• Archives of Pharmacal Research
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• v.29 no.6
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• pp.508-513
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• 2006

The effect of acteoside, a phenylpropanoid glycoside isolated from Clerodendron trichotomum Thunberg, on histamine and arachidonic acid release was investigated in RBL 2H3 cells. Histamine was dose-dependently released from RBL 2H3 cells by melittin, arachidonic acid and thapsigargin. In extracellular $Ca^{2+}-free$ solution, basal secretion of histamins increased by two fold. The response of histamine release to melittin and thapsigargin in $Ca^{2+}-free$ solution was significantly decreased, whereas the response to arachidonic acid was significantly increased as compared with those in normal solution. Acteoside inhibited histamine release induced by melittin, arachidonic acid and thapsigargin in a dose-dependent manner in the presence or absence of extracellular $Ca^{2+}$. However, the inhibitory activity of acteoside was more potent in normal solution than that in $Ca^{2+}-free$ solution. These data suggest that inhibitory mechanism of acteoside on histamine release may be related to extracellular $Ca^{2+}$. On the other hand, acteoside significantly inhibited arachidonic acid release and prostaglandin $E_2$ production Induced by $0.5\;{\mu}M$ melittin. It is possible that acteoside may be developed as an anti-inflammatory agent.

• The Korean Journal of Pain
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• v.6 no.1
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• pp.32-39
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• 1993

Despite their sometimes fatal complications such as respiratory depression when used for postoperative pain control, intravenous and epidural narcotics remain the mainstay of treatment regimens. Because of the problems, anesthesiologists are seeking alternatives. We compared the analgesic effect and complications of continuous intravenous morphine with ketorolac. Ketorolac is a non-steroidal agent with potent analgesics and moderate anti-inflammatory activity. Forty ASA physical status I or II patients were given morphine(20 patients) or ketorolac(20 patients):In the morphine group, an initial bolus dose of 2 mg i.v. was given followed by continuous infusion at a rate of 1 mg/hr for 48 hours. The ketorolac group was given initial bolus of 30 mg i.v. This was followed by continuous infusion at a rate of 3.75 mg/hr for 48 hours using a Baxter Daymate Infuser. We checked systolic, diastolic and mean arterial pressure, heart rate, visual analogue scale(VAS) and the Prince Henry Score(PHS). This was done before the initial bolus, at 5, 15, 30 and 60 min, at 2, 6, 12, 24 and 48 hours after administration. We observed the side effects nausea and vomiting, pruritus, hypotension, somnolence, urinary retention and respiratory depression. From our study we believe ketorolac in selected patients, is as effective as morphine in alleviating postoperative pain without side effects of morphine.

• Journal of Microbiology and Biotechnology
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• v.27 no.9
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• pp.1639-1648
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• 2017

Curcumin is a natural polyphenolic compound, widely acclaimed for its antioxidant, anti-inflammatory, antibacterial, and anticancerous properties. However, its use has been limited due to its low-aqueous solubility and poor bioavailability, rapid clearance, and low cellular uptake. In order to assess the effect of glycosylation on the pharmacological properties of curcumin, one-pot multienzyme (OPME) chemoenzymatic glycosylation reactions with UDP-${\alpha}-{\text\tiny{D}}$-glucose or UDP-${\alpha}-{\text\tiny{D}}$-2-deoxyglucose as donor substrate were employed. The result indicated significant conversion of curcumin to its glycosylated derivatives: curcumin 4'-O-${\beta}$-glucoside, curcumin 4',4"-di-O-${\beta}$-glucoside, curcumin 4'-O-${\beta}$-2-deoxyglucoside, and curcumin 4',4"-di-O-${\beta}$-2-deoxyglucoside. The products were characterized by ultra-fast performance liquid chromatography, high-resolution quadruple-time-of-flight electrospray ionization-mass spectrometry, and NMR analyses. All the products showed improved water solubility and comparable antibacterial activities. Additionally, the curcumin 4'-O-${\beta}$-glucoside and curcumin 4'-O-${\beta}$-2-deoxyglucoside showed enhanced anticancer activities compared with the parent aglycone and diglycoside derivatives. This result indicates that glycosylation can be an effective approach for enhancing the pharmaceutical properties of different natural products, such as curcumin.

• Korean Journal of Microbiology
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• v.54 no.1
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• pp.18-23
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• 2018

A new naturally occurring benzoic acid derivative, benzyl 2,4-di(benzyloxy)benzoate (1) and six known compounds (2-7) were isolated from the fungus, Preussia sp. found in frozen soil of the Himalaya Mountain. The structures of the new compound, together with the known compounds were determined by 1D-and 2D-NMR experiments, as well as comparison with published values. In addition, to the best of our knowledge, the known compounds 2-7 were isolated for the first time from the genus Preussia and the family Sporormiaceae. The isolates were evaluated for cancer chemopreventive potential based on their ability to inhibit nitric oxide (NO) production induced by lipopolysaccharide (LPS) in mouse macrophage RAW 264.7 cells in vitro. Compounds 1 and 2 inhibited NO production by 50.7% and 88.5% at a concentration of 100 mg/ml, respectively.

• Journal of Ginseng Research
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• v.39 no.1
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• pp.14-21
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• 2015

Background: Colorectal cancer is a leading cause of cancer-related death, and inflammatory bowel disease is a risk factor for this malignancy. We previously reported colon cancer chemoprevention potential using American ginseng (AG) in a xenograft mice model. However, the nude mouse model is not a gut-specific colon carcinogenesis animal model. Methods: In this study, an experimental colitis and colitis-associated colorectal carcinogenesis mouse model, chemically induced by azoxymethane/dextran sodium sulfate (DSS) was established and the effects of oral AG were evaluated. The contents of representative ginseng saponins in the extract were determined. Results: AG significantly reduced experimental colitis measured by the disease activity index scores. This suppression of the experimental colitis was not only evident during DSS treatment, but also very obvious after the cessation of DSS, suggesting that the ginseng significantly promoted recovery from the colitis. Consistent with the anti-inflammation data, we showed that ginseng very significantly attenuated azoxymethane/DSS-induced colon carcinogenesis by reducing the colon tumor number and tumor load. The ginseng also effectively suppressed DSS-induced proinflammatory cytokines activation using an enzyme-linked immunosorbent assay array, in which 12 proinflammatory cytokine levels were assessed, and this effect was supported subsequently by real-time polymerase chain reaction data. Conclusion: AG, as a candidate of botanical-based colon cancer chemoprevention, should be further investigated for its potential clinical utility.

• Food Science and Preservation
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• v.18 no.6
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• pp.954-960
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• 2011

The antioxidant activities of the ethanol, methanol, and water extracts of black onion were investigated. The highest extraction yield (28.56%) and total polyphenol content (13.5 mg/g) were found in the water extract. The water extract also showed the highest protective effect on the RAW 264.7 cell anti-inflammatory activity, and the water and ethanol extracts showed the highest reducing power. The water extract showed higher DPPH and ABTS radical scavenging activities (65.98 and 89.69%, respectively) than the other solvent extracts (ethanol, 47.77%; methanol, 66.12%). Hence, black onion can be used as a potent natural antioxidative source.

• The Journal of Pediatrics of Korean Medicine
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• v.35 no.3
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• pp.118-127
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• 2021

Objective The purpose of this study was to confirm the effect of Scutellaria baicalensis extract on skin damage recovery and inflammation relief in atopic dermatitis-induced mice through Endocannabinoid system (ECS) control. Methods 6-week-old Balb/C mice were divided into control group (Ctrl), atopic dermatitis induced group (ADE), palmitoylethanolamide (PEA) administered group after atopic dermatitis induced (PEAT), and Scutellaria baicalensis extract administered group after atopic dermatitis induced (SBT). Seven animals were assigned for each group. After drug administration for 3 weeks after inducing atopic dermatitis, Claudin and 8-OHdG were observed to confirm the recovery of the skin damage in each group. To confirm ECS regulation, CB1, CB2, and GPR55 were observed. To confirm the anti-inflammatory effect, Fc ε receptor, and MMP-9 was observed. Results Claudin positive reaction was significantly increased in SBT compared to ADE and PEAT. 8-OHdG positive reaction was significantly decreased in SBT compared to ADE and PEAT. CB1, CB2, and GPR55 positive responses were significantly increased in SBT compared to ADE and PEAT. Fc ε receptor and MMP-9 positivity were significantly decreased in SBT compared to ADE and PEAT. Conclusion It was confirmed that the Scutellaria baicalensis extract can reduce the inflammation of atopic dermatitis by restoring the structural damage of the skin lipid barrier through ECS activity.

• The Korean Journal of Physiology and Pharmacology
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• v.23 no.2
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• pp.103-111
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• 2019

The study is to investigate effects of andrographolide on experimental autoimmune myocarditis (EAM). Lewis rats were immunized on day 0 with porcine cardiac myosin to establish EAM. The EAM rats were treated with either andrographolide (25, 50, 100 mg/kg/day) or vehicle for 21 days. An antigen-specific splenocytes proliferation assay was performed by using the cells from control rats immunized with cardiac myosin. Survival rates, myocardial pathology and myocardial functional parameters (left ventricle end-diastolic pressure, ${\pm}dP/dt$ and left ventricular internal dimension) of EAM rats received andrographolide were significantly improved. Andrographolide treatment caused an decrease in the infiltration of $CD3^+$ and $CD14^+$ positive cells in myocardial tissue. Moreover, andrographolide treatment caused a reduction in the plasma levels of tumor necrosis factor-alpha, interleukin-17 (IL-17) and myosin-antibody, and an increase in the level of IL-10 in EAM rats. Oral administration of andrographolide resulted in the decreased expression of p-PI3K, p-Akt without any change of PI3K and Akt. Further results indicate andrographolide significantly inhibited myosin-induced proliferation in splenocytes, and this effect was inhibited by co-treatment of SC79 (Akt activator). Our data indicate andrographolide inhibits development of EAM, and this beneficial effect may be due to powerful anti-inflammatory activity and inhibitory effect on PI3K/Akt pathway.

• The Journal of Korean Medicine
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• v.40 no.2
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• pp.51-62
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• 2019

Objectives: This study was designed to evaluate the macrophages polarization of traditional Korean medicine on cardiac pain about Geum-Gwe-Yo-Ryak's two prescriptions including Kwaruhaebaekbanha-tang (KHB) and Kwaruhaebaekpaekju-tang (KHP). Materials and methods: Flow cytometry analysis was used to measure the changes in the ratio of M1 type and M2 type macrophages. Protein expression of nuclear factor-like 2 (Nrf2), heme oxygenase-1 (HO-1), inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) were measured by Western Blot, and ABCA1 and SR-B1 were detected by real time PCR (RT-PCR). Intracellular lipid accumulation was measured by Oil Red O staining (ORO staining). Results: KHB and KHP increase anti-oxidative activity related protein levels including Nrf2 and HO-1. Furthermore, KHB and KHP inhibit lipid accumulation on intracellular levels through induction of ATP binding receptor cassette subfamily A member 1 (ABCA1) and scavenging receptor class B member 1 (SR-B1), respectively. Finally, KHB and KHP also blocked pro-inflammatory mediators including tumor necrosis factor-alpha ($TNF{\alpha}$) and interleukin-6 (IL-6), iNOS and COX-2 expression. Conclusion: This study suggests that KHB and KHP potently regulate the M1/M2 macrophage polarization.

• Biomolecules & Therapeutics
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• v.27 no.4
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• pp.363-372
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• 2019

Daidzein isolated from soybean (Glycine max) has been widely studied for its antioxidant and anti-inflammatory activities. However, the protective effects of 7,8,4'-trihydroxyisoflavone (THIF), a major metabolite of daidzein, on 6-hydroxydopamine (OHDA)-induced neurotoxicity are not well understood. In the current study, 7,8,4'-THIF significantly inhibited neuronal cell death and lactate dehydrogenase (LDH) release induced by 6-OHDA in SH-SY5Y cells, which were used as an in vitro model of Parkinson's disease (PD). Moreover, pretreatment with 7,8,4'-THIF significantly increased the levels of superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH) and decreased malondialdehyde (MDA) activity in 6-OHDA-induced SH-SY5Y cells. In addition, 7,8,4'-THIF significantly recovered 6-OHDA-induced cleaved caspase-3, cleaved caspase-9, cleaved poly-ADP-ribose polymerase (PARP), increased Bax, and decreased Bcl-2 levels. Additionally, 7,8,4'-THIF significantly restored the expression levels of phosphorylated c-Jun N-terminal kinase (JNK), p38 mitogen-activated protein kinase (MAPK), extracellular signal-regulated kinase 1/2 (ERK 1/2), phosphatidylinositol 3-kinases (PI3K)/Akt, and glycogen synthase kinase-3 beta ($GSK-3{\beta}$) in 6-OHDA-induced SH-SY5Y cells. Further, 7,8,4'-THIF significantly increased the reduced tyrosine hydroxylase (TH) level induced by 6-OHDA in SH-SY5Y cells. Collectively, these results suggest that 7,8,4'-THIF protects against 6-OHDA-induced neuronal cell death in cellular PD models. Also, these effects are mediated partly by inhibiting activation of the MAPK and PI3K/Akt/$GSK-3{\beta}$ pathways.