• Biomolecules & Therapeutics
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• v.28 no.4
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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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• v.47 no.2
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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.

• Journal of Veterinary Clinics
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• v.18 no.3
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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.

• Korean Journal of Medicinal Crop Science
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• v.23 no.5
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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.

• Journal of Life Science
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• v.20 no.1
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• pp.90-96
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• 2010

Menopause increases the onset of hypertension and heart disease. Whereas it increases the blood LDL-cholesterol, triglyceride and total-cholesterol levels, the HDL-cholesterol concentration is reduced. Accordingly, we examined the effect of internal organs of Todarodes pacificus (IOT) on improvement in blood flow ability and changes in serum lipid content by using ovariectomized rats. For this study, the following four groups of 9-week-old Sprague-Dawley strain female rats were evaluated over 6 weeks: normal rats (SHAM), ovariectomized rats (CON) and ovariectomized rats that were treated with IOT extracts. Ovary removal promoted platelet aggregability. However, IOT administration in the CON group after ovary excision resulted in a hinderance of coherence. The blood vessel passing time of ovariectomized rats was slower than the SHAM group. But the blood flow ability, which was slowed down for ovary removal, was improved by IOT administration. Serum triglyceride levels were significantly reduced by IOT administration. Moreover, blood HDL-cholesterol levels were reduced by ovary removal. However, IOT administration after ovary excision significantly increase HDL-cholesterol levels. The biological activity of IOT could be confirmed from these results. Moreover, IOT can be used in the development of functional foods which are meant to improve blood circulation and anti-platelet aggregation function. According to these results, we could know that IOT improved blood flow and anti-platelet aggregation. Therefore, it is expected that IOT can be used for the development of functional foods.

• Food Science and Preservation
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• v.24 no.5
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• pp.658-665
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• 2017

The current study was performed to investigate the changes of bio-activities of Salicornia europaea (SE) depending on the different dry methods. The ethanol extracts were prepared from the freeze-drying SE (FD), hot-air drying SE (HD), and shade drying SE (SD). Their anti-oxidant and anti-thrombosis activities were compared. The yields of ethanol extraction in FD, HD, and SD were 14.4, 13.2 and 11.9%, respectively. The highest contents of total polyphenol (4.6 mg/g) and total sugar (23.4 mg/g) were shown in FD, whereas, the highest content of reducing sugar (14.6 mg/g) was observed in HD. In anti-oxidation activity assay, the FD and HD showed similar radical scavenging activities and reducing power. However, in SD, nitrite scavenging activity and reducing power were severely decreased. In anti-coagulation activity assay, the thrombin time (TT), prothrombin time (PT) and activated partial thromboplastin time (aPTT) of FD, HD and SD did not show significant changes at 5 mg/mL concentration. But the HD at 7 mg/mL had strong inhibitions against thrombin and blood coagulation factors. The platelet aggregation and hemolysis activities were not affected by dry methods. Our results suggest that both FD and HD are effective to maintain the functional ingredient of SE, and HD is economic and efficient dry process for production of functional food.

• Journal of Physiology & Pathology in Korean Medicine
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• v.20 no.6
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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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• v.13 no.3
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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, ${\beta}-sitosterol$.

• Journal of Physiology & Pathology in Korean Medicine
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• v.18 no.3
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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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• v.51 no.3
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• pp.183-187
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• 2008

Alkyl thiosulfi(o)nates, analogs of allyl-2-propene-1-thiosulfinate isolated from Allium sativum and having antibacterial activity, were chemically synthesized and their biological activities were investigated. Alkyl thiosulfinates were prepared by oxidation of corresponding disulfides with organic peroxy acid, while alkyl thiosulfonates could be obtained by oxidation of the alkyl thiosulfinates using sodium periodate. All synthetic thiosulfi(o)nates showed antibacterial activity against Staphylococcus aureus B33 and antifungal activity against Candida utilis ATCC42416. Further more synthetic alkyl thiosulfonates displayed antioxidant activity and have also prevention effect of platelet aggregation induced by collagen in rat.