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Synthesis of Piperlongumine Derivatives Isolated from Piper longum L. and their Inhibitory Activity on Aflatoxin $B_1$ Production (Piperlongumine 유도체 합성과 $Aflatoxin\;B_1$ 생성 억제 효과)

  • Lee, Sung-Eun;Choi, Won-Sik;Lee, Hyun-Sang;Lee, Young-Haeng;Park, Byeoung-Soo
    • Applied Biological Chemistry
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    • v.46 no.4
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    • pp.361-366
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    • 2003
  • Anti-aflatoxigenic studies on synthetic pyridione alkaloids were conducted. Seven derivatives using piperlongumine as a leading compound were prepared from 3,4,5-trimethoxycinnamic acid (TMCA). These derivatives were analyzed for their structural confrmation and purity by HPLC, GC, GC/MS and $1^H-NMR$. 1-piperidin-1-yl-3-(3,4,5-trimethoxyphenyl)propenone (1) reaction with piperidine; 1-morpholin-4-yl-3-(3,4,5-trimethoypenyl)propenone (2) with morpholine; 1-(3,5-dimethylpiperidin-1-yl)-3-(3,4,5-trimethoxyphenyl)propenone (3) with 3,5-dimethylpiperdine; 1-(2-methylpiperidine-1-yl)-3-(3,4,5-trimethoxyphenyl)propenone (4) with 2-methylpiperidine; 1-(3-hydroxypiperidin-1-yl)-3- (3,4,5-trimethoxyphenyl)propenone (5) with 3-hydroxypiperidine hydrochloride; 1-[3- (3,4,5-trimethoxyphenyl)acryloyl]piperidin-2-one (6) with ${\delta}-valerolactam;\; and\;ethyl\;1-[3-(3,4,5-trimethoxyphenyl)acyloyl]piperidine-4-carboxylate$ (7) with ethyl isonipectotate were synthesized respectively. All derivatives showed an inhibitory activity on aflatoxin $B_1$ production. In conclusion, we believe that they might be an agent for the control of mycotoxin in agricultural commodities.

NecroX-5 protects mitochondrial oxidative phosphorylation capacity and preserves PGC1α expression levels during hypoxia/reoxygenation injury

  • Vu, Thi Thu;Kim, Hyoung Kyu;Le, Thanh Long;Nyamaa, Bayalagmaa;Song, In-Sung;To, Thanh Thuy;Nguyen, Quang Huy;Marquez, Jubert;Kim, Soon Ha;Kim, Nari;Ko, Kyung Soo;Rhee, Byoung Doo;Han, Jin
    • The Korean Journal of Physiology and Pharmacology
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    • v.20 no.2
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    • pp.201-211
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    • 2016
  • Although the antioxidant and cardioprotective effects of NecroX-5 on various in vitro and in vivo models have been demonstrated, the action of this compound on the mitochondrial oxidative phosphorylation system remains unclear. Here we verify the role of NecroX-5 in protecting mitochondrial oxidative phosphorylation capacity during hypoxia-reoxygenation (HR). Necrox-5 treatment ($10{\mu}M$) and non-treatment were employed on isolated rat hearts during hypoxia/reoxygenation treatment using an ex vivo Langendorff system. Proteomic analysis was performed using liquid chromatography-mass spectrometry (LC-MS) and non-labeling peptide count protein quantification. Real-time PCR, western blot, citrate synthases and mitochondrial complex activity assays were then performed to assess heart function. Treatment with NecroX-5 during hypoxia significantly preserved electron transport chain proteins involved in oxidative phosphorylation and metabolic functions. NecroX-5 also improved mitochondrial complex I, II, and V function. Additionally, markedly higher peroxisome proliferator-activated receptor-gamma coactivator-$1{\alpha}$ ($PGC1{\alpha}$) expression levels were observed in NecroX-5-treated rat hearts. These novel results provide convincing evidence for the role of NecroX-5 in protecting mitochondrial oxidative phosphorylation capacity and in preserving $PGC1{\alpha}$ during cardiac HR injuries.

CHANGES OF JAW-OPENING REFLEX DEGREE ACCORDING TO ELECTROACUPUNCTURE DURATION ON ZUSANLI (족삼리의 전기침 자극에 대한 개구반사 크기의 변화)

  • Seo, Young-Ah;Song, Hyung-Geun;Na, Chang-Su;Lee, Sang-Ho
    • Journal of the korean academy of Pediatric Dentistry
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    • v.25 no.4
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    • pp.788-796
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    • 1998
  • The purpose of this study was to investigate the effect of various electroacupuncture duration induced by acupuncture point-Zusanli ($S_{36}$) electrical stimulation on inhibition of amplitude of digastric electromyogram (dEMG) evoked by noxious electrical stimuli around the mental foramen. intraperitoneal sodium pentobarbital in an initial dose of 50mg/kg and maintenance doses of 4.5mg/kg/h were given through a cannula in the femoral vein using a constant infusion pump. A pair of stimulating electrodes were inserted for noxious stimuli around the mental foramen. An irritant electronic stimuli pulse (0.2 Hz, 0.1 ms duration) was produced with an intensity of about $1.5{\times}2$ times threshold for evoking the dEMG. The anterior belly of the digastric muscle was exposed and a pair of 0.1mm wire electrodes were inserted for dEMG recording. Acupuncture point stimulation on Zusanli (2 Hz, 250 ${\mu}s$, biphasic pulse, 2 V) was delivered by Dental Electronic Anesthesia (3M, U.S.A). For periods of electronic stimulation of 10, 20, and 30min, the amplitudes of dEMG were measured on the oscilloscope and on the monitor connected to the amplifier. The following results were obtained: The dEMG was decreased to 73.4% of that in the control set after 10 min electroacupunture stimulation (Group I); The dEMG was decreased to 77.1% (10min), 54.0.% (20min) of that in the control set after 20minutes of electroacupunture stimulation (Group II). The dEMG was decreased to 73.3% (10min), 61.9% (20min), 76.2% (30min) of that in the control set after 30 min of electroacupunture stimulation (Group III). From these results, it may be that in the electroacupuncture stimulation on the Zusnali resulted in a reduction of amplitude of dEMG and that the most effective electroacupuncture stimulation period was 20min.

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Development of Cryopreservation Protocols through Droplet-vitrification and its Application to Vegetatively Propagated Crop Germplasm (영양체 유전자원의 작은방울-유리화법에 의한 초저온동결보존 실용화기술개발)

  • Kim, Haeng-Hoon;Yi, Jung-Yoon;No, Na-Young;Cho, Gyu-Taek;Yoon, Mun-Sup;Baek, Hyung-Jin;Kim, Chung-Kon
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2010.05a
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    • pp.12-12
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    • 2010
  • We developed droplet-vitrification protocol, a combination of droplet-freezing and solution-based vitrification, and applied to germplasm collections of garlic, potato, lily as well as cell lines, including hairy roots, somatic embryos. To establish a garlic cryobank, four Korean garlic field collections at Danyang, Suwon, Mokpo and Namhae were cryopreserved last five years. The protocol applied consisted of preculture for 3-4 days at $10^{\circ}C$ on solid MS medium with 0.3M sucrose, loading for 40 min in liquid medium with 35% PVS3, dehydration with PVS3 for 150 min, cooling in $5{\mu}l$ droplets of PVS3 placed on aluminum foil strips by dipping these strips in liquid nitrogen, warming them by plunging the foil strips into pre-heated($40^{\circ}C$) 0.8M sucrose solution for 30s. A total of over 900 accessions of garlic were stored in liquid nitrogen for long-term conservation using unripe inflorescences, cloves or bulbils. Twelve alternative plant vitrification solutions were designed by modifying cryoprotectant concentrations from the original PVS2 and PVS3. The results suggest that PVS2-based vitrification solutions with increased glycerol and sucrose and/or decreased DMSO and EG concentrations can be applied for medium size explants which are tolerant to chemical toxicity and moderately sensitive to osmotic stress. PVS3 and variants can be used widely when samples are heterogeneous, of large size and/or very sensitive to chemical toxicity and tolerant to osmotic stress.

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Comparative physiological and proteomic analysis of leaf in response to cadmium stress in sorghum

  • Roy, Swapan Kumar;Cho, Seong-Woo;Kwon, Soo Jeong;Kamal, Abu Hena Mostafa;Kim, Sang-Woo;Lee, Moon-Soon;Chung, Keun-Yook;Woo, Sun-Hee
    • Proceedings of the Korean Society of Crop Science Conference
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    • 2017.06a
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    • pp.124-124
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    • 2017
  • Cadmium (Cd) is of particular concern because of its widespread occurrence and high toxicity and may cause serious morpho-physiological and molecular abnormalities in in plants. The present study was performed to explore Cd-induced morpho-physiological alterations and their potentiality associated mechanisms in Sorghum bicolor leaves at the protein level. Ten-day-old sorghum seedlings were exposed to different concentrations (0, 100, and $150{\mu}M$) of $CdCl_2$, and different morpho-physiological responses were recorded. The effects of Cd exposure on protein expression patterns in S. bicolor were investigated using two-dimensional gel electrophoresis (2-DE) in samples derived from the leaves of both control and Cd-treated seedlings. The observed morphological changes revealed that the plants treated with Cd displayed dramatically altered shoot lengths, fresh weights, and relative water content. In addition, the concentration of Cd was markedly increased by treatment with Cd, and the amount of Cd taken up by the shoots was significantly and directly correlated with the applied level of Cd. Using the 2-DE method, a total of 33 differentially expressed protein spots were analyzed using MALDI-TOF/TOF MS. Of these, treatment with Cd resulted in significant increases in 15 proteins and decreases in 18 proteins. Significant changes were absorbed in the levels of proteins known to be involved in carbohydrate metabolism, transcriptional regulation, translation and stress responses. Proteomic results revealed that Cd stress had an inhibitory effect on carbon fixation, ATP production and the regulation of protein synthesis. In addition, the up-regulation of glutathione S-transferase and cytochrome P450 may play a significant role in Cd-related toxicity and stress responses. Our study provides insights into the integrated molecular mechanisms involved in response to Cd and the effects of Cd on the growth and physiological characteristics of sorghum seedlings. The upregulation of these stress-related genes may be candidates for further research and use in genetic manipulation of sorghum tolerance to Cd stress.

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Effect of Germanium Treatment on Growth and Production of Organic Germanium in Oplopanax elatus (게르마늄 처리에 따른 땃두릅나무의 생육 증진 효과 및 유기게르마늄 생산)

  • Kim, Hee Young;Seong, Eun Soo;Yoo, Ji Hye;Choi, Jae Hoo;Kang, Byeong Ju;Jeon, Mi Ran;Kim, Myong Jo;Yu, Chang Yeon
    • Korean Journal of Medicinal Crop Science
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    • v.24 no.3
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    • pp.214-221
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    • 2016
  • Background: This study was conducted to investigate the effects of germanium treatment on the growth and organic germanium production in the roots of Oplopanax elatus plantlets. Methods and Results: O. elatus plantlets were cultured in Murashige and Skoog (MS) medium with different concentrations of germanium dioxide ($GeO_2$) to analyze optimum growth conditions. Exogenous treatment of $10mg/{\ell}\;GeO_2$ promoted growth and an increase in the contents of chlorophyll a, b and carotenoid in O. elatus. The germanium accumulation and production in roots of O. elatus plantlets treated with organic germanium reached the highest levels. The growth of the aerial and underground portion of O. elatus with organic germanium was greater than that of the control. The accumulation and production of organic germanium reached the highest level ($40.89{\mu}g/plantlet$) with the treatment of $50mg/{\ell}\;GeO_2$. Antioxidant activity measured by DPPH and ABTS assays also increased with the germanium treatment and improved the DPPH and ABTS radical activity by 200% compared with that in the control. In addition, the total phenol and flavonoid contents of the plantlets with a treatment of $50mg/{\ell}\;GeO_2$ were higher than in the control. Conclusions: Taken together, the growth of O. elatus was increased with the treatment of $50mg/{\ell}\;GeO_2$ germanium and the biological references improved, with increased antioxidant activity and organic germanium production.

Role of Posterior Intralaminar Thalamic Nuclei in Acupuncture Analgesia in Rats (침진통(鍼鎭痛) 작용에 있어서 시상 후방 층판내핵(속방핵)의 역할)

  • Roh, Sik;Min, Byung-Il;Yoon, Sang-Hyub
    • The Journal of Korean Medicine
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    • v.20 no.3 s.39
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    • pp.36-44
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    • 1999
  • Objectives: It has been well known that electroacupuncture(EA) has an analgesic effect and there is a pain control system in the central nervous system(CNS). The pain control system is composed of three major nuclei, which are periaqueductal gray(PAG), raphe nuclei, and the pain inhibitory complex located in the spinal cord. It has been suggested that the analgesic effect of EA might be the result of activation of the pain control system in the CNS. However, there may be a possibility that other nuclei are also involved in this pain modulation. Thus, we investigated whether the posterior intralaminar thalamic nuclei (PTIN) are involved in the pain modulation. Methods: To measure the level of pain, the jaw opening reflex (JOR) was used as a pain index. The magnitude of JOR is estimated by averaging the area of 10 successive responses. JOR was evoked by tooth-pulp stimulation with bipolar electrode carrying stimulus with the following parameters: intensity ranging from 420uA to 680ulA, 0.3ms duration of square pulse, and 0.5 Hz. Hapkog($LI_4$) and Taechung ($LR_3$) were the chosen acupoints. The Hapkog point was stimulated ipsilaterally at 5V, 3 Hz, for 15min in total, and the Taechung was stimulated at 2-3 V, 3 Hz, and for a total of 15 or 30 minutes. Different intensities of stimulation were given the PITN; one was given at $300{\mu}A$ and the other was at 500uA. The position stimulated in these nuclei by Paxinos Atlas was AP; from bregma $-4.0{\sim}-4.3mm,\;L; 0.5{\sim}1.8mm,\;D;\;4.8{\sim}6.3mm$. Results: The Hapkog point had a significant analgesic effect (P<0.05). However, the Taechung point had no effect. Both types of stimulation in the PITN did not reveal any analgesic effects. Conclusions: From these results, it was suggested that the posterior intralaminar thalamic nuclei are not involved in the modulation of pain.

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Purification and Structure of Antioxidative Substance Derived from Tetraselmis suecica (Tetraselmis suecica유래의 항산화성 물질의 정제 및 구조)

  • Kim Se Kwon;Byun Hee Guk;Park Pyo Jam;Adachi Kyoko
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.35 no.2
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    • pp.155-161
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    • 2002
  • Tetraselmis suecica (T. suecica) of Prasinophyta was selected because the growth rate is comparatively higher and the culturing is also easy. In order to investigate antioxidative activity, the soluble elements of T. suecica were fractionated using water and organic solvents such as methanol, hexane, chloroform, ethylacetate and butanol. The chloroform fraction of T. suecica showed strong antioxidative activity. The potential antioxidative activity was detected in hexane: ethylacetate (1:5) once used the fractions by different mixtures of organic solvents. This fraction was further purified by preparative thin layer chromatography (PTLC) and repeated reverse-phase HPLC. On the basis of chemical and spectroscopic evidences obtained by UV, FT-IR, FAB-MS and NMR, the compound purified from T. suecica was identified as pheophorbide-a. The antioxidative activity of the compound was comparable to that of $\alpha$-tocopherol and could be act as an antioxidant in foods.

Modified Atmosphere Packaging of Shiitake Mushroom Packed with Perforated Film and Ceramic Films (기공필름과 광물질 연입 필름 포장한 표고버섯의 MAP효과)

  • 정문철;남궁배;이호준;임정호
    • Food Science and Preservation
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    • v.8 no.1
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    • pp.47-53
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    • 2001
  • In order to investigate the effect of two type of ceramic film(15% SiO$_2$ incorporated LDPE, 10% zeolite incorporated LDPE), perforated film and LDPE film on freshness of shiitake mushroom, weight loss, surface color and marketability of mushroom were measured during MA storage at 5 $\^{C}$ and 20$\^{C}$. The effect of packaging films on weight loss and marketability index of shiitake mushroom at 20$\^{C}$ was negligible due to its rapid physiological changes. However, the effect of packaging films on surface color of shiitake mushroom was significant at 20$\^{C}$ storage, but not at 5$\^{C}$ storage. During MA storage of shiitake mushroon, discoloration were reduced effectively by ceramic films and weight loss were by LDPE film, but they had little difference between packaging 51ms. However, there were significant differences among the packaging films in marketability of mushroom induced by water vapor inside package and accelerate its spoilage and browning. Ceramic film(15% SiO$_2$ incorporated LDPE) showed best result to maintain marketability of shiitake mushroom and zeolite incorporated film, perforated film, LDPE film in order.

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Alterations of Cerebral Metabolic Activation Following Electro-Acupuncture Stimulation on ST36 and LR3 Acu-Points in Rats (흰쥐의 족삼리 및 태충 전침자극에 따른 뇌대사활성의 변화)

  • Sohn, Young-Joo;Jung, Hyuk-Sang;Ku, Ja-Seung;Won, Ran;Kim, Yong-Suk;Park, Young-Bae;Sohn, Nak-Won
    • Journal of Acupuncture Research
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    • v.19 no.1
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    • pp.159-174
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    • 2002
  • Objective : The meridian theory in oriental medicine explains that each acu-point has a characteristic functional effect. It will be supposed that an acupuncture stimulation on different acu-point evokes different activation on different areas in the central nervous system(CNS) according to the meridian theory. On this supposition, our group tried the semi-quantitative [14C]2-deoxyglucose([14C]2-DG) autoradiography on the acupuncture stimulation to the hindlimb acu-points of Sprague-Dawley rats. Methods : A venous catheter for the intravenous administration of isotope was equipped in the right external jugular vein on 3 days prior to the [14C]2-DG study. On the day of the study, two acupuncture needles were inserted into the ST36(Zusanli) or LR3(Taichong) on the left hindlimb. Electro-acupuncture stimulation (2 Hz, 5 ms, 1~3 mA, 15 minutes) started just before the i.v. injection of [14C]2-DG ($25{\mu}Ci/rat$). The brain and the spinal cord were removed and processed for the [14C] 2-DG autoradiography. Results : The EA stimulation on ST36 reveals over 120% metaboilc activation in Arcuate nucleus, Anterior pretectal nucleus, Dorsal cochlear nucleus, Interposed cerebellar nucleus, and Nucleus of Darkschewitsch. The EA stimulation on LR3 reveals over 120% metaboilc activation in Lateral habenula nucleus, Medial vestibular nucleus, Ventromedial thalamic nucleus, Anteroventral thalamic nucleus, Anterior cingulate cortex, Dentate gyrus, Antero cortical amygdaloid nucleus, Anterior pretectal nucleus, and Dorsal tegmental nucleus compared with the non EA stimulation control group. Conclusion : These results demonstrate that the different acu-points evoke the different activations in brain areas. And with this functional brain mapping study, a new scientific elucidation for the basis of the acupuncture-meridian theory in oriental medicine through differences of activated area in CNS according to the each acupuncture point.

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