Fluorination as tool to improve bioanalytical sensitivity and COX-2-selective antitumor activity of cobalt alkyne complexes

2019 ◽  
Vol 48 (42) ◽  
pp. 15856-15868 ◽  
Author(s):  
Daniel Baecker ◽  
Victoria Obermoser ◽  
Elisabeth Anna Kirchner ◽  
Andrea Hupfauf ◽  
Brigitte Kircher ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cox 2 ◽  
Alkyne Complexes

Fluorination of the lead Co-ASS yielded antitumor active cobalt alkyne complexes that exhibited both improved COX-2 selectivity and better bioanalytical sensitivity.

scholarly journals Chlorinated cobalt alkyne complexes derived from acetylsalicylic acid as new specific antitumor agents

2018 ◽  
Vol 47 (12) ◽  
pp. 4341-4351 ◽  
Author(s):  
Victoria Obermoser ◽  
Daniel Baecker ◽  
Carina Schuster ◽  
Valentin Braun ◽  
Brigitte Kircher ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Tumor Cell Lines ◽  
Growth Inhibitory ◽  
Cox 2 ◽  
Alkyne Complexes ◽  
Inhibitory Potential ◽  
Cox 2 Inhibitors ◽  
Ht 29 ◽  
Cox 1 ◽  
Mcf 7

Chlorine-substituted [(prop-2-ynyl)-2-acetoxybenzoate]dicobalthexacarbonyl complexes are selective COX-2 inhibitors with growth-inhibitory potential against COX-1/2 containing MDA-MB-231 and HT-29 tumor cell lines. The metabolic activity of non-tumorigenic HS-5 cells and COX-1/2-independent MCF-7 cells is not influenced.

Increasing doxorubicin antitumor activity through COX-2 inhibition without increasing cardiotoxicity

2008 ◽  
Vol 6 (9) ◽  
pp. 31
Author(s):  
F. Bianchi ◽  
M. Campiglio ◽  
M. Sasso ◽  
C. Ghirelli ◽  
E. Tagliabue ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cox 2

scholarly journals COX-2 silencing enhances tamoxifen antitumor activity in breast cancer in vivo and in vitro

2014 ◽  
Vol 44 (4) ◽  
pp. 1385-1393 ◽  
Author(s):  
YE DU ◽  
AIPING SHI ◽  
BING HAN ◽  
SIJIE LI ◽  
DI WU ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Antitumor Activity ◽  
Cox 2

scholarly journals Antitumor Activities of Ethyl Acetate Extracts fromSelaginella doederleiniiHieronIn VitroandIn Vivoand Its Possible Mechanism

2015 ◽  
Vol 2015 ◽  
pp. 1-9
Author(s):  
Jia-zhi Wang ◽  
Juan Li ◽  
Ping Zhao ◽  
Wen-tao Ma ◽  
Xie-he Feng ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Ethyl Acetate ◽  
Cell Apoptosis ◽  
Mrna Level ◽  
Pcr Analysis ◽  
Antitumor Activities ◽  
Cox 2 ◽  
Ethyl Acetate Extracts

The antitumor activities of ethyl acetate extracts fromSelaginella doederleiniiHieron (SD extracts)in vitroandin vivoand its possible mechanism were investigated. HPLC method was developed for chemical analysis. SD extracts were submitted to 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay on different cells, flow cytometry, and RT-PCR analysis using HepG2 cell and antitumor activityin vivousing H-22 xenograft tumor mice. Six biflavonoids from SD extracts were submitted to molecular docking assay. The results showed that SD extracts had considerable antitumor activityin vitroandin vivowithout obvious toxicity on normal cells and could induce cell apoptosis. The mechanisms of tumorigenesis and cell apoptosis induced by SD extracts may be associated with decreasing the ratio of bcl-2 and bax mRNA level, activating caspase-3, suppressing survivin, and decreasing the gene expression of COX-2, 5-LOX, FLAP, and 12-LOX mRNA. The main active component in SD extracts is biflavonoids and some exhibited strong interactions with COX-2, 5-LOX, 12-LOX, and 15-LOX. These results offering evidence of possible mechanisms of SD extracts suppress cell proliferation and promote apoptosis and provide the molecular theoretical basis of clinical application ofS. doederleiniifor cancer therapy.

scholarly journals Targeting of the COX-2/PGE2 axis enhances the antitumor activity of T7 peptide in vitro and in vivo

Drug Delivery ◽  
2021 ◽  
Vol 28 (1) ◽  
pp. 844-855
Author(s):  
Jianrong Yang ◽  
Jingtao Zhong ◽  
Mi Zhou ◽  
Yinghong Zhou ◽  
Peng Xiu ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cox 2

Preclinical antitumor activity and mechanisms of action of apricoxib, a clinical COX-2 inhibitor.

2011 ◽  
Vol 29 (4_suppl) ◽  
pp. 543-543
Author(s):  
F. Burrows
Keyword(s):  
Antitumor Activity ◽  
Tumor Cell ◽  
Single Agent ◽  
Human Tumor ◽  
Mechanisms Of Action ◽  
Phase Ii Trials ◽  
Post Dose ◽  
Drug Concentrations ◽  
Cox 2

543 Background: Apricoxib, a selective COX-2 inhibitor, is currently in phase II trials, but its anticancer mechanisms of action could be better defined. Apricoxib inhibits COX-2 enzymatic activity and suppresses production of PGE2 and VEGF at low nanomolar concentrations but also directly inhibits tumor cell proliferation and survival with 10-20μM potency. In this study we characterized the in vivo activity of apricoxib in xenograft models of lung, breast and colorectal carcinoma. Also, we examined the relationship between the PK, PD and antitumor activity and the effect of the drug on both tumor cell-autonomous functions and aspects of the tumor-host relationship in the HT29 model. Methods: Human tumor xenografts were grown in nude mice and apricoxib was given daily PO. Drug levels were quantified by LC-MS and VEGF levels by ELISA. Vessel density, apoptosis, proliferation and EMT were assessed by immunohistochemistry. Results: Apricoxib significantly retarded tumor growth in NSCLC models and also enhanced the efficacy of SOC drugs in breast and lung tumors. In the HT29 model, the drug was active at both doses tested. Drug concentrations in plasma and tumors peaked at 2-10 μM within an hour and decreased rapidly to submicromolar levels but concentrations persisted above the active concentration for inhibition of PGE2 production for >24h. This strongly indicates that apricoxib exerts its in vivo activity via blockade of COX-2-dependent PGE2 production. Plasma VEGF levels decreased to zero for 6h post-dose, but returned to baseline by 24h. CD31 and Endomucin staining revealed no drug effect on microvessel density, although the percentage of immature vessels was reduced, as determined by pericyte coverage/NG2 expression. Apoptosis was significantly increased by TUNEL in apricoxib-treated tumors. PCNA analysis revealed a decrease in proliferating cells. ECAD expression was significantly increased in treated animals, whereas ZEB1 expression was lower, suggesting that COX-2 activity also plays an important role in EMT. Conclusions: Apricoxib possesses antitumor activity as a single agent and in combination. In the HT29 model, apricoxib inhibits tumor proliferation and survival, normalizes tumor vasculature and reverses EMT. [Table: see text]

scholarly journals Correction to: Alantolactone, a natural sesquiterpene lactone, has potent antitumor activity against glioblastoma by targeting IKKβkinase activity and interrupting NF-κB/COX-2-mediated signaling cascades

2020 ◽  
Vol 39 (1) ◽  
Author(s):  
Xun Wang ◽  
Zhenlong Yu ◽  
Chao Wang ◽  
Wei Cheng ◽  
Xiangge Tian ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Sesquiterpene Lactone ◽  
Signaling Cascades ◽  
Cox 2

An amendment to this paper has been published and can be accessed via the original article.

scholarly journals Antitumor activity of the MEK inhibitor trametinib on intestinal polyp formation in Apc Δ716 mice involves stromal COX ‐2

2015 ◽  
Vol 106 (6) ◽  
pp. 692-699 ◽  
Author(s):  
Teruaki Fujishita ◽  
Rie Kajino‐Sakamoto ◽  
Yasushi Kojima ◽  
Makoto Mark Taketo ◽  
Masahiro Aoki
Keyword(s):  
Antitumor Activity ◽  
Mek Inhibitor ◽  
Polyp Formation ◽  
Intestinal Polyp ◽  
Cox 2

scholarly journals Curcumin potentiates the potent antitumor activity of ACNU against glioblastoma by suppressing the PI3K/AKT and NF-κB/COX-2 signaling pathways

2017 ◽  
Vol Volume 10 ◽  
pp. 5471-5482 ◽  
Author(s):  
Jun Zhao ◽  
Jiabin Zhu ◽  
Xiaoshu Lv ◽  
Jinshan Xing ◽  
Shuang Liu ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Signaling Pathways ◽  
Nf Kappa B ◽  
Cox 2
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