Crystallographic analysis reveals the structural basis of the high-affinity binding of iophenoxic acid to human serum albumin

<p>Abstract</p> <p>Background</p> <p>Iophenoxic acid is an iodinated radiocontrast agent that was withdrawn from clinical use because of its exceptionally long half-life in the body, which was due in part to its high-affinity binding to human serum albumin (HSA). It was replaced by Iopanoic acid, which has an amino rather than a hydroxyl group at position 3 on the iodinated benzyl ring and, as a result, binds to albumin with lower affinity and is excreted more rapidly from the body. To understand how iophenoxic acid binds so tightly to albumin, we wanted to examine the structural basis of its interaction with HSA.</p> <p>Results</p> <p>We have determined the co-crystal structure of HSA in complex with iophenoxic acid at 2.75 Å resolution, revealing a total of four binding sites, two of which - in drugs sites 1 and 2 on the protein - are likely to be occupied at clinical doses. High-affinity binding of iophenoxic acid occurs at drug site 1. The structure reveals that polar and apolar groups on the compound are involved in its interactions with drug site 1. In particular, the 3-hydroxyl group makes three hydrogen bonds with the side-chains of Tyr 150 and Arg 257. The mode of binding to drug site 2 is similar except for the absence of a binding partner for the hydroxyl group on the benzyl ring of the compound.</p> <p>Conclusions</p> <p>The HSA-iophenoxic acid structure indicates that high-affinity binding to drug site 1 is likely to be due to extensive desolvation of the compound, coupled with the ability of the binding pocket to provide a full set of salt-bridging or hydrogen bonding partners for its polar groups. Consistent with this interpretation, the structure also suggests that the lower-affinity binding of iopanoic acid arises because replacement of the 3-hydroxyl by an amino group eliminates hydrogen bonding to Arg 257. This finding underscores the importance of polar interactions in high-affinity binding to albumin.</p

Controlling spin supercurrents via nonequilibrium spin injection.

We propose a mechanism whereby spin supercurrents can be manipulated in superconductor/ferromagnet proximity systems via nonequilibrium spin injection. We find that if a spin supercurrent exists in equilibrium, a nonequilibrium spin accumulation will exert a torque on the spins transported by this current. This interaction causes a new spin supercurrent contribution to manifest out of equilibrium, which is proportional to and polarized perpendicularly to both the injected spins and the equilibrium spin current. This is interesting for several reasons: as a fundamental physical effect; due to possible applications as a way to control spin supercurrents; and timeliness in light of recent experiments on spin injection in proximitized superconductors

KEBERTAHANAN KOSAKATA ANATOMI TUBUH MANUSIA DALAM BAHASA MUNA PADA PENUTUR BAHASA MUNA

Regional languages are one of the sources of Indonesian language development, therefore the existence of regional languages is very necessary to be maintained or preserved. Muna language is one of the regional languages in Southeast Sulawesi. The current position of the Muna Regional language has gone down. The condition of the local language-speaking community who is reluctant to use the local language and changes in the environment in which they live are one of the contributing factors. The purpose of this study was to describe the percentage level of survival of the vocabulary of the anatomy of the human body in the Muna language among Muna speakers at BTN Kendari Permai, Kendari City. This study used the theory of language survival, vocabulary, and ecolinguistics theory. The methods used in this research were qualitative and quantitative methods. The results of data analysis showed that the anatomical vocabulary of the human body in Muna language for Muna speakers at BTN Kendari Permai were still survives well. From the 40 respondents who filled out the questionnaire, 81% of the respondents still knew, understood and explained the names of their anatomy well. From the 60 vocabularies proposed in the questionnaire, 87% (52) of vocabulary still survive and 13% (8) of vocabularies have not survived

Electric control of superconducting transition through a spin-orbit coupled interface.

We demonstrate theoretically all-electric control of the superconducting transition temperature using a device comprised of a conventional superconductor, a ferromagnetic insulator, and semiconducting layers with intrinsic spin-orbit coupling. By using analytical calculations and numerical simulations, we show that the transition temperature of such a device can be controlled by electric gating which alters the ratio of Rashba to Dresselhaus spin-orbit coupling. The results offer a new pathway to control superconductivity in spintronic devices.J.L. and J.A.O. acknowledge funding via the “Outstanding Academic Fellows” programme at NTNU, the COST Action MP-1201 and the Research Council of Norway Grant numbers 205591, 216700, and 240806. J.W.A.R. and A.D.B. acknowledge funding from the Leverhulme Trust (IN-2013-033), the Royal Society and the EPSRC through the Programme Grant “Superconducting Spintronics” (EP/N017242/1), and the Doctoral Training Grant (NanoDTC EP/G037221/1

Adsorption of sodium hexanoate on α-alumina.

Neutron reflection and adsorption isotherm measurements have been used to study the adsorption behaviour of hexanoic acid onto α-alumina surfaces. Importantly, the pH dependence of the behaviour has been characterised with a pronounced maximum in adsorption identified at a pH of approximately 5, close to the pKa of the acid. The adsorbed layer is identified as a bilayer, which is reasonable given the hydrophilic nature of both side of the layer, and has a thickness of 13 Å, suggesting significant extent of interdigitation. At pH 5, the layer has much lower extent of hydration relative to the higher pH of 7, consistent with the increased total adsorption at pH 5. A number of different mechanisms for the binding of the hexanoic acid to the surface are considered. The experimental data, combined with calculations using equilibrium/binding constants of the surface and ligands, indicates that a ligand exchange reaction may be the most significant mechanism.This is the author's accepted manuscript. The final version has been published by Elsevier in the Journal of Colloid and Interface Science here: http://www.sciencedirect.com/science/article/pii/S0021979713005560

SEJARAH PENGOBATAN TRADISIONAL ORANG BUTON DI KECAMATAN BATUPOARO KOTA BAUBAU: 1986-2016

Penelitian ini bertujuan untuk menguraikan sejarah pengobatan tradisional orang Buton di Kecamatan Batupoaro Kota Baubau. Metode&nbsp; penelitian (1) &nbsp;pemilihan topik&nbsp; (2) heuristik sumber, (3) kritik sumber, (4) interpretasi, dan (5) penulisan sejarah. Hasil penelitian menunjukkan bahwa (1) pengetahuan tentang cara pengobatan tradisional pada orang Buton diperoleh secara turun-temurun. Pada umumnya, praktek pengobatan tersebut dihafal dan dipraktekkan secara berulang-ulang untuk mengobati penyakit. (2) Jenis tanaman yang digunakan sebagai obat tradisional oleh masyrakat Buton di Kecamatan Batupoaro, yaitu: mengkudu (bangkudu), daun kumis kucing (bulumuncuna mbuta), sirih (gili), pepaya (kapaya), jambu biji (bulamalaka), jahe (malala), kunyit (mantomu), serai (padamalala), jeruk nipis (makolona), jarak (ntanga-ntanga) dan pinang. (3) Cara penggunaan tanaman obat orang Buton adalah pertama-tama mengumpulkan jenis tanaman yang akan digunakan sebagai obat untuk penyembuhan penyakit. Setelah terkumpul, tanaman untuk obat tradisional kemudian diramu. Tanaman yang telah diramu kemudian disajikan sebagai obat guna penyembuhan penyakit. Kata Kunci: pengobatan tradisional, orang Buton, obat herba

Effect of Volume Fraction and Solutions Absorption on The Properties of Epoxy/Carbon Fiber Composites

The objective of this research is to study the effect of volume fraction of short carbon fibers, distilled water and diluted HCl on the mechanical properties of the composite material, and determine the diffusion coefficient. The composite material was prepared from the epoxy resin as a matrix material and the short carbon fibers as a reinforcing material at volume fractions of 3%, 5% and 7%, respectively. Bending strength, Tensile strength and Absorption Tests were carried out on the samples of the composites .The results showed that adding carbon fibers to the polymer has increased the composite material strength and consequently raised the elasticity coefficient and the tensile strength proportionally with the volume fraction. Moreover, the results showed that immersing the samples in water and acid decreased the elasticity coefficient and tensile resistance in a manner proportional to the duration of immersion, whereby the effect of acid was greater than that of water

PENINGKATAN KUALITAS KARKAS AYAM KAMPUNG SUPER MELALUI PERBAIKAN SISTEM PEMOTONGAN DI DESA ALEBO, KECAMATAN KONDA, KABUPATEN KONAWE SELATAN

Chicken slaughter had to fulfill requirements such as the slaughter done in Islamic ways and the meat processed hygienically in order to produce safe, healthy, whole, and halal. Partner farmer at Alebo, Konda Sub-district, Konawe Selatan Regency implemented a simple slaughter system with less hygienic tools and procedures that increased the risk of contamination in meat. This community partnership program aimed to increase the farmer’s information and skill in managing native chicken slaughterhouses in order to produce better carcass and fish feed from slaughter waste. The methods used in this program were physical and non-physical methods which consisted of the slaughterhouse renovation, chicken slaughter, and carcass packaging training, fish feed production using slaughter waste training, discussion, and public lecture. Results of the program show that partner farmers are able to implement Islamic and hygienic slaughter processes and use better packages for the carcass. The farmers also understand the importance of slaughter waste processing and producing fish feed as an additional product of the slaughterhouse

EDUKASI PEMBUATAN MINUMAN HERBAL SEDERHANA DARI KULIT LABU KUNING PADA MASYARAKAT KECAMATAN ABELI

Program pengabdian masyarakat oleh tim dosen S1-Farmasi ITK Avicenna mengusung tema edukasi pembuatan minuman herbal sederhana untuk kesehatan dari kulit labu kuning. Labu kuning selama ini dimanfaatkan sebagai bahan pangan, sayuran atau menjadi bahan dasar pembuatan kue. Kulit labu kuning biasanya hanya menjadi limbah atau dimanfaatkan sebagai pakan ternak. Kulit labu kuning sejauh ini disyalir memiliki kandungan kimia yang berpotensi sebagai antioksidan alami. Kegiatan Pengabdian Masyarakat ini bertujuan untuk memberikan &nbsp;edukasi pembuatan minuman herbal dari kulit buah labu kuning. Kegiatan diikuti oleh 3 orang dosen dan mahasiswa/mahasiswa S1 Farmasi ITK Avicenna. Materi dibawakan langsung oleh seorang apoteker dengan basic farmasi &nbsp;komunitas dan klinis. Kegiatan ini dihadiri oleh kalangan ibu rumah tangga, lansia dan kader posyandu. Penyuluhan dilakukan dengan metode ceramah, diskusi bersama masyarakat disertai demo cara meramu dan penyajian minuman herbal. Output dari kegiatan ini berupa minuman herbal dalam bentuk sediaan teh seduh kulit labu kuning. Penyuluhan edukasi minuman herbal ini diharapkan memberikan dampak postif dan &nbsp;manfaat terkait pemanfaatan&nbsp; kulit labu kuning untuk kesehatan serta memberi informasi alternatif penggunaan obat tradisional untuk masyarakat di Kecamatan Abeli