期刊：
Journal of Heterocyclic Chemistry,2015年52(1):296-301 ISSN：0022-152X
通讯作者：
Zheng, Xing
作者机构：
[Liu, Yun-Mei; Wang, Hui; Wang, Yu-Hong; Yao, Xu; Zheng, Xing] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.;[Liao, Duan-Fang; Zheng, Xing] Hunan Univ Chinese Med, Div Stem Cell Regulat & Applicat, State Key Lab Chinese Med Powder & Med Innovat Hu, Changsha 410208, Hunan, Peoples R China.;[Tong, Min] Xianyang Cent Hosp, Xianyang 712000, Shanxi, Peoples R China.
通讯机构：
[Zheng, Xing] U;Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.
摘要：
A series of trifluoromethylated aurone derivatives were synthesized, and the structure of 6‐hydroxy‐4‐trifluoromethylated aurone was determined by single crystal X‐ray analysis. Their anticancer activities against leucocythemia (HL‐60) and colorectal adenocarcinoma (HT‐29) were evaluated by the standard MTT method in vitro with 5‐fluorouracil as a positive contrast drug. The results showed that all the (Z)‐trifluoromethylated aurone derivatives had potential anticancer activities.
摘要：
Nasopharyngeal carcinoma (NPC) has the highest metastasis rate among head and neck cancers with unclear mechanism. WNT5A belongs to the WNT family of cysteine-rich secreted glycoproteins. Our previous high-throughput gene expression profiling revealed that WNT5A was up-regulated in highly metastatic cells. In the present study, we first confirmed the elevated expression of WNT5A in metastatic NPC tissues at both the mRNA and protein levels. We then found that WNT5A promoted epithelial-mesenchymal transition (EMT) in NPC cells, induced the accumulation of CD24-CD44+ cells and side population, which are believed to be cancer stem cell characteristics. Moreover, WNT5A promoted the migration and invasion of NPC cells in vitro, while in vivo treatment with recombinant WNT5A promoted lung metastasis. Knocking down WNT5A diminished NPC tumorigenesis in vivo. When elevated expression of WNT5A coincided with the elevated expression of vimentin in the primary NPC, the patients had a poorer prognosis. Among major signaling pathways, protein kinase C (PKC) signaling was activated by WNT5A in NPC cells. A positive feedback loop between WNT5A and phospho-PKC to promote EMT was also revealed. Taken together, these data suggest that WNT5A is an important molecule in promoting stem cell characteristics in NPC, leading to tumorigenesis and metastasis.
作者：
Wang, J.;Zou, T.;Yang, H. X.;Gong, Y. Z.;Xie, X. J.;...
期刊：
Genetics and Molecular Research,2015年14(3):8819-8828 ISSN：1676-5680
通讯作者：
Liu, H. Y.
作者机构：
[Yang, H. X.; Wang, J.] Univ South China, Key Lab Atherosclerol Hunan Prov, Inst Cardiovasc Res, Hengyang, Hunan, Peoples R China.;[Yang, H. X.; Wang, J.] Univ South China, Sch Publ Hlth, Hengyang, Hunan, Peoples R China.;[Zou, T.] Univ South China, Affiliated Hosp 1, Dept Cardiovasc Med, Hengyang, Hunan, Peoples R China.;[Gong, Y. Z.; Xie, X. J.; Liao, D. F.] Hunan Univ Chinese Med, State Key Lab Chinese Med Powder & Med Innovat Hu, Div Stem Cell Regulat & Applicat, Changsha, Hunan, Peoples R China.;[Liu, H. Y.] Metammune LLC, Morrisville, NC 27560 USA.
通讯机构：
[Liu, H. Y.] M;Metammune LLC, Morrisville, NC 27560 USA.
关键词：
Yiminsu;Insulin sensitizer;Type 2 diabetes;IgG4 Fc
摘要：
Insulin resistance is a key feature of obesity and type 2 diabetes mellitus (T2DM). Interaction of insulin with the insulin receptor (IR) leads to both its auto-phosphorylation and phosphorylation of tyrosine residues on the IR substrate (IRS) proteins, initiating the activation of intracellular signaling cascades. The metabolic effects of IRS are known to be mediated through pathways involving phosphatidyl-inositol 3-kinase (PI-3K), which result in the activation of Akt signaling. The C-terminal region of the IR ectodomain is required to facilitate the conformational changes that are required for high-affinity binding to insulin. Furthermore, the CH2 and CH3 domains in the Fc fragments of immunoglobulins are responsible for their binding to the Fc receptor, which triggers transcytosis. In this study, we created a fusion peptide of the C-terminal end of the human IR ectodomain with the IgG4 Fc fragment, including an intervening polyG fragment to ensure enough space for insulin binding. We named this new peptide "Yiminsu", meaning an insulin sensitizer. The results of our analyses show that Yiminsu significantly facilitates insulin signaling via the activation of Akt in hepatocytes in a dose- and time-dependent manner. Further studies are required to determine whether Yiminsu can act as an insulin sensitizer.
作者机构：
Hunan University of Chinese Medicine, Changsha, 410208, China;[李春] Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing, 100700, China;Hunan Engineering Center for Rapid Test and Removal of Toxic and Harmful Substances in Chinese Medicine, Changsha, 410208, China;[李亚梅; 周亚敏; 皮胜玲; 廖端芳; 林丽美; 柏玉冰; 夏伯候] Hunan University of Chinese Medicine, Changsha, 410208, China, Hunan Engineering Center for Rapid Test and Removal of Toxic and Harmful Substances in Chinese Medicine, Changsha, 410208, China
通讯机构：
[Lin, L.-M.] H;Hunan University of Chinese Medicine, Changsha, China
作者机构：
[王智; 廖端芳; 彭买姣; 严建业; 罗堃; 王炜] Key Laboratory of Modernization of Chinese Materia Medica, School of Pharmacy, Hunan University of Chinese Medicine, Changsha, 410208, China;[王元清] Laboratory of Biotechnology and Engineering, College of Life Science and Technology, Central South University of Forestry and Technology, Changsha, 410004, China;[朱承慧] School of Pharmacy, Jinan University, Guangzhou, 510632, China;[席秀利] School of Chinese Materia Medica, Guangzhou University of Chinese Medicine, Guangzhou, 510006, China
通讯机构：
[Liao, D.-F.] K;Key Laboratory of Modernization of Chinese Materia Medica, School of Pharmacy, Hunan University of Chinese Medicine, Changsha, China
关键词：
细辛;炮制;黄樟醚;马兜铃酸A;高效液相法;炒焦
摘要：
目的研究细辛中马兜铃酸 A与黄樟醚炮制减毒方法。方法采用HPLC法,对细辛生品及各个炮制品中黄樟醚、马兜铃酸A的量进行检测,以其量变化为评价指标比较不同炮制方法对毒性物质的去除效果。结果黄樟醚进样量在169.2~ 846.0 μg(r=0.999 6)有良好线性关系,平均回收率为99.83%,RSD为1.67%;马兜铃酸A进样量在11.6~58.0 ng有良好线性关系,平均回收率为101.43%,RSD为1.25%。黄樟醚的炮制去除效果的大小顺序为盐制>炒焦>米泔水制>碱制>甘草制>醋制>姜制>酒制>碱醋制>蜜制,其中盐制与炒焦对细辛中黄樟醚的去除率达到55%以上;马兜铃酸 A 的炮制去除效果的大小顺序为炒焦>碱醋制>盐制>碱制>醋制>米泔水制>甘草制>酒制>蜜制>姜制,其中炒焦对细辛中马兜铃酸A的去除率达到60%以上。结论细辛炮制后,黄樟醚和马兜铃酸 A的量都有不同程度的降低,其中以炒焦炮制最优。
