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2-methoxyestradiol

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https://www.readbyqxmd.com/read/29287795/hif-1%C3%AE-l-pgds-ppar%C3%AE-regulates-hypoxia-induced-anp-secretion-in-beating-rat-atria
#1
Xiang Li, Ying Zhang, Bo Zhang, Xia Liu, Lan Hong, Li-Ping Liu, Cheng-Zhe Wu, Xun Cui
Lipocalin-type prostaglandin D synthase (L-PGDS) and peroxisome proliferator activated receptor γ (PPARγ) play important roles in cardiovascular diseases. Nevertheless, effects of hypoxia-inducible factor 1α (HIF-1α) on L-PGDS and PPARγ protein levels and its role in hypoxia-induced atrial natriuretic peptide (ANP) secretion are unclear. In perfused beating rat atria, we observed that hypoxia significantly increased HIF-1α protein levels and stimulated ANP secretion, while upregulating L-PGDS. Hypoxia-induced ANP secretion was clearly attenuated by HIF-1α antagonist 2-methoxyestradiol, downregulating both HIF-1α and L-PGDS protein levels...
December 26, 2017: Prostaglandins & Other Lipid Mediators
https://www.readbyqxmd.com/read/29275365/2-methoxyestradiol-affects-mitochondrial-biogenesis-pathway-and-succinate-dehydrogenase-complex-flavoprotein-subunit-a-in-osteosarcoma-cancer-cells
#2
Magdalena Gorska-Ponikowska, Alicja Kuban-Jankowska, Stephan A Eisler, Ugo Perricone, Giosuè Lo Bosco, Giampaolo Barone, Stephan Nussberger
BACKGROUND/AIM: Dysregulation of mitochondrial pathways is implicated in several diseases, including cancer. Notably, mitochondrial respiration and mitochondrial biogenesis are favored in some invasive cancer cells, such as osteosarcoma. Hence, the aim of the current work was to investigate the effects of 2-methoxyestradiol (2-ME), a potent anticancer agent, on the mitochondrial biogenesis of osteosarcoma cells. MATERIALS AND METHODS: Highly metastatic osteosarcoma 143B cells were treated with 2-ME separately or in combination with L-lactate, or with the solvent (non-treated control cells)...
January 2018: Cancer Genomics & Proteomics
https://www.readbyqxmd.com/read/29242064/hypoxia-inducible-factor-1-in-clinical-and-experimental-aortic-aneurysm-disease
#3
Wei Wang, Baohui Xu, Haojun Xuan, Yingbin Ge, Yan Wang, Lixin Wang, Jianhua Huang, Weiguo Fu, Sara A Michie, Ronald L Dalman
OBJECTIVE: Mural angiogenesis and macrophage accumulation are two pathologic hallmarks of abdominal aortic aneurysm (AAA) disease. The heterodimeric transcription factor hypoxia-inducible factor 1 (HIF-1) is an essential regulator of angiogenesis and macrophage function. In this study, we investigated HIF-1 expression and activity in clinical and experimental AAA disease. METHODS: Human aortic samples were obtained from 24 AAA patients and six organ donors during open abdominal surgery...
December 11, 2017: Journal of Vascular Surgery
https://www.readbyqxmd.com/read/29227648/quinazolinone-based-anticancer-agents-synthesis-anti-proliferative-sar-anti-tubulin-activity-and-tubulin-co-crystal-structure
#4
Wolfgang Dohle, Fabrice L Jourdan, Gregory Menchon, Andrea E Prota, Paul A Foster, Pascoe Mannion, Ernest Hamel, Mark P Thomas, Philip G Kasprzyk, Eric Ferrandis, Michel O Steinmetz, Mathew P Leese, Barry V L Potter
Quinazolinone-based anti-cancer agents were designed, decorated with functional groups from a 2-methoxyestradiol-based microtubule disruptor series, incorporating the aryl sulfamate motif of steroid sulfatase (STS) inhibitors. The steroidal AB-ring system was mimicked, favoring conformations with an N-2 substituent occupying D-ring space. Evaluation against breast and prostate tumor cell lines identified 7b with DU-145 anti-proliferative activity (GI50 300 nM). A preliminary structure-activity relationship afforded compounds (e...
December 11, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29200966/microencapsulation-of-low-passage-poorly-differentiated-human-mucoepidermoid-carcinoma-cells-by-alginate-microcapsules-in-vitro-profiling-of-angiogenesis-related-molecules
#5
Sen Yang, Li-Juan Guo
Background: Human mucoepidermoid carcinoma (MEC) is regarded as the most common primary salivary malignancy. High-grade MEC has a high risk of recurrence and poor prognosis. Tumor angiogenesis, induced by poorly differentiated cancer cells of high-grade MEC, contributes to tumor growth and metastasis. Therefore, elucidating molecular mechanisms underlying the pro-angiogenic ability of poorly differentiated MEC cells is critical for the understanding of high-grade MEC progression. It is well known that three-dimensional (3D) cell culture, in contrast with conventional two-dimensional (2D) culture, provides a better approach to in vitro recapitulation of in vivo characteristics of cancer cells and their surrounding microenvironment...
2017: Cancer Cell International
https://www.readbyqxmd.com/read/29193609/endogenous-hormone-2-methoxyestradiol-suppresses-venous-hypertension-induced-angiogenesis-through-up-and-down-regulating-p53-and-id-1
#6
Xiang Zou, Li Zhang, Jie Yuan, Chunjie Yang, Zehan Wu, Jianping Song, Wei Zhu, Ying Mao, Liang Chen
Brain arteriovenous malformations (AVMs) which associate with angiogenesis due to local hypertension, chronic cerebral ischaemia and tissue hypoxia usually lead to haemorrhage, however, the therapeutic medicine for the disease is still lacking. 2-methoxyestradiol (2-ME) has been shown effective in the anti-angiogenic treatment. This study was conducted to examine whether and how 2-ME could improve the vascular malformations. Intracranial venous hypertension (VH) model produced in adult male Sprague-Dawley rats and culture of human umbilical vein endothelial cells (HUVECs) at the anoxia condition were used to induce in vivo and in vitro angiogenesis, respectively...
November 29, 2017: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/29110580/clinical-significance-of-low-2-methoxyestradiol-levels-in-serum-and-tissue-of-recurrent-juvenile-onset-laryngeal-papillomatosis
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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