Miracle-dz/UniFAR-FTUs huggingface dataset:
Gold Complexes in Anticancer Therapy: From New Design Principles to Particle-Based Delivery Systems.

The discovery of the medicinal properties of gold complexes has fuelled the design and synthesis of new anticancer metallodrugs, which have received special attention due to their unique modes of action. Current research in the development of gold compounds with therapeutic properties is predominantly focused on the molecular design of drug leads with superior pharmacological properties, e.g., by introducing targeting features. Moreover, intensive research aims at improving the physicochemical properties of gold compounds, such as chemical stability and solubility in the physiological environment. In this regard, the encapsulation or chemical grafting of gold compounds to targeted delivery vectors/materials could lead to new nanomedicines eventually reaching clinical applications. Herein, we provide an overview of the state-of-the-art progress of gold anticancer compounds but more importantly we thoroughly revise the development of nanoparticle-based delivery systems for gold chemotherapeutics.
Proper motion analysis of the jet of R Aquarii

We have observed the jet of R Aquarii at high resolution with the VLA in 1992.83 and in 1999.78. Observations in the first epoch have resolved the base of the jet which shows a helical structure. We cannot detect the expected new jet component at either epoch. This does not disprove the idea of periodic ejection. Either the timing inferred from the acceleration models, or the assumed periastron passage is incorrect. Alternatively, a single new component cannot be resolved due to the dense core. Proper motion analysis of the jet components shows that previously derived acceleration models do not fit our new data. Indeed, the first ∼1 �� of the jet, both to north-east and south-west, appears fixed and has slowly moving shocks at the termination points, whereas the positions of the outer components fit best a ballistic orbit. We propose that the components are formed due to enhanced matter flow at periastron, accelerated during the first 1 �� and then ejected as bullets. Component A at a distance of ∼4 �� from the core has broken into two parts, similar to what was previously assumed to have happened to the outermost components B and D. The disruption is probably a consequence of a reverse shock or a collision with a cloud.
Utilization of a Gender‐Based Sorting Machine for Crustacean Selection in Bioconcentration Studies with the Freshwater Amphipod Hyalella azteca

Bioconcentration factors (BCFs) are determined by fish flow‐through tests performed according to Organisation for Economic Co‐operation and Development test guideline 305. These are time‐consuming and expensive and use a large number of animals. An alternative test design using the freshwater amphipod Hyalella azteca for bioconcentration studies has been recently developed and demonstrated a high potential. For bioconcentration studies using H. azteca, male amphipods are preferred compared with female organisms. Manual sexing of male adult amphipods is, however, time‐consuming and requires care and skill. A new fully automatic sorting and dispensing machine for H. azteca based on image analysis has recently been developed by the company Life Science Methods. Nevertheless, an anesthesia step is necessary prior to the automatic selection. In the present study, we show that a single‐pulse of 90 min of tricaine at the concentration of 1 g/L can be used and is recommended to select H. azteca males manually or automatically using the sorting machine. In the second part, we demonstrate that the machine has the ability to select, sort, and disperse the males of a culture batch of H. azteca as efficiently as manual procedures. In the last part of the study, BCFs of two organic substances were evaluated using the H. azteca bioconcentration test (HYBIT) protocol, with an anesthetizing step and robotic selection compared with manual selection without an anesthetizing step. The different BCF values obtained were in accordance with those indicated in the literature and showed that an anesthetizing step had no effect on the BCF values. Therefore, these data validated the interest in this sorting machine for selecting males to perform bioconcentrations studies with H. azteca. Environ Toxicol Chem 2023;42:1075–1084. © 2023 SETAC
In-vitro Activity of Delpazolid and Comparator Agents Against Methicillin-resistant Staphylococcus aureus Involved in Bloodstream Infection

Linezolid is a treatment option for methicillin-resistant Staphylococcus aureus (MRSA) bacteremia; however, its use is restricted due to toxic effects and resistance induction [1-4]. Delpazolid (LCB01-0371) is a novel, second-generation oxazolidinone ana-log developed by LegoChem Biosciences Inc. (Daejeon, Korea)
Current and temperature variability on the continental slope

Observations of temperature and currents have been made in the lower part of the water column on the western slope of the Porcupine Bank southwest of Ireland where the water depth is about 3500 m. Moored and lowered instruments were used to study the processes that may lead to mixing and diapycnal transfer. A poleward Eulerian mean flow of about 2.5 cm s-1 is found in the bottom 250 m, with current direction rotating anticlockwise as the bottom is approached. The shear between 30 and 90 m off the bottom is, on average, geostrophic and the temperature variation at a point averaged over several tidal cycles is dominated by along-slope advection. There is, however, considerable variability, with strong semidiurnal oscillations in both current and temperature. There is a downward phase propagation in temperature at these frequencies indicating the presence of baroclinic M 2 waves. It is possible that these are responsible for the apparent along and off-slope fluxes of heat that are observed. Fluctuations with periods of 5-6 days appear to propagate polewards along slope with phase speeds of about 13 cm s-1, but have constant phase lines lying roughly north-south at an acute angle to the mean contours of the slope. Profiles of potential temperature obtained by using a lowered conductivity, temperature and depth (ctd) instrument show the presence of frequent inversions in the lower 150 m, sometimes exceeding 30 m in height. A moored array of platinum resistance thermometers sampling at 10 s intervals indicates that the inversions are associated with the semidiurnal variability in temperature, the most frequent inversions occurring when the temperature 10 m off the bottom is greatest and when the temperature is falling at higher levels with a component of the current directed upslope. Indirect estimates of the vertical diffusivity and turbulent dissipation are derived from the observed scales of inversions and the overall stratification. These are subject to considerable uncertainty but suggest that the contribution to turbulence in the boundary layer from the inversions may exceed that supplied by the shear stress on the sea bed. Sources in instability are discussed, and one is examined analytically. An exact steady or time-dependent solution of flow of a stratified fluid parallel to a sloping boundary is derived. Solutions in which the density remains statically stable are possible only when a rather delicate balance exists between flow, stratification and diffusion.
Bumetanide increases postsynaptic inhibition after chronic SCI and decreases presynaptic inhibition with step‐training

Current anti‐spastic medication significantly compromises motor recovery after spinal cord injury (SCI), indicating a critical need for alternative interventions. Because a shift in chloride homeostasis decreases spinal inhibition and contributes to hyperreflexia after SCI, we investigated the effect of bumetanide, an FDA‐approved sodium‐potassium‐chloride intruder (NKCC1) antagonist, on presynaptic and postsynaptic inhibition. We compared its effect with step‐training as it is known to improve spinal inhibition by restoring chloride homeostasis. In SCI rats, a prolonged bumetanide treatment increased postynaptic inhibition but not presynaptic inhibition of the plantar H‐reflex evoked by posterior biceps and semitendinosus (PBSt) group I afferents. By using in vivo intracellular recordings of motoneurons, we further show that a prolonged bumetanide increased postsynaptic inhibition by hyperpolarizing the reversal potential for inhibitory postsynaptic potentials (IPSPs) after SCI. However, in step‐trained SCI rats an acute delivery of bumetanide decreased presynaptic inhibition of the H‐reflex, but not postsynaptic inhibition. These results suggest that bumetanide might be a viable option to improve postsynaptic inhibition after SCI, but it also decreases the recovery of presynaptic inhibition with step‐training. We discuss whether the effects of bumetanide are mediated by NKCC1 or by off‐target effects.
Inhibition of CD73 expression or A2AR blockade reduces MRP1 expression and increases the sensitivity of cervical cancer cells to cisplatin

Recently, a link between the biological activity of CD73 in solid tumors and multidrug resistance protein (MRP) has been proposed. Cisplatin (CP) is the most widely used anticancer agent to treat advanced and recurrent cervical cancer (CC). However, multidrug resistance protein‐1 (MRP1) is overexpressed in approximately 85% of these tumors and has been strongly associated with cisplatin resistance (CPR). In this study, we examine the involvement of CD73 and the interaction of adenosine (ADO) with its receptors (ARs) in MRP1 expression in CC cells. We found that ADO positively modulates MRP1 expression in CC cells in a dose‐dependent manner. The inhibition of CD73 expression with a CD73‐targeted siRNA and A2AR blockade with the selective antagonist ZM241385 significantly decreased MRP1 expression and the extrusive capacity of CC cells, making them significantly more sensitive to CP treatment than cancer cells treated with MK‐751, a specific MRP1 inhibitor. These results suggest CD73 inhibition or blocking ADO signaling through A2AR could be strategies to reverse CPR in patients with advanced or recurrent CC, which is characterized by very low response rates to CP (10%–20%).
Data integration using information and communication technology for emergency medical services and systems

© 2023 The Korean Society of Emergency Medicine Data integration using information and communication technology for emergency medical services and systems Ji Hoon Kim Department of Emergency Medicine, Yonsei University College of Medicine, Seoul, Korea Institute for Innovation in Digital Healthcare, Yonsei University, Seoul, Korea Clin Exp Emerg Med 2023;10(2):129-131 https://doi.org/10.15441/ceem.23. 003
The evolution of early‐life telomere length, pace‐of‐life and telomere‐chromosome length dynamics in birds

Telomeres, the short DNA sequences that protect chromosome ends, are an ancient molecular structure, which is highly conserved across most eukaryotes. Species differ in their telomere lengths, but the causes of this variation are not well understood. Here, we demonstrate that mean early‐life telomere length is an evolutionary labile trait across 57 bird species (representing 35 families in 12 orders) with the greatest trait diversity found among passerines. Among these species, telomeres are significantly shorter in fast‐lived than in slow‐lived species, suggesting that telomere length may have evolved to mediate trade‐offs between physiological requirements underlying the diversity of pace‐of‐life strategies in birds. This association was attenuated when excluding studies that may include interstitial telomeres in the estimation of mean telomere length. Curiously, within some species, larger individual chromosome size predicts longer telomere lengths on that chromosome, leading to the hypothesis that telomere length also covaries with chromosome length across species. We show that longer mean chromosome length or genome size tends to be associated with longer mean early‐life telomere length (measured across all chromosomes) within a phylogenetic framework constituting up to 31 bird species. These associations were strengthened when excluding highly influential outliers. However, sensitivity analyses suggested that they were susceptible to sample size effects and not robust to the exclusion of studies that may include interstitial telomeres. Combined, our analyses generalize patterns previously found within a few species and provide potential adaptive explanations for the 10‐fold variation in telomere lengths observed among birds.
Synthesis and evaluation of novel thiazole moiety-containing compounds as antibreast cancer agents

Progesterone receptor (PR) agonists represent pivotal agents in trapping breast cancer cells through modulating the expression of estrogen receptor (ER). The present investigation aimed to test three novel thiadiazole-containing compounds as antibreast cancer agents. Test compounds were synthesized and abbreviated as 2-{(5-amino-1, 3, 4-thiazole-2-yl) amino}-4-(4-chloro-3-methylphenyl)-4-oxobutanoic acid (TAB), 4-(4-chloro-3-methylphenyl)-4-oxo 2-[(5-sulfanyl-1, 3, 4-thiadiazol-2-yl)] sulfanyl-butanoic acid (TSB) and 4-(4-chloro-3-methylphenyl)-4-oxo 2-[(5-sulfanyl-1, 3, 4-thiadiazol-2-yl)] sulphonyl-botanic acid (TSSB). Molecular docking of the test compounds with PR was simulated. The IC50 of the test compounds against both Michigan cancer foundation-7 (MCF-7) and HepG2 was determined. Ehrlich solid tumor (EST) was grown in the right thigh of the mouse as a model of breast cancer in vivo. Hepatic and renal functions, besides hematological indicators, were tested. The expression of ER and ER genes in EST was determined using real-time PCR. Immunohistochemistry was carried out for the determination of Ki-67 and cyclin-dependent kinase 1 (CDK-1) in EST. Our results revealed that TAB, TSB and TSSB reduced Ehrlich tumor size by 48, 64 and 52%, respectively, compared to the EST control group. The docking scores achieved by TAB, TSB and TSSB with PR were −9.29, −9.41 and −9.24 kcal/mol, respectively. The most potent compound against MCF-7 was TSB, with an IC50 of 3.9 g/ml. The administration of test compounds suppressed Ki-67 and CDK1, and the best effect was observed at TSB. Our findings suggest that test compounds are applicants to be antibreast cancer agents.
Global aspects of the NGC 6334 star formation complex: an infrared survey

The results of a near-IR survey of the NGC 6334 massive H II region/molecular cloud region are presented. No widespread population of embedded stars is found in the cloud within the sensitivity limit. Three new possible premain-sequence objects are found. The mapping of near-IR extended emission is shown to be invaluable in pinpointing obscured H II regions. The locations of the youngest objects in NGC 6334 relative to evolved high-mass objects and H II regions show a likely causal link involving stellar winds or ionizing radiation, in the initiation of star formation. 53 refs.
Polymorphic Lambda Calculus with Dynamic Types

In an open programming system dynamic type checking is needed to safely link statically typed components. Since type case destroys the parametricity of type abstraction, dynamically generated type names are needed to hide the implementation of abstract types. Rossberg [8] was the first to analyse the problem and to propose a calculus that solves it. We will greatly simplify Rossberg’s calculus by developing a calculus, λ F , an extension of System F that provides constructs for type case and a binder for new type names. We will also develop a calculus, λLs , that extends the simply typed λ-calculus with call-by-need evaluation as this can be used to express lazy linking of components [9]. We will prove the safety properties for both calculi.
Revisiting the orthogonality of Bessel functions of the first kind on an infinite interval

The rigorous proof of the orthogonality integral ∫ 0 ∞ &rgr; J &ngr; ( k &rgr; ) J &ngr; ( k ′ &rgr; ) d &rgr; = δ ( k − k ′ ) k ? > , for &ngr; ≥ − 1 , ? > is laborious and requires the use of mathematical techniques that, probably, are unfamiliar to most physics students, even at the graduate level. In physics, we are used to the argument that it may be proved by the use of Hankel transforms. However, the logic of the matter is the opposite, i.e., the existence of the inverse Hankel transform is a consequence of the orthogonality integral. The goal of this work is to prove this integral without circular reasoning. In this paper, using elementary properties of Bessel functions, we give a simple analytical derivation of this integral for the case where ν is an integer, zero, or half-integer not less than − 1 / 2 ? > . Then, using the asymptotic behaviour of J &ngr; ( x ) ? > , we extend the result to any &ngr; ≥ − 1 ? > . This work is of a pedagogical nature. Therefore, to add educational value to the discussion, we do not skip the details of the calculations.
Augmented Quaternion and Augmented Unit Quaternion Optimization

In this paper, we introduce and explore augmented quaternions and augmented unit quaternions, and present an augmented unit quaternion optimization model. An augmented quaternion consist of a quaternion and a translation vector. The multiplication rule of augmented quaternion is defined. An augmented unit quaternion consists of a unit quaternion and a translation vector. The augmented unit quaternions form a Lie group. By means of augmented unit quaternions, we study the error model and kinematics. Then we formulate two classical problems in robot research, i.e., the hand-eye calibration problem and the simultaneous localization and mapping (SLAM) problem as augmented unit quaternion optimization problems, which are actually real smooth spherical equality constrained optimization problems. Comparing with the corresponding unit dual quaternion optimization model, the augmented unit quaternion optimization model has less variables and removes the orthogonality constraints.
Partitioning edges of a planar graph into linear forests and a matching

We show that the edges of any planar graph of maximum degree at most 9 can be partitioned into four linear forests and a matching. Combined with known results, this implies that the edges of any planar graph G $G$ of odd maximum degree Δ≥9 ${\rm{\Delta }}\ge 9$ can be partitioned into Δ−12 $\frac{{\rm{\Delta }}-1}{2}$ linear forests and one matching. This strengthens well‐known results stating that graphs in this class have chromatic index Δ ${\rm{\Delta }}$ and linear arboricity at most ⌈(Δ+1)∕2⌉ $\lceil ({\rm{\Delta }}+1)\unicode{x02215}2\rceil $ .
Optimistic Planning by Regularized Dynamic Programming

We propose a new method for optimistic planning in infinite-horizon discounted Markov decision processes based on the idea of adding regularization to the updates of an otherwise standard approximate value iteration procedure. This technique allows us to avoid contraction and monotonicity arguments typically required by existing analyses of approximate dynamic programming methods, and in particular to use approximate transition functions estimated via least-squares procedures in MDPs with linear function approximation. We use our method to recover known guarantees in tabular MDPs and to provide a computationally efficient algorithm for learning near-optimal policies in discounted linear mixture MDPs from a single stream of experience, and show it achieves near-optimal statistical guarantees.
An Effective Nonparametric Quantile Regression Method for Solving the Crossing Problem in Data Fitting Process

Nonparametric quantile regression method can be used as the first choice for some biostatistical data. Since the nonparametric quantile regression curves are estimated individually, the quantile curves can cross, leading to an invalid distribution estimation for the response. A simple nonparametric quantile regression method is proposed to avoid the crossing problem. The method uses nonparametric conditional density function estimate instead of the conditional distribution estimate to assure quantile regression function monotonous. Both a simulation study and an analysis of real salmon lustrousness data show the significant improvement of the method in solving the quantile crossing problem for some kind of biological data.
Hierarchical analogues to fractional relaxation equations

Recently fractional calculus has become an important tool in the analysis of slow relaxation phenomena, such as stress-strain relationships in polymeric materials. In the rheological constitutive equations this implies the replacement of the first-order derivatives by fractional derivatives. Here we show that such procedures have hierarchical mechanical analogues. We focus on the generalized dashpot and the generalized Maxwell model and display the corresponding arrangements. Our models allow a transparent interpretation of the parameters which enter the fractional equations, and reveal that the internal dynamics are hierarchically constrained.
Random-Order Enumeration for Self-Reducible NP-Problems

In plenty of data analysis tasks, a basic and time-consuming process is to produce a large number of solutions and feed them into downstream processing. Various enumeration algorithms have been developed for this purpose. An enumeration algorithm produces all solutions of a problem instance without repetition. To be a statistically meaningful representation of the solution space, solutions are required to be enumerated in uniformly random order. This paper studies a set of self-reducible NP-problems in three hierarchies, where the problems are polynomially countable ($Sr_{NP}^{FP}$), admit FPTAS ($Sr_{NP}^{FPTAS}$), and admit FPRAS ($Sr_{NP}^{FPRAS}$), respectively. The trivial algorithm based on a (almost) uniform generator is in fact inefficient. We provide a new insight that the (almost) uniform generator is not the end of the story. More efficient algorithmic frameworks are proposed to enumerate solutions in uniformly random order for problems in these three hierarchies. (1) For problems in $Sr_{NP}^{FP}$, we show a random-order enumeration algorithm with polynomial delay (PDREnum); (2) For problems in $Sr_{NP}^{FPTAS}$, we show a Las Vegas random-order enumeration algorithm with expected polynomial delay (PDLVREnum); (3) For problems in $Sr_{NP}^{FPRAS}$, we devise a fully polynomial delay Atlantic City random-order enumeration algorithm with expected delay polynomial in the input size and the given error probability $\delta$ (FPACREnum), which has a probability of at least $1-\delta$ becoming a Las Vegas random-order enumeration algorithm. Finally, to further improve the efficiency of the random-order enumeration algorithms, based on the master/slave paradigm, we present a parallelization with 1.5-optimal enumeration delay and running time, along with the theoretical analysis.