ABSTRACT
The enteric nervous system (ENS) is organized into two plexuses-submucosal and myenteric-which regulate smooth muscle contraction, secretion, and blood flow along the gastrointestinal tract under the influence of the rest of the autonomic nervous system (ANS). Interstitial cells of Cajal (ICCs) are mainly located in the submucosa between the two muscle layers and at the intramuscular level. They communicate with neurons of the enteric nerve plexuses and smooth muscle fibers and generate slow waves that contribute to the control of gastrointestinal motility. They are also involved in enteric neurotransmission and exhibit mechanoreceptor activity. A close relationship appears to exist between oxidative stress and gastrointestinal diseases, in which ICCs can play a prominent role. Thus, gastrointestinal motility disorders in patients with neurological diseases may have a common ENS and central nervous system (CNS) nexus. In fact, the deleterious effects of free radicals could affect the fine interactions between ICCs and the ENS, as well as between the ENS and the CNS. In this review, we discuss possible disturbances in enteric neurotransmission and ICC function that may cause anomalous motility in the gut.
ABSTRACT
One of the most widely used strategies for drug development is the coordination of bioactive ligands to transition metals, which could improve biological activity. Moreover, the incorporation of aromatic groups to ligands may allow an enhanced lipophilicity that can influence the cellular uptake and accumulation of the metallodrugs, thus increasing their activity. Herein, we have reported the synthesis and characterization of four Pt(II) complexes [PtCl2(L)], where L = 2-(1-pyrazolyl)-2-thiazoline (PzTn), 2-(1-pyrazolyl)-1,3-thiazine (PzTz), 2-(3,5-diphenyl-1-pyrazolyl)-2-thiazoline (DPhPzTn) or 2-(3,5-diphenyl-1-pyrazolyl)-1,3-thiazine (DPhPzTz). The study was aimed at analysing their potential anticarcinogenic ability in epithelial cervix carcinoma HeLa, human promyelocytic leukemia HL-60 and human histiocytic lymphoma U-937 tumour cell lines as well as checking whether the structural factors of the organic ligand may influence their biological activity. Our findings showed that PtDPhPzTn and PtDPhPzTz were far more effective in terms of cytotoxicity than their less lipophilic counterparts (PtPzTn and PtPzTz), especially in cells derived from solid cervical tumours, thereby suggesting that modulating the lipophilicity of the ligands can help improve the cytotoxic effect of the metal complexes.
Subject(s)
Antineoplastic Agents , Cell Proliferation/drug effects , Coordination Complexes , Neoplasms , Platinum , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacokinetics , Antineoplastic Agents/pharmacology , Coordination Complexes/chemistry , Coordination Complexes/pharmacokinetics , Coordination Complexes/pharmacology , Drug Screening Assays, Antitumor , HL-60 Cells , HeLa Cells , Humans , Neoplasms/drug therapy , Neoplasms/metabolism , Platinum/chemistry , Platinum/pharmacology , U937 CellsABSTRACT
BACKGROUND: Lycopene, a bioactive red pigment, represents the most potent in vitro antioxidant among carotenoids. Virgin olive oil contains trace amounts of a wide variety of phytochemicals, which have proven to exert beneficial effects on oxidative stress. Since the ingestion of lycopene together with oil reportedly increases its bioavailability, we evaluated urinary antioxidant capacity after the consumption of a lycopene-enriched virgin olive oil (7 mg lycopene day(-1)) compared with the antioxidant effect produced after the ingestion of a virgin olive oil and a sunflower oil during 5 days, in young (25-30 years of age), middle-aged (35-55 years of age) and elderly (65-85 years of age) subjects. RESULTS: The results showed that the consumption of virgin olive oil increased urinary antioxidant capacity in middle-aged and elderly volunteers, whereas the administration of a lycopene-enriched virgin olive oil produced higher antioxidant effects in all of the three age groups assayed. CONCLUSION: The incorporation of the lycopene-enriched virgin olive oil into the diet may enhance the health-promoting effects of the virgin olive oil, contributing as a functional tool against several disorders where oxidative stress plays an important role.
