Phytochemistry Letters
·
2025
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IF 1.4
Yan-Mei Wu,Jing-Ya Mo,Yong-Yan Mei,Quan Liu,Yuan-Yuan Huang,Bei Zhou,Yi-Hang Li,Yan-Chun Wu,Jing-Quan Yuan
Trichodones D-F ( 1 - 3 ), three previously undescribed polyketide compounds featuring conjugated α - β -unsaturated ketone moieties, were isolated from the endophytic fungus Trichoderma protrudens associated with the semi-mangrove plant Hibiscus tiliaceus Linn. The structural elucidation of these compounds was accomplished through the analysis of 1D and 2D NMR spectra, complemented by HR-ESI-MS data. The absolute configurations were determined through comparative analysis of experimental CD and calculated ECD spectra. Additionally, the cytotoxic activities of compounds 1 - 3 against the human breast cancer cell line MCF-7 and the human hepatocellular carcinoma cell line HepG2 were evaluated using the CCK8 assay. Notably, compound 3 exhibited moderate inhibitory activity against HepG2 and MCF-7 cell lines with IC 50 values of 22.7 μM and 55.1 μM, respectively.
研究领域:
药理学
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有机化学
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肿瘤学
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DOI
高影响因子
Journal of Materials Chemistry B
·
2018
·Vol. 6
·期 30
·5011-5020
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IF 4.776
Jinyu Li,Yue Yang,Yibin Yu,Qi Li,Guoxin Tan,Yuanyuan Wang,Wei Liu,Weisan Pan
The synthetic clay material, LAPONITE® (LAP), having a nanodisk structure together with a negatively charged surface, has been used for effective drug encapsulation by virtue of its interlayer space. In this research effort, the LAP nanodisk was used for the first time to encapsulate the antifolic methotrexate (MTX); the MTX-loaded LAP nanodisks (LAP/MTX) demonstrated a high drug loading efficiency of 80.39%. An efficient and reliable tumor-targeting device that rests on the synthesized oligomeric hyaluronic acid-L-histidine (oHA–His) was then encapsulated in the MTX-loaded LAP disks (forming LAP/MTX/oHA–His nanohybrids). The drug released from the LAP/MTX/oHA–His nanohybrids was pH-dependent and matched the first-order kinetics that describes the diffusion mechanism. In vitro biological evaluation manifested that the MTX-loaded LAP nanocarriers, particularly the LAP/MTX/oHA–His nanohybrids that have targetability and lysosomal antineoplastic activity, can be effectively internalized by the MCF-7 cell line, and can exhibit a more prominent anticancer cytotoxicity than free MTX. In vivo studies with mice indicated that the LAP/MTX/oHA–His nanohybrids demonstrated much higher antitumor efficiency compared to the LAP/MTX nanohybrids and pure MTX. Taken together, the LAP/oHA–His, CD44 receptor targeting and pH-sensitive multifunctional nanohybrids conferred the MTX with excellent cytocompatibility, dispersion stability, sustained pH-responsive release properties, and improved anticancer activity, and may be further developed as a potential active nanoplatform for various anticancer drugs.
研究领域:
药学
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纳米技术
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癌症研究
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药物递送系统
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2024
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IF 7.7
Showkat Ali Ganie,Rayees Ahmad Naik,Ovas Ahmad Dar,Luqman Jameel Rather,Mohammed A. Assiri,Qing Li
We developed a facile method for the fabrication of a biodegradable delivery system composed of two blocks: curdlan and curcumin. This was achieved by chemical functionalization of curdlan through tosylation, amination followed by complexation with curcumin. A comprehensive evaluation of structural characterization and component stability showed that cur-cum complex exhibited better anticancer properties with enhanced thermal properties. The cur-cum complex shows pH sensitive sustained release behaviour with higher release at acidic pH and kinetic data of drug release follows the Korsmeyer-Peppas model. The cur-cum complex has ability to block the proliferation of the MCF-7 cell line as revealed by MTT assay which showed increased toxicity of cur-cum complex against these cell lines. The results obtained from western blot analysis demonstrated that the co-administration of cur and cum effectively induced apoptosis in MCF-7 cells. This effect was observed by a considerable upregulation of the Bcl-2/Bax ratio, a decline in mRNA expression of LDHA, level of lactate and LDH activity. The results clearly depict the role of functionalized curdlan as efficient carrier for curcumin delivery with prolonged, sustained release and enhanced bioavailability, thereby improving the overall anticancer activity.
研究领域:
药学
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生物医学工程
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癌症研究
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药物递送系统
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产品关联
DOI
PubMed
高影响因子
DRUG DELIVERY
·
2018
·
IF 3.095
Jiulong Zhang,Chunrong Yang,Shuang Pan,Menghao Shi,Jie Li,Haiyang Hu,Mingxi Qiao,Dawei Chen,Xiuli Zhao
Mitochondrial-targeting therapy was considered to be a promising approach for the efficient treatment of cancer while positive charge induced nonspecific cytotoxicity severely limits its application. To overcome this drawback, a novel mitochondria targeted conjugate triphenylphosphine-docetaxel (TD) has been synthesized successfully and incorporated it into liposomes (EPSLP/TD), which possessed excellent pH-sensitive characteristic, EphA 10 mediated active targetability as well as mitochondria-targeting capability. EPSLP/TD was characterized to have a small particle size, high-encapsulation efficiency and excellent pH-sensitive characteristic. Compared with DTX-loaded liposomes (EPSLP/DTX), EPSLP/TD possessed higher cytotoxicity against MCF-7 cell line. Mitochondrial-targeting assay demonstrated mitochondria-targeting moiety triphenylphosphine (TPP) could efficiently deliver DTX to mitochondria. Western immunoblotting assay indicated that EPSLP/TD could efficiently deliver antitumor drug to mitochondria and induce cell apoptosis via mitochondria-mediated apoptosis pathway. In vivo antitumor study demonstrated EPSLP/TD owed excellent in vivo antitumor activity. Histological assay demonstrated EPSLP/TD showed strongly apoptosis inducing effect, anti-proliferation effect and anti-angiogenesis effect. This work investigated the potential of hierarchical targeting pH-sensitive liposomes is a suitable carrier to activate mitochondria-mediated apoptosis pathway for cancer therapy.
研究领域:
药学
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癌症研究
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纳米技术
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药物递送系统
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产品关联
DOI
PubMed
高影响因子
Molecular Therapy-Nucleic Acids
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2017
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IF 6.392
Yingting Yu,Yi Yao,Hao Yan,Rui Wang,Zhenming Zhang,Xiaodan Sun,Lingyun Zhao,Xiang Ao,Zhen Xie,Qiong Wu
Targeted therapy for cancer is a research area of great interest, and magnetic nanoparticles (MNPs) show great potential as targeted carriers for therapeutics. One important class of cancer biomarkers is microRNAs (miRNAs), which play a significant role in tumor initiation and progression. In this study, a cascade recognition system containing multiple plasmids, including a Tet activator, a lacI repressor gene driven by the TetOn promoter, and a reporter gene repressed by the lacI repressor and influenced by multiple endogenous miRNAs, was used to recognize cells that display miRNA signals that are characteristic of cancer. For this purpose, three types of signal miRNAs with high proliferation and metastasis abilities were chosen (miR-21, miR-145, and miR-9). The response of this system to the human breast cancer MCF-7 cell line was 3.2-fold higher than that to the human breast epithelial HBL100 cell line and almost 7.5-fold higher than that to human embryonic kidney HEK293T cells. In combination with polyethyleneimine-modified MNPs, this recognition system targeted the tumor location in situ in an animal model, and an ≃42% repression of tumor growth was achieved. Our study provides a new combination of magnetic nanocarrier and gene therapy based on miRNAs that are active in vivo , which has potential for use in future cancer therapies.
研究领域:
癌症研究
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纳米技术
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基因治疗
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
Nanoscale
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2017
·Vol. 9
·期 34
·12533-12542
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IF 7.367
Cheng Gao,Fan Tang,Guiyi Gong,Jianxiang Zhang,Maggie P. M. Hoi,Simon M. Y. Lee,Ruibing Wang
In order to realize a combination of chemotherapy and selective drug release into tumor cells, novel pH-sensitive prodrugnanoparticles were designed and prepared via the self-assembly of a synthetic amphiphilic macromolecular prodrug for the selective co-delivery of doxorubicin (Dox) and curcumin (Cur). Dox was covalently conjugated to the oxidized sodium alginate through a Schiff base reaction to produce an amphiphilic macromolecular prodrug, and the prodrug was subsequently self-assembled into nanoparticles (Dox-NPs) in an aqueous solution, which were responsive to the acidic environment in tumor cells. Additionally, a second chemotherapeutic agent, Cur, was encapsulated in the core of nanoparticles (Cur–Dox-NPs) via hydrophobic effects, with a significant drug loading capacity. Cur–Dox-NPs exhibited an efficient release of both Dox and Cur in acidic media and further studies of their intracellular uptake and drug release confirmed that Dox-NPs were easily taken up by cells and selectively released the drug into the human breast cancer cell line MCF-7. In vitro cytotoxicity studies of the NPs showed a remarkable efficacy against MCF-7 cell lines, whereas an improved safety profile was observed in the human breast epithelial cell line MCF-10A. Furthermore, in vivo studies in zebrafish further confirmed an efficient absorption of Dox-NPs. In vivo cardiotoxicity experiments on a zebrafish model showed that Dox-NPs exhibited an improved cardiotoxicity profile in comparison with free Dox. This study demonstrated that this novel pH-sensitive prodrug-nanoparticle system may provide a simple and efficient platform for the selective co-delivery of multiple drugs to tumor cells.
研究领域:
药理学
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纳米技术
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肿瘤学
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药物递送系统
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产品关联
DOI
PubMed
高影响因子
BIOSENSORS & BIOELECTRONICS
·
2019
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IF 9.518
Ya Cao,Yuhao Dai,Hong Chen,Yingying Tang,Xu Chen,Ying Wang,Jing Zhao,Xiaoli Zhu
In this work, DNA-templated silver nanoclusters (DNA-AgNCs) with unique fluorescent and electrochemical properties are prepared as dual signal probes for both qualitative imaging and quantitative detection of cancer cells in an integrated system . ITO electrode that has good light transmittance and electric conductivity is employed as a substrate for dual analysis of cancer cells. ITO electrode is firstly modified by AS1141 aptamer , which could selectively bind to nucleolin overexpressed on the surface of a model breast cancer cell, MCF-7 cell line. The composite of mucin 1 antibody (anti-MUC1) and DNA-AgNCs then binds to MUC1 on the surface of captured MCF-7 cell, forming a sandwich-like structure. Therefore, our method allows noninvasive fluorescence imaging and amplified electrochemical detection using a single labeling platform, providing a biocompatible and highly specific method for adequate analysis of cancer cells. Experimental results demonstrate that strong red fluorescence of DNA-AgNCs clearly displays the loading of cancer cells on ITO electrode after dual recognition, and amplified electrochemical signals of DNA-AgNCs enable improved sensitivity toward quantitative analysis with a detection limit of 3 cells.
研究领域:
生物医学工程
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分析化学
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癌症研究
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纳米技术
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Food & Function
·
2020
·Vol. 11
·期 12
·10568-10579
·
IF 4.171
Jing Xu,Shan Jin,Fei Gan,Hui Xiong,Zhinan Mei,Yu Chen,Guangzhong Yang
The fruits of Garcinia xanthochymus can be eaten raw or processed into jams, preserves and vinegar. They provide not only vitamin and protein nutrients, but also pharmacologically active compounds, among which polycyclic polyprenylated acylphloroglucinols (PPAPs) are a major class. According to the literature, PPAPs exhibited good anti-cancer effects. This study investigated the antitumor effects and the underlying mechanism of S1 (the regioisomeric mixture of xanthochymol and guttiferone E) and S2 (the regioisomeric mixture of isoxanthochymol and cycloxanthochymol) isolated from the fruits of G. xanthochymus. In an H22 allograft mouse model, S1 and S2 could suppress the liver tumor growth and phosphorylation of STAT3. Computational modeling showed that S1 and S2 could form hydrogen bonds with the SH2 domain of STAT3. In HepG2 and MCF-7 cell lines, S1 and S2 downregulated the expression of p-STAT3Tyr705. Moreover, S1 and S2 inhibited the phosphorylation of JAK2 and Src, which are the upstream kinases of STAT3, and the expression of various STAT3-regulated genes, including anti-apoptotic (Bcl-XL, Mcl-1 and survivin), proliferative (cyclin D1) and angiogenic (VEGF) genes. As a result, S1 and S2 arrested the cell cycle and induced cell apoptosis, which were proved by the activation of cleaved caspase-3 and caspase-8. These results demonstrated that S1 and S2 from G. xanthochymus exhibited antitumor effects through the inactivation of STAT3, and could be promising candidates for cancer treatment.
研究领域:
药理学
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肿瘤学
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分子生物学
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生物化学
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产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
·
2020
·
IF 5.573
Jincan Chen,Jie Wang,Yuanyuan Deng,Baojun Li,Chengpeng Li,Yuxue Lin,Dongbin Yang,Huanyun Zhang,Lanmei Chen,Tao Wang
Two novel cyclometalated Ru(II) complexes containing isoquinoline ligand, [Ru(bpy) 2 (1-Ph-IQ)](PF 6 ), (bpy = 2,2′-bipyridine; 1-Ph-IQ = 1-phenylisoquinoline; RuIQ-1 ) and [Ru(phen) 2 (1-Ph-IQ)](PF 6 ) (phen = 1,10-phenanthroline; RuIQ-2 ) were found to show high cytotoxic activity against NCI–H460, A549, HeLa and MCF-7 cell lines. Notably, both of them exhibited IC 50 values that were an order of magnitude lower than those of clinical cisplatin and two structurally similar Ru(II)-isoquinoline complexes [Ru(bpy) 2 (1-Py-IQ)](PF 6 ) 2 ( Ru3 ) and [Ru(phen) 2 (1-Py-IQ)](PF 6 ) 2 ( Ru4 ) (1-Py-IQ = 1-pyridine-2-yl). The cellular uptake and intracellular localization displayed that the two cyclometalated Ru(II) complexes entered NCI–H460 cancer cells dominantly via endocytosis pathway, and preferentially distributed in the nucleus. Further investigations on the apoptosis-inducing mechanisms of RuIQ-1 and RuIQ-2 revealed that the two complexes could cause S, G2/M double-cycle arrest by regulating cell cycle related proteins. The two complexes also could reduce the mitochondrial membrane potential (MMP), promote the generation of intracellular ROS and trigger DNA damage, and then lead to apoptosis-mediated cell death . More importantly, RuIQ-2 exhibits low toxicity both towards normal HBE cells in vitro and zebrafish embryos in vivo . Accordingly, the developed complexes hold great potential to be developed as novel therapeutics for effective and low-toxic cancer treatment.
研究领域:
化学
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药学
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肿瘤学
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细胞生物学
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毒理学
✓ 已验证
DOI
PubMed
高影响因子
ANALYST
·
2023
·
IF 4.2
Wei Li,Huili Wang,Xinxin Ying,Zhen Liang,Jianna Li,Xiangjuan Chen,Lei Su,Xueji Zhang
Zr-metal–organic frameworks (Zr-MOFs) have received increasing interest for their use as the signal marker in the development of sandwich-structured aptasensors for the detection of exosomes. However, Zr4+ ions of the Zr-MOFs can interact with not only the exosomes, but also the aptamers, leading to possible false positives and a large background response. In the present study, we report for the first time aptasensors with Pd nanoparticle (NP)-decorated and hemin-embedded UiO-66 MOFs serving as the signal amplification marker to eliminate false positives and decrease the background response of aptasensors. To construct aptasensors for detection of exosomes, CD63-specific aptamers were tethered onto magnetic Fe3O4 particles coated with polydopamine (PDA) and UiO-66-NH2 using glutaraldehyde crosslinking for capturing the exosomes. To prepare highly catalytic Zr-MOF-based signal markers, UiO-66 MOFs were modified with hemin followed by Pd NPs. The as-prepared Pd-decorated hemin-embedded MOFs showed high catalytic activity towards the chromogenic oxidation reaction of TMB by H2O2. Moreover, the decoration with Pd NPs led to the change of the surface charge state of the catalytic hemin-embedded UiO-66 MOFs from positive to negative, weakening the interaction between the signal marker and the negatively charged aptamers. Therefore, the as-prepared aptasensors showed an improved sensing performance towards exosomes with a linear concentration range from 4.28 × 102 to 4.28 × 105 and a limit of detection (LOD) of 86.2 particles per μL. The as-prepared aptasensors also showed high sensitivity and selectivity to the exosomes from different origins including the HeLa cell line and MCF-7 cell line.
研究领域:
生物传感器
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纳米技术
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分析化学
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生物化学
✓ 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）