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Macakurzin C Derivatives as a Novel Pharmacophore for Pan-Peroxisome Proliferator-Activated Receptor Modulator

  • Hyejin Ko;Seungchan An;Hongjun Jang;Sungjin Ahn;In Guk Park;Seok Young Hwang;Junpyo Gong;Soyeon Oh;Soo Yeon Kwak;Won Jun Choi;Hyoungsu Kim;Minsoo Noh
    • Biomolecules & Therapeutics
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    • v.31 no.3
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    • pp.312-318
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    • 2023
  • The natural flavonoid macakurzin C (1) exhibited adiponectin biosynthesis-inducing activity during adipogenesis in human bone marrow mesenchymal stem cells and its molecular mechanism was directly associated with a pan-peroxisome proliferator-activated receptor (PPAR) modulator affecting all three PPAR subtypes α, γ, and δ. In this study, increases in adiponectin biosynthesis-inducing activity by macakurzin C derivatives (2-7) were studied. The most potent adiponectin biosynthesis-inducing compound 6, macakurzin C 3,5-dimethylether, was elucidated as a dual PPARα/γ modulator. Compound 6 may exhibit the most potent activity because of the antagonistic relationship between PPARδ and PPARγ. Docking studies revealed that the O-methylation of macakurzin C to generate compound 6 significantly disrupted PPARδ binding. Compound 6 has therapeutic potential in hypoadiponectinemia-related metabolic diseases.

Antioxidative and Hair-growth-promotion Effects of a Fermented Compound Composed of Five Materials (발효 5종 혼합물의 항산화 및 모발 성장 촉진 효과)

  • Lee, Ha Neul;Ha, Bae Jin
    • Journal of Life Science
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    • v.28 no.6
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    • pp.663-670
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    • 2018
  • This study was performed to confirm the antioxidative and hair-growth-promotion effects of a fermented compound composed of five materials, namely Allium cepa, Cucurbita spp., Glycine max Merr., Pinus sylvestris leaf, and Sesamum indicum. An additional compound composed of two materials was composed of Allium cepa and Cucurbita spp. Antioxidative effects were measured based on DPPH radical-scavenging activity and total flavonoid content. Fermented 5-type natural compounds (5NC) showed higher DPPH radical-scavenging activity and flavonoid content than those of fermented 2-type natural compounds (2NC). Hair-growth promotion was demonstrated in vivo. Alkaline phosphatase (ALP), oid contentontenteptidase phospactivity, and macroscopic observation were measured. Experimental animals were divided into four groups based on the samples they were administered: water, pansildil (P-CON), 5NC, and 2NC. Samples were administered orally once a day at a fixed time for four weeks. Both ALP and ${\gamma}eeksactivity$ increased in the 5NC group compared with the 2NC group. In macroscopic observation, the P-CON group grew the most and were most similar to the state before shaving. The 5NC group grew hair similar to the P-CON group. In all the results, the 5NC group showed greater antioxidative and hair-growth-promotion effects than the 2NC group. Consequently, 5NC could be used as an ingredient for hair-growth promotion.

Physiological Activities of Saccharified Cherry Tomato Gruel Containing Different Levels of Cherry Tomato Puree (방울토마토 첨가량을 달리한 당화 방울토마토죽의 항산화 및 ACE 저해 효과)

  • Kim, Jin Sook;Kim, Ja Young;Chang, Young Eun
    • Korean journal of food and cookery science
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    • v.28 no.6
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    • pp.773-779
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    • 2012
  • This study was conducted to investigate the physiological activities of saccharified cherry tomato gruel containing different levels(0, 15, 30, and 45%) of cherry tomato puree. The total phenolic compound and flavonoids contents of saccharified cherry tomato gruel with cherry tomato puree were 1.73-5.09 mg/g and 0.28-7.01 mg/g, respectively. DPPH radical scavenging activities of saccharified cherry tomato gruel with cherry tomato puree were 8.67-92.58%, respectively. The ABTS radical scavenging activities of saccharified cherry tomato gruel with cherry tomato puree ranged from 6.02 to 61.59%. The ACE inhibitory activity of cherry tomato rice gruel increased with cherry tomato puree showed a range of 38.85-62.15%, respectively. With increasing additions of cherry tomato puree, the total phenolic compound and flavonoid contents, DPPH and ABTS radical scavenging activities and, ACE inhibitory activities were increased significantly (p<0.05). In conclusion, saccharified cherry tomato gruel could be used as a gruel processing method to in order to increase the functional values of gruels.

Marker compound contents and antioxidant capacities of the taproot and lateral root of Danshen (Salvia miltiorrhiza Radix)

  • Seong, Gi-Un;Chung, Shin-Kyo
    • Journal of Applied Biological Chemistry
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    • v.63 no.1
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    • pp.23-28
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    • 2020
  • In this study, the marker compound contents of both the taproot and lateral root of Danshen (Salvia miltiorrhiza Radix), which is cultivated in Korea, were investigated. The salvianolic acid B content was the highest in the taproot (5.17-6.75%) and lateral root (3.99-5.69%). The cryptotanshinone, tanshinone I, and tanshinone IIA contents were higher in the lateral root than in the taproot of Danshen (p <0.05). Principal component analysis results revealed that the taproot was correlated to the salvianic acid A, rosmarinic acid, salvianolic acid B, and salvianolic acid A contents, whereas the lateral root was correlated to the cryptotanshinone, tanshinone I, and tanshinone IIA contents. The total phenolic content and total flavonoid content of the taproot were higher than those of the lateral root (p <0.05); however, the antioxidant activities of the taproot and lateral root of Danshen were similar. The salvianolic acid B content was correlated to the TPC of the taproot (r=0.748) and the 2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid radical scavenging activity of the lateral root (r=0.847). This study could provide useful information for the classification of Danshen as a herbal medicinal product.

Preparation of Functional Food in Combination of Tartary Buckwheat and Bean Flour Mixes by Hot Melt Extrusion Process

  • Azad, Obyedul Kalam;Kang, Wie Soo;Park, Cheol Ho
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2018.04a
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    • pp.71-71
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    • 2018
  • The aim of this study was to prepare a new functional food with enriched bioactive compound by the combination of Tartary buckwheat and bean flour mixes. Two types of bean such as: black bean and white bean with the ratio of 5, 10, 15 % were used to develope a food formulation. The solid formulation of functional food was prepared by the hot melt extrusion process (HME) at the temperature of 60, 90, $120^{\circ}C$. Total phenolic content (TPC), total flavonoid (TF) and DPPH were analysed of the prepared food by the use of spectrophotometer. Results demonstrated that TPC (254 mg/g), TF (18.22 mg/g) and DPPH (88%) were significanlty increased in the receipe of 10% black bean and 90% Tartary buckwheat mixes among the formulation at $90^{\circ}C$. As therefore, it is concluded that the optimum ratio of bean and Tartary buckwheat flour mixes should be considerd for the preparation of high quality functional food.

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Polyphenol Contents of Rumex crispus Root Extract with Hot Water and its Antioxidative Effect (소리쟁이 뿌리 열수 추출물의 폴리페놀 함량 및 추출물의 항산화 효과)

  • Yun, Young-Sim;Jeong, Kap-Seop
    • Journal of Environmental Science International
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    • v.21 no.10
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    • pp.1265-1274
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    • 2012
  • This study was conducted to investigate the extraction characteristics including total polyphenol compound content (TPC) and the antioxidative effect of Rumex crispus root extract on commercial corn oil. Extraction yield was increased with extraction temperature but decreased with extraction ratio. No significant differences in aromatics content were found among the extracts prepared with various extraction conditions; extraction ratio, extraction temperature, extraction pH and composition of extractant. Total flavonoid content of the extract was increased with extraction temperature and extraction pH, and highest value of it was found when extractant composition of ethanol in water was 75%. Total polyphenol compound content (TPC) of the extract with 10 fold extraction ratio showed the highest value, but no significant difference in TPC was found with extraction temperature. Reducing power and DPPH (${\alpha}$,${\alpha}$-diphenyl-${\beta}$-picrylhydrazyl) radical scavenging ability (RSA) of the extract in spectrophotometric absorbance were decreased with extraction ratio but increased with extraction temperature and showed 63.1%~98.4% and 67.6%~86.7% of those of ascorbic acid in reducing power and DPPH RSA, respectively. The antioxidative effects of the extract on corn oil were 84.8~93.0% of that of commercial butylated hydroxytoluene, the antioxidant index value was highest when the ethanol composition to water in extractant was equal ratio.

Anti-cancer Effects of Luteolin and Its Novel Mechanism in HepG2 Hepatocarcinoma Cell (루테올린의 간암세포 성장 억제효능 및 새로운 작용기전)

  • Hwang, Jin-Taek;Yang, Hye-Jung
    • KSBB Journal
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    • v.25 no.6
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    • pp.507-512
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    • 2010
  • In this study, we investigated the ability of luteolin, a plant derived flavonoid on hepatocarcinoma cell growth using HepG2 cell culture system. We found that luteolin increased the Smac/DIABLO releases, a mitochondrial protein that potentiates apoptosis. Luteolin also induced either transcriptional activity or expression of PPAR-gamma, a target of cancer growth that PPAR-gamma agonist sensitizes to apoptosis in certain cancer types. To find the possible upstream target molecules of PPAR-gamma activated by luteolin treatment, we used compound C, a specific inhibitor of AMP-activated protein kinase. Pre-treatment of Compound C significantly restored the activation or expression of PPAR-gamma stimulated by luteolin. This result indicated that AMPK signaling might be involved in the activation or expression of PPAR-gamma signaling pathway stimulated by luteolin. Moreover, we also found that luteolin inhibited the insulin-stimulated Akt phosphorylation as well as AICAR, a specific AMPK activator. These results propose that luteolin significantly induces cancer cell death through modulating survival signal pathways such as PPAR-gamma and Akt. AMPK signaling pathway may be an upstream regulator for survival signal pathways such as PPAR-gamma and Akt stimulated by luteolin.

Development of the Standard Analytical Methods for Compound Hawthorn Berry 60% Ethanol Extract, Ginkgo Biloba Leaf Extract and Garlic Oil Capsules (복방서양산사60%에탄올엑스.은행엽엑스.마늘유캡슐의 기준 및 시험법과 규격 설정)

  • Cho, Chang-Hee;Kim, Ji-Sun;Whang, Ji-Sang;Baek, Ju-Hyun;Park, Ju-Young;Shim, Young-Hoon;Seong, Rack-Seon;Kim, Dong-Sup;Lee, Jong-Phill;Lee, Joo-Hyeun;Sohn, Su-Jung
    • Korean Journal of Pharmacognosy
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    • v.41 no.1
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    • pp.67-72
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    • 2010
  • In the recent version of the Korea Pharmacopoeia(KP) and the Korean Herbal Pharmacopoeia(KHP), there are 563 items(181 in KP, 381 in KHP) of herbal medicines including finished drugs. Also, approximately 507 items including herbal extracts and herbal medicinal products was published in the 3th edition of Korea Pharmaceutical Codex (KPC). These items help the persons working in the pharmaceutical manufacturing field to register the drug and in research fields to develop the new drug considering as a standard specifications. This study was carried out to establish standard analytical methods for 'Compound Hawthorn Berry 60% Ethanol Extract, Ginkgo Biloba Leaf Extract and Garlic Oil Capsules' in the 3th edition of Korea Pharmaceutical Codex. Ginkgo flavonoid and terpene lactone were employed as reference compounds for analytical method. Analytical methods established in this study could be applied to a reasonable and unified quality control of G. biloba leaf extract and hawthorn berry extract.

Safflower Seed Oil and Its Active Compound Acacetin Inhibit UVB-Induced Skin Photoaging

  • Jeong, Eun Hee;Yang, Hee;Kim, Jong-Eun;Lee, Ki Won
    • Journal of Microbiology and Biotechnology
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    • v.30 no.10
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    • pp.1567-1573
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    • 2020
  • Ultraviolet (UV) is one of the major factors harmful to skin health. Irradiation with ultraviolet accelerates the decline of skin function, causing the skin to have deep wrinkles, dryness, decreased procollagen production, and degradation of collagen. Novel materials are needed to prevent the aging of the skin by blocking the effects of UV. Safflower seed oil (Charthamus tinctorius L., SSO) contains significantly high levels of unsaturated fatty acids and phytochemicals. SSO has been traditionally used in China, Japan, and Korea to improve skin and hair. Our objective in this study was to determine the effect of SSO and its active compound acacetin on UVB-induced skin photoaging in HaCaT cells and human dermal fibroblasts (HDF). SSO inhibited UVB-induced matrix metalloproteinase-1 (MMP-1) at both protein and mRNA levels in HaCaT cells and HDF. MMP-1 is known to play important roles in collagen degradation and wrinkle formation. Acacetin, a type of flavonoid, is present in SSO. Similar to SSO, acacetin also inhibited UVB-induced MMP-1 protein and mRNA levels in HaCaT cells and HDF. MMP-1 mRNA is primarily regulated by the mitogen-activated kinase (MAPK) signaling pathway. Acacetin regulated the phosphorylation of JNK1/2 and c-jun, but did not inhibit the phosphorylation of ERK1/2, p38 and AKT. Taken together, these results indicate that SSO and its active compound acacetin can prevent UVB-induced MMP-1 expression, which leads to skin photoaging, and may therefore have therapeutic potential as an anti-wrinkle agent to improve skin health.

Antioxidant Properties and Quality Characteristics of Dasik Supplemented with Longanae Arillus (용안육 다식의 항산화 활성 및 품질 특성)

  • Yang, Eun Young;Han, Young Sil;Sim, Ki Hyeon
    • The Korean Journal of Food And Nutrition
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    • v.31 no.4
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    • pp.485-494
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    • 2018
  • This study was designed to evaluate the quality characteristics and antioxidant properties of Longanae Arillus powder (added in the ratios of 0%, 25%, 50%, 75%, and 100%), which is traditionally used to render the product more suited to the modern consumer's taste for the compound Longanae Arillus Dasiks. As the consumer consumption of the proportions of Longanae Arillus increases, the moisture content and pH of the Dasik supplemented with Longanae Arillus decrease, while at the same time, a soluble solid content increases (p<0.001). The color value showed the decrease in L and b values with the increase in Longanae Arillus content, and the increase in the value of the compound with the addition of Longanae Arillus (p<0.001) can be noted. The mechanical texture of Dasik was increased by the addition of Longanae Arillus considering its hardness, adhesiveness, cohesiveness, springiness, and chewiness (p<0.001). In the sensory evaluation of the Longanae Arillus Dasik showed that people expressed an overall preference at the addition of Longanae Arillus, such as noted as being preferred with 50% in color, flavor, taste, texture, and overall acceptance of the compound (p<0.001). Regarding the antioxidant activity of Longanae Arillus Dasik, the total phenolic, flavonoid contents, DPPH radical scavenging activity, reducing power, and superoxide anion levels were found to increase with the addition of Longanae Arillus (p<0.001) with its consumer use. It is believed that Longanae Arillus Dasik, is most preferred to be added at the concentration of 50% during the Dasik preparation.