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2-methoxyestradiol

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https://www.readbyqxmd.com/read/28214650/2-methoxyestradiol-protects-against-igg-immune-complex-induced-acute-lung-injury-by-blocking-nf-%C3%AE%C2%BAb-and-ccaat-enhancer-binding-protein-%C3%AE-activities
#1
Chunguang Yan, Yanfei Shen, Qiqing Sun, Dong Yuan, Huifang Tang, Hongwei Gao
Increasing evidences indicate that 2-Methoxyestradiol (2ME2) plays an essential role in protecting against inflammatory responses. However, its effect on IgG immune complex (IC)-induced acute lung injury (ALI) remains enigmatic. In the study, by using i.p. administration of 2ME2, we evaluated its influence on IgG IC-induced pulmonary injury in mice. We found that during IgG IC-induced ALI, mice treated by 2ME2 displayed a substantial decrease in vascular permeability and neutrophil influx (represented by myeloperoxidase activity) when compared with their counterparts receiving vehicle treatment...
February 16, 2017: Molecular Immunology
https://www.readbyqxmd.com/read/28213273/2-methoxyestradiol-protects-against-ischemia-reperfusion-injury-in-alcoholic-fatty-liver-by-enhancing-sirtuin-1-mediated-autophagy
#2
Hong-Ik Cho, Min-Jong Seo, Sun-Mee Lee
Alcoholic fatty liver (AFL) is susceptible to ischemia/reperfusion (I/R) injury, responding with inflammation and extensive hepatocellular damage. Autophagy maintains cellular homeostasis and regulates inflammation and lipid metabolism. 2-Methoxyestradiol (2-ME2), an endogenous metabolite of estradiol, exhibits antioxidant and anti-inflammatory properties. This study examined the cytoprotective mechanisms of 2-ME2 on hepatic I/R in AFL, focusing on autophagy signaling. C57BL/6 mice were fed an ethanol diet (ED) to induce AFL, or a control diet (CD) for 6 weeks, and then subjected to 60 min of ischemia and 5 h of reperfusion...
February 14, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28212889/inhibition-of-proliferation-and-invasion-in-2d-and-3d-models-by-2-methoxyestradiol-in-human-melanoma-cells
#3
R R Massaro, F Faião-Flores, V W Rebecca, S Sandri, D K Alves-Fernandes, P C Pennacchi, K S M Smalley, S S Maria-Engler
Despite the recent advances in the clinical management of melanoma, there remains a need for new pharmacological approaches to treat this cancer. 2-methoxyestradiol (2ME) is a metabolite of estrogen that has shown anti-tumor effects in many cancer types. In this study we show that 2ME treatment leads to growth inhibition in melanoma cells, an effect associated with entry into senescence, decreased pRb and CyclinB1 expression, increased p21/Cip1 expression and G2/M cell cycle arrest. 2ME treatment also inhibits melanoma cell growth in colony formation assays, including cell lines with acquired resistance to BRAF and BRAF+MEK inhibitors...
February 14, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28178600/whole-flaxseed-diet-alters-estrogen-metabolism-to-promote-2-methoxtestradiol-induced-apoptosis-in-hen-ovarian-cancer
#4
Anushka Dikshit, Karen Hales, Dale Buchanan Hales
The study reported here demonstrates that a flaxseed-supplemented diet causes ovarian tumors in the laying hen to undergo apoptosis, resulting in a reduction of tumor burden, reducing the frequency and severity of ovarian cancer. We have previously shown in normal ovaries that flaxseed and its components down-regulate ERalpha and alter the expression of enzymes that metabolize estrogen. In this study, we analyzed the effects of the two main components of whole flaxseed, ligan and omega 3 fatty acids on estrogen metabolism and the estrogen receptor in ovarian tumors...
January 23, 2017: Journal of Nutritional Biochemistry
https://www.readbyqxmd.com/read/28128564/using-affinity-to-provide-long-term-delivery-of-antiangiogenic-drugs-in-cancer-therapy
#5
Edgardo Rivera-Delgado, Horst A von Recum
Antiangiogenic drugs encompass many of the different cancer drugs currently under clinical investigation. One of the drawbacks of antiangiogenic therapy, though, is that upon cessation of drug treatment tumors can recur with an accelerated growth rate. In this study we investigate the capacity of using affinity interactions between a polymer made from cyclodextrin and four antiangiogenic drugs, tranilast, SU5416, 2-methoxyestradiol, and silibinin, with the ultimate goal of creating delivery profiles on the order of antiangiogenic processes (needing weeks, rather than hours of delivery)...
February 9, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28072767/cyp3a7-1c-allele-is-associated-with-reduced-levels-of-2-hydroxylation-pathway-oestrogen-metabolites
#6
Deepti Sood, Nichola Johnson, Pooja Jain, Alexandros P Siskos, Mark Bennett, Clare Gilham, Marta Cecilia Busana, Julian Peto, Isabel Dos-Santos-Silva, Hector C Keun, Olivia Fletcher
BACKGROUND: Endogenous sex hormones are well-established risk factors for breast cancer; the contribution of specific oestrogen metabolites (EMs) and/or ratios of specific EMs is less clear. We have previously identified a CYP3A7*1C allele that is associated with lower urinary oestrone (E1) levels in premenopausal women. The purpose of this analysis was to determine whether this allele was associated with specific pathway EMs. METHODS: We measured successfully 12 EMs in mid-follicular phase urine samples from 30 CYP3A7*1C carriers and 30 non-carriers using HPLC-MS/MS...
January 2017: British Journal of Cancer
https://www.readbyqxmd.com/read/28017781/inotropic-support-against-early-brain-injury-improves-cerebral-hypoperfusion-and-outcomes-in-a-murine-model-of-subarachnoid-hemorrhage
#7
Tomoko Mutoh, Tatsushi Mutoh, Kazuhiro Nakamura, Kazumasu Sasaki, Yasuko Tatewaki, Tatsuya Ishikawa, Yasuyuki Taki
Early brain injury/ischemia is a recent therapeutic target that contributes to triggering delayed cerebral ischemia (DCI) in the setting of subarachnoid hemorrhage (SAH). This study aimed to determine the role of dobutamine for inotropic cardiac support in improving cerebral blood flow (CBF) and outcomes after experimental SAH, mediated by hypoxia-inducible factor (HIF). Thirty-one mice were subjected to SAH by endovascular perforation, and assigned to either 2% isoflurane postconditioning performed between 1 and 2...
December 23, 2016: Brain Research Bulletin
https://www.readbyqxmd.com/read/28000883/2-methoxyestradiol-inhibits-the-proliferation-and-migration-and-reduces-the-radioresistance-of-nasopharyngeal-carcinoma-cne-2-stem-cells-via-nf-%C3%AE%C2%BAb-hif-1-signaling-pathway-inactivation-and-emt-reversal
#8
Shun-Long Wu, Ya-Jun Li, Kui Liao, Lei Shi, Na Zhang, Shuang Liu, Yao-Yao Hu, Shao-Lin Li, Ying Wang
Accumulating evidence indicates that cancer stem cells (CSCs) are a source of resistance to radiation therapy (RT); however, the mechanism of this resistance remains unclear. 2-Methoxyestradiol (2-ME2) is a metabolic product of estrogen in the body. Recent studies have found that 2-ME2 regulates the activation of transcription factors, including nuclear factor (NF)-κB/hypoxia-inducible factor-1 (HIF-1), thus contributing to tumor cell apoptosis and chemosensitivity. Therefore, 2-ME2 is being studied as a potential anticancer drug...
February 2017: Oncology Reports
https://www.readbyqxmd.com/read/27943229/2-methoxyestradiol-inhibits-intracerebral-hemorrhage-induced-angiogenesis-in-rats
#9
Hai-Tao Li, Hua-Jun Zhou, Jian-Hua Zhong, Tao Tang, Han-Jin Cui, Qi-Mei Zhang, Jing-Hua Zhou, Qiang Zhang
AIM: Angiogenesis occurs after intracerebral hemorrhage (ICH). Hypoxia-inducible factor-1α (HIF-1α) is a critical regulator of angiogenesis; however, its role in the central nervous system remains controversial. 2-Methoxyestradiol (2ME2), a natural metabolite of estrogen, is known to inhibit HIF-1α. In the present study, we investigated the effect of 2ME2 in a rat model of ICH-induced angiogenesis. MATERIAL AND METHODS: Sprague-Dawley male rats were randomly divided into 5 groups: Sham operated group; ICH; ICH+2ME2; and ICH+Vehicle groups...
November 21, 2016: Turkish Neurosurgery
https://www.readbyqxmd.com/read/27923686/photoactivated-hypericin-increases-the-expression-of-sod-2-and-makes-mcf-7-cells-resistant-to-photodynamic-therapy
#10
Patrícia Kimáková, Peter Solár, Barbora Fecková, Veronika Sačková, Zuzana Solárová, Lenka Ilkovičová, Martin Kello
Photoactivated hypericin increased production of reactive oxygen species in human breast adenocarcinoma MCF-7 as well as in MDA-MB-231 cells 1h after photodynamic therapy. On the other hand, reactive oxygen species dropped 3h after photodynamic therapy with hypericin, but only in MCF-7 cells, whereas in MDA-MB-231 cells remained elevated. The difference in the dynamics of reactive oxygen species after hypericin activation was related to increased activity of SOD-2 in MCF-7 cells compared to MDA-MB-231 cells...
January 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27923186/influence-of-surface-passivation-of-2-methoxyestradiol-loaded-plga-nanoparticles-on-cellular-interactions-pharmacokinetics-and-tumour-accumulation
#11
Gopikrishna J Pillai, Bindhu Paul-Prasanth, Shantikumar V Nair, Deepthy Menon
In the present work, 2-Methoxyestradiol [2ME2] loaded PLGA nanoparticles [NPs] were stabilized with Casein or poly(ethylene glycol) [PEG] and evaluated for its cellular interactions, pharmacokinetics and tumour accumulation. Surface stabilized PLGA nanoparticles prepared through a modified emulsion route possessed similar size, surface charge, drug loading and release characteristics. Particle-cell interactions as well as the anti-angiogenesis activity were similar for both nanoformulations in vitro. However, in vivo pharmacokinetics and tumour accumulation of the drug were substantially improved for the PEGylated nanoformulation...
February 1, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/27915012/intra-laboratory-validated-human-cell-based-in-vitro-vasculogenesis-angiogenesis-test-with-serum-free-medium
#12
T Toimela, O Huttala, E Sabell, M Mannerström, J R Sarkanen, T Ylikomi, T Heinonen
Vasculogenesis and angiogenesis are the processes by which new blood vessels are formed. We have developed a serum-free human adipose stromal cell and umbilical cord vein endothelial cell based vasculogenesis/angiogenesis test. In this study, the test was validated in our GLP laboratory following the OECD Guidance Document 34 [1] using erlotinib, acetylic salicylic acid, levamisole, 2-methoxyestradiol, anti-VEGF, methimazole, and D-mannitol to show its reproducibility, repeatability, and predictivity for humans...
November 30, 2016: Reproductive Toxicology
https://www.readbyqxmd.com/read/27883247/2-methoxyestradiol-mediated-induction-of-frzb-contributes-to-cell-death-and-autophagy-in-mg63-osteosarcoma-cells
#13
Dalibel Bravo, Kristen L Shogren, Dongqing Zuo, Eric R Wagner, Gobinda Sarkar, Michael J Yaszemski, Avudaiappan Maran
Osteosarcoma is a bone tumor that mainly affects children and adolescents. Although its pathogenesis is still not fully understood, activation of Wnt signaling has been implicated in the development and metastasis of osteosarcoma. In this report, we have investigated the effect of the anti-tumor compound, 2-methoxyestradiol (2-ME) on Wnt antagonist frizzled-related protein b (Frzb), also known as secreted frizzled-related protein (sFRP)3 in human osteosarcoma (MG63) cells. Our results show that 2-ME treatment induces Frzb gene promoter activity, and increases Frzb mRNA and protein levels in osteosarcoma cells...
November 24, 2016: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/27830025/sevoflurane-postconditioning-improves-myocardial-mitochondrial-respiratory-function-and-reduces-myocardial-ischemia-reperfusion-injury-by-up-regulating-hif-1
#14
Long Yang, Peng Xie, Jianjiang Wu, Jin Yu, Tian Yu, Haiying Wang, Jiang Wang, Zhengyuan Xia, Hong Zheng
BACKGROUND: Sevoflurane postconditioning (SPostC) can exert myocardial protective effects similar to ischemic preconditioning. However, the exact myocardial protection mechanism by SPostC is unclear. Studies indicate that hypoxia-inducible factor-1 (HIF-1) maintains cellular respiration homeostasis by regulating mitochondrial respiratory chain enzyme activity under hypoxic conditions. This study investigated whether SPostC could regulate the expression of myocardial HIF-1α and to improve mitochondrial respiratory function, thereby relieving myocardial ischemia-reperfusion injury in rats...
2016: American Journal of Translational Research
https://www.readbyqxmd.com/read/27806731/in-vitro-assessment-of-a-computer-designed-potential-anticancer-agent-in-cervical-cancer-cells
#15
Michelle Helen Visagie, Seema Rummurat Jaiswal, Anna Margaretha Joubert
BACKGROUND: Computer-based technology is becoming increasingly essential in biological research where drug discovery programs start with the identification of suitable drug targets. 2-Methoxyestradiol (2ME2) is a 17β-estradiol metabolite that induces apoptosis in various cancer cell lines including cervical cancer, breast cancer and multiple myeloma. Owing to 2ME2's poor in vivo bioavailability, our laboratory in silico-designed and subsequently synthesized a novel 2ME2 analogue, 2-ethyl-3-O-sulphamoyl-estra-1,3,5(10),15-tetraen-17-ol (ESE-15-ol), using receptor- and ligand molecular modeling...
November 2, 2016: Biological Research
https://www.readbyqxmd.com/read/27798888/detection-of-redox-imbalance-in-normal-lymphocytes-with-induced-mitochondrial-dysfunction-epr-study
#16
Ekaterina Georgieva, Zhivko Zhelev, Ichio Aoki, Rumiana Bakalova, Tatsuya Higashi
The present study describes a new approach for direct imaging of redox status in live cells using paramagnetic spin-probes, which allows evaluation of the level of oxidative stress due to overproduction of superoxide. The method is based on redox cycling of cell/mitochondria-penetrating nitroxide radicals (e.g. mito-TEMPO) and their electron-paramagnetic resonance (EPR) contrast, which makes them useful molecular sensors for analysis of redox status and oxidative stress in cells and tissues. Oxidative stress was induced in normal human lymphocytes by treatment with 2-methoxyestradiol and rotenone (ME/Rot) at different concentrations...
2016: Anticancer Research
https://www.readbyqxmd.com/read/27797342/high-throughput-screening-in-niche-based-assay-identifies-compounds-to-target-preleukemic-stem-cells
#17
Bastien Gerby, Diogo F T Veiga, Jana Krosl, Sami Nourreddine, Julianne Ouellette, André Haman, Geneviève Lavoie, Iman Fares, Mathieu Tremblay, Véronique Litalien, Elizabeth Ottoni, Milena Kosic, Dominique Geoffrion, Joël Ryan, Paul S Maddox, Jalila Chagraoui, Anne Marinier, Josée Hébert, Guy Sauvageau, Benjamin H Kwok, Philippe P Roux, Trang Hoang
Current chemotherapies for T cell acute lymphoblastic leukemia (T-ALL) efficiently reduce tumor mass. Nonetheless, disease relapse attributed to survival of preleukemic stem cells (pre-LSCs) is associated with poor prognosis. Herein, we provide direct evidence that pre-LSCs are much less chemosensitive to existing chemotherapy drugs than leukemic blasts because of a distinctive lower proliferative state. Improving therapies for T-ALL requires the development of strategies to target pre-LSCs that are absolutely dependent on their microenvironment...
December 1, 2016: Journal of Clinical Investigation
https://www.readbyqxmd.com/read/27780722/gsno-promotes-functional-recovery-in-experimental-tbi-by-stabilizing-hif-1%C3%AE
#18
Mushfiquddin Khan, Tajinder S Dhammu, Mauhamad Baarine, Jinsu Kim, Manjeet K Paintlia, Inderjit Singh, Avtar K Singh
Traumatic brain injury (TBI) causes sustained disability due to compromised neurorepair mechanisms. Crucial to neurorepair and functional recovery following both TBI and stroke is hypoxia-inducible factor-1 alpha (HIF-1α). Based on reports that HIF-1α could be stabilized via S-nitrosylation, we tested the hypothesis that the S-nitrosylating agent S-nitrosoglutathione (GSNO) would stabilize HIF-1α, thereby stimulating neurorepair mechanisms and aiding in functional recovery. TBI was induced by controlled cortical impact (CCI) in adult rats...
October 22, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27760837/6%C3%AE-acetoxyanopterine-a-novel-structure-class-of-mitotic-inhibitor-disrupting-microtubule-dynamics-in-prostate-cancer-cells
#19
Claire Levrier, Martin C Sadowski, Anja Rockstroh, Brian Gabrielli, Maria Kavallaris, Melanie Lehman, Rohan A Davis, Colleen C Nelson
The lack of a cure for metastatic castrate-resistant prostate cancer (mCRPC) highlights the urgent need for more efficient drugs to fight this disease. Here, we report the mechanism of action of the natural product 6α-acetoxyanopterine (6-AA) in prostate cancer cells. At low nanomolar doses, this potent cytotoxic alkaloid from the Australian endemic tree Anopterus macleayanus induced a strong accumulation of LNCaP and PC-3 (prostate cancer) cells as well as HeLa (cervical cancer) cells in mitosis, severe mitotic spindle defects, and asymmetric cell divisions, ultimately leading to mitotic catastrophe accompanied by cell death through apoptosis...
January 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/27756753/benefits-of-multifaceted-chemopreventives-in-the-suppression-of-the-oral-squamous-cell-carcinoma-oscc-tumorigenic-phenotype
#20
Susan R Mallery, Daren Wang, Brian Santiago, Ping Pei, Steven P Schwendeman, Kari Nieto, Richard Spinney, Meng Tong, George Koutras, Brian Han, Andrew Holpuch, James Lang
Over one third of patients who have undergone oral squamous cell carcinoma (OSCC) surgical resections develop life-threatening and often untreatable recurrences. A variety of drugs, intended for management of recurrent or disseminated cancers, were designed to exploit cancer cells' reliance upon overexpressed receptors and gratuitous signaling. Despite their conceptual promise, clinical trials showed these agents lacked efficacy and were often toxic. These findings are consistent with evasion of pathway-targeted treatments via extensive signaling redundancies and compensatory mechanisms common to cancers...
January 2017: Cancer Prevention Research
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