Notes

Phylogenetic good vascular seed metabolism revealed using a macroevolutionary widespread yard.
We report here a series of coordinatively-saturated and thermodynamically stable luminescent [Ln(dtntp)(H2O)] [Ln(III) = Eu (1), Tb (2), Gd (3), Sm (4) and Dy (5)] complexes using an aminophenyl-terpyridine appended-DTPA (dtntp) chelating ligand as cell imaging and photocytotoxic agents. The N,N″-bisamide derivative of H5DTPA named as dtntp is based on 4'-(4-aminophenyl)-2,2'6',2″-terpyridine conjugated to diethylenetriamine-N,N',N″-pentaacetic acid. The structure, physicochemical properties, detailed photophysical aspects, interaction with DNA and serum proteins, and photocytotoxicity were studied. The intrinsic luminescence of Eu(III) and Tb(III) complexes due to f → f transitions used to evaluate their cellular uptake and distribution in cancer cells. The solid-state structure of [Eu(dtntp)(DMF)] (1·DMF) shows a discrete mononuclear molecule with nine-coordinated EuN3O6 distorted tricapped-trigonal prism (TTP) coordination geometry around the Eu(III). The EuN3O6 core results from three nitrogen atoms aed intracellular (cytosolic and nuclear) localization in cancer cells. The complexes 1 and 2 displayed significant photocytotoxicity in HeLa cells. These results offer a modular design strategy with further scope to utilize appended N,N,N-donor tpy moiety for developing light-responsive luminescent Ln(III) bioprobes for theranostic applications.Terahertz technology has been widely used in biomedical research. Herein, terahertz time-domain attenuated total reflection (THz TD-ATR) spectroscopy was employed to characterize and discriminate human cancer cell lines (DLD-1 and HT-29). Terahertz responses of the cell lines were measured and Savitzky-Golay algorithm was applied to smooth the spectra of refractive index, absorption coefficient and dielectric loss tangent in terahertz regime. Principal component analysis (PCA) was then adopted for feature extraction and cell characterization. Based on the processed data, cancer cell lines were discriminated by applying random forests (RF) method to analyze three characteristic parameters separately and the results from them were compared. Results indicate that absorption coefficient was the most sensitive parameter for cancer cell discrimination. Our study suggests great potential for human cancer cell recognition and provides experimental basis for liquid biopsy.Biochemical characterization of polyphenol oxidase (PPO) present in purple sweet potato (PSP) is a key step in developing efficient methodologies to control oxidative damage caused by this enzyme to the valuable components of PSP, such as caffeoylquinic acid derivatives and acylated anthocyanins. Thus, this work focused on the assessment of the effects of pH, temperature, and chemical agents on the PPO activity as well as characterization of the PPO substrate specificity towards major phenolic compounds found in PSP. The optimum conditions of enzyme activity were pH 7 and a temperature range of 20-30 °C at which phenolic substrates were oxidized with 72.5-99.8% yield. Zn2+ ions remarkably reduced PPO activity while Cu2+ ions improved enzyme performance. The highest substrate preference was shown for 3,4,5-tri-caffeoylquinic and 3,5-di-caffeoylquinic acid, followed by 5-caffeoylquinic and caffeic acid, 3,4- and 4,5-di-caffeoylquinic acids, peonidin-3-caffeoyl-p-hydroxybenzoyl-sophoroside-5-glucoside. The highest Km values were found for 4,5-feruloyl-caffeoylquinic acid and catechol.
Sleep disturbances are common in neuromyelitis optica spectrum disorder (NMOSD) and have a great impact on patients' quality of life. According to a report, there is a 64% prevalence of poor sleep quality in NMOSD patients. Therefore, this study was done to evaluate the effect of sleep disturbances on NMOSD acute exacerbations.

This case-control study was conducted at Sina Hospital in 2019. A total of 60 patients with NMOSD diagnosis were enrolled in the study (30 patients were in the remission phase while 30 patients were hospitalized due to acute attacks). Sleep disorders were evaluated in both groups. Sleep quality was assessed during the last month using the Pittsburgh Sleep Quality Index (PSQI) questionnaire. Data were analyzed by SPSS software version 21.

Among 60 patients who were evaluated in both the control and attack groups, 86.7% were female. The duration of the disease was 68.23 ± 42.89 months in the control group and 69.83 ± 6.90 in the attack group. The mean age of patients was 34.15 years old. Sleep quality was unfavorable in 30% and 56% of patients in control and attack groups, respectively. There were significant differences between the two groups in sleep latency, habitual sleep efficiency, sleep duration, and sleep disturbance.

The present study revealed that there was a significant difference in sleep quality between controls and attack patients and could show a direct relationship between sleep disorders and NMOSD attacks.
The present study revealed that there was a significant difference in sleep quality between controls and attack patients and could show a direct relationship between sleep disorders and NMOSD attacks.A fully-automated deep learning algorithm matched performance of radiologists in assessment of knee osteoarthritis severity in radiographs using the Kellgren-Lawrence grading system.
To develop an automated deep learning-based algorithm that jointly uses Posterior-Anterior (PA) and Lateral (LAT) views of knee radiographs to assess knee osteoarthritis severity according to the Kellgren-Lawrence grading system.

We used a dataset of 9739 exams from 2802 patients from Multicenter Osteoarthritis Study (MOST). The dataset was divided into a training set of 2040 patients, a validation set of 259 patients and a test set of 503 patients. A novel deep learning-based method was utilized for assessment of knee OA in two steps (1) localization of knee joints in the images, (2) classification according to the KL grading system. Our method used both PA and LAT views as the input to the model. The scores generated by the algorithm were compared to the grades provided in the MOST dataset for the entire test set as well as eed with radiologists at our institution to the same extent as the radiologists with each other. The algorithm could be used to provide reproducible assessment of knee osteoarthritis severity.Multimodal image registration has many applications in diagnostic medical imaging and image-guided interventions, such as Transcatheter Arterial Chemoembolization (TACE) of liver cancer guided by intraprocedural CBCT and pre-operative MR. The ability to register peri-procedurally acquired diagnostic images into the intraprocedural environment can potentially improve the intra-procedural tumor targeting, which will significantly improve therapeutic outcomes. However, the intra-procedural CBCT often suffers from suboptimal image quality due to lack of signal calibration for Hounsfield unit, limited FOV, and motion/metal artifacts. These non-ideal conditions make standard intensity-based multimodal registration methods infeasible to generate correct transformation across modalities. While registration based on anatomic structures, such as segmentation or landmarks, provides an efficient alternative, such anatomic structure information is not always available. One can train a deep learning-based anatomy extractor, but it requires large-scale manual annotations on specific modalities, which are often extremely time-consuming to obtain and require expert radiological readers. To tackle these issues, we leverage annotated datasets already existing in a source modality and propose an anatomy-preserving domain adaptation to segmentation network (APA2Seg-Net) for learning segmentation without target modality ground truth. The segmenters are then integrated into our anatomy-guided multimodal registration based on the robust point matching machine. Orlistat manufacturer Our experimental results on in-house TACE patient data demonstrated that our APA2Seg-Net can generate robust CBCT and MR liver segmentation, and the anatomy-guided registration framework with these segmenters can provide high-quality multimodal registrations.Targeting P-glycoprotein (P-gp, ABCB1 transporter), which plays an essential role in multi-drug resistance (MDR) in cancers, with new cytotoxic agents is a promising strategy in cancer chemotherapy. In the current study, we report the synthesis of thirteen novel pyrimidopyrrolizine, pyrimidoindolizine, and diazepinopyrrolizine derivatives. The new compounds exhibited cytotoxic activities against MCF7, A2780 and HT29 cancer cell lines (IC50 = 0.02-19.58 μM) and MRC5 (IC50 = 0.17-20.57 μM). The six most active compounds (23b, 24a,b and, 31c-e) were evaluated for their MDR reversal activities in MCF7/ADR cells. Mechanistic study using real-time PCR revealed the ability of compound 31c to inhibit P-gp. In addition, compound 31c increased the accumulation of Rho123 inside MCF7/ADR cells in a dose-dependent manner compared to verapamil. Compound 31c arrested the cell cycle of MCF7 cells at the G1 phase. Compound 31c also caused a significant dose-dependent increase of early and late apoptotic events. Molecular docking analysis revealed a high binding affinity for compound 31c toward P-gp. Like zosuquidar, compound 31c displayed one hydrogen bond and several hydrophobic interactions with amino acids in P-gp. These results indicated that compound 31c represents a potential anticancer candidate with MDR reversal activity.The cyanobacterial oligopeptides are recognized for being highly selective, efficacious and relatively safer compounds with diverse bioactivities. Azoline-based natural compounds consist of heterocycles which are reduced analogues of five-membered heterocyclic azoles. Among other varieties of azoline-based natural compounds, the heteropeptides bearing oxazoline or thiazoline heterocycles possess intrinsic structural properties with captivating pharmacological profiles, representing excellent templates for the design of novel therapeutics. The specificity of heteropeptides has been translated into prominent safety, tolerability, and efficacy profiles in humans. These peptidic congeners serve as ideal intermediary between small molecules and biopharmaceuticals based on their typically low production complexity compared to the protein-based biopharmaceuticals. The distinct bioproperties and unique structures render these heteropeptides one of the most promising lead compounds for drug discovery. The high degree of chemical diversity in cyanobacterial secondary metabolites may constitute a prolific source of new entities leading to the development of new pharmaceuticals. This review focuses on the azoline-based natural oligopeptides with emphasis on distinctive structural features, stereochemical aspects, biological activities, structure activity relationship, synthetic and biosynthetic aspects as well as mode of action of cyanobacteria-derived peptides.Malaria is a major parasitic disease in tropical and sub-tropical regions. Pertaining to the sustaining resistance in malarial parasite against the available drugs, novel treatment options are the need of the hour. In this resolve recently, focus has shifted to finding the natural alternatives that possess anti-plasmodial activity for combatting malaria. Drawing on the text written in ancient scriptures and Ayurveda, natural compounds are now being screened for their therapeutic properties. Indole is one such natural compound, present in all living organisms, it displays a range of therapeutic activities including anticancer, anti-inflammatory, antimalarial etc. In this review, we have discussed various indole scaffold as well as the semi-synthetic drugs containing indole moiety that have been synthesized for malaria treatment.
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