Dimeric C34 Derivatives Linked through Disulfide Bridges as New HIV-1 Fusion Inhibitors

C34, a 34-mer fragment peptide, is contained in the HIV-1 envelope protein gp41. A dimeric derivative of C34 linked through a disulfide bridge at its C terminus was synthesized and found to display potent anti-HIV activity, comparable with that of a previously reported PEGylated dimer of C34REG. The reduction in the size of the linker moiety for dimerization was thus successful, and this result might shed some light on the mechanism of the suppression of six-helix bundle formation by these C34 dimeric derivatives. Addition of a Gly-Cys(CH₂CONH₂)-Gly-Gly motif at the N-terminal position of a C34 monomeric derivative significantly increased the anti-HIV-1 activity. This moiety functions as a new pharmacophore, and this might provide a useful insight into the design of potent HIV-1 fusion inhibitors.     

Morphological and Genetic Diversities of Habenaria radiata (Orchidaceae) in the Kinki Area,Japan

Floral organs have evolved from leaves for reproduction, and the morphological analyses help to understand the plant diversity and evolution. Habenaria radiata (syn. Pecteilis radiata) is a terrestrial orchid living in wetlands in Japan, Russia, South Korea, and China. The habitats of this plant in Japan have been reduced because of environmental destruction and overexploitation, and thus it is on the Red List of Japan as a Near Threatened species. One of the three petals of the H. radiata flower is called a lip or labellum, which resembles a flying white bird, egret, or white heron, with its proposed function being to attract pollinators. To understand the diversity of H. radiata plants in different areas, we examined the lip morphology and phylogeny of populations from eight habitats in the Kinki area, Japan. The complex shapes of the lips were quantified and presented as a radar chart, enabling characterization of the morphological difference among populations. Phylogenetic analysis with microsatellite markers that we generated showed the variation of genetic diversity among populations, suggesting the different degrees of inbreeding, outbreeding, and vegetative propagation. Our approach offers a basic method to characterize the morphological and genetic diversity in natural populations.     

Two Triterpene Synthases from Imperata cylindrica Catalyzing the Formation of a Pair of Diastereoisomers through Boat or Chair Cyclization

Imperata cylindrica is known to produce a pair of triterpenes, isoarborinol and fernenol, that exhibit identical planar structures but possess opposite stereochemistry at six of the nine chiral centers. These differences arise from a boat or a chair cyclization of the B-ring of the substrate. Herein, we report the characterization of three OSC genes from I. cylindrica. IcOSC1 and IcOSC5 were identified as isoarborinol and fernenol synthases, respectively, while IcOSC3 was characterized as a multifunctional enzyme that produces glutinol and friedelin as its major products. Mutational studies of isoarborinol and fernenol synthases revealed that the residues surrounding the DCTAE motif partially affected the conformation of the B-ring during cyclization. Additionally, the IcOSC1-W255H mutant produced the rare triterpene boehmerol. The introduced histidine residue presumably abstracted a proton from the intermediary carbocation at C18 during the 1,2-rearrangement. Expression analysis indicated that all OSC genes were highly expressed in stems.     

Prediction of brittle fracture initiating at ends of CJP groove welded joints with defects: study into applicability of failure assessment diagram approach

A series of tests, which reproduced brittle fracture starting from the region around the terminations of complete joint penetration groove welded joints, was conducted. The joint models under study represented a portion of welded beam flange-to-through diaphragm joints in beam-to-column connections. Various artificial weld defects were installed in the welded joints prior to testing. Test results were evaluated based on the failure assessment diagram approach specified in BS 7910. The conventional failure assessment diagrams predicted occurrences of brittle fracture erring on the very conservative side as expected, especially when applied to surface defects. The failure assessment diagram approach was modified by considering the effect of enhanced apparent toughness of material due to the loss of crack tip constraint. The modified failure assessment approach was found to predict the test results well.     

Effect of filler surface treatment on the properties of recycled high‐density polyethylene/(natural rubber)/(Kenaf powder) biocomposites

Biocomposites were prepared from a kenaf core powder and recycled high‐density polyethylene/(natural rubber) blend by using an internal mixer at 165^oC and 50 rpm. The effect of the filler content and the filler surface treatment was studied. Chemical modification of kenaf filler was performed with alkali pretreatment followed by treatment with silane. Scanning electron microscopy and infrared spectroscopy studies confirmed changes in the chemical compositions and structural characteristics induced through the modification. It was found that treated biocomposites offered higher tensile strength and tensile modulus, but lower elongation at break compared with untreated biocomposites. Lower water absorption and higher thermal stability of the resultant biocomposites were also obtained when treated fillers were used. J. VINYL ADDIT. TECHNOL., 20:218–224, 2014. © 2014 Society of Plastics Engineers     

Specific Polyphenols and Tannins are Associated with Defense Against Insect Herbivores in the Tropical Oak Quercus oleoides

The role of plant polyphenols as defenses against insect herbivores is controversial. We combined correlative field studies across three geographic regions (Northern Mexico, Southern Mexico, and Costa Rica) with induction experiments under controlled conditions to search for candidate compounds that might play a defensive role in the foliage of the tropical oak, Quercus oleoides. We quantified leaf damage caused by four herbivore guilds (chewers, skeletonizers, leaf miners, and gall forming insects) and analyzed the content of 18 polyphenols (including hydrolyzable tannins, flavan-3-ols, and flavonol glycosides) in the same set of leaves using high performance liquid chromatography and mass spectrometry. Foliar damage ranged from two to eight percent per region, and nearly 90% of all the damage was caused by chewing herbivores. Damage due to chewing herbivores was positively correlated with acutissimin B, catechin, and catechin dimer, and damage by mining herbivores was positively correlated with mongolinin A. By contrast, gall presence was negatively correlated with vescalagin and acutissimin B. By using redundancy analysis, we searched for the combinations of polyphenols that were associated to natural herbivory: the combination of mongolinin A and acutissimin B had the highest association to herbivory. In a common garden experiment with oak saplings, artificial damage increased the content of acutissimin B, mongolinin A, and vescalagin, whereas the content of catechin decreased. Specific polyphenols, either individually or in combination, rather than total polyphenols, were associated with standing leaf damage in this tropical oak. Future studies aimed at understanding the ecological role of polyphenols can use similar correlative studies to identify candidate compounds that could be used individually and in biologically meaningful combinations in tests with herbivores and pathogens.     

Intuitive substitute interface

This paper proposes the “Substitute Interface” to utilize the flat surfaces of objects around us as part of an ad hoc mobile device. The substitute interface is established by the combination of wearable devices such as a head-mounted display with camera and a ring-type microphone. The camera recognizes which object the user intends to employ. When the user picks up and taps the object, such as a notebook, a virtual display is overlaid on the object, and the user can operate the ad hoc mobile device as if the object were part of the device. Display size can be changed easily by selecting a larger object. The user’s pointing/selection action is recognized by the combination of the camera and the ring-type microphone. We first investigate the usage scene of tablet devices and create a prototype that can operate as a tablet device. Experiments on the prototype confirm that the proposal functions as intended.     

Study on FBR core concepts to increase proliferation resistance of plutonium in LWR–FBR transition period

The possibility to enhance proliferation resistance of discharged plutonium in fast breeder reactor (FBR) has been investigated in terms of reactor core-design aspects. The provisional target for proliferation resistance measures based on Saito's attractiveness (ATTR) is defined. It is found that a few percent of plutonium loading and/or Am/Cm loading, which come from various types of spent fuel, might satisfy the provisional target with a minimum impact on the core neutronic performances. On Am/Cm loading core, decay heat constraints for fuel-handling aspects are found to be important and should be considered in design. There is not significant change on the current developing scenarios for light water reactor–FBR transition period by applying the measures based on Saito's ATTR. It is found that applying Kimura's proposal, 15% ²³⁸Pu content requires about 7% MA loading fraction both in the core and the blanket, and it only can be applied at limited case. The period to consume minor actinides is shorter than to consume plutonium.