Miracle-dz/UniFAR-FTUs huggingface dataset:
Synthesis of Isosteric Triterpenoid Derivatives and Antifungal Activity

Dermatomycoses are among the most widespread and common superficial and cutaneous fungal infections in humans. There is an urgent need to develop efficient and non‐toxic antimycotic agents with a specific spectrum of activity. Triterpenes have been demonstrated to exhibit a wide range of biological activities, including antifungal activities. In this study, through hemisynthesis, we aimed to obtain triterpene‐isosteric molecules from betulinic and ursolic acids to improve the antifungal activity and spectrum of action of these compounds. Six compounds were resynthesized and tested against eleven mucocutaneous and cutaneous mycotic agents. The results of the susceptibility assays were expressed as the minimal inhibitory concentration (MIC). The MIC values of the piperazinyl derivatives of ursolic and betulinic acids that were active against pathogenic yeasts were in the range of 16–32 μg/mL and 4–16 μg/mL, respectively, whereas fungicidal effects were observed at concentrations ranging from 16 to 128 μg/mL and 8 to 128 μg/mL, respectively. The piperazinyl derivative of betulinic acid exhibited an antifungal profile similar to that of terbinafine and was the most effective derivative against dermatophytes. This strategy led to a promising candidate for the development of a new antifungal agent.
Adaptive MLSE for DPSK in time- and frequency-selective channels

An adaptive equalizer structure based on a state space formulation and maximum likelihood sequence estimation (MLSE) is developed for a time-varying, frequency-selective channel. Differential phase shift keying (DPSK) is assumed at the transmitter and effective differential decoding is performed at the receiver. The standard models of a time-varying linear channel and the Karhunen-Loeve (KL) expansion underpin the receiver structure. Analytical and simulation results for the receiver are shown. The resulting receiver is a per-survivor structure.
Competition between disorder and Coulomb interaction in a two-dimensional plaquette Hubbard model

We have studied a disordered $N_{\rm c} \times N_{\rm c}$ plaquette Hubbard model on a two-dimensional square lattice at half-filling using a coherent potential approximation (CPA) in combination with a single-site dynamical mean field theory (DMFT) approach with a paramagnetic bath. Such a model conveniently interpolates between the ionic Hubbard model at $N_{\rm c}=\sqrt{2}$ and the Anderson model at $N_{\rm c} = \infty$ and enables the analysis of the various limiting properties. We confirmed that within the CPA approach a band insulator behavior appears for non-interacting strongly disordered systems with a small plaquette size $N_{\rm c} = 4$, while the paramagnetic Anderson insulator with nearly gapless density of states is present for large plaquette sizes $N_{\rm c}=48$. When the interaction $U$ is turned on in the strongly fluctuating random potential regions, the electrons on the low energy states push each other into high energy states in DMFT in a paramagnetic bath and correlated metallic states with a quasiparticle peak and Hubbard bands emerge, though a larger critical interaction $U$ is needed to obtain this state from the paramagnetic Anderson insulator ($N_{\rm c}=48$) than from the band insulator ($N_{\rm c}=4$). Finally, we observe a Mott insulator behavior in the strong interaction $U$ regions for both $N_{\rm c}=4$ and $N_{\rm c}=48$ independent of the disorder strength. We discuss the application of this model to real materials.
A New Model of Pneumococcal Lipoteichoic Acid Structure Resolves Biochemical, Biosynthetic, and Serologic Inconsistencies of the Current Model

ABSTRACT Lipoteichoic acid (LTA) is an essential bacterial membrane polysaccharide (cell wall component) that is attached to the membrane via a lipid anchor. According to the currently accepted structure of pneumococcal LTA, the polysaccharide is comprised of several repeating units, each of which starts with glucose and ends with ribitol, with the lipid anchor predicted to be Glc(β1→3)AATGal(β1→3)Glc(α1→3)-acyl2Gro, where AATGal is 2-acetamido-4-amino-2,4,6-trideoxy-d-galactose. However, this lipid anchor has not been detected in pneumococcal membranes. Furthermore, the currently accepted structure does not explain the Forssman antigen properties of LTA and predicts a molecular weight for LTA that is larger than its actual observed molecular weight. To resolve these problems, we used mass spectrometry to analyze the structure of LTA isolated from several pneumococcal strains. Our study found that the R36A pneumococcal strain produces LTA that is more representative of pneumococci than that previously characterized from the R6 strain. Analysis of LTA fragments obtained after hydrofluoric acid and nitrous treatments showed that the fragments were consistent with an LTA nonreducing terminus consisting of GalNAc(α1→3)GalNAc(β1→, which is the minimal structure for the Forssman antigen. Based on these data, we propose a revised model of LTA structure: its polysaccharide repeating unit begins with GalNAc and ends with AATGal, and its lipid anchor is Glc(α1→3)-acyl2Gro, a common lipid anchor found in pneumococcal membranes. This new model accurately predicts the observed molecular weights. The revised model should facilitate investigation of the relationship between LTA's structure and its function.
Growth-inhibitory and apoptosis-inducing effects of tanshinones on hematological malignancy cells and their structure–activity relationship

This study has investigated the growth-inhibitory and apoptosis-inducing effects of dihydrotanshinone, tanshinone I, tanshinone IIA, and cryptotanshinone on hematological malignancy cell lines, aiming to explore their structure–activity relationship. The growth-inhibitory effects of the tanshinones on K562 and Raji cells were assessed using a modified MTT assay; the apoptosis-inducing effects were assessed by fluorescence microscopy and flow cytometry analysis. The changes in cellular morphology were observed using an inverted phase-contrast microscope. MTT results revealed that these tanshinones inhibited cell proliferation in a concentration-dependent and time-dependent manner. The IC50 values of dihydrotanshinone, tanshinone I, tanshinone IIA, and cryptotanshinone for K562 cells were 3.50, 13.52, 19.32, and 47.52 &mgr;mol/l at 24 h; 1.36, 4.70, 5.67, and 22.72 &mgr;mol/l at 48 h; and 1.15, 1.59, 2.82, and 19.53 &mgr;mol/l at 72 h, and the values for Raji cells were 3.30, 4.37, 12.92, and 52.36 &mgr;mol/l at 24 h; 1.55, 1.71, 6.54, and 25.45 &mgr;mol/l at 48 h; and 1.07, 1.38, 1.89, and 18.47 &mgr;mol/l at 72 h. The flow cytometry analysis demonstrated that these tanshinones induced apoptosis of K562 cells in a concentration-dependent manner, and dihydrotanshinone as well as tanshinone I were more potent than tanshinone IIA and cryptotanshinone. Some noticeable apoptotic morphologies could be observed by fluorescence microscopy on tanshinones-treated Raji cells. Collectively, these tanshinones caused growth inhibition and apoptosis in hematological malignancy cell lines, with dihydrotanshinone being the most potent, followed by tanshinone I, tanshinone IIA, and cryptotanshinone. These results suggested that the structure of aromatic ring A enhanced the cytotoxicity and the structure of ring C may have contributed to the cytotoxicity, but the mechanisms need to be further investigated.
A Case–Control Study of a Sex-Specific Association between a 15q25 Variant and Lung Cancer Risk

Background: Genetic variants located at 15q25, including those in the cholinergic receptor nicotinic cluster (CHRNA5) have been implicated in both lung cancer risk and nicotine dependence in recent genome-wide association studies. Among these variants, a 22-bp insertion/deletion, rs3841324 showed the strongest association with CHRNA5 mRNA expression levels. However the influence of rs3841324 on lung cancer risk has not been studied in depth. Methods: We have, therefore, evaluated the association of rs3841324 genotypes with lung cancer risk in a case–control study of 624 Caucasian subjects with lung cancer and 766 age- and sex-matched cancer-free Caucasian controls. We also evaluated the joint effects of rs3841324 with single-nucleotide polymorphisms (SNP) rs16969968 and rs8034191 in the 15q25 region that have been consistently implicated in lung cancer risk. Results: We found that the homozygous genotype with both short alleles (SS) of rs3841324 was associated with a decreased lung cancer risk in female ever smokers relative to the homozygous wild-type (LL) and heterozygous (LS) genotypes combined in a recessive model [ORadjusted = 0.55, 95% confidence interval (CI), 0.31–0.89, P = 0.0168]. There was no evidence for a sex difference in the association between this variant and cigarettes smoked per day (CPD). Diplotype analysis of rs3841324 with either rs16969968 or rs8034191 showed that these polymorphisms influenced the lung cancer risk independently. Conclusions and Impact: This study has shown a sex difference in the association between the 15q25 variant rs3841324 and lung cancers. Further research is warranted to elucidate the mechanisms underlying these observations. Cancer Epidemiol Biomarkers Prev; 20(12); 2603–9. ©2011 AACR.
Induction of tumor necrosis factor alpha by the group- and type-specific polysaccharides from type III group B streptococci

Previous studies suggested that circulating tumor necrosis factor alpha (TNF-alpha) may have a pathophysiologic role in experimental neonatal sepsis induced by group B streptococci (GBS). This study was undertaken to investigate the ability of the type III and group-specific polysaccharides of GBS to induce TNF-alpha production and TNF-alpha-dependent lethality in neonatal rats. The cytokine was detected in plasma samples by the L929 cytotoxicity assay. Intracardiac injections of either polysaccharide induced dose-dependent, transient elevations in plasma TNF-alpha levels that returned to baseline values after 5 h. The group-specific antigen induced significantly higher mean peak TNF-alpha levels than the type III antigen (125 +/- 47 versus 44 +/- 15 U/ml with 70 mg/kg of body weight). Glycogen (70 mg/kg), used as a negative control, did not induce TNF-alpha. The lipopolysaccharide-neutralizing agent polymyxin B did not decrease TNF-alpha levels induced by either polysaccharide, ruling out contamination with endotoxin as a possible cause of TNF-alpha induction. Fifty percent lethal doses of the type III and group-specific antigens given as intracardiac injections were 105 and 16 mg/kg, respectively. Salmonella endotoxin, used as a positive control, had a 50% lethal dose of 0.1 mg/kg. The lethal activities of GBS polysaccharides, as well as endotoxin, were completely prevented by pretreatment of neonatal rats with the respective specific antibodies or anti-murine TNF-alpha serum. To assess the relative importance of the type-specific substance in TNF-alpha induction by whole bacteria, two unrelated GBS transposon mutants devoid of only the type-specific capsular polysaccharide (COH1-13 and COH31-15) were employed. Each of the heat-killed unencapsulated mutants was able to produce plasma TNF-alpha level elevations or TNF-alpha-dependent lethality but was significantly less efficient in these activities than the corresponding encapsulated wild-type strain. These data suggest that the presence of type-specific material on GBS is not necessary for the stimulation of TNF-alpha production. Type III capsular polysaccharide, however, can significantly increase the ability of GBS to induce TNF-alpha. Further studies will be needed to assess the importance of TNF-alpha induction by the group- and type-specific antigens in the pathophysiology of GBS disease.
ACTSA: Annotated Corpus for Telugu Sentiment Analysis

Sentiment analysis deals with the task of determining the polarity of a document or sentence and has received a lot of attention in recent years for the English language. With the rapid growth of social media these days, a lot of data is available in regional languages besides English. Telugu is one such regional language with abundant data available in social media, but it’s hard to find a labelled data of sentences for Telugu Sentiment Analysis. In this paper, we describe an effort to build a gold-standard annotated corpus of Telugu sentences to support Telugu Sentiment Analysis. The corpus, named ACTSA (Annotated Corpus for Telugu Sentiment Analysis) has a collection of Telugu sentences taken from different sources which were then pre-processed and manually annotated by native Telugu speakers using our annotation guidelines. In total, we have annotated 5457 sentences, which makes our corpus the largest resource currently available. The corpus and the annotation guidelines are made publicly available.
MicroRNA-155 Targets SMAD2 and Modulates the Response of Macrophages to Transforming Growth Factor-β*

Transforming growth factor-beta (TGF-β) is a pleiotropic cytokine with important effects on processes such as fibrosis, angiogenesis, and immunosupression. Using bioinformatics, we identified SMAD2, one of the mediators of TGF-β signaling, as a predicted target for a microRNA, microRNA-155 (miR-155). MicroRNAs are a class of small non-coding RNAs that have emerged as an important class of gene expression regulators. miR-155 has been found to be involved in the regulation of the immune response in myeloid cells. Here, we provide direct evidence of binding of miR-155 to a predicted binding site and the ability of miR-155 to repress SMAD2 protein expression. We employed a lentivirally transduced monocyte cell line (THP1–155) containing an inducible miR-155 transgene to show that endogenous levels of SMAD2 protein were decreased after sustained overexpression of miR-155. This decrease in SMAD2 led to a reduction in both TGF-β-induced SMAD-2 phosphorylation and SMAD-2-dependent activation of the expression of the CAGA12LUC reporter plasmid. Overexpression of miR-155 altered the cellular responses to TGF-β by changing the expression of a set of genes that is involved in inflammation, fibrosis, and angiogenesis. Our study provides firm evidence of a role for miR-155 in directly repressing SMAD2 expression, and our results demonstrate the relevance of one of the two predicted target sites in SMAD2 3′-UTR. Altogether, our data uncover an important role for miR-155 in modulating the cellular response to TGF-β with possible implications in several human diseases where homeostasis of TGF-β might be altered.
Relationship Between Peripheral Intravenous Catheter Dwell Time and the Development of Phlebitis and Infiltration

The purpose of this study was to evaluate whether lengthening the dwell time of peripheral IV catheters from 72 hours to 144 hours resulted in increased rates of phlebitis and/or infiltration. The study was conducted in medical/surgical units at a 110-bed teaching hospital with an IV team. Kaplan-Meier estimates of the success and failure and conditional failure probabilities were calculated for phlebitis and infiltration scores. Log rank tests were used to test for an association between the covariates and the time until failure. Drug irritation was the most significant predictor of phlebitis and infiltration rates in this study. The total difference in the estimated failure rates for the catheter lasting 6 days versus a new catheter inserted for another 3 days is 1.3%. Because the conditional failure probability estimates for days 4, 5, and 6 are slightly higher than for days 1, 2, and 3, consideration may be given to extending the dwell time of a peripheral IV catheter beyond 72 hours under certain circumstances.
Prevalence of diabetes mellitus and impaired fasting glucose levels in the Eastern Province of Saudi Arabia: results of a screening campaign.

INTRODUCTION This study aimed to estimate the prevalence of diagnosed and undiagnosed diabetes mellitus (DM) in the Eastern Province of Saudi Arabia, and to study its relationship with socioeconomic factors. METHODS The study targeted all Saudi subjects aged 30 years and above who resided in the Eastern Province in 2004. DM screening was conducted by taking the capillary fasting blood glucose (CFBG) after eight hours or more of fasting, or the casual capillary blood glucose (CCBG). A positive screening test for hyperglycaemia was defined as CFBG more than or equal to 100 mg/dl (5.6 mmol/l), or CCBG more than or equal to 140 mg/dl (7.8 mmol/l). A positive result was confirmed on another day through the measurement of fasting plasma glucose (FPG) levels from a venous sample. A diagnosis of DM was considered if FPG was more than or equal to 126 mg/dl (7.0 mmol/l), or when there was a history of a previous diagnosis. RESULTS Out of 197,681 participants, 35,929 (18.2 percent) had a positive history of DM or a positive screening test for hyperglycaemia. After confirmation by venous blood testing, the prevalence of DM dropped to 17.2 percent while the prevalence of newly diagnosed DM was 1.8 percent. The prevalence increased with age and was higher in women, widows, divorcees, those who had a low education level and the unemployed. CONCLUSION The prevalence of DM in Saudi Arabia is one of the highest reported in the world, and its yield of screening is high.
Topical provocation of fixed drug eruption

To determine whether topical provocation could be used for the diagnosis of fixed drug eruption (FDE) instead of systemic provocation, we applied the suspected drug at various concentrations (1–10%,) in either petrolatum, 94% ethanol or dimethyl sulphoxide (DMSO)as an open test on both clinically normal skin and on previous FDE lesions in 24 patients with established FDE due to phenazone salicylate, a sulphonamide, doxycycline, trimethoprim, chlormezanone, a barbiturate, or carbamazepine. In 18 of the 24 patients, local provocation of FDE was seen at sites of previous eruption but never on clinically normal skin. With some drugs, e.g. phenazone salicylate, positive provocation of FDE was seen with all the vehicles used; with sulphamethoxazole and trimethoprim, a positive result was seen only in DMSO. To study cross‐reactions to other phenazone derivatives in patients with an FDE caused by phenazone salicylate, we applied topical phenazone, aminophenazone and propyphenazone to sites of previous FDE lesions in three patients. In all three, a positive reaction was seen with phenazone, but only one patient showed positive results with aminophenazone and propyphenazone. The present study suggests that topical provocation is useful with several drugs causing FDE. Testing should always be performed on sites of previous FDE, and the sensitivity of the open topical testing can be increased in certain cases by using a vehicle which increases penetration of the drug.
Histopathological and Haematological Effects of Mosquito Coil Smoke on Lungs - An Experimental Study on Albino Rats

Introduction: Mosquito coils are the most preferred anti-mosquito products in many households of Asian countries like India. Short-term exposure to allethrin has been reported to cause toxic effects on respiratory system. Subjects and Methods: Thirty albino rats were divided into five groups (A, B, C, D, and E) of six animals each. Except group A (Control) rest (Group B-E) were exposed to mosquito coil smoke for 4, 6, 8 and 10 weeks respectively. Blood from all the animals was processed to estimate TLC (Total leucocyte count) and results thus attained were analysed using one-way ANOVA test. Rats were sacrificed to procure lung tissue, which was processed by paraffin embedding to obtain haematoxylin and Eosin stained sections. Results: There was significant increase (p value, 0.001) in TLC in all experimental groups compared to control ones. Conclusion: Degenerative changes were obtained in lung tissue of all experimental rats with maximum effect in group Adequate measures should be taken to ensure minimal exposure to coil smoke during domestic use.
Disparate effects of adenosine A1- and A2-receptor agonists on intrarenal blood flow.

Endogenous adenosine, secreted locally by the kidney during tissue hypoxia, induces heterogeneous renal hemodynamic responses. We investigated the cortical and outer medullary blood flow responses to intrarenal infusions of adenosine and adenosine A1- and A2-receptor agonists in anesthetized rats. These agents were infused into the renal interstitium through chronically implanted capsules, and blood flow was measured by laser-Doppler probes. Short (1 min, 0.05 ml) intrarenal infusions of adenosine (0.5 mumol) lowered cortical blood flow to 27 +/- 10% of baseline (n = 7, P < 0.0005). Medullary blood flow response was biphasic, i.e., a transient decrease in flow to 52 +/- 8% of baseline (n = 17, P < 0.0001) followed by a more-sustained increase in flow to 135 +/- 6% (n = 17, P < 0.0001). N6-cyclopentyladenosine, an adenosine receptor A1 agonist, reduced both cortical and medullary blood flow to 59 +/- 4% (n = 10, P < 0.0001) and 38 +/- 5% (n = 11, P < 0.0001) of baseline, respectively. By contrast, 2-[p- (carboxyethyl)phenethylamino]-5'-N-ethycarboxamidoadenosine (CGS-21680C), an adenosine receptor A2 agonist, increased dramatically the medullary blood flow to 184 +/- 15% of baseline (n = 12, P < 0.0005), without major changes in cortical flow. We conclude that intrarenal adenosine reduces cortical blood flow and predominantly increases medullary flow via A1 and A2 receptors, respectively. These hemodynamic responses could play a role in protection of the outer medulla from hypoxia.
Assessment of seasonal variations in plasma progesterone concentrations and the morphometry of corpus luteum and ovary during estrous in Nili-Ravi buffalo -

The influence of season on the plasma progesterone concentrations and morphometric values of corpus luteum and ovary was studied through ultrasonography in spring (n=10) and dry hot (n=10) seasons on alternate days during the estrous cycle regardless of estrous phases in Nili-Ravi buffaloes. The mean morphometric values of length and width of ovary and the diameter and area of corpus luteum were higher in spring than those in dry hot seasons. The plasma progesterone concentrations were determined by ELISA (Enzyme Linked Immuno Sorbent Assay) technique and influence of seasons was found significant (P
Do External Shocks Have a Permanent or a Transitory Effect on Thailand’s Tourism Industry?

Given the number and the frequency of external shocks encountered by Thailand in the last two decades, this study identifies the number and the location of the breaks and tests to determine whether the breaks have a transitory or a permanent effect on international tourist arrivals to Thailand for its top 10 source countries using both univariate and panel unit root tests with structural breaks. The findings suggest that break dates coincide with the Asian financial crisis, the September 11 attack, and the SARS and the bird flu outbreaks. The univariate unit root tests with structural breaks reject the null hypothesis of a nonstationarity in tourist arrivals from all countries. Furthermore, panel unit root tests with one and two structural breaks also reject the joint null hypothesis of a nonstationarity. These findings imply that external shocks have only a transitory effect on tourist arrivals and Thailand's tourism sector will return to its long-run equilibrium path.