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1.
Arch Pharm (Weinheim) ; 357(9): e2400242, 2024 Sep.
Article in English | MEDLINE | ID: mdl-38763904

ABSTRACT

Previously, we documented the synthesis and assessed the biological effects of chalcones containing selenium against HT-29 human colorectal adenocarcinoma cells, demonstrating their significant potential. As research on selenium-containing flavonoids remains limited, this article outlines our design and synthesis of three selenium-based flavonols and three 2-styrylchromones. We conducted evaluations of these compounds to determine their impact on human lung cancer cells (A549, H1975, CL1-0, and CL1-5) and their influence on normal lung fibroblast MRC5 cells. Additionally, we included selenium-based chalcones in our testing for comparative purposes. Our findings highlight that the simplest compound, designated as compound 1, exhibited the most promising performance among the tested molecules.


Subject(s)
Antineoplastic Agents , Chalcones , Flavonols , Humans , Antineoplastic Agents/pharmacology , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Chalcones/pharmacology , Chalcones/chemical synthesis , Chalcones/chemistry , Structure-Activity Relationship , Flavonols/pharmacology , Flavonols/chemical synthesis , Flavonols/chemistry , Cell Line, Tumor , Cell Proliferation/drug effects , Drug Screening Assays, Antitumor , Molecular Structure , Organoselenium Compounds/pharmacology , Organoselenium Compounds/chemical synthesis , Organoselenium Compounds/chemistry , Dose-Response Relationship, Drug , Chromones/pharmacology , Chromones/chemical synthesis , Chromones/chemistry , Cell Survival/drug effects , A549 Cells , Lung Neoplasms/drug therapy , Lung Neoplasms/pathology
2.
Arch Pharm (Weinheim) ; 356(4): e2200486, 2023 Apr.
Article in English | MEDLINE | ID: mdl-36587972

ABSTRACT

Selenium is an essential micronutrient that is beneficial to human health. Selenium-containing drugs have been developed as antioxidants, anti-inflammatory, and anticancer agents. However, the synthesis of selenium-containing chalcones has not been fully explored. Therefore, we report the synthesis of novel selenophene-based chalcone analogs and reveal their biological activities as anticancer agents. Among the seven synthesized molecules, compounds 6, 8, and 10 exhibited anticancer activity with IC50 values of 19.98 ± 3.38, 38.23 ± 3.30, and 46.95 ± 5.68 µM, respectively, against human colorectal adenocarcinoma (HT-29) cells. Clonogenic assays and Western blot analysis tests further confirmed that compound 6 effectively induced apoptosis in HT-29 cells through mitochondrial- and caspase-3-dependent pathways.


Subject(s)
Antineoplastic Agents , Chalcone , Chalcones , Selenium , Humans , Chalcones/pharmacology , Selenium/pharmacology , Structure-Activity Relationship , Cell Proliferation , Antineoplastic Agents/pharmacology , Apoptosis , Drug Screening Assays, Antitumor , Cell Line, Tumor , Molecular Structure
3.
Sci Rep ; 10(1): 7515, 2020 05 05.
Article in English | MEDLINE | ID: mdl-32372056

ABSTRACT

The reversible dye-terminator (RDT)-based DNA sequencing-by-synthesis (SBS) chemistry has driven the advancement of the next-generation sequencing technologies for the past two decades. The RDT-based SBS chemistry relies on the DNA polymerase reaction to incorporate the RDT nucleotide (NT) for extracting DNA sequence information. The main drawback of this chemistry is the "DNA scar" issue since the removal of dye molecule from the RDT-NT after each sequencing reaction cycle leaves an extra chemical residue in the newly synthesized DNA. To circumvent this problem, we designed a novel class of reversible (2-aminoethoxy)-3-propionyl (Aep)-dNTPs by esterifying the 3'-hydroxyl group (3'-OH) of deoxyribonucleoside triphosphate (dNTP) and examined the NT-incorporation activities by A-family DNA polymerases. Using the large fragment of both Bacillus stearothermophilus (BF) and E. coli DNA polymerase I (KF) as model enzymes, we further showed that both proteins efficiently and faithfully incorporated the 3'-Aep-dNMP. Additionally, we analyzed the post-incorporation product of N + 1 primer and confirmed that the 3'-protecting group of 3'-Aep-dNMP was converted back to a normal 3'-OH after it was incorporated into the growing DNA chain by BF. By applying all four 3'-Aep-dNTPs and BF for an in vitro DNA synthesis reaction, we demonstrated that the enzyme-mediated deprotection of inserted 3'-Aep-dNMP permits a long, continuous, and scar-free DNA synthesis.


Subject(s)
DNA Polymerase I/chemistry , DNA Replication , DNA/biosynthesis , Escherichia coli/enzymology , Geobacillus stearothermophilus/enzymology , Nucleotides/genetics , Amino Acid Motifs , Coloring Agents/chemistry , DNA Primers/genetics , Kinetics , Molecular Structure , Sequence Analysis, DNA , Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
4.
Sensors (Basel) ; 18(12)2018 Dec 16.
Article in English | MEDLINE | ID: mdl-30558381

ABSTRACT

Limited-angle iterative reconstruction (LAIR) reduces the radiation dose required for computed tomography (CT) imaging by decreasing the range of the projection angle. We developed an image-quality-based stopping-criteria method with a flexible and innovative instrument design that, when combined with LAIR, provides the image quality of a conventional CT system. This study describes the construction of different scan acquisition protocols for micro-CT system applications. Fully-sampled Feldkamp (FDK)-reconstructed images were used as references for comparison to assess the image quality produced by these tested protocols. The insufficient portions of a sinogram were inpainted by applying a context encoder (CE), a type of generative adversarial network, to the LAIR process. The context image was passed through an encoder to identify features that were connected to the decoder using a channel-wise fully-connected layer. Our results evidence the excellent performance of this novel approach. Even when we reduce the radiation dose by 1/4, the iterative-based LAIR improved the full-width half-maximum, contrast-to-noise and signal-to-noise ratios by 20% to 40% compared to a fully-sampled FDK-based reconstruction. Our data support that this CE-based sinogram completion method enhances the efficacy and efficiency of LAIR and that would allow feasibility of limited angle reconstruction.

5.
Med Biol Eng Comput ; 56(7): 1293-1303, 2018 Jul.
Article in English | MEDLINE | ID: mdl-29280093

ABSTRACT

Respiratory inductance plethysmography (RIP) sensor is an inexpensive, non-invasive, easy-to-use transducer for collecting respiratory movement data. Studies have reported that the RIP signal's amplitude and frequency can be used to discriminate respiratory diseases. However, with the conventional approach of RIP data analysis, respiratory muscle effort cannot be estimated. In this paper, the estimation of the respiratory muscle effort through RIP signal was proposed. A complementary ensemble empirical mode decomposition method was used, to extract hidden signals from the RIP signals based on the frequency bands of the activities of different respiratory muscles. To validate the proposed method, an experiment to collect subjects' RIP signal under thoracic breathing (TB) and abdominal breathing (AB) was conducted. The experimental results for both the TB and AB indicate that the proposed method can be used to loosely estimate the activities of thoracic muscles, abdominal muscles, and diaphragm. Graphical abstract ᅟ.


Subject(s)
Algorithms , Respiration , Respiratory Muscles/physiology , Female , Humans , Male , Plethysmography , Signal Processing, Computer-Assisted , Young Adult
6.
Biomed Eng Online ; 15(1): 112, 2016 Oct 06.
Article in English | MEDLINE | ID: mdl-27716248

ABSTRACT

BACKGROUND: Thoracoabdominal asynchrony is often adopted to discriminate respiratory diseases in clinics. Conventionally, Lissajous figure analysis is the most frequently used estimation of the phase difference in thoracoabdominal asynchrony. However, the temporal resolution of the produced results is low and the estimation error increases when the signals are not sinusoidal. Other previous studies have reported time-domain procedures with the use of band-pass filters for phase-angle estimation. Nevertheless, the band-pass filters need calibration for phase delay elimination. METHODS: To improve the estimation, we propose a novel method (named as instantaneous phase difference) that is based on complementary ensemble empirical mode decomposition for estimating the instantaneous phase relation between measured thoracic wall movement and abdominal wall movement. To validate the proposed method, experiments on simulated time series and human-subject respiratory data with two breathing types (i.e., thoracic breathing and abdominal breathing) were conducted. Latest version of Lissajous figure analysis and automatic phase estimation procedure were compared. RESULTS: The simulation results show that the standard deviations of the proposed method were lower than those of two other conventional methods. The proposed method performed more accurately than the two conventional methods. For the human-subject respiratory data, the results of the proposed method are in line with those in the literature, and the correlation analysis result reveals that they were positively correlated with the results generated by the two conventional methods. Furthermore, the standard deviation of the proposed method was also the smallest. CONCLUSIONS: To summarize, this study proposes a novel method for estimating instantaneous phase differences. According to the findings from both the simulation and human-subject data, our approach was demonstrated to be effective. The method offers the following advantages: (1) improves the temporal resolution, (2) does not introduce a phase delay, (3) works with non-sinusoidal signals, (4) provides quantitative phase estimation without estimating the embedded frequency of breathing signals, and (5) works without calibrated measurements. The results demonstrate a higher temporal resolution of the phase difference estimation for the evaluation of thoracoabdominal asynchrony.


Subject(s)
Abdominal Wall/physiology , Movement , Respiration , Signal Processing, Computer-Assisted , Thoracic Wall/physiology , Female , Humans , Male , Time Factors , Young Adult
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