Journal of Biomaterials and Tissue Engineering
·
2018
·Vol. 8
·期 3
·426-432
·
IF 0.781
Hu Jinghui,Wang Li,Shen Heping,Huang Yujie,Zhao Wei
The elevated expression of mammalian target of rapamycin (mTOR) is associated with the occurrence, progression, and drug resistance of various tumors. Studies have shown overexpression of mTOR and reduced expression of miR-101 in cervical cancer tissues. Bioinformatic analysis has revealed
that a targeting binding site exists between miR-101 and the 3'-UTR of mTOR mRNA. In this study we determined whether miR-101 played a role in regulating mTOR expression and influencing the proliferation, apoptosis, and drug resistance to cisplatin (DDP) of CC cells. The regulatory relationship
between miR-101 and mTOR was validated by dual-luciferase reporter gene assay. The DDP resistance cell line, CaSki/DDP, was established, and the expressions of miR-101, mTOR, p-mTOR, and p-4EBP1 in the CaSki/DDP cell line and parental CaSki cells. The effect of DDP treatment on the proliferation
and apoptosis of the two cell lines were detected by flow cytometry. CaSki/DDP cells were divided into the following four transfection groups: miR-NC group; miR-101 mimic group; si-NC group; and si-mTOR group. The expression of miR-101, MTOR, p-mTOR, and p-4EBP1 was determined, and the effect
of DDP treatment on the proliferation and apoptosis of the two cell lines we detected by flow cytometry. There was a targeted regulatory relationship between miR-101 and mTOR. The expression and apoptosis rate of miR-101 in CaSki/DDP cells were significantly lower than CaSki cells, while the
expression and proliferation of mTOR, p-mTOR, and p-4EBP1 in CaSki/DDP cells were significantly higher than CaSki cells. The transfection of miR-101 mimic or si-mTOR significantly reduced the expression of mTOR, p-mTOR, and p-4EBP1 in CaSki/DDP cells and weakened the cell proliferation ability.
DDP treatment significantly increased the apoptosis rate. The decreased expression of miR-101 is associated with CaSki/DD cell resistance to DDP. Overexpression of miR-101 can reduce the resistance of cervical cancer CaSki/DDP cells to DDP by targeted inhibition of the expression of mTOR.
研究领域:
肿瘤学
·
分子生物学
·
癌症研究
✓ 已验证
DOI
高影响因子
Frontiers in Chemistry
·
2022
·
IF 5.545
Li-Na Ke,Ling-Qi Kong,Xiu-Lian Zhu,Feng-Xu Wu,Qin-Hua Chen,Bin Li,Yun Dong,Hong-Mei Wang,Xiao-Hua Zeng
We have synthesized Rhopaladins’ analog (2E,4E)-4-chlorobenzylidene-2-(4-chlorostyryl)-N-cyclohexyl-1-(4-fluorophenyl)-5-oxopyrrolidine-2-carboxamide (RPDPRH) via a highly facile, inexpensive and green approach and verified the structural superiority of compound RPDPRH through molecular docking. Moreover, we further detected the anti-proliferation, apoptosis and HPV E6/E7 effects of RPDPRH on CaSki cells. Finally, we confirmed that compared with the previous compound (E)-N-(tert-butyl)-2-(4-chlorobenzoyl)-4-(4-fluorobenzylidene)-1-isopropyl-5-oxopyrrolidine-2-carboxamide (RPDPB), RPDPRH could better inhibit proliferation, induce apoptosis, and down-regulate HPV E6/E7 mRNA expression on Caski cells. And preliminary RT-PCR experiments have demonstrated that RPDPRH also could affect the expression of Bcl-2, Bax and Caspase-3 mRNA in Caski cells. In summary, RPDPRH has potential as an effective agent against cervical cancer and will play an important role in our subsequent research.Keywords: 4-arylidene-5-oxopyrrolidine, green synthesis, molecular docking, anti-tumor activity, apoptosis
研究领域:
化学
·
药理学
·
肿瘤学
·
分子生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
ONCOLOGY REPORTS
·
2026
·Vol. 56
·期 4
·1-12
·
IF 4.7
Seung-Hyeon Ahn,Zeeshan Ahmad Bhutta,Hwayoung Na,Hong Kyu Lee,Kyung-Chul Choi
Oncology Reports is an international journal devoted to fundamental and applied research in Oncology.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Natural Products Journal
·
2022
·Vol. 12
·期 4
·87-94
·
IF 0
Goh May P. Y.,Ahmad Norhayati,Yasin Hartini,Jama Abdalla
Background: Dillenia suffruticosa (Griff.) Mart. has been traditionally used to promote wound healing, relieve rheumatism, fever and some cancerous growths. The leaves of the local variety of D. suffruticosa lack scientific studies on its biological applications in the context of antibacterial,
antioxidant and cytotoxic activities. Objective: The objective of this study is to evaluate the antioxidant, antibacterial and cytotoxic properties of the leaves of D. suffruticosa from Brunei Darussalam. Methods: The leaves were extracted using 80% (v/v) methanol, 80% (v/v) ethanol
and aqueous. The antioxidant capacities were determined using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging and ferric ion reducing antioxidant power (FRAP) assays. The Folin-Ciocalteu and
aluminium chloride colorimetric assays were also used to evaluate the total phenolic and flavonoid contents. The antibacterial and cytotoxic activities of the extracts were determined using the Kirby-Bauer disc diffusion and MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide)
cell proliferation assays. Results: The methanolic extract of the D. suffruticosa leaves displayed the highest antioxidant activity despite having comparable phenol content when extracted using the ethanol extraction solvent. The methanolic extract also demonstrated antibacterial activity
on Staphylococcus aureus at a concentration of 50 mg/mL or above. The cytotoxicity of the methanolic extract was higher against the CaSki cell line than the A549 lung cancer cell line in the first 24 h but became more cytotoxic against A549 than CaSki at 48 h and 72 h. Conclusion: Our
findings suggest that the methanolic extract of the leaves of D. suffruticosa from Brunei Darussalam has significant antioxidant and antibacterial activity against S. aureus and moderate cytotoxicity against A549 and CaSki cell lines.
研究领域:
药理学
·
植物化学
·
肿瘤学
✓ 已验证
DOI
RSC Advances
·
2017
·Vol. 7
·期 48
·30250-30261
·
IF 3.108
Xin Liu,Yuebin Li,Jian He,Tingting Zhao,Changmei Chen,Haoshuang Gu,Xingguo Wang
A novel anticancer drug PFPSNT, paclitaxel (PTX)-loaded polymeric F127/P123 silica nanocapsules conjugated with TRAIL (tumor necrosis factor (TNF)-related apoptosis-inducing ligand), was designed and synthesized. Transmission electron microscopy (TEM), dynamic light scattering (DLS), UV-vis absorption and particle size analysis revealed that the synthesized PFPSNT was a spherical particle with a size of 24 nm and excellent colloidal stability. Drug loading efficiency (DL%) and encapsulation ratio (ER%) were 0.39% and 26.5%, and its cumulative release profile was linear. In vitro study showed that PFPSNT had marked cytotoxic and apoptotic activities towards HepG2 (liver cancer cell line) and CaSki (cervical cell line) cells with the IC50 values of 921.07 ng mL−1 and 236.24 ng mL−1, respectively. The antitumor efficacy of PFPSNT was evaluated by using a HepG2-xenografted BALB/c nu/nu mice model. In vivo study showed PFPSNT markedly inhibited HepG2 hepatocellular carcinoma, and its antitumor efficacy was more superior than those of TRAIL, PTX or PTX/F127/P123 silica nanocapsules. Our studies provided a novel strategy to synthesize anticancer nanodrugs with mutiple functions, and demonstrated that PFPSNT was a very effective anticancer drug. This novel nanodrug should be a promising drug for targeted cancer therapy to treat complex cancers.
研究领域:
药学
·
纳米技术
·
肿瘤学
·
药物递送系统
✓ 已验证
产品关联
DOI
高影响因子
JOM
·
2018
·Vol. 71
·期 1
·308-314
·
IF 2.145
Peng Xueying,Wei Lulu,Jing Xinbo,Cui Lin,Wu Jianning,Meng Guihua,Liu Zhiyong,Guo Xuhong
Herein, we exploit the unique structure, high surface area and porous structure of covalent triazine polymers (CTP) for efficient and targeted drug delivery. We have designed and synthesized a nano-covalent triazine polymer (NCTP) by using Friedel–Crafts reactions and utilized it as a drug carrier for controlled release. The salient features of as-prepared NCTP include excellent dispersibility in physiologic solution and structural stability. Furthermore, we have achieved excellent loading of doxorubicin (DOX), an anticancer drug, onto the NCTP by utilizing the π – π interactions and hydrophobic nature. The toxicity of as-prepared NCTP was assessed by CaSki and HeLa cells, and high efficacy in vitro against both types of cells has been demonstrated.
研究领域:
材料科学
·
药学
·
纳米技术
·
癌症研究
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）