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International Journal of Nanomedicine · 2023 · IF 8

Efficient delivery of Notch1 siRNA to SKOV3 cells by cationic cholesterol derivative-based liposome

Yun-Chun Zhao,Li Zhang,Shi-Sen Feng,Lu Hong,Hai-Li Zheng,Li-Li Chen,Xiao-Ling Zheng,Yi-Qing Ye,Meng-Dan Zhao,Wen-Xi Wang,Cai-Hong Zheng

A novel cationic cholesterol derivative-based small interfering RNA (siRNA) interference strategy was suggested to inhibit Notch1 activation in SKOV3 cells for the gene therapy of ovarian cancer. The cationic cholesterol derivative, N-(cholesterylhemisuccinoyl-amino-3-propyl)-N, N-dimethylamine (DMAPA-chems) liposome, was incubated with siRNA at different nitrogen-to-phosphate ratios to form stabilized, near-spherical siRNA/DMAPA-chems nanoparticles with sizes of 100–200 nm and zeta potentials of 40–50 mV. The siRNA/DMAPA-chems nanoparticles protected siRNA from nuclease degradation in 25% fetal bovine serum. The nanoparticles exhibited high cell uptake and Notch1 gene knockdown efficiency in SKOV3 cells at an nitrogen-to-phosphate ratio of 100 and an siRNA concentration of 50 nM. They also inhibited the growth and promoted the apoptosis of SKOV3 cells. These results may provide the potential for using cationic cholesterol derivatives as efficient nonviral siRNA carriers for the suppression of Notch1 activation in ovarian cancer cells.

研究领域: 癌症生物学 · 基因治疗 · 药学 · 纳米技术
✓ 已验证 DOI PubMed 高影响因子
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2015 · IF 4.152

Knockdown of STAT3 expression in SKOV3 cells by biodegradable siRNA–PLGA/CSO conjugate micelles

Yunchun Zhao,Caihong Zheng,Li Zhang,Yue Chen,Yiqing Ye,Mengdan Zhao

Biodegradable and biocompatible poly( d,l -lactic- co -glycolic acid) (PLGA)was conjugated to the 5′-thiol end of signal transducer and activator of transcription 3 (STAT3) small interfering RNA (STAT3–siRNA) via a disulfide bond. In aqueous environments, these siRNA–PLGA conjugates can spontaneously form core/shell type spherical micelles with a particle size of about 200   nm. A biodegradable, low molecular weight cationic polymer, chitosan oligosaccharide (CSO), was added to the siRNA–PLGA micelles at different nitrogen to phosphate (N/P) ratios to form stable, spherical siRNA–PLGA/CSO micelles with sizes of 150–180   nm. The siRNA–PLGA/CSO micelles were produced via ionic complexation between negatively charged siRNA and positively charged CSO on the outer shell of the micelles. The siRNA–PLGA/CSO micelles exhibited superior cellular uptake and STAT3 gene silencing efficiency in SKOV3 ovarian cancer cells when compared with siRNA/CSO complexes at the same N/P ratios with no significant differences with lipofectamine 2000. Furthermore, the siRNA–PLGA/CSO micelles showed that the efficiencies of cellular uptake and STAT3 gene silencing gradually increased with increasing N/P ratios. The siRNA–PLGA/CSO micelles also inhibited the growth of SKOV3 cells, as well as, promoted apoptosis of the cells. These results indicate that siRNA–PLGA/CSO micelles can be utilized as a novel and efficient siRNA carrier to treat a variety of diseases.

研究领域: 癌症研究 · 药学 · 纳米技术 · 分子生物学
✓ 已验证 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

Structural and anti-ovarian cancer insights into the immunoglobulin G-glabridin nanocomplex

Zhiqiang Guo,Mengdie Tian,Min Zhou,Zhuoer Li,Meijun Li

In this study, the formation of the immunoglobulin G-glabridin (IgG-GB) complex and nanocomplex was analyzed by assessing the structure, stability, solubility, and anticancer effects against the human epithelial ovarian cancer cell line SKOV3. The hydrodynamic sizes of the prepared IgG-GB nanocomplex were 190.1 ± 25.68 nm (PDI: 0.19 ± 0.02), and the solubility levels of GB in the free and nanoformulated forms were 97.28 μg/mL and 368.95 ± 59.63 μg/mL, respectively. Additionally, the IgG-GB nanocomplex exhibited a slower and more sustained release of GB in a pH-sensitive manner. Spectroscopic measurements indicated logKb values of 4.01 and 4.66 for the IgG-GB complex and the IgG-GB nanocomplex, respectively. Furthermore, the main reaction type between IgG and GB was found to be hydrophobic forces, which led to the partial folding of IgG and nanoformulated IgG. Cellular assays demonstrated that the IC50 concentrations of GB, the IgG-GB complex, and the IgG-GB nanocomplex in ovarian cancer SKOV3 cells were 10.74, 10.05, and 6.39 μM, respectively, while these amounts were > 77.84 μM in normal epithelial FHC cells. Moreover, the IgG-GB nanocomplex resulted in increased membrane leakage, mitochondrial dysfunction, and upregulation of Bax/Bcl-2 and caspase-3, along with caspase-3 activity determined by LDH, MP, real-time PCR, and enzyme activity assays. In conclusion, an efficient IgG-GB nanocomplex was potentially prepared and developed as a selective anticancer system against ovarian cancer cells.

研究领域: 药理学 · 肿瘤学 · 生物化学
✓ 已验证 DOI PubMed 高影响因子
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Journal of Nanomaterials · 2019 · IF 2.233

Synthesis of Ag@Fe3O4 Nanoparticles for Photothermal Treatment of Ovarian Cancer

Bing Liu,Jian Zhou,Bin Zhang,Jing Qu

Photothermal therapy is a promising approach for cancer treatment. In our study, we investigate the photothermal effect of different concentrations of the Ag@Fe3O4 nanoparticles on apoptosis and proliferation in the human epithelial ovarian cancer cells SKOV3. Ovarian cancer cells SKOV3 were treated with the Ag@Fe3O4 nanoparticles under an 808 nm near-infrared (NIR) laser irradiation at different concentrations. The cell proliferation was measured by the cell counting kit-8 (CCK-8) assay. The results show that the Ag@Fe3O4 nanoparticles with NIR laser irradiation could markedly inhibit the proliferation of the ovarian cancer cells SKOV3 independent of a concentration-time manner. Meanwhile, the cell morphology was also seriously damaged under the treatment of high-concentration nanoparticles. However, Ag@Fe3O4 nanoparticles have almost no obvious effect on the growth of SKOV3 cells without NIR laser illumination treatment. Therefore, it is reasonable to believe that the Ag@Fe3O4 nanoparticles have promising applications in photothermal treatment of cancer cells.

研究领域: 生物医学 · 肿瘤学 · 纳米医学
✓ 已验证 DOI 高影响因子
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COLLOIDS AND SURFACES B-BIOINTERFACES · 2019 · IF 3.973

β-Cyclodextrin coated and folic acid conjugated magnetic halloysite nanotubes for targeting and isolating of cancer cells

Xiufang Li,Jian Chen,Hui Liu,Zhiwei Deng,Jianbing Li,Tao Ren,Ling Huang,Wenqing Chen,Yanjing Yang,Shian Zhong

The study developed a simple, effective and inexpensive strategy for capturing, enriching and detecting circulating tumor cells (CTCs) by using folic acid (FA) as the targeting molecule instead of antibodies. This work constructed magnetic halloysite nanotubes (MHNTs) coated with biocompatible β-cyclodextrin (CD), and conjugated to FA via a PEG-Ad linker, to specifically capture the FA receptor (FR)-overexpressing cancer cells. The capture efficiencies of [email protected] β [email protected] for the Skov3, Hela and A549 cancer cells were 96.3%, 97.0% and 95.6% respectively. In addition, the nanoparticles were able to capture very low numbers of the cancer cells (25–500 cells/mL) from PBS and whole blood, as well as selectively capture the cancer cells over normal HEK 293 T cells. Furthermore, the captured cells were viable and grew normally in vitro , indicating the future potential of downstream analyses. This approach can be adapted for different CTCs, once the tumor-specific surface markers are identified and the efficacy of targeting ligands is established. Taken together, FA-conjugated MHNTs nanoparticles are a highly promising tool for isolating CTCs for the diagnosis and treatment of cancer.

研究领域: 纳米技术 · 癌症生物学 · 生物医学工程 · 分子生物学 · 药物递送系统
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Journal of Materials Chemistry B · 2015 ·Vol. 4 ·期 2 ·273-281 · IF 4.726

Highly efficient Gab2 siRNA delivery to ovarian cancer cells mediated by chitosan–polyethyleneimine nanoparticles

Lei Wang,Weimin Wu,Jingshuai Wang,Jianjun Wang,Xiaowen Tong,Qiaoling Hu,Lifeng Qi

Malignant bowel obstruction (MBO) is a serious complication which causes high death rate and low quality of life (QOL) for patients diagnosed at an advanced stage of ovarian cancer. RNA interference (RNAi) could be a promising method for the treatment of ovarian cancer and could decrease the morbidity of MBO. Gab2 gene is overexpressed in ovarian cancer compared with normal ovarian tissue, and regulates the migratory behaviors and E-cadherin expression via activation of the PI3K pathway in ovarian cancer cells. Here, chitosan–polyethyleneimine (PEI, Mw 1800) copolymer nanoparticles were synthesized as nanocarriers to deliver Gab2 siRNA into SKOV3 cells. The silencing effects against the Gab2 gene and the antitumor effects by the chitosan–PEI–Gab2 siRNA nanoparticles (chitosan–PEI–Gab2 NPs) were studied. Results showed that highly efficient silencing effects against Gab2 expression and its downstream effector, AKT protein, at more than 90% deregulation were obtained by chitosan–PEI NP mediated Gab2 siRNA delivery, so as to exhibit obvious antitumor effects against SKOV3 cells with low cytotoxicity, and induce cell apoptosis in early and late stages. The study will provide novel strategies to overcome MBO in ovarian cancer by the efficient knockdown of Gab2 expression.

CAS / MDL: 64-17-5 7558-80-7
研究领域: 肿瘤学 · 药学 · 纳米技术 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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MICROCHEMICAL JOURNAL · 2024 · IF 4.9

A responsive aggregation-induced emission fluorescent probe for the detection of cysteine in food, serum samples and oxidative stress environments

Minggui Gong,Jiajie Su,Ying Chen,Kaixin Zheng,Lijie Yuan,Fangyuan Qin,Huawei Niu,Yong Ye

Heavy metal ions tend to accumulate through the food chain and may cause many serious diseases. As an antioxidant, cysteine (Cys) plays a crucial role in regulating redox homeostasis. In addition, Cys is also widely used in the food industry. Therefore, the development of a convenient, sensitive, and practical tool for detecting Cys is of great significance for investigating the physiological and pathological functions of Cys induced by heavy metal ions. In this paper, a fluorescent probe NYVB with aggregation-induced emission (AIE) activities has been designed and synthesized, which featured good advantages in Cys detection, including favorable selectivity, desirable sensitivity, wide linear range, and low detection limit. The prepared solid-state sensor enabled the ratiometric visual detection of Cys. Probe NYVB has been successfully implemented for testing Cys in real food samples and serum samples with satisfactory recoveries. In addition, probe NYVB has been successfully employed for detecting endogenous and exogenous Cys in SKOV3 cells. More excitingly, probe NYVB has also been used to track the detection of Cys in H 2 O 2 , Hg 2+ , or Cu 2+ -induced redox imbalance. Overall, probe NYVB will open up a new avenue for studying Cys in the amelioration of heavy metal toxicity and has practical applications.

研究领域: 分析化学 · 生物化学 · 毒理学 · 食品科学 · 细胞生物学
✓ 已验证 产品关联 DOI 高影响因子
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JOURNAL OF NANOSCIENCE AND NANOTECHNOLOGY · 2020 ·Vol. 20 ·期 1 ·1-14 · IF 1.134

Gold Nanoshells Coated 5-Aminolevulinic Liposomes for Photothermal-Photodynamic Antitumor Therapy

Jiang Yifei,Liu Yang,Fang Siyuan,Ji Min

In this study, a novel antitumor system was designed on the basis of photodynamic therapy and photothermal therapy using gold nanoshells coated 5-aminolevulinic acid (5-ALA) liposomes (GNALs). As a widely used photosensitizer prodrug, 5-aminolevulinic acid (5-ALA)-derived protoporphyrin IX (PpIX) can accumulate to a higher level in tumors than in normal tissues. Protoporphyrin IX (PpIX) initiates a series of cytotoxic reactions after irradiation of target tissue with a measured dose of light with appropriate wavelength, which may be dependent on the generation of reactive oxygen species. Gold nanoshells can strongly absorb NIR lasers at the same time, and can generate hyperthermia to provide photothermic effects. Gold nanoshells coated 5-ALA-Liposomes (GNALs) exhibit a uniform-sized spherical shape of 185.8±0.91 nm, with a zeta potential of 33±1.6 mV. Liposomes with specific sizes ranging from 100 to 200 nm can escape into the tumor interstitial tissue and accumulate preferentially in tumor tissue owing to the EPR effect. In addition, NIR light-excited nanosystems significantly promoted antitumor effects in this study compared to single photodynamic therapy. It was also found that the increased temperature promoted inhibition rate of SKOV3 cells. The novel drug delivery system shows great potential in photothermal-photodynamic antitumor therapy.

CAS / MDL: 5451-09-2 5471-63-6
研究领域: 癌症研究 · 纳米技术 · 药物递送系统 · 治疗学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Nanoscale · 2020 ·Vol. 12 ·期 9 ·5380-5396 · IF 6.895

Novel polymeric micelles as enzyme-sensitive nuclear-targeted dual-functional drug delivery vehicles for enhanced 9-nitro-20(S)-camptothecin delivery and antitumor efficacy

Yalin Sun,Yan Liang,Na Hao,Xiaoheng Fu,Bin He,Shangcong Han,Jie Cao,Qingming Ma,Wen Xu,Yong Sun

9-Nitro-20(S)-camptothecin (9-NC) is a broad-spectrum antitumor drug used in tumor treatments, but its clinical applications and antitumor efficacy are limited by its structural instability, poor solubility, and extremely low drug utilization in tumor tissues. In this study, enzyme-sensitive nuclear-targeted dual-functional polymeric micelles were developed for 9-NC delivery with a high drug loading content (12.93 ± 0.88%), steady-state circulation, and a rapid attack at the “heart” of tumor cells. Briefly, chrysin (CHR) as a π-conjugated moiety was immobilized on the PCL terminal in the TAT–PCL amphiphiles and combined with the ALAL peptide as a linker on HA chains to yield the ultimate CHR–PCL–TAT–ALAL–HA (HATPC) amphiphiles. Spherical 9-NC-loaded micelles were obtained from the self-assembly of the dual-functional amphiphiles comprising HATPC and 9-NC with uniform nanosize (121.6 ± 5.79 nm), well-distributed morphology (PDI: 0.256), and negative surface charge (−23.2 ± 0.5 mV), yielding high stability during blood circulation. In this drug delivery system, HA acts as an active tumor-targeting instrument via CD44-receptor-mediated endocytosis; further, the ALAL peptide could be cutoff in the lysosomes of the tumor cells due to the high expression of cathepsin B, leading to lysosomal escape, while the secondary polymeric micelles targeted the tumor cell nucleus via the exposed TAT peptide. The enzyme sensitivity and nuclei targetability of the 9-NC/HATPC micelles were confirmed by dynamic light scattering and confocal laser scanning microscopy analyses. As compared to free 9-NC and traditional mPEG2k–PCL2k polymeric micelles, 9-NC/HATPC micelles were the most concentrated in the tumor cell nucleus; therefore, they exhibited the highest cytotoxicity against SKOV3 tumor cells both in vitro (IC50 = 0.03 μg mL−1) and in vivo. This enzyme-sensitive nuclear-targeted dual-functional drug delivery system involving HATPC provided a new and promising strategy for enhanced 9-NC delivery and antitumor efficacy.

CAS / MDL: 68-12-2
研究领域: 药学 · 纳米技术 · 癌症研究 · 药物递送系统
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF PHARMACEUTICAL SCIENCES · 2021 · IF 3.534

Functionalized Graphene Oxide as Drug Delivery Systems for Platinum Anticancer Drugs

Liying Wei,Guo Li,Taicheng Lu,Yiming Wei,Zhenzhen Nong,Mei Wei,Xin Pan,Qixiao Qin,Fayan Meng,Xuehua Li

Graphene Oxide , prepared by the modified Hummer's method, was modified with a series of high polymers (polyethyleneimine, polyethylene glycol , chitosan) and Folic Acid for the delivery of platinum anticancer drugs including Cisplatin , Carboplatin , Oxaliplatin and Eptaplatin . Nanocarriers were successfully prepared and characterized by Fourier transform infrared spectroscopy , X-ray diffraction and scanning electron microscope. Measurement of drug loading efficiency showed that these nanocarriers had the ability for effective delivery of the platinum anticancer drugs. The Maximum loading ratios of Cisplatin, Carboplatin, Oxaliplatin and Eptaplatin were 25.72, 161.08, 345.21 and 67.80 μg/mg. Drug release experiments in the acid environment showed that the cumulative release rate of platinum anticancer drugs from nanocarriers was higher than that in the neutral environment. The cumulative release of all three nanocarriers in the acid environment reached above 60%. In vitro cytotoxicity assay showed that those nanocarriers had a low toxicity. The cell viability rates were above 80% for all three nanocarriers. Investigation of the anticancer activity in vitro showed that those drug delivery systems had the ability to inhibit the growth of the SKOV3 cell line. These results showed that those nanocarriers were suitable for the delivery of platinum anticancer drugs. Providing preliminary advice on the potential application of the combination of platinum anticancer drugs and the functionalized Graphene Oxide nanocarriers.

研究领域: 药学 · 纳米技术 · 癌症研究 · 材料科学 · 生物医学工程
✓ 已验证 产品关联 DOI PubMed 高影响因子
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