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Robert Weis,Heinrich Berger,Marcel Kaiser,Reto Brun,Robert Saf,Werner Seebacher 대한약학회 2008 Archives of Pharmacal Research Vol.31 No.6
New alkenes, aziridines, and diamines were prepared from antiprotozoal 4-dialkylaminobicyclo[ 2.2.2]octan-2-imines to investigate the influence of several functional groups in position 2 of the ring skeleton on the antitrypanosomal and antiplasmodial activities. They were synthesized from 4-dialkylaminobicyclo[2.2.2]octan-2-imines and tested for their activities against Trypanosoma b. rhodesiense and Plasmodium falciparum K1 (resistant to chloroquine and pyrimethamine) using in vitro microplate assays. 4-Aminobicyclo[2.2.2]oct-2-enes and 3-azatricyclo[ 3.2.2.02,4]nonylamines exhibit similar antiprotozoal activities as 4-aminobicyclo[2.2.2] octanes. 4-Aminobicyclo[2.2.2]oct-2-ylamines and their N-benzyl derivatives showed decreased antiplasmodial but enhanced antitrypanosomal (IC50 = 0.22-0.41 μM) activities compared to their parent oximes and to formerly synthesized 4-amino-2-azabicyclo[3.2.2]nonanes. Some of the 4-aminobicyclo[2.2.2]oct-2-ylamines exhibit moderate in vivo activity in mice against Trypanosoma brucei brucei.
The use of JIP test to evaluate drought-tolerance of transgenic rice overexpressing OsNAC10
Redillas, Mark C.F.R.,Strasser, Reto J.,Jeong, Jin-Seo,Kim, Youn-Shic,Kim, Ju-Kon The Korean Society of Plant Biotechnology 2011 Plant biotechnology reports Vol.5 No.2
In this study, the JIP test was exploited to assess drought-tolerance of transgenic rice overexpressing OsNAC10. Two types of promoters, RCc3 (root-specific) and GOS2 (constitutive), were used to drive the transcription factor OsNAC10, a gene involved in diverse functions including stress responses. Three-month-old plants were exposed to drought for 1 week and their fluorescence kinetics was evaluated. Our results showed that drought-treated non-transgenic plants (NT) have higher fluorescence intensity at the J phase (2 ms) compared to transgenic plants, indicating a decline in electron transport beyond the reduced plastoquinone ($Q_A^-$). As manifested by negative L bands, transgenic plants also showed higher energetic connectivity and stability over NT plants under drought conditions. Also, the pool size of the end electron acceptor at the photosystem I was reduced more in NT than in transgenic plants under drought conditions. Furthermore, the transgenic plants had higher $PI_{total}$, a combined parameter that reflects all the driving forces considered in JIP test, than NT plants under drought conditions. In particular, the $PI_{total}$ of the RCc3:OsNAC10 plants was higher than that of NT plants, which was in good agreement with their differences in grain yield. Thus, the JIP test proved to be practical for evaluating drought-tolerance of transgenic plants.
Bratzdrum, Christian,Grapes, Rodney,Gieré,, Reto Elsevier 2009 Lithos Vol.113 No.3
<P><B>Abstract</B></P> <P>Three generations of calc–alkaline lamprophyre, occurring as patches or segregations in granite and as dyke swarms with a NNW–SSE trend, are associated with the Late Jurassic Shanqi–Xiaqi granite, SE China. They comprise coarse-grained, hornblende-dominated spessartite and two types of panidiomorphic kersantite: type-1 contains clinopyroxene and biotite phenocrysts, whereas type-2 is fine-grained and plagioclase-rich. The granite is characterised by large feldspar crystals and Al-rich annite. This rare occurrence of outcrops with no influence from atmospheric weathering allows the investigation of extensive alteration from hydrothermal interaction between lamprophyres and granite. At a depth of ca. 18 km, the breakdown of annite in the granite to magnetite+K-feldspar was the result of reheating above 670 °C at oxygen activities >10<SUP>−17</SUP> bar. In the lamprophyres, a variety of reactions due to autometasomatism include: breakdown of Ti-rich pargasites to chlorite, epidote, titanite; olivine to talc, tremolite, saponite, beidellite and Fe–Cr spinels; biotite to chlorite and titanite; calcic plagioclase to orthoclase, albite, epidote, chlorite and beidellite. Late-stage magmatic hydrothermal fluids from granite and lamprophyres resulted in redistribution of F, Ba, Sr, and CO<SUB>2</SUB> with the formation of calcite–fluorite veins. Amphibole-rich spessartite and biotite–diopside dominated kersantite exhibit heteromorphism in that they have similar geochemical characteristics but different mineralogies. The alkali-rich lamprophyric magmas are inferred to have been derived from melting in the mantle wedge during the subduction of the Kula Plate, and show typical backarc rift chemistry. Prior to intrusion of lamprophyre, underplating of large volumes of basaltic magma is thought to have enhanced partial melting in the overlying continental crust resulting in widespread granite magmatism in SE China.</P>
Carlo M. Oranges,Mathias Tremp,Barbara Ling,Reto Wettstein,René D. Largo,Dirk J. Schaefer 대한성형외과학회 2016 Archives of Plastic Surgery Vol.43 No.5
External volume expansion of the recipient site by suction has been proposed as a way of improving fat graft survival. The objective of this study was to present an innovative and simple intraoperative external expansion system to enhance small-volume autologous fat grafting (40–80 mL) and to discuss its background and its mechanism of action. In this system, expansion is performed using a complete vacuum delivery system known as the Kiwi VAC- 6000M with a PalmPump (Clinical Innovations). The recipient site is rapidly expanded intraoperatively 10 times for 30 seconds each with a negative pressure of up to 550 mm Hg before autologous fat injection. During this repetitive stimulation, the tissues become grossly expanded, developing macroscopic swelling that regresses slowly over the course of hours following the cessation of the stimulus. The system sets various mechanisms in motion, including scar release, mechanical stimulation, edema, ischemia, and inflammation, which provide an environment conducive for cell proliferation and angiogenesis. In order to maintain the graft construct in its expansive state, all patients are encouraged postoperatively to use the Kiwi three times daily for one minute per session over the course of three days. The handling of this system is simple for both the patients and the surgeon. Satisfactory clinical outcomes have been achieved without significant complications.
Weis, Robert,Berger, Heinrich,Kaiser, Marcel,Brun, Reto,Saf, Robert,Seebacher, Werner 대한약학회 2008 Archives of Pharmacal Research Vol.31 No.6
New alkenes, aziridines, and diamines were prepared from antiprotozoal 4-dialkylaminobicyclo[2.2.2]octan-2-imines to investigate the influence of several functional groups in position 2 of the ring skeleton on the antitrypanosomal and antiplasmodial activities. They were synthesized from 4-dialkylaminobicyclo[2.2.2]octan-2-imines and tested for their activities against Trypanosoma b. rhodesiense and Plasmodium falciparum $K_1$ (resistant to chloroquine and pyrimethamine) using in vitro microplate assays. 4-Aminobicyclo[2.2.2]oct-2-enes and 3-azatricyclo[$3.2.2.0^{2,4}$]nonylamines exhibit similar antiprotozoal activities as 4-aminobicyclo[2.2.2] octanes. 4-Aminobicyclo[2.2.2]oct-2-ylamines and their N-benzyl derivatives showed decreased antiplasmodial but enhanced antitrypanosomal ($IC_{50}\;=\;0.22-0.41\;{\mu}M$) activities compared to their parent oximes and to formerly synthesized 4-amino-2-azabicyclo[3.2.2]nonanes. Some of the 4-aminobicyclo[2.2.2]oct-2-ylamines exhibit moderate in vivo activity in mice against Trypanosoma brucei brucei.
Kataru, Raghu P.,Jung, Keehoon,Jang, Cholsoon,Yang, Hanseul,Schwendener, Reto A.,Baik, Jung Eun,Han, Seung Hyun,Alitalo, Kari,Koh, Gou Young American Society of Hematology 2009 Blood Vol.113 No.22
<P>Using a bacterial pathogen-induced acute inflammation model in the skin, we defined the roles of local lymphatic vessels and draining lymph nodes (DLNs) in antigen clearance and inflammation resolution. At the peak day of inflammation, robust expansion of lymphatic vessels and profound infiltration of CD11b+/Gr-1+ macrophages into the inflamed skin and DLN were observed. Moreover, lymph flow and inflammatory cell migration from the inflamed skin to DLNs were enhanced. Concomitantly, the expression of lymphangiogenic growth factors such as vascular endothelial growth factor C (VEGF-C), VEGF-D, and VEGF-A were significantly up-regulated in the inflamed skin, DLNs, and particularly in enriched CD11b+ macrophages from the DLNs. Depletion of macrophages, or blockade of VEGF-C/D or VEGF-A, largely attenuated these phenomena, and produced notably delayed antigen clearance and inflammation resolution. Conversely, keratin 14 (K14)-VEGF-C transgenic mice, which have dense and enlarged lymphatic vessels in the skin dermis, exhibited accelerated migration of inflammatory cells from the inflamed skin to the DLNs and faster antigen clearance and inflammation resolution. Taken together, these results indicate that VEGF-C, -D, and -A derived from the CD11b+/Gr-1+ macrophages and local inflamed tissues play a critical role in promoting antigen clearance and inflammation resolution.</P>
Synthesis and antiprotozoal activities of new 3-azabicyclo[3.2.2]nonanes
Sarfraz Ahmad,Werner Seebacher,Volker Wolkinger,Armin Presser,Johanna Faist,Marcel Kaiser,Reto Brun,Robert Saf,Robert Weis 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.8
Some antimalarial agents in use typically bear basic side chains as ligands. Such ligands were attached to the amino substituent of a bridgehead atom of already antiprotozoal active 3-azabicyclo[3.2.2]nonanes. Structure verification was done by NMR measurements. The new compounds were tested for their antiplasmodial and antitrypanosomal activities against Plasmodium falciparum K1 (multiresistant) and Trypanosoma brucei rhodesiense as well as for their cytotoxicity against L6 cells. Theiractivities are compared to those of already prepared compounds and structure–activity relationships are discussed.
The antiprotozoal potencies of newly prepared 3-azabicyclo[3.2.2]nonanes
Sarfraz Ahmad,Werner Seebacher,Johanna Faist,Marcel Kaiser,Reto Brun,Robert Saf,Robert Weis 대한약학회 2016 Archives of Pharmacal Research Vol.39 No.10
3-Azabicyclo[3.2.2]nonanes are already reported as antiprotozoal agents. Structural variations were performed by attachment of several basic side chains, being part of drugs in use, to the ring nitrogen. The structures of the new compounds were established using one and two dimensional NMR measurements. All compounds were investigated for their antiplasmodial and antitrypanosomal activities against Plasmodium falciparum K1 (multiresistant) and Trypanosoma brucei rhodesiense. Their cytotoxicity was assessed against L6 cells. The results are compared to the activities of formerly synthesized compounds. Structure–activity relationships are discussed