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Sicheng Shen Weiping Wang Zijun Chen Huihui Zhang Yuchun Yang Xiaoliang Wang Peng Fu Bingnan Han 《Marine drugs》2021,19(11)
Potassium channel Kv1.5 has been considered a key target for new treatments of atrial tachyarrhythmias, with few side effects. Four new debromoaplysiatoxin analogues with a 6/6/12 fused ring system were isolated from marine cyanobacterium Lyngbya sp. Their planar structures were elucidated by HRESIMS, 1D and 2D NMR. The absolute configuration of oscillatoxin J (1) was determined by single-crystal X-ray diffraction, and the absolute configurations of oscillatoxin K (2), oscillatoxin L (3) and oscillatoxin M (4) were confirmed on the basis of GIAO NMR shift calculation followed by DP4 analysis. The current study confirmed the absolute configuration of the pivotal chiral positions (7S, 9S, 10S, 11R, 12S, 15S, 29R and 30R) at traditional ATXs with 6/12/6 tricyclic ring system. Compound 1, 2 and 4 exhibited blocking activities against Kv1.5 with IC50 values of 2.61 ± 0.91 µM, 3.86 ± 1.03 µM and 3.79 ± 1.01 µM, respectively. However, compound 3 exhibited a minimum effect on Kv1.5 at 10 µM. Furthermore, all of these new debromoaplysiatoxin analogs displayed no apparent activity in a brine shrimp toxicity assay. 相似文献
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Soo Hwa Jang Pan Dong Ryu So Yeong Lee 《Journal of veterinary science (Suw?n-si, Korea)》2011,12(1):35-40
Voltage-gated K+ (Kv) channels have been considered to be a regulator of membrane potential and neuronal excitability. Recently, accumulated evidence has indicated that several Kv channel subtypes contribute to the control of cell proliferation in various types of cells and are worth noting as potential emerging molecular targets of cancer therapy. In the present study, we investigated the effects of the Kv1.1-specific blocker, dendrotoxin-κ (DTX-κ), on tumor formation induced by the human lung adenocarcinoma cell line A549 in a xenograft model. Kv1.1 mRNA and protein was expressed in A549 cells and the blockade of Kv1.1 by DTX-κ, reduced tumor formation in nude mice. Furthermore, treatment with DTX-κ significantly increased protein expression of p21Waf1/Cip1, p27Kip1, and p15INK4B and significantly decreased protein expression of cyclin D3 in tumor tissues compared to the control. These results suggest that DTX-κ has anti-tumor effects in A549 cells through the pathway governing G1-S transition. 相似文献
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廊道式人工湿地处理污水过程中氨氮的去除效果研究 总被引：2，自引：0，他引：2
通过廊道式人工湿地(CCW)的生产性试验工程,研究了该处理系统的性能及系统内部氨氮的变化规律.结果表明,CCW处理系统的去除效率高且稳定,氨氮的去除率平均为88%,质量去除率平均为(6.94±2.07)gN·m-2·d-1,系统内部第三单元的氨氮质量去除率最高;CCW处理系统的氨氮质量负荷率小于10gN·m-2·d-1时,质量去除率与质量负荷率呈明显的线性相关,质量负荷率大于等于20gN·m-2·d-1时,进水浓度和出水浓度之间呈明显线性相关;处理系统各处理单元及系统整体的体积去除率常数(Kv值)均大于其他湿地处理系统;CCW处理系统氨氮浓度变化与pH值的变化趋势并不一致. 相似文献
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