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排序方式: 共有250条查询结果,搜索用时 15 毫秒
101.
IJAZ AHMAD SHILIN CHEN YONG PENG SIBAO CHEN LIJIA XU 《Journal of enzyme inhibition and medicinal chemistry》2013,28(1):140-143
Phytochemical investigations on the ethyl acetate-soluble fraction of the whole plant of Buddleja crispa led to the isolation of the iridoids 1–7. Compound 2 displayed significant inhibitory potential against enzyme lipoxygenase in a concentration-dependant fashion with IC50 value of 39.7 ± 0.02μM, along with DPPH radical scavenging activity with IC50 value 0.638 mM. 相似文献
102.
Zebrafish offer a unique vertebrate model for research areas such as drug development, disease modeling and other biological exploration. There is significant conservation of genetics and other cellular networks among zebrafish and other vertebrate models, including humans. Here we discuss the recent work and efforts made in different fields of biology to explore the potential of zebrafish. Along with this, we also reviewed the concept of systems biology. A biological system is made up of a large number of components that interact in a huge variety of combinations. To understand completely the behavior of a system, it is important to know its components and interactions, and this can be achieved through a systems biology approach. At the end of the paper we present a concept of integrating zebrafish into the systems biology approach. 相似文献
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NQO1 gene polymorphism at nucleotide 609 (Pro187Ser) results in a lowering of NQO1 detoxifying activity and is associated with susceptibility to various cancers. The NQO1 genotypes were identified by RFLP in 104 bladder cancer cases and 120 control subjects in an ethnic Kashmiri population. The frequency of the variant NQO1 alleles (CT/TT) was 23.3% for controls and 32.2% for cases (P?0.05). Overall, the variant alleles were associated with a higher risk of bladder cancer in cases than in the control group (OR?=?1.90; 95% CI 1.17-3.04; P?0.01). In addition, the variant allele genotypes (CT/TT) were associated with a risk of bladder cancer that was more than threefold higher in smokers (OR?=?3.47; 95% CI 1.84-6.3; P?0.001). Results of this study strongly suggest that the variant allele of NQO1 (Pro187Ser) may affect individual susceptibility to bladder cancer, particularly among smokers, in this ethnic Kashmiri population. 相似文献
106.
Proinflammatory cytokines such as interleukin-1 beta (IL-1β) and tumor necrosis factor alpha (TNF-α) enhance degradation of cartilage-specific, type II collagen by matrix metalloproteinase-13 (MMP-13). We investigated the previously unknown role of H-Ras and reactive oxygen species (ROS) in the cytokine induction of MMP-13 gene expression in human articular chondrocytes by using pharmacological inhibitors, RNA interference (RNAi) and antioxidants. Manumycin A, an inhibitor of H-Ras farnesylation by farnesyltransferase, suppressed IL-1β- and TNF-α-induced MMP-13 mRNA and protein expression. Small interfering RNA (siRNA)-mediated H-Ras silencing down-regulated MMP-13 mRNA and protein induction by IL-1β and TNF-α. Nicotinamide adenine dinucleotide phosphate oxidase (NADPH oxidase/NOX) inhibitor, diphenyleneiodonium (DPI) suppressed cytokine-induced MMP-13 expression and superoxide production. Apocynin, another NOX inhibitor, also diminished MMP-13 induction. Deoxyglucose an antimetabolite of glucose metabolism reduced MMP-13 increase. Role of NOX-mediated ROS production was reaffirmed by the observation that the antioxidants, trolox, nordihydroguaiaretic acid (NDGA), quercetin and resveratrol downregulated cytokine-induced MMP-13 mRNA and protein expression. These results provide strong pharmacological and genetic evidence for the implication of H-Ras and NADPH oxidase-generated superoxide production in MMP-13 gene regulation by IL-1β and TNF-α. These proteins could be potentially targeted for therapeutic inhibition of MMP-13-driven cartilage erosion by using H-Ras and NOX inhibitors and antioxidants. 相似文献
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Yun W Ahmad M Chen Y Gillespie P Conde-Knape K Kazmer S Li S Qian Y Taub R Wertheimer SJ Whittard T Bolin D 《Bioorganic & medicinal chemistry letters》2011,21(23):7205-7209
In a discovery effort to find safe and effective DGAT-1 inhibitors, we have identified 2-phenyloxazole 4-carboxamide 1 as a conformationally constrained analog of a hydrazide hit, which was previously identified from high-throughput screening. Further optimization of this series has led to chemically more stable 2-phenyloxazole-based DGAT-1 inhibitor 25 with improved solubility, cell-based activity, and pharmacokinetic properties. Compound 25 also demonstrated in vivo efficacy in a diet-induced obesity (DIO) rat model. 相似文献
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Ishtiaq Ayesha Bakhtiar Attia Silas Erica Saeed Javeria Ajmal Sidra Mushtaq Iram Ali Tahir Wahedi Hussain M. Khan Wajiha Khan Uzma Anees Mariam Sultan Aneesa Murtaza Iram 《Molecular biology reports》2020,47(9):6545-6559
Molecular Biology Reports - Exposure to environmental toxicants such as Bisphenol A (BPA) has raised serious health issues globally particularly in developing countries. It is ubiquitously used in... 相似文献
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Bone modeling and remodeling is an optimization process where no agreement has been reached regarding a unified theory or model. We measured 384 pieces of bone in vivo by 64-slice CT and discovered that the bone's center of mass approximately superposes its centroid of shape. This phenomenon indicates that the optimization process of non-homogeneous materials such as bone follows the same law of superposition of center of mass and centroid of shape as that of homogeneous materials. Based upon this principle, an index revealing the relationship between the center of mass and centroid of shape of the compact bone is proposed. Another index revealing the relationship between tissue density and distribution radius is followed. Applying these indexes to evaluate the strength of bone, we have some new findings. 相似文献
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