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Urea transport and Kidd blood groups.

The gene encoding for the human erythrocyte urea transporter (HUT11 clone) has recently been cloned (Olives et al., J. Biol. Chem., 269, 3/649, 1994). It has been localized at 18q12-q21, like the Kidd blood group gene. In vitro translation experiments indicated that cDNA HUT11 could induce the synthesis of a 36 kDa protein which can be immunoprecipitated by an anti-Jk3 antibody (a human antibody produced by Jk(a-b-) individuals). This antibody also precipitates a 46-60 kDa protein from human red blood cells, except from those with Jk(a-b-) phenotype. After N-glycanase digestion, the length of

Contraction of vascular smooth muscle induced by phorbol 12,13 dibutyrate in human and rat pulmonary arteries.

1. The effect of phorbol 12,13 dibutyrate (PDB) on vascular tone was studied in both human and rat isolated pulmonary arterial strips (HPA a … isoquinolinesulphonyl)-2-methylpiperazine (H7, 50 microM), 70.5 +/- 12.2% and 56 +/- 18% (n = 5) by phloretin (100 microM) and 80.7 +/- 8.4% and 71 +/- 14% (n = 5) by staurosporine (25 nM) in HPA and RPA, respectively.6. Long term treatment (15-20 h) of arterial strips with phorbol esters (phorbol 12,13 didecanoate, or PDB) abolished the contractile respons …

HPLC-ESI-QTOF-MS profiling of antibacterial bioactive solvent fractions of Senna alata (L.) roxb (Fabaceae) leaves, and in silico prediction of pharmacokinetic, drug-likeness, and toxicity of major phyto-components.

ETHNOPHARMACOLOGICAL RELEVANCE: Medicinal plants are a rich source of new antibacterial leads. One such plant is Senna alata (L.) Roxb (Faba … phytochemicals were reported for the first time in S. alata fractions. Seven metabolites, including phloretin, 7,4'-dihydroxyflavone, isorhamnetin, apigenin, genistein, naringenin, and lactarorufin B, emerged as potential drug candidates that satisfy most of the drug candidacy criteria and PK profile amongst which apigenin, genistein, and naringenin depicte …

Enhanced expression of glucose transporter-1 in vascular smooth muscle cells via the Akt/tuberous sclerosis complex subunit 2 (TSC2)/mammalian target of rapamycin (mTOR)/ribosomal S6 protein kinase (S6K) pathway in experimental renal failure.

BACKGROUND: Chronic renal failure (CRF) is associated with increased cardiovascular mortality, and medial vascular smooth muscle cell (VSMC) … sion of GLUT1 in rat A7r5 rat embryonic aortic cells stimulated by IS in the presence or absence of phloretin, a GLUT1 inhibitor, to explore the pathogenic role of GLUT1 in uremic vasculopathy. The contribution of Akt/TSC2/mTOR/S6K signaling in modifying the GLUT1 expression was also assessed. RESULTS: Eight weeks after 5/6 nephrectomy, aortic tissue obtai …

Characterization of L-thyroxine transport into hepatocytes isolated from juvenile rainbow trout (Oncorhynchus mykiss).

Uptake of L-thyroxine (T4) by isolated trout hepatocytes was characterized after 1-min incubation of cells in a Hanks' balanced salts medium … alene sulfonic acid (1 mM), both decreased T4 uptake to 32 and 36% of controls, respectively, while phloretin (0.1 mM) and 5,5'-diphenylhydantoin, specific inhibitors of carrier-mediated transport, depressed uptake to 8 and 32% of controls, respectively. 3,5,3'-triiodo-L-thyronine (T3) decreased T4 uptake with an apparent Ki of 0.19 microM, indicating that …

Electrostimulation enhances FAT/CD36-mediated long-chain fatty acid uptake by isolated rat cardiac myocytes.

We investigated palmitate uptake and utilization by contracting cardiac myocytes in suspension to explore the link between long-chain fatty acid (FA) uptake and cellular metabolism, in particular the role of fatty acid translocase (FAT)/CD36-mediated transsarcolemmal FA transport. For this, an experimental setup was developed to electrically stimulate cardiomyocytes in multiple parallel incubations. Electrostimulation at voltages > or =170 V resulted in cellular contraction with no detrimental effect on cellular integrity. At 200 V and 4 Hz, palmitate uptake (measured after 3-min incubation) w

Voltage-gated and ATP-sensitive K+ channels are associated with cell proliferation and tumorigenesis of human glioma.

Increasing evidence indicates that potassium (K+) channels play important roles in the growth and development of human cancer. In the present study, we investigated the contribution of and the mechanism by which K+ channels control the proliferation and tumor development of U87-MG human glioma cells. A variety of K+ channel blockers and openers were used to differentiate the critical subtype of K+ channels involved. The in vitro data demonstrated that selective blockers of voltage-gated K+ (K(V)) channels or ATP-sensitive K+ (K(ATP)) channels significantly inhibited the proliferation of U87-MG

An inhibitory and beneficial effect of chlorpromazine and promethazine (C + P) on hyperglycolysis through HIF-1α regulation in ischemic stroke.

BACKGROUND: After ischemic stroke, the increased catabolism of glucose (hyperglycolysis) results in the production of reactive oxygen specie … perfusion. At the onset of reperfusion, rats received C + P with or without temperature control, or phloretin [glucose transporter (GLUT)-1 inhibitor], or cytochalasin B (GLUT-3 inhibitor). We detected brain ROS, apoptotic cell death, and ATP levels along with HIF-1α expression. Cerebral hyperglycolysis was measured by glucose, protein expression of GLUT-1/ …

[Non-targeted metabolomics analysis of exosomes derived from Glycyrrhiza uralensis].

Exosomes are nanometer-sized secretory vesicles that play a pivotal role in mediating intercellular communication. Recently， exosomes derive … lkaloids， fatty acids， and phenylpropanoids. Bioactive compounds of interest included azelaic acid， phloretin， and senkyunolide C， highlighting their potential pharmacological significance. In summary， this study demonstrates that the TIBS-based in vitro platform enables efficient， scalable， and consistent production of G. uralensis-derived exosomes with ho …

Shutting off the fuel supply to target metabolic vulnerabilities in multiple myeloma.

Pathways that govern cellular bioenergetics are deregulated in tumor cells and represent a hallmark of cancer. Tumor cells have the capacity to reprogram pathways that control nutrient acquisition, anabolism and catabolism to enhance their growth and survival. Tumorigenesis requires the autonomous reprogramming of key metabolic pathways that obtain, generate and produce metabolites from a nutrient-deprived tumor microenvironment to meet the increased bioenergetic demands of cancer cells. Intra- and extracellular factors also have a profound effect on gene expression to drive metabolic pathway

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… Phloretin (Preclinical) | Blocks cyclins and cyclin-dependent kinases and activates mitochondria-mediated cell death to promote cell death ( 61 , 75 ). Hexokinase | Vincristine | See above. Bortezomib | See above. … The efficacy of phloridzin and phloretin on tumor cell growth . Anticancer Res ( 1993 ) 13 ( 6A ): 2287–92 . 8297148 90 Kobori M Shinmoto H Tsushida T Shinohara K . Phloretin-induced apoptosis in B16 melanoma 4a5 cells by inhibition of glucose transmembrane transport . …

Natural products as metabolic modulators to enhance cancer immunotherapy: reprogramming the tumor microenvironment.

Cancer remains a major global health challenge, and although immunotherapy has achieved remarkable breakthroughs, its efficacy is often limited by tumor-induced immunosuppression within the tumor microenvironment (TME). Emerging evidence indicates that metabolic reprogramming plays a pivotal role in shaping the TME and regulating antitumor immune responses. Targeting tumor and immune cell metabolism has therefore become a promising strategy to enhance the effectiveness of cancer immunotherapy. This review first summarizes the metabolic reprogramming that occurs within the TME, including altera

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… Besides, phloretin suppresses GLUT2 expression by blocking the transcription factor HNF6 and additionally activates the p53 pathway, promoting cell cycle arrest and apoptosis ( 103 ). … Apple Polyphenol Phloretin Inhibits Colorectal Cancer Cell Growth via Inhibition of the Type 2 Glucose Transporter and Activation of p53-Mediated Signaling . J Agric Food Chem . ( 2016 ) 64 : 6826–37 . doi: 10.1021/acs.jafc.6b02861 , PMID: 27538679 104 Fang J Bao YY Zhou SH Fan J . …

Roles of volume-sensitive chloride channel in excitotoxic neuronal injury.

Excitotoxicity is associated with stroke, brain trauma, and a number of neurodegenerative disorders. In the brain, during excitotoxic insults, neurons undergo rapid swelling in both the soma and dendrites. Focal swellings along the dendrites called varicosities are considered to be a hallmark of acute excitotoxic neuronal injury. However, it is not clear what pathway is involved in the neuronal anion flux that leads to the formation and resolution of excitotoxic varicosities. Here, we assessed the roles of the volume-sensitive outwardly rectifying (VSOR) Cl- channel in excitotoxic responses in

Metabolic Reprogramming of Cancer Cells and Therapeutics Targeting Cancer Metabolism.

BackgroundCancer metabolism is a field focused on the unique alterations in metabolic pathways that occur in cancer cells, distinguishing them from the metabolic processes in normal cells.MethodsAn extensive review of the current literature on the metabolic adaptation of cancer cells was carried out in the current study.ResultsThe rapidly proliferating cells require high levels of molecules, such as glucose, amino acids, lipids, and nucleotides, along with increased energy demand (ATP). These requirements are met through alterations in the processes involving glucose, amino acid, lipid, and nu

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… Some natural chemicals, such as genistein, fasentin, apigenin, and phloretin, also demonstrated GLUT suppression and hence inhibited the proliferation of cancer cells. … Phloretin, a polyphenol, has been shown to inhibit GLUT 2 in triple‐negative breast cancer, suppressing tumor development and metastasis [ 133 ]. In addition, phloretin can block GLUT 1, which is excessively expressed in the hypoxic regions of resistant colon cancer cells. …

The skeleton: an overlooked regulator of systemic glucose metabolism in cancer?

Recent discoveries demonstrated the skeleton's role as an endocrine organ regulating whole-body glucose homeostasis. Glucose metabolism is critical for rapid cell proliferation and tumour growth through increasing glucose uptake and fermentation of glucose to lactate despite being in an aerobic environment. This hypothesis paper discusses emerging evidence on how bones can regulate whole-body glucose homeostasis with potential to impact on tumour growth and proliferation. Moreover, it proposes a clinical link between bone glucose metabolism and prognosis of cancer based on recent clinical tria

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… Interestingly, several inhibitors of glucose transporters, such as fasentin, phloretin, STF-31, and WZB117 have already been discovered, and experiments with preclinical models demonstrated their impact in reducing tumour progression ( 51 – 53 ). … The apple polyphenol phloretin inhibits breast cancer cell migration and proliferation via inhibition of signals by type 2 glucose transporter . J Food Drug Anal . ( 2018 ) 26 : 221–31 . doi: 10.1016/j.jfda.2017.03.009 PMC9332637 29389559 54 Liu Y Cao Y Zhang W Bergmeier S Qian Y Akbar H . …

Metabolic Symbiosis in Chemoresistance: Refocusing the Role of Aerobic Glycolysis.

Cellular metabolic reprogramming is now recognized as a hallmark of tumors. Altered tumor metabolism determines the malignant biological behaviors and phenotypes of cancer. More recently, studies have begun to reveal that cancer cells generally exhibit increased glycolysis or oxidative phosphorylation (OXPHOS) for Adenosine Triphosphate(ATP)generation, which is frequently associated with drug resistance. The metabolism of drug-resistant cells is regulated by the PI3K/AKT/mTOR pathway which ultimately confer cancer cells drug resistance phenotype. The key enzymes involved in glycolysis and the

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… Under hypoxic conditions, phloretin, a GLUT1 inhibitor that blocks glucose uptake and glycolysis, re-sensitized both types of cancer cells to daunorubicin's anti-cancer activity and apoptosis-inducing effects ( 34 ). …

Antioxidants in brain tumors: current therapeutic significance and future prospects.

Brain cancer is regarded among the deadliest forms of cancer worldwide. The distinct tumor microenvironment and inherent characteristics of brain tumor cells virtually render them resistant to the majority of conventional and advanced therapies. Oxidative stress (OS) is a key disruptor of normal brain homeostasis and is involved in carcinogenesis of different forms of brain cancers. Thus, antioxidants may inhibit tumorigenesis by preventing OS induced by various oncogenic factors. Antioxidants are hypothesized to inhibit cancer initiation by endorsing DNA repair and suppressing cancer progress

Lung cancer immunotherapy: progress, pitfalls, and promises.

Lung cancer is the primary cause of mortality in the United States and around the globe. Therapeutic options for lung cancer treatment include surgery, radiation therapy, chemotherapy, and targeted drug therapy. Medical management is often associated with the development of treatment resistance leading to relapse. Immunotherapy is profoundly altering the approach to cancer treatment owing to its tolerable safety profile, sustained therapeutic response due to immunological memory generation, and effectiveness across a broad patient population. Different tumor-specific vaccination strategies are

The Mediterranean Diet, a Rich Source of Angiopreventive Compounds in Cancer.

Diet-based chemoprevention of cancer has emerged as an interesting approach to evade the disease or even target its early phases, reducing its incidence or slowing down tumor progression. In its basis in the essential role of angiogenesis for tumor growth and metastasis, angioprevention proposes the use of inhibitors of angiogenesis in cancer prevention. The anti-angiogenic potential exhibited by many natural compounds contained in many Mediterranean diet constituents makes this dietary pattern especially interesting as a source of chemopreventive agents, defined within the angioprevention str

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… Evaluation of taxifolin and phloretin as antiangiogenic flavonoids: An in vivo, in vitro experimental analysis. Int. J. Pharm. Sci. 2015;7:5–12. 84. …

Energy metabolism in health and diseases.

Energy metabolism is indispensable for sustaining physiological functions in living organisms and assumes a pivotal role across physiological and pathological conditions. This review provides an extensive overview of advancements in energy metabolism research, elucidating critical pathways such as glycolysis, oxidative phosphorylation, fatty acid metabolism, and amino acid metabolism, along with their intricate regulatory mechanisms. The homeostatic balance of these processes is crucial; however, in pathological states such as neurodegenerative diseases, autoimmune disorders, and cancer, exten

Интеграция нанотехнологий в онкологию для передовых стратегий наночастиц в целевую диагностику и лечение рака.

Рак остается одной из основных глобальных проблем в области здравоохранения. Обычная терапия часто ограничивается низкой избирательностью опухолей, системной токсичностью, резистентностью к многочисленным лекарствам и неоптимальными фармакокинетиками. Нанотехнология предлагает преобразующий подход в онкологии. Она позволяет осуществлять целенаправленные поставки наркотиков, контролировать или стимулировать их высвобождение и использовать многофункциональные платформы, сочетающие в себе терапию и диагностику. Нанопчасти повышают растворимость наркотиков, продлевают циркуляцию и повышают внутрик