scholarly journals A rational design of a cancer-specific and lysosome-targeted fluorescence nanoprobe for glutathione imaging in living cells

2020 ◽  
Vol 1 (6) ◽  
pp. 1739-1744
Author(s):  
Hong Wang ◽  
Peisheng Zhang ◽  
Chonghua Zhang ◽  
Shu Chen ◽  
Rongjin Zeng ◽  
...  

A dual-targeting (both cancer cell- and lysosome-targeting) fluorescence nanoprobe was rational designed and synthesized for the efficient imaging of lysosomal GSH in cancer cells.

2021 ◽  
Author(s):  
Ping Zhou ◽  
Bo Liu ◽  
Mingming Luan ◽  
Na Li ◽  
Bo Tang

Cancer cell migration and invasion are initial steps for tumor metastasis that increases patient mortality. Tumor microenvironment is characterized by hypoxic and low nutrient-containing. Previous studies have suggested that hypoxia...


2017 ◽  
Vol 8 (1) ◽  
pp. 631-640 ◽  
Author(s):  
Jian-Jun Cao ◽  
Cai-Ping Tan ◽  
Mu-He Chen ◽  
Na Wu ◽  
De-Yang Yao ◽  
...  

We report a rational design and mechanism studies of mitochondria-immobilized iridium(iii) complexes that can kill cancer cells by targeting mitochondrial metabolism.


2020 ◽  
Vol 8 (28) ◽  
pp. 6013-6016
Author(s):  
Hengyan Liu ◽  
Ge Xu ◽  
Tianli Zhu ◽  
Rongchen Wang ◽  
Jiahui Tan ◽  
...  

A nanoprobe with good aqueous solubility and biocompatibility by trapping an H2S-activatable small molecule probe in the interior of surface cross-linked micelles was fabricated for imaging of H2S-rich cancer cells in a dual-color imaging modality.


2020 ◽  
Vol 7 (20) ◽  
pp. 4010-4019
Author(s):  
Nafees Muhammad ◽  
Cai-Ping Tan ◽  
Kamran Muhammad ◽  
Jie Wang ◽  
Nasreen Sadia ◽  
...  

We report the rational design and anticancer mechanism studies of novel mitochondria-targeting monofunctional Pt(ii)–lonidamine conjugates for the selective de-energization of cancer cells.


Author(s):  
Rui Tang ◽  
Yue Song ◽  
Mengzhen Shi ◽  
Zherui Jiang ◽  
Ling Zhang ◽  
...  

RSC Advances ◽  
2017 ◽  
Vol 7 (26) ◽  
pp. 15817-15822 ◽  
Author(s):  
Xuezhen Song ◽  
Baoli Dong ◽  
Xiuqi Kong ◽  
Chao Wang ◽  
Nan Zhang ◽  
...  

Hydrogen sulfide (H2S) could induce the proliferation of cancer cells in a concentration-dependent manner, and has close relation with the tumor growth.


2021 ◽  
Vol 4 (1) ◽  
Author(s):  
Lei Qi ◽  
Tonghe Pan ◽  
Liling Ou ◽  
Zhiqiang Ye ◽  
Chunlei Yu ◽  
...  

AbstractGraphene quantum dots (GQDs) are nano-sized graphene slices. With their small size, lamellar and aromatic-ring structure, GQDs tend to enter into the cell nucleus and interfere with DNA activity. Thus, GQD alone is expected to be an anticancer reagent. Herein, we developed GQDs that suppress the growth of tumor by selectively damaging the DNA of cancer cells. The amine-functionalized GQDs were modified with nucleus targeting TAT peptides (TAT-NGs) and further grafted with cancer-cell-targeting folic acid (FA) modified PEG via disulfide linkage (FAPEG-TNGs). The resulting FAPEG-TNGs exhibited good biocompatibility, nucleus uptake, and cancer cell targeting. They adsorb on DNA via the π–π and electrostatic interactions, which induce the DNA damage, the upregulation of the cell apoptosis related proteins, and the suppression of cancer cell growth, ultimately. This work presents a rational design of GQDs that induce the DNA damage to realize high therapeutic performance, leading to a distinct chemotherapy strategy for targeted tumor therapy.


2020 ◽  
Vol 6 (2) ◽  
Author(s):  
Lisni Noraida Waruwu ◽  
Maria Bintang ◽  
Bambang Pontjo Priosoeryanto

Green tea (Camellia sinensis) is one of traditional plants that have the potential as an anticancer. The sample used in this research commercial green tea extract. The purpose of this study was to test the antiproliferation activity of green tea extract on breast cancer cell MCM-B2 in vitro. Green tea extract fractionated using three solvents, ie water, ethanol 70%, and n-hexane. Extract and fraction of green tea water have value Lethality Concentration 50 (LC50) more than 1000 ppm. The fraction of ethanol 70% and n-hexane had an LC50 value of 883.48 ppm and 600.56 ppm, respectively. The results of the phytochemical screening of green tea extract are flavonoids, tannins, and saponins, while the phytochemical screening results of n-hexane fraction are flavonoids and tannins. Antiproliferation activity was tested on breast cancer cells MCM-B2 and normal cells Vero by trypan blue staining method. The highest MCM-B2 cell inhibitory activity was achieved at a concentration of 13000 ppm green tea extract and 1000 ppm of n-hexane fraction, 59% and 59%, respectively. The extract and n-hexane fraction of green tea are not toxic to normal Vero cells characterized by not inhibiting normal cell proliferation. Keywords: antiproliferative, cancer cell MCM-B2, commercial green tea, cytotoxicity


2020 ◽  
Vol 20 (23) ◽  
pp. 2070-2079
Author(s):  
Srimadhavi Ravi ◽  
Sugata Barui ◽  
Sivapriya Kirubakaran ◽  
Parul Duhan ◽  
Kaushik Bhowmik

Background: The importance of inhibiting the kinases of the DDR pathway for radiosensitizing cancer cells is well established. Cancer cells exploit these kinases for their survival, which leads to the development of resistance towards DNA damaging therapeutics. Objective: In this article, the focus is on targeting the key mediator of the DDR pathway, the ATM kinase. A new set of quinoline-3-carboxamides, as potential inhibitors of ATM, is reported. Methods: Quinoline-3-carboxamide derivatives were synthesized and cytotoxicity assay was performed to analyze the effect of molecules on different cancer cell lines like HCT116, MDA-MB-468, and MDA-MB-231. Results: Three of the synthesized compounds showed promising cytotoxicity towards a selected set of cancer cell lines. Western Blot analysis was also performed by pre-treating the cells with quercetin, a known ATM upregulator, by causing DNA double-strand breaks. SAR studies suggested the importance of the electron-donating nature of the R group for the molecule to be toxic. Finally, Western-Blot analysis confirmed the down-regulation of ATM in the cells. Additionally, the PTEN negative cell line, MDA-MB-468, was more sensitive towards the compounds in comparison with the PTEN positive cell line, MDA-MB-231. Cytotoxicity studies against 293T cells showed that the compounds were at least three times less toxic when compared with HCT116. Conclusion: In conclusion, these experiments will lay the groundwork for the evolution of potent and selective ATM inhibitors for the radio- and chemo-sensitization of cancer cells.


2018 ◽  
Vol 18 (17) ◽  
pp. 1483-1493
Author(s):  
Ricardo Imbroisi Filho ◽  
Daniel T.G. Gonzaga ◽  
Thainá M. Demaria ◽  
João G.B. Leandro ◽  
Dora C.S. Costa ◽  
...  

Background: Cancer is a major cause of death worldwide, despite many different drugs available to treat the disease. This high mortality rate is largely due to the complexity of the disease, which results from several genetic and epigenetic changes. Therefore, researchers are constantly searching for novel drugs that can target different and multiple aspects of cancer. Experimental: After a screening, we selected one novel molecule, out of ninety-four triazole derivatives, that strongly affects the viability and proliferation of the human breast cancer cell line MCF-7, with minimal effects on non-cancer cells. The drug, named DAN94, induced a dose-dependent decrease in MCF-7 cells viability, with an IC50 of 3.2 ± 0.2 µM. Additionally, DAN94 interfered with mitochondria metabolism promoting reactive oxygen species production, triggering apoptosis and arresting the cancer cells on G1/G0 phase of cell cycle, inhibiting cell proliferation. These effects are not observed when the drug was tested in the non-cancer cell line MCF10A. Using a mouse model with xenograft tumor implants, the drug preventing tumor growth presented no toxicity for the animal and without altering biochemical markers of hepatic function. Results and Conclusion: The novel drug DAN94 is selective for cancer cells, targeting the mitochondrial metabolism, which culminates in the cancer cell death. In the end, DAN94 has been shown to be a promising drug for controlling breast cancer with minimal undesirable effects.


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