Current Medicinal Chemistry - Volume 20, Issue 33, 2013

Salinomycin, traditionally used as an anti-coccidial drug, has recently been shown to possess anti-cancer and anti-cancer stem cell (CSC) effects, as well as activities to overcome multi-drug resistance based on studies using human cancer cell lines, xenograft mice, and in case reports involving cancer patients in pilot clinical trials. Therefore, salinomycin may be considered as a promising novel anti-cancer agent despite its largel Read More

In the past 50 years, thalidomide has undergone a remarkable metamorphosis from a notorious drug inducing birth defects into a highly effective therapy for treating leprosy and multiple myeloma. Today, most notably, thalidomide and its analogs have shown efficacy against a wide variety of diseases, including inflammation and cancer. The mechanism underlying its teratogenicity as well as its anticancer activities has been int Read More

Various epidemiological studies have demonstrated that vitamin D may play important roles in the pathogenesis and progression of cancer. Vitamin D is one of the most pivotal nutraceuticals whose active metabolite, calcitriol (1,25-dihydroxyvitamin D3), possesses anti-proliferative, pro-apoptotic, and pro-differentiating capabilities. Accumulating evidence indicates that the potential benefits of using vitamin D in cancer ar Read More

Calcitriol (1, 25-dihydroxyvitamin D3) is the most biologically active metabolite derived from the secosteroid hormone vitamin D. Apart from its calcium homeostatic effects, epidemiological studies have shown that reduced serum calcitriol levels are associated with an increased risk of some types of cancer. Numerous recent epidemiological and experimental studies have reported that it elicits anti-proliferative, apoptotic and Read More

Epidemiological and clinical studies have indicated that low vitamin D activity is not only associated with an increased cancer risk and a more aggressive tumor growth, but also connected with an aggravated liver damage caused by chronic inflammation. Meanwhile, increasing evidence has demonstrated that 1,25(OH)2D3 (the most biologically active metabolite of vitamin D) can inhibit inflammatory response in some ch Read More

Indometacin, an inhibitor of cyclooxygenase-2 (COX-2), has been shown to exert anticancer effects in a variety of cancers. However, the effect and mechanism of indometacin on high glucose (HG)-induced proliferation and invasion of pancreatic cancer (PC) cells remain unclear. Multiple lines of evidence suggest that a large portion of pancreatic cancer (PC) patients suffer from either diabetes or HG which contributing PC progres Read More

Inflammation has become a research hotspot in solid tumours and has been confirmed as a key factor in tumour development through the interactions of inflammatory mediators with gene expression, cell proliferation, and apoptosis. Pancreatic cancer (PC) is one of the most aggressive and deadliest forms of gastrointestinal cancer. A large case-control study found that aspirin, an anti-inflammatory drug, was associated Read More

To explain a bimodal pattern of hazard of relapse among early stage breast cancer patients identified in multiple databases, we proposed that late relapses result from steady stochastic progressions from single dormant malignant cells to avascular micrometastases and then on to growing deposits. However in order to explain early relapses, we had to postulate that something happens at about the time of surgery to provo Read More

Ormeloxifene is a non-steroidal Selective Estrogen Receptor Modulator (SERM) that is used as an oral contraceptive. Recent studies have shown its potent anti-cancer activities in breast, head and neck, and chronic myeloid leukemia cells. Several in vivo and clinical studies have reported that ormeloxifene possesses an excellent therapeutic index and has been well-tolerated, without any haematological, biochemical or histopa Read More

Resveratrol (trans-3,4’,5-trihydroxystilbene), a natural polyphenolic compound detected in grapes, berries, and peanuts, possesses a wide spectrum of pharmacological properties, including anti-tumor metastasis activities. However, the underlying mechanisms through which resveratrol inhibits the metastasis of pancreatic cancer are still not fully elucidated. As epithelial-to-mesenchymal transition (EMT) is a key player for metast Read More

To obtain information on anti-prostate cancer (CaP) activities of piceatannol, a metabolite biotransformed from resveratrol by cytochrome P450 CYP1B, CWR22Rv1 cells were incubated with increasing dose of piceatannol. Proliferation and apoptosis assays in exposed cells showed that piceatannol produced inhibition comparable to resveratrol. To determine whether quinone reductase 2 (NQO2) plays a role in the observ Read More