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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
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
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
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
Anna L Eriksson, Anna S Wilhelmson, Johan 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 α (ER|ga). We measured serum E2 levels in orchidectomized WT mice treated with 2ME2 66.6 μ g/day, 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...
September 15, 2016: Endocrinology
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
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
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
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
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
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
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
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
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
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
Soledad Henríquez, Paulina Kohen, Xia Xu, Timothy D Veenstra, Alex Muñoz, Wilder A Palomino, Jerome F Strauss, Luigi Devoto
OBJECTIVE: To determine tissue concentrations of E2, estrone, P, and estrogens metabolites (EMs) 2-methoxyestradiol, 2-methoxyestrone, 4-hydroxyestrone, and 16-ketoestradiol in corpus luteum (CL) of different ages, and after hCG administration; and to examine the effects of EMs on vascular endothelial growth factor (VEGF) secretion and angiogenic activity released by cultured luteinizing granulosa cells in the presence and absence of hCG. DESIGN: Experimental study...
July 2016: Fertility and Sterility
Magdalena Gorska, Alicja Kuban-Jankowska, Jaroslaw Slawek, Michal Wozniak
The pathways leading to development of neurodegenerative disease and cancer cell death may overlap. Interestingly, the main neurodegeneration-causing factors have been suggested to play a pivotal role in the regulation of tumor growth. Another common component in neurodegenerations and cancer is nitro-oxidative stress. Depending on the environmental conditions, the nitro-oxidative stress may lead to cancerogenesis or cancer cell death. On the other side, it may also result in a variety of neurodegenerative diseases...
2016: Current Medicinal Chemistry
Anushka Dikshit, Chunqi Gao, Carrie Small, Karen Hales, Dale Buchanan Hales
Flaxseed has been studied for decades for its health benefits that include anti-cancer, cardio-protective, anti-diabetic, anti-inflammatory properties. The biologically active components that mediate these effects are the omega-3 fatty acids and the lignan, secoisolariciresinol diglucoside. We have previously shown that whole flaxseed supplemented diet decreases the severity and incidence of ovarian cancer while a 15% dose of flaxseed is most protective against inflammation and estrogen-induced chemical and genotoxicity...
May 2016: Journal of Steroid Biochemistry and Molecular Biology
Yongfu Zhang, Ping Li, Qi Gao, Tommaso Simoncini, Xiaodong Fu
2-Methoxyestradiol (2-ME) reduces atherosclerotic lesion formation. However, the underlying mechanisms remain largely unknown. In this work, we investigated the effect of 2-ME on monocyte adhesion to vascular endothelial cells. Lipopolysaccharides (LPS) greatly increased the attachment of monocyte onto cultured human umbilical vascular endothelial cells (HUVECs), which was inhibited by 2-ME in a dose- and time-dependent manner, or by the vascular cell adhesion protein-1 (VCAM-1) neutralizing antibody, suggesting that a functional releationship between 2-ME and VCAM-1 may exist...
July 2016: Gynecological Endocrinology
Eleftherios P Samartzis, Patrick Imesch, Anja Twiehaus, Raghvendra K Dubey, Brigitte Leeners
Endometriosis, a painful disorder associated with infertility, is estimated to occur in approximately 7-10% of reproductive age women. Although endometriosis is considered as an estrogen-dependent disease, the role of estrogen metabolites via receptor-independent mechanisms has not yet been comprehensively clarified. In the present study, growth studies were performed comparing the effect of estradiol (E2), estrogen metabolites, that is, 2-hydroxyestradiol (2-OHE2) and 2-methoxyestradiol (2-ME), as well as estrogen-receptor-independent mechanisms using the estrogen receptor antagonist fulvestrant, on cell proliferation of endometriotic cells...
July 2016: Gynecological Endocrinology
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