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https://www.readbyqxmd.com/read/28626480/development-of-dry-powder-inhaler-containing-tadalafil-loaded-plga-nanoparticles
#1
Jaleh Varshosaz, Somayeh Taymouri, Hamed Hamishehkar, Razieh Vatankhah, Shadi Yaghubi
Inhalable dry powders containing poly lactic-co-glycolic acid (PLGA) nanoparticles (NPs) were developed for the delivery of tadalafil (TAD) for treatment of life-treating pulmonary arterial hypertension. Taguchi design was employed to evaluate the effects of different formulation variables on the physicochemical characteristics of PLGA-NPs prepared using emulsion solvent evaporation method. Inhalable PLGA-NPs of TAD were successfully prepared by co-spray drying the PLGA-NPs with inert carriers. Physicochemical characteristics and in vitro deposition of the aerosolized drug were also evaluated...
June 2017: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28615380/leucine-differentially-regulates-gene-specific-translation-in-mouse-skeletal-muscle
#2
Micah J Drummond, Paul T Reidy, Lisa M Baird, Brian K Dalley, Michael T Howard
Background: Amino acids, especially leucine, are particularly effective in promoting protein synthesis. Leucine is known to increase the rate of protein synthesis in skeletal muscle through the mechanistic target of rapamycin complex 1-dependent, as well as -independent, signaling pathways. However, the overall translation program is poorly defined, and it is unknown how the activation of these pathways differentially controls the translation of specific mRNAs.Objective: Ribosome profiling and RNA sequencing were used to precisely define the translational program activated by an acute oral dose of leucine...
June 14, 2017: Journal of Nutrition
https://www.readbyqxmd.com/read/28613839/visualization-of-endoplasmic-reticulum-aminopeptidase-1-under-different-redox-conditions-with-two-photon-fluorescent-probe
#3
Shuai Xu, Hong-Wen Liu, Xiao-Xiao Hu, Shuang-Yan Huan, Jing Zhang, Yongchao Liu, Lin Yuan, Feng-Li Qu, Xiao-Bing Zhang, Weihong Tan
Endoplasmic reticulum aminopeptidase 1 (ERAP1), a metallopeptidase belonging to M1 peptidase families, plays an important role in antigen processing in vivo. Actually, many diseases are caused by ERAP1 perturbation. Thus an efficient method for monitoring its content is extremely important for disease diagnosis and treatment. However, few fluorescent probes have been reported for efficient monitoring ERAP1 in living cells and tissues. In this work, a two-photon fluorescent probe (SNCL) containing 1, 8-naphthalimide (two-photon fluorophore), L-leucine (triggered moiety) and methyl sulphonamide moiety (endoplasmic reticulum-targeting group) for imaging ERAP1 activity in living cells was reported for the first time...
June 14, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28612342/effect-of-glycine-nitrogen-on-lettuce-growth-under-soilless-culture-a-metabolomics-approach-to-identify-the-main-changes-occurred-in-plant-primary-and-secondary-metabolism
#4
Xiao Yang, Lei Feng, Li Zhao, Xiaosong Liu, Danial Hassani, Danfeng Huang
BACKGROUND: Lettuce is a significant source of antioxidants and bioactive compounds. Nitrate is a cardinal fertilizer in horticulture and influences vegetable yield and quality; however, the negative effects of nitrate on the biosynthesis of flavonoids require further study. It is expected that using fertilizers containing organic N could promote the synthesis of health-promoting compounds. RESULTS: Lettuces were hydroponically cultured in media containing 9 mM nitrate or 9 mM glycine for 4 weeks...
June 14, 2017: Journal of the Science of Food and Agriculture
https://www.readbyqxmd.com/read/28609632/enantioselective-one-pot-synthesis-of-%C3%AE-%C3%AE-epoxy-ketones-via-aerobic-oxidation-of-cyclopropanols
#5
Gábor Zoltán Elek, Victor Borovkov, Margus Lopp, Dzmitry G Kananovich
An efficient, mild, and environmentally benign method was developed for the asymmetric synthesis of 2-oxyranyl ketones from easily available tertiary cyclopropanols. The one-pot protocol includes the aerobic oxidation of cyclopropanol derivatives catalyzed by Mn(III) complexes followed by the poly-l-leucine-assisted stereoselective elimination of water from the intermediate peroxides with DBU to afford the corresponding epoxy ketones in high yields and good-to-excellent enantioselectivities (up to 97%).
June 13, 2017: Organic Letters
https://www.readbyqxmd.com/read/28606810/tailored-design-of-multifunctional-and-programmable-ph-responsive-self-assembling-polypeptides-as-drug-delivery-nanocarrier-for-cancer-therapy
#6
Tzu-Wei Wang, Chia-Wei Yeh, Chen-Hsiang Kuan, Li-Wen Wang, Liang-Hsin Chen, Hsi-Chin Wu, Jui-Shen Sun
Breast cancer has become the second leading cause of cancer-related mortality in female wherein more than 90% of breast cancer-related death results from cancer metastasis to distant organs at advanced stage. The purpose of this study is to develop biodegradable nanoparticles composed of natural polypeptides and calcium phosphate (CaP) with sequential pH-responsivity to tumor microenvironments for active targeted drug delivery. Two different amphiphilic copolymers, poly(ethylene glycol)3400-aconityl linkage-poly(l-glutamic acid)15-poly(l-histidine)10-poly(l-leucine)10 and LyP1-poly(ethylene glycol)1100-poly(l-glutamic acid)15-poly(l-histidine)10-poly(l-leucine)10, were exploited to self-assemble into micelles in aqueous phase...
June 9, 2017: Acta Biomaterialia
https://www.readbyqxmd.com/read/28583333/dry-powder-formulation-of-kanamycin-with-enhanced-aerosolization-efficiency-for-drug-resistant-tuberculosis
#7
Mohammad A M Momin, Shubhra Sinha, Ian G Tucker, Colin Doyle, Shyamal C Das
BACKGROUND: Kanamycin, an injectable agent, is currently used to treat drug-resistant tuberculosis (TB). Parenteral kanamycin causes high systemic toxicity which could be avoided by direct delivery to the lungs. This study focused on producing a highly aerosolizable dry-powder of hygroscopic kanamycin by spray-drying with l-leucine. METHODS: Kanamycin powders were prepared with different concentrations (0, 5, 10, 15 and 20% w/w) of l-leucine using the Buchi B-290 Mini Spray-Dryer...
June 3, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28552878/medium-chain-triglycerides-in-combination-with-leucine-and-vitamin-d-benefit-cognition-in-frail-elderly-adults-a-randomized-controlled-trial
#8
Sakiko Abe, Osamu Ezaki, Motohisa Suzuki
The combined supplementation of medium-chain triglycerides (MCTs), L-leucine-rich amino acids, and cholecalciferol (vitamin D3) increase muscle strength and function in frail elderly individuals. However, their effects on cognition are unknown. We enrolled 38 elderly nursing home residents (mean age±SD, 86.6±4.8 y) in a 3-mo randomized, controlled, parallel group trial. The participants were randomly allocated to 3 groups: the first group received a L-leucine (1.2 g)- and cholecalciferol (20 μg)-enriched supplement with 6 g of MCT (LD+MCT); the second group received the same supplement with 6 g of long-chain triglycerides (LD+LCT); and the third group did not receive any supplements (control)...
2017: Journal of Nutritional Science and Vitaminology
https://www.readbyqxmd.com/read/28551425/effects-of-coating-materials-and-processing-conditions-on-flow-enhancement-of-cohesive-acetaminophen-powders-by-high-shear-processing-with-pharmaceutical-lubricants
#9
Guoguang Wei, Sharad Mangal, John Denman, Thomas Gengenbach, Kevin Lee Bonar, Rubayat Islam Khan, Li Qu, Tonglei Li, Qi Tony Zhou
This study has investigated the surface coating efficiency and powder flow improvement of a model cohesive acetaminophen powder by high shear processing with pharmaceutical lubricants via two common equipment, conical comil and high shear mixer. Effects of formulation and processing parameters on powder flow and surface coating coverage were evaluated. Both Carr's index and shear cell data indicated that processing with the lubricants using comil or high shear mixer substantially improved the flow of the cohesive acetaminophen powder...
May 24, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28536139/effects-of-leucine-supplementation-and-resistance-training-on-myopathy-of-diabetic-rats
#10
Carlos Eduardo C Martins, Vanessa B de S Lima, Brad J Schoenfeld, Julio Tirapegui
Leucine supplementation and resistance training positively influence the protein translation process and the cell signaling mTOR (mammalian target of rapamycin) pathway that regulates muscle protein balance and muscle remodeling, and thus may be therapeutic to diabetic myopathy. However, the effect of a combined intervention has not been well studied. Forty male Wistar rats were divided into five groups, control (C), diabetic control (D), diabetic + trained (DT), diabetic + L-leucine (DL), diabetic + L-leucine + trained (DLT)...
May 2017: Physiological Reports
https://www.readbyqxmd.com/read/28514978/jugular-infused-methionine-lysine-and-branched-chain-amino-acids-does-not-improve-milk-production-in-holstein-cows-experiencing-heat-stress
#11
K R Kassube, J D Kaufman, K G Pohler, J W McFadden, A G Ríus
Poor utilization of amino acids contributes to losses of milk protein yield in dairy cows exposed to heat stress (HS). Our objective was to test the effect of essential amino acids on milk production in lactating dairy cows exposed to short-term HS conditions. To achieve this objective, 12 multiparous, lactating Holstein cows were assigned to two environments (thermoneutral (THN) or HS) from days 1 to 14 in a split-plot type cross-over design. All cows received 0 g/day of essential amino acids from days 1 to 7 (negative control (NC)) followed by an intravenous infusion of l-methionine (12 g/day), l-lysine (21 g/day), l-leucine (35 g/day), l-isoleucine (15 g/day) and l-valine (15 g/day, methionine, lysine and branched-chain amino acids (ML+BCAA)) from days 8 to 14...
May 18, 2017: Animal: An International Journal of Animal Bioscience
https://www.readbyqxmd.com/read/28508902/non-zeolitic-properties-of-the-dipeptide-l-leucyl-l-leucine-as-a-result-of-the-specific-nanostructure-formation
#12
Marat A Ziganshin, Aisylu S Safiullina, Sufia A Ziganshina, Alexander V Gerasimov, Valery V Gorbatchuk
The non-zeolitic behavior of l-leucyl-l-leucine and its self-organization in solid state and from solutions with the formation of different nanostructures are reported. This dipeptide forms porous crystals, but does not exhibit molecular sieve effects typical of classical zeolites and biozeolites. The specific sorption properties of l-leucyl-l-leucine result from a change in its crystal packing from channel-type to layered-type, when binding strong proton acceptors or proton donors of molecular size greater than 18-20 cm(3) mol(-1)...
May 31, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28503045/review-of-angiotensin-converting-enzyme-inhibitory-assay-rapid-method-in-drug-discovery-of-herbal-plants
#13
REVIEW
Islamudin Ahmad, Arry Yanuar, Kamarza Mulia, Abdul Mun'im
The renin-angiotensin-aldosterone system is a signaling pathway which responsible in the blood pressure regulation. Angiotensin-converting enzyme (ACE) is one of the key elements responsible for the hypertensive mechanism. It converts angiotensin-I to angiotensin-II. The discovery history of the ACE inhibitory activity assay method has been through a long stage for decades and development continues until today. The ACE inhibitory activity has become an effective screening method in the search for new antihypertensive agents from herbal plants...
January 2017: Pharmacognosy Reviews
https://www.readbyqxmd.com/read/28494385/l-leucine-dietary-supplementation-modulates-muscle-protein-degradation-and-increases-pro-inflammatory-cytokines-in-tumour-bearing-rats
#14
Bread Cruz, André Oliveira, Maria Cristina Cintra Gomes-Marcondes
Cancer cachexia is characterised by involuntary weight loss associated with systemic inflammation and metabolic changes. Studies aimed at maintaining lean body mass in cachectic tumour-bearing hosts have made important contributions reducing the number of deaths and improving the quality of life. In recent years, leucine has demonstrated effective action in maintaining lean body mass by decreasing muscle protein degradation. Currently, there is a growing need to understand how leucine stimulates protein synthesis and acts protectively in a cachectic organism...
May 8, 2017: Cytokine
https://www.readbyqxmd.com/read/28448887/macro-raman-spectroscopy-for-bulk-composition-and-homogeneity-analysis-of-multi-component-pharmaceutical-powders
#15
Hui Wang, David Barona, Sulayman Oladepo, Lisa Williams, Susan Hoe, David Lechuga-Ballesteros, Reinhard Vehring
A new macro-Raman system equipped with a motorized translational sample stage and low-frequency shift capabilities was developed for bulk composition and homogeneity analysis of multi-component pharmaceutical powders. Different sampling methods including single spot and scanning measurement were compared. It was found that increasing sample volumes significantly improved the precision of quantitative composition analysis, especially for poorly mixed powders. The multi-pass cavity of the macro-Raman system increased effective sample volumes by 20 times from the sample volume defined by the collection optics, i...
April 23, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28422213/revisiting-the-juli%C3%A3-colonna-enantioselective-epoxidation-supramolecular-catalysis-in-water
#16
Christopher Bérubé, Xavier Barbeau, Patrick Lagüe, Normand Voyer
We describe an efficient epoxidation process leading to chiral epoxyketones using the reusable homo-oligopeptide poly-l-leucine (PLL) in pure water, without any organic co-solvent. A range of substituted epoxyketones can be accessed with good conversions and high enantioselectivities. Based on the experimental results and computational studies, we propose a mechanism that demonstrates the importance of both the α-helical structure and the presence of a hydrophobic groove of the homo-oligopeptide catalyst for reactivity and selectivity...
May 4, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28410993/development-of-a-novel-recombinant-lhrh-fusion-protein-for-therapy-of-androgen-and-estrogen-dependent-cancers
#17
Jagdish C Gupta, Rohit S Hada, P Sahai, G P Talwar
LHRH based vaccines are promising candidates for therapy of androgen and estrogen dependent cancers. We report in this communication development of a novel recombinant protein vaccine candidate against LHRH. A synthetic gene was designed in which the codon sequence in the LHRH decapeptide was modified by substituting the codon for 6-glycine with that of l-leucine. Further the LHRH(6leu) gene was linked to heat-labile enterotoxin of E. coli (LTB) as carrier. This LHRH(6leu)-LTB gene was cloned into a prokaryotic expression vector under the control of inducible and strong bacteriophage T7 promoter to over-express LHRH(leu) fused to LTB as recombinant protein in E...
June 2017: Protein Expression and Purification
https://www.readbyqxmd.com/read/28395537/three-new-amino-acid-derivatives-from-edible-mushroom-pleurotus-ostreatus
#18
Xiao-Jie Lu, Bao-Min Feng, Shao-Fei Chen, Dan Zhao, Gang Chen, Hai-Feng Wang, Yue-Hu Pei
Three new amino acid derivatives, oxalamido-L-phenylalanine methyl ester (1), oxalamido-L-leucine methyl ester (2), and lumichrome hydrolyzate (3), together with nine known compounds (4-12), were isolated from the solid culture of edible mushroom Pleurotus ostreatus. Their structures were elucidated on the basis of extensive spectroscopic analysis. The absolute configurations of 1 and 2 were established by the chiral synthesis and confirmed by circular dichroism (CD) analysis of their total synthesis products and natural isolates...
April 11, 2017: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/28393748/gut-microbiota-of-mice-putatively-modifies-amino-acid-metabolism-in-the-host-brain
#19
Takahiro Kawase, Mao Nagasawa, Hiromi Ikeda, Shinobu Yasuo, Yasuhiro Koga, Mitsuhiro Furuse
Recently, it has been found that the gut microbiota influences functions of the host brain by affecting monoamine metabolism. The present study focused on the relationship between the gut microbiota and the brain amino acids. Specific pathogen-free (SPF) and germ-free (GF) mice were used as experimental models. Plasma and brain regions were sampled from mice at 7 and 16 weeks of age, and analysed for free d- and l-amino acids, which are believed to affect many physiological functions. At 7 weeks of age, plasma concentrations of d-aspartic acid (d-Asp), l-alanine (l-Ala), l-glutamine (l-Gln) and taurine were higher in SPF mice than in GF mice, but no differences were found at 16 weeks of age...
April 10, 2017: British Journal of Nutrition
https://www.readbyqxmd.com/read/28387471/arrangement-of-proteinogenic-%C3%AE-amino-acids-on-a-cyclic-peptide-comprising-alternate-biphenyl-cored-%C3%AE-amino-acids
#20
Shohei Tashiro, Masayuki Chiba, Mitsuhiko Shionoya
Aiming at precisely arranging several proteinogenic α-amino acids on a folded scaffold, we have developed a cyclic hexapeptide comprising an alternate sequence of biphenyl-cored ζ-amino acids and proteinogenic α-amino acids such as l-leucine. The amino acids were connected by typical peptide synthesis, and the resultant linear hexapeptide was intramolecularly cyclized to form a target cyclic peptide. Theoretical analyses and NMR spectroscopy suggested that the cyclic peptide was folded into an unsymmetrical conformation, and the structure was likely to be flexible in CHCl3 ...
May 18, 2017: Chemistry, An Asian Journal
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