Abstract:
BACKGROUND:Obesity is characterized by increased long chain fatty acids (LCFA) uptake and impaired lipid metabolism in hepatocytes. Consequently, an enhanced intracellular lipid content, including sphingolipids, may lead to lipotoxicity. It is believed that resveratrol (RSV), one of the most extensively studied plant-derived polyphenols, and its interaction with sphingolipid metabolism may constitute one of the major therapeutic targets for cancer and metabolic diseases treatment. OBJECTIVE:The aim of this study was to ascertain, whether resveratrol may affect sphingolipid metabolic pathways, enzymes and transporters in a lipid overload state. METHODS:The experiments were conducted on hepatocellular carcinoma cells (HepG2) incubated with RSV and/or Palmitic Acid (PA) at the concentration of 0.5 mM and 50 µM, respectively for 16h. Intra- and extracellular sphingolipid concentrations were assessed by high-performance liquid chromatography and gas liquid chromatography. Moreover, the expression of caspase 3, selected fatty acid transporters and sphingolipid metabolism pathway proteins were estimated by Western Blot. RESULTS:RSV alone and together with PA significantly increased the intracellular concentration of ceramide, sphinganine and sphingosine as well as the expression of enzymes related to de novo ceramide synthesis pathway. Moreover, in our study, we observed augmented ceramide and sphingomyelin efflux into the incubation media in these groups. In addition, RSV substantially reduced intracellular triacylglycerols accumulation in lipid overload conditions. CONCLUSION:The above-mentioned findings suggest that RSV, at least partially, demonstrates a potential protective effect on HepG2 cells in a lipid overload state.
journal_name
Anticancer Agents Med Chemjournal_title
Anti-cancer agents in medicinal chemistryauthors
Charytoniuk T,Harasim-Symbor E,Polak A,Drygalski K,Berk K,Chabowski A,Konstantynowicz-Nowicka Kdoi
10.2174/1871520619666181224161255subject
Has Abstractpub_date
2019-01-01 00:00:00pages
121-129issue
1eissn
1871-5206issn
1875-5992pii
ACAMC-EPUB-95420journal_volume
19pub_type
杂志文章abstract:AIM:This study aimed to characterize the cellular basis of the platinum cytotoxicity of two novel platinum complexes, 3Pt and 1Pt, in comparison with that of cisplatin. 3Pt comprises anionic phosphate moieties, while 1Pt comprises neutral aromatic ligands. METHODS:We compared the cytotoxic potency of 3Pt and 1Pt with ...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/1871520615666141216151547
更新日期:2015-01-01 00:00:00
abstract::Breast cancer is the most common cancer among women, and ranks second among cancer deaths in women. Approximately 60% of all breast cancer patients have hormone-dependent breast cancer, which contains estrogen receptors and requires estrogen for tumor growth. Estradiol is biosynthesized from androgens by the cytochrom...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/187152006776930873
更新日期:2006-05-01 00:00:00
abstract:AIM:The aim of our research work is the synthesis of tetrahydroisoquinoline derivatives as anti-Angiogenesis and anti-cancer agents. BACKGROUND:Cancer is the second leading cause of deaths in United States. The current recovery rate from the advanced treatment for the cancer is unacceptably low. Therefore, identificat...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/1871520621666210112122913
更新日期:2021-01-12 00:00:00
abstract::Resistance to chemotherapy, biological and targeted therapies is an important clinical problem. Resistance can arise and/or be selected for multiple mechanisms of action. Unfortunately, acquired resistance to antitumor agents or regimens is nearly inevitable in all patients with metastatic disease. Until recently, it ...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/1871520614666140418144610
更新日期:2014-01-01 00:00:00
abstract::In the early 1960s, inorganic pyrophosphate (PPi) was found to be present in body fluids and to act as a natural inhibitor of calcification by its interaction with hydroxyapatite. In addition to inhibiting the formation of calcium phosphate, PPi also inhibited dissolution of hydroxyapatite crystals, which made it inte...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/187152012799014959
更新日期:2012-02-01 00:00:00
abstract:BACKGROUND:Pyrazole derivatives have been reported as both anticancer and antiinflammatory agents. OBJECTIVE:This study was conducted to develop new pyrazole derivatives as potential anticancer and/or antiinflammatory agents. Their molecular mechanisms of action have been investigated. METHOD:a series of new triarylp...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章
doi:
更新日期:2017-01-01 00:00:00
abstract::Polyphenol-protein interaction (PPI) is reversible in that polyphenol-protein complex can be dissociated and release the free polyphenols. The aim of this study is to evaluate the contribution of polyphenol-protein interaction on improving the DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging capacity of polyphe...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/187152012802650101
更新日期:2012-10-01 00:00:00
abstract::Apoptosis, or programmed cell death, is an important physiologic process multicellular organisms use to maintain homeostasis by providing a means for elimination of redundant cells during development. Furthermore, cells that have become damaged or are defective undergo apoptosis to prevent disease. It is an important ...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/187152009789377763
更新日期:2009-11-01 00:00:00
abstract::The phosphatidylinositol 3-kinase/Akt/mammalian target of rapamycin (PI3K/Akt/mTOR) pathway is a key regulator of authophagy. Natural products show anticancer activity and often induce apoptosis or autophagy. The crosstalk between these two types of cell death makes autophagy an interesting target since drugs targetin...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/18715206113139990130
更新日期:2013-09-01 00:00:00
abstract:BACKGROUND:Ruthenium-based anti-cancer compounds are proposed as viable alternatives that might circumvent the disadvantages of platinum-based drugs, the only metallodrugs in clinical use for chemotherapy. Organometallic complexes in particular hold great potential as alternative therapeutic agents since their cytotoxi...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章
doi:
更新日期:2017-01-01 00:00:00
abstract::Glioblastoma Multiforme (GMB) is the most aggressive primary brain tumor with poor survival rates and universal recurrence despite aggressive treatments. Recent research suggested that GBM has multiple glioma cell populations, some of which are organized in a stem cell hierarchical order with different stages of diffe...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/1871520614666140825105145
更新日期:2014-01-01 00:00:00
abstract::The study of anticancer properties from natural products has regained popularity as natural molecules provide a high diversity of chemical structures with specific biological and medicinal activity. Based on a documented library of the most common medicinal plants used by the indigenous people of North America, we scr...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/1871520614666140608150448
更新日期:2015-01-01 00:00:00
abstract:BACKGROUND:Cancer is the second leading cause of death globally. Hydrazone and hydrazone derivatives have high activity, and for this reason, these compound are greatly used by researchers to synthesize new anti-cancer drug. The aim of this research work is to synthesize novel anticancer agents. METHODS:New hydrazone ...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/1871520619666190318125824
更新日期:2019-01-01 00:00:00
abstract:BACKGROUND & PURPOSE:In evaluating new drugs for the treatment of various types of cancer, investigations have been made to discover a variety of anti-tumor compounds with less side effects on normal cells. Investigations have shown that the heterodimers S100A8 and S100A9 inhibit the enzyme casein kinase 2 and then pre...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/1871520620666200331101209
更新日期:2020-01-01 00:00:00
abstract:BACKGROUND:The 2-amino 1,3,4-thiadiazole framework has attracted considerable interest because of its prevalence in compounds possessing a wide range of pharmacological properties including anticancer/antitumor activities. Though a number of methods have been reported for the synthesis of this class of compounds, some ...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/1871520620666200409143513
更新日期:2020-01-01 00:00:00
abstract:BACKGROUND:Angiogenesis is physiological process in embryogenesis, organ development, endometrial vasculature in menstrual cycle and wound healing. Angiogenesis has also been associated with several pathological conditions such as cancer, arthritis, atherosclerosis, etc. Out of the many growth factor responsible for an...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章
doi:
更新日期:2017-01-01 00:00:00
abstract::The Src family of kinases has nine known members, all of which are nonreceptor tyrosine kinases involved in signal transduction in both normal and cancer cells. Interest in these kinases has increased recently because of the development, initial clinical success, and low toxicity of pharmacologic inhibitors. c-Src is ...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/187152007784111278
更新日期:2007-11-01 00:00:00
abstract:BACKGROUND:Cancer stem cells (CSC) are subpopulation within the tumor that acts a part in the initiation, progression, recurrence, resistance to drugs and metastasis of cancer. It is well known that epigenetic changes lead to tumor formation in cancer stem cells and show drug resistance. Epigenetic modulators and /or t...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/1871520621666201207090702
更新日期:2020-12-06 00:00:00
abstract::The metabolism of alkylating agents is accompanied by the generation of reactive oxygen species. The aim of this study was to treat estrogen receptor-positive and estrogen receptor-negative human breast cancer cells, MCF-7 and MDA-MB-231, respectively, with cisplatin and five different berenil-platinum (II) complexes,...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/1871520614666140623120809
更新日期:2014-01-01 00:00:00
abstract:INTRODUCTION:Inflammation is a vital reaction of the natural immune system that protects against encroaching agents. However, uncontrolled inflammation can lead to complications. Trigonella foenum-graecum is traditionally used as an anti-inflammatory herb. OBJECTIVES:The current study was conducted to explore the anti...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/1871520620666201005100132
更新日期:2020-10-04 00:00:00
abstract:AIM:The aim of this study is to explore the therapeutic potential of S-allylcysteine (SAC) organosulphur compound as potent immune checkpoint inhibitor PD-L1. BACKGROUND:Natural compounds have been showing tremendous anticancerous potential via suppressing the expression of genes involved in development and progressio...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/1871520620666200728121929
更新日期:2020-07-28 00:00:00
abstract::Cancer is the second leading cause of death, preceded only by cardiovascular diseases, and there is epidemiological evidence that demonstrate this tendency is emerging worldwide. Brazil has an extensive vegetal biodiversity with more than 55,000 species listed. Such biodiversity collaborates with the finding of compou...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/18715206113139990314
更新日期:2013-12-01 00:00:00
abstract:BACKGROUND:Reserpine, an indole alkaloid commonly used for hypertension, is found in the roots of Rauwolfia serpentina. Although the root extract has been used for the treatment of cancer, the molecular mechanism of its anti-cancer activity on hormonal independent prostate cancer remains elusive. METHODS:we evaluated ...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/1871520618666180209152215
更新日期:2018-01-01 00:00:00
abstract::Cancer is the main cause of death, so the search for active agents to be used in the therapy of this disease, is necessary. According to studies conducted, substances derived from natural products have shown to be promising in this endeavor. To these researches, one can associate with the aid of computational chemistr...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/1871520618666181119110934
更新日期:2019-01-01 00:00:00
abstract::Natural product extracts are a rich source of small molecules that display antitumor activity. Cantharidin, in the form of the dried body of the Chinese blister beetles: Mylabris phalerata or M. cichorii, displays antitumor activity and induces apoptosis in many types of tumor cells. Cantharidin has been used as an an...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/1871520610909040392
更新日期:2009-05-01 00:00:00
abstract::A majority of breast cancers (BC) display characteristics of epithelial cells and express estrogen receptors and/or HER-2 (a member of the epidermal growth factor receptor family). About one-fifth of BC is constituted of basal cells for which there is no specific category of proliferation regulators. Insulin-like grow...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/187152008786847747
更新日期:2008-12-01 00:00:00
abstract:BACKGROUND:Colorectal Cancer (CRC) is one of the most common fatal diseases with high morbidity. Alteration of glucose metabolism is one of the hallmarks in the development of CRC. Glucose Transporter 1 (GLUT1) is a key rate-limiting protein in hyperactive glucose metabolism and up-regulated in CRC, however, the underl...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/1871520620666200318094618
更新日期:2020-01-01 00:00:00
abstract::As early as the 1920s, the eminent physician and chemist, Otto Warburg, nominated for a second Nobel Prize for his work on fermentation, observed that the core metabolic signature of cancer cells is a high glycolytic flux. Warburg averred that the prime mover of cancer is defective mitochondrial respiration, which dri...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/1871520614666140804224637
更新日期:2014-01-01 00:00:00
abstract::The rapid approval of several novel agents has given prostate cancer patients and their treating physicians many new and effective therapeutic options. Four new medical therapies were recently approved on the basis of prolonged overall survival in castration-resistant prostate cancer (CRPC) patients: sipuleucel-T, cab...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/18715206113139990077
更新日期:2013-07-01 00:00:00
abstract::Cisplatin has a broad-spectrum antitumor activity and is widely used for the treatment of various malignant tumors. However, acquired or intrinsic resistance of cisplatin is a major problem for patients during the therapy. Recently, it has been reported cancer stem cell (CSC)-derived drug resistance is a great challen...
journal_title:Anti-cancer agents in medicinal chemistry
pub_type: 杂志文章
doi:10.2174/1871520620666200903145939
更新日期:2020-09-03 00:00:00