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排序方式: 共有112条查询结果,搜索用时 15 毫秒
1.
An examination of four species of Cirsium disclosed the presence of two new flavonoids in C. lineare. The structure of one was 5,4′-dihydroxy-6,7,3′-trimethoxyflavone (cirsilineol) 4′-monoglucoside and the other 5,3′,4′-trihydroxy-6,7-dimethoxyflavone (cirsiliol) 4′-monoglucoside. Luteolin 7-glucoside was found in C. suffultum, and pectolinarin and linarin in C. kamtschaticum and C. pectinellum. 相似文献
2.
Inactivation of TEM-1 beta-lactamase by 6-acetylmethylenepenicillanic acid 总被引:2,自引:2,他引:0
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6-Acetylmethylenepenicillanic acid is a new kinetically irreversible inhibitor of various beta-lactamases. Interaction between 6-acetylmethylenepenicillanate and purified TEM-1 beta-lactamase during the inactivation process was investigated. 6-Acetylmethylenepenicillanate inhibited the enzyme in a second-order fashion with a rate constant of 0.61 microM-1 . S-1. The apparent inactivation constant decreased in the presence of increasing concentrations of the substrate benzylpenicillin. Native enzyme (pI 5.4) was converted into two inactive forms with pI 5.25 and 5.15, the latter form being transient and readily converted into the more stable form with pI 5.15. Even a 50-fold excess of inhibitor over enzyme did not produce any other inactivated species of the enzyme. All the results obtained suggest that 6-acetylmethylenepenicillanate is a potent irreversible and active-site-directed inhibitor of TEM-1 beta-lactamase. 相似文献
3.
T Mio T Yabe M Sudoh Y Satoh T Nakajima M Arisawa H Yamada-Okabe 《Journal of bacteriology》1996,178(8):2416-2419
The CHS2 and CHS3 genes of Candida albicans were disrupted. The double disruptant was still viable. Assessment of chitin and of calcofluor white resistance shows that CHS1 is responsible for septum formation and CHS3 is responsible for overall chitin synthesis otherwise. There were only small differences in virulence to immunocompromised mice of homozygous chs2 delta amd chs3 delta null mutants. 相似文献
4.
Cloning of the macrolide antibiotic biosynthesis gene acyA, which encodes 3-O-acyltransferase, from Streptomyces thermotolerans and its use for direct fermentative production of a hybrid macrolide antibiotic. 总被引:2,自引:0,他引:2
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A Arisawa N Kawamura K Takeda H Tsunekawa K Okamura R Okamoto 《Applied microbiology》1994,60(7):2657-2660
A gene encoding the macrolide modification enzyme 3-O-acyltransferase (acyA) was cloned by chromosome walking onto the carbomycin biosynthetic region in Streptomyces thermotolerans TH475, with the 3' region of the gene encoding the macrolide modification enzyme 4"-O-acyltransferase (acyB1) as a probe. A shortened fragment (1.8 kb) containing acyA was subcloned with pIJ350. A high-level tylosin producer, Streptomyces fradiae MBBF, transformed with the plasmid could produce a hybrid macrolide, 3-O-acetyltylosin, most efficiently. 相似文献
5.
6.
N. Ohmiya Shinsuke Saga Masaharu Ohbayashi Ken-ichi Kozaki Osamu Miyaishi Miya Kobayashi Shiro Kasuya Tomiyasu Arisawa Hidemi Goto Tetsuo Hayakawa 《Histochemistry and cell biology》1997,108(1):27-34
An association between eosinophils and tissue damage has been observed in numerous disorders. However, few reports have addressed
the role of infiltrating eosinophils in gastric ulcer healing. The aim of this study was to investigate the kinetics and role
of eosinophils infiltrating experimental chronic gastric ulcers in the rat. We developed a monoclonal antibody against human
matrix metalloproteinase 1 (MMP1) purified from conditioned culture medium of human skin fibroblasts. Acetic acid-induced
gastric ulcers were resected from rats on days 1, 3, 5, 10, 20, 40, and 180 after the days of induction (day 0). Tissue specimens
were immunostained with this antibody and examined with an electron microscope. Few eosinophils were observed in the granulation
tissue until day 20. By days 40 and 180, MMP1-positive eosinophils had increased in the granulation tissue of open ulcers.
Azan staining revealed dispersed collagen fibers around infiltrating eosinophils. In contrast, scars demonstrated few eosinophils
in fibrous tissue on days 40 and 180. Eosinophils which express MMP1 infiltrate granulation tissue at the chronic stage of
gastric ulceration. The results suggest that eosinophils may play a role in tissue remodeling and deterioration of ulceration.
Accepted: 18 March 1997 相似文献
7.
8.
Shuji Yonezawa Hidekuni Yamakawa Chie Muto Motoko Hosono Takahiko Yamamoto Kazunari Hattori Masahiro Sakagami Hiroko Togame Yoshikazu Tanaka Toru Nakano Hiroshi Takemoto Mitsuhiro Arisawa Satoshi Shuto 《Bioorganic & medicinal chemistry letters》2013,23(10):2912-2915
To improve the efficacy of the conformationally restricted BACE1 inhibitors, structural modifications were investigated using two strategies: (a) modification of the terminal aromatic ring and (b) insertion of a spacer between the aromatic rings. In the latter approach, another type of inhibitor 17 bearing an ethylene spacer between two aromatic rings was found to exhibit good BACE1 inhibitory activity, while the corresponding conformationally unrestricted compound 25 showed no activity. This result revealed an interesting effect of a conformational restriction with a cyclopropane ring. 相似文献
9.
Kondoh O Takasuka T Arisawa M Aoki Y Watanabe T 《The Journal of biological chemistry》2002,277(44):41744-41749
Fks1p and Fks2p are catalytic subunits of beta-1,3-glucan synthase, which synthesize beta-1,3-glucan, a main component of the cell wall in Saccharomyces cerevisiae. Although Fks1p and Fks2p are highly homologous, sharing 88.1% identity, it has been shown that Fks2p is more sensitive than Fks1p to one of echinocandin derivatives, which inhibits beta-1,3-glucan synthase activity. Here we show a similar differential sensitivity between Fks1p and Fks2p to a novel beta-1,3-glucan synthase inhibitor, aerothricin3 [corrected]. To investigate the molecular mechanism of this differential sensitivity, we constructed a series of chimeric genes of FKSs and examined their sensitivity to aerothricin3 [corrected]. As a result, it was shown that a region around the fourth extracellular domain of Fks2p, containing 10 different amino acid residues from those of Fks1p, provided Fks1p aerothricin3 [corrected] sensitivity when the region was replaced with a corresponding region of Fks1p. In order to identify essential amino acid residues responsible for the sensitivity, each of the 10 non-conserved amino acids of Fks1p was substituted into the corresponding amino acid of Fks2p by site-directed mutagenesis. Surprisingly, only one amino acid substitution of Fks1p (K1336I) conferred Fks1p hypersensitivity to aerothricin3 [corrected]. On the other hand, reverse substitution of the corresponding amino acid of Fks2p (I1355K) resulted in loss of hypersensitivity to aerothricin3 [corrected]. These results suggest that the 1355th isoleucine of Fks2p plays a key role in aerothricin3 [corrected] sensitivity. 相似文献
10.
6-Hydroxymellein (6HM) synthase is a multifunctional polyketide enzyme induced in carrot cells, whose fully active homodimer catalyzes condensation of acyl-CoAs and the NADPH-dependent ketoreduction of the enzyme-bound intermediate. 6HM-forming activity of the synthase was markedly decreased when the reaction mixture pH was adjusted from 7.5 to 6.0. However, under these slightly acidic conditions, the acyl condensation catalyzed by the dissociated monomer enzyme was appreciably stimulated by addition of free coenzyme A (CoA). In contrast, the condensation reaction at pH 6.0 was significantly inhibited in the presence of CoA when the reaction was carried out with the NADPH-omitted dimer synthase. Among the kinetic parameters of the acyl condensation, velocity of the monomer-catalyzing reaction at the acidic pH was appreciably increased upon addition of CoA while K(m)s did not show any significant change in the presence and absence of the compound. These results suggest that CoA associates with a specific site in the dissociated monomeric form of 6HM synthase, and the velocity of the acyl condensation reaction catalyzed by the CoA-synthase complex appreciably increases in acidic conditions. 相似文献