• Biomolecules & Therapeutics
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• 제28권4호
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• pp.337-343
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• 2020

Activation of osteoclast and inactivation of osteoblast result in loss of bone mass with bone resorption, leading to the pathological progression of osteoporosis. The receptor activator of NF-κB ligand (RANKL) is a member of the TNF superfamily, and is a key mediator of osteoclast differentiation. A flavanone glycoside isolated from the fruit of Poncirus trifoliata, poncirin has anti-allergic, hypocholesterolemic, anti-inflammatory and anti-platelet activities. The present study investigates the effect of poncirin on osteoclast differentiation of RANKL-stimulated RAW264.7 cells. We observed reduced formation of RANKL-stimulated TRAP-positive multinucleated cells (a morphological feature of osteoclasts) after poncirin exposure. Real-time qPCR analysis showed suppression of the RANKL-mediated induction of key osteoclastogenic molecules such as NFATc1, TRAP, c-Fos, MMP9 and cathepsin K after poncirin treatment. Poncirin also inhibited the RANKL-mediated activation of NF-κB and, notably, JNK, without changes in ERK and p38 expression in RAW264.7 cells. Furthermore, we assessed the in vivo efficacy of poncirin in the lipopolysaccharide (LPS)-induced bone erosion model. Evaluating the micro-CT of femurs revealed that bone erosion in poncirin treated mice was markedly attenuated. Our results indicate that poncirin exerts anti-osteoclastic effects in vitro and in vivo by suppressing osteoclast differentiation. We believe that poncirin is a promising candidate for inflammatory bone loss therapeutics.

• Journal of Ginseng Research
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• 제47권2호
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• pp.237-245
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• 2023

Background: Ginsenoside Rg2 (Rg2) has a variety of pharmacological activities and provides benefits during inflammation, cancer, and other diseases. However, there are no reports about the relationship between Rg2 and atherosclerosis. Methods: We used 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) to detect the cell viability of Rg2 in vascular smooth muscle cells (VSMCs) and human umbilical vein endothelial cells (HUVECs). The expression of inflammatory factors in HUVECs and the expression of phenotypic transformation-related marker in VSMCs were detected at mRNA levels. Western blot method was used to detect the expression of inflammation pathways and the expression of phenotypic transformation at the protein levels. The rat carotid balloon injury model was performed to explore the effect of Rg2 on inflammation and phenotypic transformation in vivo. Results: Rg2 decreased the expression of inflammatory factors induced by lipopolysaccharide in HUVECs-without affecting cell viability. These events depend on the blocking regulation of NF-κB and p-ERK signaling pathway. In VSMCs, Rg2 can inhibit the proliferation, migration, and phenotypic transformation of VSMCs induced by platelet derived growth factor-BB (PDGF-BB)-which may contribute to its anti-atherosclerotic role. In rats with carotid balloon injury, Rg2 can reduce intimal proliferation after injury, regulate the inflammatory pathway to reduce inflammatory response, and also suppress the phenotypic transformation of VSMCs. Conclusion: These results suggest that Rg2 can exert its anti-atherosclerotic effect at the cellular level and animal level, which provides a more sufficient basis for ginseng as a functional dietary regulator.

• 한국임상수의학회지
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• 제18권3호
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• pp.189-194
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• 2001

The aim of this study was to investigate the anti-stress effect of xylazine on rope-restrained stress using cattle. For this study we utilized biotelemetrical methods such as body temperature, heart rate and blood analysis. Twelve cows were divided into two groups as an only rope restrained group (control) and as rope-restrain+xylazine (0.05 mg/kg, IV) treated group (experimental group). Each group was under experimental environments for 24 hours before initiation of stress. The body temperature and the heart rate were checked every 5 minutes for 24 hours in two groups. We found that the core body temperature in the experimental group was higher than that of control group. We also found hat the heart rate in experimental group was significantly lower (p<0.05) than that of control group for 90 minutes after 30 minutes of rope-restrained stress. The level of the plasma cortisol of experimental group was significantly lower (p<0.05) than that of control group for 90 minutes after the rope-restrained stress was given. We performed the blood analysis to know whether rope-restrained stress affects RBC, WBC, hemoglobin, hematocrit, and platelet values or not but we could not find the significant difference between control and experimental groups. These results suggest that the administration of xylazine might partially help to reduce rope-restrained stress in cattle.

• 한국약용작물학회지
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• 제23권5호
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• pp.385-394
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• 2015

Background : Dibenzocyclooctadiene lignans are secondary metabolites present abundantly in the fruits belonging to the genus Schisandra. According to previous studies, Schisandra lignans exhibit anti-inflammatory, anti-cancer and anti-diabetic properties, as well as an inhibitory effect on platelet aggregation. Therefore, establishing the Korean "Omija" (Schisandra chinensis) as a lignan-rich source, in addition to identifying and quantifying the lignans, is extremely valuable. Methods and Results : Dibenzocyclooctadiene lignans were analyzed with liquid chromatography using diode array detection/mass spectrometry, from methanol extracts subsequently identified by a constructed chemical library of 50 lignans. A total of 27 components of lignan including gomisin S were identified, of which schisandrin, gomisin A, gomisin N, deoxyschisandrin, ${\gamma}$-schisandrin, and schisandrin C were identified as the major components in the Korean Omija, Schisandra chinensis. These compounds were divided into two groups, S-biphenyl and R-biphenyl based on the configurations of the stereoisomers structures with contents of 661.7 and 1350.1mg per 100 g dry weight, respectively. The total lignan content averaged 2011.4mg per 100 g dry weight, of which schisandrin and gomisin N comprised the majority (771.8 and 420.5mg per 100 g dry weight respectively). Conclusions : Lignans which are present in high quantities in the ripe fruit of Schisandra chinensis are important functional compounds that play a major role in the prevention and treatment of human diseases.

• 생명과학회지
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• 제20권1호
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• pp.90-96
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• 2010

폐경과 더불어 시작되는 폐경기의 에스트로겐 변화로 발생되는 건강 문제 중 심혈관계 질환이 문제점으로 대두되고 있다. 따라서 본 연구는 갱년기 장애 시 유발되는 체내 지질 함량 증가에 있어서 오징어 부산물의 에탄올 추출물이 미치는 영향을 검토하기 위해 인위적 폐경을 유발시킬 수 있는 난소 절제 암컷 흰쥐에서 오징어 부산물의 혈행개선, 항혈소판 응집능 및 혈중 지질 함량 변화에 미치는 영향을 검토하였다. 그 결과 갱년기를 유도한 CON군은 난소절제 시 에스트로겐 결핍으로 bone turnover이 증가되어 SHAM군에 비해 혈액 중의 ALP 활성이 증가되었으나, 오징어 부산물 투여에 의해 그 활성이 유의적으로 감소하였다. 갱년기 유도로 인한 혈장 내 혈액응고인자(coagulation factors)의 지나친 활성화 및 혈소판 응집 촉진으로 CON군의 모세관 통과 시간은 지연되었으나, 오징어 부산물의 에탄올 추출물 투여로 인해 혈류의 속도가 향상 되었다. 또한 난소를 절제한 CON군의 경우 SHAM군에 비해 혈소판이 빠르게 응집되는 결과가 나타났으며, 오징어 부산물의 에탄올 추출물을 투여한 군은 CON군에 비해 혈소판 응집이 억제되는 것으로 나타났다. 난소 절제하여 갱년기 장애를 유도한 흰쥐에 오징어 부산물의 에탄올 추출물을 투여하였을 때, 혈 중 중성 지방 함량이 낮아지고 HDL-cholesterol 함량이 높아지는 결과로 보아 오징어 부산물의 에탄올 추출물 투여가 난소 절제에 의해 소실된 estrogen의 지질대사 불균형에 유익한 영향을 주어 심혈관계 질환 개선에 영향을 준 것으로 사료된다. 또한 이것은 오징어 부산물 중의 $\omega$-3 지방산 및 미지의 펩타이드류 등이 복합적으로 작용하여 난소 절제한 흰쥐의 지질대사에 유익한 효과를 준 것으로 추측되며, 이에 대한 구체적인 내용에 대해서는 앞으로 더 깊은 연구가 필요할 것으로 생각되어 진다. 이상의 결과로부터 갱년기 장애 시 유발 되는 지질 대사 이상으로 오는 심혈관계 질환에 오징어 부산물의 에탄올 추출물이 유익한 결과를 줄 것으로 사료된다.

• 한국식품저장유통학회지
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• 제24권5호
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• pp.658-665
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• 2017

식용 및 약용으로 이용되고 있는 함초를 이용한 고부가가치 제품개발을 위해, 동결건조, 열풍건조, 음건한 함초의 ethanol추출물을 조제하여 건조방법에 따른 성분 변화, 항산화 및 항혈전 활성 변화를 평가하였다. 동결건조, 열풍건조 및 음건 시료의 ethanol 추출효율은 각각 14.4, 13.2, 11.9%를 나타내어 동결건조시 수율이 음건에 비해 1.2배 높았다. 성분 분석결과, 동결건조 시료의 total polyphenol 함량은 4.6 mg/g으로 열풍건조 및 음건 시료보다 높았으며, total flavonoid 함량은 건조방법과 무관하게 4.2-4.4 mg/g을 나타내었다. 반면 총당 함량은 동결건조에서 가장 높게 나타났으며, 음건 시료는 동결건조 시료에 비해 53% 수준을 나타내었다. 환원당의 경우 열풍건조시료에서 가장 높게 나타났으며, 음건시료에 비해 3.3배 높게 나타났다. 항산화 활성 평가결과, 동결건조, 열풍건조 시료에서는 유사한 항산화 활성이 나타났으나, 음건 시료의 경우 환원력과 nitrite 소거능은 유의적으로 감소되었다. 항응고 활성의 경우, 모든 건조 시료에서 농도 의존적인 우수한 항응고 활성을 나타내었으며, 특히 열풍건조 시료에서 강력한 TT 및 aPTT 연장 활성을 나타내었다. 인간 혈소판에 대한 응집저해 활성과 적혈구 용혈활성은 건조방법에 따른 유의적인 변화는 나타나지 않았다. 본 연구결과는 함초의 유용 기능성 유지를 위해 열풍건조 및 동결건조가 필요하며, 특히 함초의 항혈전 활성을 이용하는 기능성 식품을 제조하고자 하는 경우 열풍건조를 이용하는 것이 경제적이면서 효과적임을 제시하고 있다.

• 동의생리병리학회지
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• 제20권6호
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• pp.1658-1663
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• 2006

Panax notoginseng (Buck) F.H chen. root (PNS) is used as a therapeutic agent to stop haemorrhages and a tonic to promote health in Korean and Chinses medicine. The pharmacokinetic profiles of the main PNS are still not accurately investigated. Our preliminary aim is to elucidate the pharmacokinetics features of the PNS in rats. Objective of this study is to determine whether PNS affects hepatic microvascular dysfunction elicited by gut ischemia and reperfusion (I/R), since gut I/R causes hepatic microvascular dysfunction, and to investigate the role of nitric oxide (NO). No has been found to be a modulator of the adhesive interactions between platelet and endothelial cells. Male Wistar rats were exposed to 30 min of gut ischemia followed by 60 min of reperfusion. Intravital microscopy was used to monitor the number of non-perfused sinusoids (NPS). In another set of experiments, PNS (1 g/kg pre day intragastrically) was administered to rats for 7 days. In some experiments, dexamethasone (ST) (2 mg/kg per day intravenously) was administered. In control rats, gut I/R elicited increases in the number of NPS, and plasma TNF-${\alpha}$ and ALT activities, and these changes were mitigated by the pretreatment with PNS. Pretreatment with an No synthase inhibitor diminished the protective effects of PNS on the increase in NPS and plasma TNF-${\alpha}$ levels, but not its effect on the increase in plasma ALT activities. Pretreatment with PNS increased plasma nitrite/nitrate levels. The responses caused by gut I/R were attenuated by the pretreatment with ST. Pretreatment with an NO synthase inhibitor did not affect the effect of ST. These results suggest that PNS attenuates the gut I/R-induced hepatic microvascular dysfunction and inflammatory responses such as TNF-${\alpha}$ production in the early phase via enhancement of NO production, and sequential hepatocellular damage via its anti-inflammatory effect like corticosteroid effect.

• Natural Product Sciences
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• 제13권3호
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• pp.220-224
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• 2007

To search of more selective vasculogenic relaxation activity, the antioxidant activity of silkworm male pupae was determined by measuring its radical scavenging effect on 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radicals, and anticoagulant activity of them was measured clotting time in both activated partial thromboplastin time (aPTT). Because, most of cGMP-enhancing agent such as, sildenafil, promotes thrombin-induced platelet aggregation, developed unexplained thrombic conditions including heart attack. To search more suitable and safe drug for vasculogenic relaxation, we purified silkworm pupae male extract. The ethyl acetate extract of silkworm male pupae showed strong scavenging activity in both DPPH and aPTT anticoagulant activity. The antioxidant activity potential of the individual fraction was in order of ethyl acetate > n-butanol > chloroform > n-hexane. The ethyl acetate soluble fraction exhibiting strong anti-oxidant and anticoagulant activity was further purified by repeated silica gel and Sephadex LH-20 column chromatography. Cholesterol was isolated as one of the active principles from ethyl acetate fraction, together with, minor portion, ${\beta}-sitosterol$.

• 동의생리병리학회지
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• 제18권3호
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• pp.857-862
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• 2004

The purpose of this research was to investigate the effects of supercritical fluid extract of Kamichungbieum (SFE) on allergic reaction. SFE (500 mg/kg) inhibited the systemic anaphylaxis induced by compound 48/80 or platelet activating factor and inhibited the passive cutaneous anaphylaxis (PCA) induced by anti-dinitrophenyl (DNP)-lgE and DNP-human serum albumin (HSA) in vivo. Also, SFE inhibited the SRSC-induced delayed type hypersensitivity and inhibited the hind paw edema induced by histamine. In addition, SFE inhibited the permeability of evans blue induced by acetic acid and inhibited the writhing syndrome induced by acetic acid. These results indicate that SFE may be useful for the prevention and treatment of allergy related disease.

• Applied Biological Chemistry
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• 제51권3호
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• pp.183-187
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• 2008

본 연구에서는 마늘 중의 항미생물 작용을 가지고 있는 allyl-2-propenyl-1-thiosulfinate의 유사체들인 alkyl thiosulfinate 및 이의 산화물인 thiosulfonate화합물들을 합성하고 이들의 생물 활성을 검사하였다. Alkylsulfinate는 이황화 화합물(disulfide)를 유기 과산화산으로, 또 alkyl thiosulfonate는 thiosulfinite를 sodium periodate로 산화시켜 합성하였다. 합성한 모든 alkylthiosulfinate 및 alkyl thiosulfonate들은 Staphylococcus aureus B33에 대해서는 항세균성을, Candida utilis ATCC42416에 대해서는 항곰팡이성을 나타내었다. 나아가 이들 화합물들은 항산화성과 항응고 활성도 나타내었다.