JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
·
2018
·Vol. 316
·期 1
·363-368
·
IF 1.181
Song Hu,Wang Guanquan,Wang Jing,Wang Yunhan,Wei Hongyuan,He Jiaheng,Luo Shunzhong
Porphyrin derivatives are usually used for photodynamic therapy (PDT) and labeled with raidonuclide for radiopharmaceuticals. In this work, 5,10,15,20-tetrakis (4-hydroxyphenyl) porphyrin (TPPOH) and 5,10,15,20-tetrakis (4-aminophenyl) porphyrin (TPPNH 2 ) were labeled by 131 I. 131 I-TPPOH and 131 I-TPPNH 2 were cultured with SMMC-7721 and HL-7702 cells for affinity test. The results show high uptake ratios of SMMC-7721 than HL-7702. 131 I-TPPOH and 131 I-TPPNH 2 were performed radionuclide therapy (RNT) and PDT via tumor in situ injection. At 14 days post injection, the volumes of tumors injected 131 I-TPPOH and 131 I-TPPNH 2 diminished 64 ± 11 and 54 ± 10%, respectively. The therapeutic effect is better than either single PDT or single RNT. The combination therapy of PDT and RNT could be a more effectual method for cancer therapy.
研究领域:
肿瘤学
·
核医学
·
药理学
✓ 已验证
DOI
高影响因子
MEDICINAL CHEMISTRY RESEARCH
·
2021
·Vol. 30
·期 6
·1240-1248
·
IF 1.965
Shi Bo-Ya,Wang Ze-Hao,Zhang Ning,Xie Yin-Rong,Sun Xiu-Li,Yang Hao-Nan,Wu Yi-Long,Zi Cheng-Ting,Wang Xuan-Jun,Sheng Jun
Novel glucosylated (-)-epigallocatechin-3-gallate derivatives 10 – 13 having the EGCG analogs conjugated to the d -glucosyl azide were synthesized by carrying out the copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction, and were evaluated for their cytotoxicities against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7, and SW480) using MTT assays. Compounds 10 and 11 showed the highest levels of cytotoxicity against the HL-60 cells with IC 50 values of 4.57 and 3.78 μM, respectively, and showed moderate selectivity toward cancer cell lines. Compound 11 was also shown to induce apoptosis in HL-60 cells. Most notably, inclusion of the perbutyrylated glucose residue in an EGCG derivative was concluded to lead to increased anticancer activity.
研究领域:
药物化学
·
肿瘤学
·
有机合成
✓ 已验证
产品关联
DOI
高影响因子
Journal of Physical Chemistry C
·
2021
·
IF 4.126
Long Jiao,Yixiao Wu,Yanjun Hu,Huaping Wu,Zhang Xu,Long Han,Qianqian Guo,Dongliang Li,Rong Chen
Droplet-based microfluidics, which manipulate mini-discrete droplets on surfaces to accomplish various chromogenic/fluorescence reaction-based detections, are promising for microminiaturization of analysis systems. However, rapid droplet evaporation in unsaturated surroundings is a complex problem. In this study, we proposed an ingenious concept of generating an oil/water microreactor on a superoleophobic/oleophilic-superhydrophobic/hydrophilic (SOB/OL-SHB/HL) multilevel patterned surface. A dual droplet with a nonvolatile liquid packing layer and a volatile droplet core was formed on the surface, achieving overt evaporation attenuation of the droplet core. The wettabilities of the SOB/OL-SHB/HL surface were first investigated. In addition, due to their outstanding configurability, oil/water microreactors with different pattern shapes, diverse compositions, and scale-up array configurations were obtained in a simple way. Due to the overt evaporation attenuation, the storage times of the reactants and products were markedly prolonged. Finally, as proofs of concept, oil/water microreactors were successfully applied to detect the target ion and to construct a droplet-based pH detector. The proposed oil/water microreactor on the SOB/OL-SHB/HL surface with distinct precision, flexibility, and high throughput is important to the development of high-performance microfluidic chips used in diagnosis, environment monitoring, chemical analysis, and particle synthesis.
研究领域:
分析化学
·
微流控技术
·
生物医学工程
✓ 已验证
产品关联
DOI
高影响因子
RSC Advances
·
2018
·Vol. 8
·期 72
·41377-41388
·
IF 2.936
Xiao-Qian Chi,Cheng-Ting Zi,Hong-Mei Li,Liu Yang,Yong-Feng Lv,Jin-Yu Li,Bo Hou,Fu-Cai Ren,Jiang-Miao Hu,Jun Zhou
In order to better understand the structure–activity relationship of mangostin, a series of xanthone derivatives based on α-mangostin were designed and synthesized. All the compounds were evaluated for their cytotoxicity against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7 and SW480) using MTT assays. Most of them showed cytotoxicity and most of all, compounds 1a and 2h showed the highest cytotoxic potency by HL-60 cancer cell lines with IC50 values of 5.96 μM and 6.90 μM respectively; compound 3e showed the highest cytotoxic potency against SMMC-7221 cancer cell line with IC50 values of 3.98 μM; compounds 2e and 2m showed lower cytotoxicity but higher selectivity than α-mangostin against HL-60 and SMMC-7221 cancer cell lines respectively. Structure–activity relationship analysis indicates that the maintenance of the isopentene group at C-8 is essential for the cytotoxic activity.
研究领域:
药物化学
·
肿瘤学
·
有机合成
✓ 已验证
DOI
PubMed
高影响因子
Scientific Reports
·
2020
·Vol. 10
·期 1
·1-11
·
IF 3.998
Chen Minjian,Yang Jing,Li Lei,Hu Yanhui,Lu Xiaomei,Sun Rongli,Wang Yubang,Wang Xinru,Zhang Xiaoling
Recently, celastrol has shown great potential for inducing apoptosis in acute myeloid leukemia cells, especially acute promyelocytic leukaemia cells. However, the mechanism is poorly understood. Metabolomics provides an overall understanding of metabolic mechanisms to illustrate celastrol's mechanism of action. We treated both nude mice bearing HL-60 cell xenografts in vivo and HL-60 cells as well as NB-4 cells in vitro with celastrol. Ultra-performance liquid chromatography coupled with mass spectrometry was used for metabolomics analysis of HL-60 cells in vivo and for targeted L-cysteine analysis in HL-60 and NB-4 cells in vitro . Flow cytometric analysis was performed to assess mitochondrial membrane potential, reactive oxygen species and apoptosis. Western blotting was conducted to detect the p53, Bax, cleaved caspase 9 and cleaved caspase 3 proteins. Celastrol inhibited tumour growth, induced apoptosis, and upregulated pro-apoptotic proteins in the xenograft tumour mouse model. Metabolomics showed that cysteine metabolism was the key metabolic alteration after celastrol treatment in HL-60 cells in vivo . Celastrol decreased L-cysteine in HL-60 cells. Acetylcysteine supplementation reversed reactive oxygen species accumulation and apoptosis induced by celastrol and reversed the dramatic decrease in the mitochondrial membrane potential and upregulation of pro-apoptotic proteins in HL-60 cells. In NB-4 cells, celastrol decreased L-cysteine, and acetylcysteine reversed celastrol-induced reactive oxygen species accumulation and apoptosis. We are the first to identify the involvement of a cysteine metabolism/reactive oxygen species/p53/Bax/caspase 9/caspase 3 pathway in celastrol-triggered mitochondrial apoptosis in HL-60 and NB-4 cells, providing a novel underlying mechanism through which celastrol could be used to treat acute myeloid leukaemia, especially acute promyelocytic leukaemia.
研究领域:
肿瘤学
·
药理学
·
代谢组学
·
细胞生物学
✓ 已验证
DOI
PubMed
高影响因子
Analytical Methods
·
2019
·Vol. 11
·期 41
·5250-5259
·
IF 2.378
Chenlei Gu,Xinwei Wei,Yuxiang Pan,Tao Liang,Ying Gan,Keqiang Gao,Yong Qiu,Hao Wan,Ping Wang
Drug-induced cardiac side-effects remain a major cause for the removal of drugs from the market and the termination of significant numbers of drug development projects. Many of the physiological and pharmacological reasons are still unclear. In this study, to comprehensively evaluate the cardiac side-effects of drugs, high-temporal-range evaluation with an HL-1-based impedance and long-term electrophysiology recording platform was proposed. Integrated with microscale interdigitated electrodes (IDEs) and planar microelectrodes, the platform could get reliable cell viability monitoring and extracellular electrophysiology recording simultaneously for low system signal drifting and noise (10 μV) in long-term experiments. HL-1 cardiac muscle cells were used as a target cardiac electrophysiology model because they are, by far, the only cardiomyocytes that can continuously divide while maintaining specific characteristics of adult cardiomyocytes. Vinblastine and nifedipine were introduced to verify the performance of this platform in a different time-dependent manner. According to the extracted cell viability and electrophysiological characteristics including cell impedance (namely, cell index, CI), extracellular field potential (EFP), firing rate (FR), inner-period and period-to-period intervals, the results showed that vinblastine exhibited a relatively strong effect on cell viability (maximum 79.83% decrease after 24 hours) and led to the fluctuation of inner-period intervals in long-term monitoring. In contrast, nifedipine presented a negligible effect on cell viability compared to control groups (maintaining minimum 86.20% of viability on an average after 24 hours), but a shortened QT interval (15.2% at least) was observed immediately. In summary, all the two time-dependent drug-induced results indicated that this HL-1-based impedance and long-term electrophysiology recording platform can not only monitor cell viability through the whole experiment but also possess both quick-reaction and long-term tracking ability for identical requirements, thus providing a promising and useful way for drug-induced cardiac side-effect evaluation in a high temporal range.
研究领域:
药理学
·
心脏病学
·
生物医学工程
✓ 已验证
DOI
高影响因子
JOURNAL OF HAZARDOUS MATERIALS
·
2026
·
IF 10.6
Huiliang Tang,Dawei Wang,Guozhi Deng,Qinian Wang,Chao Wu
Phthalate esters (PAEs) are ubiquitous synthetic plasticizer pollutants posing severe ecological and human health risks. This study compared microbial community structures and dibutyl phthalate (DBP) degradation kinetics of two consortia: 7-day enriched MC1 (50 mg/L DBP) and 6-cycle acclimated MC7 (50–1000 mg/L DBP), demonstrating directional DBP stress selection generated a low-diversity, highly specialized degradative community with a 25.4 mg/L/h maximum degradation rate ( V max ), 1.68-fold higher than MC1. Four dominant DBP-degrading strains were isolated from MC7; Pseudarthrobacter scleromae HL-1 showed the highest efficiency with 17.1 mg/L/h V max and complete 500 mg/L DBP removal within 72 h, broad substrate spectrum, and strong adaptability after optimization. Whole-genome sequencing and GC-MS/MS elucidated a dual-parallel DBP mineralization pathway, first reported in Pseudarthrobacter , integrating ester hydrolysis and side-chain β-oxidation. ECOSAR and Chlorella vulgaris bioassays confirmed progressive toxicity attenuation, with > 99% relative toxicity reduction after 72 h and no toxic intermediate accumulation. Natural lake water trials with trace background PAEs showed HL-1 successfully colonized aquatic environments, reshaped indigenous communities into synergistic degradative consortia, and achieved 99.2% DBP removal in 84 h. This work provides comprehensive insights into PAE biodegradation mechanisms from community to single strain and highlights HL-1 as a promising candidate for remediating PAE-polluted aquatic ecosystems.
✓ 已验证
DOI
高影响因子
Analytical Cellular Pathology
·
2023
·
IF 3.2
Fan Du,Ting Jin,Li Wang
Objective. Acute myeloid leukemia (AML) is a heterogeneous malignancy with a low long-term survival rate. The aim of this study was to investigate the effects of decitabine (DAC) treatment cell proliferation and apoptosis in AML and role of the expression of LINC00599 and, consequently, miR-135a-5p. Materials and Methods. Human promyelocytic leukemia cells (HL-60) and human acute lymphatic leukemia (CCRF-CEM) cells were treated with various concentrations of DAC. Cell proliferation in each group was detected using the cell counting kit 8. For each group, apoptosis and reactive oxygen species (ROS) levels were detected using flow cytometry. Reverse transcription polymerase chain reaction (RT-PCR) was performed to examine the expression of lncRNA LINC00599. The expression of apoptosis-related proteins was analyzed using western blotting. The regulatory relationship between miR-135a-5p and LINC00599 was verified by constructing miR-135a-5p mimics, miR-135a-5p inhibit, wild type LINC00599 3-untranslated region (UTR), and mutant LINC00599 3-UTR. Ki-67 expression in the tumor tissues of nude mice was detected using immunofluorescent assays. Results. Both DAC and LINC00599 Inhibit groups were able to significantly reduce the proliferation of HL60 and CCRF-CEM cells, increase apoptosis, upregulate the expression of Bad, cleaved caspase-3, and miR-135a-5p, downregulate the expression of Bcl-2, and elevate ROS levels in cells, with these effects being more pronounced after combined treatment with DAC and LINC00599 Inhibit. In comparison to mimic NC, the miR-135a-5p mimic group significantly decreased the relative fluorescence activity ratio of LINC00599 3-UTR wild-type CCRF-CEM cells. The LINC00599 Inhibit and miR-135a-5p mimic groups exhibited substantially reduced proliferation of HL60 and CCRF-CEM cells, increased apoptosis, upregulated Bad, cleaved caspase-3, and miR-135a-5p expression, along with downregulated Bcl-2 and LINC00599 expression and increased ROS levels in cells; these effects were more pronounced after LINC00599 Inhibit was combined with miR-135a-5p mimics. In vivo experiments revealed that both DAC and LINC00599 Inhibit were able to considerably reduce the long diameter, short meridian, volume, and mass of tumors, increase miR-135a-5p expression, and decrease LINC00599 and ki-67 expression in tumor tissues of nude mice. This effect was more pronounced when the DAC and LINC00599 Inhibit were used in combination. Conclusion. DAC regulates the expression of miR-135a-5p by regulating the expression of LINC00599, which in turn affects cell proliferation, apoptosis, and tumor proliferation. Our findings provide a theoretical basis for improving the clinical outcome of AML.
研究领域:
肿瘤学
·
血液学
·
分子生物学
·
药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Journal of Cardiovascular Translational Research
·
2023
·
IF 3.4
Wang Li,Wang Chuanhe,Sun Zhaoqing,Du Aolin,Shan Fei,Sun Zhijun
Myocardial ischemia/reperfusion (MI/R) injury induces myocardial damage and dysfunction. Increasing evidence has confirmed that circular RNAs (circRNAs) play crucial roles in regulating MI/R. Mmu-circ-0001380 has identified to be highly expressed in myocardium of MI/R mouse model. However, its biological function and molecular mechanism in MI/R injury are still unclear. Here, we demonstrated that knockdown of cric-0001380 attenuated myocardial injury of MI/R mice. In vitro , silence of circ-0001380 significantly enhanced viability, and inhibited apoptosis and oxidative stress in HL-1 cells under oxygen–glucose deprivation/reoxygenation (OGD/R). Mmu-miR-106b-5p interacted with circ-0001380, and suppressed the expression of pleckstrin homology domain and leucine rich repeat protein phosphatase 2 (Phlpp2). The miR-106b-5p/Phlpp2 axis mediated the effect of circ-0001380 on OGD/R-induced apoptosis through regulating the phosphorylation of p38, and further involved in regulating the viability and oxidative stress of HL-1 cells. In conclusion, circ-0001380 downregulation relieves MI/R injury via regulating the miR-106b-5p/Phlpp2 axis. Graphical Abstract The present study indicates that mmu-circ-0001380 exacerbates the myocardial ischemia/reperfusion injury through modulating the miR-106b-5p/Phlpp2 axis in vitro and in vivo .
研究领域:
心脏病学
·
分子生物学
·
细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS
·
2021
·
IF 4.698
Xixi Song,Minghui Wang,Hongchao Jiao,Jingpeng Zhao,Xiaojuan Wang,Hai Lin
Ghrelin, classically known as a central appetite-stimulating hormone, has recently been recognized to play an important role in peripheral tissue energy metabolism. In chicken, contrary to mammal, ghrelin acts as an anorexia signal, increased by fasting and further elevated after refed. In the present study, the effect of ghrelin on glucose/lipid utilization by peripheral tissues was investigated. Injection of exogenous acyl ghrelin reduced plasma triglyceride and glucose levels of chickens at both fasting and fed status. In the in vitro cultured chicken primary hepatocytes, adipocytes, and myoblasts, ghrelin suppressed glucose uptake , stimulated fatty acids uptake and oxidation , and decreased TG content. In hepatocyte, ghrelin increased the activities of LPL and HL, and upregulated the expression levels of gene ACC , CPT1 , and PPARα . Ghrelin treatment markedly increased the protein level of p-ACC, PPARγ, PGC1α, and CPT1 in hepatocytes, adipocytes and myoblasts. Inhibition of AMPK activity by Compound C had no influence on glucose uptake by hepatocyte, adipocyte, and myoblast, but further amplified the stimulated fatty acid uptake of adipocyte by ghrelin. The present result demonstrates that ghrelin facilitates the uptake and oxidation of fatty acid and cut down the utilization of glucose by the liver, muscle, and adipose tissues. The result suggests that ghrelin functions as a signal of fatty acid oxidation. The study provides a vital framework for understanding the intrinsic role of ghrelin as a crucial factor in the concerted regulation of metabolic substrate of hepatocytes, adipocytes, and myoblasts.
研究领域:
内分泌学
·
代谢
·
动物生理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
APOPTOSIS
·
2023
·Vol. 28
·期 3
·607-626
·
IF 7.2
Yu Li-Ming,Dong Xue,Huang Tao,Zhao Ji-Kai,Zhou Zi-Jun,Huang Yu-Ting,Xu Yin-Li,Zhao Qiu-Sheng,Wang Zhi-Shang,Jiang Hui,Yin Zong-Tao,Wang Hui-Shan
Ferroptosis contributes to the pathogenesis of atrial fibrillation (AF), although the mechanisms are still largely uncovered. The current study was designed to explore the pharmacological effects of icariin against ethanol-induced atrial remodeling, if any, and the mechanisms involved with a focus on SIRT1 signaling. Excessive ethanol-treated animals were administered with Ferrostatin-1, Erastin or icariin to evaluate the potential effects of icariin or ferroptosis. Then, the underling mechanisms was further explored in the in vitro experiments using HL-1 atrial myocytes. Excessive ethanol administration caused significant atrial damage as evidenced by increased susceptibility to AF, altered atrial conduction pattern, atrial enlargement, and enhanced fibrotic markers. These detrimental effects were reversed by Ferrostatin-1 or icariin treatment, while Erastin co-administration markedly abolished the beneficial actions conferred by icariin. Mechanistically, ethanol-treated atria exhibited markedly up-regulated pro-ferroptotic protein (PTGS2, ACSL4, P53) and suppressed anti-ferroptotic molecules (GPX4, FTH1). Icariin treatment inhibited ethanol-induced atrial ferroptosis by reducing atrial mitochondrial damage, ROS accumulation and iron overload. Interestingly, the in vivo and in vitro data showed that icariin activated atrial SIRT1-Nrf-2-HO-1 signaling pathway, while EX527 not only reversed these effects, but also abolished the therapeutic effects of icariin. Moreover, the stimulatory effects on GPX4, SLC7A11 and the suppressive effects on ACSL4, P53 conferred by icariin were blunted by EX527 treatment. These data demonstrate that ferroptosis plays a causative role in the pathogenesis of ethanol-induced atrial remodeling and susceptibility to AF. Icariin protects against atrial damage by inhibiting ferroptosis via SIRT1 signaling. Its role as a prophylactic/therapeutic drug deserves further clinical study.
研究领域:
心脏病学
·
药理学
·
分子生物学
·
细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ACS Sensors
·
2019
·
IF 6.944
Liping Liu,Zhen Fang,Xiangjiang Zheng,Dongmei Xi
A straightforward yet efficient, nanopore-based strategy that enables the sensitive detection of copper(II) ion (Cu2+) and real-time monitoring of a click reaction is provided. Two single-stranded DNAs (ssDNAs) are designed to act as the preprobes, one being modified with an azide and the other an alkyne. The presence of Cu2+ induces the ligation of two ssDNAs via click reaction, leading to the formation of a forked DNA which can quantitatively generate characteristic current signatures when interacts with α-hemolysin (α-HL) nanopore. The assay facilitates a highly selective and sensitive measurement of Cu2+ without the need for labels or signal amplification. More importantly, this nanopore platform exhibits excellent performance in real-time monitoring of a copper(I) ion (Cu+)-catalyzed click reaction at the single-molecule level, by recording the current signals of the forked DNA generated by click chemistry. The proposed strategy is believed to play an important role in both nanopore sensing and characterization of chemistry reactions, especially coupling reactions.
研究领域:
纳米孔传感
·
化学反应表征
·
生物分析化学
·
分子生物学
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）