INDUSTRIAL CROPS AND PRODUCTS
·
2024
·
IF 5.6
Xiaohui Zhang,Zhengyu Hu,Yuanqi Duan,Yuxin Jiang,Weiwei Xu,Pengcheng Yang,Wei Zhou,Jinfeng Sun,Gao Li
The purpose of this study was to optimize the extraction process of polysaccharides from the stems of Panax ginseng C. A. Meyer using different solvents (water, acid and alkali), and investigate their protective effects on PC12 cells against Amyloid-β 1–42 (Aβ 1–42 )-induced cell apoptosis. Three polysaccharides (W-GSP, Ac-GSP and Al-GSP) were prepared and optimized: liquid to material ratio 27:1 mL/g, extraction temperature 89°C, extraction time 2.9 h and 0.3 mol/L HCl/NaOH. The results of characterization indicated that the monosaccharides of W-GSP (703.80 kDa), Ac-GSP (641.38 kDa) and Al-GSP (457.04 kDa) all composed mannose, rhamnose, glucuronic acid, galacturonic acid, glucose, galactose, xylose and arabinose with different molar ratios. Interestingly, W-GSP possessed a lower uronic acid, higher molecular weight, rougher surface and poorer thermal stability, whereby W-GSP exhibited a protective effect against Aβ 1–42 -induced apoptosis in PC12 cells by mediating the JNK signaling pathway, restoring the mitochondrial membrane potential and reducing intracellular ROS levels. This study should be provided the theoretical basis for the study and exploitation of polysaccharides from the stems of Panax ginseng C. A. Meyer.
研究领域:
药理学
·
植物化学
✓ 已验证
产品关联
DOI
高影响因子
Journal of Macromolecular Science Part A-Pure and Applied Chemistry
·
2023
·
IF 2.5
Yunxin Zhang,Jiange Liu
Current clinical therapies for invasive breast cancer have low therapeutic effectiveness and substantial systemic adverse effects, leading to poor patient compliance. In this investigation, we developed dual anticancer drugs (sorafenib (SFB) and kaempferol (KMF)) encapsulated in PEGylated gold nanomaterial (PEG-AuNPs@SFB/KMF) for a drug delivery system targeting breast cancer to circumvent this problem. Subsequent research examined whether pH affects drug release. The current study results show that sorafenib and kaempferol work better together than each treatment individually in eliciting cytotoxic effects. In vitro cytotoxicity studies confirmed that PEG-AuNPs@SFB/KMF were more effective than sorafenib alone in MCF-7 and MDA-MB-231 cells, with less toxicity in NIH3T3 cells. The cancer cell proliferation was measured by Click-iT EdU assay, which indicates that the NPs effectively induce apoptosis in cancer cells. The different biochemical staining (acridine orange and ethidium bromide (AO-EB and nuclear staining (DAPI)) methods confirmed the morphological investigation of the cells. PEG-AuNPs@SFB/KMF increased apoptosis ratio, confirmed by flow cytometric analysis via Annexin V-FITC/PI staining methods. Therefore, we believe that the built multifunctional nanocarrier based on developed nanoparticle delivery could be an alternative therapeutic strategy for breast cancer therapy.
研究领域:
纳米医学
·
药学
·
肿瘤学
·
药物递送系统
·
生物化学
✓ 已验证
DOI
高影响因子
JOURNAL OF CONTROLLED RELEASE
·
2017
·
IF 7.786
Songzhi Xie,Long Zhao,Xiaojie Song,Maosheng Tang,Chuanfei Mo,Xiaohong Li
The use of bacteria as drug carriers meets several challenges, such as biocompatibility, motility deterioration after drug loading and lack of in vivo verification. Escherichia coli Nissle 1917 (EcN) is one of the best studied probiotic strains, and doxorubicin (DOX) is conjugated onto EcN in the current study via acid-labile linkers of cis -aconitic anhydride (EcN-ca-Dox), realizing the bacteria-directed accumulation and acid-responsive release of anticancer drugs in tumors. The drug conjugation has maintained the bacterial motion profiles of over 9 μm/s and cell viability of over 70%. After 3 h and 3 days of intravenous injection of EcN-ca-Dox, DOX accumulations in tumors are determined as 12.9% and 6.4% of the injected doses per gram of tissue, respectively, which are much higher than the commonly used nanocarriers . Compared with free DOX and DOX-conjugated EcN via stable linkers of succinic anhydride , the EcN-ca-Dox treatment improves the antitumor efficacy with respect to the tumor growth inhibition, prolongation of animal survivals, and apoptosis induction of tumor cells. In addition, EcN has been cleaned off from tumors and other tissues after antimicrobial treatment. Thus, the acid-labile EcN conjugates provide a safe and concise strategy to enhance the temporal and spatial controllability of anticancer drugs.
研究领域:
药理学
·
肿瘤学
·
生物技术
·
药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Frontiers in Oncology
·
2022
·
IF 5.738
Li Tian,Zhou An-Di,Bai Li-Fei,Zhang Xiao-Yang,Zhou Yu-Ting,Yang Hai-Li,Xu Le-Tian,Guo Xin-Qin,Zhu Xi-Yu,Wang Dong-Jin,Gu Hong-Wei,Wang Xiao-Ming
Cancer is one of the most serious diseases threatening human health, so it is particularly important to develop effective tumor-targeting drugs. As the first CDK4/6 inhibitor, palbociclib effectively inhibits tumor proliferation by blocking the cell cycle to the G1 phase. 10-HCPT is a Topo I inhibitor; however, its clinical application has been greatly limited due to its high toxicity. Based on the successful development of double target inhibitors, three novel palbociclib derivatives (HP-1, HP-2, and HP-3) were designed and synthesized from Palbociclib and 10-HCPT, and their biological activities were investigated. At first, the possible binding sites of the three compounds to Topo I and CDK4/6 were predicted by molecular docking. Then, we evaluated the anti-proliferative effects of the three palbociclib derivatives. In general, human lung cancer cells were more sensitive to HP-1, HP-2, and HP-3, especially NCI-H460. In addition, cell cycle arrest and apoptosis induction were investigated by flow cytometry. The three palbociclib derivatives, especially HP-1, had obvious cell cycle arrest phenomenon on NCI-H460 cells and induced apoptosis of NCI-H460 cells significantly. In the end, it was proved that these three drugs had obvious cyclin-dependent kinase inhibitory activities. In short, all the data showed that HP-1, HP-2, and HP-3 could play anti-cancer roles by acting on dual targets and had the characteristics of high efficiencies and low toxicities, which opened up a new idea for the study of palbociclib derivatives.
研究领域:
肿瘤学
·
药物化学
·
药物设计
✓ 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
International Journal of Nanomedicine
·
2018
·
IF 4.37
Xin Jin,Qing Yang,Ning Cai
Introduction Ginsenoside compound K (CK) has effects on cell-cycle regulation, tumor growth inhibition, and apoptosis induction. However, it has limited applications in clinical settings because of its low solubility and poor absorption. Methods To overcome these limitations, we aimed to develop a mixed micellar system composed of phosphatidylcholine (PC) and 1,2-distearoyl-sn-glycero-3-phosphoethanolamine polyethylene glycol 2000 (DSPE PEG 2000; DP). CK encapsulated in PC/DP mixed micelles had enhanced solubility, permeability, and retention effects. Results Compared to free CK, the CK PC/DP micellar system exhibited improved anticancer effects in vitro, including cell-cycle arrest, apoptosis, and anti-invasion in human lung carcinoma A549 cells. The significant proapoptotic effect was reflected by increased chromosomal condensation, annexin V/propidium iodide staining, and related protein expression. In vitro cellular uptake and optical mouse imaging in vivo suggested that the improved antitumor effect was caused primarily by enhanced uptake and tumor targeting. Furthermore, an in vivo antitumor efficacy study indicated that the CK mixed micelles significantly inhibited tumor growth, thereby decreasing tumor volume at the end of the experiment as compared with that in the control mice. Histological analysis confirmed the antitumor effect with low toxicity. Conclusion The PC/DP micellar system was an effective drug delivery system for CK in tumor therapy.
研究领域:
药学
·
肿瘤学
·
药物递送系统
·
药理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Nanoscale
·
2020
·Vol. 12
·期 7
·4473-4490
·
IF 6.895
Jinmao Zou,Shangxiang Chen,Yaqing Li,Linjuan Zeng,Guoda Lian,Jiajia Li,Shaojie Chen,Kaihong Huang,Yinting Chen
Precise diagnosis and effective treatment are crucial to the prognosis of pancreatic ductal adenocarcinoma (PDAC). Magnetic iron oxide nanoparticles (IONPs) are superior magnetic resonance imaging (MRI) contrast agents, while antibodies are significant immunotherapy reagents. Herein, we firstly generated a novel nanocomposite combining triple single chain antibodies (scAbs) and IONPs for the detection and treatment of PDAC. Methods: Triple scAbs (scAbMUC4, scAbCEACAM6, scFvCD44v6, MCC triple scAbs) were conjugated to the surface of polyethylene glycol modified IONPs (IONPs-PEG), forming the IONPs-PEG-MCC triple scAbs nanocomposite. Characterization of the nanocomposite was performed, and its cytotoxicity, specificity, and apoptosis induction were evaluated. In vivo MRI study and anti-pancreatic cancer effect assessment were performed in tumor-bearing nude mice. Results: The size of the IONPs-PEG-MCC triple scAbs nanocomposite was about 23.6 nm. The nanocomposite was non-toxic to normal pancreatic ductal epithelial cells, and could specifically bind to and be internalized by MUC4/CEACAM6/CD44v6-expressing PDAC cells. With an r2 relaxivity of 104.2 mM−1 s−1, the IONPs-PEG-MCC triple scAbs nanocomposite could significantly shorten the MRI T2-weighted signal intensity both in vitro and in vivo. The IONPs-PEG-MCC triple scAbs nanocomposite also showed a favorable anti-pancreatic cancer effect. Conclusion: In the present study, the IONPs-PEG-MCC triple scAbs nanocomposite was firstly confirmed as a bi-functional nanocomposite in both MRI and treatment, providing its critical clinical transformation potential in PDAC detection and treatment.
研究领域:
纳米技术
·
医学影像
·
肿瘤学
·
生物医学工程
·
药学
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）