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2-methoxyestradiol

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https://www.readbyqxmd.com/read/27883247/2-methoxyestradiol-mediated-induction-of-frzb-contributes-to-cell-death-and-autophagy-in-mg63-osteosarcoma-cells
#1
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
#2
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
#3
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
#4
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...
October 2016: Anticancer Research
https://www.readbyqxmd.com/read/27797342/high-throughput-screening-in-niche-based-assay-identifies-compounds-to-target-preleukemic-stem-cells
#5
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
#6
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
#7
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...
October 19, 2016: 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
#8
Susan R Mallery, Daren Wang, Brian Santiago, Ping Pei, Steven Schwendeman, Kari Nieto, Richard Spinney, Meng Tong, George Koutras, Byungdo B Han, Andrew S Holpuch, James C Lang
Over 1/3 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...
October 18, 2016: 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
#9
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
#10
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
#11
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
#12
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
#13
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
https://www.readbyqxmd.com/read/27127126/impact-of-apparent-antagonism-of-estrogen-receptor-%C3%AE-by-fulvestrant-on-anticancer-activity-of-2-methoxyestradiol
#14
Magdalena Gorska, Roksana Maja Wyszkowska, Alicja Kuban-Jankowska, Michal Wozniak
Osteosarcoma is one of the most malignant bone tumors of childhood and adolescence. Interestingly, the presence of estrogen receptors α and β has been reported in human bone cells, including osteosarcoma. Thus, inhibitors of estrogens such as fulvestrant, are considered candidates for novel endocrine therapy in treatment of osteosarcoma. Another anticancer agent that seems to be very effective in treatment of osteosarcoma is a derivative of 17β-estradiol, 2-methoxyestradiol. The aim of this study was to determine the anticancer activities of pure anti-estrogen, fulvestrant and combined treatment of fulvestrant and 2-methoxyestradiol towards highly metastatic osteosarcoma 143B cells...
May 2016: Anticancer Research
https://www.readbyqxmd.com/read/27094790/isoflurane-postconditioning-with-cardiac-support-promotes-recovery-from-early-brain-injury-in-mice-after-severe-subarachnoid-hemorrhage
#15
Tomoko Mutoh, Tatsushi Mutoh, Kazumasu Sasaki, Yukiko Yamamoto, Yoshiharu Tsuru, Hirokazu Tsubone, Tatsuya Ishikawa, Yasuyuki Taki
AIMS: Neurocardiac dysfunction is a life-threatening systemic consequence of subarachnoid hemorrhage (SAH) that contributes to triggering delayed cerebral ischemia (DCI). This study aimed to determine the impact of dobutamine cardiac support during isoflurane postconditioning on post-SAH DCI. MAIN METHODS: Male C57BL/6 mice were subjected to SAH, SAH plus isoflurane postconditioning, or SAH plus isoflurane postconditioning with dobutamine. Severity of SAH was graded from 1 to 4 (mild, 1-2; severe, 3-4) based on T2*-weighted magnetic resonance imaging (MRI)...
May 15, 2016: Life Sciences
https://www.readbyqxmd.com/read/27093553/cytochrome-p450-1a2-metabolizes-17%C3%AE-estradiol-to-suppress-hepatocellular-carcinoma
#16
Jianwai Ren, George G Chen, Yi Liu, Xianwei Su, Baoguang Hu, Billy C S Leung, Y Wang, Rocky L K Ho, Shengli Yang, Gang Lu, C G Lee, Paul B S Lai
Hepatocellular carcinoma (HCC) occurs more frequently in men than in women. It is commonly agreed that estrogen plays important roles in suppressing HCC development, however, the underlying mechanism remains largely unknown. Since estrogen is mainly metabolized in liver and its metabolites affect cell proliferation, we sought to investigate if the liver-specific cytochrome P450 1A2 (CYP1A2) mediated the inhibitory effect of estrogen on HCC. In this study, the expression of estrogen-metabolizing enzyme CYP1A2 was determined in HCC tissues and cell lines...
2016: PloS One
https://www.readbyqxmd.com/read/27082496/hif-1%C3%AE-inhibition-by-2-methoxyestradiol-induces-cell-death-via-activation-of-the-mitochondrial-apoptotic-pathway-in-acute-myeloid-leukemia
#17
Nana Zhe, Shuya Chen, Zhen Zhou, Ping Liu, Xiaojing Lin, Meisheng Yu, Bingqing Cheng, Yaming Zhang, Jishi Wang
The bone marrow microenvironment plays an important role in the development and progression of AML. Leukemia stem cells are in a hypoxic condition, which induces the expression of HIF-1α. Aberrant activation of HIF-1α is implicated in the poor prognosis of patients with acute myeloid leukemia (AML). Herein, we investigated the expression of HIF-1α in AML and tested 2-methoxyestradiol (2ME2) as a candidate HIF-1α inhibitor for the treatment of AML. We found that HIF-1α was overexpressed in AML. HIF-1α suppression by 2ME2 significantly induced apoptosis of AML cells, and it outperformed traditional chemotherapy drugs such as cytarabine...
June 2, 2016: Cancer Biology & Therapy
https://www.readbyqxmd.com/read/27069147/nitro-oxidative-stress-is-involved-in-anticancer-activity-of-17%C3%AE-estradiol-derivative-in-neuroblastoma-cells
#18
Magdalena Gorska, Alicja Kuban-Jankowska, Ryszard Milczarek, Michal Wozniak
Neuroblastoma is one of the most common childhood malignancies and the primary cause of death from pediatric cancer. Derivatives of 17β-estradiol, 2-methoxyestradiol, as well as selective estrogen receptor modulators, such as fulvestrant, are novel potentially active anticancer agents. In particular, 2-methoxyestradiol is effective in treatment of numerous malignancies, including breast and prostate cancer, Ewing sarcoma, and osteosarcoma. Herein, we treated neuroblastoma SH-SY5Y cells with physiologically and pharmacologically relevant concentrations of 2-methoxyestradiol...
April 2016: Anticancer Research
https://www.readbyqxmd.com/read/27061927/oxidative-pathways-in-response-to-polyunsaturated-aldehydes-in-the-marine-diatom-skeletonema-marinoi-bacillariophyceae
#19
Alessandra A Gallina, Anna Palumbo, Raffaella Casotti
Polyunsaturated aldehydes (PUA) have recently been shown to induce reactive oxygen species (ROS) and possibly reactive nitrogen species (RNS, e.g., peroxynitrite) in the diatom Skeletonema marinoi (S. marinoi), which produces high amounts of PUA. We now are attempting to acquire better understanding of which reactive molecular species are involved in the oxidative response of S. marinoi to PUA. We used flow cytometry, the dye dihydrorhodamine 123 (DHR) as the main indicator of ROS (but which is also known to partially detect RNS), and different scavengers and inhibitors of both nitric oxide (NO) synthesis and superoxide dismutase activity (SOD)...
August 2016: Journal of Phycology
https://www.readbyqxmd.com/read/27020471/recent-advances-in-chemistry-and-pharmacology-of-2-methoxyestradiol-an-anticancer-investigational-drug
#20
REVIEW
B Sathish Kumar, Dushyant Singh Raghuvanshi, Mohammad Hasanain, Sarfaraz Alam, Jayanta Sarkar, Kalyan Mitra, Feroz Khan, Arvind S Negi
2-Methoxyestradiol (2ME2), an estrogen hormone metabolite is a potential cancer chemotherapeutic agent. Presently, it is an investigational drug under various phases of clinical trials alone or in combination therapy. Its anticancer activity has been attributed to its antitubulin, antiangiogenic, pro-apoptotic and ROS induction properties. This anticancer drug candidate has been explored extensively in last twenty years for its detailed chemistry and pharmacology. Present review is an update of its chemistry and biological activity...
June 2016: Steroids
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