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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
#1
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 = 240.93 min) 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/28841308/palladium-ii-chloride-complexes-of-n-n-disubstituted-imidazole-2-thiones-syntheses-structures-and-catalytic-performances-in-suzuki-miyaura-and-sonogashira-coupling-reactions
#2
Li-Ming Zhang, Hai-Yan Li, Hong-Xi Li, David James Young, Yong Wang, Jian-Ping Lang
Reactions of PdCl2 with 2 equiv of N,N'-disubstituted-imidazole-2-thiones R(1)R(2)C3N2S (R(1) = R(2) = Me (1a), (i)Pr (1b), Cy (1c), C6Me3H2 (1d); R(1) = Me, R(2) = Ph (1e)) under the different conditions afford five mononuclear complexes trans-[(R(1)R(2)C3N2S)2PdCl2] (R(1) = R(2) = Me (2a), (i)Pr (2b), Cy (2c), C6Me3H2 (2d); R(1) = Me, R(2) = Ph (2e)) and five binuclear Pd(II) complexes [(PdCl2){μ-(R(1)R(2)C3N2S)}]2 (R(1) = R(2) = Me (3a), (i)Pr (3b), Cy (3c), C6Me3H2 (3d); R(1) = Me, R(2) = Ph (3e)), respectively...
August 25, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28809416/heteroleptic-nickel-ii-dinhc-complexes-and-an-unusual-reverse-carbene-transfer-reaction-to-silver-i
#3
Han Vinh Huynh, Christine Hui Min Koh, Van Ha Nguyen
A series of rare [NiX2((Me)CCprop)] complexes bearing the cis-chelating benzimidazole-derived dicarbene ligand (Me)CCprop and varying anionic coligands (2, X = N3; 3, X = NCS; 4, X = I; 5, X = O2CCF3) have been prepared and coligand dependent structural and spectroscopic features have been evaluated. This study also revealed an unusual 'reverse' carbene transfer reaction from nickel to silver giving the disilver species [Ag2X2(μ-κ(2-Me)CCprop)] (6, X = OAc; 7, X = O2CCF3). A preliminary catalytic study of two representative Ni(II) diNHC complexes in the aqueous and phosphine-free Suzuki-Miyaura coupling reaction of aryl halides is reported as well...
August 29, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/28801594/deficiency-in-catechol-o-methyltransferase-is-linked-to-a-disruption-of-glucose-homeostasis-in-mice
#4
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/28698966/two-skin-cell-lines-from-wild-type-and-albino-japanese-flounder-paralichthys-olivaceus-establishment-characterization-virus-susceptibility-efficient-transfection-and-application-to-albinism-study
#5
Ruoqing Wang, Nianwei Zhang, Renkai Wang, Shengpeng Wang, Na Wang
In order to provide an applicable cell platform to study fish pathology and skin pigmentation, two cell lines derived from skin tissues of wild-type and albino Japanese flounder were established and named JFSK_wt and JFSK_alb, respectively. These two cell lines were cultured for 45 passages within approximately 300 days. JFSK_wt and JFSK_alb cells were maintained in Dulbecco's Modified Eagle's Medium and Ham's F-12 Nutrient Mixture (DMEM/F12) supplemented with antibiotics, fetal bovine serum (FBS), 2-mercaptoethanol (2-Me), N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid (HEPES), and basic fibroblast growth factor (bFGF)...
December 2017: Fish Physiology and Biochemistry
https://www.readbyqxmd.com/read/28693141/effect-of-2-methoxyestradiol-on-sk-lms-1-uterine-leiomyosarcoma-cells
#6
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/28671476/molecular-group-13-metallaborates-derived-from-m-o-m-cleavage-promoted-by-bh3
#7
Erandi Bernabé-Pablo, Vojtech Jancik, Diego Martínez-Otero, Joaquín Barroso-Flores, Mónica Moya-Cabrera
The reaction of metalloxanes [{(Me)LM(OH)}2(μ-O)] [M = Al (1), Ga (2); (Me)L = CH{CMe(NAr)}2(-), Ar = 2,4,6-Me3C6H2, Me = methyl] with an excess of BH3·D (D = tetrahydrofuran (THF), SMe2) affords annular metallaborate systems achieved through M-O-M cleavage. Compound 1 led exclusively to the formation of eight-membered ring systems [{(Me)LAl(μ-O){B(O(n)Bu)}(μ-O)}2] (3) and [{(Me)LAl(μ-O)(BH)(μ-O)}2] (6), while for 2 the unprecedented six-membered ring systems [{((Me)LGa)2(μ-O)}(μ-O)2{B(O(n)Bu)}] (4) and [((Me)LGa)(μ-O)2{(BO(n)Bu)2(μ-O)}] (5) were observed...
July 17, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28669142/polymorphism-in-the-intron-20-of-porcine-o-linked-n-acetylglucosamine-transferase
#8
Jong Gug Kim, Dan Nonneman, Doo-Wan Kim, Sangsu Shin, Gary A Rohrer
OBJECTIVE: O-linked N-acetylglucosamine (O-GlcNAc) transferase (OGT) catalyzes the addition of O-GlcNAc and GlcNAcylation has extensive crosstalk with phosphorylation to regulate signaling and transcription. Pig OGT is located near the region of chromosome X that affects follicle stimulating hormone level and testes size. The objective of this study was to find the variations of OGT between European and Chinese pigs. METHODS: Pigs were tested initially for polymorphism in OGT among European and Chinese pigs by polymerase chain reaction and sequencing at the U...
August 2017: Asian-Australasian Journal of Animal Sciences
https://www.readbyqxmd.com/read/28666718/performance-of-microbiological-serological-molecular-and-modified-seminal-plasma-methods-in-the-diagnosis-of-brucella-abortus-in-semen-and-serum-of-bovine-bulls
#9
G Nardi Júnior, J Megid, L A Mathias, L Paulin, A F Vicente, A Cortez, F J P Listoni, G H B Lara, R G Motta, M G M Chacur, F M Monteiro, M G Ribeiro
Brucellosis remains as a major infectious disease of domestic animals and is considered a re-emerging zoonosis in several countries. B. abortus infections in bulls are related to reproductive tract infections, although infected animals show transient serological titers or nonreactor status. Thus, diagnosis of bovine brucellosis based exclusively on serological tests probably underestimates B. abortus infections in bulls. In this scenario, three hundred thirty-five serum samples from reproductively mature bovine bulls were subjected simultaneously to standard serodiagnosis using the rose Bengal test (RBT), 2-mercaptoethanol (2-ME), complement fixation (CFT), and fluorescence polarization assay (FPA)...
June 27, 2017: Biologicals: Journal of the International Association of Biological Standardization
https://www.readbyqxmd.com/read/28617500/decamethyltitanocene-hydride-intermediates-in-the-hydrogenation-of-the-corresponding-titanocene-%C3%AE-2-ethene-or-%C3%AE-2-alkyne-complexes-and-the-effects-of-bulkier-auxiliary-ligands
#10
Jiří Pinkas, Róbert Gyepes, Ivana Císařová, Jiří Kubišta, Michal Horáček, Karel Mach
(1)H NMR studies of reactions of titanocene [Cp*2Ti] (Cp* = η(5)-C5Me5) and its derivatives [Cp*(η(5):η(1)-C5Me4CH2)TiMe] and [Cp*2Ti(η(2)-CH2[double bond, length as m-dash]CH2)] with excess dihydrogen at room temperature and pressures lower than 1 bar revealed the formation of dihydride [Cp*2TiH2] (1) and the concurrent liberation of either methane or ethane, depending on the organometallic reactant. The subsequent slow decay of 1 yielding [Cp*2TiH] (2) was mediated by titanocene formed in situ and controlled by hydrogen pressure...
June 27, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/28536143/aurora-kinase-a-promotes-ar-degradation-via-the-e3-ligase-chip
#11
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...
May 23, 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
#12
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/28468327/quasi-living-polymerization-of-propene-with-an-isotactic-specific-zirconocene-catalyst
#13
Kei Nishii, Miyuki Murase, Takeshi Shiono
Propene polymerization with isotactic (iso)-specific C₂-symmetric rac-Me₂Si(2-Me-Benz(e)-Ind)₂ZrCl₂ (1) and rac-Me₂Si(2-Me-4-Ph-1-Ind)₂ZrCl₂ (2) were conducted under various conditions for achieving iso-specific living polymerization of propene. When Complex 1 was activated with trialkylaluminum-free modified methylaluminoxane (dMMAO) at -40 °C, the number-average molecular weight (Mn) linearly increased against the polymerization time to reach Mn = 704,000 within 15 min of polymerization, although the molecular weight distributions was broad (Mw/Mn < 3)...
May 2, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28461606/catechol-o-methyltransferase-deficiency-leads-to-hypersensitivity-of-the-pressor-response-against-angiotensin-ii
#14
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/28396280/high-oral-bioavailability-of-2-methoxyestradiol-in-peg-plga-micelles-microspheres-for-cancer-therapy
#15
XinHong Guo, CaiPing Chen, Xin Liu, PanPan Hou, XiaoNan Guo, Fang Ding, ZhiHao Wang, YuRong Hu, Zhi Li, ZhenZhong Zhang
The development of effective oral preparations of 2-methoxyestradiol (2-ME) has been a worldwide problem. In this study, breakthrough progress has been made in oral delivery of 2-ME by encapsulating 2-ME micelles in pH-responsive microspheres. 2-ME micelles with small particle size (58 nm) and high drug loading (7.94±0.23%) were successfully prepared and showed slower release characteristics and 12.8 times higher cytotoxicity on 4T1 cells than free 2-ME. The pH-sensitive microspheres could slowly release 82% of 2-ME micelles for 10 h in PBS (7...
April 7, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28376733/efficacy-of-intravitreal-injection-of-2-methoxyestradiol-in-regression-of-neovascularization-of-a-retinopathy-of-prematurity-rat-model
#16
COMPARATIVE STUDY
Azza Mohamed Ahmed Said, Rania Gamal Eldin Zaki, Rania A Salah Eldin, Maha Nasr, Samar Saad Azab, Yaser Abdelmageuid Elzankalony
BACKGROUND: Retinopathy of prematurity (ROP) is one of the targets for early detection and treatment to prevent childhood blindness in world health organization programs. The purpose of study was to evaluate the efficacy of intravitreal injection of 2-Methoxyestradiol (2-ME) nanoemulsion in regressing neovascularization of a ROP rat model. METHODS: A prospective comparative case - control animal study conducted on 56 eyes of 28 healthy new born Sprague Dawley male albino rat...
April 4, 2017: BMC Ophthalmology
https://www.readbyqxmd.com/read/28342193/metabolism-of-the-tryptamine-derived-new-psychoactive-substances-5-meo-2-me-dalt-5-meo-2-me-alcht-and-5-meo-2-me-dipt-and-their-detectability-in-urine-studied-by-gc-ms-lc-ms-n-and-lc-hr-ms-ms
#17
Achim T Caspar, Jonas B Gaab, Julian A Michely, Simon D Brandt, Markus R Meyer, Hans H Maurer
Many N,N-dialkylated tryptamines show psychoactive properties and were encountered as new psychoactive substances. The aims of the presented work were to study the phase I and II metabolism and the detectability in standard urine screening approaches (SUSA) of 5-methoxy-2-methyl-N,N-diallyltryptamine (5-MeO-2-Me-DALT), 5-methoxy-2-methyl-N-allyl-N-cyclohexyltryptamine (5-MeO-2-Me-ALCHT), and 5-methoxy-2-methyl-N,N-diisopropyltryptamine (5-MeO-2-Me-DIPT) using GC-MS, LC-MS(n) , and LC-HR-MS/MS. For metabolism studies, urine was collected over a 24-h period after administration of the compounds to male Wistar rats at 20 mg/kg body weight (BW)...
March 24, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28319723/occurrence-of-and-exposure-to-benzothiazoles-and-benzotriazoles-from-textiles-and-infant-clothing
#18
Wenbin Liu, Jingchuan Xue, Kurunthachalam Kannan
Benzothiazoles (BTHs) and benzotriazoles (BTRs) are used in a wide range of applications, including rubber vulcanization and corrosion inhibition. Limited studies have reported the occurrence of BTHs and BTRs in textiles, including children's clothing. In this study, 79 textile samples (raw as well as tailored) collected in Albany, New York, USA, were analyzed to determine the occurrence of BTH, BTR and their seven common derivatives. BTH, 2-methylthio-benzothiazole (2-Me-S-BTH) and 2-hydroxy-benzothiazole (2-OH-BTH) were found in textiles at a detection rate (DR) of 86%, 54% and 19%, respectively...
March 15, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28214920/detection-of-brucella-sp-infection-through-serological-microbiological-and-molecular-methods-applied-to-buffaloes-in-maranh%C3%A3-o-state-brazil
#19
Larissa Sarmento Dos Santos, Joicy Cortez Sá, Diego Luiz Dos Santos Ribeiro, Nancyleni Pinto Chaves, Juliana Pinto da Silva Mol, Renato Lima Santos, Tatiane Alves da Paixão, Alcina Vieira de Carvalho Neta
The aim of the current study is to diagnose Brucella spp. infection using methods such as serology, bacterial isolation, and molecular analysis in buffaloes bred in Maranhão State. In order to do so, 390 samples of buffalo serum were subjected to serological tests, to Rose Bengal Plate Test (RBPT) and to 2-mercaptoethanol (2-ME) combined with slow agglutination test (SAT). Vaginal swabs were collected from seropositive animals and subjected to bacterial isolation and to generic PCR. According to the serological test, 16 animals had a positive reaction to the confirmatory test (2-ME/SAT)...
April 2017: Tropical Animal Health and Production
https://www.readbyqxmd.com/read/28128569/potential-energy-curves-for-the-low-lying-electronic-states-of-k2-from-ab-initio-calculations-with-all-electrons-correlated
#20
Patrycja Skupin, Monika Musiał, Stanisław A Kucharski
The electron affinity (EA) calculations based on the equation-of-motion coupled cluster method proved to be an efficient scheme in the treatment of potential energy curves (PECs) for alkali molecular ions, Me2(+). The EA approach provides description of states obtained by an attachment of one electron to the reference, which for the Me2(+) is a doubly ionized Me2(+2) system. The latter has a very concrete advantage in the calculations of the PECs, since it dissociates into the closed-shell fragments (Me2(+2) → Me(+) + Me(+)); hence, the restricted Hartree-Fock reference can be used in the whole range of interatomic distances...
February 8, 2017: Journal of Physical Chemistry. A
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