Thermodynamics of partitioning of the antimalarial drug mefloquine in phospholipid bilayers and bulk solvents

The antimalarial drug mefloquine binds avidly to phospholipids in biomembranes. The thermodynamics of the partitioning process in dimyristoylphosphatidylcholine (DMPC) bilayers was investigated to give some insight into the drug-phospholipid interaction. Thermodynamic parameters for the partition equilibria were evaluated from the equilibrium partition coefficients measured as a function of temperature. Negative values of delta H and delta S were obtained for the transfer of mefloquine from the aqueous to the gel phase of the phospholipid. The partitioning is enthalpy controlled which suggests that mefloquine interacts strongly with the phospholipid phase. In contrast, the partitioning of mefloquine into the liquid crystalline phase of DMPC is entropy controlled which is typical of a hydrophobic interaction between mefloquine and the aqueous phase. The partitioning of mefloquine into the bulk solvents octanol and hexane were found to be enthalpy and entropy controlled, respectively. The enthalpy dominated partitioning of mefloquine into gel phase DMPC and octanol is attributed to the occurrence of hydrogen bonding and van der Waals interactions between solute and solvent. The flat shape of mefloquine may further aid its interaction with the orderly domains of the lipidic/organic phase. This is apparent from a comparison of the partitioning characteristics of another structurally related but conformationally different molecule, quinine into DMPC and octanol.     

Membrane fusion induced by the HIV type 1 fusion peptide: modulation by factors affecting glycoprotein 41 activity and potential anti-HIV compounds

Peptides representing a sequence of 23 amino acid residues at the N terminus of human immunodeficiency virus type 1 (HIV-1) envelope glycoprotein gp41 bind and subsequently induce fusion of large unilamellar vesicles (LUV), an activity presumably related to gp41 function in viral infection. These in vitro effects can be modulated by several factors that are known to affect HIV-1 infectivity and gp41-mediated virus-cell fusion. Peptide-induced membrane fusion but not peptide binding can be inhibited by two factors known to block gp41 activity: a polar amino acid substitution V --> E in position 2 and the presence of the N-terminal hexapeptide of gp41 in addition to the parent sequence. Whereas inclusion of the alternative gp120 receptor galactosylceramide in membranes has virtually no effect, membrane cholesterol stimulates fusion activity. In view of its putative physiological relevance, we have used the fusion activity of the peptides as a tool to evaluate the inhibitory effect of antivirals that might target this sequence. We describe three dissimilar effects: Amphotericin B inhibits in a cholesterol-independent way peptide-induced fusion but not binding, human serum albumin inhibits binding and consequently fusion, and dextran sulfate (M(r) 5000) does not affect either binding or fusion.     

Mechanical properties of a modified acrylic bone cement with etoxytriethyleneglycol monomethacrylate

With the aim of improving some of the disadvantages of the acrylic bone cements, an acrylic bone cement based on polymethyl methacrylate has been modified by substituting different quantities, up to 20%, of the monomer methyl methacrylate (MMA) with the same amount of ethoxytriethyleneglycol monomethacrylate (TEG). The addition of this new monomer decreased noticeably the maximum temperature and increased both setting and working times. Mechanical testing revealed that the introduction of TEG gave rise to a less fragile bone cement by increasing slightly the total deformation without any change in the rest of the tensile parameters.     

Phosphatidylinositol-dependent membrane fusion induced by a putative fusogenic sequence of Ebola virus

The membrane-interacting abilities of three sequences representing the putative fusogenic subdomain of the Ebola virus transmembrane protein have been investigated. In the presence of calcium, the sequence EBO(GE) (GAAIGLAWIPYFGPAAE) efficiently fused unilamellar vesicles composed of phosphatidylcholine, phosphatidylethanolamine, cholesterol, and phosphatidylinositol (molar ratio, 2:1:1:0.5), a mixture that roughly resembles the lipid composition of the hepatocyte plasma membrane. Analysis of the lipid dependence of the process demonstrated that the fusion activity of EBO(GE) was promoted by phosphatidylinositol but not by other acidic phospholipids. In comparison, EBO(EA) (EGAAIGLAWIPYFGPAA) and EBO(EE) (EGAAIGLAWIPYFGPAAE) sequences, which are similar to EBO(GE) except that they bear the negatively charged glutamate residue at the N terminus and at both the N and C termini, respectively, induced fusion to a lesser extent. As revealed by binding experiments, the glutamate residue at the N terminus severely impaired peptide-vesicle interaction. In addition, the fusion-competent EBO(GE) sequence did not associate significantly with vesicles lacking phosphatidylinositol. Tryptophan fluorescence quenching by vesicles containing brominated phospholipids indicated that the EBO(GE) peptide penetrated to the acyl chain level only when the membranes contained phosphatidylinositol. We conclude that binding and further penetration of the Ebola virus putative fusion peptide into membranes might be governed by the nature of the N-terminal residue and by the presence of phosphatidylinositol in the target membrane. Moreover, since insertion of such a peptide leads to membrane destabilization and fusion, the present data would be compatible with the involvement of this sequence in Ebola virus fusion.     

Enhancement of a WLAN-Based Internet Service

A wireless LAN (WLAN)-based Internet service, called NESPOT, of Korea Telecom (KT), the biggest telecommunication and Internet service company in Korea, has been operational since early 2002. As the numbers of subscribers and deployed access points (APs) increase, KT has been endeavoring to improve its service quality as well as the network management. In this paper, we introduce a joint effort between Seoul National University (SNU) and KT to achieve it. We have been addressing two major issues as part of the joint project thus far: (1) a unified WLAN management/maintenance tool; and (2) real-time traffic support enhancement. We present our on-going efforts as well as some preliminary results. Some issues, which need further attention for the future NESPOT service enhancement, are also introduced.The work reported in this paper was financed and supported by KT. Any opinions, findings, and conclusions or recommendations expressed in this publication are those of the authors and do not necessarily reflect the views of KT. Youngkyu Choi is an M.S. candidate in the department of electrical engineering at Seoul National University (SNU), Seoul, Korea. He received his B.S. with honors in electrical engineering from SNU in 2002. He has a lot of project experiences related with system software development. His current research interests are the design of MAC layer from distributed system to centralized cellular system, resource management in next-generation (4G) cellular system, and mathematical analysis of system performance. He had served in the Korean Army for 3 years from 1998. Sekyu Park is a research staff at the Multimedia & Wireless Networking Lab. (MWNL), Seoul National University (SNU), Seoul, Korea. Before joining MWNL in September 2003, he was with MMC Technology, Seoul, Korea as a Research Staff for five years. His current research interests are in the area of wireless/mobile networks and embedded OS. Sunghyun Choi is an assistant professor at the School of Electrical Engineering, Seoul National University (SNU), Seoul, Korea. Before joining SNU in September 2002, he was with Philips Research USA, Briarcliff Manor, New York, USA as a Senior Member Research Staff and a project leader for three years. He received his B.S. (summa cum laude) and M.S. degrees in electrical engineering from Korea Advanced Institute of Science and Technology (KAIST) in 1992 and 1994, respectively, and received Ph.D. at the Department of Electrical Engineering and Computer Science, The University of Michigan, Ann Arbor in September, 1999. His current research interests are in the area of wireless/mobile networks with emphasis on the QoS guarantee and adaptation, resource management, wireless LAN and PAN, next-generation mobile networks, data link layer protocols, and connection and mobility management. He authored/coauthored over 45 technical papers and book chapters in the areas of wireless/mobile networks and communications. He is the technical program co-chair for ACM International Workshop on Wireless Mobile Applications and Services on WLAN Hotspots (WMASH’2004). He is currently serving on program committees of a number of leading wireless and networking conferences including IEEE INFOCOM, IEEE GLOBECOM, and IEEE VTC. He is also a guest co-editor for a special issue on “Emerging WLAN Applications and Technologies” of Wiley Wireless Communications and Mobile Computing Journal. He is an active participant and contributor of the IEEE 802.11 WLAN standardization committee. Dr. Choi was a recipient of the Korea Foundation for Advanced Studies Scholarship and the Korean Government Overseas Scholarship during 1997–1999 and 1994–1997, respectively. Go Woon Lee is a researcher at Service Development Laboratory, Korea Telecom (KT), Seoul, Korea. She received her B.S. degrees in computer science and material engineering from Korea Advanced Institute of Science and Technology (KAIST) in 1995. She was with Microsoft Korea R&D Group as a research staff in 1995. She received M.S. degree in information & communication from Kwang-Ju Institute of Science and Technology (K-JIST) in 1998. Her current research interests are in the area of wireless/mobile networks with emphasis on data link layer protocols, remote diagnosis, and wireless service management. Jaehwan Lee is a researcher at Korea Telecom (KT), Seoul, Korea. He received his B.S. and M.S. degrees in electrical engineering from Seoul National University (SNU) in 1998 and 2000, respectively. His master’s research was about estimation theory related to Global Positioning System (GPS) and image processing in robot soccer. His current research interest is to analyze and enhance the performance of wireless/mobile networks (IEEE 802.11, sensor networks and mobile ad-hoc networks) regarding QoS, energy-efficiency and high-throughput considering hand-off and inter-networking with heterogeneous networks. Before joining wireless LAN group in KT, he developed the Web-GIS (Geographical Information System) client-server system from 2000 to 2001. Hanwook Jung, Ph.D joined KT in 1985 and got his Ph.D degree with the company finalcial scholarship of KT from 1991 to 1996 at SUNY at Buffalo. His thesis is about “Wireless signal transmission over Fiber by subcarrier multiplexing” which is current heavily utilized for PCS and cellular repeater line. From 1985 to 1991, he had developed a Videotex service which is now known as Hitel. From 1996 to 1999, he developed 26GHz broadband wireless local loop system and contributed to get the license from the government. Since 1999, he has led a business model and service with wireless LAN. The KT Wi-Fi public service, “NESPOT” has 300,000 subscribers and 10,000 public hotspots. In 2003 he was promoted as an assistant vice president leading NESPOT research team to enhance KT’s broadband with 5,000,000 subscribers. His vision regarding next generation communications service is believed to be true by combining the broadband access and wireless technology including WiFi wireless LAN, UWB, and bluetooth in those areas such as wireless home-networking, device-to-device communications, and ubiqutous networking.This revised version was published online in August 2005 with a corrected cover date.     

The inhibitive action of bound water in the passive film of stainless steel against chloride corrosion

The stability of passivated 304 stainless steel specimens in the presence of chloride ions was investigated in relation to the amount of bound water in the passive film. As a measure of the stability the induction period for pit initiation and number of the anodic fluctuation prior to pit initiation were used. The amount of bound water was controlled by varying of passivation potentials, passivation times and passivation temperatures. Two kinds of bound water with different inhibitive action against corrosion by chloride ions were found in the passive film.     

Effects of perceptual training on unmatched samples of brain-injured and familial retarded children.

41 brain-injured (Bl) and 39 familial retarded (FR) children matched for CA but not for MA were 1st tested on 1 set of ambiguous pictures, then trained on a 2nd set, and then retested on the 1st set both immediately and 1 mo. following training. Results showed that although the BI group had a significantly higher IQ than the FR group, they nevertheless took more trials to reach a lower level of post-training performance. The difference between the groups reached statistical significance, however, only when the MA differential favoring the BI group was controlled by the analysis of covariance procedure. (PsycINFO Database Record (c) 2010 APA, all rights reserved)