Biomed Research International
·
2021
·
IF 3.411
Fengqin Wang,Hanzhong Zhang,Zhigang Cheng
EPHA2 is a member of the ephrin receptor tyrosine kinase family and is closely related to the malignant tumor progression. The effect of EPHA2 on OSCC is not clear. This study explored the role of EPHA2 and AKT/mTOR signaling pathways in Cal-27 cell invasion and migration. The expression of EPHA2 and EPHA4 in human OSCC and normal oral tissue was detected by immunohistochemistry. EPHA2-overexpressing and EPHA2-knockdown Cal-27 cells were established, and the cells were treated with an AKT inhibitor (MK2206) and mTOR inhibitor (RAD001). The expression of EPHA2 was detected by qRT-PCR, cell proliferation was evaluated by MTT assay, cell migration and invasion were examined by scratch and Transwell assay, and cell morphology and apoptosis were assessed by Hoechst 33258 staining. Western blot was performed to detect the expression of proteins related to AKT/mTOR signaling, cell cycle, and pseudopod invasion. EPHA2 and EPHA4 were highly expressed in clinical human OSCC. Overexpression of EPHA2 promoted the proliferation, migration, and invasion of Cal-27 cells, inhibited cell cycle blockage and apoptosis, and enhanced the activity of the AKT/mTOR signaling pathway. MK2206 (AKT inhibitor) and RAD001 (mTOR inhibitor) reversed the effect of EPHA2 overexpression on the biological behavior of Cal-27 cells. EPHA2 promotes the invasion and migration of Cal-27 human OSCC cells by enhancing the AKT/mTOR signaling pathway.
研究领域:
肿瘤学
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分子生物学
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细胞生物学
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产品关联
DOI
PubMed
高影响因子
MEDICINAL CHEMISTRY RESEARCH
·
2023
·
IF 2.6
Long Xing,Yang Peilin,Chen Lin,Zhong Wen,Chen Shaofeng,Li Yanping,Lin Shijie,Tian Wei
Oral cancer severely affects the quality of life of patients, and the primary treatment is surgery, due to a lack of specific drugs. Aloe emodin, a natural product of anthraquinone, is considered a potential antitumor drug. However, it has poor water solubility and low biological activity. In this study, we designed and synthesized a novel aloe emodin–hydroxyethyl piperazine hybrid dihydrochloride ( AE-NPC ), which improved the water solubility and antitumor activity of aloe emodin in vitro. According to the results, the IC 50 value of AE-NPC on CAL-27 cancer cells was 14.4 ± 2.9 μM. The flow cytometry results showed that AE-NPC induced the production of reactive oxygen species (ROS) and apoptosis in CAL-27 cells. The spectroscopy and molecular docking results showed that AE-NPC can be well intercalated into DNA grooves. Further molecular mechanism studies revealed that AE-NPC not only regulates the expression levels of key proteins (Bax/Bcl-2, cytochrome C, cleaved caspase-9 and cleaved caspase-3) of the mitochondrial apoptotic pathway but also activates the expression levels of a key protein ( γ -H 2 AX) of the DNA damage pathway. Therefore, AE-NPC induces CAL-27 cell apoptosis via DNA damage and mitochondrial pathways. This study provides new insights into the further development of anthraquinone compounds as potential chemotherapeutic agents for oral cancer treatment.
The novel aloe emodin derivative AE-NPC induces oral cancer CAL-27 cells apoptosis through ROS production, DNA damage and mitochondrial pathways. The anthraquinone compound AE-NPC may be a potential agent for the treatment of oral cancer.
研究领域:
肿瘤学
·
药理学
·
化疗
·
细胞生物学
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分子生物学
✓ 已验证
DOI
高影响因子
FUEL PROCESSING TECHNOLOGY
·
2022
·
IF 8.129
Wang Li,Wen-Ying Li,Xing-Bao Wang,Jie Feng
During direct coal liquefaction , selective C al –O bond cleavage is critical for phenol production. In this study, anisole and benzyl phenyl ether were chosen as the oxygen-containing model compounds. Radical-induced sites of benzyl phenyl ether were investigated using the Fukui function and energy barrier calculation. The promotion routes of the C al –O bond cleavage in anisole and benzyl phenyl ether by radicals were illustrated. The formation of o -benzyl phenol was regarded as a sign of benzyl radical-induced pyrolysis based on the most optimal path. The competitive process between the optimal path and β-bond scission path was analyzed from the rate constant perspective. Radical-induced pyrolysis made remarkable differences in product selectivity for benzyl phenyl ether. Similarly, the cleavage of the C al –C al bond can also be promoted using two methods of radical induction, which is referred to as a radical chain process. In contrast to benzyl phenyl ethers, the induced pyrolysis of the C al –C al bond in bibenzyl is more likely to occur via β-bond scission after the H of CH 2 is abstracted by a radical. The findings of this research would provide a theoretical foundation for comprehending the radical mechanism of direct coal liquefaction.
研究领域:
化学工程
·
能源科学
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产品关联
DOI
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2025
·
IF 5.6
Chen-yan Li,Shuo-hua Xie,Min Deng,Gan-rong Huang,Yan-Qiang Huang,Shu-fang Li
Objectives Oral squamous cell carcinoma (OSCC) is a major malignancy affecting the oral, jaw, and facial regions. In this study, we synthesized a cinnamaldehyde-thiosemicarbazone-zinc (II) complex (CTZn) to inhibit OSCC cell proliferation. Methods We investigated the inhibitory effects of CTZn on OSCC using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, cell colony formation assays, wound-healing/scratch assays and transwell invasion assays. Flow cytometry (FCM) was performed to explore the CTZn's impact on apoptosis and cell-cycle progression. Through in vivo experiments, its antitumor activity activity was evaluated in OSCC xenograft mouse models and orthotopic tumor model mice. The mechanisms of CTZn were explored by detecting targeted metabolites, and performing drug affinity responsive target stability (DARTS) experiments, molecular docking analyses and Western blot assays. Levels of reactive oxygen species (ROS), oxidized and reduced nicotinamide adenine dinucleotide phosphate (NADP⁺/NADPH), glutathione (GSH), and 6-phosphogluconate dehydrogenase (PGD) protein in CAL-27 cells were also determined. Results These findings demonstrated that CTZn inhibited CAL-27 cell growth in vitro in a time- and concentration-dependent manner, with an IC 50 value of 1.642 to 2.223μmol/L, and CTZn also exerted anti-tumor activity in vivo . CTZn also inhibited PGD messenger RNA (mRNA), and protein expression, reduced NADP+/NADPH and GSH levels, and significantly increased ROS levels, thereby inducing oxidative stress. Conclusion CTZn impairs mitochondrial function, decreases ATP, levels, and induces G₂-phase arrest and apoptosis in CAL-27 cells. Therefore, it is an ideal drug for treating OSCC.
研究领域:
肿瘤学
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药理学
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生物无机化学
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分子生物学
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癌症研究
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产品关联
DOI
PubMed
高影响因子
BIOCHEMICAL ENGINEERING JOURNAL
·
2020
·
IF 3.475
Yu Zhang,Xiaohui Di,Wen Wang,Miaojia Song,Qiang Yu,Zhongming Wang,Zhenhong Yuan,Xiaoyan Chen,Huijuan Xu,Ying Guo
Methyl-2-furoate (MF) is a high-value compound, and can be produced via esterification of furoic acid derived from biobased furfural. Herein, CAL-B and [bmim][PF 6 ] were the most efficient lipase and organic medium for MF production, respectively. Based on mass action law and reaction reversibility, a mathematical model was developed. Data analysis showed the newly proposed binary regression was apparently more suitable compared to the commonly used unitary regression. The enzymatic promotion factor m i for esterification and hydrolysis was 1.8159 and 0, while the alcohol inhibition factor n i was 0 and 0.06436, respectively. Both the activation energy E a, i for esterification and hydrolysis was 84 kJ/mol, and the pre-exponential factor A i was 7.1408×10 13 and 7.8962×10 13 , respectively. Kinetics study demonstrated that CAL-B held significantly more dominant esterification activity compared to hydrolysis activity, whereas alcohol just inhibited hydrolysis activity instead of esterification activity, and the relationship between esterification/hydrolysis rate constants k i and temperature agreed with Arrhenius equation. The maximum MF yield was 82.5 % at 24 h, and the yield decreased to 75.4 % after 1 re-use of CAL-B, but maintained about 20 % for next 4 cycles. Totally, the developed model and binary regression analysis method is ideal for in-depth examination of lipase-catalyzed kinetics in heterogeneous system.
研究领域:
生物化学
·
酶工程
✓ 已验证
DOI
高影响因子
MedComm
·
2023
·Vol. 4
·期 5
·e354
·
IF 9.9
Yina Zhang,Liying Wang,Jiajia Shao,Yanning Liu,Yining Lu,Jing Yang,Siduo Xu,Jingkang Zhang,Minwei Li,Xiangrui Liu,Min Zheng
Calcipotriol (CAL) has been widely studied as a fibrosis inhibitor and used to treat plaque psoriasis via transdermal administration. The clinical application of CAL to treat liver fibrosis is bottlenecked by its unsatisfactory pharmacokinetics, biodistribution, and side effects, such as hypercalcemia in patients. The exploration of CAL as a safe and effective antifibrotic agent remains a major challenge. Therefore, we rationally designed and synthesized a self-assembled drug nanoparticle encapsulating CAL in its internal hydrophobic core for systematic injection (termed NPs/CAL) and further investigated the beneficial effect of the nanomaterial on liver fibrosis. C57BL/6 mice were used as the animal model, and human hepatic stellate cell line LX-2 was used as the cellular model of hepatic fibrogenesis. Immunofluorescence staining, flow cytometry, western blotting, immunohistochemical staining, and in vitro imaging were used for evaluating the efficacy of NPs/CAL treatment. We found NPs/CAL can be quickly internalized in vitro, thus potently deactivating LX-2 cells. In addition, NPs/CAL improved blood circulation and the accumulation of CAL in liver tissue. Importantly, NPs/CAL strongly contributed to the remission of liver fibrosis without inducing hypercalcemia. Overall, our work identifies a promising paradigm for the development of nanomaterial-based agents for liver fibrosis therapy.
研究领域:
药理学
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纳米技术
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肝病学
·
药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2019
·
IF 8.355
Jinchen Ma,Daofeng Mei,Weiwei Peng,Xin Tian,Danyan Ren,Haibo Zhao
Calcium looping (CaL) is extensively used in post-combustion capture of CO 2 and sorption-enhanced steam methane reforming because of its advantages of low cost and theoretically high CO 2 -capture capacity. Despite this, unstable reactivity of sorbent (CaO) and significant heat requirement for CaCO 3 calcination were always encountered in CaL. To address the aforementioned issues, a core-shell structured CaO-CuO/MgO@Al 2 O 3 sorbent (CCMA for short) was synthesized via the self-assembly template synthesis (SATS) method, and systematically investigated in terms of carbonation, calcination-reduction and oxidation cycles. In comparison to wet-mixing CaO-CuO material (CC), MgO-supported CaO-CuO (CCM) and Al 2 O 3 -supported CaO-CuO (CCA), the CCMA performed the highest CO 2 uptake capacity, which was quite stable at around 0.08 [g CO 2 ∙(g material) −1 ] in the 30 cyclic tests. In calcination-reduction stage, CaO in CCMA can be fully recovered by the decomposition of CaCO 3 , meanwhile the corresponding heat requirement can be compensated by the exothermic reaction between CuO and CH 4 , i.e., thermal neutrality can be achieved by using CCMA. The Cu in reduced CCMA can be subsequently oxidized back to CuO in the oxidation stage with a conversion of 97–98%, which is much higher than CC, CCM and CCA. After cycles, no serious sintering was observed for the CCMA and the measured crushing strength (1.4 N) was sufficient for fluidization, which, in combination with its high reactivity, makes this material very promising for CaL-CLC process.
研究领域:
能源科学
·
材料科学
✓ 已验证
DOI
高影响因子
JOURNAL OF ORGANOMETALLIC CHEMISTRY
·
2023
·
IF 2.3
Wei Tian,Jingni Wang,Wen Zhong,Hao Huang,Mingyu Ji,Tingting Yang,Shijie Lin,Shaofeng Chen,Peilin Yang
Two new anthraquinone-organotin complexes [Ph 3 Sn(O 2 CC 14 H 7 O 2 ) · MeOH] · MeOH ( AQS01 ) and Cy 3 Sn(O 2 CC 14 H 7 O 2 ) ( AQS02 ) were synthesized and characterized by elemental analysis, IR, 1 H NMR, 13 C NMR, 119 Sn NMR, X-ray crystallography and thermo-gravimetric analysis. Incorporation of 9,10-anthraquinone with organotin successfully enhanced its anticancer activity. Interestingly, the anti-proliferative activity of AQS01 against CAL-27 cells in vitro was almost 10-fold that of mitoxantrone and 40-fold that of cisplatin. Flow cytometry showed that AQS01 could induce apoptosis and arrest cell cycle in S phase. UV–visible absorption spectrometry and molecular docking showed that AQS01 can be well embedded in the double helix of DNA. Moreover, AQS01 induced cell death by upregulating the expression level of the DNA damage protein γ -H 2 AX and activating the mitochondrial apoptotic signaling pathway (Bax/Bcl-2). Therefore, AQS01 can be used as a potential anticancer drug and has potential for further research.
研究领域:
无机化学
·
有机金属化学
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癌症研究
·
生物化学
·
药理学
✓ 已验证
DOI
高影响因子
Pharmaceutics
·
2024
·Vol. 16
·期 9
·1130
·
IF 4.9
Xiao Li,Zhiyin Li,Yue Su,Jia Zhou,Yuxiang Li,Qianqian Zhao,Xia Yang,Leilei Shi,Lingyue Shen
In the present work, we pioneered a coordinated self-assembly approach aimed at fabricating carrier-free hybrid nanoparticles to address the inherent challenges of the anaerobic microenvironment and the oxidative resistance induced by reductive glutathione (GSH) in photodynamic therapy (PDT). In these nanoparticles, protoporphyrin IX (PP), HIF-1α inhibitor ofN, Nʹ-(2,5-Dichlorosulfonyl) cystamine KC7F2 (KC), and the cofactor Fe3+present hydrogen bond and coordination interaction. The nanoparticles exhibited efficient cellular uptake by CAL-27 cells, facilitating their accumulation in tumors by enhanced permeability and retention (EPR) effect. Under irradiation at 650 nm, the formation of cytotoxic singlet oxygen (1O2) would be enhanced by the synergy effect on the Fenton reaction of Fe3+ion and the downregulation of the HIF-1α, leading to the improved PDT efficacy both in vitro and in vivo biological studies. Our work opens a new supramolecular approach to prepare hybrid nanoparticles for effective synergy therapy with PDT against cancer cells.
研究领域:
纳米技术
·
癌症治疗
·
生物医学工程
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药学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
APPLIED ORGANOMETALLIC CHEMISTRY
·
2019
·Vol. 33
·期 10
·e5120
·
IF 3.259
Dongdong Li,Luyao Wang,Ernesto Yagüe,Linlin Dai,Xiumei Zhao,Zibo Yang,Shuang Zhi,Yunhui Hu
An innovative ternary copper(II) complex, [Cu(Cl-PIP)(Tyr)Cl] n , has been synthesized and characterized using infrared spectroscopy, elemental analysis and single-crystal X-ray diffraction analysis. X-ray crystallography indicates that the Cu atom is five-coordinated in a square-pyramidal configuration. The unit forms a one-dimensional chain along the crystallographic c -axis. The complex was screened for cytotoxicity against a panel of eight human cancer cell lines, namely MDA-MB-231, CAL-51, K562, HeLa, SGC-7901, A549, MCF-7 and SMMC-7721. The best anticancer activity was obtained with triple-negative breast cancer CAL-51 and MDA-MB-231 cell lines, with IC 50 values in the range 0.035–0.10 μM, and this was better than using carboplatin. The complex inhibits proteasomal chymotrypsin-like activity, and docking studies reveal its interaction with 20S proteasome. In addition, the complex causes accumulation of ubiquitinated proteins, induces apoptosis and inhibits cell proliferation, indicating its great potential as a novel therapy for triple-negative breast cancer.
研究领域:
癌症研究
·
化学
·
药理学
·
分子生物学
·
细胞生物学
✓ 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）