• The Korean Journal of Physiology and Pharmacology
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• 제23권6호
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• pp.459-466
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• 2019

Dipeptidyl peptidase (DPP)-4 inhibitors, or gliptins, are a class of oral hypoglycemic drugs that have been widely used as a second-line treatment for type 2 diabetes. Gliptins, which were introduced for clinical use a decade ago, have been shown to be beneficial against nonalcoholic fatty liver disease/nonalcoholic steatohepatitis (NASH) in animals and humans. Cenicriviroc (CVC), a dual antagonist of C-C chemokine receptor type 2 and 5, is currently under investigation against NASH and fibrosis. It was previously discovered that evogliptin (EVO) reduces hepatic steatosis in diet-induced obese animals but the effectiveness of EVO on NASH remains unexplored. Here, we compared the effectiveness of EVO and CVC against NASH and fibrosis in mice fed a high-fat and high-fructose diet (HFHF). Biochemical and histological analyses showed that mice fed a HFHF for 20 weeks developed severe hepatic steatosis and inflammation with mild fibrosis. Administration of EVO (0.2% wt/wt) for the last 8 weeks of HFHF feeding significantly reduced hepatic triglyceride accumulation, inflammation, and fibrosis as well as restored insulin sensitivity, as evidenced by lowered plasma insulin levels and the improvement in insulin tolerance test curves. Treatment of mice with CVC (0.1% wt/wt) inhibited hepatic inflammation and fibrogenesis with similar efficacy to that of EVO, without affecting hepatic steatosis. CVC treatment also reduced plasma insulin concentrations, despite no improvement in insulin tolerance. In conclusion, EVO administration efficiently ameliorated the development of NASH and fibrosis in HFHF-fed mice, corroborating its therapeutic potential.

• 대한화학회지
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• 제35권4호
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• pp.379-388
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• 1991

이핵성 네자리 Schiff base cobalt(II) 착물로서 [Co(II)$_2$(SMPD)$_2$(L)$_2$] 및 [Co(II)$_2$(SPPD)$_2$(L)$_2$](L ; Py, DMSO, 및 DMF)들을 합성하여 원소분석, IR-spectrum 및 T. G. A을 측정하여 이핵성임을 확인하였다. 지지전해질로서 0.1M-TEAP을 포함한 비수용매(Py, DMSO 및 DMF)인 10 mM-착물용액에서 순환전압전류법과 DPP법으로 전기화학적 성질을 측정한 결과 일핵성인 Co(II)(SOPD)(L)$_2$는 일전자의 확산지배적인 두 단계 환원과정이 0.1 M TEAP-Py와 0.1 M TEAP-DMSO 용액에서는 가역 및 준가역적으로 일어나지만, 이핵성인 [Co(II)$_2$(SMPD)$_2$(L)$_2$] and [Co(II)$_2$(SPPD)$_2$(L)$_2$] 착물들은 비수용매에서 일전자의 확산지배적이고, 비가역적 네단계 환원과정이 Co(III)$_2\;{\longrightarrow^e}$ Co(III)Co(II) ${\longrightarrow^e}$ Co(II)$_2\;{\longrightarrow^e}$ Co(II)Co(I) ${\longrightarrow^e}$ Co(I)$_2$으로 일어남을 알았다.

• Toxicological Research
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• 제16권2호
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• pp.141-146
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• 2000

Phthalate esters are used extensively as a plasticizer in the manufacture of plastic products such as PVC bags and medical devices. Recently, phthalate esters have been shown to induce endocrine system mediated responses. However. only a Jew studies have been conducted for estrogenic activity of phthalate esters. In this study estrogenic activities of seven phthalate esters. butyl benzyl phthalate (BBP), di(2-ethylhexyl) phthalate (DEHP), di-n-butylphthalate (DBP), diethylphthalate (DEP), di-n-pentylphthalate (DPP), di-n-propylphthalate (DPrP) and dicyclohexylphthalate (DCHP), were examined in vitro using E-screen assay and competitive binding assay. From the E-screen assay, BBP. DEHP. DBP and DEP showed weak estrogenic activity at the concentration of 5 $\mu\textrm{M}$. The relative proliferative effect (RPE) and the relative proliferative potency (RPP) were 50~70% and 0.01%. respectively, when compared with 500 pM of 17$\beta$-estradiol (E2). In competitive binding assay with the rat uterine estrogen receptor (ER), BBP and DEP showed weak binding potency ［(l/$10^4$~1/$10^5$ of E2］ while DEHP and DBP scarcely bound to ER. These results suggest that some phthalate esters have weak estrogenic activities in vitro.

• 한국가금학회지
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• 제23권4호
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• pp.169-175
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• 1996

An experiment was conducted with male broiler chicks to determine the effect of different dietary phosphorus sources and evaluate the biological availability of phosphorus sources. The biological availability of phosphorus from dicalcium phosphate (DCP) was used as a reference standard (100%) compared to defluorinate phosphate (DFP). DCP and DFP was supplemented to a corn-soy basal diet at levels of 0.05, 0.15, 0.25, 0.35%. Each of 24 pens of 10 male broiler chicks with three replications was used for three weeks. The results indicated that weight gain, feed in-take, feed efficiency, nonphytic phosphorus (NPP) and tibia ash were significantly different among treatments. Dietary supplemental phosphorus of DFP improved weight gain, NPP intake and feed efficiency consistently, whereas supplements of DCP did not show consistent increase. Regression equations was used for the availability of DPP compared with DCP when percent bone ash was a function of total phosphorus in the diet. The percent (%) bone ash of DFP groups compared to that of DCP groups showed a value of 59.98% as a slope ratio. DFP indicated lower biological availability compared to DCP, but it's dietary supplementation tended to increase bone ash and maximize the growth of young broiler chicks.

• 대한한방내과학회지
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• 제40권6호
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• pp.1294-1302
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• 2019

Objective: Glucagon-like peptide 1 (GLP-1), one of the gut peptide hormones, has an action to induce satiety, and its effect as an anti-obesity agent is known. Recently, it has been reported that many herbal medicines have an anti-diabetic effect through inhibition of DPP-4 enzyme and inducing of GLP-1 secretion. It is therefore suggested that GLP-1 may be effective for the treatment of obesity. In this study, we report a case of male obese patients treated with herbal medicine as a GLP-1 secretagogue. Methods: In this study, the patient took a fixed prescription of herbal medicine for 10 weeks and recorded his weight at each visit. Results: This prescription produced significant weight loss (BMI loss>5%). In the follow-up period after two weeks, the trend of weight loss was observed continuously. Conclusion: This prescription can be an alternative to ephedra herba-based obesity treatment.

• International Journal of Oral Biology
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• 제36권4호
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• pp.167-172
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• 2011

LAR-RPTP (leukocyte common antigen-related receptor protein tyrosine phosphatase) is an important regulator in the nervous system, but little is known about its expression pattern in rat trigeminal ganglion (TG) neurons. To examine whether LAR-RPTP is expressed in the TG in the current study, we sacrificed rats at 0, 7, 10 and 56 day postpartum (dpp) and a second group of rats at 3 and 5 days after an experimental tooth extraction as a TG injury model. RT-PCR was then used to determine the level of LAR-RPTP expression in the TG and immunohistology was employed to detect the subcellular localization of the protein. The mRNA expression of LAR-RPTP during the developmental stages in the TG was found to gradually increase. After experimental tooth extraction however, these transcript levels had significantly decreased at three days. LAR-RPTP protein signals in the TG were found to be cytoplasmic in the normal animals but interestingly, at five days after an experimental tooth extraction, these signals were rare. These results indicate that LAR-RPTP may be regulated during both the developmental as well as regenerative processes that take place in the TG. This further suggests that LAR-RPTP is not only involved in primary axonogenesis but possibly also in the molecular control of axons during TG repair.

• 환경위생공학
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• 제20권2호
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• pp.39-46
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• 2005

This study was Performed to survey and evaluate the contents of Plasticizers such as DEP(diethyl phthalate), DPrP(di-n-Phthalate), DBP(di-n-butyl Phthalate), DPP(di-n-pentyl Phthalate), DCHP(dicyclohexyl phthalate), BBP (butylbenzyl phthalate), DEHP(di-(2-ethylhexyl) phthalate) and DEHA(di-(2-ethylheryl) adipate), which are suspected as endocrine disruptors, in food and drug PVC packaging. Tested samples were 5 food wraps, 35 food containers, 40 food and drug packages(type of tablet and capsule) in Gyeonggi-Do area. The contents of DEHA in wrap were 188.9g/kg, 203.1g/kg, 238.4g/kg, 290.9g/kg and 308.3g/kg, respectively, while the other plasticizers were not detected. DEHP was used in 4 samples of food containers and DEHP contents were 4.7g/kg, 30.7g/kg, 35.8g/kg and 53.4g/kg, respectively. In food and drug packaging materials(type of tablet and capsule), the plasticizers were not detected.

• 한국동물생명공학회지
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• 제36권4호
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• pp.203-211
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• 2021

Diabetic mellitus (DM) is a carbohydrate metabolic disorder that involves high blood sugar because insulin works abnormally. Type 2 diabetes accounts for most of them. However, diabetes treatments such as GLP-1 and DPP-4 inhibitors commonly caused side effects including gastrointestinal disorders. Grifola frondosa (G. frondosa) revealed various pharmacological effects in recent studies. It has a variety of anti-cancer polysaccharides through host-mediated mechanisms. D-fraction in G. frondosa has apoptotic effects, promoting myeloid cell proliferation and differentiation into granulocytes-macrophages. It has also been shown to reduce the survival rate of breast cancer cells. Though, no further study has been conducted on the specific effects of G. frondosa in the db/db mouse. Therefore, we would like to research the blood glucose improving effect of G. frondosa, a natural material, in type 2 diabetes model mouse, in this study. G. frondosa was administered to the disease model mouse (BKS.Cg-+Lepr^db/+Lepr^db/OlaHsd) for 8 weeks to monitor weight and blood glucose changes every week. And we evaluated anti-diabetes effects by checking biomarker changes shown through blood. Experiment did not show statistically significant weight differences, but control groups showed significantly higher weight gain than G. frondosa administered groups. We collected blood from the tail veins of the db/db mouse each week. As a result, the lowest blood sugar level was shown in the 500 mg/kg group of G. frondosa. Glucose in the blood was examined with HBA1c, and 7.8% was shown in the 500 mg/kg administration group, lower than in other groups. These results suggest the potential improvements of diabetes in G. frondosa.

• 대한화장품학회지
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• 제45권3호
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• pp.217-224
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• 2019

프탈레이트는 내분비계 교란 물질로서 성호르몬과 구조가 유사하여 주로 생식독성과 발달독성을 나타낸다. 이번 연구에서는 우리나라 화장품규제 물질인 3종 프탈레이트 이외 어린이제품 안전공통기준, EU 화장품 기준(EC No. 1223/2009) 등에서 규제하고 있는 프탈레이트 종류를 추가하여 총 11종 프탈레이트에 관하여 분석을 실시하였다. GC-MS/MS를 이용하여 분석조건을 설정하였고 분석방법에 대한 유효성 검증 결과 특이성, 직선성, 회수율, 정밀성, 정량한계 등을 만족하였다. 유효성이 검증된 시험방법을 이용하여 네일 화장품 및 네일 관련 제품 82건을 대상으로 분석을 실시하였다. 네일 폴리시에서는 DBP, BBP, DEHP, DPP, DIBP, DIDP 등 6종의 프탈레이트가 $1.0{\sim}59.8{\mu}g/g$의 농도로 검출되었으나 우리나라 화장품기준에 적합하였다. 인조손톱에서는 DIBP, DBP 2종에서 $1.1{\sim}2.6{\mu}g/g$, 글루에서 DBP, DEHP 2종 $1.4{\sim}2.5{\mu}g/g$, 스티커 DIBP, DBP, DEHP 3종에서 $2.5{\sim}33.3{\mu}g/g$ 의 결과가 나왔고 '어린이제품 공통안전기준'을 적용시 모두 적합하였다. DIBP는 우리나라에는 규제물질이 아니지만 DBP (86.6%), DEHP (63.4%)에 이어 14.6%의 검출률을 나타내었다. 현재 우리나라 기준으로는 네일제품이 프탈레이트에 대해 안전하다고 판단되지만 비규제물질에 대한 지속적인 감시와 연구도 필요할 것으로 사료된다.

• 약학회지
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• 제52권5호
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• pp.331-344
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• 2008

Recently, the FDA (Food and Drug Administration) of the United States and many advanced countries remark biomarkers and surrogate endpoints as a critical path tool on model based drug development. Economic, technical and social profit on model based drug development like a reduction of the length of research and development have been achieved. Therefore we summarize previous studies about biomarkers and surrogate endpoints and suggest a development direction of therapeutic agents. In diabetes mellitus (DM) and osteoporosis, there are remarkable increases in number of patients and most of patients take medicine during their whole lifetime. For this reason, many patients with DM and osteoporosis have a tolerance on their medicine. We expect that research and development on biomarkers and surrogate endpoints will contribute to new drug development on DM and osteoporosis. Biomarkers for DM are blood levels of glucose, insulin, ${HbA}_{1c}$, CRP, alpha-glucosidase, adiponectin and DPP-4. Among these, validated surrogate endpoints for DM are blood levels of glucose, insulin and ${HbA}_{1c}$ Biomarkers for osteoporosis are BMD, BMC, trabecular volume, ICTP, DPD, osteocalcin, the activity of osteoclast and production of osteoblast. The validated surrogate endpoints for osteoporosis are BMD only. This review summarizes all suggested biomarkers and surrogate endpoints in DM and osteoporosis. The biomarkers are classified by drugs, and the method of validation for surrogate endpoints is suggested. This information would contribute to suggest a direction of DM and osteoporosis therapeutic agent development.