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排序方式: 共有126条查询结果,搜索用时 171 毫秒
1.
Since researchers began studying the mechanism of flavonoids’ anticancer activity, little attention has been focused on the modulation of redox state in cells as a potential chemotherapeutic strategy. However, recent studies have begun identifying that the anticancer effect of flavonoids occurs both in their antioxidative activity which scavenges ROS and their prooxidative activity which generates ROS. Against this backdrop, this study attempts to achieve a comprehensive analysis of the individual and separate study findings regarding flavonoids’ modulation of redox state in cancer cells. It focuses on the mechanism behind the anticancer effect, and mostly on the modulation of redox potential by flavonoids such as quercetin, hesperetin, apigenin, genistein, epigallocatechin-3-gallate (EGCG), luteolin and kaempferol in both in vitro and animal models. In addition, the clinical applications of and bioavailability of flavonoids were reviewed to help build a treatment strategy based on flavonoids’ prooxidative potential. 相似文献
2.
Valeria Ciaffaglione Prof. Maria N. Modica Prof. Valeria Pittalà Prof. Giuseppe Romeo Prof. Loredana Salerno Dr. Sebastiano Intagliata 《ChemMedChem》2021,16(23):3496-3512
The development of potent antitumor agents with a low toxicological profile against healthy cells is still one of the greatest challenges facing medicinal chemistry. In this context, the “mutual prodrug” approach has emerged as a potential tool to overcome undesirable physicochemical features and mitigate the side effects of approved drugs. Among broad-spectrum chemotherapeutics available for clinical use today, 5-fluorouracil (5-FU) is one of the most representative, also included in the World Health Organization model list of essential medicines. Unfortunately, severe side effects and drug resistance phenomena are still the primary limits and drawbacks in its clinical use. This review describes the progress made over the last ten years in developing 5-FU-based mutual prodrugs to improve the therapeutic profile and achieve targeted delivery to cancer tissues. 相似文献
3.
The physical sorption of a series of cyclophosphamide drug derivatives with formula where x = 2, X = F (2), Cl (3), Br (4); x = 3, X = F (5), Cl (6), Br (7) and x = 4, X = F (8), Cl (9), Br (10) on the surface of fullerene C60 was studied using density functional theory (DFT) at B3LYP and B3PW91 levels. The most negative binding energies obtained using the B3LYP approach and corrected for geometrical BSSE and dispersion energies (gCP-D3-ΔEbinding) were measured for compounds 8 (among isolated drugs) and 13 (among complexes). The dipole moments of isolated drugs were obtained close to those of their complexes with C60 (∼4.0–5.5 Debye) indicating their hydrophililic nature that is an appropriate property appealing for drug delivery in biological media. The adsorption of all drugs on the surface of fullerene was endergonic with all of the ΔGadsorption > 0. The ΔHadsorption values at B3PW91 level were only negative for complexes 14–16 indicating their exothermic adsorption nature. The HOMO–LUMO band gaps of complexes 11–19 were about 2.7 eV and are comparable with the gap in C60 but are much smaller than the gaps in isolated drugs 2–10 (6.5–8.0 eV) reflecting the increase in electrical conductivities upon complexation. The QTAIM data supported the covalent character of the C–O, C–N and N–H bonds, the intermediate character of PO, P–O and P–N bonds while the electrostatic nature of PO…C(fullerene) interactions. According to the gCP-D3-ΔEbinding binding energies and ΔHadsorption values at B3LYP level, it seems that the complexes 12 and 13 can be the most promising prodrug + carrier delivery systems.
Graphical abstract
4.
Tea Kulisic-Bilusic Ingrid SchmöllerKerstin Schnäbele Laura SiracusaGiuseppe Ruberto 《Food chemistry》2012,132(1):261-267
The present study assessed the influence of essential oil and aqueous infusion from wild-grown caper (Capparis spinosa L.) on cell growth, NF-κB activation, apoptosis and cell cycle in the human colon carcinoma cell line, HT-29. Methyl isothiocyanate (92.06%), a degradation product of glucosinolate glucocapparin, was detected as major component of essential oil from caper leaves and flower buds. Aqueous infusion of caper showed an interesting and variegate compositional pattern containing several phenolic compounds, among which a flavonol glycoside, rutin (quercetin 3-O-rutinoside, 50.7%) and 5-caffeoyl-quinic acid (chlorogenic acid, 17.5%) were detected as dominant. Caper essential oil and aqueous infusion showed time- and dose-dependent high inhibitory effect on HT-29 cell proliferation. In addition, they induced the inhibition on nuclear factor κB (NF-κB) activity in a dose-dependent manner, while they did not show any effect on apoptosis in HT-29 cells. Flow cytometric analysis indicated that treatment with caper essential oil and aqueous infusion resulted in G2/M cell cycle arrest in a dose-dependent manner. Presented results suggest that caper contains volatile and non-volatile compounds which potentially can play an important role in colon cancer prevention. 相似文献
5.
Crispin R. Dass 《Drug development and industrial pharmacy》2013,39(1):1-5
ABSTRACTDeoxyribozymes (DNAzymes) are DNA residue-based molecules capable of specific cleavage of complementary mRNA. As such, they are more stable counterparts for the earlier discovered ribozymes. A handful of studies have shown the potential of DNAzymes against cancer both in cell culture and importantly in vivo models. This relatively new molecular entity may progress to clinical trials provided that more extensive testing is carried out at the preclinical stage. While a significant amount of work has gone into chemically stabilizing the molecule, delivery is one area that needs particular attention. 相似文献
6.
Ana López Tarek El-Naggar Montserrat Dueñas Teresa Ortega Isabel Estrella Teresa Hernández Mª Pilar Gómez-Serranillos Olga Mª Palomino Mª Emilia Carretero 《Food chemistry》2013
Legumes are the base´s diet in several countries. They hold a high nutritional value, but other properties related to human health are nowadays being studied. The aim of this work was to study the influence of processes (boiling or germination) on the phenolic composition of dark beans (Phaseolus vulgaris L. c.v. Tolosana) and their effect on their antioxidant, neuroprotective and anticancer ability. Phenolic composition of raw and processed dark beans was analysed by HPLC-PAD and HPLC–ESI/MS. The antioxidant activity was evaluated by ORAC. Astrocytes cultures (U-373) have been used to test their neuroprotective effect. Anticancer activities were evaluated on three different cell lines (renal adenocarcinoma (TK-10), breast adenocarcinoma (MCF-7) and melanoma (UACC-62)) by sulphorhodamine B method. Qualitative and quantitative differences in phenolic composition have been observed between raw and processed dark beans that influence the antioxidant activity, mainly for germinated samples which show a decrease of antioxidant capacity. Although every assayed extracts decreased reactive oxygen species release and exhibited cytotoxicity activities on cancer cell lines, raw beans proved to be the most active in neuroprotective and antitumoral effects; this sample is especially rich in phenolic compounds, mainly anthocyanins. This study further demonstrated that phenolic composition of dark beans is related with cooking process and so with their neuroprotective and anticancer activity; cooking of dark beans improves their digestion and absorption at intestinal level, while maintaining its protective ability on oxidative process at cellular level. 相似文献
7.
The objectives of the present study were to investigate anthocyanin profiles and their biological properties, including antioxidant, anticancer, and antiallergic, from the red petals of Korean edible rose (Rosa hybrida cv. Noblered). The acidic methanol extract of this species showed potent biological activities at a concentration of 50 μg/mL. Its anthocyanins were characterised as cyanidin 3,5-di-O-glucoside and pelargonidin 3,5-di-O-glucoside using reversed-phase C18 column chromatography, NMR spectroscopy, and HPLC-DAD-ESI/MS analysis. Cyanidin 3,5-di-O-glucoside was the predominant constituent (375 mg/100 g), representing about 85% of total content. Cyanidin 3,5-di-O-glucoside exhibited good scavenging activity against DPPH radical with IC50 value of 55.2 μg/mL; pelargonidin 3,5-di-O-glucoside showed potent anticancer effects against LNCap (human prostate cell line), ACHN (human renal cell line) and MOLT-4F (human leukaemia cell line) cell cultures, with IC50 values of 6.43, 18.3, and 6.78 μg/mL, respectively. Antiallergic activities were only moderate. 相似文献
8.
Squid gelatin hydrolysates with antihypertensive, anticancer and antioxidant activity 总被引:2,自引:0,他引:2
A. Alemn E. Prez-Santín S. Bordenave-Juchereau I. Arnaudin M.C. Gmez-Guilln P. Montero 《Food research international (Ottawa, Ont.)》2011,44(4):1044-1051
Gelatin obtained from giant squid (Dosidicus gigas) inner and outer tunics was hydrolyzed by seven commercial proteases (Protamex, Trypsin, Neutrase, Savinase, NS37005, Esperase and Alcalase) to produce bioactive hydrolysates. The Alcalase hydrolysate was the most potent angiotensin-converting enzyme (ACE) inhibitor (IC50 = 0.34 mg/mL) while the Esperase hydrolysate showed the highest cytotoxic effect on cancer cells, with IC50 values of 0.13 and 0.10 mg/mL for MCF-7 (human breast carcinoma) and U87 (glioma) cell lines, respectively. The radical scavenging capacity of gelatin increased approximately 3-fold for Protamex, Neutrase and NS37005 hydrolysates and between 7 and 10-fold for Trypsin, Savinase, Esperase and Alcalase hydrolysates. Trypsin, Savinase, Esperase and Alcalase hydrolysates had a metal chelating capacity above 80% whereas Protamex, Neutrase and NS37005 hydrolysates registered less than 25%. The antioxidant activity measured by FRAP (ferric ion reducing power) was largely unaffected by the enzyme used, increasing approximately 2-fold for all hydrolysates. The most active hydrolysates (Alcalase and Esperase) were comprised mostly of peptides with molecular weights ranging from 500 to 1400 Da, however, a clear relationship between bioactive properties and molecular weight distribution of all the hydrolysates was not fully established. 相似文献
9.
Hyun-Ju Kwon Sin-Yonug Bae Kwang-Hyeon Kim Chang-Hee Han Sang-Hae Cho Soo-Wan Nam Yung Hyun Choi Byung-Woo Kim 《Food chemistry》2007,104(1):196-201
Marine organisms are rich sources of new, biologically active compounds. Seaweeds have traditionally been used as food, but have also been used as folk medicine, particularly by coastal peoples. Recently, much attention has been paid to the anticancer activity of seaweed. Thus, we have screened organic extracts of seaweeds for their anticancer activity against human cell lines, and selected Corallina pilulifera as a candidate for use in treatment. The ethanolic extracts of Corallina pilulifera (EECP) showed cytotoxic activity against human cervical adenocarcinoma cell line, HeLa. The IC50 of EECP against the HeLa cells was 250 μg/ml. Treatment of HeLa cells with various concentrations of EECP resulted in growth inhibition and induction of apoptosis in a dose-dependent manner. In Western blot analysis, apoptosis in the HeLa cells was associated with the release of cytochrome C from mitochondria into the cytosol, activation of caspase-3 and caspase-8, and proteolytic cleavage of PARP (poly (ADP-ribose) polymerase). These results strongly suggest that EECP may be a potential candidate in the field of anticancer drug discovery. 相似文献
10.