Characterization of the early stage aminoshikimate pathway in the formation of 3-amino-5-hydroxybenzoic acid: the RifN protein specifically converts kanosamine into kanosamine 6-phosphate

The biosynthesis of 3-amino-5-hydroxybenzoic acid (AHBA), precursor of the ansamycin and mitomycin antibiotics, proceeds by the aminoshikimate pathway from 3,4-dideoxy-4-amino-D-arabino-heptulosonic acid 7-phosphate (aminoDAHP). Identification of RifN, product of one of three genes from the rifamycin biosynthetic gene cluster known to be essential for aminoDAHP formation, as a specific kanosamine (3-deoxy-3-amino-D-glucose) 6-kinase establishes kanosamine and its 6-phosphate as specific intermediates in AHBA formation. This suggests a hypothetical reaction sequence for aminoDAHP formation, and thus for the early steps of AHBA biosynthesis, starting from UDP-D-glucose and introducing the nitrogen by oxidation and transamination at C-3.     

Simultaneous Determination of Pioglitazone and Glimepiride by High-Performance Thin-Layer Chromatography

JPC – Journal of Planar Chromatography – Modern TLC -     

Type II seesaw and the PAMELA/ATIC signals

We discuss how the cosmic ray signals reported by the PAMELA and ATIC/PPB-BETS experiments may be understood in a Standard Model (SM) framework supplemented by type II seesaw and a stable SM singlet scalar boson as dark matter. A particle physics explanation of the ‘boost’ factor can be provided by including an additional SM singlet scalar field.     

Sensitive,Selective, Precise and Accurate LC–MS Method for Determination of Clonidine in Human Plasma

A selective and sensitive liquid chromatography–mass spectrometric method in ESI (+ve) mode was developed and validated completely in human plasma. Clonidine and IS, carbamazapine, were extracted from human plasma via liquid–liquid extraction with ethyl acetate. Following evaporation under nitrogen, the residue was reconstituted with mobile phase and analyzed using API 4000 LC–MS–MS system. An isocratic program with binary mobile phases (0.1% formic acid in water and acetonitrile) was used to separate interference peaks by a C18 analytical column. Linearity range was 0.49–73.98 ng mL⁻¹. The intra- and inter-day accuracy and precision were within acceptable limits (≤15%). This method was successfully applied to a single dose 25 μg tablets BE study of clonidine in healthy male volunteers.

     

Synthesis,characterization, and evaluation of biological activities of new 4′‐substituted ruthenium (II) terpyridine complexes: Prospective anti‐inflammatory properties

The synthesis and characterization of Ru (II) terpyridine complexes derived from 4′ functionalized 2,2′:6′,2″‐terpyridine (tpy) ligands are reported. The heteroleptic complexes comprise the synthesized ligands 4′‐(2‐thienyl)‐ 2,2′:6′,2″‐terpyridine) or (4′‐(3,4‐dimethoxyphenyl)‐2,2′:6′,2″‐terpyridine and (dimethyl 5‐(pyrimidin‐5‐yl)isophthalate). The new complexes [Ru(4′‐(2‐thienyl)‐2,2′:6′,2″‐terpyridine)(5‐(pyrimidin‐5‐yl)‐isophthalic acid)Cl₂] ( 9 ), [Ru(4′‐(3,4‐dimethoxyphenyl)‐2,2′:6′,2″‐terpyridine)(5‐(pyrimidin‐5‐yl)‐isophthalic acid)Cl₂] ( 10 ), and [Ru(4′‐(2‐thienyl)‐2,2′:6′,2″‐terpyridine)(5‐(pyrimidin‐5‐yl)‐isophthalic acid)(NCS)₂] ( 11 ) were characterized by ¹H‐ and ¹³C‐NMR spectroscopy, C, H, N, and S elemental analysis, UPLC‐ESI‐MS, TGA, FT‐IR, and UV‐Vis spectroscopy. The biological activities of the synthesized ligands and their Ru (II) complexes as anti‐inflammatory, antimicrobial, and anticancer agents were evaluated. Furthermore, the toxicity of the synthesized compounds was studied and compared with the standard drugs, namely, diclofenac potassium and ibuprofen, using hemolysis assay. The results indicated that the ligands and the complex 9 possess superior anti‐inflammatory activities inhibiting albumin denaturation (89.88–100%) compared with the standard drugs (51.5–88.37%) at a concentration of 500 μg g^?1. These activities were related to the presence of the chelating N‐atoms in the ligands and the exchangeable chloro‐ groups in the complex. Moreover, the chloro‐ and thiophene groups in complex 9 produce a higher anticancer activity compared with its isothiocyanate derivative in the complex 11 and the 3,4‐dimethoxyphenyl moiety in complex 10 . Considering the toxicity results, the synthesized ligands are nontoxic or far less toxic compared with the standard drugs and the metal complexes. Therefore, these newly synthesized compounds are promising anti‐inflammatory agents in addition to their moderate unique broad antimicrobial activity.     

Polymerization of Ion-Pair Comonomers of Related Structures

Two ion-pair comonomers of 2-methacryloyloxyethyltrimethyl-ammonium 2-methacryloyloxyethanesulfonate (METMAMES) and 3-acrylamido-3-methylbutyltrimethylammonium 2-acrylamido-2-methylpropanesulfonate have been synthesized. The spontaneous and radical homocopolymerizations of these monomer pairs, wherein no nonpolymerizable counterions are present, have also been studied. Moreover, the intrinsic viscosity of the homocopolymer derived from METMA MES was found to increase with increasing KCl concentration in aqueous solutions.     

An updated overview of diamond-like carbon coating in tribology

During the last two decades, the industry (including scientists) has focused on diamond-like carbon (DLC) coating because of its wide range of application in various fields. This material has numerous applications in mechanical, electrical, tribological, biomedical, and optical fields. Severe friction and wear in some machine parts consumes high amount of energy, which makes the process energy inefficient. Thus, DLC coating can be an effective means to lower the friction and wear rate. Some important process variables that affect the tribological characteristics of DLC coating are adhesion promoter intermediate layer, substrate surface roughness, hydrogen incorporation or hydrogen non involvement, and coating deposition parameters (e.g., bias voltage, etching, current, precursor gas, time, and substrate temperature). Working condition of DLC-coated parts also affects the tribological characteristics, such as temperature, sliding speed and load, relative humidity, counter surface, and lubrication media (DLC additive interaction). Different types of lubricated oils and additives are used in engine parts to minimize friction and wear. DLC can be coated to the respective engine parts; however, DLC does not behave accordingly after coating because of lubricant oil and additive interaction with DLC. Some additive interacts positively and some behave negatively because of the tribochemical reactions between DLC coating and additives. Numerous conflicting views have been presented by several researchers regarding this coating additive interaction, resulting in unclear determination of true mechanism of such interaction. However, lubricant additive has been established to be more inert to DLC coating compared with uncoated metal surface because the additive is fabricated in such a way that it can react with metal surfaces. In this article, the tribological characteristics of different types of DLC coating in dry and lubricated conditions will be presented, and their behavior will be discussed in relation to working condition and processing parameters.     

Median lethal dose, antimalarial activity, phytochemical screening and radical scavenging of methanolic Languas galanga rhizome extract

The methanolic extract of Languas galanga rhizomes was investigated for antimalarial activity against Plasmodium berghei (NK65) infections in mice. The median lethal dose was determined to ascertain the safety of the extract in ICR mice of both sexes. The antimalarial activities during early and established infections, as well as the prophylactic activity were evaluated. Phytochemical screening and radical scavenging activity of the extract were also investigated to elucidate the possible mechanism of the antimalarial properties. The acute oral toxicity (LD??) of Languas galanga extract in mice was established to be 4.998 mg/kg. The extract of Languas galanga rhizomes demonstrated significant antiplasmodial activity in all the three models of the antimalarial evaluations. Phytochemical screening revealed the presence of some vital antiplasmodial constituents such as terpenoids and flavonoids. The extract also exhibited a moderate capacity to scavenge the free radicals. The rhizome extract of Languas galanga thus possesses antimalarial activity, which explains the rational usage of this plant in traditional Malaysian medicine.     

Crystallisation progress in Si-rich ultra-soft nanocomposite alloy fabricated by melt spinning

The crystallisation process and the ultras-soft magnetic properties of amorphous/nanocomposite alloy Fe_73.5Si_17.5B₅Nb₃Cu₁ fabricated by conventional melt-spinning technique are systematically investigated in terms of thermal analysis and in-situ measurement of magnetisation dynamics. The thermal analysis using differential scanning calorimetry showed that crystallisation from Fe-based amorphous state to α-Fe(Si) started at . Further heating the sample leads to a transformation from the α-Fe(Si) to Fe-B phases at . Crystallisation activation energies were determined using two models: Kissinger and John-Mehl-Avrami (JMA), which were consistent to each other with a value of . High resolution transmission electron microscopy investigation revealed an ultrafine structure of α-Fe(Si) nanocrystallite with mean size of 12.5 nm embedded in an amorphous matrix. At a volume fraction of 86% of α-Fe(Si) phase, optimum soft magnetic properties were obtained with very high permeability of 110,000 and a very low coercivity of 0.015 Oe by annealing the amorphous alloy at in 40 min.     

New fermions at the LHC and mass of the Higgs boson

Unification at MGUT∼3×¹⁰¹⁶ GeV$M_{\mathrm{GUT}}\sim 3\times {10}^{16}\text{GeV}$ of the three Standard Model (SM) gauge couplings can be achieved by postulating the existence of a pair of vectorlike fermions carrying SM charges and masses of order 300 GeV–1 TeV. The presence of these fermions significantly modifies the vacuum stability and perturbativity bounds on the mass of the SM Higgs boson. The new vacuum stability bound in this extended SM is estimated to be 117 GeV, to be compared with the SM prediction of about 128 GeV. An upper bound of 190 GeV is obtained based on perturbativity arguments. The impact on these predictions of type I seesaw physics is also discussed. The discovery of a relatively ‘light’ Higgs boson with mass ∼117 GeV$\sim 117\text{GeV}$ could signal the presence of new vectorlike fermions within reach of the LHC.