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울금 추출물의 5-Alpha Reductase Ⅱ 활성 저해 효과
김종연(Jong Yeon Kim),이정윤(Jeong Yoon Lee),윤호근(Ho-Geun Yoon),김용재(Yungjae Kim),전우진(Woojin Jun),황권택(Kwon Tack Hwang),차민석(Min Seok Cha),이유현(Yoo-Hyun Lee) 한국식품영양과학회 2014 한국식품영양과학회지 Vol.43 No.2
본 연구에서는 울금(Curcuma longa L.)의 다양한 추출물을 대상으로 5-alpha reductase의 활성 저해 정도를 측정하였다. 5-Alpha reductase는 T에서 활성형 남성호르몬인 DHT로 전환을 담당하며, 전립선비대에서는 혈액에서 DHT농도가 높다. Rat의 전립선조직 균질액과 5-alpha reductase를 과발현시킨 LNCaP 세포 균질액을 대상으로 측정한 결과, 100 μg/mL의 농도에서 울금의 열수추출물(CL-HW)과 20% 에탄올추출물(CL-E20)이 5-alpha reductase 활성을 효과적으로 저해하였다. 특히 CL-HW는 100 μg/mL의 농도에서 80% 이상의 유의적 억제효과를 보였으며, CL-E20은 50 μg/mL의 농도부터 80% 이상의 감소효과를 보였다. 이 같은 결과에서 CL-HW 및 CL-E20은 5-alpha reductase의 억제활성이 있으며, 이는 전립선비대 치료소재로 개발될 수 있는 가능성이 있음을 제안한다. 5-Alpha reductase Ⅱ, which converts testosterone (T) to dihydrotestosterone (DHT), is a crucial enzyme Ⅱ in benign prostatic hyperplasia. Inhibitory effects of Curcuma longa L. (CL) extracts on 5-alpha reductase Ⅱ activity were investigated in rat prostate tissue homogenates as well as LNCaP cells expressing human 5-alpha reductase Ⅱ. Hot water extract (CL-HW) of Curcuma longa L. significantly inhibited 5-alpha reductase activity by over 80% at a concentration of 100 μg/mL, whereas 20% ethanol extracts (CL-E20) of Curcuma longa L. exhibited significant inhibitory activity from 50 μg/mL. These results indicated that Curcuma longa L is a potent 5-alpha reductase Ⅱ inhibitor for benign prostatic hyperplasia treatment.
The Crytal and Molecular Structure of Morpholinothiosemicarbazide
구정회,김훈섭,신현소,이영자,Chung Hoe Koo,Hoon Sup Kim,Hyun So Shin,Yungja Lee Korean Chemical Society 1973 대한화학회지 Vol.17 No.2
몰포리노치오세미카바자이드의 결정 구조가 X-선 해석에 의하여 결정되었다. 세포 상수는 a=4.19(2), b=6.56(2), c=26.67(4)$A^{\circ}$ 이고, 단위 세포는 4분자를 포함하며, 공간 군은 $P2_12_12_1$이다. 원자좌표치는 최소자승법으로 정밀화하였으며 R값은 651개의 관측 반사를 써서 계산한 결과 0.07이다. 아미노 질소 원자는 a-축에 평행한 2회의 나선 축에 의하여 옮겨지는 다른 분자의 황원자와 3.48 및 3.49$A^{\circ}$의 수소결합을 하고 있으며 아미노 질소 원자는 a-축에 평행한 2회의 나선 축에 의하여 옮겨지는 다른 분자의 아미노 질소 원자와 3.04${\AA}$의 수소결합을 하고 있다. 이들 3개의 수소결합은 분자들을 2회의 나선축 부근에 배열하게 한다. 수소결합 이외로 분자들을 연결하는 힘은 van der waals의 힘이다. The crystal structure of morpholinothiosemicarbazide has been determined by single crystal X-ray analysis. The lattice constants are a = 4.19(2), b = 6.56(2) and c = 26.67(4)${\AA}$. The unit cell contains 4 molecules and the space group is$P2_12_12_1$. The atomic parameters have been refined by least-squares method to a final R value of 0.07, based on the 651 observed reflexions. The amino nitrogen atom forms hydrogen bonds to the sulfur atoms of the other molecules related by the two-fold screw axis parallel to the a-axis, the distances of the hydrogen bonds being 3.48 and 3.49${\AA}$. On the other hand, the imino nitrogen atom forms a hydrogen bond to the amino nitrogen atom of the other molecule related by the two-fold screw axis parallel to the a-axis, the distance of the hydrogen bond being 3.04${\AA}$. These three hydrogen bonds arrange the molecules around the two-fold screw axis. Apart from the hydrogen bonding system the structure is held together by van der Waals forces.
Adaptive current tDCS up to 4 mA
Khadka, Niranjan,Borges, Helen,Paneri, Bhaskar,Kaufman, Trynia,Nassis, Electra,Zannou, Adantchede L.,Shin, Yungjae,Choi, Hyeongseob,Kim, Seonghoon,Lee, Kiwon,Bikson, Marom Elsevier 2020 Brain stimulation Vol.13 No.1
<P><B>Abstract</B></P> <P><B>Background</B></P> <P>Higher tDCS current may putatively enhance efficacy, with tolerability the perceived limiting factor.</P> <P><B>Objective</B></P> <P>We designed and validated electrodes and an adaptive controller to provide tDCS up to 4 mA, while managing tolerability. The adaptive 4 mA controller included incremental ramp up, impedance-based current limits, and a Relax-mode where current is transiently decreased. Relax-mode was automatically activated by self-report VAS-pain score >5 and in some conditions by a Relax-button available to participants.</P> <P><B>Methods</B></P> <P>In a parallel-group participant-blind design with 50 healthy subjects, we used specialized electrodes to administer 3 daily session of tDCS for 11 min, with a lexical decision task as a distractor, in 5 study conditions: adaptive 4 mA, adaptive 4 mA with Relax-button, adaptive 4 mA with historical-Relax-button, 2 mA, and sham. A tablet-based stimulator with a participant interface regularly queried VAS pain score and also limited current based on impedance and tolerability. An Abort-button provided in all conditions stopped stimulation. In the adaptive 4 mA with Relax-button and adaptive 4 mA with historical-Relax-button conditions, participants could trigger a Relax-mode ad libitum, in the latter case with incrementally longer current reductions. Primary outcome was the average current delivered during each session, VAS pain score, and adverse event questionnaires. Current delivered was analyzed either excluding or including dropouts who activated Abort (scored as 0 current).</P> <P><B>Results</B></P> <P>There were two dropouts each in the adaptive 4 mA and sham conditions. Resistance based current attenuation was rarely activated, with few automatic VAS pain score triggered relax-modes. In conditions with Relax-button option, there were significant activations often irrespective of VAS pain score. Including dropouts, current across conditions were significantly different from each other with maximum current delivered during adaptive 4 mA with Relax-button. Excluding dropouts, maximum current was delivered with adaptive 4 mA. VAS pain score and adverse events for the sham was only significantly lower than the adaptive 4 mA with Relax-button and adaptive 4 mA with historical-Relax-button. There was no difference in VAS pain score or adverse events between 2 mA and adaptive 4 mA.</P> <P><B>Conclusions</B></P> <P>Provided specific electrodes and controllers, adaptive 4 mA tDCS is tolerated and effectively blinded, with acceptability likely higher in a clinical population and absence of regular querying. Indeed, presenting participants with overt controls increases rumination on sensation.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Designed and validated an adaptive controller with electrode to maximize tDCS upto 4 mA while maintaining tolerability. </LI> <LI> Conditions with overt subject controls increase rumination on sensation, decreasing tolerability. </LI> <LI> No difference in VAS or adverse events among 2 mA, adaptive 4 mA, and sham. </LI> <LI> Adaptive 4 mA tDCS is relatively tolerated with specific electrodes and controller. </LI> </UL> </P>