Pyroptotic cell-derived microparticle: An atherogenic factor in infectious diseases
作者：
Sun, Shao-wei;Tong, Wen-juan;Zheng, Gui-qiong;Tuo, Qin-hui;Lei, Xiao-yong;...
期刊：
Medical Hypotheses ,2021年146:110370 ISSN：0306-9877
通讯作者：
Liao, DF
作者机构：
[Lei, Xiao-yong; Sun, Shao-wei; Zheng, Gui-qiong] Univ South China, Inst Pharm & Pharmacol, Sch Pharmaceut Sci, Hengyang 421001, Hunan, Peoples R China.;[Tong, Wen-juan] Univ South China, Affiliated Hosp 1, Dept Gynecol & Obstet, Hengyang 421001, Hunan, Peoples R China.;[Liao, DF; Liao, Duan-fang; Tuo, Qin-hui] Hunan Univ Chinese Med, Med Sch, 300 Xueshi Rd, Changsha 410208, Hunan, Peoples R China.
通讯机构：
[Liao, DF ] H;Hunan Univ Chinese Med, Med Sch, 300 Xueshi Rd, Changsha 410208, Hunan, Peoples R China.
关键词：
Article;atherosclerosis;cell activation;cell adhesion;cell infiltration;cell migration;cell proliferation;endothelium cell;endothelium injury;human;infection;membrane microparticle;monocyte;nonhuman;pyroptosis;vascular smooth muscle cell;communicable disease;complication;macrophage;pyroptosis;Atherosclerosis;Cell-Derived Microparticles;Communicable Diseases;Humans;Macrophages;Pyroptosis
摘要：
Chronic infection is considered a risk factor for atherosclerosis. The link between infectious agents and atherosclerosis is manifested by the presence of infection-induced pyroptotic cells in atherosclerotic lesions. Pyroptosis is an inflammatory form of programmed cell death that occurs most frequently upon infection. However, inflammation is not the only cause by which pyroptosis involved in atherosclerosis. During pyroptosis, a large amount of microparticles are released from pyroptotic cells, which not only transfer inflammatory mediators to arterial vessel, but also mediate the interaction between a variety of cells, leading to endothelial injury, macrophage infiltration, vascular smooth muscle cell migration and proliferation, thereby accelerating atherosclerosis. Thus, we proposed hypothesis that pyroptotic cell-derived microparticle is an atherogenic factor in infectious diseases.
语种：
英文
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A novel salvianolic acid A analog with resveratrol structure and its antioxidant activities in vitro and in vivo
作者：
Qiu, Jin-Mei;Qin, Chang-Feng;Wu, Shen-Gen;Ji, Tong-Ying;Tang, Guo-Tao;...
期刊：
Drug Development Research ,2021年82(1):108-114 ISSN：0272-4391
通讯作者：
Cao, Xuan;Xie, Zhi-Zhong
作者机构：
[Xie, Zhi-Zhong; Cao, Xuan; Xie, ZZ; Lei, Xiao-Yong; Tang, Guo-Tao; Qin, Chang-Feng; Ji, Tong-Ying; Qiu, Jin-Mei; Wu, Shen-Gen] Univ South China, Hunan Prov Key Lab Tumour Microenvironm Respons D, 28 Chang Sheng Rd, Hengyang City 421001, Hunan, Peoples R China.;[Xie, Zhi-Zhong] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang, Peoples R China.
通讯机构：
[Cao, X; Xie, ZZ] U;Univ South China, Hunan Prov Key Lab Tumour Microenvironm Respons D, 28 Chang Sheng Rd, Hengyang City 421001, Hunan, Peoples R China.
关键词：
antioxidant;free radical scavenging ability;resveratrol;salvianolic acid A
摘要：
<jats:title>Abstract</jats:title><jats:p>E‐DRS is a novel salvianolic acid A (SAA) analog, which was synthesized from resveratrol (RES) and methyldopate. Its structure is similar to that of SAA, but the 3′,4′‐dihydroxy‐<jats:italic>trans</jats:italic>‐stilbene group and the ester structure in SAA were replaced by the RES structure and an amine group, respectively. E‐DRS scavenged free oxygen radicals effectively, including superoxide anion (ascorbic acid > E‐DRS > SAA ≥ rutin > RES) and DPPH radical (rutin > E‐DRS ≥ ascorbic acid > SAA > RES), and exhibited powerful total antioxidant capacity (ascorbic acid > E‐DRS > SAA ≥ rutin > RES) in vitro. Furthermore, oral administration of E‐DRS dose‐dependently and significantly decreased CCl<jats:sub>4</jats:sub>‐induced oxidative stress in mice as indicated by the decreased content of hepatic malondialdehyde (MDA). In addition, oral administration of E‐DRS also increased the content of nonenzymatic antioxidant glutathione (GSH) and the activity of antioxidant enzymes such as catalase (CAT) and superoxide dismutase (SOD) in the liver of mice. All these results demonstrated that E‐DRS had good antioxidant activities both in vitro and in vivo, and could be a potential antioxidant agent after further optimization and evaluation.</jats:p>
语种：
英文
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Design, synthesis, and biological evaluation of 3 ',4 ',5 '-trimethoxy evodiamine derivatives as potential antitumor agents
作者：
Peng, Yijiao;Xiong, Runde;Li, Zhen;Peng, Junmei;Xie, Zhi-Zhong;...
期刊：
Drug Development Research ,2021年82(7):1021-1032 ISSN：0272-4391
通讯作者：
He, Dongxiu;Tang, Guotao
作者机构：
[Peng, Yijiao; Tang, Guotao; He, Dongxiu; Xiong, Runde] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang City, Peoples R China.;[Li, Zhen; Xie, Zhi-Zhong; Peng, Yijiao; Lei, Xiao-Yong; Tang, Guotao; He, Dongxiu; Peng, Junmei; Xiong, Runde] Hunan Prov Key Lab Tumor Microenvironm Respons Dr, Hengyang City, Hunan, Peoples R China.;[He, Dongxiu; Tang, Guotao] Univ South China, Hunan Prov Key Lab Tumour Microenvironm Respons D, 28 Chang Sheng Rd, Hengyang City 421001, Hunan, Peoples R China.
通讯机构：
[He, DX; Tang, GT] U;Univ South China, Hunan Prov Key Lab Tumour Microenvironm Respons D, 28 Chang Sheng Rd, Hengyang City 421001, Hunan, Peoples R China.
关键词：
evodiamine;microtubule assembly;trimethoxy benzene
摘要：
<jats:title>Abstract</jats:title><jats:p>A series of compounds bearing 3′,4′,5′‐trimethoxy module into the core structure of evodiamine were designed and synthesized. The synthesized compounds were screened in vitro for their antitumor potential. MTT results showed that compounds <jats:bold>14a–14c</jats:bold> and <jats:bold>14i–14j</jats:bold> had significant effects, with compound <jats:bold>14h</jats:bold> being the most prominent, with an IC<jats:sub>50</jats:sub> value of 3.3 ± 1.5μM, which was lower than evodiamine and 5‐Fu. Subsequent experiments further confirmed that compound <jats:bold>14h</jats:bold> could inhibit cell proliferation and migration, and induce G2/M phase arrest to inhibit the proliferation of HGC‐27 cells, which is consistent with the results of the cytotoxicity experiment. Besides, <jats:bold>14h</jats:bold> could inhibit microtubule assembly and might kill tumor cells by inhibiting VEGF and glycolysis. All experimental results indicate that compound <jats:bold>14h</jats:bold> might be a potential drug candidate for the treatment of gastric cancer and was worthy of further study.</jats:p>
语种：
英文
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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.
语种：
英文
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Long non-coding RNA GAS5 in human cancer (Review)
作者：
Yang, Xiaoyan;Xie, Zhizhong;Lei, Xiaoyong* ;Gan, Runliang*
期刊：
ONCOLOGY LETTERS ,2020年20(3):2587-2594 ISSN：1792-1074
通讯作者：
Gan, Runliang;Lei, Xiaoyong
作者机构：
[Gan, Runliang; Yang, Xiaoyan] Univ South China, Hengyang Med Coll, Canc Res Inst, 28 Western Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.;[Yang, Xiaoyan; Xie, Zhizhong; Lei, Xiaoyong] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Hunan, Peoples R China.;[Yang, Xiaoyan; Xie, Zhizhong; Lei, Xiaoyong] Univ South China, Inst Pharm & Pharmacol, 28 Western Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.
通讯机构：
[Gan, Runliang; Lei, Xiaoyong] U;Univ South China, Hengyang Med Coll, Canc Res Inst, 28 Western Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.;Univ South China, Inst Pharm & Pharmacol, 28 Western Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.
关键词：
growth arrest specific transcript 5;long untranslated RNA;protein p53;unclassified drug;angiogenesis;antineoplastic activity;Article;breast carcinoma;cancer prognosis;cancer staging;carcinogenesis;cell invasion;cell proliferation;cell viability;colorectal cancer;DNA damage;down regulation;endometrium cancer;esophageal squamous cell carcinoma;GAS5 gene;gene;gene expression level;gene overexpression;glioblastoma;human;liver cell carcinoma;lung cancer;lymph node metastasis;malignant neoplasm;MAPK signaling;melanoma;neuroblastoma;osteosarcoma;ovary cancer;Pi3K/Akt signaling;prostate carcinoma;quality of life;squamous cell carcinoma;stomach cancer;tumor growth;tumor suppressor gene;tumor volume;uterine cervix cancer
摘要：
Long non-coding RNAs (lncRNAs) constitute a group of >200-nucleotide ncRNA molecules. lncRNAs regulate several cell functions, such as proliferation, apoptosis, invasion and metastasis. Meanwhile, lncRNAs are abnormally expressed in human malignancies, where they suppress or promote tumor growth. The present study focused on growth arrest-specific transcript 5 (GAS5), a well-known lncRNA that acts as a tumor suppressor but is suppressed in multiple types of cancer, including mammary carcinoma, prostate cancer, colorectal cancer, gastric cancer, melanoma, esophageal squamous cell carcinoma, lung cancer, ovarian cancer, cervical cancer, gliomas, osteosarcoma, pancreatic cancer, bladder cancer, kidney cancer, papillary thyroid carcinoma, neuroblastoma, endometrial cancer and liver cancer. Notably, GAS5 is overexpressed in liver cancer, potentially functioning as an oncogene. In the present study, the diagnostic and therapeutic roles of GAS5 in different tumors were reviewed, with a summary of the potential clinical application of the lncRNA, which may help identify novel study directions for GAS5. © 2020 Spandidos Publications. All rights reserved.
语种：
英文
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Nuclear factor erythroid 2 (NF-E2)-related factor 2 (Nrf2) in autophagy-induced hepatocellular carcinoma
作者：
Zhou, Juan;Zhang, Xinxin;Tang, Huifang;Yu, Jia;Zu, Xuyu;...
期刊：
Clinica Chimica Acta ,2020年506:1-8 ISSN：0009-8981
通讯作者：
Lei, Xiaoyong
作者机构：
[Hu, Juan; Yang, Xiaoyan; Xie, Zhizhong; Tan, Fang; Li, Qing; Zhou, Juan; Lei, Xiaoyong; Zhang, Xinxin; Yu, Jia] Univ South China, Key Lab Tumor Microenvironm Response Drug Res, Inst Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Hunan, Peoples R China.;[Tang, Huifang; Zu, Xuyu] Univ South China, Affiliated Hosp 1, Hengyang 421001, Hunan, Peoples R China.
通讯机构：
[Lei, Xiaoyong] U;Univ South China, Key Lab Tumor Microenvironm Response Drug Res, Inst Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Hunan, Peoples R China.
关键词：
Nrf2;autophagy;chemoresistance;hepatocellular carcinoma;oxidant stress
摘要：
Autophagy, an evolutionarily conserved catabolic process, is the most important pathogenic events in the development and progression of liver diseases. Deregulation of Nrf2 is proposed to play a key pathogenic role in hepatocellular carcinoma (HCC). Under certain pathophysiological conditions, such as oxidative stress, impaired autophagy is accompanied by the Nrf2 activation that leads to the detrimental effects favoring the proliferation and survival of HCC. Elucidating its role and potential mechanism is essential for understanding tumorigenesis and the development of effective clinical application. Nrf2 is participated in HCC proliferation, migration and invasion through autophagy pathways. These includes the negatively regulated-Nrf2 by Keap1 that participates in HCC tumorigenesis via regulating ROS production, in which autophagy may contribute to oxidant metabolic reprogramming of HCC cells. Post-transcriptional modifications, such as phosphorylation and ubiquitination of Nrf2, can be positively or negatively induced by multiple transcription factors. Nrf2 exhibits chemoresistance through its binding sites in the promoter region of the target genes. Nrf2 may be a valuable potential biomarker and therapeutic strategy for diagnostics, prognostics and treatment of HCC. © 2020
语种：
英文
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环磷酞胺最大耐受量与节律化疗建立小鼠乳腺癌细胞凋亡的研究
作者：
刘柳成;周爽;皮益苑;简鸣;雷小勇
期刊：
医药界 ,2019年(1):0024-0024 ISSN：2095-4808
作者机构：
湖南省衡阳市南华大学药物药理研究所
关键词：
环磷酞胺;节律化疗;乳腺癌
摘要：
环磷酰胺最大耐受量联合低剂量节律化疗可抑制肿瘤组织生长、抗肿瘤血管生成、促进肿瘤细胞凋亡,不增加毒副作用。本文则以综述的形式了解环磷酞胺最大耐受量与节律化疗建立小鼠乳腺癌细胞凋亡的临床研究。
语种：
中文
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“双轨联动”的药学创新人才培养模式探索与实践
作者：
贺冬秀;雷小勇;喻翠云;李兰芳;魏华;...
期刊：
教育现代化 ,2019年(57):1-3 ISSN：2095-8420
作者机构：
南华大学药学院
关键词：
双轨联动;药学创新人才;培养模式;探索实践
摘要：
为适应医药行业对药学人才的需求和人的发展需求,本校药学院通过确立"双轨联动"的教育理念、构建"四层递进"的创新人才培养路径、设置"三个对应"的学科交叉课程群、搭建"科教融合、校企合作"创新人才培养平台、采用"三个结合"措施打造"双师型"的创新教学团队等方式构建"药物研发+生产实践"双轨联动的药学创新人才培养模式,培养药学创新人才,为我国医药行业的发展提供合格人才。
语种：
中文
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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.
语种：
英文
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药物性肝损害病因及诊治研究进展
作者：
简鸣;阳学风;周爽;皮益苑;雷小勇
期刊：
世界华人消化杂志 ,2019年27(11):715-720 ISSN：1009-3079
通讯作者：
Lei, X.-Y.
作者机构：
南华大学药物药理研究所 湖南省衡阳市421001;南华大学附属南华医院消化内科 湖南省衡阳市421002;[阳学风] 南华大学附属南华医院;[雷小勇; 周爽; 皮益苑; 简鸣] 南华大学
通讯机构：
Institute of Pharmacy and Pharmacology, University of South China, 28 Changsheng West Road, Xiangxiang District, Hengyang, Hunan Province, China
关键词：
药物性肝损害;病因;发病机制;诊断;治疗
摘要：
药物性肝损害(drug induced liver injury, DILI)是临床常见的一种药物不良反应,严重会引起急性肝衰竭甚至危及生命.目前常用且明确可以引起DILI的药物已经超过1000种,已经成为当今一项重点关注的世界医疗安全问题.本文对DILI发病因素、发病机制,诊断和治疗方法进行了综述,为改善DILI的预防和预后提供参考.
语种：
中文
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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.
语种：
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.
语种：
英文
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Cytoplasmic M‑CSF facilitates apoptosis resistance by inhibiting the HIF‑1α/BNIP3/Bax signalling pathway in MCF‑7 cells
作者：
Zhang, Mengxia;Liu, Qi;Li, Lijun;Ning, Jing;Tu, Jian;...
期刊：
ONCOLOGY REPORTS ,2019年41(3):1807-1816 ISSN：1021-335X
通讯作者：
Tang, SS
作者机构：
[Zhang, Mengxia] Hunan Univ Chinese Med, Dept Histol & Embryol, Changsha 410208, Hunan, Peoples R China.;[Tang, SS; Tang, Shengsong] Hunan Univ Med, Hunan Prov Key Lab Antibody Based Drug & Intellig, Huaihua 418000, Hunan, Peoples R China.;[Zhang, Mengxia; Liu, Qi; Mo, Zhongcheng] Univ South China, Clin Anat & Reprod Med Applicat Inst, Dept Histol & Embryol, Hengyang 421001, Hunan, Peoples R China.;[Tang, Shengsong; Lei, Xiaoyong; Tu, Jian; Li, Lijun] Univ South China, Insitute Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.;[Ning, Jing; Tang, Shengsong] Hunan Univ Med, Dept Pharmacol, Huaihua 418000, Hunan, Peoples R China.
通讯机构：
[Tang, SS ] H;Hunan Univ Med, Hunan Prov Key Lab Antibody Based Drug & Intellig, Huaihua 418000, Hunan, Peoples R China.
关键词：
caspase 3;caspase 9;colony stimulating factor 1;doxorubicin;hoe 33342;hypoxia inducible factor 1alpha;protein Bax;protein BNip3;antineoplastic antibiotic;BAX protein, human;BCL2 protein, human;BNIP3 protein, human;colony stimulating factor 1;CSF1 protein, human;doxorubicin;HIF1A protein, human;hypoxia inducible factor 1alpha;membrane protein;oncoprotein;protein Bax;protein bcl 2;antiapoptotic activity;apoptosis;Article;binding affinity;controlled study;down regulation;flow cytometry;human;human cell;immunoprecipitation;MCF-7 cell line;priority journal;protein expression;protein protein interaction;signal transduction;upregulation;Western blotting;apoptosis;breast tumor;drug effect;drug resistance;female;MCF-7 cell line;metabolism;multidrug resistance;pathology;signal transduction;Antibiotics, Antineoplastic;Apoptosis;bcl-2-Associated X Protein;Breast Neoplasms;Doxorubicin;Drug Resistance, Multiple;Drug Resistance, Neoplasm;Female;Humans;Hypoxia-Inducible Factor 1, alpha Subunit;Macrophage Colony-Stimulating Factor;MCF-7 Cells;Membrane Proteins;Proto-Oncogene Proteins;Proto-Oncogene Proteins c-bcl-2;Signal Transduction
摘要：
Macrophage colony-stimulating factor (M-CSF), a tumour marker, is related to tumour cell anti-apoptosis and drug resistance. However, the role of M-CSF in MCF-7 cells is unknown. In the present study, the effect and mechanism of M-CSF on hypoxia-inducible factor-1α (HIF-1α)/BCL2/adeno-virus E1B 19 kDa-interacting protein 3 (BNIP3)/Apoptosis Regulator BAX signalling in human breast cancer MCF-7 cells were investigated. Western blotting revealed that the expression of HIF-1α, BNIP3, Bax, caspase-3 and caspase-9 was lower in MCF-7-M cells compared to MCF-7 and MCF-7-C cells treated with adriamycin (ADM). Immunoprecipitation combined with western blotting was used to detect the interaction between Bcl-2 and BNIP3 or Bax protein. MCF-7-M cells had a higher amount of Bax binding to Bcl-2 compared to MCF-7 cells or MCF-7-C cells, while the amount of BNIP3 binding to Bcl-2 was decreased in MCF-7-M cells. Hoechst 33342 staining and flow cytometry were utilized to evaluate the effect of M‑CSF on apoptosis in MCF-7 cells treated with ADM. Compared to ADM-treated MCF-7 cells, the apoptotic rate of MCF-7-M cells was significantly decreased. These effects were dependent on the concentration of ADM. In conclusion, cytoplasmic M-CSF suppressed apoptosis by inhibiting the HIF-1α/BNIP3/Bax signalling pathway, which potentiated the dissociation of Bcl-2 from Bcl-2-BNIP3 compounds and the formation of Bcl-2-Bax compounds. © 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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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.
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英文
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TWEAK及其受体Fn14信号通路与肺部疾病的研究进展
作者：
管馨馨;张建华;雷小勇
期刊：
中国医师杂志 ,2018年20(4):635-638 ISSN：1008-1372
作者机构：
南华大学药学与生物科学学院, 湖南省衡阳,421001;[管馨馨; 雷小勇; 张建华] 南华大学
关键词：
TNF相关凋亡诱导配体;受体,TNF相关凋亡诱导配体;综述
摘要：
肿瘤坏死因子样凋亡微弱诱导剂(TWEAK)是肿瘤坏死因子超家族的新成员之一。TWEAK通过细胞间的相互作用或旁分泌方式与其受体成纤维细胞生长因子诱导早期反应蛋白14(Fn14)结合,调节细胞的增殖、分化、迁移、凋亡和炎症等多种活动。TWEAK/Fn14信号通路在肺损伤、哮喘以及肺癌等肺部疾病发生发展过程中的作用日益受到关注。
语种：
中文
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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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长链非编码RNAs参与类风湿关节炎免疫调控的机制研究进展
作者：
周爽;皮益苑;简鸣;张鑫鑫;周娟;...
期刊：
中国临床药理学杂志 ,2018年34(22):2654-2656 ISSN：1001-6821
作者机构：
[周爽; 皮益苑; 简鸣; 张鑫鑫; 周娟; 雷小勇] 南华大学药物药理研究所, 湖南省分子靶标新药研究协同创新中心, 湖南, 衡阳, 421001
关键词：
长链非编码RNAs;类风湿关节炎;免疫调控
摘要：
长链非编码RNAs是一类转录本长度超过200 nt、不能编码蛋白的RNAs。lncRNAs表达紊乱或调节失常可通过多途径、多层次广泛参与风湿性疾病的免疫应答、细胞分化及发生发展。因此,lncRNAs有望成为类风湿关节炎治疗的潜在靶点,为逆转类风湿关节炎的治疗提供新思路、新策略。
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.
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英文
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药学研究生药用高分子材料学教学改革初探
作者：
刘阳;贺艳;喻翠云;贺冬秀;雷小勇;...
期刊：
广州化工 ,2018年46(17):128-129 ISSN：1001-9677
作者机构：
南华大学药学与生物科学学院,湖南省分子靶标新药研究协同创新中心,湖南衡阳421001;[贺艳; 郑兴; 雷小勇; 刘阳; 喻翠云; 贺冬秀; 陈临溪] 南华大学
关键词：
药用高分子材料学;教学改革;研究生
摘要：
药用高分子材料学是药学类专业研究生的一门重要的基础课程,在创新性药学高级人才的培养中发挥了重要作用。为了提高课程的教学质量,培养研究生的创新能力,以南华大学药学研究生为例,在对该课程的教学现状进行分析的基础上,从教学内容的选择、教学方法的采用、自主学习的加强等方面,对该课程的教学改革进行了初步探讨。
语种：
中文
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