• Bulletin of the Korean Chemical Society
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• v.25 no.9
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• pp.1331-1335
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• 2004

Angiogenesis is essential for the growth and persistence of solid tumors. Their metastases, anti-angiogenesis could lead to the suppression of tumor growth. One of the main strategies of cancer treatment is developing molecules of anti-angiogenic activity. In this study, two angiogenic inhibitors, Ang3 (KLFDF) and Ang4 (XLFDF) derived from KLYDY, which is the sequence of angiostatin active sites kringle 5, were designed and synthesized. Previously we reported the activities and structures of two inhibitors, Ang1 (KLYDY) and Ang2 (KLWDF). In order to investigate the effect of Phe substitution, Ang3 was designed with a sequence of KLFDF. In order to reduce conformational flexibility of side chain in Lys, Ang4 was designed with a sequence of XLFDF, where X has amino substituted phenyl ring. Solution structures of those inhibitors were investigated using NMR spectroscopy and their activities as angiogenesis inhibitors were studied. Ang1 and Ang2 show angiogenic activities, while Ang3 and Ang4 have no activities and have extended structures compared to Ang1 and Ang2. Therefore, Phe rings do not have effective hydrophobic interactions with other aromatic residues in Ang3 and Ang4. The representative structure of Ang2 has a stable intramolecular hydrogen bond. Therefore, intramolecular hydrogen bonding might be more important in stabilizing the structure than the hydrophobic interactions in these inhibitors. More rigid structure, which can be expected to have higher activities and better match with the receptor bound conformations, can be obtained with a constrained cyclic structure. Further peptidomimetic approaches should be tried to develop angiogenesis inhibitors.

• Economic and Environmental Geology
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• v.51 no.4
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• pp.345-358
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• 2018

In this study, we have performed electron probe micro analyzer (EPMA), X-ray differaction (XRD), inductively coupled plasma spectroscopy (ICP), Fourier transform Raman spectroscopy (FT-Raman), far-infrared (FIR), nuclear magnetic resonance (NMR), and pH-DO Analyses for characterizing medicinal mineralogy aspect of the black tourmaline (Shantung, china), black and pink tourmaline (Minas Geraris, Brazil), black touemaline (Daeyu mine, Korea). In addition, heating effects of the tourmaline sauna as well as the effects of tourmaline powder-added soap on skin troubles have been investigated. It has been revealed that chemical composition of the tourmaline is either high in Fe-, Al-, B-rich types. Ratio of the K-Ca, Na-K, and Fe-B reflects the component change property of solid solution. $CaO/CaO+Na_2O$ and MgO/FeO+MgO ratio show high positive correlation. When tourmaline reacts with distilled water, extended reaction time DO values approximately decrease and it stabilizes at DO = 10. Otherwise, pH values increase until 6 hours and it stabilizes at pH = 8 after 24 hours. Distilled water changes to alkaline when it reacts with tourmaline powder and particles. Tourmaline showed lower absorption spectrum strength and transmittance at short wave, where absorption spectrum wavelength and strength were determined by the content of the composition elements and characteristics of crystallography. Increase of the Fe content has been confirmed to be the cause for the reduction of irradiation. For the chemical composition and spectral property of the tourmaline particle samples, it has been found that Si and Fe contents show positive correlation with Far-Infrared irradiation, while Al and Mg contents show negative correlation. For tourmaline powder, it has been confirmed that $^{17}O-NMR$ FWHM (full width at half maximum) decreases when reacts with distilled water. Tourmaline sauna (approximately $100^{\circ}C$) was found to increase $0.5-1.5^{\circ}C$ of body temperature, average of 12 heartbeat, and 10mg Hg of blood pressure. Tourmaline soap had very good aesthetic effect to skin and was confirmed to have above the average improvements to skin troubles (e.g., allergy or atopy).