Synthesis, photophysical properties and in vitro evaluation of a chlorambucil conjugated ruthenium(ii) complex for combined chemo-photodynamic therapy against HeLa cells

2017 ◽  
Vol 5 (24) ◽  
pp. 4623-4632 ◽  
Author(s):  
Jing-Xiang Zhang ◽  
Mei Pan ◽  
Cheng-Yong Su

We designed a new heteroleptic Ru(ii) complex CHL-RuL as an imaging-guided chemotherapy/PDT agent, which shows a moderate antiproliferative effect in dark and strong photodynamic inhibitory effect against HeLa cells.

2019 ◽  
Vol 23 (11n12) ◽  
pp. 1505-1514 ◽  
Author(s):  
Xing Guo ◽  
Hao Wu ◽  
Wei Miao ◽  
Yangchun Wu ◽  
Erhong Hao ◽  
...  

Subcellular organelle-targeted photosensitizers have recently reported to be effective photodynamic therapy (PDT) agents. In this work, three porphyrin-derived photosensitizers, containing one, two or four triphenylphosphonium targeting groups, were synthesized and characterized by NMR, HRMS, UV-vis and fluorescence spectroscopy. These photosensitizers showed similar photophysical properties to classical porphyrins and exhibited excellent [Formula: see text]O[Formula: see text] quantum yields in acetonitrile. Subcellular colocalization indicated that all three photosensitizers specifically stain the mitochondria of HeLa cells. Photosensitizer mito-dp, containing two triphenylphosphonium cations was found to be the most uptaken by cells and exhibited the best PDT effect with an effective phototoxicity (IC[Formula: see text] (light) [Formula: see text] 12.4 nM), suggestive of a higher practicable potential of mitochondria-targeted PDT agents in cancer therapy.


2021 ◽  
Vol 22 (15) ◽  
pp. 8106
Author(s):  
Tianming Song ◽  
Yawei Qu ◽  
Zhe Ren ◽  
Shuang Yu ◽  
Mingjian Sun ◽  
...  

Despite the numerous available treatments for cancer, many patients succumb to side effects and reoccurrence. Zinc oxide (ZnO) quantum dots (QDs) are inexpensive inorganic nanomaterials with potential applications in photodynamic therapy. To verify the photoluminescence of ZnO QDs and determine their inhibitory effect on tumors, we synthesized and characterized ZnO QDs modified with polyvinylpyrrolidone. The photoluminescent properties and reactive oxygen species levels of these ZnO/PVP QDs were also measured. Finally, in vitro and in vivo experiments were performed to test their photodynamic therapeutic effects in SW480 cancer cells and female nude mice. Our results indicate that the ZnO QDs had good photoluminescence and exerted an obvious inhibitory effect on SW480 tumor cells. These findings illustrate the potential applications of ZnO QDs in the fields of photoluminescence and photodynamic therapy.


2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Delizhaer Reheman ◽  
Jing Zhao ◽  
Shan Guan ◽  
Guan-Cheng Xu ◽  
Yi-Jie Li ◽  
...  

Abstract Pyrazolone complexes have strong anti-tumor and antibacterial properties, but the anti-tumor mechanism of pyrazolone-based copper complexes has not been fully understood. In this study, the possible mechanism and the inhibitory effect of a novel pyrazolone-based derivative compound [Cu(PMPP-SAL)(EtOH)] on human cervical cancer cells (HeLa cells) was investigated. [Cu(PMPP-SAL)(EtOH)] effectively inhibited proliferation of HeLa cells in vitro with an IC50 value of 2.082 after treatment for 72 h. Cell cycle analysis showed apoptosis was induced by blocking the cell cycle in the S phase. [Cu(PMPP-SAL)(EtOH)] promoted the loss of mitochondrial membrane potential, release of cytochrome c, PARP cleavage, and activation of caspase-3/9 in HeLa cells. Additionally, [Cu(PMPP-SAL)(EtOH)] inhibited the PI3K/AKT pathway and activated the P38/MAPK, and JNK/MAPK pathways. [Cu(PMPP-SAL)(EtOH)] also inhibited the phosphorylation of Iκ-Bα in the NF-κB pathway activated by TNF-α, thus restricting the proliferation of HeLa cells which were activated by TNF-α. In conclusion, [Cu(PMPP-SAL)(EtOH)] inhibited the growth of HeLa cells and induced apoptosis possibly via the caspase-dependent mitochondria-mediated pathway. These results suggest that [Cu(PMPP-SAL)(EtOH)] can be a potential candidate for the treatment of cervical cancer.


2012 ◽  
Vol 22 (1) ◽  
pp. 38-42 ◽  
Author(s):  
Ningyue Gan ◽  
Gang Chen ◽  
Weijiang Zhang ◽  
Jianwei Zhou

ObjectivePlants belonging to the genus Celastrus exhibit antitumor activity and the ability to reverse multidrug resistance in tumor cells; however, it remains unclear whether the compound oleanen from Celastrus hypoleucus also exhibits antitumor activity. The objective of this study was to explore the inhibitory effect of 12-oleanene-3β, 6α-diol (oleanen) on the proliferation of cervical cancer HeLa cells in vitro, as well as its relative mechanism.MethodsHeLa cells were treated with different concentrations of oleanen for different times. Cell proliferation was determined by 3-(4,5)-dimethylthiahiazo (-z-y1)-3,5-di-phenytetrazoliumromide assay. Cell apoptosis was evaluated by flow cytometry and caspases activities assay. The expression of several proapoptotic proteins belonging to the Bcl-2 family, such as Bax, Bim, and Bad, was detected by Western blot.ResultsOleanen mainly inhibited the proliferation of HeLa cells at the G0 to G1 and G2 to M phases, and the IC50 of oleanen for cells was significantly higher at 24 hours compared to 48 hours (17.45 ± 3.71 vs 9.02 ± 0.83 μg/mL, respectively; P < 0.05). The significant increase in activity of caspase 3/7, caspase 6 in oleanen-treated HeLa cells indicated that oleanen promoted the apoptosis of HeLa cells. The activity of caspase 9 representing the endogenous apoptotic pathways also increased obviously in oleanen treatment. Furthermore, the increase in the expression of Bim was the most significant among the Bcl-2 family after oleanen treatment.ConclusionOleanen up-regulates the expression of Bim and other proapoptotic molecules to activate the endogenous apoptosis pathway, thus promoting apoptosis and inhibiting proliferation of human cervical cancer HeLa cells in vitro.


2017 ◽  
Vol 14 (11) ◽  
pp. 3789-3800 ◽  
Author(s):  
Preeti Kumari ◽  
Shreya Jain ◽  
Balaram Ghosh ◽  
Vladimir Zorin ◽  
Swati Biswas

2015 ◽  
Vol 33 (3) ◽  
pp. 776-791 ◽  
Author(s):  
Fernanda Belincanta Borghi-Pangoni ◽  
Mariana Volpato Junqueira ◽  
Sabrina Barbosa de Souza Ferreira ◽  
Larissa Lachi Silva ◽  
Bruno Ribeiro Rabello ◽  
...  

2018 ◽  
Vol 3 (2) ◽  
pp. 47-52
Author(s):  
Aditya K. Karim ◽  
Sismindari Sismindari

Dianella nemorosa Lam. was known containing alkaloids, terpenoid, phenolic compouds and tanin. Antiproliferative effect of D. nemorosa leaves methanol exctract, which demonstrated to have an in vitro cytotoxic effect on cancer cell line. The aim of research was examined the effect antiproliferative methanol extract of D. nemorosa leaves against MKN45 (gastric cancer) cell line. Leaves powder extracted using methanol. Antiproliferative effect was determined by Cell Proliferation Reagents WST-1 ((2-(4-iodophenyl)-3-(4-nitro-phenyl)-5-(2,4-disulfophenyl)-2H-tetrazolium monosodium salt). Test for 1h, 2h, and 4h after incubated for 72h was done. The result of this research showed that methanol exctract from D. nemorosa possessed remarkable no had antiproliferative activity against MKN45 cell line. The result indicated methanol extract of D. nemorosa leaves selective inhibitory effect or antiproliferative against cell line. Key words: Dianella nemorosa, Antiproliferative, MKN 45, and WST-1


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