• The Journal of Korean Obstetrics and Gynecology
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• v.19 no.4
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• pp.1-16
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• 2006

Purpose : The purpose of this research was to investigate the effects of Kamibojoongikkitang (KBT) on the immune cells in C57BL/6 mice. Methods : KBT (500mg/kg) was administerd p.o. once a day for 7 days. Results : KBT decreased the cell viability of thymocytes in vivo and in vitro system and decreased the cell viability of splenocytes in vivo, but increased the viability of splenocytes in vitro system. In addition, KBT did not affect the population of helper T (Th) cells and cytotoxic T (Tc) cells in thymocytes and decreased the population of T- and B-lymphocytes and the population of Th and Tc cells in splenocytes. Furthermore, KBT did not affect the production of ${\gamma}%-interferon and interleukin-4 in splenocytes. KBT increased the production of nitric oxide in vivo but decreased the production of nitric oxide in vitro system. KBT enhanced the phagocytic activity of peritoneal macrophages in vivo, but decreased the phagocytic activity in vitro. Conclusion : KBT has an inhibitory action on the specific immune response via decrease of the cell viability of thymocytes and splenocytes and has a potent action on the non-specific immunity via increase of phagocytic activity of peritoneal macrophages.

• Journal of Oriental Neuropsychiatry
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• v.18 no.2
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• pp.101-132
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• 2007

Objective : This research investigates the effect of the NogYongDaeBoTang,(NYDBT) on Alzheimer's disease. Method : The effects of the NYDBT extract on (1) $IL-1{\beta}$, IL-6, and $TNF-{\alpha}$ mRNA of PC-12 cells treated with LPS; (2) acetylcholinesterase(AChE), amyloid precursor proteins(APP), and glial fibrillary acidic protein(GFAP) mRNA the AChE activity and the APP production of PC-12 cell treated with CT-105; (3) the behavior; (4) expression of $IL-1{\beta}$, $TNF-{\alpha}$, MDA, $IL-1{\beta}$ mRNA, and $TNF-{\alpha}$ mRNA; (5) the infarction area of the hippocampus, and brain tissue injury in Alzheimer‘s diseased mice induced with ${\beta}A$ were investigated. Results : 1. The NYDBT extract suppressed the expression of $IL-1{\beta}$, IL-6 and $TNF-{\alpha}$ mRNA in BV2 microglia cell line treated with LPS. 2. The NYDBT extract suppressed the expression of $IL-1{\beta}$, IL-6, and $TNF-{\alpha}$ protein production in BV2 microglia cell line treated with LPS. 3. For the NYDBT extract group a significant inhibitory effect on the memory deficit was shown for the mice with Alzheimer's disease induced by $A{\beta}$ in the Morris water maze experiment, which measured stop-through latency, and distance movement-through latency. 4. The NYDBT extract suppressed the over-expression of $IL-1{\beta}$ protein, $TNF-{\alpha}$ protein, MDA, and CD68/CD11b, in the mice with Alzheimer's disease induced by $A{\beta}$. 5. The NYDBT extract reduced the infarction area of hippocampus, and controlled the injury of brain tissue in the mice with Alzheimer's disease induced by $A{\beta}$. 6. The NYDBT extract reduced the Tau protein, GFAP protein, and presenilin1/2 protein (immunohistochemistry) of hippocampus in the mice with Alzheimer's disease induced by $A{\beta}$. Conclusions : These results suggest that the NYDBT extract may be effective for the prevention and treatment of Alzheimer's disease.

• Journal of Mushroom
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• v.19 no.3
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• pp.176-183
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• 2021

In this study, the anti-inflammatory activity of an extract of the fruiting body of the Tuber himalayense (TH) truffle collected from oak growing areas in Korea was investigated. The extract was not cytotoxic at concentrations below 100 ㎍/mL in an experiment evaluating inflammation inhibitory effect in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. LPS-induced nitric oxide (NO) and prostaglandin E2 (PGE₂) production was inhibited by the extract in a concentration-dependent manner. Western blot assay results indicated that the anti-inflammatory activity of TH extract was likely caused by the reduced production of NO and PGE₂ via suppression of induced NO synthase and cyclooxygenase-2 gene expression. In addition, TH extract effectively inhibited the production of interleukin (IL)-1β and IL-6 by macrophages. Thus, TH extract effectively inhibits the overexpression of various inflammatory mediators and could be valuable in formulating anti-inflammatory foods and medicines that target these components.

• Molecules and Cells
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• v.41 no.6
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• pp.545-552
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• 2018

Spleen tyrosine kinase (SYK) is a cytosolic non-receptor protein tyrosine kinase. Because SYK mediates key receptor signaling pathways involving the B cell receptor and Fc receptors, SYK is an attractive target for autoimmune disease and cancer treatments. To date, representative oral SYK inhibitors, including fostamatinib (R406 or R788), entospletinib (GS-9973), cerdulatinib (PRT062070), and TAK-659, have been assessed in clinical trials. Here, we report the crystal structures of SYK in complex with two newly developed inhibitors possessing 4-aminopyrido[4,3-D]pyrimidine moieties (SKI-G-618 and SKI-O-85). One SYK inhibitor (SKI-G-618) exhibited moderate inhibitory activity against SYK, whereas the other inhibitor (SKI-O-85) exhibited a low inhibitory profile against SYK. Binding mode analysis indicates that a highly potent SYK inhibitor might be developed by modifying and optimizing the functional groups that interact with Leu377, Gly378, and Val385 in the G-loop and the nearby region in SYK. In agreement with our structural analysis, one of our SYK inhibitor (SKI-G-618) shows strong inhibitory activities on the ${\beta}$-hexosaminidase release and phosphorylation of SYK/Vav in RBL-2H3 cells. Taken together, our findings have important implications for the design of high affinity SYK inhibitors.

• The Journal of Korean Medicine
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• v.42 no.4
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• pp.10-24
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• 2021

Objectives: Yongdamsagan-tang (YST) and Paljung-san (PJS) in traditional medicine and finasteride in modern medicine are used to treat benign prostatic hyperplasia (BPH). In recent, the use of combination herbal remedies with conventional drugs has been increasing. Therefore, we investigated the anti-inflammatory effects of these drugs to treat BPH and the influence of herbal formulas on finasteride metabolism. Methods: The inhibitory effects of the herbal formulas and finasteride on the production of inflammatory mediators and cytokines were determined in lipopolysaccharide (LPS)-treated RAW 264.7 cells. Additionally, the influence of herbal formulas on activities of human drug metabolizing enzymes (DMEs) was assessed using human microsomal enzymes. Results: We observed that YST, PJS and finasteride inhibited the production of nitric oxide (NO), prostaglandin E₂ (PGE₂) and interleukin-6 (IL-6) in RAW 264.7 cells. The half maximal inhibitory concentration (IC₅₀) of YST on PGE₂ production was calculated to be below 25 ㎍/mL. YST inhibited the activity of uridine diphosphate-glucuronosyltransterase (UGT) 1A4 with an IC₅₀ value of 49.35 ㎍/mL. The activities of cytochrome P450 (CYP) 1A2, CYP2B6, CYP2C19, CYP3A4, and UGT1A1 were inhibited by PJS (IC₅₀ < 100 ㎍/mL, each). Although PJS and YST inhibited the activities of CYP3A4 and UGT1A4, respectively, these formulas may not influence the metabolism of finasteride because the IC₅₀ values of herbal formulas on DMEs are too high to affect metabolism. Conclusions: Our results suggest that the combination of finasteride and YST or PJS might not influence their drug metabolism and that the drugs may have synergistic effects against BPH.

• Journal of the Korean Applied Science and Technology
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• v.38 no.6
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• pp.1543-1552
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• 2021

Atractylodes japonica has been widely used in a traditional Korean herbal medicine exerting various pharmacological activities such as diauretic action, asriction, anti-allergy, neuroprotective activity, anti-cancer, immunomodulation and gastrointestinal protective effect. This study was to investigate the antioxidant, nitric oxide and inflammatory cytokines production of A. japonica extract by water and 70% ethanol. DPPH and ABTS free radical scavenging activity were increased in a dose-dependent manners with both extracts and there was no difference with extract solvents. 70% ethanol extract of A. japonica showed a very strong inhibitory effect on NO production. Both extracts of A. japonica significantly reduce the expression of iNOS and COX-2 proteins involved in NO prodction. A. japonica extract by water and 70% ethanol inhibited LPS-induced proinflammatory cytokines such as IL-6 and IL-1b. In this study, 70% ethanol extract of A. japonica significantly suppresses LPS-induced NO and inflammatory cytokine production. Therefore it can be widely used to treat and improve inflammatory diseases.

• Journal of Nutrition and Health
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• v.56 no.6
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• pp.615-628
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• 2023

Purpose: Increasing levels of domestic fine dust (DFD) have emerged as a serious problem that threatens public health by causing chronic respiratory diseases and skin aging. The present study was performed to investigate the inhibitory effects of Gryllus bimaculatus (the two-spotted cricket), which has recently attracted attention as an edible insect in South Korea, on DFD-induced aging and inflammation. Methods: To verify that DFD causes skin aging and investigate the anti-aging effect of an aqueous ethanolic-Gryllus bimaculatus extract (AE-GBE), human diploid fibroblasts (HDF) were treated with 100 ㎍/mL of European reference material (ERM)-CZ100 dust for 24 hrs in the presence or absence of 100 ㎍/ml AE-GBE. Aging and cellular toxicities were assessed by measuring reactive oxygen species (ROS) levels, DNA fragmentation, and β-galactosidase activity. The protein levels of cyclooxygenase (COX) 2, matrix metalloproteinase (MMP)-1, and collagen were measured by western blot, and the mRNA expressions of inflammation-related genes were assayed by quantitative reverse transcriptase polymerase chain reaction. Results: Treatment with ERM-CZ100 induced an aged phenotype in HDF cells, as evidenced by increased ROS levels, DNA fragmentation, and senescence-associated β-galactosidase activity, but cotreatment with AE-GBE significantly reduced these inductions. The mRNA expressions of pro-inflammatory cytokines, such as interleukin (IL)-1β, IL-6, and tumor necrosis factor-α, induced by ERM-CZ100 were also reduced by AE-GBE cotreatment, which also reduced COX2 expression. Moreover, ERM-CZ100-induced MMP-1 expression and reduced collagen type I expression were recovered by AE-GBE treatment. Conclusion: These results suggest that AE-GBE is a potential treatment for domestic fine dust-induced skin inflammation and inflammaging.

• Journal of Korean Medicine Rehabilitation
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• v.26 no.3
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• pp.31-49
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• 2016

Objectives The study was designed to evaluate the healing effects of Joaguihwan (JGH) extract on Anti-oxidation, Anti-inflammatory in RAW 264.7 Cells and factors related with bone metabolism in skull fractured Rat. Methods The fracture healing effect of JGH was measured by scavenging activities of1,1-diphenyl-2-picryl-hydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS) and nitric oxide (NO) in RAW 264.7 cells. The inhibitory effect against the production of inflammatory mediators including interleukin-$1{\beta}$ (IL-$1{\beta}$), interleukin-6 (IL-6), tumor necosis factors-${\alpha}$ (TNF-${\alpha}$) expression was inhibited in RAW 264.7 cells was experimented using JGH. The effects of JGH on healing fractured rats was measured by osteocalcin, calcitonin, CTXII, TGF-${\beta}$, BMP-2, Insulin, ALP in the serum. and was checked every 3 weeks from 0 week to 6week using x-ray. Results 1. DPPH free radica and ABTS scavenging activity of JGH were increased according to concentration of JGH in RAW 264.7 Cells. 2. In the experiment, NO, IL-$1{\beta}$, IL-6, TNF-${\alpha}$ all showed decrease, in general. Especially NO and IL-$1{\beta}$ showed significantly decrease at a concentration of 10, 100 (${\mu}g/ml$). 3. In the production of osteocalcin in the serum, JGH 200, 400 mg/kg experimental group showed significant increased effect at 2 weeks. 4. In the production of calcitonin in the serum. JGH 200 mg/kg experimental group showed significant increased effect at 4, 6 weeks. JGH 400 mg/kg experimental group showed significant increased effect at 2, 4, 6 weeks. 5. In the production of CTX, TGF-${\beta}$, BMP-2 in the serum, experimental group showed increased effect. but no significant effect. 6. In the production of insulin in the serum. JGH 200, 400 mg/kg experimental group showed significant decrease effect at 2, 4, 6 weeks. 7. In the production of ALP in the serum. JGH 200 mg/kg experimental group showed significant increased effect at 2, 4, 6 weeks. JGH 400 mg/kg experimental group showed significant increased effect at 4, 6 weeks. 8. In the change of X-ray, the experimental group showed better healing effects on skull fractured rats than control group. Conclusions From above results, JGH showed healing effect on Anti-oxidation, Anti-inflammatory in RAW 264.7 Cells, factors related with bone metabolism in the serum of skull fractured rat and x-ray, which is expected to be applied in clinics.

• Archives of Pharmacal Research
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• v.19 no.3
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• pp.235-239
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• 1996

Six, heretofore undescribed, $5^I-Methyl-5^I-(5-Substituted uracil-1-ylmethyl)-2^I-oxo-3^I-methylenetetrahydrofurans(F, Cl, Br, l, CH_3, H)(6a-f)$were synthesized and evaluated against three cell lines (FM-3A, P-388 and U-937). For the preparation of .alpha.-methylene-.gamma.-butyrolactone bearing 5-substituted uracils (6a-f), the effcient Reformatsky type reaction was employed which involves the treatment of ethyl .alpha.(bromomethyl) acrylate and zinc with the respective 5-substituted uracil-1-ylacetones (5a-f). The acetone derivatives (5a-f) were directly obtained by the respective alkylation reaction of 5-substituted uracils with chloroacetone in the presence of $K_{2}$$CO_{3}$(or NaH). These lactone compounds 6a-f exhibited moderate to significant activity in all of the three cell lines, and 6b, 6c and 6e showed significant antitumor activities (inhibitory concentrations ($IC_{50}$) ranged from 1.3-3.8 .mu.g/ml.

• Food Science and Biotechnology
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• v.17 no.5
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• pp.947-952
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• 2008

The unripe fruit of Momordica charantia (MC) has been shown to possess antidiabetic activity. However, the mechanism of its antidiabetic action has not been fully understood. In this study, the effects of the aqueous ethanolic extract of MC (AEE-MC) were evaluated on the apoptosis in pancreatic $\beta$-cells treated with a combination of the cytokines, interleukin (IL)-$1{\beta}$, tumor necrosis factor (TNF)-$\alpha$, and interferon (IFN)-$\gamma$. In MIN6N8 cells, the inhibitory effect of AEE-MC was significantly observed at 2 to 50 ${\mu}g/mL$: a 26.2 to 55.6% decrease of cytoplasmic DNA fragments quantified by an immunoassay. The molecular mechanisms, by which AEE-MC inhibited $\beta$-cell apoptosis, appeared to involve the inhibition on the expression of p21, Bax, and Bad, the up-regulation of Bcl-2 and Bcl-$X_L$, and the inhibition on the cleavage of caspase-9, -7, and -3 and poly (ADP-ribose) polymerase. This study suggests that MC may inhibit cytokine-induced apoptosis in $\beta$-cells and, thus, may contribute via this action to the antidiabetic influence in diabetes.