APPLIED ORGANOMETALLIC CHEMISTRY
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2015
·Vol. 29
·期 7
·481-486
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IF 2.248
Chuanzhu Gao,Yan Zhang,Tianshuai Wang,Ji Chen,Yunxu Qian,Bo Yang,Shaohua Gou,Peng Dong,Yingjie Zhang
Seven dinuclear platinum(II) complexes with a novel chiral tetradentate ligand, (1 R ,1′ R ,2 R ,2′ R )- N 1 , N 1′ -(1,4-phenylenebis(methylene))dicyclohexane-1,2-diamine, were designed, synthesized and spectrally characterized. All the complexes were evaluated for their in vitro cytotoxicity against human HepG-2, A549, HCT-116 and MCF-7 cancer cell lines. The results indicated that all compounds showed positive biological activity against HepG-2, A549 and HCT-116 cancer cell lines. In particular, compounds D7 and D2 showed better activity than carboplatin against HepG-2 and A549 and compound D7 also showed an activity close to that of oxaliplatin. Copyright © 2015 John Wiley & Sons, Ltd.
研究领域:
药物化学
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肿瘤学
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金属配合物化学
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DOI
高影响因子
PHARMACEUTICAL CHEMISTRY JOURNAL
·
2024
·Vol. 57
·期 8
·1174-1178
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IF 0.8
Zheng Qing-Xuan,Wang Rui,Li Hui-Jing,Dehaen Wim,Huai Qi-Yong
Oleanolic acid (OA) is a natural product with certain antitumor activity. In order to enhance its cytotoxicity, a total of five derivatives of OA were designed and synthesized. Their cytotoxicity against MDA-MB-231cells (human breast cancer cells), A549 cells (human nonsmall cell lung cancer cells) and BEAS-2B cells (human cervical cancer cells) were evaluated by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method. The results indicated that these target compounds have a wide molar activity range and some of them showed better activity than the commercial drug, doxorubicin. Compound 2a induces apoptosis of 14, 27, and 56% of MDA-MB-231 cells at 2, 4, and 8 mM respectively, and shows a linear correlation of concentration.
研究领域:
肿瘤学
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药物化学
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分子药理学
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天然产物化学
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转化医学
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DOI
高影响因子
LUMINESCENCE
·
2015
·Vol. 31
·期 3
·813-820
·
IF 1.518
Hongjing Cui,Ran Wang,Ying Zhou,Chang Shu,Fengjuan Song,Wenying Zhong
To date, several fluorescent probes modified by a single targeting agent have been explored. However, studies on the preparation of dual-function quantum dot (QD) fluorescent probes with dual-targeting action and a therapeutic effect are rare. Here, a dual-targeting CdTe/CdS QD fluorescent probe with a bovine serum albumin–glycyrrhetinic acid conjugate and arginine-glycine-aspartic acid was successfully prepared that could induce the apoptosis of liver cancer cells and showed enhanced targeting in in vitro cell imaging. Therefore, the as-prepared fluorescent probe in this work is an efficient diagnostic tool for the simultaneous detection of liver cancer and breast cancer cells. Copyright © 2015 John Wiley & Sons, Ltd.
研究领域:
生物医学工程
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癌症研究
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分子影像学
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产品关联
DOI
PubMed
高影响因子
TOXICOLOGY
·
2021
·
IF 4.221
Tongkuo Yuan,Jiaojiao Sun,Jingjing Tian,Jia Hu,Huancai Yin,Jian Yin
This paper aimed to systemically investigate the role of adenosine triphosphate-binding cassette (ABC transporters) in the detoxification of non-substrate nanoparticles including titanium dioxide (n-TiO 2 , 5−10 nm) and gold (AuNPs, 3 nm, 15 nm, and 80 nm, named as Au-3, Au-15 and Au-80) in human lung cancer (A549) and human cervical cancer (HeLa) cells. All these nanoparticles were of larger hydrophilic diameters than the channel sizes of ABC transporters, thus should not be the substrates of membrane proteins. After 24-h treatment, they induced significant cytotoxicity as reflected by the reduction in cell viability and glutathione (GSH) contents, as well as the increase in reactive oxygen species (ROS) level. At median-lethal concentrations (10 mg/L n-TiO 2 , 2 mg/L Au-3, 5 mg/L Au-15, and 10 mg/L Au-80 for A549 cells; 20 mg/L n-TiO 2 , 2 mg/L Au-3, 5 mg/L Au-15, and 10 mg/L Au-80 for Hela cells), all the nanoparticles significantly induced the gene expressions and activities of ABC transporters including P-glycoprotein (PGP) and multidrug resistance associated protein 1 (MRP1). Addition of transporter inhibitors enhanced the ROS levels produced by nanoparticles, but didn’t alter their death-inducing effects and intracellular accumulations. With specific suppressors, transcription factors like nuclear factor-erythroid 2-related factor-2 (NRF2) and pregnane X receptor (PXR) were proved to be important in the induction of ABC transporters by nanoparticles. After all, this paper revealed a damage-dependent modulation of ABC transporters by non-substrate nanoparticles. The up-regulated ABC transporters could help in reducing the oxidative stress produced by nanoparticles. Such information should be useful in assessing the environmental risk of nanoparticles, as well as their interactions with other chemical toxicants or drugs.
研究领域:
毒理学
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分子生物学
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药理学
✓ 已验证
DOI
PubMed
高影响因子
Colloid and Interface Science Communications
·
2021
·
IF 4.914
Yimei Yin,Lian Guan,Yaxin Wang,Yue Ma,Jianming Pan,Yinxian Peng,Guoqing Pan
Herein, a drug nanocarrier capable of recognizing sialic acid (SA) was prepared by grafting SA-imprinted hydrogel layer on mesoporous silica nanoparticles (MSNs). On cancer cells, the terminal of glycoproteins and lipids on cell membrane usually overexpression of SA, thus SA-imprinted mesoporous nanocarriers (SIMNs) may show cancer selectivity and targeted drug delivery. In this study, a typical therapeutic drug doxorubicin (DOX) was filled into the mesoporous channels of SIMNs to obtain a DOX-loaded nanomaterial ( [email protected] ). Human hepatocellular carcinoma cells (HepG-2) were selected to demonstrated the tumor targeted drug delivery of [email protected] We verified that the combination of mesoporous nanocarriers with SA recognition sites gives our [email protected] the ability to target SA-overexpressed cancer cells and enhance cancer cellular uptake, finally leading to improved inhibition of cancer cell proliferation . Our study would offer a good idea for the engineering of drug nanocarriers with targeted cancer theranostics.
研究领域:
纳米技术
·
药剂学
·
肿瘤学
✓ 已验证
DOI
高影响因子
JOURNAL OF CHEMICAL RESEARCH
·
2020
·
IF 0.593
Ding Liu,Qizhi Zhang,Lang Zhang,Wenmei Yu,Huizhi Long,Jun He,Yunmei Liu
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.
研究领域:
肿瘤学
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药理学
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化学合成
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产品关联
DOI
高影响因子
Chinese Herbal Medicines
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2018
·
IF 0
Ding Liu,Yan-peng Li,Hong-xiu Shen,Yang Li,Jun He,Qi-zhi Zhang,Yun-mei Liu
Objective To design and synthesize a series of chrysin derivatives and evaluate the antitumor activities with MTT assay , so as to investigate molecular structure-activity relationship with molecular docking . Methods Target products were synthesized with high yield by substitution reaction, hydrolysis reaction, esterification reaction, and saponification reaction in sequence, and activities of all compounds were evaluated with human gastric carcinoma cell lines MGC-803 and human breast carcinoma cell lines MCF-7 through standard MTT assay. Molecular docking results were calculated with Surflex Geom X programme of Sybyl X-2.0 version workstation. Results 7- O -amino acids chrysin derivatives 6a – 6l were synthesized and their inhibitory effects were evaluated by comparing the material chrysin with positive control drug 5-fluorouracil (5-FU). Among these derivatives, compound 5b (IC 50 = 24.50 ± 2.26 µmol/L), 5k (IC 50 = 24.30 ± 2.19 µmol/L), and 6f (IC 50 = 24.61 ± 2.01 µmol/L) showed better inhibitory activities against MGC-803 cell lines, and compound 5g (IC 50 = 13.15 ± 1.73 µmol/L) and 5j (IC 50 = 12.34 ± 1.25 µmol/L) showed better inhibitory activities against MCF-7 cell lines than chrysin and 5-FU. Molecular docking scores showed a credible consistency compared with MTT results. Conclusion Compounds 5b, 5d, 5g, 5j, 5k , and 6f showed good antiproliferative effects on specific tumor cells, and compound 5g should be researched further when according to molecular docking.
研究领域:
药理学
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肿瘤学
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药物化学
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产品关联
DOI
JOURNAL OF HETEROCYCLIC CHEMISTRY
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2014
·Vol. 52
·期 2
·473-477
·
IF 0.873
Hongxia Liu,Libo Li,Shaikh Qurat-ul-ain,Tao Jiang
A series of novel 2,6-disubstituted purine derivatives were designed and synthesized from 2,6-dichloropurine. The structures of target compounds were determined by 1 H-NMR, 13 C-NMR, and HRMS. The synthesized compounds were evaluated for their inhibitory activities against lung cancer cell lines of A549 and liver cancer cell lines of Bel-7402. 2-(4-Benzyloxy-phenylamino)-6-(cyclohexylamino)purine( 3 ), 2-(4-chloro-phenylamino)-6-( n -butylamino)purine ( 5 ), 2-(4-morpholinoamino)-6-(4-hydroxy-phenylamino)purine ( 9 ), and 2-(4- O -galactosyl-phenylamino)-6-(cyclohexylamino)purine ( 12 ) exhibited moderate inhibitory activity.
研究领域:
药物化学
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肿瘤学
·
有机合成
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DOI
高影响因子
MICROCHIMICA ACTA
·
2018
·Vol. 185
·期 3
·1-7
·
IF 5.705
Xu Yujuan,Zhang Peng,Wang Zhen,Lv Shaoping,Ding Caifeng
Gold nanoclusters (AuNCs) protected with a bovine serum albumin (BSA) coating are known to emit red fluorescence (peaking at 650 nm) on photoexcitation with ultraviolet light (365 nm). On addition of Cu(II) ions, fluorescence is quenched because Cu(II) complexes certain amino acid units in the BSA chain. Fluorescence is, however, restored if pyrophosphate (PPi) is added because it will chelate Cu(II) and remove it from the BSA coating on the AuNCs. Because PPi is involved in the function of telomerase, the BSA@AuNCs loaded with Cu(II) can act as a fluorescent probe for determination of the activity of telomerase. A fluorescent assay was worked out for telomerase that is highly sensitive and has a wide linear range (10 nU to 10 fM per mL). The fluorescent probe was applied to the determination of telomerase activity in cervix carcinoma cells via imaging. It is shown that tumor cells can be well distinguished from normal cells by monitoring the differences in intracellular telomerase activity.
Gold nanoclusters (AuNCs) protected by bovine serum albumin (BSA) and displaying red photoluminescence were prepared as fluorescent probe for the determination of telomerase activity and used for imaging of cervix carcinoma (HeLa) cells.
研究领域:
生物化学
·
分子生物学
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癌症研究
·
纳米技术
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Journal of Hepatocellular Carcinoma
·
2025
·
IF 3.4
Jiayuan Zhang,Tian Tian,Shanshan Tian,Jinhai Yao,Yingwan Zhang,Rujia Xie,Ting Yang,Bing Han
Purpose This study aims to investigate the mechanism of action of arsenic-based agents against hepatocellular carcinoma (HCC) and to identify effective drug targets for HCC treatment.Methods Huh7 and HepG2 cells treated with NaAsO2 were assessed for cell viability, pyroptosis, migration, and invasion after undergoing lentiviral transfection. An orthotopic liver tumor model was established and divided into a model group and a treatment group. Proteins associated with QRICH1, PRMT1, cGAS-STING, and the classical pyroptosis pathway were quantified using Western blotting. The intracellular expression and localization of PRMT1 and NLRP3 in HCC were analyzed through cellular immunofluorescence. Co-immunoprecipitation (Co-IP) was performed to examine the protein interactions between PRMT1 and cGAS, as well as between STING and NLRP3. Chromatin immunoprecipitation (ChIP) was used to confirm QRICH1 enrichment in the PRMT1 promoter region.Results NaAsO2 treatment significantly inhibited the proliferation of Huh7 and HepG2 cells and effectively blocked their migration and invasion capabilities, while promoting cellular pyroptosis. Quantitative polymerase chain reaction(QRCR) and ChIP assays confirmed that NaAsO2 regulates PRMT1 expression by down-regulate QRICH1 binding in the PRMT1 promoter region. Additionally, NaAsO2 decreased the expression of the QRICH1-PRMT1 complex and upregulated the cGAS-STING signaling pathway, activating the downstream NLRP3-dependent classical pyroptosis pathway. Overexpression of QRICH1 reversed these effects.Conclusion NaAsO2 inhibits the expression of the QRICH1-PRMT1 axis, activates cGAS-STING signaling pathway transduction, and induces pyroptosis in HCC cells, thereby increasing the infiltration of immune cells in liver cancer tissues.
研究领域:
分子生物学
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肿瘤学
·
药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
FOOD CHEMISTRY
·
2018
·
IF 4.946
Yongsheng Chen,Jiangwei Liu,Sheng Geng,Yonglan Liu,Hanjun Ma,Jie Zheng,Benguo Liu,Guizhao Liang
Herein, we perform the regioselective acetylation of phloridzin catalyzed by immobilized Candida antarctica lipase B (CALB). We show that the enzyme amount and reaction time can significantly influence the composition of mono-, di- and tri-acetylated phloridzin in the product. The last acetylated derivative of phloridzin is isolated and identified as 4, 3″, 6″-3-O-acetyl-phloridzin by HPLC, UV, IR, MS and NMR. Molecular docking suggests that the first acetylation of phloridzin catalyzed by CALB occurs in 6″-OH, followed by 3″-OH, then 4-OH. During this process, hydrogen bond and hydrophobic forces play an important role in maintaining the binding interaction of CALB with phloridzin or its acetylated derivatives. Although, tri-acetylated phloridzin has moderate to minimal adverse-effects on LO-2, its anti-proliferative activity against human HepG2 cancer cells is superior to that of phloridzin, which attributes to its high capacity of inducing cell apoptosis, retarding cell cycle, lowering mitochondrial membrane potential and scavenging intracellular ROS.
研究领域:
生物化学
·
药物化学
·
肿瘤学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Applied Materials & Interfaces
·
2014
·
IF 5.9
Arsalan Ahmed,Sen Liu,Yutong Pan,Shanmei Yuan,Jian He,Yong Hu
Three kinds of amphiphilic copolymer, that is, poly(ε-caprolactone)-SS-poly(ethylene glycol) (PCL-SS-PEG), poly(ε-caprolactone)-polyethylenimine (PCL-PEI), and poly(ε-caprolactone)-polyethylenimine-folate (PCL-PEI-Fol) were synthesized and self-assembled into surface engineered hybrid nanoparticles (NPs). Morphological studies elucidated the stable, spherical, and uniform sandwich structure of the NPs. PCL-PEI and PCL-SS-PEG segments have introduced pH and reduction responsive characteristics in these NPs, while PCL-PEI-FA copolymers could provide specific targeting capability to cancer cells. The stimuli responsive capabilities of these NPs were carried out. Negative-to-positive charge reversible property, in response to the pH change, was investigated by zeta potential and nuclear magnetic resonance (NMR) measurements. The structure cleavage, due to redox gradient, was studied by dynamic light scattering (DLS) and transmission electron microscopy (TEM). These NPs showed controlled degradation, better drug release, less toxicity, and effective uptake in MCF-7 breast cancer cells. These multifunctional NPs showed promising potential in the treatment of cancer.
研究领域:
药学
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纳米技术
·
癌症研究
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）