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1.
Kanna Adachi Tomoshi Yamada Hayate Ishizuka Mana Oki Shunsuke Tsunogae Noriko Shimada Osamu Chiba Tatsuya Orihara Prof. Dr. Masafumi Hidaka Prof. Dr. Takatsugu Hirokawa Dr. Minami Odagi Prof. Dr. Keiichi Konoki Prof. Dr. Mari Yotsu-Yamashita Prof. Dr. Kazuo Nagasawa 《Chemistry (Weinheim an der Bergstrasse, Germany)》2020,26(9):2025-2033
A novel series of C12-keto-type saxitoxin (STX) derivatives bearing an unusual nonhydrated form of the ketone at C12 has been synthesized, and their NaV-inhibitory activity has been evaluated in a cell-based assay as well as whole-cell patch-clamp recording. Among these compounds, 11-benzylidene STX ( 3 a ) showed potent inhibitory activity against neuroblastoma Neuro 2A in both cell-based and electrophysiological analyses, with EC50 and IC50 values of 8.5 and 30.7 nm , respectively. Interestingly, the compound showed potent inhibitory activity against tetrodotoxin-resistant subtype of NaV1.5, with an IC50 value of 94.1 nm . Derivatives 3 a – d and 3 f showed low recovery rates from NaV1.2 subtype (ca 45–79 %) compared to natural dcSTX ( 2 ), strongly suggesting an irreversible mode of interaction. We propose an interaction model for the C12-keto derivatives with NaV in which the enone moiety in the STX derivatives 3 works as Michael acceptor for the carboxylate of Asp1717. 相似文献
2.
Sachiko Kaidzu Kazunobu Sugihara Masahiro Sasaki Aiko Nishiaki Hiroyuki Ohashi Tatsushi Igarashi Masaki Tanito 《Photochemistry and photobiology》2023,99(4):1142-1148
Basal cells in the corneal limbus play an important role in the turnover cycle because they are the source of all cells that constitute the corneal epithelium. We examined the penetration depth of ultraviolet (UV) light in the corneal limbus and assessed the safety of Far-UV-C on stem cells in the basal area of the corneal limbus. Rats were irradiated with UV at peaks of 207, 222, 235, 254 and 311 nm while under anesthesia. The UV penetration depth in the rat corneal limbal epithelium was wavelength dependent: 311 nm UV-B and 254 nm UV-C reached the basal cells of the epithelium, and 235 nm radiation reached the middle area; however, 207 and 222 nm UV-C reached only the superficial layer of the epithelium. Porcine cornea, which is similar to the human eye in size and structure, were irradiated with 222 and 254 nm UV-C. As in rats, 222 nm UV-C reached only the superficial layer of the porcine corneal limbal epithelium. These results indicate that Far-UV-C, such as radiation of wavelengths of 207 and 222 nm, could not reach corneal epithelial stem cells, i.e. the cells remained intact. It is unlikely that the turnover of the corneal epithelium is obstructed or disrupted by exposure to Far-UV-C. 相似文献
3.
Chikako Nishigori Nozomi Yamano Makoto Kunisada Aiko Nishiaki-Sawada Hiroyuki Ohashi Tatsushi Igarashi 《Photochemistry and photobiology》2023,99(2):335-343
Life on earth has constantly coped with the impact of solar radiation, especially solar ultraviolet radiation (solar UV). Various biological mechanisms protect us from solar UV. New devices emitting shorter wavelengths UV-C, i.e. <254 nm emitted by conventional UV germicidal lamps, have emerged. These shorter wavelength UV-C emitting devices are useful for various purposes, including microorganism inactivation. However, as solar UV-C does not reach the earth surface, biological impacts of UV-C has been studied using 254 nm germicidal lamps, and those using shorter wavelength UV-C is rarely known. To balance the utility and risk of UV-C, the biological effect of these new UV-C emitting devices must be investigated. In addition, our knowledge of biological impacts of the wavelength-dependent entire UV (100–400 nm) must be enhanced. In this review, we briefly summarize the biological impacts of shorter wavelength UV-C. Mechanisms of UV-C-induced cellular damage and factors affecting the microorganism inactivation efficiency of UV-C have been discussed. In addition, we theoretically estimate the probable photocarcinogenic action spectrum of shorter wavelength UV-C. We propose that increasing the knowledge on UV-C will facilitate the adoption of shorter wavelength UV-C emitting new devices in an optimal and appropriate manner. 相似文献
4.
A Strategy to Control the Reactivation of Frustrated Lewis Pairs from Shelf‐Stable Carbene Borane Complexes 下载免费PDF全文
Dr. Yoichi Hoshimoto Takuya Kinoshita Prof. Dr. Masato Ohashi Prof. Dr. Sensuke Ogoshi 《Angewandte Chemie (International ed. in English)》2015,54(40):11666-11671
N‐Phosphine oxide substituted imidazolylidenes (PoxIms) have been synthesized and fully characterized. These species can undergo significant changes to the spatial environment surrounding their carbene center through rotation of the phosphine oxide moiety. Either classical Lewis adducts (CLAs) or frustrated Lewis pairs (FLPs) are thus formed with B(C6F5)3 depending on the orientation of the phosphine oxide group. A strategy to reactivate FLPs from CLAs by exploiting molecular motions that are responsive to external stimuli has therefore been developed. The reactivation conditions were successfully controlled by tuning the strain in the PoxIm–B(C6F5)3 complexes so that reactivation only occurred above ambient temperature. 相似文献
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6.
Some characteristics of strain-induced anisotropy and effects of strain-rate on them are experimentally investigated under non-proportional loadings at elevated temperature. By applying combined loadings of axial force and internal pressure to thin-walled tubes of an aluminium alloy at 200°C, inelastic stress-responses are observed at several constant strain-rates along bilinear strain trajectories. It is found that a softening of material and a non-coaxiality between stress and inelastic strain-increment deviators occur after the corner of bilinear strain trajectory. These phenomena appear more markedly and then decay more gradually with the increase of corner angle and/or strain-rate. Experimental results are qualitatively discussed in terms of the activation of piled-up dislocations as well as the so-called back stress and drag stress. 相似文献
7.
A test tunnel for the study of airfoil performances under air/water two-phase flow condition has been designed and constructed. This facility will serve for a better understanding of the flow phenomena and characteristics of hydraulic machinery under gas/ liquid two-phase flow operating conditions. At the test section of the tunnel, a two-dimensional isolated airfoil or a cascade of airfoils is installed in a two-phase inlet flow with a uniform velocity (up to 10 m/s) and void fraction (up to 12%) distribution. The details of the tunnel structure and the measuring systems are described and the basic characteristics of the constructed tunnel are also given. As an example of the test results, void fraction distribution around a test airfoil is shown.Dedicated to the 60th Birthday of Professor Klaus Gersten 相似文献
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9.
Self‐Assembled Fibers Containing Stable Organic Radical Moieties: Alignment and Magnetic Properties in Liquid Crystals 下载免费PDF全文
Hiroki Eimura Yoshikazu Umeta Prof. Dr. Hiroko Tokoro Prof. Dr. Masafumi Yoshio Prof. Dr. Shin‐ichi Ohkoshi Prof. Dr. Takashi Kato 《Chemistry (Weinheim an der Bergstrasse, Germany)》2016,22(26):8872-8878
Macroscopically oriented stable organic radicals have been obtained by using a liquid–crystalline (LC) gel composed of an l ‐isoleucine‐based low molecular weight gelator containing a 2,2,6,6‐tetramethylpiperidine 1‐oxyl moiety. The LC gel has allowed magnetic measurements of the oriented organic radical. The gelator has formed fibrous aggregates in liquid crystals via intermolecular hydrogen bonds. The fibrous aggregates of the radical gelator are formed and oriented on cooling by applying a magnetic field to the mixture of liquid crystals and the gelator. Superconducting quantum interference device (SQUID) measurements have revealed that both oriented and nonoriented fibrous aggregates exhibited antiferromagnetic interactions, in which super‐exchange interaction constant J is estimated as ?0.89 cm?1. 相似文献
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