作者机构：
[Wang, Zhe; Liu, Yunmei; Zou, Liu; Liu, Juan; Zheng, X; Tang, GT; Tang, Guotao; Zheng, Xing; Deng, Xiangping; Xie, Zhizhong; Lei, Xiaoyong; Xiong, Shujuan; Xiong, Runde; Cao, Xuan] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang, Peoples R China.;[Chen, Yanming] Mu Dan Jiang You Bo Pharmacert Co Ltd, Mudanjiang, Peoples R China.
通讯机构：
[Zheng, X; Tang, GT] U;Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang, Peoples R China.
关键词：
Chrysin;benzimidazole;synthesis;anticancer
摘要：
A series of chrysin benzimidazole derivatives were synthesised and evaluated for their anticancer activity in the search for potential anticancer agents. Among them, compound 18 displayed the most potent anti-proliferative activity against MFC cells with IC50 values of 25.72 ± 3.95 μM. The flow cytometry results displayed that compound 18 induced apoptosis of MFC cells in a dose-dependent manner and caused the cell cycle to be arrested in the G0/G1 phase. Furthermore, the preliminary anticancer activity in vivo was also studied in tumour-bearing mice, and the compound 18 exerted good inhibition effect on tumour growth. These results suggested that compound 18 had good anticancer activity, which could be a potential anticancer agent after further optimisation and evaluation.
摘要：
Apelin is the endogenous peptide APJ receptor, while APJ is a member of the G protein-coupled receptors family. Recent evidence strongly suggests that Apelin/APJ system influences apoptosis in various diseases through different signal pathways. In this review, we discuss the possible mechanisms by which the Apelin/APJ system inhibits apoptosis, including the phosphatidylinositol-3-kinase (PI3K)/Akt, ERK1/2, caspase signaling, and autophagy pathway. We also summarize the role of Apelin/APJ system in apoptosis in myocardial ischemia-reperfusion (l/R) injury, pulmonary artery hypertension, retinal neovascular disease, acute renal injury, skeletal homeostasis, and gastrointestinal diseases. Apelin/APJ system decreases myocardial infarction size and alleviates myocardial l/R injury by inhibiting cardiomyocytes apoptosis. However, Apelin/APJ system improves pulmonary artery hypertension via increasing apoptosis. Apelin/APJ system exerts neuroprotective effect by blocking apoptosis and participates in the recovery of retinal neovascular disease by suppressing apoptosis. Apelin/APJ system also shows anti-apoptotic effect against acute renal injury and plays a role in regulating skeletal homeostasis. In gastrointestinal disease, Apelin/APJ system plays a potential physiological role in gastrointestinal cytoprotection by regulating apoptosis. We hope that a better understanding of the Apelin/APJ system will help to discover new disease pathogenesis and find possible therapeutic targets of the Apelin/APJ system essential for various diseases.
作者机构：
[Liu, Jie; He, Ruo-Hui; Zhou, Hong-Hao; Tang, Yong-Jun; He, Yi-Jing] Cent S Univ, Xiangya Hosp, Dept Clin Pharmacol, Changsha 410008, Hunan, Peoples R China.;[Liu, Jie; He, Ruo-Hui; Zhou, Hong-Hao; Tang, Yong-Jun; He, Yi-Jing] Cent S Univ, Hunan Key Lab Pharmacogenet, Inst Clin Pharmacol, Changsha 410078, Hunan, Peoples R China.;[Liu, Jie; He, Ruo-Hui; Zhou, Hong-Hao; Tang, Yong-Jun; He, Yi-Jing] Univ South China, Cooperat Innovat Ctr Mol Target New Drug Study, Hengyang 421001, Hunan, Peoples R China.;[McLeod, Howard L.] H Lee Moffitt Canc Ctr & Res Inst, Div Populat Sci, DeBartolo Family Personalized Med Inst, Tampa, FL 33612 USA.
通讯机构：
[Liu, Jie] C;Cent S Univ, Xiangya Hosp, Dept Clin Pharmacol, Changsha 410008, Hunan, Peoples R China.
关键词：
cancer progression;polymorphisms;tumor biology behaviors;beta-adrenergic receptors;beta-blockers
摘要：
β-ARs are extensively spread in different tissues of our body, which could be activated by neurotransmitters norepinephrine and epinephrine to mediate physiological function and abnormal states including cancer. Recently, β-AR blockers could have significant implications in cancer therapy. But the precise molecular mechanisms are far from being fully understood. Through identifying the β-AR system signal pathways relevant to cancer, we can understand the mechanisms of β-blockers used for cancer treatment. What's more, retrospective clinical data made β-blockers jump out of the traditional field of cardiovascular disease and strengthened our confidence in cancer therapy. At last, genetic studies of β-adrenergic system offered crucial genes to analyze the effects of polymorphisms on cancer susceptibility, therapy response and prognosis of cancer patients.
作者：
Liu, Ai Ling*;Liao, Hong Qing;Li, Zhi Liang;Liu, Jun;Zhou, Cui Lan;...
期刊：
Asian Pacific Journal of Cancer Prevention,2016年17(12):5087-5094 ISSN：1513-7368
通讯作者：
Liu, Ai Ling
作者机构：
[Xie, Hong Yan; Li, Zhi Liang; Peng, Cui Ying; Liu, Ai Ling; Liu, Jun] Institute of Biological Science, The Key Laboratory of Biological Toxicology and Ecological Restoration of Hengyang City, School of Pharmaceutical and Biological Science, Heng Yang, Hunan Province, 421001, China;[Liao, Hong Qing] Reproductive Health Hospital of Nanhua-Xinghui in Hengyang City, Heng Yang, Hunan Province, 421001, China;[Zhou, Cui Lan] Department of Anatomy, University of South China, Heng Yang, Hunan Province, 421001, China;[Guo, Zi Fen] Institute of Pharmacy and Pharmacology, University of South China, Heng Yang, Hunan Province, 421001, China
通讯机构：
[Liu, Ai Ling] I;Institute of Biological Science, The Key Laboratory of Biological Toxicology and Ecological Restoration of Hengyang City, School of Pharmaceutical and Biological Science, University of South China, Heng yang 421001, Hunan Province, China. Email:
关键词：
Liu, Ai Ling;Liao, Hong Qing;Li, Zhi Liang;Liu, Jun;Zhou, Cui Lan;Guo, Zi Fen;Xie, Hong Yan;Peng, Cui Ying;mTOR signaling pathway;PCOS;ovarian cancer
摘要：
mTOR, the mammalian target of rapamycin, is a conserved serine/threonine kinase which belongs to the phosphatidyl-linositol kinase-related kinase (PIKK) family. It has two complexes called mTORC1 and mTORC2. It is well established that mTOR plays important roles in cell growth, proliferation and differentiation. Over-activation of the mTOR pathway is considered to have a relationship with the development of many types of diseases, including polycystic ovary syndrome (PCOS) and ovarian cancer (OC). mTOR pathway inhibitors, such as rapamycin and its derivatives, can directly or indirectly treat or relieve the symptoms of patients suffering from PCOS or OC. Moreover, mTOR inhibitors in combination with other chemical-molecular agents may have extraordinary efficacy. This paper will discuss links between mTOR signaling and PCOS and OC, and explore the mechanisms of mTOR inhibitors in treating these two diseases, with conclusions regarding the most effective therapeutic approaches.
摘要：
In order to investigate Cd accumulation, subcellular distribution, and local-ization in soybean seedlings leaves, soybean seedlings were cultivated in solution containing different concentrations of Cd. The results showed that most Cd associ-ated with the cellwal s and soluble fractions, and a minor part of Cd presented in mitochondria fractions, nuclear and chloroplast fractions, especial y exposure to high Cd concentrations. Under 20.00 mg/L Cd stress, Cd subcellular distribution fol owed a sequence as： soluble fractions （55.00%）＆gt;cellwal s （30.0%）＆gt;mitochondria fractions （8.21%）＆gt;nuclear and chloroplast fractions （6.79%）. Deposited Cd black particles were observed in cellwal s, chloroplasts, nuclei, and vacuoles through electrical microscope slice. This fact indicated that the cellwal s of soybean leaves were the first protecting organel es from Cd toxicity, and the cellwal s and soluble fractions were the main place for Cd storage. Due to Cd accumulated in the organel es, the intercellular space was enlarged and the subcellular structure was damaged, especial y for the chloroplasts.
摘要：
目的:研究乙型肝炎病毒(hepatitis B virus,HBV)重组腺病毒对HepG2细胞的IL-17R和接头蛋白Actl表达的影响,以及HBV对IL-17诱导NF-kB活化的影响.方法:采用实时荧光定量PCR(real-time PCR)检测HepG2细胞的IL-17、IL-17R和Actl的mRNA表达;蛋白免疫印迹法(Westem blot)检测IL-17R和Actl的蛋白表达；免疫荧光检测NF-kB核移位；ELISA检测上清的IL-17含量.结果:各组HepG2细胞培养上清液中均未检测到1L-17且亦未检测HepG2细胞有IL-17的mRNA表达；HBV重组腺病毒组的IL-17RmRNA和蛋白的表达明显低于相应浓度对照组(0.68±0.02 vs 0.89±0.03,0.33±0.06 vs0.81±0.01,0.12±0.01 vs 0.86±0.05,P＜0.05;蛋白:0.84±0.12 vs l.01±0.13,0.56±0.09vs l.01±0.08,0,24±0.08 vs 0.98±0.05),且呈剂量和时间依赖性.但HBV重组腺病毒组与对照组比较,对HepG2细胞接头蛋白Actl的mRNA和蛋白表达水平无明显影响；同时HBV重组腺病毒能抑制IL-17R诱导HepG2细胞的NF-kB活化,但HBV重组腺病毒与对照组比较,对接头蛋白Acti在mRNA和蛋白表达水平上影响无明显变化；同时HBV重组腺病毒能抑制IL- 17 R诱-导HepG2细胞的NF-kB活化,结论:HBV重组腺病毒可降低HepG2细胞的IL- 17R mRNA和蛋白的表达,抑制IL-17R诱导HepG2细胞的NF-kB活化,对HepG2细胞的IL-17R信号通路发挥抑制作用.
