1,25-(OH)_2D_3 protects pancreatic beta cells against H_2O_2-induced apoptosis through inhibiting the PERK-ATF4-CHOP pathway
作者：
Hu, Xiaobo;Hu, Cong;Liu, Jun;Wu, Zhuan;Duan, Tingting;...
期刊：
生物化学与生物物理学报 ,2021年53(1):46-53 ISSN：1672-9145
通讯作者：
Zhaohui Cao
作者机构：
[Hu, Cong; Cao, Zhaohui; Hu, Xiaobo; Duan, Tingting; Liu, Jun; Wu, Zhuan] Univ South China, Hengyang Med Sch, Dept Biochem, Key Lab Ecol Environm & Crit Human Dis Prevent Hu, Hengyang 421001, Peoples R China.;[Hu, Cong; Cao, Zhaohui; Hu, Xiaobo; Duan, Tingting; Liu, Jun; Wu, Zhuan] Univ South China, Hengyang Med Sch, Dept Biochem, Hengyang 421001, Peoples R China.;[Hu, Cong; Cao, Zhaohui; Hu, Xiaobo; Duan, Tingting; Wu, Zhuan] Univ South China, Key Lab Typ Environm Pollut & Hlth Hazards, Hengyang 421001, Peoples R China.;[Hu, Cong] Yiyang Cent Hosp, Yiyang 413000, Peoples R China.
通讯机构：
[Zhaohui Cao] T;The Key Laboratory of Ecological Environment and Critical Human Diseases Prevention of Hunan Province Department of Education, Department of Biochemistry, Hengyang Medical School, University of South China , Hengyang 421001, China<&wdkj&>Department of Biochemistry, Hengyang Medical School, University of South China , Hengyang 421001, China<&wdkj&> The Key Laboratory of Typical Environmental Pollution and Health Hazards, University of South China , Hengyang 421001, China
关键词：
1,25-(OH)2D3;MIN6 cells;PERK;diabetes;endoplasmic reticulum stress
摘要：
Endoplasmic reticulum (ER) stress plays a critical role in pancreatic beta cell destruction which leads to the pathogenesis of type 1 diabetes mellitus (T1DM). Vitamin D (VD) has been reported to reduce the risk of T1DM; however, it remains unknown whether VD affects ER stress in pancreatic beta cells. In this study, we investigated the role of the active form of VD, 1,25-dihydroxyvitamin D3 [1,25-(OH)(2)D-3], in ER stress-induced beta cell apoptosis and explored its potential mechanism in mouse insulinoma cell line mouse insulinoma 6 (MIN6). The results of cell counting kit-8 (CCK8) and flow cytometric analyses showed that 1,25-(OH)(2)D-3 caused a significant increase in the viability of MIN6 cells injured by H2O2. The protein kinase like ER kinase (PERK) signal pathway, one of the most conserved branches of ER stress, was found to be involved in this process. H2O2 activated the phosphorylation of PERK, upregulated the activating transcription factor 4 (ATF4) and C/EBP homologous protein (CHOP) expression, and subsequently initiated cell apoptosis, which were significantly reversed by 1,25-(OH)(2)D-3 pretreatment. In addition, GSK2606414, a specific inhibitor of PERK, suppressed PERK phosphorylation and reduced the expressions of ATF4 and CHOP, leading to a significant decrease in beta cell apoptosis induced by H2O2. Taken together, the present findings firstly demonstrated that 1,25-(OH)(2)D-3 could prevent MIN6 cells against ER stress-associated apoptosis by inhibiting the PERK-ATF4-CHOP pathway. Therefore, our results suggested that 1,25-(OH)(2)D-3 might serve as a potential therapeutic target for preventing pancreatic beta cell destruction in T1DM.
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Effect of vitamin D supplementation on pancreatic β-cell destruction and type 1 diabetes
作者：
Hu Xiao-Bo;Duan Ting-Ting;Liu Jun;Zhu Gao-Lu;Cao Zhao-Hui;...
期刊：
中华医学杂志(英文版) ,2021年134(1):41-43 ISSN：0366-6999
作者机构：
[Shao-Long Feng] The Institute of Preventive Medicine, School of Public Health, Guilin Medical University, Guilin, Guangxi 541004, China.;[Ting-Ting Duan; Gao-Lu Zhu] The Key Laboratory of Ecological Environment and Critical Human Diseases Prevention, Education Department of Hunan Province, Department of Biochemistry, Hengyang Medical School, University of South China, Hengyang, Hunan 421001, China;The Key Laboratory of Typical Environmental Pollution and Health Hazards, Hunan Province, University of South China, Hengyang, Hunan 421001, China;[Xiao-Bo Hu; Jun Liu; Zhao-Hui Cao] The Key Laboratory of Ecological Environment and Critical Human Diseases Prevention, Education Department of Hunan Province, Department of Biochemistry, Hengyang Medical School, University of South China, Hengyang, Hunan 421001, China<&wdkj&>The Key Laboratory of Typical Environmental Pollution and Health Hazards, Hunan Province, University of South China, Hengyang, Hunan 421001, China
摘要：
Type 1 diabetes (T1D) is an organ-specific autoimmune disease with loss of pancreatic β-cells, characterized by reduced insulin levels and increased blood glucose. The incidence of T1D is increasing by approximately 2% to 5% worldwide every year and becoming a global health problem. Vitamin D (VD) deficiency was reported to be a risk factor in the development of T1D. Recent studies showed that supplementation of VD alleviated disease symptoms in T1D patients. However, a few randomized controled trials (RCTs) demonstrated the clinical effect of VD treatment with inconsistent findings. This article aimed to evaluate the effect of VD supplementation in T1D, which is helpful to develop an adjuvant therapy for T1D.
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FB-15 inhibits MGC-803 cells growth by regulating energy metabolism
作者：
Deng, Xiangping;Pi, Yiyuan;Li, Zhongli;Xiong, Runde;Liu, Juan;...
期刊：
Chemico-Biological Interactions ,2020年327:109186 ISSN：0009-2797
通讯作者：
Lei, Xiaoyong;Tang, Guotao
作者机构：
[Deng, Xiangping; Xie, Zhizhong; Li, Zhongli; Liu, Juan; Lei, Xiaoyong; Pi, Yiyuan; Zhao, Jingduo; Tang, Guotao; Xiong, Runde] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang City, Hunan, Peoples R China.;[Deng, Xiangping; Xie, Zhizhong; Lei, Xiaoyong; Pi, Yiyuan; Zhao, Jingduo; Tang, Guotao] Hunan Prov Key Lab Tumor Microenvironm Respons Dr, Hengyang City, Hunan, Peoples R China.;[Pi, Yiyuan] Xiangnan Univ, Chenzhou City, Hunan, Peoples R China.;[Lei, XY; Tang, Guotao] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.
通讯机构：
[Lei, XY; Tang, GT] U;Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.
关键词：
Antitumor;FB-15;HIF-1α;MGC-803;Tubulin
摘要：
In this study, we scrutinized the anticancer effects of FB-15 on human gastric carcinoma MGC-803 cells in vitro and vivo, and its preliminary effect on tubulin and HIF-1α. We confirmed that FB-15 not only inhibited the proliferation of a large number of cells in a concentration and time-dependent manner but also inhibited proliferation of a single cell to form clones. FB-15 manifested little cytotoxicity for normal stomach cells GES-1. The flow cytometry analysis displayed that FB-15 induced apoptosis MGC-803 cells and mainly arrested cells in the S phase in a concentration-dependent manner. The results of the wound healing assay indicated that FB-15 suppressed cell migration. Furthermore, the western blotting showed that FB-15 down-regulated the expression of β3-tubulin and HIF-1α, consistent with Immunohistochemical assay. The binding modes of FB-15 with tubulin were clarified by molecular docking. FB-15 significantly suppressed the growth of MGC-803 gastric cancer tumors. The inhibitory effect of FB-15 on tumor growth was superior to 5-Fu. Taken together, these results provided evidence for FB-15 to be used as an effective anticancer drug candidate for gastric cancer. © 2020 Elsevier B.V.
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Nobiletin reduces LPL-mediated lipid accumulation and pro-inflammatory cytokine secretion through upregulation of miR-590 expression
作者：
He, Ping-Ping;Shen, Qian-Qian;Wen, Min;Zou, Jie-Qiong;Wang, Yan;...
期刊：
Biochemical and Biophysical Research Communications ,2019年508(1):97-101 ISSN：0006-291X
通讯作者：
Ouyang, Xin-Ping;Tang, Chao-Ke
作者机构：
[Liu, Juan; He, Ping-Ping; Zou, Jie-Qiong; Shen, Qian-Qian; Wang, Yan; Wen, Min; Chen, Ye-Shi; Yang, Jiao-Xing; Su, Hua; Hu, Li-Zhi] Univ South China, Sch Nursing, Hengyang 421001, Hunan, Peoples R China.;[He, Ping-Ping; Ouyang, Xin-Ping; Tang, Chao-Ke] Univ South China, Inst Cardiovasc Res, Key Lab Atherosclerol Hunan Prov, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Hunan, Peoples R China.;[Liu, Juan; Zou, Jie-Qiong; Wang, Yan; Yang, Jiao-Xing; Hu, Li-Zhi] Univ South China, Affiliated Hosp 1, Hengyang 421001, Hunan, Peoples R China.;[Zheng, Xi -Long] Univ Calgary, Dept Biochem & Mol Biol, Libin Cardiovasc Inst Alberta, Cumming Sch Med,Hlth Sci Ctr, 3330 Hosp Dr NW, Calgary, AB T2N 4N1, Canada.;[Ouyang, Xin-Ping] Univ South China, Dept Physiol, Neurosci Inst, Hengyang Med Coll, Hengyang 421001, Hunan, Peoples R China.
通讯机构：
[Ouyang, Xin-Ping; Tang, Chao-Ke] U;Univ South China, Dept Physiol, Hengyang 421001, Hunan, Peoples R China.;Univ South China, Inst Cardiovasc Res, Hengyang 421001, Hunan, Peoples R China.
关键词：
*Atherosclerosis;*LPL;*MiR-590;*Nobiletin
摘要：
Nobiletin has protective effects on cardiovascular diseases, but the mechanism is not clear. In this study, we examined whether nobiletin affects the expression of miR-590/LPL and its relative effects on lipid accumulation and pro-inflammatory cytokine secretion in human THP-1 macrophages. RT-qPCR analysis showed that nobiletin increased the expression of miR-590. Western blot analysis showed that nobiletin-suppressed LPL expression was enhanced by miR-590 mimic and abrogated by miR-590 inhibitor. Oil Red 0 staining and high-performance liquid chromatography assays showed that nobiletin attenuated lipid accumulation in macrophages. Treatment with nobiletin and miR-590 mimic decreased cellular lipid accumulation, whereas treatment with miR-590 inhibitor increased cellular lipid accumulation. ELISA illustrated that nobiletin alleviated pro-inflammatory cytokine secretion in macrophages as measured by, which was reduced by miR-590 mimic and increased by miR-590 inhibitor. In conclusion, nobiletin may alleviate lipid accumulation and secretion of pro-inflammatory cytokines by enhancing the inhibitory effect of miR-590 on LPL expression, suggesting a promising strategy for potential drug development for atherosclerosis. (C) 2018 Elsevier Inc. All rights reserved.
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英文
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Therapeutic activity of DCC-2036, a novel tyrosine kinase inhibitor, against triple-negative breast cancer patient-derived xenografts by targeting AXL/MET
作者：
Shen, Yingying;Zhang, Wei;Liu, Jianghua;He, Jun;Cao, Renxian;...
期刊：
International Journal of Cancer ,2019年144(3):651-664 ISSN：0020-7136
通讯作者：
Zu, Xuyu;Jiang, Yuyang
作者机构：
[Zhong, Jing; Zu, Xuyu; Cao, Renxian; Peng, Xiuda; Liu, Jianghua; Ding, Wenjun; Shen, Yingying] Univ South China, Inst Clin Med, Affiliated Hosp 1, 69 Chuanshan Rd, Hengyang 421001, Hunan, Peoples R China.;[Zhang, Wei] Tsinghua Univ, Sch Med, Dept Biol, Beijing, Peoples R China.;[Cao, Renxian; Liu, Jianghua] Univ South China, Affiliated Hosp 1, Dept Metab & Endocrinol, Hengyang, Hunan, Peoples R China.;[He, Jun] Univ South China, Affiliated Hosp 1, Dept Spine Surg, Hengyang, Hunan, Peoples R China.;[Chen, Xiguang] Univ South China, Affiliated Hosp 1, Dept Med Oncol, Hengyang, Hunan, Peoples R China.
通讯机构：
[Zu, Xuyu] U;[Jiang, Yuyang] T;Univ South China, Inst Clin Med, Affiliated Hosp 1, 69 Chuanshan Rd, Hengyang 421001, Hunan, Peoples R China.;Tsinghua Univ, Grad Sch Shenzhen, Guangdong Prov Key Lab Chem Biol, Lishui Rd, Shenzhen 518055, Peoples R China.
关键词：
*AXL;*DCC-2036;*MET;*PDX;*TNBC
摘要：
Triple-negative breast cancer (TNBC) is insensitive to endocrine therapies and targeted therapies to human epidermal growth factor receptor-2 (HER2), estrogen receptor (ER) and progesterone receptor (PR). New targets and new targeted therapeutic drugs for TNBC are desperately needed. Our study confirmed that DCC-2036 inhibited the proliferation, invasion, migration and epithelial-mesenchymal transition (EMT) of TNBC cells as well as induced apoptosis. Moreover, the antiproliferative activity of DCC-2036 was more efficient than that of most clinical drugs. In addition, the combination of DCC-2036 and cisplatin or lapatinib had synergistic effects on TNBC cells. Mechanistically, DCC-2036 targeted AXL/MET, especially AXL, and regulated the downstream PI3K/Akt-NFkappaB signaling to exert its antitumor effect in TNBC. DCC-2036 also inhibited the growth and metastasis of xenografted MDA-MB-231 cells (AXL/MET-high TNBC cells) but not MDA-MB-468 cells (AXL-low TNBC cells) in NSG mice in vivo. Furthermore, DCC-2036 significantly inhibited tumor growth and invasion of AXL/MET-high TNBC PDX tumors but not AXL/MET-low TNBC PDX tumors. These results highlighted the roles of AXL/MET in cancer growth and metastasis and further verified that the critical targets of DCC-2036 are AXL and MET, especially AXL. In addition, there was no significant toxicity of DCC-2036 even at a high dosage. Therefore, DCC-2036 may be a potential compound to treat TNBC, especially for tumors with AXL/MET overexpression.
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英文
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Design, synthesis and broad-spectrum Bcr-Abl inhibitory activity of novel thiazolamide-benzamide derivatives
作者：
Liu, Juan;Huang, Honglin;Deng, Xiangping;Xiong, Runde;Cao, Xuan;...
期刊：
RSC Advances ,2019年9(4):2092-2101 ISSN：2046-2069
通讯作者：
Peng, Junmei
作者机构：
[Xu, Shiyu; Deng, Xiangping; Liu, Juan; Huang, Honglin; Tang, Guotao; Wu, Xin; Peng, Junmei; Xiong, Runde; Cao, Xuan] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang, Peoples R China.
通讯机构：
[Peng, Junmei] U;Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang, Peoples R China.
摘要：
Bcr-Abl plays an important role in the pathogenesis and development of chronic myeloid leukemia (CML). But Bcr-Abl is prone to mutation, so it increases the difficulty of clinical treatment. Therefore, it is crucial to design a new class of broad-spectrum Bcr-Abl inhibitors. Herein, forty novel thiazolamide-benzamide derivatives were synthesized and evaluated their broad-spectrum Bcr-Abl inhibitory activities. The newly synthesized compounds were characterized by using spectrum data ( 1 H NMR, APCI-MS and IR) and elemental analysis. The protein kinase results indicated that eight compounds (3a, 3e, 3m, 3n, 3p, 4c, 4f, 4g) showed high activities to wild-type and T315I mutation. The most potent compound 3m exhibited an Abl IC 50 value as low as 1.273 μM and showed inhibition to the T315I mutant with IC 50 value 39.89 μM. 3m could prove to be a new promising lead compound for the further development of broad-spectrum Bcr-Abl inhibitors to overcome clinical acquired resistance. © The Royal Society of Chemistry.
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英文
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A pH-sensitive prodrug strategy to co-deliver DOX and TOS in TPGS nanomicelles for tumor therapy
作者：
Xiong, Shujuan;Wang, Zhe;Liu, Juan;Deng, Xiangping;Xiong, Runde;...
期刊：
Colloids and Surfaces B: Biointerfaces ,2019年173:346-355 ISSN：0927-7765
通讯作者：
Tang, Guotao
作者机构：
[Wang, Zhe; Deng, Xiangping; Xie, Zhizhong; Liu, Juan; Lei, Xiaoyong; Xiong, Shujuan; Tang, Guotao; Xiong, Runde; Cao, Xuan] Univ South China, Inst Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang, Peoples R China.;[Xiong, Shujuan] Peoples Hosp Yiyang, Yiyang, Peoples R China.;[Chen, Yanming] Jiuzhitang Co Ltd, Changsha, Hunan, Peoples R China.;[Tang, Guotao] Univ South China, Changsheng Rd 28, Hengyang 421001, Hunan, Peoples R China.
通讯机构：
[Tang, Guotao] U;Univ South China, Changsheng Rd 28, Hengyang 421001, Hunan, Peoples R China.
关键词：
Co-delivery;Low toxicity;pH-sensitive;Prodrug;Tumor therapy
摘要：
This work has presented a novel strategy for designing pH-sensitive TOS-H-DOX prodrug-loaded TPGS nanomicelles for co-delivery TOS and DOX to enhance tumor therapy and reduce the toxic side effects. DOX was covalently conjugated to the vitamin E succinate through hydrazone bond to produce an pH-sensitive prodrug TOS-H-DOX (amido bond as a control, TOS-A-DOX), which was responsive to the acidic environment in tumor cells, and the prodrugs were subsequently encapsulated in the core of TPGS nanomicelles via hydrophobic effects with a significant drug loading capacity. The pH-sensitive prodrug nanomicelles TOS-H-DOX/TPGS exhibited potent release of DOX in acidic media relative to the pH-insensitive prodrug nanomicelles TOS-A-DOX/TPGS, and further studies of their intracellular uptake and intracellular localization demonstrated that TOS-H-DOX/TPGS nanomicelles can be effectively taken up by cells and drugs can be released. In vitro results confirmed that TOS-H-DOX/TPGS nanomicelles exhibited significant antitumor cell proliferation activity compared to TOS-A-DOX/TPGS and free DOX, TPGS. Furthermore, in vivo studies further confirmed an excellent synergistic antitumor efficacy in MCF-7 tumor-bearing nude mice model. More importantly, the H&E staining of the heart, liver, kidney tissue sections of experimental nude mice showed that TOS-H-DOX/TPGS nanomicelles can reduce damage to them. © 2018 Elsevier B.V.
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英文
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FS-7 inhibits MGC-803 cells growth in vitro and in vivo via down-regulating glycolysis
作者：
Deng, Xiangping;Li, Zhongli;Xiong, Runde;Liu, Juan;Liu, Renbo;...
期刊：
Biomedicine & Pharmacotherapy ,2019年109:1659-1669 ISSN：0753-3322
通讯作者：
Xie, Zhizhong;Tang, Guotao
作者机构：
[Li, Zhongli; Liu, Juan; Tang, Guotao; Peng, Junmei; Zheng, Xing; Deng, Xiangping; Xie, Zhizhong; Liu, Renbo; Lei, Xiaoyong; Xiong, Runde; Cao, Xuan] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target, Inst Pharm & Pharmacol, Hengyang, Peoples R China.;[Chen, Yanming] Jiuzhitang Co Ltd, Changsha, Hunan, Peoples R China.;[Xie, ZZ; Tang, GT] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.
通讯机构：
[Xie, ZZ; Tang, GT] U;Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.
关键词：
FS-7;MGC-803;Anticancer;HIF-1 alpha;Glycolysis
摘要：
In this study, we investigated the anticancer effects of FS-7, a flavonoid salicylate derivative, in human gastric carcinoma MGC-803 cell line and studied its preliminary anticancer effects. FS-7 displayed greater in vitro cytotoxicity against MGC-803 cell line compared with 5-Fu and had a certain extent of selectivity to cancer cells. The flow cytometry analysis revealed that FS-7 induced apoptosis MGC-803 cells and mainly caused cells arrest in the G2/M phase in a concentration-dependent manner. Additionally, FS-7 inhibited the colony formation and cell migration in a concentration-dependent manner. Notably, FS-7 noticeably down-regulated glycolysis-related protein HIF-1 alpha, HK-II and PFKP expression in a concentration-dependent manner, possibly causing glycolysis inhibition. Importantly, compared with 5-Fu, FS-7 showed better anticancer activity in the MGC-803 xenograft murine tumor models. Collectively, the present study provided a promising anticancer drug candidate for gastric cancer therapy.
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英文
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β-blockers inhibit the viability of breast cancer cells by regulating the ERK/COX-2 signaling pathway and the drug response is affected by ADRB2 single-nucleotide polymorphisms
作者：
Xie, Wan-Ying;He, Ruo-Hui;Zhang, Jun;He, Yi-Jing;Wan, Zan;...
期刊：
ONCOLOGY REPORTS ,2019年41(1):341-350 ISSN：1021-335X
通讯作者：
Liu, Jie
作者机构：
[Xie, Wan-Ying; Liu, Jie; Mcleod, Howard L.; He, Ruo-Hui; Li, Zhi; Tang, Yong-Jun; Wan, Zan; He, Yi-Jing; Zhou, Cheng-Fang] Cent S Univ, Xiangya Hosp, Dept Clin Pharmacol, 110 Xiangya Rd, Changsha 410008, Hunan, Peoples R China.;[Xie, Wan-Ying; Liu, Jie; He, Ruo-Hui; Li, Zhi; Wan, Zan; He, Yi-Jing; Zhou, Cheng-Fang] Cent S Univ, Inst Clin Pharmacol, Hunan Key Lab Pharmacogenet, Changsha 410078, Hunan, Peoples R China.;[Liu, Jie; He, Ruo-Hui; Li, Zhi; He, Yi-Jing] Univ South China, Cooperat Innovat Ctr Mol Target New Drug Study, Hengyang 421001, Hunan, Peoples R China.;[Zhang, Jun] Cent S Univ, Xiangya Hosp, Dept Nephrol, Changsha 410008, Hunan, Peoples R China.;[Tang, Yong-Jun] Cent S Univ, Xiangya Hosp, Dept Pediat, Changsha 410008, Hunan, Peoples R China.
通讯机构：
[Liu, Jie] C;Cent S Univ, Xiangya Hosp, Dept Clin Pharmacol, 110 Xiangya Rd, Changsha 410008, Hunan, Peoples R China.
关键词：
3 isopropylamino 1 (7 methyl 4 indanyloxy) 2 butanol;beta 2 adrenergic receptor;beta adrenergic receptor blocking agent;cyclooxygenase 2;messenger RNA;metoprolol;mitogen activated protein kinase 1;mitogen activated protein kinase 3;propranolol;3 isopropylamino 1 (7 methyl 4 indanyloxy) 2 butanol;ADRB2 protein, human;beta 2 adrenergic receptor;beta adrenergic receptor blocking agent;cyclooxygenase 2;mitogen activated protein kinase;propanolamine derivative;propranolol;PTGS2 protein, human;ADRB2 gene;apoptosis;Article;breast cancer cell line;cell viability;controlled study;ERK COX 2 signaling pathway;G1 phase cell cycle checkpoint;human;human cell;MDA-MB-231 cell line;priority journal;protein phosphorylation;single nucleotide polymorphism;cell survival;down regulation;drug effect;drug screening;G2 phase cell cycle checkpoint;gene expression regulation;genetics;HEK293 cell line;metabolism;phosphorylation;signal transduction;triple negative breast cancer;tumor cell line;Adrenergic beta-Antagonists;Apoptosis;Cell Line, Tumor;Cell Survival;Cyclooxygenase 2;Down-Regulation;Drug Screening Assays, Antitumor;Extracellular Signal-Regulated MAP Kinases;G2 Phase Cell Cycle Checkpoints;Gene Expression Regulation, Neoplastic;HEK293 Cells;Humans;Phosphorylation;Polymorphism, Single Nucleotide;Propanolamines;Propranolol;Receptors, Adrenergic, beta-2;Signal Transduction;Triple Negative Breast Neoplasms
摘要：
The β 2 -adrenergic receptor (β 2 -AR, encoded by the ADRB2 gene) is a member of the G-protein-coupled receptor superfamily that can be stimulated by catecholamines. Studies in vivo and in vitro have confirmed that β-blockers (β-AR antagonists) exert antitumor effects on various tumors. Furthermore, ADRB2 single-nucleotide polymorphisms (SNPs) have been identified to alter the expression and conformation of β 2 -AR, which may alter the β-blocker drug response. The aim of the present study was to investigate the effect of β-blockers on triple-negative breast cancer cells and determine whether ADRB2 SNPs affect the response to β-blocker drugs. Propranolol and ICI 118,551 significantly inhibited the viability of MDA-MB-231 cells, arrested cell cycle progression at G 0 /G 1 and S phase and induced cell apoptosis. Western blot analysis indicated that the phosphorylation levels of extracellular-signal-regulated kinase (ERK)1/2 and the expression levels of cyclo-oxygenase 2 (COX-2) were significantly decreased following β-blocker treatment. Four haplotypes, which comprised ADRB2 SNPs rs1042713 and rs1042714, were transfected into 293 cells. After 24 and 48 h of transfection, ADRB2 mRNA expression was significantly decreased in mutant groups compared with the wild-type group. The ADRB2 SNPs exerted no effect on cell viability, but did affect the drug response of ICI 118,551. Furthermore, ADRB2 SNPs also affected the regulatory function of ICI 118,551 on the ERK/COX-2 signaling pathway. Collectively, propranolol and ICI 118,551 inhibited the viability of MDA-MB-231 cells by downregulating the ERK/COX-2 signaling pathway and inducing apoptosis. The results of the present study indicated that SNPs rs1042713 and rs1042714 of ADRB2 affected the response to ICI 118,551, and the underlying molecular mechanism was elucidated. © 2019 Spandidos Publications. All rights reserved.
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Design, synthesis, and preliminary biological evaluation of 3′,4′,5′-trimethoxy flavonoid salicylate derivatives as potential anti-tumor agents
作者：
Deng, Xiangping;Liu, Renbo;Li, Junjian;Li, Zhongli;Liu, Juan;...
期刊：
NEW JOURNAL OF CHEMISTRY ,2019年43(4):1874-1884 ISSN：1144-0546
通讯作者：
Tang, Guotao
作者机构：
[Deng, Xiangping; Xie, Zhizhong; Li, Zhongli; Liu, Renbo; Liu, Juan; Lei, Xiaoyong; Tang, Guotao; Li, Junjian; Xiong, Runde; Zheng, Xing] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.
通讯机构：
[Tang, Guotao] U;Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.
关键词：
4 [5 (4 methyl 1 piperazinyl)[2,5' bi 1h benzimidazol] 2' yl]phenol;6 phosphofructokinase;7 hydroxy 2 (3,4,5 trimetocyphenyl) 4h chromen 4 one;antineoplastic agent;flavonoid;fluorouracil;hypoxia inducible factor 1alpha;salicylic acid derivative;tubulin;unclassified drug;antineoplastic activity;apoptosis;Article;cell cycle;colony formation;controlled study;crystal structure;drug cytotoxicity;drug design;drug synthesis;female;flow cytometry;HCT 116 cell line;human;human cell;priority journal;Western blotting
摘要：
According to the pharmacophore combination principle, a set of new 3′,4′,5′-trimethoxy flavonoid salicylate derivatives were designed, synthesized, and evaluated for biological activity. The cytotoxicity evaluation revealed that compound 10v exhibited higher potency than 5-Fu against HCT-116 cells. Preliminary biological activity studies showed that compound 10v could inhibit the colony formation and migration of HCT-116 cells. Besides, the Hoechst 33258 staining assay and flow cytometry revealed that treatment with compound 10v induced the apoptosis of HCT-116 cells in a concentration-dependent manner, while it had no effect on their cell cycle. The WB analysis suggested that HIF-1α, tubulin, HK-2, and PFK might be the potential pharmacophore targets of compound 10v. Tubulin was a potential drug target for compound 10v, which was explained by analyzing the crystal structure of compound 10v complexed with tubulin. These results indicated that compound 10v might be a promising anti-tumor agent candidate, deserving further optimization and evaluation. © The Royal Society of Chemistry and the Centre National de la Recherche Scientifique.
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Anti-proliferative activity and structure-activity relationship of honokiol derivatives.
作者：
Lin, Ding;Yan, Zhongzhong;Chen, Aiyu;Ye, Jiao;Hu, Aixi* ;...
期刊：
Bioorganic & Medicinal Chemistry ,2019年27(16):3729-3734 ISSN：0968-0896
通讯作者：
Hu, Aixi
作者机构：
[Lin, Ding; Ye, Jiao; Chen, Aiyu; Yan, Zhongzhong; Hu, Aixi] Hunan Univ, Coll Chem & Chem Engn, Changsha 410082, Hunan, Peoples R China.;[Lin, Ding] Zhejiang A&F Univ, Dept Tradit Chinese Med, Hangzhou 311300, Zhejiang, Peoples R China.;[Liu, Juan; Peng, Junmei] Univ South China, Coll Pharm & Biol Sci, Hengyang 421000, Peoples R China.;[Wu, Xiaoyun] Southern Med Univ, Guangdong Prov Key Lab New Drug Screening, Sch Pharmaceut Sci, Guangzhou 510515, Guangdong, Peoples R China.
通讯机构：
[Hu, Aixi] H;Hunan Univ, Coll Chem & Chem Engn, Changsha 410082, Hunan, Peoples R China.
关键词：
3D-QASR;Anti-proliferative;Honokiol;Structure-activity relationship;Theoretical calculations
摘要：
As a known natural product with anti-tumor activity, honokiol has been widely researched and structural modified. Lots of honokiol derivatives have been found to possess good anti-proliferative activity and showed great potential in cancer therapy, but the SAR (structure-activity relationship) was still confused. Here in, the SAR were comprehensively researched by summary of reported derivatives and synthesis of novel derivatives. Amongst novel derivatives, the promising compounds A6 and A10 exhibited potent and selective anti-proliferative activities against K562 cell line with the IC50 values of 5.04 and 7.08 μM respectively. The SAR was discussed around honokiol and 79 derivatives by the means of CoMFA and theoretical calculation, which provided useful suggestion for further structural optimization of honokiol derivatives. © 2019 Elsevier Ltd
语种：
英文
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Design, synthesis and biological evaluation of tryptamine salicylic acid derivatives as potential antitumor agents.
作者：
Xiong, Runde;He, Dongxiu;Deng, Xiangping;Liu, Juan;Lei, Xiaoyong;...
期刊：
RSC Medicinal Chemistry ,2019年10(4):573-583 ISSN：2632-8682
通讯作者：
Tang, Guotao
作者机构：
[Deng, Xiangping; Xie, Zhizhong; Liu, Juan; Lei, Xiaoyong; Tang, Guotao; He, Dongxiu; Peng, Junmei; Xiong, Runde; Cao, Xuan] Univ South China, Inst Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang, Peoples R China.;[Chen, Yanming] Jiuzhitang Co Ltd, Changsha, Hunan, Peoples R China.
通讯机构：
[Tang, Guotao] U;Univ South China, Inst Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang, Peoples R China.
关键词：
2 hydroxy 3 methyl n [2 (5 methyl 1h indol 3 yl)ethyl] benzamide;2 hydroxy 4 methyl n [2 (5 methyl 1h indol 3 yl)ethyl] benzamide;2 hydroxy n [2 (1h indol 3 yl)ethyl] 3 methyl benzamide;2 hydroxy n [2 (1h indol 3 yl)ethyl] 4 methyl benzamide;2 hydroxy n [2 (1h indol 3 yl)ethyl]benzamide;2 hydroxy n [2 (5 methyl 1h indol 3 yl)ethyl]benzamide;4 chloro 2 hydroxy n [2 (1h indol 3 yl)ethyl]benzamide;4 chloro 2 hydroxy n [2 (5 methyl 1h indol 3 yl)ethyl]benzamide;4 chloro n [2 (5 chloro 1h indol 3 yl)ethyl] 2 hydroxybenzamide;5 bromo 2 hydroxy n [2 (1h indol 3 yl)ethyl]benzamide;5 bromo 2 hydroxy n [2 (5 methyl 1h indol 3 yl)ethyl] benzamide;5 bromo n [2 (5 bromo 1h indol 3 yl)ethyl] 2 hydroxybenzamide;5 bromo n [2 (5 chloro 1h indol 3 yl) ethyl] 2 hydroxybenzamide;5 chloro 2 hydroxy n [2 (1h indol 3 yl)ethyl]benzamide;5 chloro 2 hydroxy n [2 (5 methyl 1h indol 3 yl)ethyl]benzamide;5 chloro n [2 (5 chloro 1h indol 3 yl)ethyl] 2 hydroxybenzamide;antineoplastic agent;hexokinase;hexokinase 2;n [2 (5 bromo 1h indol 3 yl)ethyl] 2 hydroxy 3 methyl benzamide;n [2 (5 bromo 1h indol 3 yl)ethyl] 2 hydroxy 3 methylbenzamide;n [2 (5 bromo 1h indol 3 yl)ethyl] 2 hydroxy 4 methylbenzamide;n [2 (5 bromo 1h indol 3 yl)ethyl] 2 hydroxy benzamide;n [2 (5 bromo 1h indol 3 yl)ethyl] 4 chloro 2 hydroxybenzamide;n [2 (5 bromo 1h indol 3 yl)ethyl] 5 chloro 2 hydroxybenzamide;n [2 (5 chloro 1h indol 3 yl) ethyl] 2 hydroxy 4 methylbenzamide;n [2 (5 chloro 1h indol 3 yl)ethyl] 2 hydroxy 3 methylbenzamide;n [2 (5 chloro 1h indol 3 yl)ethyl] 2 hydroxy benzamide;salicylic acid derivative;unclassified drug;A-549 cell line;antineoplastic activity;antiproliferative activity;apoptosis;Article;cancer inhibition;cell migration;concentration response;down regulation;drug design;drug determination;drug potency;drug structure;drug synthesis;drug targeting;flow cytometry;G2 phase cell cycle checkpoint;HeLa cell line;Hep-G2 cell line;in vitro study;MCF-7 cell line;priority journal;protein expression;structure activity relation;Western blotting
摘要：
A series of tryptamine salicylic acid derivatives were synthesized and their antiproliferative activity against MGC-803, MCF-7, HepG2, A549 and HeLa cell lines was evaluated. The structure-activity relationship (SAR) study revealed that different substitutions of the C5 and C3′-C5′ positions have certain effects on the anti-proliferation activity. The growth assay revealed that N-[2-(5-bromo-1H-indol-3-yl)-ethyl]-2-hydroxy-3-methyl-benzamide (E20) showed the most potent and broad-spectrum anticancer inhibition of all the cell lines evaluated, and was only more potent than 5-Fu for the gastric cancer cell line. Preliminary studies indicated that compound E20 could inhibit colony formation and migration of MGC-803 cells. The flow cytometry (FCM) results showed that compound E20 arrested the cell cycle in the G2/M phase and induced apoptosis of MGC-803 cells in a concentration-dependent manner. In addition, the western blot results showed that E20 can down-regulate the expression of hexokinase 2. Our studies suggest that the framework of N-[2-(5-bromo-1H-indol-3-yl)-ethyl]-2-hydroxy-3-methyl-benzamide may be consider as a new type of chemical for designing effective anti-cancer drugs targeting gastric cancer cells. © 2019 The Royal Society of Chemistry.
语种：
英文
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Apelin/APJ system: A critical regulator of vascular smooth muscle cell
作者：
Luo, Xuling;Liu, Jiaqi;Zhou, Hong* ;Chen, Linxi*
期刊：
JOURNAL OF CELLULAR PHYSIOLOGY ,2018年233(7):5180-5188 ISSN：0021-9541
通讯作者：
Zhou, Hong;Chen, Linxi
作者机构：
[Luo, Xuling; Liu, Jiaqi; Zhou, Hong; Chen, Linxi] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.
通讯机构：
[Zhou, H; Chen, LX] U;Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.
关键词：
apelin;apelin receptor;apelin;apelin receptor;APLNR protein, human;atherosclerosis;blood vessel calcification;cell function;cell migration;cell proliferation;chronic kidney failure;human;hypertension;muscle contraction;muscle relaxation;nonhuman;priority journal;Review;vascular disease;vascular smooth muscle cell;cardiac muscle cell;cell motion;genetics;MAPK signaling;metabolism;pathology;pathophysiology;smooth muscle cell;vascular smooth muscle;Apelin;Apelin Receptors;Atherosclerosis;Cell Movement;Cell Proliferation;Humans;Hypertension;MAP Kinase Signaling System;Muscle, Smooth, Vascular;Myocytes, Cardiac;Myocytes, Smooth Muscle;Renal Insufficiency, Chronic
摘要：
APJ, an orphan G protein-coupled receptor, is first identified through homology cloning in 1993. Apelin is endogenous ligand of APJ extracted from bovine stomach tissue in 1998. Apelin/APJ system is widely expressed in many kinds of cells such as endothelial cells, cardiomyocytes, especially vascular smooth muscle cell. Vascular smooth muscle cell (VSMC), an integral part of the vascular wall, takes part in many normal physiological processes. Our experiment firstly finds that apelin/APJ system enhances VSMC proliferation by ERK1/2-cyclin D1 signal pathway. Accumulating studies also show that apelin/APJ system plays a pivotal role in mediating the function of VSMC. In this paper, we review the exact role of apelin/APJ system in VSMC, including induction of proliferation and migration, enhance of contraction and relaxation, inhibition of calcification. Furthermore, we discuss the role of apelin/APJ system in vascular diseases, such as atherosclerosis, hypertension, and chronic kidney disease (CKD) from the point of VSMC. Above all, apelin/APJ system is a promising target for managing vascular disease. © 2017 Wiley Periodicals, Inc.
语种：
英文
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Design, synthesis and biological evaluation of 3′,4′,5′-trimethoxy flavonoid benzimidazole derivatives as potential anti-tumor agents
作者：
Wang, Zhe;Deng, Xiangping;Xiong, Runde;Xiong, Shujuan;Liu, Juan;...
期刊：
RSC Medicinal Chemistry ,2018年9(2):305-315 ISSN：2632-8682
通讯作者：
Zheng, Xing;Tang, Guotao
作者机构：
[Wang, Zhe; Deng, Xiangping; Liu, Juan; Lei, Xiaoyong; Xiong, Shujuan; Zheng, Xing; Tang, Guotao; Xiong, Runde; Cao, Xuan] Univ South China, Inst Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang, Peoples R China.;[Chen, Yanming] Mu Dan Jiang You Bo Pharmaceut Co Ltd, Mudanjiang, Peoples R China.
通讯机构：
[Zheng, X; Tang, GT] U;Univ South China, Inst Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang, Peoples R China.
关键词：
3',4',5' trimethoxy flavonoid benzimidazole derivative;7 (2 bromoethoxy) 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 (3 bromopropoxy) 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 (4 bromobutoxy) 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 hydroxy 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [2 [1h benz[d]imidazol 1 yl]ethoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [2 [2 chloro 1h benz[d]imidazol 1 yl]ethoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [2 [2 methyl 1h benz[d]imidazol 1 yl]ethoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [2 [2 [trifluoromethyl] 1h benz[d]imidazol 1 yl]ethoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [2 [5 methoxy 1h benz[d]imidazol 1 yl]ethoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [2 [5 methyl 1h benz[d]imidazol 1 yl]ethoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [2 [5,6 dimethyl 1h benz[d]imidazol 1 yl]ethoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [2 [6 nitro 1h benz[d]imidazol 1 yl]ethoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [3 (2 chloro 1h benz[d]imidazol 1 yl)propoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [3 [1h benz[d]imidazol 1 yl]propoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [3 [2 chloro 1h benz[d]imidazol 1 yl]propoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [3 [2 methyl 1h benz[d]imidazol 1 yl]propoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [3 [2 [trifluoromethyl] 1h benz[d]imidazol 1 yl]propoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [3 [5 methoxy 1h benz[d]imidazol 1 yl]propoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [3 [5 methyl 1h benz[d]imidazol 1 yl]propoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [3 [5,6 dimethyl 1h benz[d]imidazol 1 yl]propoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [3 [6 nitro 1h benz[d]imidazol 1 yl]propoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [4 [1h benz[d]imidazol 1 yl]butoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [4 [2 chloro 1h benz[d]imidazol 1 yl]butoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [4 [2 methyl 1h benz[d]imidazol 1 yl]butoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [4 [5 nitro 1h benz[d]imidazol 1 yl]butoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;antineoplastic agent;benzimidazole derivative;flavonoid;fluorouracil;unclassified drug;unindexed drug;animal cell;antineoplastic activity;antiproliferative activity;apoptosis;Article;controlled study;cytotoxicity assay;drug design;drug synthesis;flow cytometry;G1 phase cell cycle checkpoint;human;human cell;IC50;in vitro study;in vivo study;mouse;nonhuman;priority journal;tumor growth
摘要：
A series of 3′,4′,5′-trimethoxy flavonoids with benzimidazole linked by different chain alkanes have been designed and synthesized. The potential activity of these compounds as anti-tumor agents was evaluated by cytotoxicity assay in MGC-803 (human gastric cancer), MCF-7 (human breast cancer), HepG-2 (human hepatoma) and MFC (mouse gastric cancer) tumor cell lines. Among them, compound 15 7-(3-(2-chloro-1H-benzo[d]imidazol-1-yl)propoxy)-2-(3,4,5-trimethoxyphenyl)-4H-chromen-4-one displayed the most potent antiproliferative activity, with IC50 values of 20.47 ± 2.07, 43.42 ± 3.56, 35.45 ± 2.03 μM and 23.47 ± 3.59 μM, respectively. The flow cytometry (FCM) results showed that compound 15 caused the cell cycle to be arrested in G1 phase and induced apoptosis of MFC cells in a dose-dependent manner. In addition, compound 15 exhibited a significant inhibitory effect on tumor growth in vivo. All the results outlined the great potential of compound 15 for further exploitation as anti-tumor agent. © 2018 The Royal Society of Chemistry.
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英文
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PREPARATION OF SCUTELLARIN LOADED TPGS POLYMERIC MICELLES AND EVALUATION OF ITS PHARMACOKINETICS AND PHARMACODYNAMICS EFFECTS IN RATS
作者：
Zou, Liu;Xiong, Shujuan;Deng, Xiangping;Liu, Juan;Xiong, Runde;...
期刊：
ACTA POLONIAE PHARMACEUTICA ,2018年75(6):1305-1312 ISSN：0001-6837
通讯作者：
Guo, Yu;Tang, Guo Tao
作者机构：
[Wang, Zhe; Deng, Xiangping; Guo, Yu; Zou, Liu; Liu, Juan; Xiong, Shujuan; Guo, Y; Tang, Guo Tao; Xiong, Runde; Cao, Xuan] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang, Peoples R China.;[Zou, Liu] Liuzhou Municipal Matern & Child Healthcare Hosp, Liuzhou, Guangxi, Peoples R China.;[Chen, Yanming] Jiuzhitang Co Ltd, Beijing, Peoples R China.
通讯机构：
[Guo, Y; 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：
scutellarin;TPGS;polymeric micelles;antithrombotic drugs
摘要：
To improve the clinical effect of scutellarin by extending the action time in vivo, scutellarin loaded polymeric micelles were developed by D-alpha tocopherol polyethylene glycol 1000 succinate (Scu/TPGS). Scu/TPGS were prepared using film solvent diffusion methods and characterized on the basis of their particle size, zeta potential, and drug encapsulation efficiency. Dynamic dialysis was used to study the release behavior of the polymeric micelles in vitro. Its pharmacokinetic characteristics and antithrombotic efficacy were studied by intravenous injection in rats. The results showed that Scu/TPGS were spherical, 20.09 +/- 2.62 nm in size and a slow release in vitro. The pharmacokinetic parameter T-1/2 of Scu/TPGS was 762.12 +/- 46.56 min compared with commercial injection of 59.30 +/- 10.67 min (p < 0.05). At the 1 mg/kg dose, the thrombolysis effect of micellar group was stronger than that of the commercial group (p < 0.05). In conclusion, TPGS polymer micelles provided a valid strategy in chemotherapy for cerebrovascular diseases with poor water solubility and poor lipid solubility drugs such as scutellarin.
语种：
英文
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ROS-Autophagy pathway mediates monocytes-human umbilical vein endothelial cells adhesion induced by apelin-13
作者：
Liu, Meiqing;Li, Hening;Zhou, Qun;Zhao, Hong;Lv, Deguan;...
期刊：
JOURNAL OF CELLULAR PHYSIOLOGY ,2018年233(10):6839-6850 ISSN：0021-9541
通讯作者：
Chen, Zhe;Li, Lanfang;Chen, Linxi
作者机构：
[Huang, Shifang; Lv, Deguan; Jiang, Jinyong; Tang, Mingzhu; Wu, Di; Liu, Meiqing; Zhao, Hong; Hu, Haoliang; Chen, Zhe; Li, Lanfang; Chen, Linxi; Liu, Jiaqi; Li, Hening; He, Lu; Zhou, Qun; Cao, Jiangang; Wu, Lele] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.;[Liu, Meiqing] Second Peoples Hosp Yunnan Prov, Dept Pharm, Kunming, Yunnan, Peoples R China.;[Li, Hening] First Peoples Hosp Yueyang, Dept Pharm, Yueyang, Hunan, Peoples R China.;[Zhou, Qun] Hunan Univ Med, Coll Pharm, Huaihua, Peoples R China.
通讯机构：
[Chen, Z; Li, LF; Chen, LX] U;Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.
关键词：
acetylcysteine;apelin;apelin 13;beclin 1;catalase;hydroxychloroquine;intercellular adhesion molecule 1;rapamycin;reactive oxygen metabolite;reduced nicotinamide adenine dinucleotide phosphate oxidase;reduced nicotinamide adenine dinucleotide phosphate oxidase 4;small interfering RNA;unclassified drug;apelin-13 peptide;reactive oxygen metabolite;reduced nicotinamide adenine dinucleotide phosphate oxidase;signal peptide;animal experiment;animal model;animal tissue;Article;atherosclerosis;atherosclerotic plaque;autophagosome;autophagy;cell adhesion;controlled study;coronary artery tissue;human;human cell;immunohistochemistry;monocyte;mouse;nonhuman;oxidative stress;priority journal;protein expression;THP-1 cell line;umbilical vein endothelial cell;animal;autophagy;cell culture;drug effect;knockout mouse;metabolism;monocyte;physiology;signal transduction;umbilical vein;umbilical vein endothelial cell;Animals;Autophagy;Cells, Cultured;Human Umbilical Vein Endothelial Cells;Humans;Intercellular Signaling Peptides and Proteins;Mice, Knockout;Monocytes;NADPH Oxidases;Reactive Oxygen Species;Signal Transduction;Umbilical Veins
摘要：
Apelin is the endogenous ligand of APJ receptor. Both monocytes (MCs) and human umbilical vein endothelial cells (HUVECs) express apelin and APJ, which play important roles in the physiological processes of atherosclerosis. Our previous research indicated that apelin-13 promoted MCs-HUVECs adhesion. Here, we further explore the mechanism responsible for MCs-HUVECs adhesion induced by apelin-13. Apelin-13 promoted reactive oxygen species (ROS) generation and NOX4 expression in HUVECs. Apelin-13 inducedautophagy, increased proteins beclin1 and LC3-II/I expression and induced autophagy flux in HUVECs, which was blocked by NAC, catalase and DPI. Autophagy flux induced by apelin-13 was inhibited by NAC and catalase but not hydroxychloroquine (HCQ). NAC, catalase, and DPI prevented apelin-13 induced ICAM-1 expression in HUVECs. Rapamycin enhanced MCs–HUVECs adhesion that was reversed by NAC, catalase, and DPI. Down-regulation of beclin1 and LC3 by siRNA blocked MCs-HUVECs adhesion. Apelin-13 induced atherosclerotic plaque and increased NOX4, LC3-II/I expression in ApoE−/−(HFD) mouse model. Our results demonstrated that apelin-13 induced MCs–HUVECs adhesion via a ROS-autophagy pathway. © 2018 Wiley Periodicals, Inc.
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英文
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案例+讨论式教学法在研究生《生态学》教学中的应用
作者：
刘俊;胡劲松;朱允华;谢红艳;彭翠英
期刊：
教育教学论坛 ,2018年(29):237-238 ISSN：1674-9324
作者机构：
南华大学药学与生物科学学院,生物毒理与生态修复衡阳市重点实验室,湖南 衡阳 421001;[朱允华; 胡劲松; 刘俊; 彭翠英; 谢红艳] 南华大学
关键词：
讨论式教学法;研究生;创新教育;探索
摘要：
为了顺应社会对生物学高级专业创新型人才的需求,根据案例教学法和讨论教学法的特点,学校修订了生物学专业硕士研究生的《生态学》教学大纲,并组建了专门的教学团队。在教师的引导下,研究生围绕教学案例自主查阅文献、组织材料,进行课堂案例讨论。案例+讨论式教学既提高了研究生的创新能力和语言组织、表达能力,也增强了学生自主学习、获取知识的能力。
语种：
中文
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Synthesis and evaluation of antitumour activity in vitro and in vivo of chrysin salicylate derivatives
作者：
Deng, Xiangping;Zhao, Zihao;Xiong, Shujuan;Xiong, Runde;Liu, Juan;...
期刊：
Natural Product Research ,2018年32(18):2178-2186 ISSN：1478-6419
通讯作者：
Liu, Yunmei;Tang, Guotao
作者机构：
[Wang, Zhe; Liu, Yunmei; Zou, Liu; Liu, Juan; Tang, Guotao; Zheng, Xing; Deng, Xiangping; Xie, Zhizhong; Liu, YM; Tang, GT; Lei, Xiaoyong; Xiong, Shujuan; Zhao, Zihao; Xiong, Runde; Cao, Xuan] Univ South China, Inst Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang, Peoples R China.;[Zhao, Zihao] Xiangtan Cent Hosp, Pharm Dept, Xiangtan, Peoples R China.;[Chen, Yanming] Mu Dan Jiang You Bo Pharmacert Co Ltd, Mudanjiang, Peoples R China.
通讯机构：
[Liu, YM; Tang, GT] U;Univ South China, Inst Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang, Peoples R China.
关键词：
antineoplastic agent;chrysin;chrysin salicylate derivative;fluorouracil;salicylic acid derivative;unclassified drug;antineoplastic agent;chrysin;flavonoid;salicylic acid derivative;animal experiment;animal model;animal tissue;antineoplastic activity;Article;cancer cell line;cell cycle G1 phase;cell cycle S phase;controlled study;drug efficacy;drug megadose;drug potency;drug screening;drug structure;drug synthesis;flow cytometry;Hep-G2 cell line;human;human cell;IC50;in vitro study;in vivo study;MCF-7 cell line;MFC cell line;MGC-803 cell line;mouse;nonhuman;stomach carcinoma;animal;cell proliferation;drug effect;structure activity relation;synthesis;tumor cell line;Animals;Antineoplastic Agents;Cell Line, Tumor;Cell Proliferation;Drug Screening Assays, Antitumor;Flavonoids;Hep G2 Cells;Humans;MCF-7 Cells;Mice;Salicylates;Structure-Activity Relationship
摘要：
A series of chrysin salicylate derivatives as potential antitumour agents were synthesised and evaluated their antitumour activities in vitro and in vivo. Most of the compounds exhibited moderate to good activities against MCF-7 cells, HepG2 cells, MGC-803cells and MFC cells. Among them, compound 3f showed the most potent activity against MGC-803 cells and MFC cells with IC50 values of 23.83±3.68 and 27.34±5.21μM, respectively. The flow cytometry assay reconfirmed that compound 3f promoted the occurrence of tumour cells’ G1/S block under the inhibiting effect of compound 3f. Compound 3f possessed higher antitumour efficacy in tumour-bearing mice, compared with the positive control 5-Fu and the blank control saline. © 2017, © 2017 Informa UK Limited, trading as Taylor & Francis Group.
语种：
英文
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Expression and Purification of Tag-removed Human IL37 by Digestion on Beads in Escherichia coli
作者：
Wu, Daichao;Li, Guoqing;Ma, Yao;Liu, Jin;Li, Yukun;...
期刊：
PROTEIN AND PEPTIDE LETTERS ,2018年25(11):996-1002 ISSN：0929-8665
通讯作者：
Chen, Yongheng;Tan, Sijie;Li, Meixiang
作者机构：
[Li, Yukun; Tan, Sijie; Bai, Junhui; Liu, Jin; Li, Meixiang; Wu, Daichao; Wang, Juan] Univ South China, Hengyang Med Coll, Inst Clin Anat & Reprod Med, Dept Histol & Embryol, Hengyang 421001, Hunan, Peoples R China.;[Wu, Daichao; Li, Guoqing] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Hunan, Peoples R China.;[Ma, Yao] Univ South China, Network Informat Ctr, Hengyang 421001, Hunan, Peoples R China.;[Chen, Yongheng] Cent S Univ, XiangYa Hosp, Chinese Minist Hlth, Lab Struct Biol,Key Lab Canc Prote, Changsha 410008, Hunan, Peoples R China.;[Chen, Yongheng] Cent S Univ, XiangYa Hosp, Changsha 410008, Hunan, Peoples R China.
通讯机构：
[Chen, Yongheng] C;[Tan, SJ; Li, MX] U;Cent S Univ, XiangYa Hosp, Changsha 410008, Hunan, Peoples R China.;Univ South China, Hengyang Med Coll, Hengyang 421000, Peoples R China.
关键词：
Soluble expression;purification;interleukin 37;Escherichia coli;digestion on beads;inflammatory diseases.
摘要：
Background: Human Interleukin 37 (IL37), a unique anti-inflammatory cytokine of IL1 family member, plays critical roles in innate and adaptive immunity and inflammation. Objective: Preparation of high purity and tag-removed recombinant IL37 protein (rIL37) is critical for its clinical application. Method: In this study, we constructed an N-terminal cleavable GST-fused IL37 expression vector for recombinant expression. Results: Subsequent to transformation and optimization of the induction temperature, the soluble expression level of rIL37 was 306.5 mg/L of culture medium at 18 °C induction in Escherichia coli. Meanwhile, rIL37 was digested on beads by GST-HRV3C protease during GST affinity chromatography. After further purification, the purity of rIL37 was higher than 99 %. Finally, the anti-inflammatory activity of tag-removed protein was verified by the results showing that rIL37 suppressed IL1β production in PBMCs. Conclusion: This work presents a protocol to produce high purity and tag-removed rIL37 with anti-inflammatory activity, which provides the firm basis for advancing clinical application in human IL37-related inflammatory diseases. © 2018 Bentham Science Publishers.
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英文
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基于生态系统理论的和谐家庭经营与建设方法创新
作者：
刘俊;张红艳;朱允华;胡劲松;彭翠英
期刊：
南华大学学报(社会科学版) ,2018年19(5):59-63 ISSN：1673-0755
作者机构：
南华大学药学与生物科学学院,湖南衡阳,421001;[胡劲松; 朱允华; 张红艳; 刘俊; 彭翠英] 南华大学
关键词：
生态系统;家庭生态系统:和谐家庭;方法论
摘要：
婚姻家庭是一个由众多利益相关成员组成的复杂适应系统,称之为家庭生态系统。家庭生态系统如同自然生态系统一样,也具有整体性、开放性、协同性、层次性、稳定性和演替性等基本特征。随着婚姻家庭自身和外部环境复杂性的加剧,如何利用和遵循生态系统的特性和规律来经营和建设家庭生态系统,成为婚姻家庭战略规划的重要内容。从家庭生态系统的基本特性出发,进行婚姻家庭的战略分析和规划,能够为切实提升家庭生态系统的适应性、促进婚姻的稳定与家庭和谐发展等方面提供方法论上的指导。
语种：
中文
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