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A multifunctional scatterometer system and optimized radar signal processing for simultaneous observation of various physical oceanographic parameters are described in this paper. Existing observation methods with microwave remote sensing techniques generally use several separate systems such as scatterometer, altimeter, and Doppler radar for sea surface monitoring, which are inefficient in system operation and cross-analysis of each observation data. To improve this point, we integrated separate measurement functions into a single observation system by adding a measurement function of Doppler frequency to the existing system. So it enables to simultaneously measure the range and polarimetric responses of backscattering as well as movements of the sea surface. Here, the simultaneous measurement function of Doppler frequency was implemented by sampling an FMCW (frequency modulated continuous wave) radar signal as 2D raw data consisting of fast- and slow-time samples, i.e., the range and backscattering of radar target signals are analyzed from the fast-time samples while the Doppler frequency by the radar target’s movement extracts from the slow-time samples. Through the Fourier transformed-based range-Doppler signal process, distance (R), backscattering (σ°), and Doppler frequency (fD) are sequentially extracted from the 2D raw data, and a correlation to the physical oceanographic parameters is analyzed. Operability of the proposed system was examed through total 3 times of field campaigns from June 2017 to August 2020 and the observation data retrieved by the radar measurement data (R, σ°, fD) was also cross-analyzed with in-situ data: e.g., tide, significant wave height, and wind speed and direction. Differences in the comparative results as an observational accuracy are as follows. Tidal level (Root Mean Square Error 0.169 m (R)), significant wave height (RMSE 0.127 m (R), 0.362 m (σ°)), wind speed (RMSE 1.880 m/s (fD), 2.094 m/s (σ°)) and direction (18.84° (fD)).

This manuscript presents a self-interferometric phase analysis technique for sea surface observation using a single scatterometer system. The self-interferometric phase is proposed to complement the imprecise analysis results due to the very meager signal strength measured at a high incident angle of more than 30°, which is a vulnerability of the existing analysis method using the Doppler frequency based on the backscattered signal strength. Moreover, compared to conventional interferometry, it is characterized by the phase-based analysis using consecutive signals from a single scatterometer system without any auxiliary system or channel. To apply the interferometric signal process on the moving sea surface observation, it is necessary to secure a reference target; however, this is hard to solve in practice. Hence, we adopted the back-projection algorithm to project the radar signals onto a fixed reference position above the sea surface, where the theoretical model for extracting the self-interferometric phase was derived from the radar-received signal model applying the back-projection algorithm. The observation performance of the proposed method was verified using the raw data collected at the Ieodo Ocean Research Station in Republic of Korea. In the observation result for wind velocity at the high incident angles of 40° and 50°, the self-interferometric phase analysis technique shows a better performance of a correlation coefficient of more than about 0.779 and an RMSE (root-mean-square error) of about 1.69 m/s compared to the existing method of a correlation coefficient of less than 0.62 and RMSE of more than 2.46 m/s.

A sea surface imaging technique for an emergency response using a ready-made frequency modulated continuous wave&ndash, synthetic aperture radar (FMCW SAR) system and its experimental results are described in this paper. The optimal range of radiowave incidence angle for sea surface imaging was analyzed by a theoretical scattering model and measurement data, and it was properly applied to the FMCW SAR system by readjusting the delayed-dechirp process. Raw data acquired through flight experiments were reconstructed to SAR image by the range-doppler algorithm. To verify the performance of the reconstructed sea surface image, dual-channel images collected by the configuration of the along-track interferometry were used, and then performance indicators such as signal attenuation, coherence, and phase difference were analyzed. Through this experimental study, it was confirmed that the ready-made FMCW SAR system without a function of the incident angle control can also conduct limited missions for maritime observation. It is possible to be an alternative resource for emergency response, in which the cases are requiring urgent maritime disaster detection and analysis.

Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is an enzyme that catalyzes hydrolysis of 3'-phosphotyrosyl bonds and is involved in repair of irreversible topoisomerase I (Top1)-DNA covalent complexes. Tdp1 inhibitors are regarded as potential cancer therapeutics in combination with Top1 inhibitors, which are currently used to treat human cancers. While screening for Tdp1 inhibitors, we discovered a novel compound, JBIR-21 (1), from the culture of an anamorphic fungus, RF-13305. The structure of 1 was established by extensive NMR and MS analyses. Compound 1 showed inhibitory activity against Tdp1 (IC(50) value, 18 μM) and cytotoxic activity against cancer cell lines (IC(50) values, 3.5-13 μM). Compound 1 also exhibited antitumor activity in a mouse xenograft model without adverse effects.

Postmortem examinations of tissues of humans and rodents with a host of neurodegenerative conditions, including Alzheimer's and Parkinson's diseases, have identified oxidative damage in proteins, lipids, and DNA. The aim of this study was to better understand the cellular mechanisms of neuronal cell degeneration induced via oxidative stress and the protective roles of bioactive substance. In order to achieve this aim, we established a screening program to discover therapeutic agents that exhibit preferential neuroprotective activity in H(2)O(2)-treated PC12 cells. During the course of our screening program, we isolated an active compound, SG-168, from Dendrobium nobile Lindley and identified it as a neuroprotective agent. SG-168 was identified as a compound with an acetal skeleton, a prototypical compound, by electrospray ionization-mass spectrometry analysis and various nuclear magnetic resonance spectroscopic methods. The protective effect of SG-168 in PC12 cells with H(2)O(2)-induced oxidative damage was investigated by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide reduction assay. As expected, incubation with H(2)O(2) for 2 hours resulted in cell viability of 31.8% compared to the control, while pretreatment of SG-168 increased cell viability by 15-50% compared to the H(2)O(2)-stressed control cells. These results showed that SG-168 inhibits H(2)O(2)-induced apoptotic cell death. Interestingly, flow cytometric analysis showed that H(2)O(2)-treated PC12 cells incubated with SG-168 exhibited greatly suppressed apoptosis. In summation, the results of this study suggest that SG-168 has potential as a new antioxidant agent against neuronal diseases.

Teicoplanin, a glycopeptide antibiotic, is composed of five main components, denoted T-A2-1 to T-A2-5. We investigated the use of glycerol as a carbon source affecting the teicoplanin components and its acyl moieties. As a result, we show the change of teicoplanin components, as well as an increase of total teicoplanin yields, caused by the addition of glycerol to the production medium. Analysis of the total cell lipids upon the addition of glycerol also showed a corresponding change in the proportion of teicoplanin, suggesting that glycerol strongly affects a change of teicoplanin branched acyl moieties.

Using β-glucosidase to hydrolyze glycosides into aglycones, the present study attempted to improve the bio-activity of the extract from mulberry leaves. When varying the ethanol fraction, pH, and temperature of the extract, the optimum conditions for the enzyme reaction were identified as a 10% ethanol fraction in the extract, pH 5.0, and 40 °C temperature. Under these optimum conditions, the enzyme reaction produced a remarkable increase in the anti-oxidation and tyrosinase inhibition activities of the extract by as much as 219.5% and 230.9%, respectively. This improved bio-activity of the extract was due to the hydrolysis of the glycoside polyphenols rutin, isoquercitrin, and astragalin into the aglycone polyphenols quercetin and kaempferol. Furthermore, the enzymatic hydrolysis of the extract by β-glucosidase also produced some additional benefits that are critical factors for the skin absorption of bio-active ingredients, including an improved hydrophobicity (239.41%) and reduced mean molecular weight (from 387.3 to 291.4), resulting in a significantly enhanced skin permeability (513%).

Glucose deprivation is a fundamental feature of poorly vascularized solid tumors and leads to activation of the molecular chaperone GRP78, which is associated with the unfolded protein response (UPR), a stress-signaling pathway, in tumor cells. We recently isolated an active compound, M126, that inhibits transcription from a GRP78 promoter reporter construct. M126 was identified as valinomycin by various spectroscopic methods. We found that valinomycin prevents UPR-induced protein expression, such as GRP78 and GRP94. The GRPs-inhibitory action of valinomycin severe hypoglycemic and results in selective cell death of the stressed cancer cells. Our findings demonstrate that GRP78 may be an excellent target for the use of cancer chemotherapy in the treatment of solid tumors.

Summary Transplantation of preserved amniotic membrane has been known to be effective in clinical treatment of severely damaged ocular surfaces. Amniotic membrane showed inhibitory effects on serine proteinase such as proteinase of A. castellanii , trypsin, and plasmin and metallo- proteinase, collagenase. However, elastase and proteinases of P. aeruginosa, S. aureus , and A. fumigatus were not inhibited by amniotic membrane. In Western blot analysis, at least five proteinase inhibitors including α1-antitrypsin, α1-antichymotrypsin, inter-α1-trypsin inhibitor, α2-macroglobulin and α2-antiplasmin, were detected in amniotic membrane. These suggest that the therapeutic effect of amniotic membrane, at least in part, may be due to the roles of proteinase inhibitors in the amniotic membrane. These inhibitors may contribute the therapeutic effects of amniotic membrane by inhibiting proteinases which can cause persistent corneal destruction by proteolytic degradation of cornea.

In the course of our chemical screening program for new secondary metabolites, we isolated a new compound JBIR-66 (1) from the culture broth of the tunicate-derived actinomycete, Saccharopolyspora sp. SS081219JE-28. The structure of 1 was determined to be (3Z,6E,8E)-N-(4-acetamido-3-hydroxybutyl)-2-hydroxy-4,8-dimethylundeca-3,6,8-trienamide on the basis of extensive NMR and MS spectroscopic data.

Cancer cells in poorly vascularized solid tumors are constantly or intermittently exposed to stressful microenvironments, including glucose deprivation, hypoxia, and other forms of nutrient starvation. These tumor-specific conditions, especially glucose deprivation, activate a signaling pathway called the unfolded protein response (UPR), which enhances cell survival by induction of the stress proteins. We have established a screening method to discover anticancer agents that could preferentially inhibit tumor cell viability under glucose-deprived conditions. Here we identify arctigenin (ARC-G) as an active compound that shows selective cytotoxicity and inhibits the UPR during glucose deprivation. Indeed, ARC-G blocked expression of UPR target genes such as phosphorylated-PERK, ATF4, CHOP, and GRP78, which was accompanied by enhanced phosphorylation of eIF2α during glucose deprivation. The UPR inhibition led to apoptosis involving a mitochondrial pathway by activation of caspase-9 and -3. Furthermore, ARC-G suppressed tumor growth of colon cancer HT-29 xenografts. Our results demonstrate that ARC-G can be served as a novel type of antitumor agent targeting the UPR in glucose-deprived solid tumors. J. Cell. Physiol. 224:33–40, 2010 © 2010 Wiley-Liss, Inc.

The Journal of Antibiotics (2009) 62, 283–285; doi:10.1038/ja.2009.22; published online 20 March 2009Keywords: histone deacetylase; histone deacetylase inhibitor; Streptomyces; trichostatinHistone deacetylases (HDACs) play an important role in the epige-netic regulation of gene expression by catalyzing the removal of acetylgroups from lysine residue of histone protein, stimulating chromatincondensation and promoting transcriptional repression.

The screening for active compounds against malignant pleural mesothelioma (MPM) cells produced by Streptomyces sp. AK-AB27 resulted in the isolation of two compounds with a dodecahydrodibenzo[b,d]furan skeleton named JBIR-23 (1) and -24 (2). Their structures were established on the basis of extensive NMR and MS analyses. Compounds 1 and 2 exhibited cytotoxic effects against several MPM cell lines.

Colorectal cancer is the third most common cause of cancer-related deaths in the world. Surgical intervention followed by chemotherapy remains the primary approach to treatment since colon cancers remain refractory to most chemotherapeutic agents. Based on that, we established a program to screen natural products for cytotoxic activity, employing the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reduction assay system utilizing HT-29 human colon cancer cells. During the course of our screening, we found that the methanolic extract of silkworm droppings (SDME) has cytotoxic effects on HT-29 cells. In the present study, we investigated the possible mechanisms by which SDME exerts its antiproliferative activity in HT-29 cells. As expected, SDME inhibited growth of HT-29 cells in a dose-dependent manner as assessed by the MTT reduction assay, the lactate dehydrogenase release assay, and the colony formation assay. We also investigated whether the apoptotic effects induced by SDME involve the caspase pathway using the caspase colorimetric assay. Interestingly, caspase-9 and -3, but not caspase-8, were activated in response to SDME treatment. Taken together, these results clearly indicate that the induction of apoptosis by SDME involves a mitochondrial-mediated pathway and strongly suggest that SDME may potentially be a chemotherapeutic agent for human colon cancer.

Cell surface adhesion molecules are thought to play an important role in establishing intercellular contacts that are necessary for immunological reactions. Intercellular adhesion molecule-1 (ICAM-1, CD54) is a crucial adhesion molecule in mediating cell to cell adhesion during inflammatory responses, including non-MHC-restricted cytotoxicity. In this study, the sICAM-1 levels of ten healthy control subjects and seven generalized active vitiligo patients were measured by ELISA. The sICAM-1 levels were also correlated with the clinical courses in 33 patients with active vitiligo, who received systemic steroid treatment for 3 months. The average serum level of sICAM-1 was significantly higher in patients with active vitiligo than in the healthy control subjects. The sICAM-1 levels significantly decreased after systemic steroid treatment in the clinically improved group. These results suggest that immune activation is involved in active vitiligo and that changes of sICAM-1 levels can be a marker in the course of vitiliginous lesions.