• 생약학회지
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• 제52권4호
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• pp.257-266
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• 2021

This study evaluated several in vitro activities including the preliminary assessment of the anti-cancer, anti-inflammatory, and anti-diabetic effects of tree sprout extracts. Chlorogenic, caffeic, and p-coumaric acid contents in tree sprouts were analyzed using high-performance liquid chromatography and an ultraviolet detector. Among the studied tree sprout extracts, the ethanol (EtOH) extract of Rhus verniciflua exhibited the most potent anti-cancer effect by suppressing the cell viability of a human gastric adenocarcinoma cell line, with an IC₅₀ of 7.06 ㎍/mL. The EtOH extract of Morus alba (MAB) inhibited the secretion of nitric oxide (NO) at a concentration of 100 ㎍/mL, with an IC₅₀ of 83.44 ㎍/mL. Moreover, the EtOH extract of Securinega suffruticosa inhibited NO secretion with the lowest IC₅₀ of 54.42 ㎍/mL. The EtOH extract of Fraxinus mandschurica was the only extract with effective α-glucosidase inhibitory activity. The total content of chlorogenic, caffeic, and p-coumaric acids was the highest in MAB (14.63 mg/g ext.). In conclusion, the beneficial activities of the tree sprout extracts with high phenolic acid content were generally high. Our results provide a theoretical basis for the development of health-promoting supplements and functional foods.

• Journal of Microbiology and Biotechnology
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• 제25권7호
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• pp.1047-1055
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• 2015

For the search of a potent first-in-class compound to inactivate macrophages responsible for inflammatory responses, in the present study, we investigated the anti-nflammatory effects of YH-1118, a novel synthetic compound, in a lipopolysaccharide (LPS)-stimulated mouse macrophage cell line, Raw 264.7. YH-1118 inhibited LPS-induced nitric oxide (NO) production and inducible NO synthase (iNOS) expression at both the protein and mRNA levels. The suppression of LPS-induced iNOS expression by YH-1118 was mediated via nuclear factor kappa B (NF-κB), but not activator protein-1 (AP-1) transcription factor. This was supported by the finding that YH-1118 attenuated the phosphorylation of inhibitor of κBα (IκBα) and nuclear translocation and DNA binding activity of NF-κB. Through the mechanisms that YH-1118 inhibited the activation of IκB kinases (IKKs), upstream activators of NF-κB, or p38 MAPK, YH-1118 significantly suppressed LPS-induced production of pro-inflammatory cytokines, tumor necrosis factor-α, interleukin-1β (IL-1β), and IL-6 (p < 0.05). In conclusion, our results suggest that YH-1118 inhibits LPS-induced inflammatory responses by blocking IKK and NF-κB activation in macrophages, and may be a therapeutic candidate for the treatment of various inflammatory diseases.

• BMB Reports
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• 제51권10호
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• pp.538-543
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• 2018

Pancreatic beta cell destruction and dysfunction induced by cytokines is a major cause of type 1 diabetes. Paraoxonase 1 (PON1), an arylesterase with antioxidant activity, has been shown to play an important role in preventing the development of diabetes in transgenic mice. However, no studies have examined the anti-diabetic effect of PON1 delivered to beta cells using protein transduction. In this study, we expressed the cell-permeable PON1 fused with PEP-1 protein transduction domain (PEP-1-PON1) to investigate whether transduced PEP-1-PON1 protects beta cells against cytokine-induced cytotoxicity. PEP-1-PON1 was effectively delivered to INS-1 cells and prevented cytokine-induced cell destruction in a dose-dependent manner. Transduced PEP-1-PON1 significantly reduced the levels of reactive oxygen species (ROS) and nitric oxide (NO), DNA fragmentation, and expression of inflammatory mediators, endoplasmic reticulum (ER) stress proteins, and apoptosis-related proteins in cytokine-treated cells. Moreover, transduced PEP-1-PON1 restored the decrease in basal and glucose-stimulated insulin secretion induced by cytokines. These data indicate that PEP-1-PON1 protects beta cells from cytokine-induced cytotoxicity by alleviating oxidative/nitrosative stress, ER stress, and inflammation. Thus, PEP-1-mediated PON1 transduction might be an effective method to reduce the extent of destruction and dysfunction of pancreatic beta cells in autoimmune diabetes.

• Mycobiology
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• 제39권3호
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• pp.187-193
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• 2011

Botryosphaeran, a water-soluble exopolysaccharide of the ${\beta}-(1{\rightarrow}3;1{\rightarrow}6)$-D-glucan type that has been isolated from the culture medium of Botryosphaeria rhodina MAMB-05 grown in submerged fermentation using glucose as the sole carbon source, was previously demonstrated to be non-genotoxic in peripheral blood and bone marrow, and exhibited strong anticlastogenic activity. In the present study, the effects of botryosphaeran were investigated in streptozotocin-induced diabetic rats as well as in high-fat diet-fed hyperlipidemic Wistar rats. The plasma glucose level was reduced by 52% in the diabetic group of rats after administration of 12 mg botryosphaeran/kg body weight of the rats (b.w.)/day by gavage over 15 days. A reduction in the median ration intake was accompanied by an increase in the median body weight gain, as well as the efficiency of food conversion. These results demonstrate that botryosphaeran has protective effects by reducing the symptoms of cachexia in Diabetes mellitus. Botryosphaeran administered by gavage at a concentration of 12 mg botryosphaeran/kg b.w./day over 15 days also reduced the plasma levels of total cholesterol and low density lipoprotein-cholesterol by 18% and 27%, respectively, in hyperlipidemic rats. Based on these findings, we conclude that botryosphaeran possesses hypoglycemic and hypocholesterolemic properties in conditions of diabetes mellitus and hyperlipidemia, respectively, and may be used as an oral anti-diabetic agent.

• 동의생리병리학회지
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• 제22권6호
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• pp.1509-1517
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• 2008

The flowers and buds of Lonicera Flower (LF), are used in Korean herbal medicine for latent-heat-clearing, antipyretic, detoxicant and anti-inflammatory ailments. This plant is used worldwide for the treatment of many types of inflammatory disease including respiratory infections, diabetes mellitus, rheumatoid arthritis and play an important role in immune reaction. These pharmaceutical effects of LF looks like to be related to its antioxidant capacity and phytochemicals containing in LF. In this study, the antioxidant activity of extract from LF was studied in vitro methods by measuring the antioxidant activity by TEAC, measuring the scavenging effects on reactive oxygen species (ROS) [superoxide anion, hydroxyl radical] and on reactive nitrogen species (RNS) [nitric oxide and peroxynitrite] as well as measuring the inhibitory effect on $Cu^{2+}$ induced human LDL oxidation and the inhibitory effect on collagen induced platelet aggregation. The LF extracts were found to have a potent scavenging activity, as well as an inhibitory effect on LDL oxidation and on platelet aggregation. In conclusion, the LF extracts have anti-oxidative and anti-atherosclerotic effects in vitro system, which can be used for developing pharmaceutical drug against oxidative stress and atherosclerosis.

• 동의생리병리학회지
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• 제23권6호
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• pp.1320-1331
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• 2009

Oxidative stress and inflammation are important events in the development of chronic inflammatory diseases including arthritis, atherosclerosis, diabetes, hypertension. Cynomorium songaricum (CS) has been used as a traditional Korean herbal medicine, and it is currently used in traditional clinics to treat frequent urination, spermatorrhea, weakness of the sinews and constipation in the folk medicine. The aim of this study was to determine whether fractionated extracts of CS inhibit free radical generation such as DPPH radical, superoxide radical, nitric oxide and peroxynitrite, production of nitrite an index of NO, $PGE_2$, iNOS, COX-2 and pro-inflammatory cytokines in lipopolysaccharide (LPS)-treated RAW 264.7 macrophages. Cytotoxic activity of extracts on RAW 264.7 cells was measured using 5-(3-caroboxymeth-oxyphenyl)-2H-tetra-zolium inner salt (MTS) assay. Our results indicated that the most superior extract which scavenged DPPH radical, reactive oxygen species (ROS) and RNS was CS ethyl acetate extract (CSEA). Moreover, CSEA significantly inhibited the LPS-induced NO, $PGE_2$ production and iNOS, COX-2 expression accompanied by an attenuation of TNF-$\alpha$, IL-$1{\beta}$ and IL-6 formation in macrophages. Furthermore, CSEA treatment also blocked LPS-induced intracellular ROS production and the activation of NF-${\kappa}B$. These findings indicate that CSEA inhibits the production of pro-inflammatory mediators and cytokines via the suppression of ROS production and NF-${\kappa}B$ activation. Take together, these results indicate that CSEA has the potential for use as an natural anti-oxidant and an agent of anti-chronic inflammatory diseases.

• 생명과학회지
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• 제17권11호
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• pp.1571-1575
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• 2007

본 연구는 당뇨병으로 인한 산화적 스트레스에 대한 함박잎새버섯분말의 효과를 밝히기 위하여 SD계 흰쥐를 STZ로 당뇨를 유발하여 간 및 신장 조직에서 조사하였다. 또한 당뇨흰쥐에 함박잎새버섯분말 1-2% 첨가하여 6주간 식이하였다. 산화적 스트레스의 지표물질인 LPO를 비롯하여 유발원 XOD 활성도를 측정하였다. 또한 이에 따른 간조직 손상 확인을 위해 혈청 ALT와 AST 활성도를 측정하였다. 특히 함박잎새버섯분말의 항산화적 효능을 위해 이들 지표물질들과 더불어 항산화체계의 중요 요소인 GSH 농도와 GST 활성도를 당뇨군, 당뇨-잎새버섯분말투여군 그리고 정상군에서 측정하였다. 당뇨군은 정상군과 비교하여 LPO 농도를 비롯하여 XOD 활성도가 유의하게 높았다. 특히 이러한 결과로 추정되는 간 조직 손상이 정상군보다 유의하게 높은 ALT 및 AST 활성도가 혈청에서 확인되었다. 그러나 당뇨-잎새버섯분말투여군에서는 LPO 농도, XOD 활성도를 비롯하여 조직손상의 지표인 ALT 및 AST 활성도가 당뇨군보다 유의하게 감소하였다. 항산화물질인 GSH 농도는 당뇨군 및 당뇨-잎새버섯분말투여군 비교에서 유의한 차이가 없었으나 GST 활성도는 당뇨-잎새버섯분말투여군이 당뇨군보다 유의하게 높았다. 따라서 당뇨유발성 산화적 스트레스에 대한 잎새버섯분말의 효능은 GSH 농도 변화보다 GST 활성도를 증가시키고 또한 산화적 스트레스의 유발원인 XOD 활성도 감소의 유도를 통해 이루어지는 것으로 추정된다. 결론적으로 당뇨는 산화적 스트레스를 증가시키며 조직손상을 유발한다. 그러나 함박잎새버섯분말은 항산화물질 및 효소계의 활성도를 증가시켜 당뇨유발-산화적 스트레스 감소를 유도하여 조직 손상을 감소시키는 것이 확인되었다.

• 한국임상수의학회지
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• 제27권4호
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• pp.348-365
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• 2010

Artemisia capillaries THUNB is a perennial herb that belongs to the family compositae spp. and the most common plant among the various herbal folk remedies used in treatment of abdominal pain, hepatitis, chronic liver disease, jaundice and coughing in Korea. The object of this study is to observe the dosage-dependent anti-obestic effects of an aqueous extracts of dried aqueous extracts of stems of Artemisia capillaris Thunberg. [Artemisiae capillaris Herba, In-Jin in Korean, INJ] on 45%/Kcal high fat diet (HFD) supplied mice. 45%/Kcal rodent HFD are supplied to ICR mice from 1 week before initiation of INJ administration throughout the 12 weeks, and after the end of 12 weeks of 62.5, 125 and 250 mg/kg/day of INJ administration, the efficacy was divided into five categories 1) hypoglycemic, 2) hepato-protective, 3) nephroprotective, 4) hypolipemic, and 5) anti- obesity effects. The effects were compared to those of simvastatin (for hypolipemic activity), silymarin (for hepatoprotective and free radical scavenger effects) and metformin (for hypoglycemic and related anti-obesity effects). 7 animals per group (8 groups; total 56adapted mice on HFD were selected base on the body weight at 6 days after initiation of HFD supply) were used in this experiment. INJ and all three different reference drugs were directly suspended or dissolved in distilled water, and administered at a volume of 10 mL/kg, once a day for 84 days from 1 week after HFD supply. As results of 91 days of continuous HFD supply, mice showed marked obese states, hyperglycemia, hyperlipemia, liver damages and kidney damages. These mean the obesity, diabetes, diabetic hepatopathies, nephropathies and hyperlipemia were induced by HFD supply. After end of 84 days of continuous treatment of three different dosages of INJ, all diabetes related complications were inhibited; relatively favorable anti-obesity, hypolipemic, hepatoprotective, hypoglycemic and nephroprotective effects. These favorable effects showed relatively good dose-relations between all three different dosages of INJ treated, and INJ 250 mg/kg showed enough favorable effects on diabetes and related four complications tested as compared with one of each three different references. Otherwise, the efficacy of 62.5 and 125 mg/kg of INJ was somewhat slighter than those of all three reference drugs. Therefore, the suitable effective dosage of INJ is considered as 250 mg/kg/day in the present study. The overall anti-obesity effects of INJ 250 mg/kg-treated group was similar or more favorable than those of metformin 250 mg/kg-treated group, and INJ 250 mg/kg showed slighter hypoglycemic effects with silymarin 100 mg/kg and metformin 250 mg/kg, similar hypolipemic effects with simvastatin 10 mg/kg, and similar hepatoprotective effects with silymarin 100 mg/kg, and similar nephroprotective effects with that of silymarin 100 mg/kg and metformin 250 mg/kg, respectively. Obese, hyperglycemia, hyperlipemia, steatohepatitis and related nephropathies induced by HFD supply were dramatically inhibited by 84 days of continuous treatment of all three different dosages of INJ. It is, therefore expected that INJ extracts will be a favorable alternative agent for diet-related diabetes and complications.

• Asian-Australasian Journal of Animal Sciences
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• 제30권1호
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• pp.111-118
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• 2017

Objective: Adipose tissue plays a key role in the development of obesity and diabetes. We previously reported that lignosulfonic acid suppresses the rise in blood glucose levels through the inhibition of ${\alpha}$-glucosidase activity and intestinal glucose absorption. The purpose of this study is to examine further biological activities of lignosulfonic acid. Methods: In this study, we examined the effect of lignosulfonic acid on differentiation of 3T3-L1 cells. Results: While lignosulfonic acid inhibited proliferation (mitotic clonal expansion) after induction of differentiation, lignosulfonic acid significantly increased the size of accumulated lipid droplets in the cells. Semi-quantitative reverse transcription polymerase chain reaction analysis showed that lignosulfonic acid increased the expression of the adipogenic transcription factor, peroxisome proliferator-activated receptor gamma ($PPAR{\gamma}$), leading to increased glucose transporter 4 (Glut-4) expression and 2-deoxyglucose uptake in differentiated 3T3-L1 cells. Additionally, feeding lignosulfonic acid to diabetic KK-Ay mice suppressed increase of blood glucose level. Conclusion: Lignosulfonic acid may be useful as a functional anti-diabetic component of food.

• 생약학회지
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• 제37권3호
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• pp.190-195
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• 2006

Obesity is associated with a number of pathological disorders such as non-insulin-dependent diabetes, hypertension, hyperlipidemia, and cardiovascular diseases. Bangpoongtongsungsankamibang (BTSK) has been widely used in the oriental medicine for the treatment of several diseases associated with inflammatory abnormalities in cardiovascular and nervous system. The BTSK is the modified prescription of Bangpoongtongsungsankamibang in which sea tangle (Laminaria japonica) were added. This study was carried out to detemine the anti-obestic effects of BTSK. Pretreatment with the BTSK at daily dose of 100 or 200 mg/kg (p.o.) far 4 weeks reduced serum triglyceride, total cholesterol contents in rat induced by Poloxamer-407 or Triton WR-1339, respectively. Furthermore, post-treatment with BTSK far four weeks also inhibited body weight gain, adipose tissue mass and hyperlipidemia induced by the high fat diet for six weeks. The BTSK shifted serum total-, HDL- and LDL-cholesterol levels toward the values of normal group, suggesting that BTSK has hypolipldemlc effects. The rats fed BTSK reduced lipid peroxide and hydroxy radical in the rat blood and increased superoxide dismutase (SOD) activity compared to the control group. Taken together, these results superoxide that BTSK improve hyperlidemia and obesity via the upregulation of anti-oxidative mechanism.