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Anxiolytic-like Effects of the Methanol Extract of Sophorae Fructus (괴각(Sophorae Fructus) 메탄올 추출물의 항불안 효과)

  • Oh, Han Saem;Lee, Gil Yong;Jung, Ji Wook
    • Food Science and Preservation
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    • v.19 no.5
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    • pp.767-773
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    • 2012
  • The purpose of this study was to investigate the anxiolytic-like effect of the methanol extract of Sophorae fructus (MESF) using elevated plus-maze (EPM), open field test, and horizontal wire test in mice. MESF was orally administered at doses of 50, 100, 200, or 400 mg/kg to ICR mice 1 h before behavioral evaluation. The control group was given an equal volume of 10% Tween 80, and the positive control group was given diazepam (1 mg/kg, i.p.). The administration of MESF significantly increased the percentage of time spent in open arms and the entries into the open arms of the EPM compared with the 10% Tween 80-treated control group (p < 0.05). In addition, the anxiolytic-like activities of MESF were antagonized by flumazenil (a GABAA antagonist, 10 mg/kg) but not by WAY-100635 (a 5-HT1A antagonist, 0.3 mg/kg). Futhermore, there were no changes in the locomotor activity and myorelaxant effects of the experimental group, as opposed to the 10% Tween 80-treated control group. Therefore, these findings suggest that MESF promotes the anxiolytic-like activity mediated by the GABAergic nervous system in mice.

Constitutive Activation of $p70^{S6k}$ in Cancer Cells

  • Kwon, Hyoung-Keun;Bae, Gyu-Un;Yoon, Jong-Woo;Kim, Yong-Kee;Lee, Hoi-Young;Lee, Hyang-Woo;Han, Jeung-Whan
    • Archives of Pharmacal Research
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    • v.25 no.5
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    • pp.685-690
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    • 2002
  • The mitogen-stimulated serine/threonine kinase $p70^{S6k}$ plays an important role in the progression of cells from $G_0/G$_1$$ to S phase of the cell cycle by translational up-regulation of a family of mRNA transcripts family of mRNA transcripts which contain polypyrimidine tract at their 5 transcriptional start site. Here, we report that $p70^{S6k}$ was constitutively phosphorylated and activated to various degrees in serum-deprived AGS, A2058, HT-1376, MG63, MCF7, MDA-MB-435S, MDA-MB-231 and MB-157. Rapamycin treatment induced a significant dephosphorylation and inactivation of $p70^{S6k}$ in all cancer cell lines, while wortmannin, a specific inhibitor of PI3-K, caused a mild dephosphorylation of $p70^{S6k}$ in AGS, MDA-MB-435S and MB-157. In addition, SQ20006, methylxanthine phosphodiesterase inhibitor, reduced the phosphorylation of $p70^{S6k}$ in all cancer cells tested. Consistent with inhibitory effect of rapamycin on $p70^{S6k}$ activity, rapamycin inhibited [$^3H$]-thymidine incorporation and increased the number of cells at $G_{0}G_{1}$ phase. Furthermore, these inhibitory effects were accompanied by the decrease in growth of cancer cells. Taken together, the results indicate that the antiproliferative activity of rapamycin might be attributed to cell cycle arrest at $G_{0}G_{1}$ phase in human cancer cells through the inhibition of constitutively activated $p70^{S6k}$ of cancer cells and suggest $p70^{S6k}$ as a potential target for therapeutic strategies aimed at preventing or inhibiting tumor growth.

Obesity among Secondary School Girls in Ulsan Area (울산지역 중학교 여학생의 비만실태에 관한 연구)

  • 김혜경
    • Journal of the East Asian Society of Dietary Life
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    • v.6 no.1
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    • pp.33-39
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    • 1996
  • The aim of this study is to estimate the prevalence of obesity and factors with it Ulsan secondary school girls. A cross-sectional study involving a sample of 485 students aged 12 to 15 years was obtained form secondary schools. Obesity was determined using body mass index(BMI=wt/Ht$^2$). The findings revealed that the average BMI was 19.3, and 4.5% of girls were either overweight and obese(BMI$\geq$25). Subjects were grouped into three categories based on the BMI, sibling obesity, self-consciousness of obesity, eating patterns such as eating snack after dinner and prejudice in food selection, and food frequency score were significantly associated nth BMI, while nutrition knowledge score was not associated with BMI. The fact that several social, environmental and health factors are associated with obesity means that a multisectorial intervention program must be considered in order to decrease the problem of overweight among secondary girls. Such program should include dietary intervention to modify food habits, nutrition education through mass media, introducing information on prevention and control obesity in school curriculum, and allocating sufficient time in the school schedule for exercise activities.

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Antitumor Activity of 7-[2-(N-Isopropylamino)ethyl]-(20s)-camptothecin, CKD602, as a Potent DNA Topoisomerase I Inhibitor

  • Lee, Jun-Hee;Lee, Ju-Mong;Kim, Joon-Kyum;Ahn, Soon-Kil;Lee, Sang-Joon;Kim, Mie-Young;Jew, Sang-Sup;Park, Jae-Gab;Hong, Chung-Il
    • Archives of Pharmacal Research
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    • v.21 no.5
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    • pp.581-590
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    • 1998
  • We developed a novel water-soluble camptothecin analobue, CKD602, and evaluated the inhibition of topoisomerase I and the antitumor activities against mammalian tumor cells and human tumor xenografts. CKD602 was a nanomolar inhibitor of the topoisomerase I enzyme in the cleavable complex assay. CKD602 was found to be 3 times and slightly more potent than topotecan and camptothecin as inhibitors of topoisomerase, respecitively. In tumor cell cytotoxicity, CKD602 was more potent than topotecan in 14 out of 26 human cancer cell lines tested, while it was comparable to camptothecin. CKD602 was tested for the in vivo antitumor activity against the human tumor xenograft models. CKD602 was able to imduce regression of established HT-29, WIDR and CX-1 colon tumors, LX-1 lung tumor, MX-1 breast tumor and SKOV-3 ovarian tumor as much as 80, 94, 76, 67, 87% and 88%, respectively, with comparable body weight changes to those of topotecan. Also the therapeutic margin (R/Emax: maximum tolerance dose/$ED-{58}$) of CKD602 was significantly higher than that of topotecan by 4 times. Efficacy was determined at the maximal tolerated dose levels using schedule dependent i.p. administration in mice bearing L1210 leukemia. On a Q4dx4 (every 4 day for 4 doses) schedule, the maximum tolerated dose (MTD) was 25 mg/kg per administration, which caused great weight loss and lethality in <5% tumor bearing mouse. this schedule brought significant increase in life span (ILS), 212%, with 33% of long-term survivals. The ex vivo antitumor activity of CKD602 was compared with that of topotecan and the mean antitumor index (ATI) values recorded for CKD602 were significantly higher than that noted for topotecan. From these results, CKD602 warrants further clinical investigations as a potent inhibitor of topoisomerase I.

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Effect of Gamma Irradiation on Physiological Activity of Citrus Essential Oil (감마선 조사가 감귤 정유의 생리활성에 미치는 영향)

  • Kim, Hyun-Joo;Jo, Cheorun;Lee, Na-Young;Son, Jun-Ho;Yook, Hong-Sun;Yook, Hong-Sun;Byun, Myung-Woo
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.34 no.6
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    • pp.797-804
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    • 2005
  • Physiological activity of citrus essential oil (CEO) was determined to examine possible use of the food processing by-product as a functional material for food and cosmetic composition. The effect of gamma irradiation on the change of physiological activity also investigated at 0, 10 and 20 kGy. Limonene contents of CEO was $88.3\pm1.30\%$. Electron donating ability of CEO was $69\%$. Lipid oxidation was retarded by CEO. CEO showed antimicrobial activity against 1 yeast,4 molds and 4 bacteria species tested. More than $80\%$ of inhibition of cancer cell growth was presented by CEO using A549, HT29, HepG2, B16F10 and G361 cells at a 500 ppm level. Irradiation of CEO did not affect any physiological functions. A Salmonella mutagenicity assay indicated that the 20 kGy irradiated CEO did not show any mutagenicity Therefore, CEO, which is a major by-product in citrus processing, could be used as a functional material in various application.

Physiological Characteristics and Anti-Obesity Effect of Lactobacillus plantarum K6 isolated from Kimchi (김치에서 분리한 Lactobacillus plantarum K6의 생리적 특성 및 비만억제효과)

  • Kim, Seulki;Lim, Sang-Dong
    • Journal of Dairy Science and Biotechnology
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    • v.35 no.4
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    • pp.221-231
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    • 2017
  • This study aimed to investigate the physiological characteristics and anti-obesity effects of a newly isolated bacterium, Lactobacillus plantarum K6. L. plantarum K6 showed good ${\alpha}-amylase$ inhibitory activity ($96.78{\pm}3.29%$), ${\alpha}-glucosidase$ inhibitory activity ($92.55{\pm}9.62%$), and lipase inhibitory activity ($85.17{\pm}0.79%$), and the strain inhibited the adipocyte differentiation of 3T3-L1 cells ($27.4{\pm}1.4%$) when present at a concentration of $100{\mu}g/mL$. L. plantarum K6 was isolated from kimchi and its physiological characteristics were investigated. A comparison of the sensitivity of the isolate to 15 different antibiotics showed that L. plantarum K6 is highly sensitive to erythromycin and highly resistant to vancomycin, ampicillin, and polymyxin B. This strain also showed high arylamidase and ${\beta}-galactosidase$ activities. Moreover, it was relatively tolerant to bile acid and low pH, and displayed resistance to Escherichia coli, Salmonella Typhimurium, Listeria monocytogenes, and Staphylococcus aureus, with rates of 51.8%, 42.4%, 61.6%, and 54.9%, respectively. No bio genic amines were produced. L. plantarum K6 also showed high adhesion activity to HT-29 cells compared to L. rhamnosus GG. These results demonstrate that Lactobacillus plantarum K6 has potential as a probiotic with anti-obesity effects.

Four Novel Synthetic Tryptamine Analogs Induce Head-Twitch Responses and Increase 5-HTR2a in the Prefrontal Cortex in Mice

  • Abiero, Arvie;Ryu, In Soo;Botanas, Chrislean Jun;Custodio, Raly James Perez;Sayson, Leandro Val;Kim, Mikyung;Lee, Hyun Jun;Kim, Hee Jin;Seo, Joung-Wook;Cho, Min Chang;Lee, Kun Won;Yoo, Sung Yeun;Jang, Choon-Gon;Lee, Yong Sup;Cheong, Jae Hoon
    • Biomolecules & Therapeutics
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    • v.28 no.1
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    • pp.83-91
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    • 2020
  • Tryptamines are monoamine alkaloids with hallucinogenic properties and are widely abused worldwide. To hasten the regulations of novel substances and predict their abuse potential, we designed and synthesized four novel synthetic tryptamine analogs: Pyrrolidino tryptamine hydrochloride (PYT HCl), Piperidino tryptamine hydrochloride (PIT HCl), N,N-dibutyl tryptamine hydrochloride (DBT HCl), and 2-Methyl tryptamine hydrochloride (2-MT HCl). Then, we evaluated their rewarding and reinforcing effects using the conditioned place preference (CPP) and self-administration (SA) paradigms. We conducted an open field test (OFT) to determine the effects of the novel compounds on locomotor activity. A head-twitch response (HTR) was also performed to characterize their hallucinogenic properties. Lastly, we examined the effects of the compounds on 5-HTR1a and 5-HTR2a in the prefrontal cortex using a quantitative real-time polymerase chain reaction (qRT-PCR) assay. None of the compounds induced CPP in mice or initiated SA in rats. PYT HCl and PIT HCl reduced the locomotor activity and elevated the 5-HTR1a mRNA levels in mice. Acute and repeated treatment with the novel tryptamines elicited HTR in mice. Furthermore, a drug challenge involving a 7-day abstinence from drug use produced higher HTR than acute and repeated treatments. Both the acute treatment and drug challenge increased the 5-HTR2a mRNA levels. Ketanserin blocked the induced HTR. Taken together, the findings suggest that PYT HCl, PIT HCl, DBT HCl, and 2-MT HCl produce hallucinogenic effects via 5-HTR2a stimulation, but may have low abuse potential.

A Study on the Necessity and Direction of Regulations on the Emission of Hazardous and Noxious Substances from Marine Industrial Facilities (해양산업시설의 위험유해물질 해양배출 규제체계 개선의 필요성과 규제방향에 대한 연구)

  • Lee, Moonjin;Kim, Kyewon;Kang, Wonsoo
    • Journal of the Korean Society of Marine Environment & Safety
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    • v.27 no.6
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    • pp.737-743
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    • 2021
  • In this paper, the current status of marine industrial facilities, regulatory legal systems, and emission status of hazardous and noxious substances (HNS) in these facilities were analyzed, and the direction of improvement of the regulatory system was presented accordingly. As a result of the analysis, it is estimated that about 1,100 marine industrial facilities are subject to the Marine Environment Management Act of 2007. It is estimated that 190 kinds of hazardous substances are discharged from these marine industrial facilities and are highly likely to flow into the ocean, of which 20 are estimated to be discharged into the water system. However, due to the lack of relevant laws and regulation, it is difficult to clearly determine whether the discharged material corresponds to an exceptional discharged material, making it difficult to effectively enforce regulations in the field. For this reason, effective regulatory enforcement is difficult in the regulatory field. The marine environment management law should clearly stipulate the exceptional emission standards and types of substances, and clarify the selection system, risk assessment system, and emission information collection and monitoring system for related Hazardous and Noxious Substances.

The study of anti-inflammatory effect of Hyeonto-dan extract in RAW 264.7 macrophage (현토단(玄兎丹)의 RAW 264.7 대식 세포에서의 항염증 효과에 관한 연구)

  • Kim, Ma-Ryong;Kang, Ok-Hua;Kong, Ryong;Seo, Yun-Soo;Zhou, Tian;Kim, Sang-A;Kim, Eun-Su;Sin, Min-A;Lee, Young-Seob;Kwon, Dong-Yeul
    • The Korea Journal of Herbology
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    • v.32 no.2
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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 $TNF-{\alpha}$.

Anthropometric Measurements and Biochemical Nutritional Status of the Older Residents (50 years and over) in Andong Area (2) (안동주변 농촌지역 50세 이상 주민의 신체계측치 및 생화학적 영양상태에 관한 연구 (2))

  • Lee, Hye-Sang;Kwun, In-Sook;Kwon, Chong-Suk
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.37 no.12
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    • pp.1599-1608
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    • 2008
  • This study aimed to assess the health status based on the anthropometric and biochemical measurements of middle-aged and elderly people living in Andong area. The subjects were 1,384 people (532 males, 852 females) aged 50 years and over (average 62.7 years). The mean anthropometric values for males and females were heights of 163.7 and 151.5 cm; weights 63.6 and 57.3 kg; body mass index (BMI) 23.6 and $24.9kg/m^2$; body fat 21.8 and 31.8%, respectively. Height and weight were lower, however, waist circumference (in female) and BMI were higher than those of the 2001 National Health and Nutrition Survey (NHNS). Obesity incidences of male and female subjects were 28.7% and 47.3% by BMI; 25.8% and 50.8% by % body fat; and 15.6% and 80.9% by waist circumference, respectively. Also, abdominal adiposity was very severe in female subjects of 50s. The mean biochemical measurements of male and female were as follows: systolic and diastolic blood pressure 136.9, 83.8 mmHg and 133.6, 82.5 mmHg; hemoglobin (Hb) 14.3 and 13.0 g/dL; hematocrit (Ht) 44.7 and 39.8%; blood albumin 4.15 and 4.04 g/dL; total-cholesterol 170.0 and 183.1 mg/dL; HDL-cholesterol 43.6 and 42.7 mg/dL; fasting blood glucose 96.7 and 93.0 mg/dL, respectively. Also, the prevalence of biochemically abnormal subjects according to each cut-off point of biochemical measurements were analyzed. The results for male and female were; hypertension 58.0% and 47.2%; iron deficient anemia 19.3% and 20.6% by Hb, 7.2% and 11.9% by Ht; hypoalbuminemia 9.8% and 11.7%; diabetes 12.0% and 10.2%; hypercholesterolemia 19.5% and 30.5%, respectively. From those results we found that hypoalbuminemia, hypertension and hypercholesterolemia were prevalent, and obesity in females of 50s, iron-deficient anemia and diabetes in males of 70 years and over were significant health problems in this area. Therefore, it seems to be necessary to examine their health status periodically and provide the appropriate health and nutrition education program, which includes low sodium intake, balanced diet, exercise and weight control, to prevent the occurrence of chronic diseases.