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George Wu, Dan Powers, Stanley Yeung, Frank Chen, Kelly Neelon
Prophylaxis or therapy with a combination of a neurokinin 1 (NK-1) receptor antagonist (RA), a 5-hydroxytryptamine- 3 (5-HT3) RA, and dexamethasone is recommended by international antiemesis guidelines for the prevention of chemotherapy-induced nausea and vomiting for patients receiving highly emetogenic chemotherapy and for select patients receiving moderately emetogenic chemotherapy. VARUBI (rolapitant) is a substance P/NK-1 RA that was recently approved by the U.S. Food and Drug Administration as an injectable emulsion in combination with other antiemetic agents in adults for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy...
January 2018: International Journal of Pharmaceutical Compounding
Anran Hu, Chen Chen, Michael D Mantle, Bettina Wolf, Lynn F Gladden, Ali Rajabi-Siahboomi, Shahrzad Missaghi, Laura Mason, Colin D Melia
PURPOSE: Investigate the extended release behaviour of compacts containing mixtures of hydrophilic HPMC and PEO in hydrating media of differing ionic strengths. METHODS: The extended release behaviour of various HPMC:PEO compacts was investigated using dissolution testing, confocal microscopy and magnetic resonance imaging, with respect to polymer ratio and ionic strength of the hydrating media. RESULTS: Increasing HPMC content gave longer extended release times, but a greater sensitivity to high ionic dissolution environments...
May 2017: Pharmaceutical Research
Ebru Goncu, Ramazan Uranlı, Gozde Selek, Osman Parlak
Steroid hormone 20-hydroxyecdysone is known as the systemic regulators of insect cells; however, how to impact the fate and function of mature and stem cells is unclear. For the first time, we report ecdysone regulatory cascades in both mature midgut cell and stem cell fractions related to developmental events by using histological, immunohistochemical, biochemical and gene expression analysis methods. Ecdysone receptor-B1 (EcR-B1) and ultraspiracle 1 (USP-1) mRNAs were detected mainly in mature cells during programmed cell death (PCD)...
2016: Journal of Insect Science
Anne Olazabal-Herrero, Iraia García-Santisteban, Jose Antonio Rodríguez
Ubiquitin-specific protease (USP)1 is a member of the USP family of deubiquitinating enzymes. Efficient USP1 activity requires binding to its cofactor USP1-associated factor 1 (UAF1), and the USP1-UAF1 deubiquitinase complex has important roles in regulating DNA damage-related processes. USPs show common folding of their catalytic domain, with three subdomains termed Thumb, Palm, and Fingers. The Fingers subdomain appears to be the primary site for ubiquitin binding. In USP1, the Fingers subdomain also mediates its interaction with UAF1, and thus represents a crucial, but poorly characterized, motif in USP1...
March 2016: FEBS Journal
Jinjun Cao, Yichen Liu, Yuhui Yang, Huaijiang Zhang, Zhen Li, Qingpo Yang, Songdou Zhang, Qingwen Zhang, Xiaoxia Liu
Ecdysteroids play an important role in the growth, development, and reproduction of insects. The ecdysteroid signal is transduced through a heterodimeric complex of two nuclear receptors: the ecdysone receptor (EcR) and the ultraspiracle (USP). To investigate the role of USP during the development of Grapholita molesta, ultraspiracle (USP) cDNA was obtained from the transcriptome of G. molesta and verified by PCR. The deduced amino acid sequence of G. molesta USP (GmUSP) was highly homologous to those of other lepidopterans, especially the Manduca sexta USP-1 isoform...
December 2015: Comparative Biochemistry and Physiology. Part B, Biochemistry & Molecular Biology
Leandro Vairo, Emiliano Medei, Danúbia S Dos Santos, Deivid C Rodrigues, Regina C S Goldenberg, Antonio C Campos De Carvalho
Pluripotent mouse embryonic stem cells (mESC) are cell lines derived from the inner cell mass of blastocyst-stage early mammalian embryos. Since ion channel modulation has been reported to interfere with both growth and differentiation process in mouse and human ESC it is important to characterize the electrophysiological properties of newly generated mESC and compare them to other lines. In this work, we studied the intercellular communication by way of gap junctions in a Brazilian derived mESC (USP-1, generated by Dr...
March 2015: Anais da Academia Brasileira de Ciências
Weiting Yang, Tao Tian, Hong-Yue Wu, Qing-Jiang Pan, Song Dang, Zhong-Ming Sun
Six uranyl phosphonates and sulfonates have been hydrothermally synthesized, namely, (H2tib)[(UO2)3(PO3C6H5)4]·2H2O (UPhP-1), Zn(pi)2(UO2)(PO3C6H5)2 (UPhP-2), Zn(dib)(UO2)(PO3C6H5)2·2H2O (UPhP-3), (HTEA)[(UO2)(5-SP)] (USP-1), (Hdib)2[(UO2)2(OH)(O)(5-SP)] (USP-2), and Zn(phen)3(UO2)2(3-SP)2 (USP-3) (tib = 1,3,5-tri(1H-imidazol-1-yl)benzene, pi = 1-phenyl-1H-imidazole, dib = 1,4-di(1H-imidazol-1-yl)benzene, TEA = triethylamine, phen = 1,10-phenanthroline, 5-SP = 5-sulfoisophthalic acid, and 3-SP = 3-sulfoisophthalic acid)...
March 4, 2013: Inorganic Chemistry
Weizhao Yang, Yin Qi, Ke Bi, Jinzhong Fu
BACKGROUND: Understanding how organisms adapt to high-elevation environments at a genome scale provides novel insights into the process of adaptive evolution. Previous studies have mainly focused on endothermic organisms, while poikilothermic species may have evolved different mechanisms to cope with high-elevation environments. In this context, we sequenced transcriptomes of a pair of closely related anuran species, Rana chensinensis and R. kukunoris, which inhabit respective low- and high-elevation habitats...
2012: BMC Genomics
Hywel D Williams, Kevin P Nott, David A Barrett, Rob Ward, Ian J Hardy, Colin D Melia
"Biorelevant" media for the fed stomach, including fat emulsions, are routinely used during in vitro testing of solid dosage forms. However, their complexity undoubtedly creates difficulties in identifying factors which affect drug release. Here, we show fats can directly influence drug release from hydroxypropyl methylcellulose (HPMC; Methocel K4M) matrices which are often subjected to biorelevant testing. Model fat systems included milk (0.1%-3.5% fat) and the parenteral emulsion Intralipid® (20%-30% fat)...
November 2011: Journal of Pharmaceutical Sciences
Sang Min Nam, Chan Young Im, Hyung Keun Lee, Eung Kweon Kim, Tae-Im Kim, Kyoung Yul Seo
OBJECTIVE: To compare the reliability and the agreement in measuring central corneal thickness (CCT) using the following technologies: RTVue Fourier-domain optical coherence tomography (Optovue, Inc., Fremont, CA), Pentacam (Oculus, Inc., Wetzlar, Germany), and ultrasonic pachymetry (USP; Pocket-II; Quantel Medical, Inc., Bozeman, MT). DESIGN: Evaluation of diagnostic test. PARTICIPANTS: One hundred four eyes of 52 healthy subjects (mean age ± standard deviation, 28...
November 2010: Ophthalmology
Vivian Gray, Gregg Kelly, Min Xia, Chris Butler, Saji Thomas, Stephen Mayock
Since its inception, the dissolution test has come under increasing levels of scrutiny regarding its relevance, especially to the correlation of results to levels of drug in blood. The technique is discussed, limited to solid oral dosage forms, beginning with the scientific origins of the dissolution test, followed by a discussion of the roles of dissolution in product development, consistent batch manufacture (QC release), and stability testing. The ultimate role of dissolution testing, "to have the results correlated to in vivo results or in vivo in vitro correlation," is reviewed...
June 2009: Pharmaceutical Research
Michael D Kraft, Cary E Johnson, Christopher Chung, Frank Julian
PURPOSE: The stability of metoprolol tartrate injection 1 mg/mL undiluted and 0.5 mg/mL in 0.9% sodium chloride injection and 5% dextrose injection was studied. METHODS: Sample set A contained 50 mL of Metoprolol Tartrate Injection, USP, 1 mg/mL transferred directly from the vials. Sample set B contained 50 mL of metoprolol 0.5 mg/mL diluted with 0.9% sodium chloride injection, and sample set C contained 50 mL of metoprolol 0.5 mg/mL diluted with 5% dextrose. All samples were prepared in triplicate and stored at room temperature...
April 1, 2008: American Journal of Health-system Pharmacy: AJHP
T Sekimoto, M Iwami, S Sakurai
Programmed cell death (PCD) in Bombyx mori anterior silk glands (ASGs) is triggered by 20-hydroxyecdysone (20E). We examined the expression profiles and effects of 20E on 11 transcription factor genes in the fifth instar to determine whether they demonstrate the hierarchical control seen in Drosophila PCD. Results indicate that EcR-A and usp-2, but not EcR-B1 or usp-1, may be components of the ecdysone receptor complex. Up-regulation of E75A, BHR3, and three BR-C isoforms, but not E75B, appeared to be associated with the induction of PCD...
June 2006: Insect Molecular Biology
Judy A Schnurr, Kathleen K Storey, Hans-Joachim G Jung, David A Somers, John W Gronwald
Arabidopsis UDP-sugar pyrophosphorylase (AtUSP) is a broad substrate enzyme that synthesizes nucleotide sugars. The products of the AtUSP reaction can act as precursors for the synthesis of glycolipids, glycoproteins, and cell wall components including pectin and hemicellulose. AtUSP has no close homologs in Arabidopsis and its biological function has not been clearly defined. We identified two T-DNA insertional mutant lines for AtUSP, usp-1 and usp-2. No homozygous individuals were identified and progeny from plants heterozygous for usp-1 or usp-2 showed a 1:1 segregation ratio under selection...
August 2006: Planta
Kiyoshi Hiruma, Lynn M Riddiford
MHR3 is an ecdysone-inducible transcription factor whose expression in both Manduca sexta epidermis and the Manduca GV1 cell line is induced by 20-hydroxyecdysone (20E) in vitro. There are four putative ecdysone response elements (EcRE) in the 2.6-kb flanking region of the MHR3 promoter. The most proximal, EcRE1, is necessary for activation of the promoter by 20E in the GV1 cells because the mutation of EcRE1 caused the loss of responsiveness to 20E. Previous studies showed that EcR-B1/USP-1 bound only to EcRE1 and high levels of this complex increased the 20E-induced activation, whereas the presence of high USP-2 prevented this increased activation...
August 15, 2004: Developmental Biology
X Sun, Q Song, B Barrett
Tebufenozide and methoxyfenozide have been previously shown to significantly reduce fecundity and cause vitellogenin accumulation in hemolymph of the codling moth Cydia pomonella L. In the present study, the effects of these ecdysone agonists, tebufenozide and methoxyfenozide, on the expression of ecdysone receptor (EcR), ultraspiracle protein (USP) and other proteins in the ovaries of C. pomonella L., were investigated at both the translational and/or transcriptional levels with an aim to elucidate the mechanisms by which the fecundity was reduced...
August 2003: Insect Biochemistry and Molecular Biology
M A Sukoyan, A Y Kerkis, M R B Mello, I E Kerkis, J A Visintin, L V Pereira
Embryonic stem cells are totipotent cells derived from the inner cell mass of blastocysts. Recently, the development of appropriate culture conditions for the differentiation of these cells into specific cell types has permitted their use as potential therapeutic agents for several diseases. In addition, manipulation of their genome in vitro allows the creation of animal models of human genetic diseases and for the study of gene function in vivo. We report the establishment of new lines of murine embryonic stem cells from preimplantation stage embryos of 129/Sv mice...
May 2002: Brazilian Journal of Medical and Biological Research, Revista Brasileira de Pesquisas Médicas e Biológicas
M J Behnen, L A West, F R Liewehr, T B Buxton, J C McPherson
The purpose of this study was to evaluate the antimicrobial activity of several calcium hydroxide (Ca(OH)2) preparations in root canal dentin infected with Enterococcus faecalis. Roots of extracted bovine incisors were prepared to standardized cylindrical test specimens of 5 mm in height; the smear layer was removed, and the specimens were incubated for 24 h at 37 degrees C in bacteriological culture medium that contained 7.0 x 10(4) colony forming units per milliliter of E. faecalis. The specimens were mounted in individual 4-mm diameter culture wells, and the test material was applied to fill the canal lumen...
December 2001: Journal of Endodontics
Q Lan, K Hiruma, X Hu, M Jindra, L M Riddiford
MHR3, a homolog of the retinoid orphan receptor (ROR), is a transcription factor in the nuclear hormone receptor family that is induced by 20-hydroxyecdysone (20E) in the epidermis of the tobacco hornworm, Manduca sexta. Its 2.7-kb 5' flanking region was found to contain four putative ecdysone receptor response elements (EcREs) and a monomeric (GGGTCA) nuclear receptor binding site. Activation of this promoter fused to a chloramphenicol acetyltransferase (CAT) reporter by 2 micrograms of 20E per ml in Manduca GV1 cells was similar to that of endogenous MHR3, with detectable CAT by 3 h...
July 1999: Molecular and Cellular Biology
K Hiruma, T Shinoda, F Malone, L M Riddiford
Insect molting and metamorphosis are orchestrated by ecdysteroids with juvenile hormone (JH) preventing the actions of ecdysteroids necessary for metamorphosis. During the molt and metamorphosis of the dorsal abdominal epidermis of the tobacco hornworm, Manduca sexta, the isoforms involved in the ecdysone receptor (EcR)/Ultraspiracle (USP) complex change with the most dramatic switch being the loss of USP-1 and the appearance of USP-2 during the larval and pupal molts. We show here that this switch in USP isoforms is mediated by high 20-hydroxyecdysone (20E) and that the presence of JH is necessary for the down-regulation of USP-1 mRNA...
January 1999: Development Genes and Evolution
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