scholarly journals Epigallocatechin-3-gallate suppresses the expression of HSP70 and HSP90 and exhibits anti-tumor activity in vitro and in vivo

BMC Cancer ◽  
2010 ◽  
Vol 10 (1) ◽  
Author(s):  
Phan LCHB Tran ◽  
Soo-A Kim ◽  
Hong Seok Choi ◽  
Jung-Hoon Yoon ◽  
Sang-Gun Ahn
Keyword(s):  
Author(s):  
Ya-Nan Li ◽  
Ni Ning ◽  
Lei Song ◽  
Yun Geng ◽  
Jun-Ting Fan ◽  
...  

Background: Deoxypodophyllotoxin, isolated from theTraditional Chinese Medicine Anthriscus sylvestris, is well-known because of its significant antitumor activity with strong toxicity in vitro and in vivo. Objective: In this article, we synthesized a series of deoxypodophyllotoxin derivatives, and evaluated their antitumor effectiveness.Methods:The anti tumor activity of deoxypodophyllotoxin derivatives was investigated by the MTT method. Apoptosis percentage was measured by flow cytometer analysis using Annexin-V-FITC. Results: The derivatives revealed obvious cytotoxicity in the MTT assay by decreasing the number of late cancer cells. The decrease of Bcl-2/Bax could be observed in MCF-7, HepG2, HT-29 andMG-63 using Annexin V-FITC. The ratio of Bcl-2/Bax in the administration group was decreased, which was determined by the ELISA kit. Conclusion: The derivatives of deoxypodophyllotoxin could induce apoptosis in tumor cell lines by influencing Bcl-2/Bax.


2021 ◽  
Vol 12 (5) ◽  
Author(s):  
Xuxing Shen ◽  
Chao Wu ◽  
Meng Lei ◽  
Qing Yan ◽  
Haoyang Zhang ◽  
...  

AbstractCarfilzomib, a second-generation proteasome inhibitor, has significantly improved the survival rate of multiple myeloma (MM) patients, but its clinical application is still restricted by drug resistance and cardiotoxicity. Here, we identified a novel proteasome inhibitor, D395, and assessed its efficacy in treating MM as well as its cardiotoxicity at the preclinical level. The activities of purified and intracellular proteasomes were measured to determine the effect of D395 on the proteasome. CCK-8 and flow cytometry experiments were designed to evaluate the effects of D395 on cell growth and apoptosis. The effects of D395 and carfilzomib on serum enzyme activity, echocardiography features, cardiomyocyte morphology, and hERG channels were also compared. In our study, D395 was highly cytotoxic to MM cell lines and primary MM cells but not normal cells, and it was well tolerated in vivo. Similar to carfilzomib, D395 inhibited osteoclast differentiation in a dose-dependent manner. In particular, D395 exhibited lower cardiotoxicity than carfilzomib in all experiments. In conclusion, D395 is a novel irreversible proteasome inhibitor that has remarkable anti-MM activity and mild cardiotoxicity in vitro and in vivo.


Cancers ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 1027
Author(s):  
Nishant Mohan ◽  
Xiao Luo ◽  
Yi Shen ◽  
Zachary Olson ◽  
Atul Agrawal ◽  
...  

Both EGFR and VEGFR2 frequently overexpress in TNBC and cooperate with each other in autocrine and paracrine manner to enhance tumor growth and angiogenesis. Therapeutic mAbs targeting EGFR (cetuximab) and VEGFR2 (ramucirumab) are approved by FDA for numerous cancer indications, but none of them are approved to treat breast cancers. TNBC cells secrete VEGF-A, which mediates angiogenesis on endothelial cells in a paracrine fashion, as well as promotes cancer cell growth in autocrine manner. To disrupt autocrine/paracrine loop in TNBC models in addition to mediating anti-EGFR tumor growth signaling and anti-VEGFR2 angiogenic pathway, we generated a BsAb co-targeting EGFR and VEGFR2 (designated as anti-EGFR/VEGFR2 BsAb), using publicly available sequences in which cetuximab IgG backbone is connected to the single chain variable fragment (scFv) of ramucirumab via a glycine linker. Physiochemical characterization data shows that anti-EGFR/VEGFR2 BsAb binds to both EGFR and VEGFR2 in a similar binding affinity comparable to parental antibodies. Anti-EGFR/VEGFR2 BsAb demonstrates in vitro and in vivo anti-tumor activity in TNBC models. Mechanistically, anti-EGFR/VEGFR2 BsAb not only directly inhibits both EGFR and VEGFR2 in TNBC cells but also disrupts autocrine mechanism in TNBC xenograft mouse model. Furthermore, anti-EGFR/VEGFR2 BsAb inhibits ligand-induced activation of VEGFR2 and blocks paracrine pathway mediated by VEGF secreted from TNBC cells in endothelial cells. Collectively, our novel findings demonstrate that anti-EGFR/VEGFR2 BsAb inhibits tumor growth via multiple mechanisms of action and warrants further investigation as a targeted antibody therapeutic for the treatment of TNBC.


Oncotarget ◽  
2017 ◽  
Vol 8 (43) ◽  
pp. 73766-73773 ◽  
Author(s):  
Sachiko Arai ◽  
Kenji Kita ◽  
Azusa Tanimoto ◽  
Shinji Takeuchi ◽  
Koji Fukuda ◽  
...  

Oncotarget ◽  
2017 ◽  
Vol 9 (4) ◽  
pp. 4593-4606 ◽  
Author(s):  
Ka-Wai Tam ◽  
Chi-Tang Ho ◽  
Shih-Hsin Tu ◽  
Wen-Jui Lee ◽  
Ching-Shui Huang ◽  
...  

Author(s):  
Charlemagne Gnoula ◽  
Véronique Mégalizzi ◽  
Nancy De Nève ◽  
Sébastien Sauvage ◽  
Fabrice Ribaucour ◽  
...  

Haematologica ◽  
2019 ◽  
Vol 105 (4) ◽  
pp. 1032-1041 ◽  
Author(s):  
Anna Vidal-Crespo ◽  
Alba Matas-Céspedes ◽  
Vanina Rodriguez ◽  
Cédric Rossi ◽  
Juan G. Valero ◽  
...  

RSC Advances ◽  
2019 ◽  
Vol 9 (54) ◽  
pp. 31758-31772
Author(s):  
Yiren Yang ◽  
Liping Long ◽  
Xinxin Zhang ◽  
Kairu Song ◽  
Da Wang ◽  
...  

Barrigenol-like triterpenoids (BATs) showed promising anti-tumor, anti-inflammatory and anti-Alzheimer's activities, while, the inhibitory strength was usually affected by their states with aglycones or glycosides.


Author(s):  
Nathalie Corvaia ◽  
Sven Berger ◽  
Thierry Wurch ◽  
Nicolas Boute ◽  
Matthieu Broussas ◽  
...  

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