• Title/Summary/Keyword: Pharmacological profile

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Effects of Protocatechuic Acid Derived from Rubus coreanus on the Lipid Metabolism in High Cholesterol Diet-induced Mice (복분자 유래 성분 protocatechuic acid 투여가 고콜레스테롤 식이로 유도된 생쥐의 지질대사에 미치는 영향)

  • Koo, Hyun Jung;Kang, Se Chan;Jang, Seon-A;Kwon, Jung-Eun;Sohn, Eunsoo;Sohn, Eun-Hwa
    • Korean Journal of Plant Resources
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    • v.27 no.4
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    • pp.271-278
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    • 2014
  • Rubus coreanus has been used as a traditional medicine in Asia because of its various pharmacological properties. This study examined the effects of protocatechuic acid (PCA), one of phenolic compounds derived from R. coreanus on the lipid metabolism in high cholesterol diet-induced mice. A total of 30 male C57BL/6 mice were divided into 5 groups with 6 mice in each group as follows: (1) Control mice received normal diet (ND). (2) Mice received high-cholesterol diet (HCD) plus water, 10% sucrose solution and treated daily oral phosphate-buffered-saline (PBS) of equal volumes through gavage. (3) Mice received HCD and treated daily with 25 mg/kg b.w./day of PCA (4) with 50 mg/kg b.w./day or (5) with 10 mg/kg b.w./day of simvastatin via oral gavage for 12 weeks. Body weights were measured weekly for a period of experiment. After treatment, liver, thymus, spleen and kidney were harvested and weighed, and the lipid metabolite profiles (total cholesterol, triglyceride (TG), HDL-cholesterol (HDL-c), LDL-cholesterol (LDL-c) and liver-damaging markers (GOT and GPT) in serum were examined. PCA significantly reduced the total cholesterol, TG, LDL-c level and increased the HDL-c level. PCA administration also significantly reduced the levels of GOT and GPT. These results indicate that the PCA could be used as a functional material for lowering lipid and an adjuvant for the treatment of hyperlipemia.

Pharmacological Profile of KR-31125, an Orally Active AT1 Receptor Antagonist (안지오텐신 수용체 리간드 KR-31125의 생체 내 활성에 관한 연구)

  • Lee, Sung-Hou
    • Journal of Life Science
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    • v.20 no.7
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    • pp.969-976
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    • 2010
  • In vivo studies of KR-31125 (2-butyl-5-dimethoxymethyl-6-phenyl-7-methyl-3-[[2'-(1H-tetrazol-5-yl) biphenyl-4-yl]methyl]-3H-imidazo[4,5-b]pyridine) were performed in pithed rats, conscious angiotensin II (AII) challenged normotensive rats, renal hypertensive rats (RHRs) and furosemide-treated beagle dogs. KR-31125 induced a non-parallel right shift in the dose-pressor response curve to AII ($ID_{50}$: 0.095 mg/kg) with a dose-dependent reduction in the maximum responses in pithed rats. Compared to losartan, this antagonistic effect was about 18 times more potent, presenting competitive antagonism. Other agonists such as norepinephrine and vasopressin did not alter the responses induced by KR-31125. Orally administered KR-31125 had no agonistic effect and dose-dependently inhibited the pressor response to AII with a slightly weaker potency ($ID_{50}$: 0.25 and 0.47 mg/kg, respectively) in the AII-challenged normotensive rat model, but with a more rapid onset of action than losartan (time to $E_{max}$: 30 min for KR-31125 and 6 hr for losartan). KR-31125 produced a dose-dependent antihypertensive effect with a higher potency than losartan in RHRs, and these effects were confirmed in furosemide-treated dogs where they presented a dose-dependent and long-lasting (>8 hr) antihypertensive effect with a rapid onset of action (time to $E_{max}$: 2-4 hr), as well as a 20-fold greater potency than losartan. These results suggest that KR-31125 is a potent, orally active $AT_1$ receptor antagonist that can be applied to the development of new diagnostic and research tools as an added exploratory potential of $AT_1$ receptor antagonist.

Assessment of the Therapeutic Potential of Persimmon Leaf Extract on Prediabetic Subjects

  • Khan, Mohd M.;Tran, Bao Quoc;Jang, Yoon-Jin;Park, Soo-Hyun;Fondrie, William E.;Chowdhury, Khadiza;Yoon, Sung Hwan;Goodlett, David R.;Chae, Soo-Wan;Chae, Han-Jung;Seo, Seung-Young;Goo, Young Ah
    • Molecules and Cells
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    • v.40 no.7
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    • pp.466-475
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    • 2017
  • Dietary supplements have exhibited myriads of positive health effects on human health conditions and with the advent of new technological advances, including in the fields of proteomics, genomics, and metabolomics, biological and pharmacological activities of dietary supplements are being evaluated for their ameliorative effects in human ailments. Recent interests in understanding and discovering the molecular targets of phytochemical-gene-protein-metabolite dynamics resulted in discovery of a few protein signature candidates that could potentially be used to assess the effects of dietary supplements on human health. Persimmon (Diospyros kaki) is a folk medicine, commonly used as dietary supplement in China, Japan, and South Korea, owing to its different beneficial health effects including anti-diabetic implications. However, neither mechanism of action nor molecular biomarkers have been discovered that could either validate or be used to evaluate effects of persimmon on human health. In present study, Mass Spectrometry (MS)-based proteomic studies were accomplished to discover proteomic molecular signatures that could be used to understand therapeutic potentials of persimmon leaf extract (PLE) in diabetes amelioration. Saliva, serum, and urine samples were analyzed and we propose that salivary proteins can be used for evaluating treatment effectiveness and in improving patient compliance. The present discovery proteomics study demonstrates that salivary proteomic profile changes were found as a result of PLE treatment in prediabetic subjects that could specifically be used as potential protein signature candidates.

Experimental and FEMLAB Simulation Study of Ibuprofen Racemate Separation in HPLC (Ibuprofen Racemate의 HPLC 분리실험과 FEMLAB 전산모사 연구)

  • Lee, Eun;Chang, Sang-Mork;Kim, Jong-Min;Kim, Woo-Shick;Kim, In-Ho
    • KSBB Journal
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    • v.21 no.3
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    • pp.224-229
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    • 2006
  • FEMLAB is a powerful interactive environment for modeling, solving all kinds of scientific and engineering problems based on partial differential equations(PDEs). Separation process of chiral compound in HPLC columns was simulated by FEMLAB. To study change of elution profile with isotherm models, non-competitive and competitive Langmuir adsorption isotherm were adopted. Separated material was (R, S)-ibuprofen [(R, S)-2-(4-isobutyl phenyl) propionic acid], an anti-inflammatory agent, which retain the pharmacological activity in the (S)-(+)-enantiomer. Sample concentrations were changed from 0.5 mg/ml to 2.0 mg/ml at a flow rate of 1 ml/min and flow rate varied from 1 ml/min to 3 ml/min at an ibuprofen concentration of 2.0 mg/ml and $20{\mu}l$ of injection volume. Simulated results were well fitted with experimental data.

Paralytic shellfish toxins (PSTs) and tetrodotoxin (TTX) of Korean pufferfish

  • Lee, Ka Jeong;Ha, Kwang Soo;Jung, Yeoun Joong;Mok, Jong Soo;Son, Kwang Tae;Lee, Hee Chung;Kim, Ji Hoe
    • Fisheries and Aquatic Sciences
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    • v.24 no.11
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    • pp.360-369
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    • 2021
  • Paralytic shellfish toxins (PSTs) and tetrodotoxin (TTX) are neurotoxins that display pharmacological activity that is similar to that of specific sodium channel blockers; they are the principle toxins involved in shellfish and puffer fish poisoning. In Korea, puffer fish is a very popular seafood, and several cases of accidental poisoning by TTX have been reported. Therefore, it is necessary to determine whether puffer fish poisoning incidents are caused by PSTs or by TTX. In this study, we used mouse bioassay (MBA) and liquid chromatograph-tandem mass spectrometry (LC-MS/MS) to determine the presence of PSTs and TTX in puffer fish from an area near Mireuk-do, Tong-Yeong on the southern coast of Korea from January through March, 2014. The toxicity of PSTs and TTX extracts prepared from three organs of each specimen was analyzed by MBA. Most of the extracts killed mice with typical signs of TTX and PSTs. The LC-MS/MS analysis of seven specimens of Takifugu pardalis and Takifugu niphobles, each divided into muscles, intestines, and liver, were examined for TTX. In T. pardalis, the TTX levels were within the range of 1.3-1.6 ㎍/g in the muscles, 18.8-49.8 ㎍/g in the intestines, and 23.3-96.8 ㎍/g in the liver. In T. niphobles, the TTX levels were within the range of 2.0-4.5 ㎍/g in the muscles, 23.9-71.5 ㎍/g in the intestines, and 28.1-114.8 ㎍/g in the liver. Additionally, the toxicity profile of the detected PSTs revealed that dcGTX3 was the major component in T. pardalis and T. niphobles. When PSTs were calculated as saxitoxin equivalents the levels were all less than 0.5 ㎍/g, which is below the permitted maximum standard of 0.8 ㎍/g. These findings indicate that the toxicity of T. pardalis and T. niphobles from the southern coast of Korea is due mainly to TTX and that PSTs do not exert an effect.