• Biomolecules & Therapeutics
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• 제27권3호
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• pp.311-317
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• 2019

Mast cells are the most prominent effector cells of Type 1 hypersensitivity immune responses. CYC116 [4-(2-amino-4-methyl-1,3-thiazol-5-yl)-N-[4-(morpholin-4-yl)phenyl] pyrimidin-2-amine] is under development to be used as an anti-cancer drug, but the inhibitory effects of CYC116 on the activation of mast cells and related allergy diseases have not reported as of yet. In this study, we demonstrated, for the first time, that CYC116 inhibited the degranulation of mast cells by antigen stimulation ($IC_{50}$, ${\sim}1.42{\mu}M$). CYC116 also inhibited the secretion of pro-inflammatory cytokines including TNF-${\alpha}$ ($IC_{50}$, ${\sim}1.10{\mu}M$), and IL-6 ($IC_{50}$, ${\sim}1.24{\mu}M$). CYC116 inhibited the mast cell-mediated allergic responses, passive cutaneous anaphylaxis (ED50, ~22.5 mg/kg), and passive systemic anaphylaxis in a dose-dependent manner in laboratory experiments performed on mice. Specifically, CYC116 inhibited the activity of Fyn in mast cells and inhibited the activation of Syk and Syk-dependent signaling proteins including LAT, $PLC{\gamma}$, Akt, and MAP kinases. Our results suggest that CYC116 could be used as an alternative therapeutic medication for mast cell-mediated allergic disorders, such as atopic dermatitis and allergic rhinitis.

• 대한본초학회지
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• 제29권1호
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• pp.53-60
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• 2014

Objectives : Bojungikgitang (BJT), the Oriental medical prescription has been traditionally used about improvement of immune response and infective disease at Asian nation. In this study, we has compared about the anti-inflammatory and antioxidative effects on BJT of three countries including Korea (Korean Traditional Medicine, KTM), China (Traditional Chinese Medicine, CTM) and Japan (Japanese Traditional Medicine, JTM). Methods : We has basically using LPS-stimulated RAW 264.7 cells. The expression of these inflammatory mediators has measured using enzyme-linked immunosorbent assay (ELISA) and reverse transcription polymerase chain reaction (RT-PCR). Also, free radical scavenging assay has tested for anti-oxidative activity as well as the contents of total flavonoid and polyphenol. Results : As a result, we were founded the inhibitory effects of BJT (KTM, CTM, JTM) on LPS-induced production of NO, TNF-${\alpha}$ and IL-6 as well as the anti-oxidative activities. Especially the KTM was most effective in anti-inflammatory and anti-oxidative activities. Conclusions : These results indicate that BJT (KTM, CTM, JTM) has a good anti- inflammatory and anti-oxidative effects. But, there were degree of effects on between pharmacopoeia of the countries. Thus, further study is required that find appropriate methods for extracting as well as establish of standardized processes in order to improve the quality of BJT (KTM, CTM, JTM) as an anti-inflammatory and anti-oxidative agent for treatment of inflammatory diseases.

• 생약학회지
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• 제43권4호
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• pp.328-337
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• 2012

In order to investigate anti-inflammatory, anti-allergic and anti-obesity activities of Samchulkunbi-tang (SCT; Shen zhu jian pi-tang) water and 70% ethanol (EtOH) extracts, in vitro inhibitory activities against nitric oxide (NO), prostaglandin $E_2$ $PGE_2$), interleukin (IL)-6 and tumor necrosis factor (TNF)-${\alpha}$ production in lipopolysaccharide-stimulated RAW 264.7 cells, and macrophage-derived chemokine (MDC/CCL22) and regulated on activation of normal T-cell-expressed and -secreted (RANTES/CCL5) production in TNF-${\alpha}$/interferon-${\gamma}$-stimulated HaCaT and BEAS-2B cells as well as glycerol-3-phosphate dehydrogenase (GPDH) activity and leptin production in 3T3-L1 cells were determined. A HPLC was used for quantification of the seven marker components (albiflorin, paeoniflorin, liquiritin, naringin, hesperidin, poncirin and glycyrrhizin) of SCT water and 70% EtOH extracts. SCT showed inhibitory effects against MDC and RANTES production in HaCaT cells, as well as RANTES production in BEAS-2B cells. In addition, SCT reduced not only NO, $PGE_2$, IL-6 and TNF-${\alpha}$ production in RAW 264.7 cells, but also GPDH activity and leptin production in 3T3-L1 cells. Furthermore, the biological activities and the contents of six compounds (except paeoniflorin) were higher in 70% EtOH extract than water extract. These results suggest that SCT has anti-inflammatory, anti-allergic and anti-obesity activities. These efficacies of 70% EtOH extract are relatively higher than that of water extract.

• 치위생과학회지
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• 제12권2호
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• pp.155-162
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• 2012

본 연구는 소목(Caesalpinia sappan L.)의 6가지 유기용매 분획물 중 IP-3의 항균활성을 및 부착능을 측정하고 다음과 같은 결과를 얻었다. 1. Methanol에 의해 분리된 소목의 항균 물질 수율은 총 4.8%로 나타났으며, 여러 분획물 가운데 EtOAc 분획물(IP-3)에서 3.94%로 가장 높은 수율을 보였다. 2. 소목의 EtOAc 분획물에서 최종 정제된 활성물질은 UV 288.3 nm에서 최대 흡수피크를 나타내었으며, NMR spectrum을 통해 brazilin(($C_{16}H_{14}O_5$)으로 확인되었다. 3. S. mutans에 대한 소목의 EtOAc 분획물의 항균 활성은 최소억제농도(MIC) 3.1 mg/ml에서 균의 생장을 억제하였다. 4. S. mutans 부착억제효과는 하이드록시아파타이트(HA)를 S. mutans와 24 시간 동안 함께 배양한 대조군은 균 부착률이 높게 관찰되었으나, 소목의 EtOAc 분획물을 처리한 군에서는 HA에 S. mutans의 부착이 매우 적게 나타났다. 이상의 결과를 통해, 소목에서 추출된 EtOAc 분획에 존재하는 brazilin이 구강 내 우식원성세균에 강한 항균력을 가지고 있는 것으로 판단되며, 특히 S. mutans의 부착 억제능이 확인되어 우식원성 균주에 대한 생약치료제로 활용이 가능할 것으로 사료된다.

• 한국수산과학회지
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• 제42권5호
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• pp.434-441
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• 2009

This study was conducted to compare the biological activities of 7 melania snails from the family Pleuroceridae (Semisulcospira coreana, Koreanomelania nodifila, Semisulcospira forticosta, Koreoleptoxis globus ovalis, Semisulcospira libertina, Semisulcospira tegulata and Semisulcospira gottschei) in Korea. Among the 7 species, S. coreana, Korean. nodifila, S. forticosta and S. gottschei showed over 80% cytotoxicities on three cancer cell lines (SNU-1, A549 and Hep 3B) compared to the non-treatment, whereas S. libertina and S. tegulata showed almost no growth inhibition activities on the same cancer cell lines. In relation to ACE inhibition activity, only S. coreana, Korean. nodifila, and S. forticosta showed over 60% ACE inhibition activities, whereas other melania snails exhibited inhibition activities of lower than 25%. DPPH radical scavenging activities were also determined, and used to categories melania snails into three groups based on Duncan's multiple range test at P<0.05. The amount of TNF-${\alpha}$ produced by in vitro mouse peritoneal macrophage was determined according to bioactivity on L-929 cells. Three melania snails, S. coreana, Korean. nodifila and S. gottschei, exhibited 95.2%, 89.7% and 93.7% cell death(%) on L-929 cells, respectively. Glucose-6-phosphate dehydrogenase inhibitory activity was also obtained in the extract of S. coreana (31.9%) and Korean. nodifila (28.1%), showing that these extracts can be used as supplemental dietary health foods. In conclusion, we believe that the extracts of melania snails should be given due consideration in functional health food development.

• 한국약용작물학회지
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• 제12권3호
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• pp.243-248
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• 2004

인간 면역 세포 중 하나인 T세포에 대한 각 시료의 생육촉진 활성은 시료의 1.0 g/l에서 기준물질로 사용한 유향열매의 정유 성분이 T세포의 생육촉진 활성 측정에서 가장 좋은 활성을 나타내었으며, 노간주나무의 열매의 정유성분이 줄기 부분의 정유 성분보다 높은 생육 촉진 활성을 보였다. T 세포의 각 cell 당 $TNF-{\alpha}$의 분비량을 살펴보면 모든 시료의 정유 성분들이 배양 2일째 최대분비량을 나타내었고, IL-6의 경우는 모든 시료들이 배양 시간 의존적으로 증가하는 경향을 나타내었다. 유방암 세포인 MCF-7에 대한 각 시료의 생육 억제 활성은 각 정유 성분에 대하여 농도 의존적인 경향을 나타내었으며, 가장 좋은 활성을 나타낸 시료는 노간주나무 열매의 정유 성분으로 약 84%의 높은 생육 억제 활성을 나타내었으며, 유향 열매와 노간주나무 줄기의 정유 성분들도 약 80%에 가까운 높은 생육 억제 활성을 나타내었다. 간암 세포인 Hep3B에 대한 각 정유 성분들의 암세포 생육 억제 활성도 유방암 세포와 같이 각 정유 성분에 대하여 농도 의존적인 경향을 나타내었으며, 유향 열매의 정유 성분이 약 83%의 높은 생육 억제 활성을 나타내어 가장 좋은 활성을 나타내었다. 항암 및 면역기능의 역할에 대한 분자수준에서의 검증을 위해 HL-60 세포의 분화도를 살펴본 결과, 배양 시간 의존적으로 분화도가 증가하는 경향을 나타내었으며, 유향열매의 정유 성분이 Control 군에 비하여 1.38배의 증진활성을 나타내어 가장 높은 분화도를 나타내었으며, 노간주 열매의 정유 성분이 줄기의 정유 성분에 비하여 높은 분화도를 나타내었다.

• 대한본초학회지
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• 제30권4호
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• pp.81-88
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• 2015

Objectives : The aim of present study was to evaluate the beneficial effect of Scutellariae Radix (SR) and Scutellariae Radix EtOH-heated at 200℃ (SR200) using lipopolysaccharide (LPS) treated intestine of mice.Methods : Extract of SR and SR200 were orally administrated. Their effects were compared with vehicletreated LPS and normal groups. Subsequently, we measured reactive oxygen species (ROS) and nitric oxide in the serum and western blotting in the intestine.Results : The average weight in LPS treated (Vehicle) group was lowered significantly compare to that in non-treated normal group and this weight loss in the vehicle group was effectively prevented by the administration of SR and SR200 respectively. The increased oxidative stress biomarker levels such as reactive oxygen species (ROS) and nitric oxide (NO) in the serum was markedly decreased by treated with SR200. The decreased levels of superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx) induced by LPS injection were significantly restored by both SR and SR200 treatment. Moreover, increased inflammatory mediators and cytokines such as inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in the LPS treated vehicle mice were significantly decreased through down-regulation c-JUN through reduction of oxidative stress.Conclusions : SR and SR200 could have benefit effect through down-regulation of abnormal oxidative stress in LPS induced intestine injury mice. Moreover, The anti-inflammatory activity of SR200 extract was better than SR extract in the LPS induced intestine injury mice.

• 한국자원식물학회지
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• 제28권5호
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• pp.591-599
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• 2015

본 연구는 까마귀쪽나무 열매 70% 주정에탄올 추출물을 가지고 제작된 인체적용시험시료(LJTM)의 항염증 및 골관절염 biomarker의 변화를 통한 관절건강 기능성식품을 개발하기 위하여 인체적용시험시료를 제작한 후 이에 대한 유효성분의 함량을 평가하고, 인체적용시험전에 그 효력이 유지됨을 확인하기 위하여 수행되었다. 본 연구에 사용된 시료 LJTM은 NO생성이 억제되는 농도에서 세포독성이 관찰되지 않았으며, TNF-α와 IL-6 생성이 농도 의존적으로 억제되고 PGE₂를 억제하였다. 또한 동물시험에서 골관절염의 biomarker인 MMP-2, 3, 7, 9와 TIMP-1, 2에 대한 mRNA 발현이 농도 의존적으로 억제되었으며, 중추신경계 및 말초신경계에 의한 통증을 억제하는 것으로 평가되었다. 따라서 까마귀쪽나무 열매 70% 추출물이 함유된 인체적용시험시료(LJTM)는 골관절염과 진통억제에 우수한 효과가 있는 것으로 확인되었다.

• 생명과학회지
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• 제26권6호
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• pp.640-645
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• 2016

본 연구에서는 녹차 유래 polyphenol 중의 하나인 epigallocatechine gallate (EGCG)를 이용한 신경염증 억제 효과를 확인하였다. LPS로 유도된 미세아교세포의 활성화로 분비되는 nitric oxide (NO)와 pro-inflammatory cytokine을 포함하여 iNOS, TNF-a와 IL-1b 유전자의 발현과 LPS 수용체인 TLR-4의 활성에 미치는 EGCG의 억제 효능을 확인하였다. Latex beads를 이용한 phagocytotic activity를 확인한 결과 LPS로 유도된 미세아교세포 활성에 의한 식균활성이 EGCG에 의해 억제되는 것을 볼 수 있었다. 뿐만 아니라, BV-2 미세아교세포 조건배지를 이용하여 도파민성 신경세포 SN4741의 세포 사멸확인에서도 EGCG에 의한 보호 효과를 확인하였다. 본 연구 결과는 녹차 유래 polyphenol인 EGCG의 신경염증 반응억제효능과 신경퇴행성 질환 제어 가능성을 확인하였다. 본 연구의 결과는 녹차 유래 polyphenol인 EGCG의 신경염증 반응과 그로 인한 신경 퇴행성 질환 제어 가능성을 제시하였다.

• 대한본초학회지
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• 제32권2호
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• pp.77-85
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• 2017

Objectives : This study aimed to investigate the unknown mechanisms behind the anti- inflammatory activity of Hyeonto-dan(HT) 70% ethanol extract on LPS-stimulated RAW 264.7 cells. Methods : Cells were treated with Hyeonto-dan 1 h prior to addition of 200 ng/mL of LPS. Cell viability was measured by the MTS assay. Nitric oxide levels were determined by the Griess assay. $PGE_2$ were measured using EIA kit. Pro-inflammatory cytokine production was measured by the enzyme-linked immunosorbent assay (ELISA). The expression of COX-2, iNOS, and MAPKs was investigated by Western blot, qRT-PCR. $NF-{\kappa}B$/p65 localization and interaction of the TLR-4 receptor with LPS was examined by immunofluorescence assays. Results : Hyeonto-dan had no cytotoxicity at the measured concentration. Hyeonto-dan inhibited NO production and pro-inflammatory cytokines such as IL-6, $TNF-{\alpha}$, and PGE2 as well as the protein and mRNA expression of iNOS and COX-2. Moreover, Hyeonto-dan inhibited the interaction between LPS and TLR-4 in murine macrophages. It suppressed phosphorylation of extracellular signal-regulated kinase (ERK 1/2), c-jun N-terminal kinase (JNK 1/2) and p38. Finally, it inhibited translocation of $NF-{\kappa}B$ in response to competitive LPS. Conclusions : Based on the results of this study, Hyeonto-dan inhibited the binding of TLR-4 receptor to LPS and inhibited the phosphorylation of extracellular signaling pathway MAPKs. These inhibitory effects are thought that the amount of $NF-{\kappa}B$ delivered to the nucleus was decreased and the inflammatory reaction was prevented by decreasing the production of LPS-induced $PGE_2$, NO, IL-6 and $TNF-{\alpha}$.