Discovery of new polycyclic polyprenylated acylphloroglucinols with diverse architectures as potent cyclooxygenase-2 inhibitors

2020 ◽  
Vol 7 (11) ◽  
pp. 1349-1357 ◽  
Author(s):  
Shuangshuang Xie ◽  
Changxing Qi ◽  
Yulin Duan ◽  
Qianqian Xu ◽  
Yaping Liu ◽  
...  
Keyword(s):  
Therapeutic Target ◽  
Inflammatory Diseases ◽  
Cyclooxygenase 2 ◽  
Chronic Inflammatory Diseases ◽  
Cox 2 ◽  
Cyclooxygenase 2 Inhibitors

Cyclooxygenase-2 (COX-2) is a significant therapeutic target of chronic inflammatory diseases.

scholarly journals Impact of new cyclooxygenase 2 inhibitors on human cytomegalovirus replication in vitro

2021 ◽  
pp. 135965352110640
Author(s):  
D Andouard ◽  
R Gueye ◽  
S Hantz ◽  
C Fagnère ◽  
B Liagre ◽  
...  
Keyword(s):  
Human Cytomegalovirus ◽  
Hcmv Infection ◽  
Laboratory Strain ◽  
Cyclooxygenase 2 ◽  
Immunocompromised Patients ◽  
Toxic Compound ◽  
Cox 2 ◽  
Cyclooxygenase 2 Inhibitors ◽  
Strain Ad169

Background Human cytomegalovirus (HCMV) is involved in complications on immunocompromised patients. Current therapeutics are associated with several drawbacks, such as nephrotoxicity. Purpose: As HCMV infection affects inflammation pathways, especially prostaglandin E2 (PGE2) production via cyclooxygenase 2 enzyme (COX-2), we designed 2'-hydroxychalcone compounds to inhibit human cytomegalovirus. Study design We first selected the most efficient new synthetic chalcones for their effect against COX-2-catalyzed PGE2. Study sample Among the selected compounds, we assessed the antiviral efficacy against different HCMV strains, such as the laboratory strain AD169 and clinical strains (naïve or multi-resistant to conventional drugs) and toxicity on human cells. Results The most efficient and less toxic compound (chalcone 7) was tested against HCMV in combination with other antiviral molecules: artesunate (ART), baicalein (BAI), maribavir (MBV), ganciclovir (GCV), and quercetin (QUER) using Compusyn software. Association of chalcone 7 with MBV and BAI is synergistic, antagonistic with QUER, and additive with GCV and ART. Conclusion These results provide a promising search path for potential bitherapies against HCMV.

Seasonal Episodic Paroxysmal Hemicrania Responding to Cyclooxygenase-2 Inhibitors

Cephalalgia ◽  
2004 ◽  
Vol 24 (5) ◽  
pp. 414-415 ◽  
Author(s):  
HC Siow
Keyword(s):  
Cyclooxygenase 2 ◽  
Response To Treatment ◽  
Paroxysmal Hemicrania ◽  
Autonomic Symptoms ◽  
Chronic Paroxysmal Hemicrania ◽  
Cox 2 ◽  
Cox 2 Inhibitors ◽  
Cyclooxygenase 2 Inhibitors

Chronic paroxysmal hemicrania (CPH) was first described by Sjaastad who also described a remitting form of this condition (1, 2). This new entity was named episodic paroxysmal hemicrania (EPH) in 1987 by Kudrow (3). It is characterized by brief, frequent attacks of unilateral orbital or temporal pain with associated autonomic symptoms. Most cases respond to indomethacin. A seasonal variant of EPH has been described (4), but never a response to treatment with cyclooxygenase (COX)-2 inhibitors.

From indomethacin to a selective COX-2 inhibitor: Development of indolalkanoic acids as potent and selective cyclooxygenase-2 inhibitors

1996 ◽  
Vol 6 (6) ◽  
pp. 725-730 ◽  
Author(s):  
W.C. Black ◽  
C. Bayly ◽  
M. Belley ◽  
C.-C. Chan ◽  
S. Charleson ◽  
...  
Keyword(s):  
Cyclooxygenase 2 ◽  
Inhibitor Development ◽  
Cox 2 ◽  
Cyclooxygenase 2 Inhibitors

Dual Human Carbonic Anhydrase/Cyclooxygenase-2 Inhibitors: A Promising Approach for Cancer Treatment

2021 ◽  
Vol 21 ◽  
Author(s):  
Mohammad Mahboubi-Rabbani ◽  
Afshin Zarghi
Keyword(s):  
Carbonic Anhydrase ◽  
Combination Therapy ◽  
Active Site ◽  
Inhibitory Action ◽  
Cyclooxygenase 2 ◽  
X Ray ◽  
Cox 2 ◽  
Human Carbonic Anhydrase ◽  
Cancer Chemoresistance ◽  
Cyclooxygenase 2 Inhibitors

: Human carbonic anhydrase (hCA) and cyclooxygenase-2 (COX-2) have been known for a long to be chiefly involved in both the pathogenesis and progression of cancer and cancer chemoresistance. Interestingly, there is emerging evidence that the sulfonamide-type COX-2 selective inhibitors (coxibs) demonstrate inhibitory action against the cancer-related hCA isoforms, confirmed by X-ray crystal structures for celecoxib and valdecoxib complexes with the hCA active site. Consequently, the antineoplastic activity of the sulfonamide coxibs may be justified by the contribution of hCA inhibition to such processes in addition to COX-2 inhibition. Accordingly, these compounds' anti-tumoral activity should be further explored for their possible use in cancer prevention and combination therapy; however, few papers deal with this issue. Beginning with a brief description of the main molecular and catalytic features of both enzymes and their roles in tumor physiology, this review covers a survey of the most recent evidence regarding the molecules targeting one or both of hCA and COX-2, also providing insights into their mechanism of action and efficacy in preventing cancer.

Effect of Cyclooxygenase-2 Inhibitors on Blood Pressure

2003 ◽  
Vol 37 (3) ◽  
pp. 442-446 ◽  
Author(s):  
Deanna L Johnson ◽  
Tina M Hisel ◽  
Beth Bryles Phillips
Keyword(s):  
Blood Pressure ◽  
Cyclooxygenase 2 ◽  
Data Sources ◽  
Selective Inhibitors ◽  
Data Synthesis ◽  
Hypertensive Patients ◽  
Search Terms ◽  
Clinical Literature ◽  
Cox 2 ◽  
Cyclooxygenase 2 Inhibitors

OBJECTIVE: To evaluate the effect of cyclooxygenase-2 selective inhibitors (CSIs) on blood pressure. DATA SOURCES: Clinical literature accessed through MEDLINE (1966–May 2002). Key search terms included COX-2 selective inhibitors; anti-inflammatory agents, nonsteroidal; celecoxib; rofecoxib; and hypertension. DATA SYNTHESIS: Data from prospective studies on the effects of CSIs on blood pressure are conflicting. Several studies have reported increased blood pressure as an adverse effect of CSIs. CONCLUSIONS: Additional studies are needed to evaluate the effects of CSIs on blood pressure. CSIs should be used with caution in hypertensive patients and blood pressure monitored closely if a CSI is indicated.

Cyclooxygenase-2 (COX-2) in multiple myeloma: prognostic factor or therapeutic target?

2007 ◽  
Vol 136 (1) ◽  
pp. 163-164 ◽  
Author(s):  
Roger G. Owen ◽  
Im Fan ◽  
Sheila J. M. O'Connor ◽  
Rebecca A. Rollett ◽  
J. Anthony Child ◽  
...  
Keyword(s):  
Multiple Myeloma ◽  
Prognostic Factor ◽  
Therapeutic Target ◽  
Cyclooxygenase 2 ◽  
Cox 2

Cyclooxygenase-2 (COX-2) in Multiple Myeloma: Prognostic Marker or Therapeutic Target?.

Blood ◽  
2006 ◽  
Vol 108 (11) ◽  
pp. 5051-5051
Author(s):  
Roger G. Owen ◽  
Im Fan ◽  
Sheila J.M. O’Connor ◽  
Faith E. Davies ◽  
Rebecca A. Rollett ◽  
...  
Keyword(s):  
Multiple Myeloma ◽  
Monoclonal Antibody ◽  
Bone Marrow ◽  
Therapeutic Target ◽  
Plasma Cells ◽  
Prognostic Significance ◽  
Cyclooxygenase 2 ◽  
Lymphoid Cells ◽  
Bone Marrow Biopsies ◽  
Cox 2

Abstract Cyclooxygenase-2 (COX-2) is the key enzyme involved in prostaglandin synthesis. It appears to support the growth of a number of solid tumours including colon, breast, ovary, lung and uterine cervix and may be an important therapeutic target in at least some of these tumours. COX-2 expression has recently been evaluated (by immunohistochemistry using polyclonal anti-COX-2 antibodies) in multiple myeloma (MM) where expression was documented in 33–57% of patients. COX-2 expression in these studies was strongly associated with an adverse outcome. In addition there is some emerging data to suggest that the use of aspirin in MM may improve survival rates. In order to further evaluate this we have used a monoclonal antibody (Clone SP21, Labvision, Fremont, Ca) to assess COX-2 expression in both normal and neoplastic plasma cells. 52 specimens were assessed using standard streptavidin-biotin immunoperoxidase techniques using a known COX-2+ colon cancer as a positive control. Strong uniform COX-2 expression was seen in 32/33 (97%) of myeloma patients assessed and was also documented in all patients with MGUS (n=10). COX-2 expression was also documented in reactive plasmacytic lesions (oral mucosa, skin and lymph node, n=6) as well as normal bone marrow plasma cells (n=6). Megakaryocytes stained positively in all bone marrow biopsies examined and provided a useful positive internal control while erythroid, myeloid and lymphoid cells were consistently negative. We would conclude that COX-2 is strongly expressed by both normal and neoplastic plasma cells suggesting that COX-2 is a potential therapeutic target in MM. The apparent increase in the proportion of myeloma patients expressing COX-2 in the present study reflects the use of a monoclonal antibody in our immunohistology studies. The fact that polyclonal antibodies identify a lower proportion of patients who appear to have an inferior outcome suggests that the level of expression is of prognostic significance rather than its presence or absence. This is worthy of further study using more appropriate techniques such as RQ-PCR.

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