235 MODULATION OF ERK PHOSPHORYLATION BY GINSENG EXTRACT (GE) AFFECTS SORAFENIB SUSCEPTIBILITY IN HUMAN CANCER CELL LINES AND IN VIVO ANIMAL MODEL

2011 ◽  
Vol 54 ◽  
pp. S97-S98
Author(s):  
N.H. Lee ◽  
M.K. Kim ◽  
H.J. Park ◽  
J.S. Rho ◽  
H.Y. Woo ◽  
...  
2020 ◽  
Author(s):  
Ewen Calder ◽  
Anna Skwarska ◽  
Deborah Sneddon ◽  
Lisa Folkes ◽  
Ishna N. Mistry ◽  
...  

The design and synthesis of four hypoxia-activated prodrugs of the KDAC inhibitor panobinostat is described. Initial validation of these compounds using isolated enzymes, and in two human cancer cell lines, reveals that the nitroimidazole-based prodrug (NI-Pano, CH-03) undergoes efficient bioreduction and fragmentation to release the parent drug, panobinostat. NI-Pano was identified as the optimum compound for use in further studies in cells, spheroid tumor models, and <i>in vivo</i>.


2021 ◽  
Author(s):  
Lukas Clemens Böckelmann ◽  
Theresa Felix ◽  
Simona Calabrò ◽  
Udo Schumacher

Abstract Background YKL-40, also known as non-enzymatic chitinase-3 like-protein-1 (CHI3L1), is a glycoprotein expressed and secreted mainly by inflammatory cells and tumor cells. Accordingly, several studies demonstrated elevated YKL-40 serum levels in cancer patients and found YKL-40 to be correlated with a poor prognosis and disease severity in some tumor entities. YKL-40 was suggested to be involved in angiogenesis and extracellular matrix remodeling. As yet, however, its precise biological function remains elusive. Methods As YKL-40 protein expression has only been investigated in few malignancies, we employed immunohistochemical detection in a large multi-tumor tissue microarray consisting of 2,310 samples from 72 different tumor entities. In addition, YKL-40 protein expression was determined in primary mouse xenograft tumors derived from human cancer cell lines. Results YKL-40 could be detected in almost all cancer entities and was differently expressed depending on tumor stage and subtype (e.g., thyroid cancer, colorectal cancer, gastric cancer and ovarian cancer). While YKL-40 was absent in in vitro grown human cancer cell lines, YKL-40 expression was upregulated in xenograft tumor tissues in vivo. Conclusions These data provide new insights into YKL-40 expression at the protein level in various tumor entities and its regulation in tumor models. Our data suggest that upregulation of YKL-40 expression is a common feature in vivo and is finely regulated by tumor cell-microenvironment interactions.


Oncotarget ◽  
2016 ◽  
Vol 7 (27) ◽  
pp. 41363-41379 ◽  
Author(s):  
Kowthar Y. Salim ◽  
Saman Maleki Vareki ◽  
Wayne R. Danter ◽  
Serban San-Marina ◽  
James Koropatnick

2020 ◽  
Author(s):  
Ewen Calder ◽  
Anna Skwarska ◽  
Deborah Sneddon ◽  
Lisa Folkes ◽  
Ishna N. Mistry ◽  
...  

The design and synthesis of four hypoxia-activated prodrugs of the KDAC inhibitor panobinostat is described. Initial validation of these compounds using isolated enzymes, and in two human cancer cell lines, reveals that the nitroimidazole-based prodrug (NI-Pano, CH-03) undergoes efficient bioreduction and fragmentation to release the parent drug, panobinostat. NI-Pano was identified as the optimum compound for use in further studies in cells, spheroid tumor models, and <i>in vivo</i>.


Author(s):  
Zeenat Ayoub ◽  
Sumera Banoo Malik ◽  
Archana Mehta

Adiantum capillus-veneris, commonly known as maidenhair fern belongs to family Pteridaceae, has traditionally been used in various medicinal preparations as demulcent, expectorant, emmenagogue, diuretic etc. in the form of oil, paste, decoction and powder. It has also prominent role in hair growing and has anti-microbial, anti-inflammatory, anti-diabetic, anti-nociceptive and antioxidant properties of therapeutic interest. This study aimed to investigate the in vitro cytotoxic activity of fractions of ethanolic extract isolated from the aerial part of A. capillus-veneris against some human cancer cell lines such as colon (HCT-116), lung (A549), breast (MCF-7) and pancreatic (MIA PaCa-2) and tumor cell proliferation/inhibition was assessed using MTT assay. The in vivo anticancer activity of hexane fraction was also evaluated against murine Ehrlich ascites carcinoma (EAC) model. The results confirmed that all the fractions of ethanolic extract exhibited promising in vitro inhibition of tumor cell proliferation when tested against different human cancer cell lines. Among all, hexane fraction proved to be more effective having IC50 values 21.72, 22.67, 26.25 μg/mL, for HCT- 116, A-549, MCF-7, respectively, but chloroform fraction revealed to be more cytotoxic against Mia-PACA-2 having IC50 value 14.72 μg/mL. Higher cytotoxic activity is found to be associated with lower IC50 values. The findings showed that all five fractions exhibited dose-dependent killing capabilities in various human derived cancer cell lines at 48 h of treatment. Hexane fraction was found to inhibit tumour growth development by 16.95%, 41.12% and 82.07% at 50, 100 and 200 mg/kg body weight, respectively. Additionally, this fraction was predicted to be non-toxic at the tested doses. The findings indicate that A. capillus-veneris herb is an antineoplastic agent and suggest that further studies evaluating the isolation of active antitumor compounds from A. capillus-veneris and their mechanism(s) of action are necessary.


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