• Proceedings of the Plant Resources Society of Korea Conference
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• 2021.04a
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• pp.54-54
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• 2021

The Melanoma Research Coalition reported melanoma affects humans of various races. This study was conducted to confirm the inhibitory effect of melanogenesis in B16 F10 cells of Nypa fruticans Wurmb of ethyl acetate fraction (NEF). Nypa fruticans Wurmb is an important component of the East Asian mangrove vegetation. It belongs to Araceae family. Traditionally, N. fruticans was used to treat various diseases such as asthma, sore throat, liver disease, a pain reliever, and can also be used as sedative and carminative. The present study, the inhibitory effect on melanogenesis was determined by Western blotting and RT-qPCR. The level of expression of tyrosinase, TRP-1, and TRP-2 is regulated by microphthalmia-associated transcription factor (MITF) and cAMP, and cAMP affects the activity of protein kinase A (PKA). Activated PKA stimulates the phosphorylation of cAMP-reactive element-binding protein (CREB) in the nucleus, thereby increasing the amount of MITF expression and enhancing melanogenesis. Western blotting and RT-qPCR analysis showed that NEF treatment decreased the expression of tyrosinase. Similarly, TRP-1 and TRP-2 levels were decreased, which were decreased significantly at compared with the untreated control. Also, NEF attenuated the IBMX mediated increase in the intracellular cAMP level and the phosphorylation of PKA. In conclusion, NEF significantly inhibited the expressions of melanogenesis through cAMP/PKA/CREB signaling pathways.

• The Korean Journal of Pain
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• v.8 no.2
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• pp.257-265
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• 1995

Patient-Controlled Analgesia (PCA) has been widely used for postoperative pain relief. Meperidine is useful for PCA and has efficient analgesia, rapid onset, and low incidence of adverse effect. To compare the analgesic effect, total dose and hourly dose, side effect and neonatal status of breast feeding with meperidine via intravenous or epidural PCA for 48 hours after Cesarean Section, 40 parturient women undergoing elective Cesarean Section were randomly divided into two groups. Each respective group of 20 parturient women received meperidine via one of the intravenous PCA after general anesthesia with enflurane (IVPCA group) and the epidural PCA after general anesthesia with enflurane (IVPCA group) and the epidural PCA after epidural block with 2% lidocaine 20ml combined with general anesthesia with only $N_2O$ and $O_2$ (EpiPCA group) when they first complained of pain in recovery room. Following the administration of analgesic initial dose, parturient women of IVPCA group were allowed intravenous meperidine 10 mg every 8 minutes when they felt pain. The EpiPCA group received additional bolus dose of meperidine 2 mg and bupivacaine 0.7 mg were administered every 8 minutes as requested the patients with hourly continuous infusion of meperidine 4 mg and bupivacaine 1.4 mg. Data was collected during the 48 hours observation period including visual analog scale (VAS) pain scores, total meperidine dose, hourly dose during 48 hours and each time interval, incidence of adverse effect, satisfaction, and neonatal status with breast feeding. VAS pain scores of analgesic effect in EpiPCA group was significantly lower than in IVPCA group at 2 hours after the initial pain after Cesarean Section. Total dose and hourly dose of meperidine significantly reduced in EpiPCA group. Hourly dose of meperidine at each time interval significantly reduced during first 6 hours and from 12 hours to 24 hours in EpiPCA group. The side effects in IVPCA group were mainly sedation, nausea, and local irritation of skin. And EpiPCA group experienced numbness and itching. The degree of satisfaction of parturient women was 88.2 % in IVPCA group and 85.7 % in EpiPCA group. We did not observe any sedation, abnormal behavior, or seizure like activity in any neonates of breast feeding. From the above results we conclude that epidural PCA was more efficiently analgesic, less sedative, and consumptional, and safer for neonate than intravenous PCA, and could be an alternative method to intravenous PCA.

• Journal of the korean academy of Pediatric Dentistry
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• v.32 no.3
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• pp.499-508
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• 2005

The purpose of this study were to evaluate the effect on the reversion of sedation induced by midazolam with flumazenil and to determine the plasma concentration of flumazenil according to the method of administration. Intranasal and intravenous flumazenil were administered to sedated health volunteers aged from 23 to 25 years, in doses typical of those used clinically to induce sedation with midazolam and for reversal with flumazenil. Objective assessment for degree of sedation and vital signs, plasma concentration were made for 2 hours period. 1. Systolic and diastolic blood pressure, $SpO_2$ were not changed by adminstration of flumazenil in sedated subject with midazolam, but pulse rate was increased temporarily. 2. Flumazenil showed the reversal of the sedative effect induced by midazolam regardless of administration methods. But intravenous administration showed more effect on the degree and the duration of reversion than intranasal administration with the exception of on set time. 3. Peak plasma concentration of flumazenil administered by intranasal route reached after 2 min and that of flumazenil administered by intravenous route was 4 min. Thus uptake of flumazenil did not showed any difference in accordance with the adminstration route. 4. Administration of flumazenil resulted in the temporary increase of midazolam plasma concentration.

• The Korean Journal of Pain
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• v.33 no.2
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• pp.108-120
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• 2020

From the perspective of the definition of pain, pain can be divided into emotional and sensory components, which originate from potential and actual tissue damage, respectively. The pharmacologic treatment of the emotional pain component includes antianxiety drugs, antidepressants, and antipsychotics. The anti-anxiety drugs have anti-anxious, sedative, and somnolent effects. The antipsychotics are effective in patients with positive symptoms of psychosis. On the other hand, the sensory pain component can be divided into nociceptive and neuropathic pain. Non-steroidal anti-inflammatory drugs (NSAIDs) and opioids are usually applied for somatic and visceral nociceptive pain, respectively; anticonvulsants and antidepressants are administered for the treatment of neuropathic pain with positive and negative symptoms, respectively. The NSAIDs, which inhibit the cyclo-oxygenase pathway, exhibit anti-inflammatory, antipyretic, and analgesic effects; however, they have a therapeutic ceiling. The adverse reactions (ADRs) of the NSAIDs include gastrointestinal problems, generalized edema, and increased bleeding tendency. The opioids, which bind to the opioid receptors, present an analgesic effect only, without anti-inflammatory, antipyretic, or ceiling effects. The ADRs of the opioids start from itching and nausea/vomiting to cardiovascular and respiratory depression, as well as constipation. The anticonvulsants include carbamazepine, related to sodium channel blockade, and gabapentin and pregabalin, related to calcium blockade. The antidepressants show their analgesic actions mainly through inhibiting the reuptake of serotonin or norepinephrine. Most drugs, except NSAIDs, need an updose titration period. The principle of polypharmacy for analgesia in case of mixed components of pain is increasing therapeutic effects while reducing ADRs, based on the origin of the pain.

• Journal of Acupuncture Research
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• v.26 no.1
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• pp.121-133
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• 2009

Objectives : The purpose of this study is to find out the clinical possibility of Bufonis Venenum used without toxicity and side effect. Methods : We investigated the pharmacological effects, toxicity and processing of Bufonis Venenum through the literatures and studies. Results : Bufonis Venenum is made by parotid gland of dermato gland of Bufo bufo gargarizns or B. melanostictus Schneider, and it is dried for using. The medical ation of Bufonis Venenum are cardiotonic, respiration stimulation, anticancer, topical anesthesia. The toxic symptoms of Bufonis Venenum are relative with digestive, circulatory, nervous system similared with digitalis toxicity. It is important to take 0.015-0.03g by mouth, external use about 1-4% 0.5-3ml and 2-8ml injections by 20ml mix to 5% dextrose fluid. Bufonis Venenum is processed to prevent toxicity and evaluate efficacy by alcohol and milk. There are 68 prescription consisted by Bufonis Venenum in KTKP(Korean Traditional Knowledge Portal). They usually use for antiabcess, anticancer with Moschus moschiferus(麝香), Cinnabar(朱砂). Conclusions : The results from above literary studies show that internal, external medicine and Aqua-acupuncture of Bufonis Venenum could be clinically used to sedative, antiinflammatory, anticancer and topical ataralgesia without toxity through optimum dose and processing.

• The Korean Journal of Pharmacology
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• v.19 no.1
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• pp.77-84
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• 1983

The behavioral pattern of an animal is influenced by endogenous and endogenous stimuli such as humoral secretion, neurohumoral transmitters, drugs, light and environmental change. It has teen known that adenosine is a normal constituent of brain, and has sedative or hypnotic effects and anticonvulsant effects, inhibiting the spontaneous firing of cells in the brain via membrane adenosine receptors. Recent studies suggest that the excitatory responses to xanthines in the CNS might be related to the competitive antagonism of xanthines to adenosine. This study was undertaken to Investigate the effects of adenosine and the CNS stimulants such as picrotoxin, strychnine and caffeine on the spontaneous activity of mire, and to examine the influence of adenosine on the seizures induced by large doses of CNS stimulants. Subjects were $20{\sim}30\;g$ adult mice, and the spontaneous activity was measured using the Selective Activity Meter after intraperitoneal injection of adenosine (10 mg/kg), caffeine (100 mg/kg), strychnine(0.2 mg/kg) or picrotoxin(0.5 mg/kg) with or without adenosine pretreatment. The seizures were induced with caffeine(200, 250 and 300 mg/kg), strychnine(1.25 and 1.5 mg/kg) or picrotoxin(10 and 15 mg/kg). The results are summarized as follows : 1) The spontaneous activity in mite was significantly inhibited between 10 and 20 minutes after adenosine treatment. 2) Caffeine and picrotoxin increased the motor activity significantly while strychnine had no effect on the activity. 3) The ambulatory activity in the caffeine, strychnine and picrotoxin treated groups was significantly inhibited by adenosine pretreatment. 4) The seizures were observed with caffeine(200, 250 and 300 m9/kg), strychnine(1.25 and 1.5 mg/kg) or picrotoxin(10 and 15 mg/kg). The caffeine induced seizures were inhibited by adenosine pretreatment, but the strychnine or picrotoxin induced seizures were not affected.

• Ocean and Polar Research
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• v.27 no.1
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• pp.59-65
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• 2005

To assess the effect of anaesthetic on stress response in cultured sweetfish (Plecoglossus altivelis) during transportation, the levels of plasma cortisol, glucose, lactic acid, $Na^+,\;K^+,\;Cl^-$, osmolality and survival were determined. The transportation was performed in square boxes where liquefied oxygen was saturated in polyethylene bags. Fish transportation was carried by car for 2 hours after anaesthesis with lidocaine-HCl/1,000 ppm $NaHCO_3$ in experiment. Mean plasma cortisol concentration before transportation was 170.7ng/ml. After transportation, the levels of plasma cortisol increased to 518.5ng/ml (Control), 461.9ng/ml (Sham control), 369.4ng/ml (20ppm anaesthetic), 304.0ng/ml (40 ppm anaesthetic), 405.7ng/ml (80 ppm anaesthetic) and 499.1ng/ml (160ppm anaesthetic) in each experimental groups, respectively (p<0.05). However levels of glucose, lactic acid, $Na^+,\;Cl^-$ and osmolality in 40ppm anaesthetic group did not show significant differences in this before and after transportation (P>0.05). These result reveal an anaesthetic lidocaine HCl/1,000ppm $NaHCO_3$ is effective as sedative for transportation mixture in this species. This research provides baseline data on cortisol, glucose, lactic acid, $Na^+,\;K^+,\;Cl^-$, osmolality and survival for anaesthetic transportation.

• Biomolecules & Therapeutics
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• v.24 no.2
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• pp.115-122
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• 2016

Sleep, which is an essential part of human life, is modulated by neurotransmitter systems, including gamma-aminobutyric acid (GABA) and dopamine signaling. However, the mechanisms that initiate and maintain sleep remain obscure. In this study, we investigated the relationship between melatonin (MT) and dopamine D2-like receptor signaling in pentobarbital-induced sleep and the intracellular mechanisms of sleep maintenance in the cerebral cortex. In mice, pentobarbital-induced sleep was augmented by intraperitoneal administration of 30 mg/kg MT. To investigate the relationship between MT and D2-like receptors, we administered quinpirole, a D2-like receptor agonist, to MT- and pentobarbital-treated mice. Quinpirole (1 mg/kg, i.p.) increased the duration of MT-augmented sleep in mice. In addition, locomotor activity analysis showed that neither MT nor quinpirole produced sedative effects when administered alone. In order to understand the mechanisms underlying quinpirole-augmented sleep, we measured protein levels of mitogen-activated protein kinases (MAPKs) and cortical protein kinases related to MT signaling. Treatment with quinpirole or MT activated extracellular-signal-regulated kinase 1 and 2 (ERK1/2), p38 MAPK, and protein kinase C (PKC) in the cerebral cortex, while protein kinase A (PKA) activation was not altered significantly. Taken together, our results show that quinpirole increases the duration of MT-augmented sleep through ERK1/2, p38 MAPK, and PKC signaling. These findings suggest that modulation of D2-like receptors might enhance the effect of MT on sleep.

• Korean Journal of Plant Resources
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• v.24 no.3
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• pp.314-318
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• 2011

Saururus chinensis is used as a raw material of an anti-rheumatic, poultice, sedative and stomachic. The tea of dried Saururus chinensis leaves has a function of relaxing pains in back and breast and of treating stomach ailments. The plant has the functions of anti-inflammatory, depurative, diuretic, febrifuge and refrigerant. The extraction of functional material is carried out by methanol and ethanol solvents. Mechanochemical grinding is applied as a pretreatment process before extraction to enhance the extraction efficiency by increasing the surface area of the materials while changing the chemical properties of the materials. Extraction of functional materials from the Saururus chinensis after grinding as a pretreatment using the mechanochemical technology was accomplished in this study to investigate the effect of grinding on the antioxidant activities of the extract. Saururus chinensis was ground by the planetary ball mill and the morphology was analyzed by SEM. Mechanochemical pretreatment increased the yields of functional materials from 5.9 g to 6.4, 7.0, and 8.1 g after grinding of 30 minutes, 1 hour and 2 hours, respectively. Nitrite scavenging ability increased from 53.0-71.0% to 61.0-79.0% for the methanol extraction in the solution of pH 1.2. Also, Electron donating abilities were increased from 7.90-33.51% to 11.97-38.51% for the methanol extraction. The extract concentration for the half inhibition of DPPH radicals was reduced from $278{\mu}g/mL$ in the original sample to $263{\mu}g/mL$ in the sample after grinding for the methanol extraction.

• Journal of Physiology & Pathology in Korean Medicine
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• v.25 no.1
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• pp.29-36
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• 2011

Nardostachyts chinensis (N. chinensis) belonging to the family Valerianaceae has been used to elicit stomachic and sedative effects. The MAPKs are serine/threonine kinases involved in the regulation of various cellular responses, such as cell proliferation, differentiation and apoptosis. The PKC also plays a key role in regulating the response of hematopoietic cells to both physiological and pathological inducers of proliferation and differentiation. This study investigated the signaling pathways on the U937 cell differentiation induced by N. chinensis. N. chinensis induced the differentiation of U937 cells, as shown by increased of differentiation surface antigen CD11b. Activation of ERK increased time-dependently in differentiation of U937 cells induced by N. chinensis, but activations of JNK and p38 were unaffected. Inhibitor of ERK (PD98059) significantly reduced CD11b expression induced by N. chinensis in U937 cells. In addition, N. chinensis increased protein level of PKC ${\beta}$I and PKC ${\beta}$II isoforms, but the protein level of PKC ${\alpha}$ and PKC ${\gamma}$was constant. PKC inhibitors (GF 109203X and H-7) inhibited U937 cell differentiation and the ERK activation induced by N. chinensis. These results indicated that PKC and ERK may be involved in U937 cell differentiation induced by N. chinensis.