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JOURNAL OF MICROENCAPSULATION · 2020 · IF 2.287

Novel folated pluronic F127 modified liposomes for delivery of curcumin: preparation, release, and cytotoxicity

Ziling Li,Xiangyuan Xiong,Shengfeng Peng,Xing Chen,Wei Liu,Chengmei Liu

Aim: A novel folated pluronic F127 (FA-F127) was synthesised, so as to modify liposomes with FA group on the surface, and evaluate the effects of FA-F127 modification on the properties of the modified liposomes.Methods: FA was linked to one end of pluronic F127, via the terminal OH group, to obtain FA-F127 and the structure was characterised. FA-F127 modified curcumin liposomes (cur-FA-F127-Lps) were prepared. The physicochemical characteristics of cur-FA-F127-Lps, including morphology and particle size, were studied. The in vitro cytotoxicity of cur-FA-F127-Lps against KB cancer cells was determined by MTT tests.Results: The effects of FA-F127 modification on the average particle size, PDI, curcumin encapsulation efficiency and microstructure were not significant. Compared with nonfolated F127 liposomes (cur-F127-Lps), cur-FA-F127-Lps exhibited significantly higher cytotoxicity towards KB cells.Conclusions: Folic acid modified liposomes provide a novel strategy to improve the chemotherapeutic efficacy of hydrophobic bioactive compounds.

CAS / MDL: 458-37-7
研究领域: 药剂学 · 药物递送系统 · 纳米技术 · 肿瘤学
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Nanomaterials · 2016 ·Vol. 6 ·期 6 ·113 · IF 2.69

Targeting and Photodynamic Killing of Cancer Cell by Nitrogen-Doped Titanium Dioxide Coupled with Folic Acid

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

CAS / MDL: 919-30-2
研究领域: 纳米技术 · 癌症研究 · 材料科学 · 治疗学
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FOOD AND CHEMICAL TOXICOLOGY · 2023 · IF 4.3

Piperlongumine induces apoptosis and autophagy via the PI3K/Akt/mTOR pathway in KB human cervical cancer cells

Eun-Ji Han,Eun-Young Choi,Su-Ji Jeon,Sang-Woo Lee,Jun-Mo Moon,Soo-Hyun Jung,Bumseok Kim,Sung-Dae Cho,Jeong-Seok Nam,Changsun Choi,Jeong-Hwan Che,Ji-Youn Jung

Natural products are continuously being researched to develop safe and effective treatment options for cervical cancer , the fourth most common cancer in women. Piperlongumine (PL), an amide alkaloid mainly present in long pepper , exhibits neuroprotective and anti-cancer properties. However, the specific effect of PL in cervical cancer and the relationship between the anti-cancer pathway and autophagy remain unclear. Therefore, we aimed to investigate PL-induced apoptosis in KB human cervical cancer cells and the relationship between apoptosis and autophagy therein. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and wound-healing assays showed that PL treatment suppressed KB cell viability and proliferation. Apoptosis was identified through 4′,6-diamidino-2-phenylindole and annexin V-propidium iodide staining, increased cleaved-poly (ADP-ribose) polymerase and Bcl-2 associated X levels, and decreased B cell lymphoma 2 levels. Acridine orange staining and increased microtubule-associated protein 1A/1B-light chain 3-II and Beclin-1 levels confirmed autophagy. We determined that KB cell-related autophagy exerted cytoprotective effects using the autophagy inhibitors 3-methyladenine and hydroxychloroquine . PL treatment promoted apoptosis by inhibiting the phosphatidylinositol-3-kinase (PI3K)/protein kinase B/mammalian target of rapamycin pathway in KB cells; inhibiting the pathway using PI3K inhibitors increased autophagy. We suggest that PL is a potential natural anticancer agent for cervical cancer treatment.

研究领域: 肿瘤学 · 药理学 · 细胞生物学 · 天然产物化学
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2019 · IF 3.571

Establishment and Use of Human Mouth Epidermal Carcinoma (KB) Cells Overexpressing P-Glycoprotein To Characterize Structure Requirements for Flavonoids Transported by the Efflux Transporter

Yajing Fang,Mengmeng Xia,Fuqiang Liang,Weiwei Cao,Siyi Pan,Xiaoyun Xu

This study was aimed to determine the mechanism for flavonoid poor absorption related to P-glycoprotein (P-gp). The cellular uptake (CU) of 40 flavonoids was investigated in P-gp overexpressing KB/multidrug-resistant (MDR) cells. A total of 9 flavonoids, including 5,7,3′,4′-tetramethoxyflavone, with a significant (p < 0.05) CUKBE (2.90 ± 0.146 μmol/g) higher than CUKBP (1.57 ± 0.129 μmol/g) were identified as P-gp substrates. Besides, 8 substrates, including tangeretin, showed a significant (p < 0.05) CUKB (9.72 ± 1.09 μmol/g) higher than its CUKBP (7.36 ± 0.692 μmol/g). A total of 7 of 17 flavonoid substrates stimulated the P-gp efflux of rhodamine 123, and most substrates increased P-gp expression in KB/MDR cells. Docking analyses showed a good correlation (R = 0.764; p < 0.01) between efflux fold and S_scoring of flavonoids to the P-gp model, indicating consistency between in silico and in vitro results. A structure–affinity relationship exhibited that 3-OH, 5-OH, 3′-OCH3, and 4′-OCH3 are crucial for flavonoids binding to P-gp. These results provide valuable information for finding a solution to improve the absorption of flavonoids.

研究领域: 药理学 · 癌症研究 · 分子生物学
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RSC Advances · 2014 ·Vol. 4 ·期 94 ·51950-51959 · IF 3.708

A FITC-doped silica coated gold nanocomposite for both in vivo X-ray CT and fluorescence dual modal imaging

Jie Feng,Di Chang,Zhifei Wang,Bin Shen,Jinjin Yang,Yanyun Jiang,Shenghong Ju,Nongyue He

Dual-modal imaging contrast agents with unique X-ray computed tomography (CT) and optical imaging capabilities have attracted much attention in recent years. Herein, the new silica hybrid nanocomposites containing Au nanoparticles and FITC dyes (FITC–Au@SiO2) were investigated as this kind of contrast agent. TEM characterization showed that the as-synthesized FITC–Au@SiO2 nanoprobes were uniform in morphology with the average size of 90 nm. After the PEGylation, the obtained FITC–Au@SiO2@PEG exhibited good dispersion stability under different conditions. The MTT assay suggested that FITC–Au@SiO2@PEG didn't show appreciable toxicity toward KB cells even at high concentration of up to 1000 μg mL−1. In addition, it was found that FITC–Au@SiO2@PEG could cross the cell membrane and enter into the cytoplasm during the incubation with cells. In vivo dual modal optical/CT imaging of C57BL/6J mice uncovered that within 2 h post-injection FITC–Au@SiO2@PEG nanoprobes preferred to accumulate in the liver and were gradually cleared through the enterohepatic circulation system, which could bring novel opportunities to the next generation of dual-modality contrast agents.

研究领域: 纳米技术 · 生物医学工程 · 医学成像
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TALANTA · 2016 · IF 4.035

A supramolecular material for dual-modal imaging and targeted cancer therapy

Shanyue Guan,Ruizheng Liang,Chunyang Li,Min Wei

Recently, how to design a formulation system with simultaneous diagnosis and therapy toward cancer has attracted tremendous attention. Herein, a supramolecular material was prepared via a facile method by the co-intercalation of folic acid (FA) and doxorubicin (DOX) into the gallery of Gd 3+ -doped layered double hydroxides (LDHs), followed by surface adsorption of fluorescein isothiocyanate (FITC). This supramolecular agent was proved to exhibit excellent magnetic resonance imaging (MRI) and fluorescence imaging (FI) behavior, as well as chemotherapy toward cancer (KB cell). The co-intercalated FA enables an efficient and selective drug delivery with good specificity. This work provides a facile approach for the fabrication of a drug formulation with dual-modal imaging and targeted therapy, which could be potentially used in the practical chemotherapy and medical imaging.

研究领域: 药学 · 纳米技术 · 生物医学工程 · 癌症研究 · 材料科学
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