keyword
MENU ▼
Read by QxMD icon Read
search

2-methoxyestradiol

keyword
https://www.readbyqxmd.com/read/28072767/cyp3a7-1c-allele-is-associated-with-reduced-levels-of-2-hydroxylation-pathway-oestrogen-metabolites
#1
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 10, 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
#2
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
#3
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
#4
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
#5
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
#6
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...
November 29, 2016: 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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
https://www.readbyqxmd.com/read/27681649/red-maca-lepidium-meyenii-did-not-affect-cell-viability-despite-increased-androgen-receptor-and-prostate-specific-antigen-gene-expression-in-the-human-prostate-cancer-cell-line-lncap
#16
P Díaz, H Cardenas, P A Orihuela
We examined whether aqueous extract of Lepidium meyenii (red Maca) could inhibit growth, potentiate apoptotic activity of two anticancer drugs Taxol and 2-methoxyestradiol (2ME) or change mRNA expression for the androgen target genes, androgen receptor (Ar) and prostate-specific antigen (Psa) in the human prostate cancer cell line LNCaP. Red Maca aqueous extract at 0, 10, 20, 40 or 80 μg/ml was added to LNCaP cells, and viability was evaluated by the MTS assay at 24 or 48 hr after treatment. Furthermore, LNCaP cells were treated with 80 μg/ml of red Maca plus Taxol or 2ME 5 μM and viability was assessed 48 hr later...
October 2016: Andrologia
https://www.readbyqxmd.com/read/27631553/the-bone-sparing-effects-of-2-methoxyestradiol-are-mediated-via-estrogen-receptor-%C3%AE-in-male-mice
#17
Anna L Eriksson, Anna S Wilhelmson, Johan B Fagman, Henrik Ryberg, Antti Koskela, Juha Tuukkanen, Åsa Tivesten, Claes Ohlsson
2-Methoxyestradiol (2ME2), a metabolite of 17β-estradiol (E2), exerts bone sparing effects in animal models. We hypothesized that the underlying mechanism is back conversion of 2ME2 to E2, which subsequently acts via estrogen receptor (ER)α. We measured serum E2 levels in orchidectomized wild-type (WT) mice treated with 2ME2 66.6 μg/d or placebo. In placebo-treated animals, E2 was below the detection limit. In 2ME2-treated mice, the serum E2 level was 4.97 ± 0.68 pg/mL. This corresponds to the level found in diesterus in cycling female mice...
November 2016: Endocrinology
https://www.readbyqxmd.com/read/27526090/determination-of-estrogenic-compounds-in-milk-and-yogurt-samples-by-hollow-fibre-liquid-phase-microextraction-gas-chromatography-triple-quadrupole-mass-spectrometry
#18
Giovanni D'Orazio, Javier Hernández-Borges, Antonio Vicente Herrera-Herrera, Salvatore Fanali, Miguel Ángel Rodríguez-Delgado
An environmentally friendly method based on hollow-fibre liquid-phase microextraction (HF-LPME) was developed for the extraction of selected estrogenic compounds (i.e. four natural sexual hormones: estrone, 17β-estradiol, 17α-estradiol and estriol; two exoestrogens: 17α-ethynylestradiol and 2-methoxyestradiol; two synthetic stilbenes: dienestrol and hexestrol; and five resorcylic acid lactones: zearalenone, α-zearalanol, β-zearalanol, α-zearalenol and β-zearalenol), from whole cow and semi-skimmed goat milk and whole natural yogurt...
October 2016: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/27473145/hypoxia-induced-resistance-to-cisplatin-mediated-apoptosis-in-osteosarcoma-cells-is-reversed-by-gambogic-acid-independently-of-hif-1%C3%AE
#19
Wei Zhao, Shi-Qi Xia, Jin-Peng Zhuang, Zhi-Peng Zhang, Chang-Cheng You, Jing-Long Yan, Gong-Ping Xu
In vitro evidence of hypoxia-induced resistance to cisplatin (CDDP)-mediated apoptosis exists in human osteosarcoma (OS). Gambogic acid (GA) is a promising chemotherapeutic compound that could increase the chemotherapeutic effectiveness of CDDP in human OS cells by inducing cell cycle arrest and promoting apoptosis. This study examined whether GA could overcome OS cell resistance to CDDP. Hypoxia significantly reduced levels of CDDP-induced apoptosis in the OS cell lines MG63 and HOS. However, combined treatment with GA and CDDP revealed a strong synergistic action between these drugs, and higher protein levels of the apoptosis-related factor Fas, cleaved caspase-8 and cleaved caspase-3 and lower expression of hypoxia-inducible factor (HIF)-1α are detected in both cell lines...
September 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27243036/2-methoxyestradiol-alleviates-experimental-autoimmune-uveitis-by-inhibiting-lymphocytes-proliferation-and-t-cell-differentiation
#20
Linxinyu Xu, Tianshu Yang, Shaobo Su, Fang Wang
Purpose. To investigate the effect of 2-Methoxyestradiol (2ME2) on experimental autoimmune uveitis (EAU) and the mechanism. Method. C57BL/6 male mice were used to establish the EAU model. 2ME2 was abdominal administrated in D0-D13, D0-D6, and D7-D13 and control group was given vehicle from D0-D13. At D14, pathological severity was scored. Lymphocyte reaction was measured using MTT assay. T cell differentiation in draining lymph nodes and eye-infiltrating cells was tested by flow cytometry. Proinflammatory cytokines production from lymphocytes was determined by ELISA...
2016: BioMed Research International
keyword
keyword
44687
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"