associated with psoriasis, such as activation of signal transducer and activator of transcription 3 (STAT3), might be involved in the underlying pathomechanism of drug eruption caused by temozolomide.
Psoriasiform drug eruption is defined as condition similar to psoriasis triggered by drug administration, including de novo development of psoriasis or exacerbation of pre‐existing psoriasis. We report a case who developed psoriasiform lesions following administration of temozolomide, a remedy for glioblastoma,although cutaneous adverse events by this drug was very rare.
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FZAB, GIS, IJS, KILJ, NLZOH, NUK, OILJ, SAZU, SBCE, SBMB, UL, UM, UPUK
Depression is the disorder with the greatest socioeconomic burdens. Its diagnosis is still based on an operational diagnosis derived from symptoms, and no objective diagnostic indicators exist. Thus, ...the present study aimed to develop an artificial intelligence (AI) model to aid in the diagnosis of depression from electroencephalography (EEG) data by applying machine learning to resting-state EEG and transcranial magnetic stimulation (TMS)-evoked EEG acquired from patients with depression and healthy controls. Resting-state EEG and single-pulse TMS-EEG were acquired from 60 patients and 60 healthy controls. Power spectrum analysis, phase synchronization analysis, and phase-amplitude coupling analysis were conducted on EEG data to extract feature candidates to apply different types of machine learning algorithms. Furthermore, to address the limitation of the sample size, dimensionality reduction was performed in a manner to increase the quality of information by featuring robust neurophysiological metrics that showed significant differences between the two groups. Then, nine different machine learning models were applied to the data. For the EEG data, we created models combining four modalities, including (1) resting-state EEG, (2) pre-stimulus TMS-EEG, (3) post-stimulus TMS-EEG, and (4) differences between pre- and post-stimulus TMS-EEG, and evaluated their performance. We found that the best estimation performance (a mean area under the curve of 0.922) was obtained using receiver operating characteristic curve analysis when linear discriminant analysis (LDA) was applied to the combination of the four feature sets. This study showed that by using TMS-EEG neurophysiological indices as features, it is possible to develop a depression decision-support AI algorithm that exhibits high discrimination accuracy.
The first catalytic dehydrative condensation of the benzylic C–H bonds of toluene and p-xylene with aromatic aldehydes is reported herein. This protocol provides highly atom-economical access to ...stilbene and p-distyrylbenzene derivatives, whereby water is the sole byproduct. The reaction is based on the deprotonation–functionalization of benzylic C–H bonds through η6-complexation of the arenes, which is realized for the first time using a catalytic amount of a transition metal activator. The key to the success of this method is the use of a sulfonamide anion as a catalyst component, which appears to facilitate not only the deprotonation of the benzylic C–H bonds but also the formation of a C–C bonds via an electrophilic tosylimine intermediate.
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IJS, KILJ, NUK, PNG, UL, UM
The atmospheric concentrations of both gas-phase and particulate-phase polycyclic aromatic hydrocarbons (PAHs) including 16 US Environmental Protection Agency priority PAHs (16 PAHs) were measured in ...eleven cities across Japan. Using the measured average concentrations and toxic equivalency factors (TEF) of the 16 PAHs, the benzoapyrene (BaP)-toxic equivalent for eight major PAHs was obtained: the ratio of BaP to the eight major PAH toxicities ranged from 0.23 to 0.47. Among the target PAHs, from the viewpoint of carcinogenicity, we focused on benzocfluorene (BcFE), which was detected in both the gas and particulate phase in contrast to BaP. The relative potency factor (RPF) of BcFE was evaluated as 6.46 based on its cancer slope factor relative to that of BaP determined in the benchmark dose calculations for mice. The relative carcinogenic risk of BcFE to BaP was obtained by multiplying the averaged concentrations of BaP and BcFE by the RPF value: the risk of BcFE was 6.8 and 5.1 times higher than that of BaP in summer and winter, respectively. These results show that the collection of atmospheric samples including the gas phase is important when assessing the carcinogenic risk of atmospheric PAHs.
•Overall atmospheric concentration levels of PAHs across Japan were measured.•Atmospheric concentrations of BcFE, CPcdP, and BjF were similar to that of BaP.•Benchmark dose method was applied to evaluate carcinogenic risk.•Carcinogenic risk of BcFE for mice was 5–7 times higher than that of BaP.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
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