Digital twin technology can be used for disaster safety management of underground utility tunnels, which are social infrastructures. To verify its efficiency in an underground utility tunnel, it must ...be implemented and monitored in the real world. Therefore, the state of information about an object and the position of an object in the real world, which can change upon movement, should be correspondingly reflected in the digital model. Underground utility tunnels are monitored through closed circuit television (CCTV) cameras because the main infrastructure facilities are installed in a long and narrow form, which limits access to them. Therefore, synchronization of a digital twin model of an underground utility tunnel requires a method for identifying the location of an object through an installed CCTV camera. This study compares the DenseDepth transfer learning method and the coordinate system conversion method through floor plan projection to estimate depth using a single CCTV camera installed in an underground utility tunnel. The coordinate system conversion method through floor plane projection showed an error of 0.23 m to 1.5 m within a 50 m range. The DenseDepth transfer learning method showed an error of 1 m to 3 m; therefore, it was considered unsuitable for distance estimation. The coordinate system conversion method through floor plane projection showed a smaller error even at a longer distance than the DenseDepth transfer learning method. Therefore, the coordinate system conversion method through floor plane projection was considered more suitable than the DenseDepth transfer learning method for depth estimation using a single camera.
(Lardizabalaceae) has been used as a traditional herbal medicine in Korea and China for its anti-inflammatory and analgesic properties. As part of a bioprospecting program aimed at the discovery of ...new bioactive compounds from Korean medicinal plants, a phytochemical study of
leaves was carried out leading to isolation of two oleanane-type triterpene saponins, 3-
-
-d-glucopyranosyl (1→2)-
-l-arabinopyranosyl oleanolic acid-28-
-
-d-glucopyranosyl (1→6)-
-d-glucopyranosyl ester (
) and 3-
-
-l-arabinopyranosyl oleanolic acid-28-
-
-d-glucopyranosyl (1→6)-
-d-glucopyranosyl ester (
). Their structures were established unambiguously by spectroscopic methods such as one- and two-dimensional nuclear magnetic resonance and infrared spectroscopies, high-resolution electrospray ionization mass spectrometry and chemical reactions. Their anti-inflammatory activities were examined for the first time with an animal model for the macrophage-mediated inflammatory response as well as a cell-based assay using an established macrophage cell line (RAW 264.7) in vitro. Together, it was concluded that the saponin constituents, when they were orally administered, exerted much more potent activities in vivo than their sapogenin core even though both the saponins and the sapogenin molecule inhibited the RAW 264.7 cell activation comparably well in vitro. These results imply that saponins from
leaves have a definite advantage in the development of oral medications for the control of inflammatory responses.
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IZUM, KILJ, NUK, PILJ, PNG, SAZU, UL, UM, UPUK
T cell stimulation usually requires direct contact with viable antigen-presenting cells (APCs). However, we show here that small exosome-like membrane vesicles shed from APCs can be recognized ...by$na\ddot{\imath} ve\>CD8^+$T cells in the absence of viable APCs. T cell antigen receptor-dependent binding of vesicles by CD8+cells is MHC class I/peptide-specific and requires that the vesicles coexpress intercellular adhesion molecule 1 (ICAM-1, CD54), although not B7 (B7-1). In the absence of B7, T cell binding of vesicles is nonimmunogenic. By contrast, vesicles expressing both ICAM-1 and B7 are strongly immunogenic and cause purified APC-depleted CD8+cells to mount peptide-specific proliferative responses and differentiate into effector cells.
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BFBNIB, NMLJ, NUK, PNG, SAZU, UL, UM, UPUK
In this study, we developed a bioanalytical method using liquid chromatography coupled to triple quadrupole tandem mass spectrometry (LC-MS/MS) to apply to a pharmacokinetic study of inotodiol, which ...is known for its anti-cancer activity. Plasma samples were prepared with alkaline hydrolysis, liquid–liquid extraction, and solid-phase extraction. Inotodiol was detected in positive mode with atmospheric pressure chemical ionization by multiple-reaction monitoring mode using LC-MS/MS. The developed method was validated with linearity, accuracy, and precision. Accuracy ranged from 97.8% to 111.9%, and the coefficient of variation for precision was 1.8% to 4.4%. The developed method was applied for pharmacokinetic study, and the mean pharmacokinetic parameters administration were calculated as follows: λz 0.016 min−1; T1/2 49.35 min; Cmax 2582 ng/mL; Cl 0.004 ng/min; AUC0–t 109,500 ng×min/mL; MRT0–t 32.30 min; Vd 0.281 mL after intravenous administration at dose of 2 mg/kg and λz 0.005 min−1; T1/2 138.6 min; Tmax 40 min; Cmax 49.56 ng/mL; AUC0–t 6176 ng×in/mL; MRT0–t 103.7 min after oral administration. The absolute oral bioavailability of inotodiol was 0.45%, similar to nonpolar phytosterols. Collectively, this is the first bioanalytical method and pharmacokinetic study for inotodiol.
Eight compounds were isolated from the leaves of Clerodendrum inerme, including one new rearranged abietane diterpene, crolerodendrum B (1). Their structures were determined by means of spectroscopic ...methods including one-dimensional and two-dimensional nuclear magnetic resonance (1-D and 2-DNMR), high-resolution electrospray ionisation mass spectrometry (HR-ESI-MS) and circular dichroism (CD). The DPPH radical scavenging and cytotoxic activities of isolated compounds against MCF7 (breast), HCT116 (colon) and B16F10 (melanoma) cancer cell lines were evaluated. Compounds 1, 3 and 4 exhibited strong DPPH radical-scavenging effects (ED
50
values of 17.6 ± 2.1, 10.1 ± 0.8 and 11.3 ± 0.3 μM, respectively) and 4 showed strong cytotoxicity against the HCT116 cell line (IC
50
= 3.46 ± 0.01 μM).
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BFBNIB, GIS, IJS, KISLJ, NUK, PNG, UL, UM, UPUK
The total synthesis and evaluation of iso-duocarmycin SA (5) and iso-yatakemycin (6), representing key analogues of the corresponding natural products incorporating an isomeric alkylation subunit, ...are detailed. This pyrrole isomer of the natural alkylation subunit displayed an enhanced reaction regioselectivity and a 2-fold diminished stability. Although still exceptionally potent, the iso-duocarmycin SA derivatives and natural product analogues exhibited a corresponding approximate 3−5-fold reduction in cytotoxic activity L1210 IC50 for (+)-iso-duocarmycin SA = 50 pM and for (+)-iso-yatakemycin = 15 pM consistent with their placement on a parabolic relationship correlating activity with reactivity. The DNA alkylation selectivity of the resulting key natural product analogues was unaltered by the structure modification in spite of the minor-groove presentation of a potential H-bond donor. Additionally, a unique ortho-spirocyclization with such derivatives was explored via the preparation, characterization, and evaluation of 34 that is incapable of the more conventional para-spirocyclization. Although 34 proved sufficiently stable for isolation and characterization, it displayed little stability in protic solvents (t 1/2 = 0.19 h at pH 3, t 1/2 = 0.20 h at pH 7), a pH-independent (H+ independent) solvolysis rate profile at pH 3/4−7, and a much reduced cytotoxic potency, but a DNA alkylation selectivity and efficiency comparable to those of duocarmycin SA and iso-duocarmycin SA. The implications of these observations on the source of the DNA alkylation selectivity and catalysis for this class of natural products are discussed.
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T cells absorb nanometric membrane vesicles, derived from antigen presenting cells, via dual receptor/ligand interactions of T cell receptor (TCR) with cognate peptide/major histocompatibility ...complex (MHC) complex plus lymphocyte function‐associated antigen 1 (LFA‐1) with intercellular adhesion molecule 1. Our studies have shown that TCR‐mediated signaling is also critically involved in the vesicle absorption, which is likely for the activation of LFA‐1. In an effort to systematically investigate the signaling process involved in the vesicle absorption process, we exploited chemical biology tools and screened chemical libraries to identify small molecules to interfere with the absorption process. Interestingly, it was found in the course of the study that brief treatments (1 hour) with various mitochondrial antagonists, including complex I, II, III, IV and V inhibitors,, resulted in ubiquitous inhibition of the vesicle absorption at concentrations not compromising viability of T cells. Further studies revealed that the mitochondrial drug treatments caused impairment of specific membrane‐proximal TCR signaling event(s). Thus, the activation of Akt and PLC‐γ1 and entry of extracellular Ca2+ following TCR triggering were severely compromised, while polymerization of monomeric actins immediately monitored upon triggering of TCRs appeared to progress normally even after the treatments. Dynamic F‐actin rearrangement concurring with the vesicle absorption was, however, also found to be impeded by the drug treatments, implying that the inhibition by the drug treatments of downstream signaling events at least in part resulted from the impairment of directional relocation of signaling and cell surface molecules accompanying with actin rearrangement.
Grant Funding Source: Supported by Chungnam National University Grant (2013‐1892)
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BFBNIB, FZAB, GIS, IJS, KILJ, NLZOH, NUK, OILJ, SBCE, SBMB, UL, UM, UPUK
Complementary to studies that provided the first yatakemycin total synthesis resulting in its structure revision and absolute stereochemistry assignment, a second-generation asymmetric total ...synthesis is disclosed herein. Since the individual yatakemycin subunits are identical to those of duocarmycin SA (alkylation subunit) or CC-1065 (central and right-hand subunits), the studies also provide an improvement in our earlier total synthesis of CC-1065 and, as detailed herein, have been extended to an asymmetric total synthesis of (+)-duocarmycin SA. Further extensions of the studies provided key yatakemycin partial structures and analogues for comparative assessments. This included the definition of the DNA selectivity (adenine central to a five-base-pair AT sequence, e.g., 5‘-AAAAA), efficiency, relative rate, and reversibility of ent-(−)-yatakemycin and its comparison with the natural enantiomer (identical selectivity and efficiency), structural characterization of the adenine N3 adduct confirming the nature of the DNA reaction, and comparisons of the cytotoxic activity of the natural product (L1210, IC50 = 5 pM) with those of its unnatural enantiomer (IC50 = 5 pM) and a series of key partial structures including those that probe the role of the C-terminus thiomethyl ester. The only distinguishing features between the enantiomers is that ent-(−)-yatakemycin alkylates DNA at a slower rate (k rel = 0.13) and is reversible, whereas (+)-yatakemycin is not. Nonetheless, even ent-(−)-yatakemycin alkylates DNA at a faster rate and with a greater thermodynamic stability than (+)-duocarmycin SA, illustrating the unique characteristics of such “sandwiched” agents.
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Lymphocyte function-associated antigen 1 (LFA-1), a member of beta2-integrin family, exerts multiple roles in host T cell immunity and has been identified as a useful drug-development target for ...inflammatory and autoimmune diseases. Applying the findings that primary resting T cells absorb nanometric membrane vesicles derived from antigen presenting cells (APC) via dual receptor/ligand interactions of T cell receptor (TCR) with cognate peptide-major histocompatibility complex (MHC) complex (pMHC) and LFA-1 with its ligand, intercellular adhesion molecule-1 (ICAM-1), and that signaling cascades triggered by TCR/pMHC interaction take a part in the vesicle-absorption, we established a cell-based high throughput assay for systematic investigation, via isolation of small molecules modulating the level of vesicle-absorption, of molecular mechanisms underlying the T cell absorption of APC-derived vesicles, i.e., structural basis of TCR/pMHC and LFA-1/ICAM-1 interactions and TCR-mediated LFA-1 activation. As primary T cells along with physiological ligands expressed in biological membrane are used and also individual cells in assay samples are analyzed by flow cytometry, results obtained using the assay system hold superior physiological and therapeutic relevance as well as statistical precision.
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DOBA, IZUM, KILJ, NUK, PILJ, PNG, SAZU, SIK, UILJ, UKNU, UL, UM, UPUK
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