CANCER SCIENCE
·
2012
·Vol. 103
·期 8
·1434-1439
·
IF 3.325
Bing Xiu Ren,Fan Yang,Gao Hong Zhu,Zi Xing Huang,Hua Ai,Rui Xia,Xi Jiao Liu,Man Lu,Bin Song
To develop a molecular probe for MRI detection of human tumor telomerase reverse transcriptase (hTERT) mRNA expression. Uniformly phosphorothioate-modified hTERT antisense oligonucleotide (ASON) homing hTERT mRNA was labeled with gadolinium (Gd) through the bifunctional chelator 1,4,7, 10-tetraazacyclododecane-N, N', N'', N'''-tetraacetic acid (DOTA) stirred within 45 minutes at 60°C. The Gd labeled probes were characterized in vitro . The cellular uptake rate and biodistribution of 99m Tc-DOTA-ASON was measured instead of that of Gd-DOTA-ASON. A549 lung adenocarcinoma model was established in BALB/c nude mice and Gd-DOTA-ASON was injected intraperitoneally and MR images were acquired using 7.0T Micro-MRI (Bruker Biospec, Ettlingen, Germany) at different time points. Immunohistochemical analysis of telomerase activity of each xenograft was operated two days after in vivo imaging. The binding efficiency of Gd-DOTA-ASON reached as high as 71.7 ± 4.5% ( n = 6). Gd-DOTA-ASON displayed perfect stability in fresh human serum at 37°C for 24 h. Compared with normal lung cells, A549 cells showed an obviously higher uptake of 99m Tc-DOTA-ASON than that of lung cells (10.5 ± 2.7% vs. 4.8 ± 2.6%, P < 0.05). The signal intensity of A549 xenografts can be enhanced by Gd-DOTA-ASON and the signal to noise ratio (SNR) of tumor to muscle reached 2.37 and maintained a relatively high level within 6 h after injection. The activity of hTERT in A549 tumors can be suppressed by Gd-DOTA-ASON in pathological slices. The results of this study show that Gd-DOTA-ASON can be a promising intracellular MR contrast probe for targeting telomerase-positive carcinomas. ( Cancer Sci, doi: 10.1111/j.1349-7006.2012.02316.x, 2012)
研究领域:
医学影像学
·
分子生物学
·
肿瘤学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF NON-CRYSTALLINE SOLIDS
·
2018
·
IF 2.488
Xia Guo,Wenfeng Li,Heping Wang,Yan-Ying Fan,Huifang Wang,Xianghua Gao,Baolong Niu,Xuechen Gong
In the study, amorphous calcium phosphate (ACP) nanoparticles were prepared by the coprecipitation method to optimize release profile of curcumin (Cur) and avoid burst releases, which were used to overcome the weakness of Cur, such as poor chemical stability and bioavailability. To find the best preparation condition, the influence of reaction concentration, temperature, time and pH on crystal phase of the samples was investigated by XRD and FTIR. The results showed that amorphous calcium phosphate (ACP) was obtained, when pH value and the concentration of PO 4 3− were 8 and 0.024 mM, prepared at 30 °C for 10 min. In vitro drug release assay, ACP nanoparticles showed high loading capacity of Cur and favorable pH-responsive drug release properties. Furthermore, the Cur-load ACP nanoparticles showed an excellent ability to scavenge free radical and damage A549 cells, resulting in a high antioxidant properties and low cell viability. Therefore, the as-prepared nanoparticles have promising applications in the food and biomedical fields.
研究领域:
材料科学
·
药理学
·
生物医学工程
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2023
·
IF 8.2
Xuelian Wang,Wenhui Liu,Yeling Li,Lingling Ma,Zhen Lin,Jing Xu,Yuanqiang Guo
The combination of selenium and polysaccharides is one of the significant ways to ameliorate the anti-cancer effects of polysaccharides. PLP50-1, a homogeneous polysaccharide purified from the aqueous extract of Paeonia lactiflora , had a molecular weight of 1.52 × 10 4 Da and consisted of α -D-Glc p -(1→, →4)- α -D-Glc p -(1→, →6)- α -D-Glc p -(1→, →4,6)- α -D-Glc p -(1→, and →6)- β -D-Fru f -(2→. PLP50-1 showed weak anti-tumor effects against A549 cells. To ameliorate the activity of PLP50-1, the complex nanoparticles combining P. lactiflora polysaccharide with selenium were constructed successfully. Structural properties of the polysaccharide-based selenium nanoparticles (PLP-SeNPs) were clarified using various means. The results displayed that a kind of monodisperse spherical nanoparticles containing high selenium content (39.1 %) with controllable size was constructed and showed satisfactory stability. The cellular anti-tumor assay indicated that PLP-SeNPs had stronger antiproliferative activity against A549 cells than PLP50-1. Additionally, the zebrafish experiments displayed that PLP-SeNPs inhibited the proliferation and migration of A549 cells significantly and blocked the angiogenesis.
研究领域:
药理学
·
纳米技术
·
癌症研究
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Open Life Sciences
·
2016
·Vol. 11
·期 1
·542-551
·
IF 0
Huanan Wang,Ming Yao,Wenqing Xu
Cancer is the second leading cause of death worldwide. Traditional antitumor drugs exhibit severe cytotoxic and side effects. Lung cancer needs new and more effective treatment approaches. Coumarin derivatives can act on various tumor cells and show anti-proliferative activity through various mechanisms, including mitochondrial signaling cascades that regulate development and apoptosis of cells. Mitochondria-targeted coumarin derivatives have not been reported yet. Taking advantage of the fact that cancer cells frequently have higher mitochondria membrane potential, we synthesized a mitochondria-targeted 6-(nicotinamide) methyl coumarin by coupling 6-methyl coumarin to nicotinamide. Our results demonstrate that 6-(nicotinamide) methyl coumarin preferentially kills A549 cells through inducing A549 cells apoptosis, mediated by increasing ROS level and causing mitochondrial depolarization. Strikingly, the viability of the A31 cells treated with 6-(nicotinamide) methyl coumarin did not decrease, indicating that 6-(nicotinamide) methyl coumarin preferentially accumulates in A549 cells and A549 cells are much more susceptible to 6-(nicotinamide) methyl coumarin treatment compared with A31 cells.
研究领域:
肿瘤学
·
药理学
·
细胞生物学
✓ 已验证
产品关联
DOI
Nanoscale
·
2014
·Vol. 6
·期 24
·14772-14783
·
IF 6.739
Danling Yang,Rongfeng Zou,Yu Zhu,Ben Liu,Defan Yao,Juanjuan Jiang,Junchen Wu,He Tian
Polydiacetylene (PDA) micelles have been widely used to deliver anticancer drugs in the treatment of a variety of tumours and for imaging living cells. In this study, we developed an effective strategy to directly conjugate magainin II (MGN-II) to the surface of PDA micelles using a fluorescent dye. These stable and well-defined PDA micelles had high cytotoxicity in cancer cell lines, and were able to reduce the tumour size in mice. The modified PDA micelles improved the anticancer effects of MGN-II in the A549 cell line only at a concentration of 16.0 μg mL−1 (IC50). In addition, following irradiation with UV light at 254 nm, the PDA micelles gave rise to an energy transfer from the fluorescent dye to the backbone of PDA micelles to enhance the imaging of living cells. Our results demonstrate that modified PDA micelles can not only be used in the treatment of tumors in vitro and in vivo in a simple and directed way, but also offer a new platform for designing functional liposomes to act as anticancer agents.
研究领域:
癌症研究
·
生物医学工程
·
药物递送系统
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
SYNTHETIC COMMUNICATIONS
·
2023
·
IF 2.1
Jun Yang,Guang-Ping Liang,Xiong-Li Liu
To investigate the effects and mechanisms of 4-(1H-indol-1-yl)-4-oxobutanoic acid spliced podophyllotoxin derivatives (3a–3l) on tumor cells. The MTT method was adopted to evaluate (3a–3l) antitumor activity in vitro against A549 cells, A549/DDP cells, MCF-7 cells. The results showed that compound 3l had the most prominent inhibitory effect and high selectivity with IC50 18.53 ± 1.51 µM against A549/DDP cells. Meanwhile, the effects of compound 3l on the nuclear state, cell cycle and apoptosis of A549/DDP cells showed that compound 3l induced apoptosis by delaying the G2/M phase of A549/DDP cell cycle. In addition, molecular docking of compound 3l also showed that it could form a good hydrogen bond with ARG-158 (d = 2.6, 2.7 Å) and HIS-406 (d = 2.5 Å) at the colchicine site of tubulin. Compound 3l could provide lead compound for the development of new multi-drug resistant anti-tumor drugs.
研究领域:
药理学
·
肿瘤学
·
化学
·
分子生物学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF THE INDIAN CHEMICAL SOCIETY
·
2025
·
IF 3.4
Xinxin Zhou,Yicheng Mei,Baowei Yang,Jing Wang,Huiling Tang,Xiaolong Zhang,Changchun Liu
Eight 4-(morpholinyl arylamino)quinazoline-6-carbamoyl carboxylic acid methyl esters and four 4-(morpholinyl arylamino)quinazoline-6-carbamoyl hydroxamic acid derivatives were designed and synthesized by integrating morpholine moieties into the 4-aminoquinazoline scaffold, with additional modifications at the 6-position of quinazoline ring. The antitumor potential of these twelve derivatives was evaluated against human lung cancer A549 cells and breast cancer MDA-MB-231 cells using the Cell Counting Kit-8 (CCK-8) proliferation assays. The bioassay results indicated that most of the derivatives exhibited moderate to potent in vitro antiproliferative activity against both cancer cells. Particularly, compound 7bb demonstrated superior potency against MDA-MB-231 cells and A549 cells, with half maximal inhibitory concentration (IC 50 ) values of 4.286 and 4.720 μM, respectively, compared to the reference drug afatinib (IC 50 = 7.640 and 5.173 μM, respectively). This study provides valuable insights for the development of novel antitumor agents based on the 4-aminoquinazoline scaffold.
研究领域:
药物化学
·
肿瘤学
✓ 已验证
DOI
高影响因子
CyTA-Journal of Food
·
2016
·
IF 0.769
Xu Si,Zhongkai Zhou,Dandan Bu,Jing Li,Padraig Strappe,Chris Blanchard
Polysaccharides were extracted from corn bran (CBPs) and then modified by a sulfating reaction to obtain sulfated corn bran polysaccharides (SCBPs). Synthesized sulfated polysaccharides were located in the equatorial bonds of monosaccharide residues. A more orderly and smooth surface of SCBPs was observed. Single factor experiment results showed 2.0 g of aminosulfonic acid, 60 mL of N-dimethylformamide and 2.5 h of reaction time were the optimum conditions for SCBPs preparation. Phenolic content of SCBPs significantly decreased with increasing concentration of aminosulfonic acid, while it increased with increasing DMF concentration and reaction time. SCBPs had higher DPPH, ABTS and iron chelating capacity under the optimum conditions. SCBPs significantly inhibited the proliferation of A549 and HepG2 cell lines, which was associated with the up-regulation at the mRNA expression level of pro-apoptotic genes CASP3, CASP8, CASP9 and reduced expression of p53, gene Bcl-2 and gene iNOS.
研究领域:
生物化学
·
药理学
·
细胞生物学
·
分子生物学
✓ 已验证
DOI
高影响因子
Food Bioscience
·
2021
·
IF 4.24
Yonglu Li,Yiru Zhang,Yaxuan Wang,Xin Yu,Ting Yu,Xiaodong Zheng,Qiang Chu
With high morbidity and mortality, non-small cell lung cancer (NSCLC) has become a challenge for humans, because its clinic chemotherapies still remain unsatisfactory. In this study, the leaf part of a traditional Chinese plant, Tetrastigma hemsleyanum (TL), was studied, and its main flavones compounds were extracted and purified (TLF), which were composed of 5-caffeoylquinic acid, 3-caffeoylquinic acid, 4-caffeoylquinic acid, quercetin-3-O-rutinoside and kaempferol-3-O-rutinoside. To study the anti-NSCLC ability of TLF, in vitro and in vivo studies were done. TLF inhibited the proliferation and migration of A549 cells and caused mitochondrial dysfunction. TLF significantly suppressed the tumor weight and volume, and down-regulated Ki67, proliferation cell nuclear antigen (PCNA) and vascular endothelial growth factor (VEGF) productions. To determine the intrinsic mechanism, proteins alternations were measured in solid tumors, and results showed that TLF blocked the Akt/mTOR pathway, and thereby induced autophagy, triggering Bcl and Caspase-dependent pathways, resulting in A549 cells’ apoptosis. This study indicated that TLF is a potential candidate to be an anti-NSCLC drug, or a supplementary resource for chemotherapy.
研究领域:
肿瘤学
·
药理学
·
分子生物学
·
中医药学
✓ 已验证
产品关联
DOI
高影响因子
Nanomaterials
·
2016
·Vol. 6
·期 6
·113
·
IF 2.69
Jin Xie,Xiaobo Pan,Mengyan Wang,Longfang Yao,Xinyue Liang,Jiong Ma,Yiyan Fei,Pei-Nan Wang,Lan Mi
Titanium dioxide (TiO2) has attracted wide attention as a potential photosensitizer (PS) in photodynamic therapy (PDT). However, bare TiO2can only be excited by ultraviolet illumination, and it lacks specific targeting ligands, which largely impede its application. In our study, we produced nitrogen-doped TiO2and linked it with an effective cancer cell targeting agent, folic acid (FA), to obtain N-TiO2-FA nanoconjugates. Characterization of N-TiO2-FA included Zeta potential, absorption spectra and thermogravimetric analysis. The results showed that N-TiO2-FA was successfully produced and it possessed better dispersibility in aqueous solution than unmodified TiO2. The N-TiO2-FA was incubated with human nasopharyngeal carcinoma (KB) and human pulmonary adenocarcinoma (A549) cells. The KB cells that overexpress folate receptors (FR) on cell membranes were used as FR-positive cancer cells, while A549 cells were used as FR-negative cells. Laser scanning confocal microscopy results showed that KB cells had a higher uptake efficiency of N-TiO2-FA, which was about twice that of A549 cells. Finally, N-TiO2-FA is of no cytotoxicity, and has a better photokilling effect on KB cells under visible light irradiation. In conclusion, N-TiO2-FA can be as high-value as a PS in cancer targeting PDT.Keywords:titanium dioxide nanoparticle;photodynamic therapy;cancer cell targeting;folic acid
研究领域:
纳米技术
·
癌症研究
·
材料科学
·
治疗学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ANALYST
·
2021
·Vol. 146
·期 17
·5403-5412
·
IF 4.616
Shiying Zhou,Xianfeng Wang,Liuyi Jiang,Human Sun,Danqun Huo,Changjun Hou
Two different electrochemical sensors (Hemin-G4/Au/GCE and Hemin-G4/Au/ITO) were developed and applied to explore the electrocatalytic capacity of H2O2 reduction. Due to the excellent catalytic activity of Hemin-G4 and high conductivity of gold nanoparticles, both electrodes show excellent electrochemical performances towards H2O2 with a low LOD (0.67 μM for Hemin-G4/Au/GCE and 0.65 μM for Hemin-G4/Au/ITO), rapid response (<4 s), and high selectivity and sensitivity (314.33 μA mM−1 cm−2 for Hemin-G4/Au/GCE and 322.22 μA mM−1 cm−2 for Hemin-G4/Au/ITO). The two electrodes allow sensitive capture of H2O2 produced by A549 cells. Compared with the conventional method of detection in cell suspensions, an ITO electrode with a large specific surface area and good biocompatibility can provide a promising platform for cell adhesion, so as to realize real-time and in situ detection of extracellular H2O2. The experimental results show that A549 cells can adhere to the surface of the Hemin-G4/Au/ITO electrode and grow well. This is benefitted from the three-dimensional structure of the Hemin-G4/Au hydrogel, which provides a suitable microenvironment for cell adhesion and growth. Furthermore, the in situ detection shows a faster response time than that of in-solution detection. This is because the H2O2 generated by the cells can be directly captured by the ITO electrode, which avoids diffusion from the solution to the electrode. These results indicate that the self-supporting hydrogel modified ITO electrode has great application prospects in basic biomedical research and continuous dynamic surveillance of diseases.
研究领域:
电化学
·
生物传感器
·
生物医学工程
·
细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Journal of Functional Foods
·
2024
·
IF 3.8
Yuan Liang,Qing Wang,Dianwen Zhang,Yiyao Gong,Qiuyan Jiang,Cong Ma,Libo Si,Tiehua Zhang,Jie Zhang,Zheng Ma
In this work, ginsenoside CK was confirmed as an EGFR tyrosine kinase inhibitor, with an IC 50 value of 32.58 ± 0.09 μM. Molecular docking showed that ginsenoside CK could fit into EGFR binding pocket, thereby acting as a ligand for EGFR. Ginsenoside CK inhibited proliferation of A549 cells as well as induced its apoptosis via downregulating anti-apoptotic factors and upregulating apoptosis induction factors. Ginsenoside CK alone and combined with gefitinib inhibited the tumor progression of A549 lung cancer xenografts in BALB/c nude mice. ELISA assay showed that ginsenoside CK combined with gefitinib alleviated the inflammatory response by suppressing the release of pro-inflammatory cytokines, indicating better inhibitory effects than ginsenoside CK or gefitinib alone. This work further confirmed that ginsenoside CK regulated the EGFR/MAPK/ERK signaling both in vitro and in vivo . In conclusion, ginsenoside CK can exhibit the anti-lung cancer effect via acting as an EGFR tyrosine kinase inhibitor.
研究领域:
肿瘤学
·
药理学
·
分子生物学
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）