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Pena, Ike Dela,Yoon, Seo Young,Kim, Hee Jin,Park, Sejin,Hong, Eun Young,Ryu, Jong Hoon,Park, Il Ho,Cheong, Jae Hoon The Korean Society of Ginseng 2014 Journal of Ginseng Research Vol.38 No.1
Background: Although ginsenosides such as Rg1, Rb1 and Rg3 have shown promise as potential nutraceuticals for cognitive impairment, their use has been limited due to high production cost and low potency. In particular, the process of extracting pure Rg3 from ginseng is laborious and expensive. Methods: We described the methods in preparing ginseol k-g3, an Rg3-enriched fraction, and evaluated its effects on scopolamine-induced memory impairment in mice. Results: Ginseol k-g3 (25-200 mg/kg) significantly reversed scopolamine-induced cognitive impairment in the passive avoidance, but not in Y-maze testing. Ginseol k-g3 (50 and 200 mg/kg) improved escape latency in training trials and increased swimming times within the target zone of the Morris water maze. The effect of ginseol k-g3 on the water maze task was more potent than that of Rg3 or Red ginseng. Acute or subchronic (6 d) treatment of ginseol k-g3 did not alter normal locomotor activity of mice in an open field. Ginseol k-g3 did not inhibit acetylcholinesterase activity, unlike donezepil, an acetylcholinesterase inhibitor. Rg3 enrichment through the ginseol k-g3 fraction enhanced the efficacy of Rg3 in scopolamine-induced memory impairment in mice as demonstrated in the Morris water maze task. Conclusion: The effects of ginseol k-g3 in ameliorating scopolamine-induced memory impairment in the passive avoidance and Morris water maze tests indicate its specific influence on reference or long-term memory. The mechanism underlying the reversal of scopolamine-induced amnesia by ginseol k-g3 is not yet known, but is not related to anticholinesterase-like activity.
dela Pena, Irene Joy I.,Kim, Hee Jin,Botanas, Chrislean Jun,de la Pena, June Bryan,Van Le, Thi Hong,Nguyen, Minh Duc,Park, Jeong Hill,Cheong, Jae Hoon The Korean Society of Ginseng 2017 Journal of Ginseng Research Vol.41 No.2
Background: Panax vietnamensis Ha et Grushv. or Vietnamese ginseng (VG) is a recently discovered ginseng species. Studies on its chemical constituents have shown that VG is remarkably rich in ginseng saponins, particularly ocotillol saponins. However, the psychopharmacological effects of VG have not been characterized. Thus, in the present study we screened the psychopharmacological activities of VG in mice. Methods: VG extract (VGE) was orally administered to mice at various dosages to evaluate its psychomotor (open-field and rota-rod tests), sedative-hypnotic (pentobarbital-induced sleeping test), anti-stress (cold swimming test), anxiolytic (elevated plus-maze test), and cognitive (Y-maze and passive-avoidance tests) effects. Results: VGE treatment increased the spontaneous locomotor activity, enhanced the endurance to stress, reduced the anxiety-like behavior, and ameliorated the scopolamine-induced memory impairments in mice. In addition, VGE treatment did not alter the motor balance and coordination of mice and did not potentiate pentobarbital-induced sleep, indicating that VGE has no sedative-hypnotic effects. The effects of VGE were comparable to those of the Korean Red Ginseng extract. Conclusion: VG, like other ginseng products, has significant and potentially useful psychopharmacological effects. This includes, but is not limited to, psychomotor stimulation, anxiolytic, antistress, and memory enhancing effects.
Ike Dela PENA,정재훈,한덕현,김붕년 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.4
Methylphenidate is the most prescribed stimulantmedication for attention-deficit/hyperactivity disorder(ADHD). Despite the well documented clinical benefits ofthe drug, several questions remain unanswered concerningthe effects of extended methylphenidate use (e.g. canmethylphenidate be abused by ADHD patients? doesrepeated methylphenidate treatment produce addiction?). Preclinical studies can help address the long-term safety ofclinical treatments, moreover animal studies providevaluable information on the details of drug actions. Thespontaneously hypertensive rat (SHR), bred from normotensiveWistar Kyoto rat strain, is considered as the bestvalidated and the most widely used animal model ofADHD. We reviewed the findings of research reports thatinvestigated the abuse and dependence liability of methylphenidatein SHR. In particular, we surveyed the studieswhich investigated the effects of methylphenidate pretreatmenton subsequent methylphenidate-induced conditionedplace preference or self-administration for they maygive insights into the abuse or dependence liability of longtermmethylphenidate treatment in ADHD.
Ike Dela PENA,June Bryan dela Pen˜a,김붕년,한덕현,노민수,정재훈 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.5
Attention-deficit/hyperactivity disorder (ADHD),the most commonly diagnosed neurobehavioral disorder ofchildhood, is usually treated with psychostimulants (e.g.,amphetamine). Little is known about the neuronal and behavioralconsequences of chronic amphetamine use or abuse inindividuals with ADHD. Of all ADHD animal models, thespontaneously hypertensive rat (SHR) is the most validated andwidely used. Here, we analyzed striatal transcriptomes inamphetamine-pretreated SHRs (5 mg/kg, i.p. for 7 days [twicedaily]), which showed a conditioned place preference to andself-administration of amphetamine. Microarray analysesrevealed increased mRNA expression of 55 genes ([1.65-foldincrease), while 17 genes were downregulated (\0.6-fold) inthe striatum of SHRs. The main functional categories overrepresentedamong the differentially expressed genes in thestriatum include those involved in transcription (e.g., Cebpb,Per2), genes associated with angiogenesis (e.g., Kdr, Klf5), celladhesion (e.g., Col11a1, Ctgf), apoptosis (e.g., Nfkbia, Perp)and neuronal development (e.g., Egr2, Nr4a3). In conclusion,we dissected the striatal transcriptional responses to the reinforcingeffects of repeated amphetamine treatment in the SHRmodel ofADHD. Future studies should determine the influenceof these altered transcripts on amphetamine reinforcement inamphetamine-treated SHRs, and the clinical relevance of thepresent findings with regard to amphetamine use/abuse inADHD individuals.
Ike dela Pena,Seo Young Yoon,Hee Jin Kim,Sejin Park,Eun Young Hong,Jong Hoon Ryu,Il Ho Park,Jae Hoon Cheong 고려인삼학회 2014 Journal of Ginseng Research Vol.38 No.1
Background: Although ginsenosides such as Rg1, Rb1 and Rg3 have shown promise as potential nutraceuticals for cognitive impairment, their use has been limited due to high production cost and low potency. In particular, the process of extracting pure Rg3 from ginseng is laborious and expensive. Methods: We described the methods in preparing ginseol k-g3, an Rg3-enriched fraction, and evaluated its effects on scopolamine-induced memory impairment in mice. Results: Ginseol k-g3 (25e200 mg/kg) significantly reversed scopolamine-induced cognitive impairment in the passive avoidance, but not in Y-maze testing. Ginseol k-g3 (50 and 200 mg/kg) improved escape latency in training trials and increased swimming times within the target zone of the Morris water maze. The effect of ginseol k-g3 on the water maze task was more potent than that of Rg3 or Red ginseng. Acute or subchronic (6 d) treatment of ginseol k-g3 did not alter normal locomotor activity of mice in an open field. Ginseol k-g3 did not inhibit acetylcholinesterase activity, unlike donezepil, an acetylcholinesterase inhibitor. Rg3 enrichment through the ginseol k-g3 fraction enhanced the efficacy of Rg3 in scopolamineinduced memory impairment in mice as demonstrated in the Morris water maze task. Conclusion: The effects of ginseol k-g3 in ameliorating scopolamine-induced memory impairment in the passive avoidance and Morris water maze tests indicate its specific influence on reference or long-term memory. The mechanism underlying the reversal of scopolamine-induced amnesia by ginseol k-g3 is not yet known, but is not related to anticholinesterase-like activity.
윤서영,Ike Dela PENA,김성목,Tae Sun Woo,신찬영,손건호,박해일,이용수,류종훈,Mingli Jin,Kyeong-Man KIM,정재훈 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.1
In previous studies we have demonstrated thatthe c-aminobutryic acid-A (GABA-A) receptor antagonistoroxylin A has an awakening effect and it also repressesADHD-like behaviors (hyperactivity, impulsivity andinattention) in the spontaneously hypertensive rat (SHR)model of attention-deficit hyperactivity disorder (ADHD). We hypothesized that the effects of oroxylin A wereexerted via the GABA-A receptor given the important roleof the GABAergic system in ADHD. However, it is possiblethat aside from the GABAergic system, oroxylin Amay influence other systems especially those implicated inADHD (e.g. DAergic, etc.). To test this hypothesis, weevaluated the effects of GABA agonist, or dopamine (DA)antagonist in oroxylin A-induced alleviation of ADHD-likebehaviors in SHR. SHR showed inattention and impulsivityas measured by the Y-maze and the electro-foot shockaversive water drinking tests, respectively. Oroxylin Asignificantly improved these behaviors, furthermore, itseffect on SHR impulsivity was attenuated by haloperidol, aDA antagonist, but not by baicalein, an agonist of theGABA-A receptor. In vitro studies showed that oroxylin Ainhibited DA uptake similar to methylphenidate, a dopaminetransporter blocker, but did not influence norepinephrineuptake unlike atomoxetine, a selective NEreuptake inhibitor. Collectively, the present findings suggestthat oroxylin A improves ADHD-like behaviors inSHR via enhancement of DA neurotransmission and notmodulation of GABA pathway as previously reported. Importantly, the present study indicates the potential therapeuticvalue of oroxylin A in the treatment of ADHD.
Convulsion-related activities of Scutellaria flavones are related to the 5,7-dihydroxyl structures
Yoon, S.Y.,dela Pena, I.C.,Shin, C.Y.,Son, K.H.,Lee, Y.S.,Ryu, J.H.,Cheong, J.H.,Ko, K.H. North-Holland ; Elsevier Science Ltd 2011 european journal of pharmacology Vol.659 No.2
We screened the major bioactive flavones isolated from Scutellaria baicalensis (baicalin, baicalein and oroxylin A) for their convulsion related activities. In electrogenic response score system and the pentylenetetrazole seizure model, baicalein but not oroxylin A and baicalin exhibited anticonvulsant effects. In vitro studies also revealed that baicalein induced intracellular Cl<SUP>-</SUP> influx, whereas oroxylin A blocked muscimol- and baicalein-induced intracellular Cl<SUP>-</SUP> influx. The anticonvulsant effect of baicalein was inhibited by flumazenil, a benzodiazepine(BZD) receptor antagonist. Therefore, anticonvulsive effect of baicalein was mediated by the BZD binding site of GABA<SUB>A</SUB> receptor. The 5, 7-dihydroxyl group is present in the structure of the three flavones. It is postulated that this group played a key role in inducing convulsion-related activities.
Brusas, John Raymund,Dela Pena, Eden May B. The Korean Electrochemical Society 2021 Journal of electrochemical science and technology Vol.12 No.4
Deep eutectic solvents have been established as feasible metal electroplating solvent alternatives over traditional toxic aqueous plating baths. However, water, either added intentionally or unintentionally, can significantly influence the solvent's physical properties and performance, thereby hindering its industry application. In this study, the hygroscopicity, or the ability to absorb moisture from the environment, of synthesized ethaline (1:2 choline chloride:ethylene glycol) was investigated. The kinematic viscosity, electrical conductivity, electrochemical window, and water content of ethaline were monitored over a 2-week period. Karl Fischer titration tests showed that ethaline exposed to the atmosphere displayed significant hygroscopicity compared to its unexposed counterpart. <sup>1</sup>H NMR spectroscopy revealed that water vapor was readily absorbed at the surface due to the hydrophilic groups present in the ethaline molecule. Water uptake resulted in the decrease in viscosity, increase in electrical conductivity and narrowing of the electrochemical window of ethaline. Solution heating at 100℃ removed the absorbed moisture and allowed the recovery of the solvent's initial properties.