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2-methoxyestradiol

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https://www.readbyqxmd.com/read/29110580/clinical-significance-of-low-2-methoxyestradiol-levels-in-serum-and-tissue-of-recurrent-juvenile-onset-laryngeal-papillomatosis
#1
Danling Liu, Jiadong Wang, Yanan Xu
Objective We aim to explore the correlation between serum and tissue 2-methoxyestradiol (2-ME-2) levels and recurrence of juvenile-onset respiratory papillomatosis (JORRP). Study Design Retrospective cohort studies. Settings Laboratory of Otolaryngology, Department of Head and Neck Surgery, Renji Hospital, School of Medicine, Shanghai Jiaotong University. Subjects and Methods Sixty-four patients diagnosed with JORRP in our department from January 2007 to December 2012 were enrolled. Patients were divided into recurrence and nonrecurrence groups, with 32 patients in each group...
November 1, 2017: Otolaryngology—Head and Neck Surgery
https://www.readbyqxmd.com/read/29109098/2-methoxyestradiol-reverses-the-pro-carcinogenic-effect-of-l-lactate-in-osteosarcoma-143b-cells
#2
REVIEW
Magdalena Gorska-Ponikowska, Alicja Kuban-Jankowska, Agnieszka Daca, Stephan Nussberger
BACKGROUND/AIM: According to the reverse Warburg effect, tumor cells may metabolize lactate as an energy source and shuttle L-lactate to neighboring cancer cells, adjacent stroma, and vascular endothelial cells, thus inducing metabolic reprogramming. An increased tumor L-lactate level strictly correlates with increased metastasis, tumor recurrence and a poor outcome. A potent anticancer agent that may act on L-lactate activated cells is 2-metoxyestradiol. Thus, the aim of the study was to evaluate whether a potent anticancer agent, 2-methoxyestradiol, is able to reverse L-lactate-induced metabolic reprogramming in osteosarcoma 143B cells...
November 2017: Cancer Genomics & Proteomics
https://www.readbyqxmd.com/read/29054710/novel-p-carborane-containing-multitarget-anticancer-agents-inspired-by-the-metabolism-of-17%C3%AE-estradiol
#3
Asako Kaise, Kiminori Ohta, Yasuyuki Endo
The female hormone 17 β-estradiol (E2) is synthesized from estrone by steroid sulfatase (STS), and metabolized into 2-methoxyestradiol (2-ME), whereby the biological activity of the latter is substantially different from that of E2. Based on the metabolic pathways of E2, a carborane-containing 2-ME mimic (1c) and its derivatives (1 and 2) were designed and synthesized as novel multitarget anticancer agents. Bissulfamate 1f exhibited potent STS-inhibitory activity and tubulin-polymerization-inhibitory activity...
October 12, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29031938/design-synthesis-and-antiproliferative-effect-of-17%C3%AE-amide-derivatives-of-2-methoxyestradiol-and-their-studies-on-pharmacokinetics
#4
Xiufang Shi, Zhihao Wang, Feng Xu, Xiang Lu, Haifeng Yao, Dandan Wu, Shuaijun Sun, Ruifang Nie, Shuo Gao, Panpan Li, Liwen Xia, Zhenzhong Zhang, Cong Wang
A series of 17β-amide-2-methoxyestradiol compounds were synthesized with an aim to enhance the antiproliferative effect of 2-methoxyestradiol. The antiproliferative activity of 2-methoxyestradiol analogs against human cancer cells was investigated. 2-methoxy-3-benzyloxy-17β-chloroacetamide-1,3,5(10)-triene (5e) and 2-methoxy-3-hydroxy-17β-butyramide-1,3,5(10)-triene (6c) had comparable or better antitumor activity than 2-methoxyestradiol. The elimination half-life of 6c (t1/2β=240.93min) is ten times longer than 2-ME and the area under the curve was seven times (AUC0-tmin=2068...
October 12, 2017: Steroids
https://www.readbyqxmd.com/read/28817836/sitting-physical-activity-and-serum-oestrogen-metabolism-in-postmenopausal-women-the-women-s-health-initiative-observational-study
#5
Hannah Oh, Hannah Arem, Charles E Matthews, Nicolas Wentzensen, Kerryn W Reding, Louise A Brinton, Garnet L Anderson, Sally B Coburn, Jane A Cauley, Chu Chen, Deborah Goodman, Ruth M Pfeiffer, Roni T Falk, Xia Xu, Britton Trabert
BACKGROUND: Prolonged sitting and lower levels of physical activity have been associated with increased levels of parent oestrogens (oestrone and oestradiol), the key hormones in female cancers, in postmenopausal women. However, it is unknown whether sitting and physical activity are associated with circulating oestrogen metabolite levels. METHODS: Among 1804 postmenopausal women enrolled in the Women's Health Initiative Observational Study, 15 serum oestrogens/oestrogen metabolites were quantified using liquid chromatography-tandem mass spectrometry...
September 26, 2017: British Journal of Cancer
https://www.readbyqxmd.com/read/28810190/design-synthesis-and-biological-evaluation-of-novel-2-methoxyestradiol-analogs-as-dual-selective-estrogen-receptor-modulators-serms-and-antiangiogenic-agents
#6
Kejing Lao, Yejun Wang, Mingqi Chen, Jingjing Zhang, Qidong You, Hua Xiang
2-methoxyestradiol is a novel agent showing both anti-angiogenic and vascular disrupting properties. In this study, a series of 11α-substituted 2-methoxyestradiol analogs have been designed and synthesized targeting dual ERα and microtubulin. Biological evaluation was performed on their anti-proliferative activities against 5 different cell lines. The results indicated that most compounds exhibited good activities, in which compound 24c and 30c showed the best activity with low micromolar IC50 (2.73 μM -7...
October 20, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28801594/deficiency-in-catechol-o-methyltransferase-is-linked-to-a-disruption-of-glucose-homeostasis-in-mice
#7
Megumi Kanasaki, Swayam Prakash Srivastava, Fan Yang, Ling Xu, Sumiyo Kudoh, Munehiro Kitada, Norikazu Ueki, Hyoh Kim, Jinpeng Li, Satoru Takeda, Keizo Kanasaki, Daisuke Koya
2-methoxyestradiol (2-ME), an estrogen metabolite generated via catechol-o-methyltransferase (COMT), is multifunctional methoxy-catechol. Here, we report that COMT deficiency leads to glucose intolerance and 2-ME rescues COMT-deficient-associated metabolic defects. Liver COMT protein was suppressed in high fat diet (HFD)-fed or in pregnant mice. COMT suppression, by Ro41-0960 or siRNA, in HFD fed mice or in pregnant mice exacerbated glucose intolerance; 2-ME intervention ameliorated these defects. 2-ME effects on glucose tolerance were associated with AMPK phosphorylation in the liver and in islet cells...
August 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28795302/novel-combination-of-2-methoxyestradiol-and-cyclophosphamide-enhances-the-antineoplastic-and-pro-apoptotic-effects-on-s-180-ascitic-tumour-cells
#8
Srabantika Mallick, Atish Barua, Goutam Paul, Samarendra Nath Banerjee
Sarcoma 180 (S-180) tumour cell line is a stable murine tumour cell line with 98-99% stumour takes capacity in Swiss albino mouse - Mus musculus. 2 Methoxyestradiol (2ME) - a promising anti-neoplastic and anti-angiogenic agent, showed toxicity to host body in higher concentration. Cyclophosphamide (CP), the anti-neoplastic agent has long been used as a chemotherapeutic drug for treatment of different cancers. Our studies have shown that the combination effect of 2ME and CP on S-180 tumour cell line is anti-proliferative and less toxic...
August 10, 2017: Journal of Cell Communication and Signaling
https://www.readbyqxmd.com/read/28729825/dexmedetomidine-protects-mouse-brain-from-ischemia-reperfusion-injury-via-inhibiting-neuronal-autophagy-through-up-regulating-hif-1%C3%AE
#9
Cong Luo, Ming-Wen Ouyang, Ying-Ying Fang, Shu-Ji Li, Quan Zhou, Jun Fan, Zai-Sheng Qin, Tao Tao
Stroke is the leading cause of death in China and produces a heavy socio-economic burden in the past decades. Previous studies have shown that dexmedetomidine (DEX) is neuroprotective after cerebral ischemia. However, the role of autophagy during DEX-mediated neuroprotection after cerebral ischemia is still unknown. In this study, we found that post-conditioning with DEX and DEX+3-methyladenine (3-MA) (autophagy inhibitor) reduced brain infarct size and improved neurological deficits compared with DEX+RAPA (autophagy inducer) 24 h after transient middle cerebral artery artery occlusion (tMCAO) model in mice...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28693141/effect-of-2-methoxyestradiol-on-sk-lms-1-uterine-leiomyosarcoma-cells
#10
Ji-Sun Lee, Changhwan Ahn, Hee Young Kang, Eui-Bae Jeung
An endogenous metabolite of 17β-estradiol, 2-methoxyestradiol (2-ME), has affinity for estrogen receptors. This compound was reported to be a promising antitumor drug due to its anti-proliferative effects on a wide range of tumor cell types. Numerous previous studies have been performed to evaluate the cytotoxic effects of 2-ME on tumor cell lines in following the induction of G2/M cell cycle arrest and subsequent apoptosis. Uterine leiomyosarcoma (ULMS) is a relatively rare malignant smooth muscle cell tumor that develops in the uterus muscle layer...
July 2017: Oncology Letters
https://www.readbyqxmd.com/read/28624453/folic-acid-attenuates-cobalt-chloride-induced-pge2-production-in-huvecs-via-the-no-hif-1alpha-cox-2-pathway
#11
Yuming Liang, Xiaozhou Zhen, Kaiwen Wang, Jing Ma
Prostaglandin E2 (PGE2), an important lipid inflammatory mediator involved in the progression of vascular diseases, can be induced by hypoxia in many cell types. While folic acid has been shown to protect against inflammation in THP-1 cells during hypoxia and hypoxia-induced endothelial cell injury, whether it might do so by attenuating PGE2 production remains unclear. To investigate this we constructed a hypoxia-induced injury model by treating human umbilical vein endothelial cells (HUVECs) with cobalt chloride (CoCl2), which mimics the effects of hypoxia...
August 19, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28612593/dosimetric-comparison-between-single-and-dual-arc-volumetric-modulated-arc-radiotherapy-and-intensity-modulated-radiotherapy-for-nasopharyngeal-carcinoma-using-a-simultaneous-integrated-boost-technique
#12
Sivakumar Radhakrishnan, Anuradha Chandrasekaran, Yugandhar Sarma, Saranganathan Balakrishnan, Janardhan Nandigam
Backround: Plan quality and performance of dual arc (DA) volumetric modulated arc therapy (VMAT) , single arc (SA) VMAT and nine field (9F) intensity modulated radiotherapy were compared using a simultaneous integrated boost (SIB) technique. Methods: Twelve patients treated in Elekta Synergy Platform (mlci2) by 9F-IMRT were replanned with SA/DA-VMAT using a CMS Monaco Treatment Planning System (TPS) with Monte Carlo simulation. Target delineation was conducted as per Radiation Therapy Oncology Protocols (RTOG0225 and 0615)...
May 1, 2017: Asian Pacific Journal of Cancer Prevention: APJCP
https://www.readbyqxmd.com/read/28565876/effects-of-17%C3%AE-estradiol-and-2-methoxyestradiol-on-the-oxidative-stress-hypoxia-inducible-factor-1-pathway-in-hypoxic-pulmonary-hypertensive-rats
#13
Li Wang, Quan Zheng, Yadong Yuan, Yanpeng Li, Xiaowei Gong
The present study aimed to investigate the effects of 17β-estradiol (E2) and 2-methoxyestradiol (2ME) on the oxidative stress-hypoxia inducible factor-1 (OS-HIF-1) pathway in hypoxic pulmonary hypertensive rats. Female Sprague-Dawley rats were divided randomly into 4 groups, as follows: i) Control (Group A); ii) ovariectomy (OVX) + hypoxia (Group B); iii) OVX + hypoxia + E2 injection (Group C); and iv) 2ME injection (Group D). The rats were maintained under hypoxic conditions for 8 weeks, and mean pulmonary artery pressure (mPAP) and pulmonary arteriole morphology were measured...
May 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28555342/microchip-electrophoresis-with-laser-induced-fluorescence-detection-for-the-determination-of-the-ratio-of-nitric-oxide-to-superoxide-production-in-macrophages-during-inflammation
#14
Giuseppe Caruso, Claudia G Fresta, Joseph M Siegel, Manjula B Wijesinghe, Susan M Lunte
It is well known that excessive production of reactive oxygen and nitrogen species is linked to the development of oxidative stress-driven disorders. In particular, nitric oxide (NO) and superoxide (O2(•-)) play critical roles in many physiological and pathological processes. This article reports the use of 4-amino-5-methylamino-2',7'-difluorofluorescein diacetate and MitoSOX Red in conjunction with microchip electrophoresis and laser-induced fluorescence detection for the simultaneous detection of NO and O2(•-) in RAW 264...
July 2017: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/28536432/nuclear-translocation-of-hif-1%C3%AE-induced-by-influenza-a-h1n1-infection-is-critical-to-the-production-of-proinflammatory-cytokines
#15
Xinkun Guo, Zhaoqin Zhu, Wanju Zhang, Xiaoxiao Meng, Yong Zhu, Peng Han, Xiaohui Zhou, Yunwen Hu, Ruilan Wang
Infection with the influenza A (H1N1) virus is a major challenge for public health because it can cause severe morbidity and even mortality in humans. The over-secretion of inflammatory cytokines (cytokine storm) is considered to be a key contributor to the severe pneumonia caused by H1N1 infection. It has been reported that hypoxia-inducible factor 1-alpha (HIF-1α) is associated with the production of proinflammatory molecules, but whether HIF-1α participates in the acute inflammatory responses against H1N1 infection is still unclear...
May 24, 2017: Emerging Microbes & Infections
https://www.readbyqxmd.com/read/28536143/aurora-kinase-a-promotes-ar-degradation-via-the-e3-ligase-chip
#16
Sukumar Sarkar, David L Brautigan, James M Larner
Reducing the levels of the androgen receptor (AR) is one of the most viable approaches to combat castration-resistant prostate cancer. Previously, we observed that proteasomal-dependent degradation of AR in response to 2-methoxyestradiol (2-ME) depends primarily on the E3 ligase C-terminus of HSP70-interacting protein (STUB1/CHIP). Here, 2-ME stimulation activates CHIP by phosphorylation via Aurora kinase A (AURKA). Aurora A kinase inhibitors and RNAi knockdown of Aurora A transcript selectively blocked CHIP phosphorylation and AR degradation...
August 2017: Molecular Cancer Research: MCR
https://www.readbyqxmd.com/read/28511459/a-comparison-of-2-methoxyestradiol-value-in-women-with-severe-preeclampsia-versus-normotensive-pregnancy
#17
John Wantania, Ahsanuddin Attamimi, Rukmono Siswishanto
INTRODUCTION: Preeclampsia is a pregnancy complication characterized by high blood pressure and proteinuria. Endothelial dysfunction is a major theory suggested as its aetiology. It is caused by anti-angiogenic condition characterized by low Vascular Endothelial Growth Factor (VEGF). An estradiol metabolite, called 2-Methoxy Estradiol (2-ME), is produced with the help of Catechol-O-Methyltransferase (COMT). This substance has an important role in VEGF expression. A 2-ME is suppressed in women with preeclampsia...
March 2017: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/28461606/catechol-o-methyltransferase-deficiency-leads-to-hypersensitivity-of-the-pressor-response-against-angiotensin-ii
#18
COMPARATIVE STUDY
Norikazu Ueki, Keizo Kanasaki, Megumi Kanasaki, Satoru Takeda, Daisuke Koya
Catechol-O-methyltransferase (COMT) metabolizes 2-hydroxyestradiol into 2-methoxyestradiol (2-ME); COMT deficiency has shown to be associated with hypertension in men and preeclampsia, the disease associated with hypersensitivity of pressor response against angiotensin II (Ang II). Here, we found that COMT deficiency could explain the hypersensitivity of pressor response against Ang II in mice because of the lack of 2-ME-dependent suppression of angiotensin II receptor type 1 (AT1R). Male C57BL/6 mice were subjected to COMT inhibitor (COMTi: 25 mg/kg per day) or oil (control) for 4 weeks, with or without low-dose Ang II infusion (ANGII: 70 ng/kg per minute) for the last 3 weeks...
June 2017: Hypertension
https://www.readbyqxmd.com/read/28416586/2-methoxyestradiol-a-17%C3%AE-estradiol-metabolite-with-gender-independent-therapeutic-potential
#19
EDITORIAL
Raghvendra K Dubey
No abstract text is available yet for this article.
June 2017: Hypertension
https://www.readbyqxmd.com/read/28416584/2-methoxyestradiol-reduces-angiotensin-ii-induced-hypertension-and-renal-dysfunction-in-ovariectomized-female-and-intact-male-mice
#20
COMPARATIVE STUDY
Ajeeth K Pingili, Karen N Davidge, Shyamala Thirunavukkarasu, Nayaab S Khan, Akemi Katsurada, Dewan S A Majid, Frank J Gonzalez, L Gabriel Navar, Kafait U Malik
Cytochrome P450 1B1 protects against angiotensin II (Ang II)-induced hypertension and associated cardiovascular changes in female mice, most likely via production of 2-methoxyestradiol. This study was conducted to determine whether 2-methoxyestradiol ameliorates Ang II-induced hypertension, renal dysfunction, and end-organ damage in intact Cyp1b1(-/-), ovariectomized female, and Cyp1b1(+/+) male mice. Ang II or vehicle was infused for 2 weeks and administered concurrently with 2-methoxyestradiol. Mice were placed in metabolic cages on day 12 of Ang II infusion for urine collection for 24 hours...
June 2017: Hypertension
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