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C Haanen
Current opinion in investigational drugs (London, England : 2000), 2(5), 677-683 (2001-09-25)
It has been repeatedly observed that non-steroidal anti-inflammatory drugs, in particular sulindac and derivatives, may effectively prevent colorectal cancer. It has become apparent that exisulind (sulindac sulfone) induces apoptosis in tumor cells. Cell biological studies provided circumstantial evidence that the...
M T Taylor et al.
Cancer research, 60(23), 6607-6610 (2000-12-16)
Both the sulfide and sulfone metabolites of sulindac, a nonsteroidal anti-inflammatory drug, display anticarcinogenic effects in experimental models. Sulindac sulfide inhibits cyclooxygenase (COX) enzyme activities and has been reported to suppress ras-dependent signaling. However, the mechanisms by which sulindac sulfone...
The developmental toxicity of indomethacin and sulindac.
A Lione et al.
Reproductive toxicology (Elmsford, N.Y.), 9(1), 7-20 (1995-01-01)
Jason L Liggett et al.
Biochimica et biophysica acta, 1840(1), 322-331 (2013-10-02)
Nonsteroidal anti-inflammatory drugs (NSAIDs) are well known for treating inflammatory disease and have been reported to have anti-tumorigenic effects. Their mechanisms are not fully understood, but both cyclooxygenase (COX) dependent and independent pathways are involved. Our goal was to shed...
Konstantinos Katoumas et al.
Cancer prevention research (Philadelphia, Pa.), 8(7), 642-649 (2015-05-06)
The antineoplastic properties of the NSAID sulindac have long been studied. The purpose of this study was to explore sulindac's in vivo effects on oral squamous cell carcinoma (SCC) oncogenesis using the hamster cheek pouch oral carcinogenesis model (HOCM). Thirty...
Paul J Limburg et al.
Lung cancer (Amsterdam, Netherlands), 79(3), 254-261 (2012-12-25)
Sulindac represents a promising candidate agent for lung cancer chemoprevention, but clinical trial data have not been previously reported. We conducted a randomized, phase II chemoprevention trial involving current or former cigarette smokers (≥30 pack-years) utilizing the multi-center, inter-disciplinary infrastructure...
L Saso et al.
Archives of pharmacal research, 24(2), 150-158 (2001-05-08)
The activity of nonsteroidal antiinflammatory drugs (NSAIDs) in rheumatoid arthritis is not only due to the inhibition of the production of prostaglandins, which can even have beneficial immunosuppressive effects in chronic inflammatory processes. Since we speculated that these drugs could...
Jigar Pravinchandra Modi et al.
Brain research, 1576, 91-99 (2014-06-27)
The present study analyzed whether administration of sulindac, a non-steroidal anti-inflammatory drug (NSAID) would prevent, attenuate or repair ischemia induced brain injury and reverse functional impairment in a focal ischemia model of stroke. Male Sprague-Dawley rats (weight 250-300 g) were...
Shigeru Tatebe et al.
Biochemical and biophysical research communications, 290(5), 1427-1433 (2002-02-01)
Nonsteroidal anti-inflammatory drugs (NSAIDs) have been demonstrated to suppress colorectal tumorigenesis. NSAIDs have also been used to treat inflammatory illnesses. However, the underlying mechanisms of action by NSAIDs have not been completely elucidated. In this study, we reported that among...
Zhichao Liu et al.
PLoS computational biology, 7(12), e1002310-e1002310 (2011-12-24)
Drug-induced liver injury (DILI) is a significant concern in drug development due to the poor concordance between preclinical and clinical findings of liver toxicity. We hypothesized that the DILI types (hepatotoxic side effects) seen in the clinic can be translated...
Stephen P Fink et al.
Carcinogenesis, 36(2), 291-298 (2014-12-17)
Non-steroidal anti-inflammatory drugs prevent colorectal cancer by inhibiting cyclooxygenase (COX) enzymes that synthesize tumor-promoting prostaglandins. 15-hydroxyprostaglandin dehydrogenase (15-PGDH) is a tumor suppressor that degrades tumor-promoting prostaglandins. Murine knockout of 15-PGDH increases susceptibility to azoxymethane-induced colon tumors. It also renders these...
Wan-Ling Liu et al.
Journal of chromatography. A, 1395, 32-40 (2015-04-15)
In this study, an organic polymer monolithic columns, which were prepared via in situ polymerization of alkyl methacrylate-ester (AMA), divinylbenzene (DVB) and vinylbenzyl trimethylammonium chloride (VBTA, charged monomer), were developed as adsorbent for solid-phase microextraction (SPME). Different parameters affecting the...
Stephen X Skapek et al.
Pediatric blood & cancer, 60(7), 1108-1112 (2013-01-03)
Desmoid fibromatosis (desmoid tumor, DT) is a soft tissue neoplasm prone to recurrence despite complete surgical resection. Numerous small retrospective reports suggest that non-cytotoxic chemotherapy using tamoxifen and sulindac may be effective for DT. We evaluated the safety and efficacy...
F M Giardiello
Cancer metastasis reviews, 13(3-4), 279-283 (1994-12-01)
Sulindac is useful in regression of adenomatous polyps. In addition to orally administered sulindac, rectal preparations also appear to be efficacious [32]. However, further studies are necessary to determine whether regression of adenomas, the precursor of colorectal cancer, will cause...
S Flis et al.
Anticancer research, 26(4B), 3033-3041 (2006-08-05)
The development of colon cancer is probably angiogenesis-dependent. Recently, sulindac sulfide was shown to possess anti-angiogenic activity. In the present work, the question of whether this activity reflects a specific interaction with angiogenesis or is secondary to the effect of...
Xue Zhou et al.
Journal of cellular and molecular medicine, 19(5), 1103-1113 (2015-02-24)
Pulmonary fibrosis (PF) is a disease with an unknown cause and a poor prognosis. In this study, we aimed to explore the pathogenesis of PF and the mechanism of sulindac in attenuating bleomycin (BLM)-induced PF. The rat PF model was...
Mohanad Zbidah et al.
Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology, 30(4), 1072-1082 (2012-12-04)
Sulindac sulfide, a non-steroidal anti-inflammatory drug (NSAID), stimulates apoptosis of tumor cells and is thus effective against malignancy. In analogy to apoptosis of nucleated cells, erythrocytes may undergo eryptosis, an apoptosis-like suicidal erythrocyte death, characterized by cell shrinkage and cell...
D E Duggan
Drug metabolism reviews, 12(2), 325-337 (1981-01-01)
Sulindac is a prodrug which, following absorption, rapidly attains a metabolic equilibrium with its active pharmacophore, the sulfide metabolite. At the level of the whole body, the reversible interconversion sulindac in equilibrium sulfide, and the differing distributional and excretory properties...
[Sulindac--drug therapy for familial adenomatous polyposis?].
J Zundler et al.
Medizinische Klinik (Munich, Germany : 1983), 88(1), 35-38 (1993-01-15)
W R Waddell
Clinical science (London, England : 1979), 95(3), 385-388 (1998-09-09)
1.Sulindac, cis-5-fluoro-2-methyl-1-(p-methylsulphinylbenzylidene)indene-3-ace tic acid, inhibits growth of colon polyps and cancers. This effect has been attributed to inhibition of prostaglandin synthesis but more recent observations indicate that, in vitro, cells that do not have cyclo-oxygenase nor RNA for synthesis of...
Howard S Moskowitz et al.
Oral oncology, 48(11), 1136-1145 (2012-06-27)
Targeting the epidermal growth factor receptor (EGFR) using the tyrosine kinase inhibitor (TKI) erlotinib has demonstrated activity in aerodigestive tract malignancies. Co-targeting of the G-protein-coupled receptor cyclooxygenase (COX) with EGFR inhibitors has shown promise in preclinical models and early phase...
David W Greening et al.
Biochimica et biophysica acta, 1834(11), 2293-2307 (2013-08-01)
Colorectal cancer (CRC) is a major cause of mortality in Western populations. Growing evidence from human and rodent studies indicate that nonsteroidal anti-inflammatory drugs (NSAIDs) cause regression of existing colon tumors and act as effective chemopreventive agents in sporadic colon...
Stefano Fogli et al.
European journal of medicinal chemistry, 45(11), 5100-5107 (2010-08-31)
The non-steroidal anti-inflammatory drug (NSAID) sulindac exhibits cyclooxygenase (COX)-dependent and COX-independent chemopreventive properties in human cancer. The present study was aimed at investigating whether the hydroxamic acid substitution for the carboxylic acid group could enhance the in vitro antitumor and...
Sandeep C Chaudhary et al.
Toxicology and applied pharmacology, 268(3), 249-255 (2013-01-01)
Nitric oxide (NO)-releasing non-steroidal anti-inflammatory drugs (NO-NSAIDs) which have been synthesized to reduce gastro-intestinal and cardiovascular toxicities of NSAIDs, possess anti-proliferative, pro-apoptotic and anti-cancer activities. Here, we show that NO-sulindac inhibited UVB-induced skin tumorigenesis in SKH-1 hairless mice. Topical application...
Haonan Li et al.
Carcinogenesis, 34(9), 2090-2098 (2013-05-22)
Sulindac has been identified as a competitive inhibitor of aldo-keto reductase 1B10 (AKR1B10), an enzyme that plays a key role in carcinogenesis. AKR1B10 is overexpressed in pancreatic ductal adenocarcinoma (PDAC) and exhibits lipid substrate specificity, especially for farnesyl and geranylgeranyl....
Nathaniel S Rial et al.
Expert review of gastroenterology & hepatology, 6(4), 507-517 (2012-08-30)
To reduce the morbidity and mortality from colorectal cancer (CRC), current clinical practice focuses on screening for early detection and polypectomy as a form of secondary prevention, complemented with surgical interventions when appropriate. No pharmaceutical agent is currently approved for...
[A case of sulindac induced acute pancreatitis].
M Uchihara et al.
Nihon Shokakibyo Gakkai zasshi = The Japanese journal of gastro-enterology, 89(9), 2073-2076 (1992-09-01)
Jenny M Pedersen et al.
Journal of medicinal chemistry, 51(11), 3275-3287 (2008-05-07)
The chemical space of registered oral drugs was explored for inhibitors of the human multidrug-resistance associated protein 2 (MRP2; ABCC2), using a data set of 191 structurally diverse drugs and drug-like compounds. The data set included a new reference set...
Jason L Liggett et al.
Cancer letters, 346(2), 217-224 (2014-02-04)
Non-steroidal anti-inflammatory drugs (NSAIDs) are used extensively for analgesic and antipyretic treatments. In addition, NSAIDs reduce the risk and mortality to several cancers. Their mechanisms in anti-tumorigenesis are not fully understood, but both cyclooxygenase (COX)-dependent and -independent pathways play a...
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