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101.
Yosuke Toyota Sayaka Nomura Makoto Makishima Yuichi Hashimoto Minoru Ishikawa 《Bioorganic & medicinal chemistry letters》2017,27(12):2776-2780
Anti-inflammatory effects of peroxisome proliferator-activated receptor gamma (PPRAγ) ligands are thought to be largely due to PPARγ-mediated transrepression. Thus, transrepression-selective PPARγ ligands without agonistic activity or with only partial agonistic activity should exhibit anti-inflammatory properties with reduced side effects. Here, we investigated the structure-activity relationships (SARs) of PPARγ agonist rosiglitazone, focusing on transrepression activity. Alkenic analogs showed slightly more potent transrepression with reduced efficacy of transactivating agonistic activity. Removal of the alkyl group on the nitrogen atom improved selectivity for transrepression over transactivation. Among the synthesized compounds, 3l exhibited stronger transrepressional activity (IC50: 14 μM) and weaker agonistic efficacy (11%) than rosiglitazone or pioglitazone. 相似文献
102.
Seasonal recruitment and survival strategies of Palisada cervicornis comb. nov. (Ceramiales,Rhodophyta) in coral reefs
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103.
Intraspecific Variation of Floral Scent Chemistry in Magnolia kobus DC. (Magnoliaceae) 总被引:1,自引:0,他引:1
Magnolia kobus was examined at 32 sites in Japan (109 female-stage flowers from 52 plants) by GC-MS. Major chemical compounds (a total of
36 chemicals) emitted from the flowers were: linalool (and its oxides), limonene, cis- and trans-β-Ocimene, benzaldehyde, benzyl alcohol, benzyl cyanide, and 2-aminobenzaldehyde. Linalool and its oxides were
the most abundant components of floral scents in 21 individuals. The rate at which chemical volatiles were emitted ranged
from 0.002 to 0.929 μg/flower/hour (average 0.211). High quantitative and qualitative variation in floral scent chemistry among individuals was
found throughout the range of M. kobus, especially in central Honshu. The high variability in floral scent chemistry may be due to the importance of visual cues
in the reproductive biology of M. kobus which flowers in early spring, resulting in decreased selection for specific floral scent profiles. Alternatively, different
scent compounds or chemical profiles may be equally effective in attracting pollinators.
Received 25 June 2001/ Accepted in revised form 25 August 2001 相似文献
104.
The volatile components of 25 taxa of the liverwort family Frullaniaceae from New Zealand, Australia and South America have been analyzed by GC-MS. The present Frullania species are chemically divided into five major types: (1) sesquiterpene lactones, (2) sesquiterpene lactones-bibenzyls, (3) bibenzyls, (4) 2-alkanone and (5) triterpene types; the latter two chemo-types are newly proposed for the genus. Schusterella chevalierii, belonging to the Frullaniaceae, is closely related chemically to the sesquiterpene lactone type of the Frullania species since it elaborates two eudesmanolides, beta-cyclocostunolide and dihydro-beta-cyclocostunolide as major components. 相似文献
105.
106.
Tetsuro Maruyama Yasunori Akutsu Akiko Suganami Yutaka Tamura Hiromichi Fujito Tomoki Ouchi Naoki Akanuma Yuka Isozaki Nobuyoshi Takeshita Isamu Hoshino Masaya Uesato Taro Toyota Hideki Hayashi Hisahiro Matsubara 《PloS one》2015,10(4)
Introduction
Photodynamic therapy (PDT) is a less invasive option for cancer treatment that has evolved through recent developments in nanotechnology. We have designed and synthesized a novel liposome system that includes an indocyanine green (ICG) derivative, ICG-C18, in its bilayer. In addition to its use as an optical imager to visualize blood, lymphatic, and bile flow, ICG has also been used as an optical sensitizer. In the present report, we evaluate the use of our novel liposome system, LP-ICG-C18, in PDT for squamous cell carcinoma in an autologous murine model.Materials and Methods
An excitation pulse beam (300 μJ/pulse) of a single band (800 nm) was used for sensitization. The cytotoxicity of the photodynamic therapy was evaluated in terms of cellular morphology changes, methyl thiazolyl tetrazolium (MTT) assay results, and terminal deoxynucleotidyl transferase-mediated deoxyuridine triphosphate-biotin nick end labeling (TUNEL) staining. We tested the enhanced permeability and retention effect of LP-ICG-C18 in tumor-bearing C3H/He mice using a near-infrared fluorescence imaging system and fluorescence microscopy. We also examined the antitumor effect of PDT by measuring tumor volume in tumor-bearing mice.Results
Cell death and apoptosis were only observed in the PDT group receiving LP-ICG-C18. LP-ICG-C18 itself had no cytotoxic activity and showed good biocompatibility. LP-ICG-C18 accumulated on the tumor 24 hours after injection and was retained for approximately 3 weeks. Tumor cell apoptosis following PDT with LP-ICG-C18 was also observed under optical microscopy, MTT assay, and TUNEL staining.Conclusion
These findings suggest that LP-ICG-C18 may be an effective intervening material in PDT for malignant disease. 相似文献107.
Wild type of bovine thrombin has been crystallized in a ligand-free form by the hanging drop vapor diffusion method with polyethylene glycol 4000 and 2-propanol. The crystals belong to space group P4 3 2 12 with unit cell parameters of a = b = 87.7 A, c = 195.9 A. X-ray diffraction data were collected to 2.8 A resolution. 相似文献
108.
SNP analyses of growth factor genes EGF, TGFbeta-1, and HGF reveal haplotypic association of EGF with autism 总被引:1,自引:0,他引:1
Toyoda T Nakamura K Yamada K Thanseem I Anitha A Suda S Tsujii M Iwayama Y Hattori E Toyota T Miyachi T Iwata Y Suzuki K Matsuzaki H Kawai M Sekine Y Tsuchiya K Sugihara G Ouchi Y Sugiyama T Takei N Yoshikawa T Mori N 《Biochemical and biophysical research communications》2007,360(4):715-720
Autism is a pervasive neurodevelopmental disorder diagnosed in early childhood. Growth factors have been found to play a key role in the cellular differentiation and proliferation of the central and peripheral nervous systems. Epidermal growth factor (EGF) is detected in several regions of the developing and adult brain, where, it enhances the differentiation, maturation, and survival of a variety of neurons. Transforming growth factor-beta (TGFbeta) isoforms play an important role in neuronal survival, and the hepatocyte growth factor (HGF) has been shown to exhibit neurotrophic activity. We examined the association of EGF, TGFbeta1, and HGF genes with autism, in a trio association study, using DNA samples from families recruited to the Autism Genetic Resource Exchange; 252 trios with a male offspring scored for autism were selected for the study. Transmission disequilibrium test revealed significant haplotypic association of EGF with autism. No significant SNP or haplotypic associations were observed for TGFbeta1 or HGF. Given the role of EGF in brain and neuronal development, we suggest a possible role of EGF in the pathogenesis of autism. 相似文献
109.
T Ohara K Matsuda D Shibuya Y Eda T Yuki S Asaki T Toyota T Kurokawa R Sasaki 《Life sciences》1989,44(20):1499-1504
When experimental acute gastric mucosal lesions were produced in guinea pig by water-immersion and restraint stress, superoxide dismutase (SOD)-like substance in the plasma increased. On analysis by gel filtration, it was shown that the molecular weight of the increased SOD-like plasma substance was about 130,000, and even after treatment with trypsin, 84% of this substance remained. Since the molecular weight of intracellular SOD is about 40,000, it seems that this substance is similar to extracellular SOD, located on the endothelial cell-surface, as previously reported by Marklund et al. Our results suggest that in the presence of acute gastric mucosal lesions, SOD-like plasma substance is not identical to intracellular SOD, which derived from cell destruction by stress or free radical-induced microvascular damage or by hemolysis. Furthermore, this substance may itself work as a scavenger of free radicals generated under conditions, such as these described in the present experiment. 相似文献
110.
N Katagiri T Shiraishi H Sato A Toyota C Kaneko K Yusa T Oh-hara T Tsuruo 《Biochemical and biophysical research communications》1992,184(1):154-159
Two enantiomers of 9-(c-4,t-5-bishydroxymethylcyclopent-2-en-r-1-yl)-9H- adenine (BCA) which showed a potent and selective anti-HIV effects have been synthesized and evaluated against human immunodeficiency virus type 1. The result demonstrated that the potent-HIV activity of racemic BCA is expressed solely by the (-) isomer. 相似文献