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11.
12.
Vicente Gomes Phan Van Ngan Claude de Broyer Maria José deA. C. Rocha Passos 《Hydrobiologia》1993,262(2):109-113
Mitotic and meiotic chromosomes of the Antarctic lysianassoid amphipod Waldeckia obesa are described. The modal chromosome number is n = 25 and 2n = 50. The potential applications of cytogenetical studies in this group are discussed. 相似文献
13.
Bui Hai Ninh Duong Thi Dung Bui Huu Tai Pham Hai Yen Nguyen Xuan Nhiem Truong Thi Thu Hien Do Thi Trang Nguyen Van Tuyen Le Tuan Anh Nguyen Thi Hoai Phan Van Kiem 《化学与生物多样性》2023,20(3):e202201048
A new isopropyl chromone ( 1 ) and a new flavanone glucoside ( 2 ) together with eleven known compounds ( 3–13 ) were isolated from the leaves of Syzygium cerasiforme (Blume) Merr. & L.M.Perry. Their structures were elucidated as 5,7-dihydroxy-2-isopropyl-6,8-dimethyl-4H-chromen-4-one ( 1 ), 5,7-dihydroxyflavanone 7-O-β-D-(6′′-O-galloylglucopyranoside) ( 2 ), strobopinin ( 3 ), demethoxymatteucinol ( 4 ), pinocembrin-7-O-β-D-glucopyranoside ( 5 ), (2S)-hydroxynaringenin-7-O-β-D-glucopyranoside ( 6 ), afzelin ( 7 ), quercetin ( 8 ), kaplanin ( 9 ), endoperoxide G3 ( 10 ), grasshopper ( 11 ), vomifoliol ( 12 ), litseagermacrane ( 13 ) by the analysis of HR-ESI-MS, NMR, and CD spectral data. Compounds 1 , 2 , 5 , 6 and 10 inhibited NO production on LPS-activated RAW264.7 cells with IC50 values of 12.28±1.15, 8.52±1.62, 7.68±0.87, 9.67±0.57, and 6.69±0.34 μM, respectively, while the IC50 values of the other compounds ranging from 33.38±0.78 to 86.51±2.98 μM, compared to that of the positive control, NG-monomethyl-L-arginine acetate (L-NMMA) with an IC50 value of 32.50±1.00 μM. 相似文献
14.
Doan Minh Sang Ik Ho Na Dr. Duong Tien Anh Do Thi Mai Dung Nguyen Thi Thu Hang Nguyen T. Phuong-Anh Assoc. Prof. Dr. Pham-The Hai Assoc. Prof. Dr. Dao Thi Kim Oanh Dr. Truong Thanh Tung Soo Jung Lee Joo Hee Kwon Prof. Dr. Jong Soon Kang Prof. Dr. Sang-Bae Han Assoc. Prof. Dr. Dinh Thi Thanh Hai Prof. Dr. Nguyen-Hai Nam 《化学与生物多样性》2023,20(5):e202201030
Herein, we report the design, synthesis and evaluation of novel (E)-3-(3-oxo-4-substituted-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl)-N-hydroxypropenamides ( 4 a – i , 7 a – g ) targeting histone deacetylases. Three human cancer cell lines were used to test the cytotoxicity of the synthesized compounds (SW620, colon; PC-3, prostate; NCI−H23, lung cancer); inhibitory activity towards HDAC; anticancer activity; as well as their impact on the cell cycle and apoptosis. As a result, compounds 4 a – i bearing the alkyl substituents seemed to be less potent than the benzyl-containing compounds 7 a – g in all biological assays. Compounds 7 e – f were found to be the most active HDAC inhibitors with IC50 of 1.498±0.020 μM and 1.794±0.159 μM, respectively. In terms of cytotoxicity and anticancer assay, 7 e and 7 f also showed good activity with IC50 values in the micromolar range. In addition, the cell cycle and apoptosis of SW620 were affected by compound 7 f in almost a similar manner to that of reference compound SAHA. Docking assays were carried out for analysis the binding mode and selectivity of this compound toward 8 HDAC isoforms. Overall, our data confirmed that the inhibition of HDAC plays a pivotal role in their anticancer activity. 相似文献
15.
Summary Using a combinatorial peptide library method, we identified YIYGSFK as an efficient and specific peptide substrate for pp60c-src protein tyrosine kinase (PTK) [Lam et al., Int. J. Pept. Protein Res., 45 (1995) 587]. Employing YIYGSFK as a template, we synthesized and evaluated a series of pseudosubstrate-based inhibitors for pp60c-src. We found that the efficiency of a given inhibitor was highly dependent on the specific tyrosine analog used at the phosphorylation site of the substrate. One of these pseudosubstrate inhibitors, YI(2-Nal)GSFK, selectively inhibited the kinase activity of pp60c-src, with a Ki of 24 M. This peptide inhibitor exhibited selectivity for pp60c-src as compared to other PTKs tested, such as c-Abl and Bcr-Abl. Our results suggest that selective inhibitors for a specific PTK can be developed when the structure of a specific and efficient small peptide substrate for this PTK can be used as a template for structure modification.Abbreviations 1-Nal
l-1-naphthylalanine
- 2-Nal
l-2-naphthylalanine
- BOP
benzotriazolyl-N-oxy-tris(dimethylamino)-phosphonium hexafluorophosphate
- BSA
bovine serum albumin
- cAPK
cyclic AMP-dependent protein kinase
- DIEA
diisopropylethylamine
- EGFR
epidermal growth factor receptor
- Fmoc
fluorenylmethoxycarbonyl
- HOBt
1-hydroxybenzotriazole
- MES
2-[N-morpholino]ethanesulfonic acid
- PBS
phosphate-buffered salts
- pCl
l-p-chlorophenylalanine
- pF
l-p-fluorophenylalanine
- PTK
protein tyrosine kinase
- TLC
thin-layer chromatography 相似文献
16.
Pham Thi Huan Rona Taylor Alf A. Lindberg Naresh K. Verma 《Microbiology and immunology》1995,39(7):467-472
The glucosyl transferase gene (gtr) from bacteriophage phage X (SfX) caused partial conversion of serotype Y (group antigen 3, 4) to X (group antigen 7, 8) when introduced into a candidate vaccine strain of Shigella flexneri serotype Y (SFL124). The gtr gene caused conversion of O-antigens but did not eliminate the adsorption of the corresponding phage SfX. The hybrid strain expressing both group antigens 7, 8 and 3, 4 showed 75% protection when immunized guinea pigs were challenged with a wild-type S. flexneri serotype X strain. No protection was observed against serotype Y challenge, although group antigen 3, 4 was detected in the LPS of the hybrid strain. This suggests the importance of O-antigen immunity in the host defense against shigellosis. 相似文献
17.
Prostaglandins of the E-series (PGEs) and PGI2 will inhibit formylmethionylleucylphenylalanine-(f-Met-Leu-Phe) induced lysosomal enzyme release and superoxide-anion (O2-) production by neutrophils. The inhibitory effects of PGEs and PGI2 on neutrophil functional responses have been correlated with their ability to increase intracellular cAMP. In this study we have examined the effects of PGEs and PGI2 on f-Met-Leu-Phe- and phorbol-myristate-acetate-induced rat neutrophil membrane potential changes using an optical probe of membrane potential 3,3-dipropylthiodicarbocyanine iodide. 15-(S)-15-methyl-PGE1 (15-methyl-PGE1), a stable analogue of PGE1 and PGI2 inhibited f-Met-Leu-Phe-induced transmembrane potential changes in a dose-dependent manner. This inhibition was correlated with the ability of these agents to increase intracellular cAMP levels and inhibit O2- production and degranulation. In contrast, 15-methyl-PGE1 and PGI2, did not inhibit phorbol-myristate-acetate-induced transmembrane potential changes and O2- production. These results suggest independent mechanisms of activation of neutrophils by phorbol myristate acetate and f-Met-Leu-Phe, and they also suggest that the inhibitory effects of prostaglandins and cAMP on f-Met-Leu-Phe-stimulated cells is at a step or steps prior to activation of those processes involved in effecting changes in transmembrane potential, which are common to both stimuli. 相似文献
18.
Human genes for glutathione S-transferases 总被引:11,自引:2,他引:9
The tissue distribution of different glutathione S-transferases (GST) is analysed by electrophoresis. The existence of GST"e" (erythrocyte), GST3, GST1, and GST2 is confirmed. GST"e" the fastest and most thermolabile of different GST analysed is observed only in erythrocyte cells. GST3 which migrates more slowly than GST"e" is present in all tissues and cells analysed, excepted for erythrocyte cells in which only GST"e" is observed. GST1 presents a polymorphism with four phenotypes, 1, 1/2, 2, and 0 controlled by three alleles 1, 2, and 0 (null). With the sample of 56 livers analysed the different frequencies obtained are 9%, 5%, 43%, 43% for the phenotypes 1, 1/2, 2, and 0 respectively and 0.074 (p), 0.279 (q), 0.647 (r) for the alleles, 1, 2, and 0 (null). GST2 presents variant patterns due probably, in the majority of cases, to post-synthetic modifications rather than allelic variation. Two new GST are described, GST4 and GST5. GST4 abundant in muscle tissue is a dimeric protein. GST4 forms with GST1 a heterodimeric band. GST5 is observed in brain homogenates. For the chromosome localization the results obtained by man (leucocytes)-mouse somatic cell hybrid analysis indicate that the gene for leucocytes GST is on chromosome 11. This gene is the structural GST3 gene. 相似文献
19.
Nuclear DNA amounts were determined by cytofluorometry for twelve species and subspecies of the genus Xenopus. Absolute values, in pg per nucleus, were obtained by direct comparison with human lymphocyte nuclei. The lowest DNA amount (3.55 pg) was found in X. tropicalis, which possess only 20 chromosomes, and the highest (16.25 pg), in the hexaploid X. ruwenzoriensis, with 108 chromosomes. The two recently discovered tetraploid species, X. sp.n. and X. vestitus have, respectively, 12.57 and 12.83 pg of DNA. Among the species and subspecies with 36 chromosomes, the DNA content ranges from 6.35 to 8.45 pg. 相似文献
20.