作者： Ma, Yun;Liu, Yixuan;Jiang, Zhisheng*

期刊： Biomedicine & Pharmacotherapy,2020年128:110251 ISSN：0753-3322

通讯作者： Jiang, Zhisheng

作者机构： [Liu, Yixuan; Jiang, Zhisheng; Ma, Yun] Univ South China, Hunan Int Sci & Technol Cooperat Base Arterioscle, Key Lab Arteriosclerol Hunan Prov, Inst Cardiovasc Dis,Hengyang Med Sch, Hengyang 421001, Peoples R China.;[Liu, Yixuan; Ma, Yun] Univ South China, Inst Biochem & Mol Biol, Hengyang 421001, Peoples R China.;[Ma, Yun] Dept Educ, Key Lab Ecol Environm & Crit Human Dis Prevent Hu, Hengyang 421001, Peoples R China.;[Ma, Yun] Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Peoples R China.;[Jiang, Zhisheng] Univ South China, Hengyang Med Sch, Hengyang 421001, Peoples R China.

通讯机构： [Jiang, Zhisheng] U;Univ South China, Hengyang Med Sch, Hengyang 421001, Peoples R China.

关键词： Circular RNAs;MicroRNA sponge;Nervous system diseases;Biomarker

摘要： Circular RNAs (circRNAs) are a class of newly-identified non-coding RNA that lack 5’ (cap) and 3’ (polyadenylation) ends and are linked by a covalent bond to form a closed loop structure. In comparison to linear RNAs, circRNAs are more resistant to exonuclease RNase R-mediated degradation with a much stronger stability due to the absence of 3’ terminals. Consequently, the extraordinary nature of circRNAs enables it to be potentially used as a biomarker and gene targeting. Similarly, circRNAs can play a significant regulatory role in gene expression where it can indirectly regulate the expression of the downstream target genes of microRNAs (miRNAs) by miRNA sponges. The aim of this review is to highlight the function of circRNAs as well as their vital roles in the central nervous system (CNS) regulation and neurological diseases. © 2020 The Authors

语种： 英文

作者： Liu, Yi;Li, Hongguang;Wang, Shuzhi;Yin, Weidong;Wang, Zongbao*

期刊： Biomedicine & Pharmacotherapy,2020年129:110321 ISSN：0753-3322

通讯作者： Wang, Zongbao

作者机构： [Liu, Yi; Li, Hongguang] Shaoguan Univ, Med Coll, Dept Med Technol, Shaoguan 512026, Guangdong, Peoples R China.;[Wang, Zongbao; Yin, Weidong; Wang, Shuzhi] Univ South China, Sch Pharm, Hengyang 421001, Hunan, Peoples R China.;[Wang, Zongbao; Yin, Weidong; Wang, Shuzhi] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Hunan, Peoples R China.;[Wang, Zongbao] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Sch Pharm, Hengyang 421001, Hunan, Peoples R China.

通讯机构： [Wang, Zongbao] U;Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Sch Pharm, Hengyang 421001, Hunan, Peoples R China.

关键词： Lipoprotein lipase activator;Diabetic nephropathy;Swine, Miniature;Nutrient stress;Oxidative stress;Renal fibrosis

摘要： It is well-recognized that hyperlipidemia and lipid peroxidation contribute to the progression of diabetic nephropathy (DN), which is associated with oxidative stress (OS) and fibrotic lesions. Ibrolipim, a specific lipoprotein lipase activator, has been proved to reduce hyperglycemia and hyperlipidemia, suppress renal lipid deposition, and also protect renal damage. However, the underlying mechanisms of its renoprotective effect are not clearly elaborated. Herein, the present study was to identify whether the putative mechanism of Ibrolipim was related to OS and fibrogenesis in diabetic minipigs fed by high-sucrose and high-fat diet (HSFD) with or without Ibrolipim for 5 months. Compared with the normal control diet, nutrient stress induced by HSFD caused moderate glomerulosclerosis and tubulointerstitial fibrosis, and promoted renal ultrastructural and functional abnormalities. These abnormalities were correlated with renal OS and fibrogenesis characterized by the increased levels of reactive oxygen species (ROS), malondialdehyde, hydroxyproline, collagen type Ⅳ alpha 1 and fibronectin, and decreased contents of reduced glutathione and total antioxidant capacity in kidneys. Ibrolipim significantly ameliorated these abnormalities in HSFD-fed minipigs. In addition, Ibrolipim diminished HSFD-induced nicotinamide-adenine dinucleotide phosphate oxidase-4 activation to reduce ROS production, and enhanced the expression and activity of antioxidant enzymes (i.e. superoxide dismutase 1, catalase and glutathione peroxidase 1) to increase ROS elimination, resulting in obvious suppression of renal OS. Meanwhile, Ibrolipim not only inhibited the upregulation of transforming growth factor-β1 but also partially reversed the downregulation of matrix metalloproteinase 2, and then prevented extracellular matrix (ECM) accumulation. Taken together, Ibrolipim exhibits anti-oxidative and anti-fibrotic effects via modulating the rebalance of renal ROS and ECM metabolism, and ultimately attenuates the progression of nephropathy in diet-induced diabetic minipigs.

语种： 英文

作者： 刘映;李帑洛;郭玉;彭俊梅;贺冬秀

期刊： 教育教学论坛,2020年(29):169-170 ISSN：1674-9324

作者机构： 南华大学 药学与生物科学学院药学系,湖南省分子靶标新药研究协同创新中心,湖南 衡阳 421001;[李帑洛; 彭俊梅; 郭玉; 刘映; 贺冬秀] 南华大学

关键词： “雨课堂”;教学模式改革;化学实验

摘要： 智慧型教学工具的应用不断地渗透到高校的教学改革中。借助通过"雨课堂"平台,对"药物化学实验"课程进行教学改革研究。实践表明,基于"雨课堂"的翻转式教学模式可以进行个性化课堂设计,增强教学互动,完善课程评价,提高学生的主观能动性,能够实现更好的教学效果。

语种： 中文

作者： 李帑洛;符枫雪;郭玉;刘映;王冉;...

期刊： 应用化工,2020年49(4):926-928 ISSN：1671-3206

作者机构： 南华大学 药学与生物科学学院 药学系,湖南 衡阳 421001;湖南省分子靶标新药研究协同创新中心,湖南 衡阳 421001;南华大学 医学院 组织学与胚胎学教研室,湖南 衡阳 421001;南华大学 医学院应用解剖与生殖医学研究所,湖南 衡阳 421001;[王冉; 符枫雪; 李帑洛; 郭玉; 刘映; 何伟国] 南华大学

关键词： 总黄酮;小麦胚芽;超声辅助;提取

摘要： 超声辅助提取小麦胚芽中黄酮类化合物,考察料液比、乙醇体积分数、提取时间、提取温度对小麦胚芽黄酮得率的影响。结果表明,各因素影响的主次顺序为:乙醇体积分数>料液比>提取温度>提取时间;提取最佳工艺为:料液比1∶30 g/mL,乙醇体积分数40%,提取时间60 min,提取温度50℃。在此最佳条件下,小麦胚芽总黄酮的得率为1.52%。

语种： 中文

作者： Liu, Ding;Zhang, Qizhi;Zhang, Lang;Yu, Wenmei;Long, Huizhi;...

期刊： Journal of Chemical Research,2020年44(7-8):494-504 ISSN：1747-5198

通讯作者： Liu, Yunmei

作者机构： [Liu, Yunmei; Yu, Wenmei; Liu, Ding; Zhang, Qizhi; Long, Huizhi] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.;[Liu, Yunmei; Yu, Wenmei; Liu, Ding; Zhang, Qizhi; Long, Huizhi] Hunan Prov Key Lab Tumor Microenvironm Respons Dr, Hengyang, Peoples R China.;[Zhang, Lang; He, Jun] Univ South China, Inst Chem & Chem Engn, Hengyang, Peoples R China.

通讯机构： [Liu, Yunmei] U;Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.

关键词： porphyrins;chrysins;porphyrin-chrysin derivatives;synthesis;antitumor

摘要： Photodynamic therapy is a promising cancer treatment with the advantages of low toxicity, high efficiency, and noninvasiveness. In this study, 23 novel porphyrin–chrysin derivatives are synthesized using alkyl carbon chains as bridges. We use human gastric cancer cells (MGC-803) and human cervical cancer cells to evaluate the in vitro antitumor activity of all the porphyrin–chrysin derivatives, with 5-fluorouracil (5-Fu) as a positive control. Several of the prepared compounds showed effective photodynamic killing effects, among which 5-hydroxy-2-phenyl-7-(2-(4-(10,15,20-tris(4-hydroxyphenyl)porphyrin-5-yl)phenoxy)ethoxy)-4H-chromen-4-one shows the highest antiproliferation activity on human cervical cancer cells, with a half maximal inhibitory concentration of 26.51 ± 1.15 µM. Flow cytometry analysis showed that human cervical cancer cell apoptosis might be induced by G1 phase arrest. © The Author(s) 2020.

语种： 英文

作者： Liu, Yuping;Cong, Yong;Ma, Wei;Kang, Guiying;Meng, Chao;...

期刊： ACS BIOMATERIALS SCIENCE & ENGINEERING,2020年6(5):2812-2821 ISSN：2373-9878

通讯作者： Yu, Cuiyun;Wei, Hua

作者机构： [Liu, Yuping; Wei, Hua; Cong, Yong; Ma, Wei; Meng, Chao; Kang, Guiying; Liu, Fangjun] Lanzhou Univ, Coll Chem & Chem Engn, State Key Lab Appl Organ Chem, Key Lab Nonferrous Met Chem & Resources Utilizat, Lanzhou 730000, Gansu, Peoples R China.;[Wei, Hua; Yu, Cuiyun; Wei, H] Univ South China, Dept Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Peoples R China.

通讯机构： [Yu, CY; Wei, H] U;[Wei, Hua] L;Univ South China, Dept Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Peoples R China.;Lanzhou Univ, Coll Chem & Chem Engn, State Key Lab Appl Organ Chem, Key Lab Nonferrous Met Chem & Resources Utilizat, Lanzhou 730000, Gansu, Peoples R China.

关键词： AB(2) unit;click coupling;RAFT polymerization;hyperbranched polymer template;controlled drug release

摘要： Facile preparation of hyperbranched polymers (HPs) has been advanced tremendously by the use of either various multifunctional agent-mediated controlled living radical polymerizations or a highly reactive ABx unit-modulated self-stepwise polymerizations. However, it remains, to our knowledge, a significant challenge to prepare HPs with simultaneously precisely controlled degree of branching (DB) and biorelevant signal-triggered degradation property for controlled release applications due to the respective limitations of the aforementioned two strategies. For this purpose, a triple functional AB2 unit, A-SS-B2 chain transfer agent (AB2 CTA), that integrates the merits of both multifunctional agents and highly reactive ABx units was designed and synthesized successfully to include a disulfide bond for reduction-triggered polymer degradation toward promoted intracellular release of encapsulated cargoes, a trithiocarbonate group for a universal reversible addition-fragmentation chain transfer (RAFT) polymerization of any vinyl-based monomer, and three terminal groups consisting of one azide and two alkyne functions for the generation of hyperbranched topology via a self-click coupling-based polymerization. A subsequent self-click polymerization of the resulting AB2 CTA by click coupling in the presence of CuSO4·5H2O and sodium ascorbate (NaVc) generated a hyperbranched polymer template (HPT) with precisely modulated DB and a plurality of CTA units for a universal reversible addition-fragmentation chain transfer (RAFT) polymerization of any vinyl-containing monomer. The HPT was next used as a multimacro-CTA for RAFT polymerization of a typical hydrophilic monomer, oligo(ethylene glycol) monomethyl ether methacrylate (OEGMA), to demonstrate the potential of this HPT for a robust and facile production of bioreducible hyperbranched polymers for controlled release applications. The synthesized HPT-4-POEGMA can form unimolecular micelles with enhanced stability due to the hyperbranched structure, and the size of micelles varied in the range from 82.4 to 140.3 nm by a modulation of the molar feed ratio of monomer to HPT and polymerization time. More importantly, HPT-POEGMA micelles incubated with 10 mM glutathione (GSH) showed reduction-triggered cleavage of the disulfide links and polymer degradation for promoted intracellular doxorubicin (DOX) release and enhanced therapeutic efficiency. Taken together, this triple functional AB2 CTA provided a powerful means for the facile preparation of bioreducible hyperbranched polymers with precisely controlled DB for controlled release applications. Copyright © 2020 American Chemical Society.

语种： 英文

作者： Meng, Chao;Cao, Yufei;Sun, Lu;Liu, Yuping;Kang, Guiying;...

期刊： BIOMATERIALS SCIENCE,2020年8(15):4206-4215 ISSN：2047-4830

通讯作者： Wei, Hua

作者机构： [Wei, Hua; Meng, Chao] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Thrget New Dr, Hengyang 421001, Peoples R China.;[Wei, Hua; Meng, Chao] Univ South China, Dept Pharm & Pharmacol, Hengyang 421001, Peoples R China.;[Liu, Yuping; Wei, Hua; Peng, Jinlei; Ma, Wei; Deng, Kaicheng; Ma, Liwei; Sun, Lu; Meng, Chao; Cao, Yufei; Kang, Guiying] Lanzhou Univ, Coll Chem & Chem Engn, State Key Lab Appl Organ Chem, Key Lab Nonferrous Met Chem & Resources Utilizat, Lanzhou 730000, Gansu, Peoples R China.

通讯机构： [Wei, Hua] U;[Wei, Hua] L;Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Thrget New Dr, Hengyang 421001, Peoples R China.;Univ South China, Dept Pharm & Pharmacol, Hengyang 421001, Peoples R China.;Lanzhou Univ, Coll Chem & Chem Engn, State Key Lab Appl Organ Chem, Key Lab Nonferrous Met Chem & Resources Utilizat, Lanzhou 730000, Gansu, Peoples R China.

摘要： Fabrication of cyclic graft (cg) copolymer-based polymeric prodrugs by conjugation of drug molecules to cg copolymers via a dynamic covalent bond capable of responding to biorelevant signals integrates simultaneously the merits of cg copolymers and polymeric prodrugs for enhanced stability of nanocarriers and precise modulation of drug release kinetics. To completely eliminate the compromised drug conjugation efficiency due to the steric hindrance of hydrophilic grafts, it will be useful to develop cg polymeric prodrugs with heterogeneous grafts composed of hydrophilic polymers and drug species, respectively. For this purpose, we reported in this study the synthesis of cyclic graft polymeric prodrugs with heterogeneous grafts of hydrophilic oligo (ethylene glycol) (OEG) and reducibly conjugated camptothecin (CPT), cg-poly(oligo(ethylene glycol) monomethyl ether methacrylate)-b-poly((2-hydroxyethyl methacrylate)-disulfide link-camptothecin) (cg-P(OEGMA)-b-P(HEMA-SS-CPT), cg-prodrugs), via an integrated strategy of a previously reported diblock copolymer-based template and post-polymerization intermolecular click conjugation of a reducible CPT prodrug. The micelles self-assembled from cg-prodrugs on one hand had sufficient salt stability due to the branched cg structure, and on the other hand showed a reduction-triggered cleavage of the disulfide link for a promoted CPT release. Most importantly, we uncovered two interesting phenomena of the cg-based polymeric prodrugs as delivery vehicles: (i) the dimensions of both self-assemblies formed by the cg and bottlegraft (bg) polymers depend substantially on the molecular size of the cg and bg polymers likely due to the steric hindrance of the grafted structures of the cg and bg molecules and relatively low aggregation number of the self-assembled structures, and (ii) cg-prodrug-based micelles exhibited greater in vitro cytotoxicity against cancer cells despite the lower drug loading content (DLC) than the bg-based analogues, which results primarily from the faster reduction-triggered degradation and drug release as well as the greater cellular uptake efficiency of the former micelle prodrugs. Taken together, the developed cg-prodrugs provide great potential for chemotherapy, and the aforementioned interesting results will definitely inspire more upcoming studies on the future design and development of novel cg polymers for biomedical applications. This journal is © The Royal Society of Chemistry.

语种： 英文

作者： Zeng, Ying;Ren, Mei;Li, Yukun;Liu, Yanli;Chen, Cong;...

期刊： Cancer Letters,2020年492:136-146 ISSN：0304-3835

通讯作者： Zeng, Xi;Su, Qi

作者机构： [Li, Yukun; Su, Bo; Su, Qi; Ling, Hui; Su, Jian; Zeng, Ying; Zeng, Xi; Su, Q; Xia, Hong; Liu, Fang] Univ South China, Canc Res Inst, Hunan Prov Key Lab Canc Cellular & Mol Pathol, Hengyang 421001, Hunan, Peoples R China.;[Ren, Mei; Chen, Cong; Su, Qi; Jiang, Hao; Zeng, Xi; Liu, Yanli] Univ South China, Affiliated Hosp 1, Ctr Gastr Canc Res Hunan Prov, Hengyang, Peoples R China.;[Su, Jian] Univ South China, Affiliated Hosp 2, Dept Pathol, Hengyang, Peoples R China.;[Su, Bo] Univ South China, Inst Pharm & Pharmacol, Key Lab Pharmacoprote, Hunan Prov Univ, Hengyang, Peoples R China.;[Zeng, Ying] Univ South China, Sch Nursing, Hengyang, Peoples R China.

通讯机构： [Zeng, X; Su, Q] U;Univ South China, Canc Res Inst, Hunan Prov Key Lab Canc Cellular & Mol Pathol, Hengyang 421001, Hunan, Peoples R China.

关键词： Chemosensitivity;Gastric cancer;Invasion;Proliferation;RhoGDI2

摘要： Gastric cancer (GC) is the fifth most common primary malignancy in humans. Rho GDP dissociation inhibitor 2 (RhoGDI2) is overexpressed in multiple cancer types, but the role of RhoGDI2 in GC has not been elucidated. This study aims to determine the level of RhoGDI2 in GC and to confirm the effect of its inhibition or overexpression on GC cell migration, invasion and chemosensitivity. RhoGDI2 level is significantly enhanced in human GC tissue samples in comparison with normal gastric epithelium and corresponding para-cancerous samples. The expression of RhoGDI2 is correlated with clinicopathological parameters and prognosis. Transfection in combination with miRNA targeting of RhoGDI2 in GC cell lines remarkably downregulates GC cell migration and invasion and reduces the mRNA levels of Rac1, Pak1 and LIMK1. The inhibition of RhoGDI2 downregulates GC cell migration and invasion by attenuating the EMT cascade via the Rac1/Pak1/LIMK1 pathway. Knockdown of RhoGDI2 is a potential therapeutic strategy for GC.

语种： 英文

作者： Zhang, Miao;Liu, Ying;Peng, Jinlei;Liu, Yuping;Liu, Fangjun;...

期刊： Polymer Chemistry,2020年11(38):6139-6148 ISSN：1759-9954

通讯作者： Wei, Hua

作者机构： [Zhang, Miao; Liu, Yuping; Peng, Jinlei; Wei, Hua; Ma, Wei; Ma, Liwei; Liu, Fangjun] Lanzhou Univ, State Key Lab Appl Organ Chem, Key Lab Nonferrous Met Chem & Resources Utilizat, Lanzhou 730000, Gansu, Peoples R China.;[Zhang, Miao; Liu, Yuping; Peng, Jinlei; Wei, Hua; Ma, Wei; Ma, Liwei; Liu, Fangjun] Lanzhou Univ, Coll Chem & Chem Engn, Lanzhou 730000, Gansu, Peoples R China.;[Wei, Hua; Liu, Ying; Yu, Cui-Yun] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Peoples R China.;[Wei, Hua; Liu, Ying; Yu, Cui-Yun] Univ South China, Dept Pharm & Pharmacol, Hengyang 421001, Peoples R China.

通讯机构： [Wei, Hua] L;[Wei, Hua] U;Lanzhou Univ, State Key Lab Appl Organ Chem, Key Lab Nonferrous Met Chem & Resources Utilizat, Lanzhou 730000, Gansu, Peoples R China.;Lanzhou Univ, Coll Chem & Chem Engn, Lanzhou 730000, Gansu, Peoples R China.;Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Peoples R China.

摘要： Cyclic polymers have outperformed their linear analogues for controlled release applications in terms of greater stability and better therapeutic efficiency due to the endless chain topology. However, to our knowledge, there have been thus far only a few examples of the fabrication of pH-sensitive cyclic polymers for drug delivery applications. To further improve the colloidal stability of the previously synthesized cyclic poly(N,N-dimethylaminoethyl methacrylate) (PDMAEMA) for drug delivery applications via a facile yet efficient approach, it will be useful and straightforward to incorporate a hydrophilic monomer for copolymerization with DMAEMA. For this purpose, we reported in this study the preparation of pH-sensitive cyclic statistical copolymers, P(OEGMA-st-DMAEMA)s, with two different compositions by atom transfer radical polymerization (ATRP) of oligo(ethylene glycol) monomethyl ether methacrylate (OEGMA) and DMAEMA and subsequent "intra-chain" click cyclization of the a-alkyne-.-azide linear precursor. A further comparison study on the micelle stability revealed that the spherical micelles self-assembled from c-P(OEGMA(4)-st-DMAEMA(38)) (C) with both smaller hydrodynamic size than that of the micelles of the linear analogue, l-P(OEGMA(4)-st-DMAEMA(38)) (L), and greater salt stability than that of the micelles of c-P (OEGMA(8)-st-DMAEMA(38)) were screened to be the optimal micelle construct for drug delivery applications. Flow cytometry (FCM) analysis confirmed greater cellular uptake efficiency of doxorubicin (DOX)loaded C (C@DOX) micelles than that of the L (L@DOX) ones. More importantly, the C@DOX micelles showed comparable in vitro cytotoxicity against the cancer cell line (HeLa cells) but lower in vitro cytotoxicity against the normal cell line (HUVEC cells) relative to the L@DOX formulation after 72 h of incubation. Therefore, this study not only developed a facile approach to improve the colloidal stability of a cyclic polycation, but also presented a pH-sensitive cyclic copolymer-based nanoplatform with great potential for anticancer drug delivery.

语种： 英文

作者： Zou, Ju;Wu, Daichao*;Li, Tao;Wang, Xianwen;Liu, Yan;...

期刊： PATHOLOGY RESEARCH AND PRACTICE,2019年215(2):229-234 ISSN：0344-0338

通讯作者： Wu, Daichao;Tan, Sijie

作者机构： [Liu, Yan; Zou, Ju] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hunan Prov Key Lab Special Pathogens Prevent & Co, Dept Parasitol,Hengyang Med Coll, Hengyang 421001, Hunan, Peoples R China.;[Tan, Sijie; Wu, Daichao] Univ South China, Hengyang Med Coll, Dept Histol & Embryol, Inst Clin Anat & Reprod Med, Hengyang 421001, Hunan, Peoples R China.;[Li, Tao; Wang, Xianwen] Univ South China, Hengyang Med Coll, Grade 2015 Clin Med, Hengyang 421001, Hunan, Peoples R China.;[Wu, Daichao; Tan, SJ] Univ South China, Hengyang Med Coll, Inst Clin Anat & Reprod Med, 28 W Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.

通讯机构： [Wu, DC; Tan, SJ] U;Univ South China, Hengyang Med Coll, Inst Clin Anat & Reprod Med, 28 W Changsheng Rd, Hengyang 421001, Hunan, Peoples R China.

关键词： biological marker;programmed death 1 ligand 1;CD274 protein, human;programmed death 1 ligand 1;bladder cancer;cancer risk;cancer susceptibility;colorectal cancer;disease marker;esophageal squamous cell carcinoma;genetic association;genetic linkage;genetic polymorphism;genetic variability;human;liver cell carcinoma;meta analysis;non small cell lung cancer;ovary cancer;Review;single nucleotide polymorphism;stomach cancer;systematic review;genetic predisposition;genetics;genotype;neoplasm;odds ratio;B7-H1 Antigen;Genetic Predisposition to Disease;Genotype;Humans;Neoplasms;Odds Ratio;Polymorphism, Single Nucleotide

摘要： Programmed death ligand 1(PD-L1) mediated immune escape play important roles in the development of cancer. The gene polymorphism of PD-L1, in particular rs4143815 C > G, has been associated with the cancer risks, but with conflicting results. Therefore, this meta-analysis was aimed to assess the association between rs4143815 C > G and cancer susceptibility. A systematic literature search was performed to select the studies and the pooled odds ratio (OR) with 95% confidence interval (CI) was used to evaluate the strength of association. Eleven eligible studies containing 3711 cases and 3704 controls were enrolled in the meta-analysis. The results suggested that there is a strong association between rs4143815 C > G and the cancer risks (G vs. C: OR = 1.386, 95% CI: 1.132–1.696, p = 0.002; GG vs. CG + CC: OR = 1.843 95% CI: 1.300–2.613, p = 0.002; GG + CG vs. CC: OR = 1.280, 95% CI: 1.040–1.576, p = 0.020). Subgroup analysis based on cancer type suggested that PD-L1 rs4143815 C > G might increase the susceptibility to gastric cancer (G vs. C: OR = 1.842, 95% CI: 1.403–2.418, p < 0.001) and bladder cancer (G vs. C: OR = 2.015, 95% CI: 1.556–2.608, p < 0.001), and genotype GG carriers of PD-L1 rs4143815 C > G might have higher risks of HCC (GG vs. CG + CC: OR = 2.226 95% CI: 1.562–3.172, p < 0.001). PD-L1 rs4143815 C > G might confer an increased cancer risk, indicating this SNP may contribute to the pathogenesis of cancer and might be used as a potential biomarker to predict the susceptibility to cancer. © 2018 Elsevier GmbH

语种： 英文

作者： 李曼玉;杨梅芳;刘美香;姚旭;彭俊梅;...

期刊： 化学世界,2019年60(11):784-788 ISSN：0367-6358

作者机构： 南华大学药学与生物科学学院药学系 药学与生物科学学院药学实验中心 湖南省分子靶标新药研究协同创新中心,湖南衡阳,421001;[杨梅芳; 刘美香; 彭俊梅; 姚旭; 李曼玉; 刘映] 南华大学

关键词： 类黄酮类化合物;乙酰胆碱酯酶抑制剂

摘要： 建立类黄酮类乙酰胆碱酯酶抑制剂的三维定量构效关系(3D-QSAR)模型。采用Topomer CoMFA法研究类黄酮类乙酰胆碱酯酶抑制剂的构效关系。建立了可靠、合理的类黄酮类乙酰胆碱酯酶抑制剂Topomer CoMFA模型(q~2=0.812,r~2=0.921,r_(pred)~2=0.531)。建立的Topomer CoMFA模型揭示了类黄酮类化合物分子与其体外乙酰胆碱酯酶抑制活性间的关系,可以有助于合理设计具有更好活性的乙酰胆碱酯酶抑制剂。

语种： 中文

作者： Chen, Hainan;Liu, Yijian;Gui, Qingjun;Zhu, Xiao;Zeng, Lin;...

期刊： Peptides,2019年111(1):118-126 ISSN：0196-9781

通讯作者： He, Jin;Yin, Kai

作者机构： [Gao, Ling; Chen, Hainan; Yin, Kai; Feng, Juling; Jackson, Ampadu O.; Li, Yi; Gui, Qingjun; Qing, Jina; Zhu, Xiao] Univ South China, Med Sch, Res Lab Clin & Translat Med, Hengyang 421001, Peoples R China.;[Chen, Hainan; Yin, Kai; Zhu, Xiao] Univ South China, Inst Cardiovasc Res, Key Lab Atherosclerol Hunan Prov, Hengyang 421001, Peoples R China.;[Liu, Yijian] Third Hosp Changsha, Changsha 410000, Hunan, Peoples R China.;[Zeng, Lin] Univ South China, Affiliated Hosp 1, Dept Neurol, Hengyang 421001, Peoples R China.;[Meng, Jun; He, Jin] Univ South China, Affiliated Hosp 1, Funct Dept, Hengyang 421001, Hunan, Peoples R China.

通讯机构： [He, Jin; Yin, Kai] U;Univ South China, Affiliated Hosp 1, Funct Dept, Hengyang 421001, Hunan, Peoples R China.;Univ South China, Res Lab Clin & Translat Med, Hengyang 421001, Peoples R China.

关键词： collagen;ghrelin;ghrelin receptor;hydroxymethylglutaryl coenzyme A reductase kinase;Smad2 protein;Smad3 protein;Smad7 protein;sodium chloride;transforming growth factor beta1;ghrelin;ghrelin receptor;acute heart infarction;animal experiment;Article;attenuation;body weight;CAEC cell line;controlled study;coronary artery ligation;drug blood level;drug mechanism;epithelial mesenchymal transition;heart muscle fibrosis;heart weight;human;human cell;human cell culture;in vitro study;in vivo study;left anterior descending coronary artery;male;nonhuman;priority journal;protein expression;protein phosphorylation;rat;serum;signal transduction;animal;blood;cardiomyopathy;cell culture;echocardiography;enzyme linked immunosorbent assay;epithelial mesenchymal transition;fibrosis;fluorescent antibody technique;heart infarction;metabolism;real time polymerase chain reaction;Sprague Dawley rat;Western blotting;Animals;Blotting, Western;Cardiomyopathies;Cells, Cultured;Echocardiography;Enzyme-Linked Immunosorbent Assay;Epithelial-Mesenchymal Transition;Fibrosis;Fluorescent Antibody Technique;Ghrelin;Humans;Male;Myocardial Infarction;Rats;Rats, Sprague-Dawley;Real-Time Polymerase Chain Reaction;Receptors, Ghrelin

摘要： Ghrelin, a peptide hormone produced in the gastrointestinal tract, has recently been found to be associated with the onset of myocardial fibrosis (MF). The exact mechanism, however, remains elusive. This study sought to identify the function and mechanism of ghrelin on MF after acute myocardial infarction (AMI). AMI was established in Spraque-Dawley rats by ligation of the left anterior descending (LAD). Ghrelin or saline was intraperitoneally injected two times per day for 8 weeks after ligation. The weight of heart (mg) and the weight ratio of heart to body (mg/g) as well as the fibrotic area were increased, while serum level of ghrelin was decreased after AMI. Ghrelin significantly ameliorated MF and decreased deposition of collagens in perivascular fibrosis area. In addition, ghrelin inhibited Endothelial-to-mesenchymal transition (EndMT), a crucial process for MF, in perivascular fibrosis area and TGF-β1-induced human coronary artery endothelial cells (HCAECs). Mechanistically, ghrelin persistently decreased the phosphorylation of Smad2/3 and enhanced the expression of Smad7 and p-AMPK in vivo and in vitro. After the abolition of Smad7, GHSR-1a and AMPK pathway, the effect of ghrelin on EndMT was significantly inhibited. In conclusion, these results presented a novel finding that ghrelin attenuated MF after AMI via regulation EndMT in a GHSR-1a/AMPK/Smad7- dependent manner. © 2018 Elsevier Inc.

语种： 英文

作者： Li, Yang;Xiao, Jie;Zhang, Qizhi;Yu, Wenmei;Liu, Mengqin;...

期刊： Bioorganic & Medicinal Chemistry,2019年27(3):568-577 ISSN：0968-0896

通讯作者： Liu, Yunmei;He, Jun

作者机构： [Xiao, Jie; Liu, Yunmei; Yu, Wenmei; Guo, Yu; Zhang, Qizhi; Li, Yang] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.;[He, Jun] Univ South China, Inst Chem & Chem Engn, Hengyang 421001, Peoples R China.;[Liu, Mengqin] Hengyang Normal Univ, Inst Chem & Mat Sci, Hengyang 421001, Peoples R China.

通讯机构： [Liu, Yunmei; He, Jun] U;Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.;Univ South China, Inst Chem & Chem Engn, Hengyang 421001, Peoples R China.

关键词： Anti-tumor;Drug target;Inhibitors of protein kinases;Quinazoline derivatives;Structure-activity relationship

摘要： Quinazoline was originally utilized as an anti-tumor treatment, and its various derivatives can be directly extracted from plants. In recent years, protein kinases (PK) have been well recognized in the development of tumor drugs. Functionally, PK serves a vital role in the apoptosis, proliferation, differentiation, migration and cell cycle of tumor cells. Due to its good physicochemical properties, quinazoline skeleton, a superior type of PK inhibitor, has been extensively used in anti-tumor drug design. An increasing number of studies on quinazoline synthesis have been reported and used by different groups to effectively develop novel derivatives. Thus, several studies have been approved for the use of quinazoline derivatives as inhibitors of other kinases, including Src and histone deacetylase. The aim of the present review was to summarize the mechanism of quinazoline compounds as PK inhibitors, their biological structure-activity relationship such as the substituted quinazoline compounds with different functional groups in the apoptotic process, and their effect on the proliferation of tumor cells. The development of novel agents based on the antitumor functions of quinazoline molecular compounds may improve the clinical outcomes of the affected population, particularly in patients with cancer.

语种： 英文

作者： Kang, Guiying;Sun, Lu;Liu, Yuping;Meng, Chao;Ma, Wei;...

期刊： LANGMUIR,2019年35(38):12509-12517 ISSN：0743-7463

通讯作者： Wei, Hua;Yu, Cuiyun

作者机构： [Liu, Yuping; Wei, Hua; Ma, Wei; Ma, Liwei; Sun, Lu; Wang, Baoyan; Meng, Chao; Kang, Guiying] Lanzhou Univ, Key Lab Nonferrous Met Chem & Resources Utilizat, State Key Lab Appl Organ Chem, Lanzhou 730000, Gansu, Peoples R China.;[Liu, Yuping; Wei, Hua; Ma, Wei; Ma, Liwei; Sun, Lu; Wang, Baoyan; Meng, Chao; Kang, Guiying] Lanzhou Univ, Coll Chem & Chem Engn, Lanzhou 730000, Gansu, Peoples R China.;[Wei, Hua; Yu, Cuiyun; Wei, H] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Peoples R China.;[Wei, Hua; Yu, Cuiyun; Wei, H] Univ South China, Dept Pharm & Pharmacol, Hengyang 421001, Peoples R China.

通讯机构： [Wei, Hua] L;[Yu, CY; Wei, H] U;Lanzhou Univ, Key Lab Nonferrous Met Chem & Resources Utilizat, State Key Lab Appl Organ Chem, Lanzhou 730000, Gansu, Peoples R China.;Lanzhou Univ, Coll Chem & Chem Engn, Lanzhou 730000, Gansu, Peoples R China.;Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang 421001, Peoples R China.

关键词： Copper compounds;Cyclization;Ethylene;Hydrophobicity;Loading;Micelles;Motion Picture Experts Group standards;Polyethylene oxides;Ring opening polymerization;Targeted drug delivery;Topology;Amphiphilic diblock copolymers;Azide-alkyne cycloaddition;Controlled drug release;Drug delivery applications;Drug loading capacity;Hydrophobic moieties;Self-assembly behaviors;Topological effects;Controlled drug delivery;doxorubicin;drug carrier;macrogol;polycaprolactone;polyester;chemistry;delayed release formulation;HeLa cell line;human;kinetics;micelle;Delayed-Action Preparations;Doxorubicin;Drug Carriers;HeLa Cells;Humans;Kinetics;Micelles;Polyesters;Polyethylene Glycols

摘要： Polymer topology exerts a significant effect on its properties and performance for potential applications. Cyclic topology and its derived structures have been recently shown to outperform conventional linear analogues for drug delivery applications. However, an amphiphilic tadpole-shaped copolymer consisting of a cylic hydrophobic moiety has rarely been explored. For this purpose, a tadpole-shaped amphiphilic diblock copolymer of poly(ethylene oxide)-b-(cyclic poly(ϵ-caprolactone)) (mPEG-b-cPCL) was synthesized successfully via ring-opening polymerization (ROP) of ϵ-CL using a mPEG-based macroinitiator with both a hydroxyl and an azide termini and subsequent intrachain Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAc) click cyclization. A comparison study on the self-assembly behaviors, in vitro drug loading and drug release profiles, and degradation properties of the resulting mPEG-b-cPCL (C) with those of the linear counterpart (mPEG-b-PCL, L) revealed that mPEG-b-cPCL micelles are a better formulation than the micelles formed by the linear counterparts in terms of micelle stability, drug loading capacity, and the degradation property. Interestingly, compared to the single degradation of L, C exhibited a slower two-stage degradation process including the topological change from tadpole shape to linear conformation and the subsequent degradation of a linear polymer. This study therefore uncovered the topological effect of a hydrophobic moiety on the properties of the self-assembled micelles and developed a complementary alternative to enhance the micelle stability by introducing a cyclic hydrophobic segment. © 2019 American Chemical Society.

语种： 英文

作者： 李冲;文翔昊;刘映;李帑洛;李海艳;...

期刊： 现代肿瘤医学,2019年27(7):1135-1140 ISSN：1672-4992

作者机构： [李冲; 文翔昊] 南华大学附属南华医院;南华大学药物药理研究所;[李海艳; 李帑洛; 郭玉; 刘映] 南华大学

关键词： 乳腺癌细胞条件培养基;骨转移;增殖;Notch信号

摘要： 目的:探讨MDA-MB-231、MCF-7乳腺癌细胞条件培养基对hFOB1.19成骨细胞的增殖抑制作用与Notch信号通路的相关性。方法:MTT法检测MDA-MB-231、MCF-7乳腺癌细胞条件培养基对hFOB1.19细胞的增殖抑制效果;Western Blot与qRT-PCR分别检测hFOB1.19细胞的Notch1、Jagged1、Hes1蛋白与mRNA的表达。结果:MDA-MB-231、MCF-7条件培养基抑制hFOB1.19细胞增殖,DAPT（Notch阻断剂）可明显降低MDA-MB-231、MCF-7条件培养基对hFOB1.19细胞增殖的抑制作用。MDA-MB-231、MCF-7条件培养基上调hFOB1.19细胞Notch1、Jagged1、Hes1的mRNA和蛋白的表达,并随着条件培养基浓度的增加,以上指标的表达呈先上升而后下降的趋势。Notch阻断剂DAPT明显抑制两细胞条件培养基对hFOB1.19细胞的Notch1、Jagged1、Hes1 mRNA和蛋白表达的上调作用。结论:MDA-MB-231、MCF-7条件培养基对hFOB1.19细胞增殖抑制作用的机制与Notch信号通路相关。

语种： 中文

作者： 刘映;谢秀珍;李曼玉;杨梅芳;刘美香;...

期刊： 广州化工,2018年46(13):20-23 ISSN：1001-9677

作者机构： 南华大学药学与生物科学学院 药学实验中心,湖南 衡阳 421001;南华大学药学与生物科学学院药学系,湖南 衡阳 421001;湖南省分子靶标新药研究协同创新中心,湖南 衡阳 421001;南华大学药学与生物科学学院药学系,湖南 衡阳,421001;[杨梅芳; 谢秀珍; 周珂; 刘美香; 彭俊梅; 姚旭; 李曼玉; 刘映] 南华大学

关键词： 阿魏酸酰胺类化合物;乙酰胆碱酯酶抑制剂;三维定量构效关系

摘要： 采用比较分子场分析（Co MFA）和比较分子相似性分析法（Co MSIA）建立阿魏酸酰胺类乙酰胆碱酯酶抑制剂的三维定量构效关系（3D-QSAR）模型,研究阿魏酸酰胺类乙酰胆碱酯酶抑制剂的构效关系。结果表明,建立的Co MFA-1（Q2=0.576,r2=0.992）和Co MSIA（Q2=0.468,r2=0.987）模型可靠、合理,揭示了阿魏酸酰胺类化合物与其体外乙酰胆碱酯酶抑制活性间的关系,可为合理设计新的具有更好活性的乙酰胆碱酯酶抑制剂提供科学依据。

语种： 中文

作者： 刘映;彭俊梅;姚旭;丁岚;李帑洛;...

期刊： 广州化工,2018年46(12):148-149+167 ISSN：1001-9677

作者机构： 南华大学药学与生物科学学院药学系,湖南省分子靶标新药研究协同创新中心,湖南 衡阳 421001;[丁岚; 李帑洛; 彭俊梅; 姚旭; 涂剑; 刘映; 贺冬秀; 唐国涛] 南华大学

关键词： 协同创新;研究型;实验课程体系

摘要： 高校实验室作为培养创新思维与创新能力的重要场所, 在创新型人才的培养过程中至关重要.南华大学药学实验中心依托湖南省"分子靶标新药研究协同创新中心"平台的优势资源, 巧妙地将科学研究与实验课程相结合, 在课程体系、评价方式、师资队伍建设、资源共享等方面进行了一系列改革与探索, 推进了研究型实验课程体系的构建与完善.

语种： 中文

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

作者： Long, Xiaokang;Zeng, Yao-Fu;Liu, Yunmei;Liu, Ying;Li, Tangluo;...

期刊： RSC Advances,2018年8(54):31201-31212 ISSN：2046-2069

通讯作者： Guo, Yu

作者机构： [Liu, Yunmei; Liu, Ying; Li, Tangluo; Guo, Yu; Long, Xiaokang; Liao, Lanqing; Zeng, Yao-Fu] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.

通讯机构： [Guo, Yu] U;Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.

摘要： Genistein amino acid derivatives 4a–4d were synthesized and evaluated for their cytotoxic activities against MCF-7, Hela, MGC-803 and HCT-116 cell lines by MTT assays in vitro. The results revealed that compounds 4a–4d showed better activity than the parent compound genistein. Particularly, compound 4b displayed the most significant anticancer activity against MGC-803 with an IC50 value of 12.08 μM. In addition, the mechanisms of interaction between genistein, compounds 4a–4d and BSA were investigated via multi-spectroscopic techniques such as ultraviolet (UV) spectroscopy, fluorescence, circular dichroism (CD), and molecular docking under physiological conditions. The results suggested that endogenous fluorescence of BSA could be quenched by genistein and compounds 4a–4d via forming BSA-compound complex, which meant a static quenching mechanism was involved. The negative values of enthalpy (ΔH) and entropy (ΔS) indicated that interactions between BSA and the ligands were spontaneous, and hydrogen bonding and van der Waals interactions were involved in the BSA-compound complexion formation. The UV, synchronous and 3D fluorescence results revealed that the micro-environment of tryptophan and conformation of BSA were changed after binding to ligands. CD analysis demonstrated the variation in the secondary structure and that the α-helix content of BSA decreased. Eventually, molecular docking was executed to forecast the binding forces and binding sites between BSA and compounds 4a–4d.

语种： 英文

作者： Wang, Zhe;Deng, Xiangping;Xiong, Shujuan;Xiong, Runde;Liu, Juan;...

期刊： Natural Product Research,2018年32(24):2900-2909 ISSN：1478-6419

通讯作者： Zheng, Xing;Tang, Guotao

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： antineoplastic agent;benzimidazole derivative;chrysin;compound 10;compound 11;compound 12;compound 13;compound 14;compound 15;compound 16;compound 17;compound 18;compound 19;compound 21;compound 22;compound 23;compound 3;compound 4;compound 5;compound 6;compound 7;compound 8;compound 9;fluorouracil;unclassified drug;antineoplastic agent;benzimidazole derivative;chrysin;flavonoid;animal experiment;animal model;antineoplastic activity;antiproliferative activity;apoptosis;Article;breast cancer;cancer inhibition;cell cycle arrest;cell cycle G0 phase;cell cycle G1 phase;controlled study;dose response;drug design;drug megadose;drug potency;drug screening;drug synthesis;Hep-G2 cell line;IC50;in vitro study;in vivo study;male;MCF-7 cell line;mouse;nonhuman;animal;cell cycle;cell proliferation;chemistry;drug effect;drug screening;human;synthesis;tumor cell line;xenograft;Animals;Antineoplastic Agents;Apoptosis;Benzimidazoles;Cell Cycle;Cell Line, Tumor;Cell Proliferation;Drug Design;Drug Screening Assays, Antitumor;Flavonoids;Heterografts;Humans;Mice

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 IC 50 values of 25.72±3.95μM. 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. © 2017, © 2017 Informa UK Limited, trading as Taylor & Francis Group.

语种： 英文