A Nonpeptidic Reverse-Turn Scaffold Stabilized by Urea-Based Dual Intramolecular Hydrogen Bonding

Medda, Amiya K.,Park, Chul Min,Jeon, Aram,Kim, Hyunwoo,Sohn, Jeong-Hun,Lee, Hee-Seung American Chemical Society 2011 ORGANIC LETTERS Vol.13 No.13

<P>A novel nonpeptidic reverse-turn scaffold containing urea fragments that are connected by a conformationally constrained <SMALL>d</SMALL>-prolyl-<I>cis</I>-1,2-diaminocyclohexane (<SMALL>d</SMALL>-Pro-DACH) linker is reported. The scaffold adopts a well-defined reverse-turn conformation that is stabilized by dual intramolecular hydrogen bonding in both solution and solid states.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/orlef7/2011/orlef7.2011.13.issue-13/ol201247x/production/images/medium/ol-2011-01247x_0007.gif'></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/ol201247x'>ACS Electronic Supporting Info</A></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/ol201247x'>ACS Electronic Supporting Info</A></P>

Hub Status and Indexation of Container Ports

박용안,Francesca MEDDA 한국해운물류학회 2015 The Asian journal of shipping and Logistics Vol.31 No.2

Although ports play a traditional role as loading and connecting centers for cargo and passengers, container ports as intermodal junctions have undergone continuous and diverse changes since the late 1950s as a result of technological advancements and transport network expansion. In order to shed light on the port transformation process, the objective of the present paper is to develop a hub index for container ports to evaluate the hub status of container ports within shipping networks, inland networks, and various logistics services. This study develops two sub-indexes of port classification and capacity, and combines cases of these two sub-indexes into various types in order to find a proper port hub index. The paper demonstrates how different types of port hub index are useful measurements for evaluating outputs and inputs of container ports. In a case analysis we show that the indexes of period variables and lagged variables have more explanatory power with regard to changes of port throughputs and high correlation with inputs.

Cardiac Autonomic Control and Neural Arousal as Indexes of Fatigue in Professional Bus Drivers

Lecca, Luigi I.,Fadda, Paolo,Fancello, Gianfranco,Medda, Andrea,Meloni, Michele Occupational Safety and Health Research Institute 2022 Safety and health at work Vol.13 No.2

Background: Bus driving is a mentally demanding activity that requires prolonged attention to ensure safety. The aim of the study was to assess mental fatigue caused by driving a public bus and to find a profile of workers at higher risk. Methods: We evaluated changes of critical flicker fusion (CFF) (index of central arousal) and heart rate variability (HRV) (index of autonomic balance) in a 6-hour driving shift on a real route, in 31 professional bus drivers, and we tested the influence of personal factors such as sleep quality, BMI, and age. Paired t-test was used to test differences of CFF and HRV between both initial and final phase of driving, while multiple linear regression tested the influence of personal variables on the indexes of mental fatigue. Results: Results showed that CFF significantly decreased after 6 hours of bus driving (41.91 Hz, sd 3.31 vs. 41.15 Hz, sd 3.15; p = 0.041), and heart rate significantly decreased in the final phase of driving, with respect to the initial phase (85 vs. 78 bpm, p = 0.027). Increasing age (beta = -0.729, p = 0.022), risk of obstructive sleep apnea syndrome (beta = -0.530, p = 0.04), and diurnal sleepiness (beta = -0.406, p = 0.017) showed a significant effect on influencing mental fatigue. Conclusion: Elderly drivers at higher risk of sleep disorders are more prone to mental fatigue, when exposed to driving activity. Monitoring indexes of central arousal and autonomic balance, coupled with the use of structured questionnaires can represent a useful strategy to detect profile of workers at higher risk of mental fatigue in such duty.

Development of a Novel Imaging Agent for Determining Albumin Uptake in Solid Tumors

S. Daum,J. P. Magnusson,L. Pes,J. Garcia Fernandez,S. Chercheja,F. Medda,F. I. Nollmann,S. D. Koester,P. Perez Galan,A. Warnecke,K. Abu Ajaj,Felix Kratz 대한핵의학회 2019 핵의학 분자영상 Vol.53 No.3

Purpose The purpose of this study was to investigate the albumin-binding compound 111In-C4-DTPA as an imaging agent for the detection of endogenous albumin accumulation in tumors. Methods 111In-C4-DTPA was injected in healthy nude mice for pharmacokinetic and biodistribution studies (10 min, 1, 6, 24, and 48 h, n = 4) and subsequently in tumor-bearing mice for single-photon emission computed tomography/X-ray-computed tomography (SPECT/CT) imaging studies. Four different human tumor xenograft models (LXFL529, OVXF899, MAXFTN401, and CXF2081) were implanted subcutaneously unilaterally or bilaterally (n = 4–8). After intravenous administration of 111In-C4-DTPA, SPECT/CT images were collected over 72 h at 4–6 time points. Additionally, gamma counting was performed for the blood, plasma, lungs, heart, liver, spleen, kidneys, muscle, and tumors at 72 h post-injection. Results 111In-C4-DTPA bound rapidly to circulating albumin upon injection, and the radiolabeled albumin conjugate thus formed was stable in murine and human serum. SPECT/CT images demonstrated a time-dependent uptake with a maximum of 2.7– 3.8% ID/cm3 in the tumors at approximately 24 h post-injection and mean tumor/muscle ratios in the range of 3.2–6.2 between 24 and 72 h post-injection. The kidneys and bladder were the predominant elimination organs. Gamma counting at 72 h postinjection showed 1.3–2.5% ID/g in the tumors and mean tumor/muscle ratios in the range of 4.9–9.4. Conclusion 111In-C4-DTPA bound rapidly to circulating albumin upon injection and showed time-dependent uptake in the tumors demonstrating a potential for clinical application as a companion imaging diagnostic for albumin-binding anticancer drugs.

Conformational Lock and Dissociative Thermal Inactivation of Lentil Seedling Amine Oxidase

( S. Zahra Moosavi Nejad ),( Ali Akbar Moosavi Movahedi ),( Mostafa Rezaei Tavirani ),( Giovanni Floris ),( Rosaria Medda ) 생화학분자생물학회 2003 BMB Reports Vol.36 No.2

The kinetics of thermal inactivation of copper-containing amine oxidase from lentil seedlings were studied in a 100 mM potassium phosphate buffer, pH 7, using putrescine as the substrate. The temperature range was between 47-60℃. The thermal inactivation curves were not linear at 52 and 57℃; three linear phases were shown. The first phase gave some information about the number of dimeric forms of the enzyme that were induced by the higher temperatures using the conformational lock pertaining theory to oligomeric enzyme. The conformational lock caused two additional dimeric forms of the enzyme when the temperature increased to 50℃. The second and third phases were interpreted according to a dissociative thermal inactivation model. These phases showed that lentil amine oxidase was reversibly-dissociated before the irreversible thermal inactivation. Although lentil amine oxidase is not a thermostable enzyme, its dimeric structure can form conformational lock, conferring a structural tolerance to the enzyme against heat stress.

Sardinian honeys as sources of xanthine oxidase and tyrosinase inhibitors

Di Petrillo, Amalia,Santos-Buelga, Celestino,Era, Benedetta,Gonzalez-Paramas, Ana Maria,Tuberoso, Carlo Ignazio Giovanni,Medda, Rosaria,Pintus, Francesca,Fais, Antonella 한국식품과학회 2018 Food Science and Biotechnology Vol.27 No.1

Sardinian honeys obtained from different floral sources (Arbutus, Asphodelus, Eucalyptus, Thistle, and Sulla) were evaluated for their ability to inhibit tyrosinase and xanthine oxidase enzymes and for their antioxidant activity. Physicochemical parameters, total phenolic, and flavonoids content were also determined. Honey from Arbutus flowers had the highest antioxidant activity followed by Eucalyptus and Thistle ones. These three honeys showed good tyrosinase and xanthine oxidase inhibition properties. Thus, these Sardinian honeys could have a great potential as antioxidant sources for pharmaceutical and cosmetic applications.

Conformational Lock and Dissociative Thermal Inactivation of Lentil Seedling Amine Oxidase

Moosavi-Nejad, S. Zahra,Moosavi-Movahedi, Ali-Akbar,Rezaei-Tavirani, Mostafa,Floris, Giovanni,Medda, Rosaria Korean Society for Biochemistry and Molecular Biol 2003 Journal of biochemistry and molecular biology Vol.36 No.2

The kinetics of thermal inactivation of copper-containing amine oxidase from lentil seedlings were studied in a 100 mM potassium phosphate buffer, pH 7, using putrescine as the substrate. The temperature range was between $47-60^{\circ}C$. The thermal inactivation curves were not linear at 52 and $57^{\circ}C$; three linear phases were shown. The first phase gave some information about the number of dimeric forms of the enzyme that were induced by the higher temperatures using the "conformational lock" pertaining theory to oligomeric enzyme. The "conformational lock" caused two additional dimeric forms of the enzyme when the temperature increased to $57^{\circ}C$. The second and third phases were interpreted according to a dissociative thermal inactivation model. These phases showed that lentil amine oxidase was reversibly-dissociated before the irreversible thermal inactivation. Although lentil amine oxidase is not a thermostable enzyme, its dimeric structure can form "conformational lock," conferring a structural tolerance to the enzyme against heat stress.