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Taemoon Song, Ji Eun Park, Young Keun Chung
[Rh(COD)Cl]2/xantphos/Cs2CO3 efficiently catalyzes the reductive N-alkylation of aryl nitro compounds with alcohols by a borrowing-hydrogen strategy to afford the corresponding imine products in good to excellent yield. In the absence of xantphos, the [Rh(COD)Cl]2/Cs2CO3 catalytic system behaves as an effective catalyst for the dehydrogenative cou-pling of alcohols to esters, with nitrobenzene as hydrogen-acceptor. The reactivity of the rhodium catalytic system can be easily manipulated to selectively afford the imine or ester...
March 14, 2018: Journal of Organic Chemistry
Benjamin R Pittman-Polletta, Allison Quach, Ali I Mohammed, Michael Romano, Krishnakanth Kondabolu, Nancy J Kopell, Xue Han, Michelle M McCarthy
Cortico-basal ganglia-thalamic (CBT) β oscillations (15-30 Hz) are ele- vated in Parkinson's disease and correlated with movement disability. To date, no experimental paradigm outside of loss of dopamine has been able to specifically elevate β oscillations in the CBT loop. Here, we show that activation of striatal cholinergic receptors selectively increased β oscillations in mouse striatum and motor cortex. In individuals showing simultaneous β increases in both striatum and M1, β partial directed coherence (PDC) increased from striatum to M1 (but not in the reverse direction)...
March 12, 2018: European Journal of Neuroscience
Rui Huang, Jiawei Li, Dereje Kebebe, Yumei Wu, Bing Zhang, Zhidong Liu
Tumor-targeted delivery is considered a crucial component of current anticancer drug development and is the best approach to increase the efficacy and reduce the toxicity. Nanomedicine, particularly ligand-based nanoparticles have shown a great potential for active targeting of tumor. Cell penetrating peptide is one of the promising ligands in a targeted cancer therapy. In this study, the gambogic acid-loaded nanostructured lipid carrier (GA-NLC) was modified with two kinds of cell penetrating peptides (cRGD and RGERPPR)...
November 2018: Drug Delivery
Karolina Kubiasová, Václav Mik, Jaroslav Nisler, Martin Hönig, Alexandra Husičková, Lukáš Spíchal, Zuzana Pěkná, Olga Šamajová, Karel Doležal, Ondřej Plíhal, Eva Benková, Miroslav Strnad, Lucie Plíhalová
Isoprenoid cytokinins play a number of crucial roles in the regulation of plant growth and development. To study cytokinin receptor properties in plants, we designed and prepared fluorescent derivatives of 6-[(3-methylbut-2-en-1-yl)amino]purine (N6 -isopentenyladenine, iP) with several fluorescent labels attached to the C2 or N9 atom of the purine moiety via a 2- or 6-carbon linker. The fluorescent labels included dansyl (DS), fluorescein (FC), 7-nitrobenzofurazan (NBD), rhodamine B (RhoB), coumarin (Cou), 7-(diethylamino)coumarin (DEAC) and cyanine 5 dye (Cy5)...
March 7, 2018: Phytochemistry
Gregory T Sigurdson, Peipei Tang, M Mónica Giusti
The color expression of anthocyanins can be affected by a variety of environmental factors and structural characteristics. Anthocyanin acylation (type and number of acids) is known to be key, but the influence of acyl isomers (with unique stereochemistries) remains to be explored. The objective of this study was to investigate the effects of cis-trans configuration of the acylating group on the spectral and colorimetric properties of anthocyanins. Petunidin-3-rutinoside-5-glucoside (Pt-3-rut-5-glu) and Delphinidin-3-rutinoside-5-glucoside (Dp-3-rut-5-glu) and their cis and trans coumaroylated derivatives were isolated from black goji and eggplant, diluted in pH 1-9 buffers, and analyzed spectrophotometrically (380-700 nm) and colorimetrically (CIELAB) during 72 h of storage (25 °C, dark)...
March 7, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Eduardo Chagas Silva, Pramuditha L Abhayawardhana, Anatoliy V Lygin, Clark L Robertson, Mei Liu, Zhijun Liu, Raymond W Schneider
Although previous research showed that the purple symptom of Cercospora leaf blight (CLB) is associated with lower biomass of Cercospora cf. flagellaris and lower concentrations of cercosporin, a reactive oxygen species producer, as compared to blighted leaves, the hypothesis that the purple symptom is a plant reaction to the pathogen has never been tested. In this study, we demonstrated that high levels of coumestrol (COU) were associated with purple symptoms of CLB and that COU has strong antioxidant activity...
February 16, 2018: Phytopathology
Yihua Yang, Yingcai Meng, Enbo Zhang, Jinsong Ding
Lipid-polymer hybrid nanoparticles composed of polymer cores and lipid shells have been intensively studied as cancer drug delivery systems. The aim of the present study was to investigate the effect of phosphatidylcholine (PC) on physicochemical properties, stability and cellular uptake of lipid-poly(lactic-co-glycolic acid) (PLGA) hybrid nanoparticles. Coumarin-6 (cou-6) loaded hybrid nanoparticles (NPs) were prepared using PC with different alkyl chain lengths from C12 to C18, and were characterized by transmission electron microscopy (TEM), dynamic light scattering (DLS), and encapsulation efficiency (EE)...
July 1, 2018: Journal of Nanoscience and Nanotechnology
Xiaoxu Zhao, Zijing Ding, Jianyi Chen, Jiadong Dan, Sock Mui Poh, Wei Fu, Stephen J Pennycook, Wu Zhou, Kian Ping Loh
Manipulation of lattice strain is emerging as a powerful means to modify the properties of low dimensional materials. Most approaches rely on external forces to induce strain and the role of interlayer van der Waals (vdW) coupling in generating strain profiles in homo-bilayer transition metal dichalcogenides (TMDC) films is rarely considered. Here, by ap-plying atomic-resolution electron microscopy and density functional theory (DFT) calcula-tions, we observed that the mirror twin boundary (MTB) modifies the interlayer vdW cou-pling in bilayer TMDC films, leading to the development of local strain for a few nanome-ters in the vicinity of the MTB...
January 31, 2018: ACS Nano
D J Khalaf, C M Avilés, A A Azad, K Sunderland, T Todenhöfer, B J Eigl, D Finch, L Le, A Atwell, B Keith, C Kollmannsberger, K N Chi
INTRODUCTION: Recently, a prognostic index including six risk factors (RFs) (unfavourable ECOG performance status [PS], presence of liver metastases, short response to luteinizing hormone-releasing hormone [LHRH] agonists/antagonists, low albumin, increased alkaline phosphatase [ALP] and lactate dehydrogenase [LDH]) was developed from the COU-AA-301 trial in post-chemotherapy metastatic castration-resistant prostate cancer (mCRPC) patients treated with abiraterone acetate. Our primary objective was to evaluate this model in a cohort of chemotherapy-naive mCRPC patients receiving abiraterone...
December 1, 2017: Canadian Urological Association Journal, Journal de L'Association des Urologues du Canada
Yungan Tao, Anne Auperin, Christian Sire, Michel Martin, Marie-Gabrielle Saliou, Etienne Bardet, Xu Shan Sun, Thierry Chatellier, Clotilde Morand, Alexandre Cornely, Moussa Angokai, Alessia Di Rito, Ketty Kichenin, Pierre Blanchard, Ida D'Onofrio, Jean Bourhis
PURPOSE: Concomitant cetuximab and radiation therapy (RT) can induce severe radiodermatitis in patients with head and neck cancer (HNC). OTD70DERM, a regenerating agent (RGTA), is a structural and functional analogue of glycosaminoglycans. Preclinical studies have shown that topical RGTA can markedly reduce radiation-induced mucosal and cutaneous toxicities without tumor protection. The present study aimed to evaluate the effect of topical RGTA on radiodermatitis in patients with HNC undergoing RT and cetuximab, for whom RT-induced skin reactions are frequent and/or severe...
November 1, 2017: International Journal of Radiation Oncology, Biology, Physics
D Cella, S Traina, T Li, K Johnson, K F Ho, A Molina, N D Shore
Background: Patient-reported outcomes (PROs) are used to assess benefit-risk in drug development. The relationship between PROs and clinical outcomes is not well understood. We aimed to elucidate the relationships between changes in PRO measures and clinical outcomes in metastatic castration-resistant prostate cancer (mCRPC). Patients and methods: We investigated relationships between changes in self-reported fatigue, pain, functional well-being (FWB), physical well-being (PWB) and prostate cancer-specific symptoms with overall survival (OS) and radiographic progression-free survival (rPFS) after 6 and 12 months of treatment in COU-AA-301 (N = 1195) or COU-AA-302 (N = 1088)...
December 11, 2017: Annals of Oncology: Official Journal of the European Society for Medical Oncology
Elena S Izmailova, John A Wagner, Eric D Perakslis
The development of innovative wearable technologies has raised great interest in new means of data collection in healthcare and biopharmaceutical research and development. Multiple applications for wearables have been identified in a number of therapeutic areas; however, researchers face many challenges in the clinic, including scientific methodology as well as regulatory, legal, and operational hurdles. To facilitate further evaluation and adoption of these technologies, we highlight methodological and logistical considerations for implementation in clinical trials, including key elements of analytical and clinical validation in the specific context of use (COU)...
December 5, 2017: Clinical Pharmacology and Therapeutics
Makoto Yoritate, Yoshito Takahashi, Hayato Tajima, Chisato Ogihara, Takashi Yokoyama, Yasuki Soda, Takeshi Oishi, Takaaki Sato, Noritaka Chida
A unified total synthesis of stemoamide-type alkaloids is reported. Our synthetic approach features the chemoselective convergent assembly of five-membered building blocks via stemoamide as the common precursor to tetracyclic natural products. The synthesis consists of two successive coupling reactions of the three five-membered building blocks. The first coupling reaction is the vinylogous Michael addition/reduction sequence, which enables the gram-scale synthesis of stemoamide. The second coupling reaction is a chemoselective nucleophilic addition to stemoamide...
December 20, 2017: Journal of the American Chemical Society
Pankaj Dangle, Utsav Bansal, Rajeev Chaudhry, Glenn M Cannon, Francis X Schneck, Michael C Ost
OBJECTIVE: To elucidate the trends in urological causes for renal transplant in the pediatric population using a national database. Little is known about the specific pediatric urologic conditions and resultant trends that precede renal transplantation. MATERIAL AND METHODS: We reviewed the United Network for Organ Sharing (UNOS) database for pediatric patients (<18 years old) who underwent renal transplantation from January 1988- September 2015. We included those patients who received a renal transplant due to a urologic condition...
November 14, 2017: Urology
Felipe Q S Guerra, Rodrigo S A Araújo, Janiere P Sousa, Viviane A Silva, Fillipe O Pereira, Francisco J B Mendonça-Junior, José M Barbosa-Filho, Julio Abrantes Pereira, Edeltrudes O Lima
Fungal infections have become a concern for health professionals, and the emergence of resistant strains has been reported for all known classes of antifungal drugs. Among the fungi causing disease, we highlight those that belong to the genus Aspergillus. For these reasons, the search for new antifungals is important. This study examines the effects of a coumarin derivative, 4-acetatecoumarin (Cou-UMB16) both alone and together with antifungal drugs, and its mode of action against Aspergillus spp. Cou-UMB16 was tested to evaluate its effects on mycelia growth, and germination of Aspergillus spp...
October 12, 2017: Brazilian Journal of Microbiology: [publication of the Brazilian Society for Microbiology]
Yong Zhang, Jing Li, Weiqi Zhang, Rongsheng Wang, Qiaoqing Qiu, Feng Luo, Yasufumi Hikichi, Kouhei Ohnishi, Wei Ding
Hydroxycinnamic acids (HCAs) are typical monocyclic phenylpropanoids, including cinnamic acid (Cin), coumaric acid (Cou), caffeic acid (Caf), ferulic acid (FA) and their isomers, and involved in the interactions between pathogens and host plants. Here, we focused on the impact of HCAs on expression of type III secretion system (T3SS) in Ralstonia solanacearum. FA significantly induced the expression of the T3SS and some type III effectors (T3Es) genes in hrp-inducing medium, while did not the other HCAs. However, exogenously supplemented FA did not affect the T3SS expression in planta and the elicitation of the hypersensitive response (HR) in tobacco leaves...
2017: Frontiers in Plant Science
Kurt Miller, Joan Carles, Jürgen E Gschwend, Hendrik Van Poppel, Joris Diels, Sabine D Brookman-May
BACKGROUND: In the COU-AA-302 study (NCT00887198), abiraterone acetate plus prednisone (AAP) significantly improved outcomes in patients with metastatic castration-resistant prostate cancer (mCRPC) versus prednisone alone. Baseline clinical parameters predicting that treatment response could help inform clinical decisions were explored. OBJECTIVE: To identify patients who derive the greatest clinical benefit from AAP treatment. DESIGN, SETTING, AND PARTICIPANTS: A total of 1088 mCRPC patients treated with either AAP or prednisone in the first-line setting in COU-AA-302 were included in this post hoc analysis...
September 20, 2017: European Urology
Jing Tang, Jianming Li, Guo Li, Haitao Zhang, Ling Wang, Dai Li, Jinsong Ding
Idiopathic pulmonary fibrosis is a progressive, fatal lung disease with poor survival. The advances made in deciphering this disease have led to the approval of different antifibrotic molecules, such as pirfenidone and nintedanib. An increasing number of studies with particles (liposomes, nanoparticles [NPs], microspheres, nanopolymersomes, and nanoliposomes) modified with different functional groups have demonstrated improvement in lung-targeted drug delivery. In the present study, we prepared, characterized, and evaluated spermidine (Spd)-modified poly(lactic-co-glycolic acid) (PLGA) NPs as carriers for fluorofenidone (AKF) to improve the antifibrotic efficacy of this drug in the lung...
2017: International Journal of Nanomedicine
Jinyu Li, Guoxin Tan, Bingchao Cheng, Dandan Liu, Weisan Pan
To facilitate the hydrophobic drugs modeled by coumarin-6 (Cou-6) acrossing the cornea to the anterior chamber of the rabbit eye, chitosan (CS) derivatives including chitosan-N-acetyl-l-cysteine (CS-NAC), chitosan oligosaccharides (COS) and carboxymethyl chitosan (CMCS) modified nanostructured lipid carriers (NLCs) were designed and characterized. We found that, with similar size distribution and positivecharges, different CS derivatives based on NLCs led to distinctive delivery performance. In vivo precorneal retention study on rabbits revealed that these CS derivatives coating exhibited a stronger resistant effect than Cou-6 eye drops and Cou-6-NLC (P<0...
November 2017: European Journal of Pharmaceutics and Biopharmaceutics
Charles J Ryan, Thian Kheoh, Jinhui Li, Arturo Molina, Peter De Porre, Joan Carles, Eleni Efstathiou, Philip W Kantoff, Peter F A Mulders, Fred Saad, Kim N Chi
BACKGROUND: Radiographic progression-free survival (rPFS) is associated with overall survival (OS) in chemotherapy-naïve metastatic castration-resistant prostate cancer (mCRPC) patients. Using readily assessable baseline clinical and laboratory parameters, we developed a prognostic index model for rPFS in chemotherapy-naïve mCRPC patients without visceral disease who were treated with abiraterone acetate plus prednisone. METHODS: Data from the abiraterone acetate plus prednisone arm of COU-AA-302 were used...
July 25, 2017: Clinical Genitourinary Cancer
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