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21.
This study addresses the influence the 7-substituent on the cytotoxicity of pyrrolo[1,2-alpha]-benzimidazole quinones possessing a 6-aziridinyl group (PBIs) and a 6-acetamido group (APBIs). Reduction of a PBI to the aziridinyl hydroquinone results in both nucleophile trapping (alkylation) and 1,5-sigmatropic shift reactions. The latter process is essentially an internal redox reaction wherein the hydroquinone causes reductive opening of the aziridinyl ring. The 7-substituent controls the fate of the aziridinyl ring by means of steric and electronic effects. An electron-rich 7-substituent favors the 1,5-sigmatropic shift reaction. If the 7-substituent distorts the 6-aziridinyl group from the conformation required for the 1,5-sigmatropic shift, then nucleophile trapping occurs. The 7-methyl substituent results in significant nucleophilic trapping, and the 7-unsubstituted and 7-methoxy substituents favor the 1,5-sigmatropic reaction. Thus, the 7-methyl PBIs show the most cytotoxicity of the analogues studied. The APBIs are cytotoxic only as quinones, and reduction to the hydroquinone results in loss of activity. Consistent with this observation, the change from 7-methyl to the more electron-rich 7-methoxy results in a substantial loss of APBI cytotoxicity as well as decreased topoisomerase II inhibition. The mechanism of inhibition is thought to involve the interacalation of only electron deficient APBIs into DNA. 相似文献
22.
The magnetization of a melt-texture growth (MTG) HTSC ring has been studied. It is shown that the magnetic field inside the ring is larger than the external field under a certain range of external magnetic fields. We have also investigated the magnetic field dependence of the response of a detective coil near a rotating superconducting ring. The responses of the MTG sample are different for different cooling methods. 相似文献
23.
根据托海拱坝5号坝段、7号坝段例垂线实测资料分析,说明了新疆寒冷地区坝体采取聚胺脂喷涂施工措施后对坝体变形的影响,以及右坝肩渗漏对右坝肩岩体的影响,分析结果为托海水电站通过国家电力公司大坝安全监察中心大坝安全首次定检提供了科学依据。 相似文献
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Asymptotic stability of finite-dimensional linear continuous-time periodic (FDLCP) systems is studied by harmonic analysis. It is first shown that stability can be examined with what we call the harmonic Lyapunov equation. Another necessary and sufficient stability criterion is developed via this generalized Lyapunov equation, which reduces the stability test into that of an approximate FDLCP model whose transition matrix can be determined explicitly. By extending the Gerschgorin theorem to linear operators on the linear space l2, yet another disc-group criterion is derived, which is only sufficient. Stability of the lossy Mathieu equation is analyzed as a numerical example to illustrate the results 相似文献
28.
Successful operation of the Synchronous Overlap and Add (SOLA) algorithm for Time Scale Modification (TSM) of speech is closely tied to the proper choice of parameters. This paper investigates the quality of time scale modified speech under different values of primary parameters. Based on Mean Opinion Score (MOS) tests and Bark Spectral Distortion (BSD) measure, the proper choices of synthesis shift (Ss) and the duration of the shift search interval (K max?) are given experimentally. The conclusions can be helpful for operating the SOLA algorithm for time scale modification of speech. 相似文献
29.
XIAO Chang-jiang SUN Ming ZHOU Hong-yan LIU Sui-xin LONG Kai-chao HE Fei LI Tong 《中南工业大学学报(英文版)》2005,12(Z1)
Objective Study on the effect of NF-κB in ox-LDL injured HUVEC-304 and the intervention with the serum of Tongmai Decoction. Methods Tongmai Decoction herbage-contained serum was made by the serum pharmacology methods, then the HUVEC-304 cells were divided into 5 groups and incubated for 24 h: 1) normal group;2) fetal calf serum group; 3) ox-LDL group; 4) simvastatin group; 5) Tongmai Decoction group. RT-PCR was used to determine the mRNA of NF-κB in the cells, Western Blot Assay was used to determine the protein content of NF-κB in the cells. Results 1) Compared with the cells in normal group and serum control group , the endothelial cells in ox-LDL group are seriously injured, while those in Tongmai Decoction group grow better; 2) Compared with the cells in normal group and fetal calf serum group, the expressions of NF-κB gene and protein are up-regulated in ox-LDL group(P<0.05, P<0.01); 3) Compared with the cells in ox-LDL group, the expression of NF-κB gene and protein in Tongmai Decoction group are significantly down-regulated, there is no difference between Tongmai Decoction group and simvastatin group(P>0.05). Conclusion Tongmai Decoction can protect the injured endothelial cells, up-regulate the expressions of NF-κB gene and protein content. 相似文献