• Title/Summary/Keyword: lignan

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Quantification of Fargesin in Mouse Plasma Using Liquid Chromatography-High Resolution Mass Spectrometry: Application to Pharmacokinetics of Fargesin in Mice

  • Lee, Min Seo;Lim, Chang Ho;Bang, Young Yoon;Lee, Hye Suk
    • Mass Spectrometry Letters
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    • v.13 no.1
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    • pp.20-25
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    • 2022
  • Fargesin, a tetrahydrofurofuranoid lignan isolated from Flos Magnoliae, shows anti-inflammatory, anti-oxidative, anti-allergic, and anti-hypertensive activities. To evaluate the pharmacokinetics of fargesin in mice, a sensitive, simple, and selective liquid chromatography-high resolution mass spectrometric method using electrospray ionization and parallel reaction monitoring mode was developed and validated for the quantification of fargesin in mouse plasma. Protein precipitation of 6 µL mouse plasma with methanol was used as sample clean-up procedure. The standard curve was linear over the range of 0.2-500 ng/mL in mouse plasma with the lower limit of quantification level at 0.2 ng/mL. The intra- and inter-day coefficient variations and accuracies for fargesin at four quality control concentrations including were 3.6-11.3% and 90.0-106.6%, respectively. Intravenously injected fargesin disappeared rapidly from the plasma with high clearance values (53.2-55.5 mL/min/kg) at 1, 2, and 4 mg/kg doses. Absolute bioavailability of fargesin was 4.1-9.6% after oral administration of fargesin at doses of 1, 2, and 4 mg/kg to mice.

Inhibitory Effects of Dietary Schisandra Supplements on CYP3A Activity in Human Liver Microsomes

  • Kang, Bae-Gon;Park, Eun-Ji;Park, So-Young;Liu, Kwang-Hyeon
    • Mass Spectrometry Letters
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    • v.13 no.4
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    • pp.152-157
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    • 2022
  • Schisandra chinensis and its fruits have been used as a traditional herbal medicine to treat liver dysfunction, fatigue, and chronic coughs. Several in vitro and in vivo studies suggested that dibenzocyclooctadiene lignans present in Schisandra fruits strongly inhibit CYP3A4 activity. However, reports on the inhibitory potential of dietary Schisandra supplements against CYP3A activity are limited despite their increasing consumption as dietary supplements. In this study, we evaluated the CYP3A-inhibitory potential of four dietary Schisandra supplements in human liver microsomes. At a concentration of 0.05 mg/mL, Schisandra supplements from Nature's Way, Swanson, Planetary Herbals, and Only Natural inhibited CYP3A activity by 93.9, 70.8, 33.6, and 24.8%, respectively. Nature's Way, which exhibited the strongest inhibition against CYP3A, had the highest contents of gomisin B and gomisin C, which potently inhibit CYP3A activity. The in vivo pharmacokinetics of this product should be examined to determine whether the clinical relevance of inhibiting CYP3A activity by dietary Schisandra supplementation.

Polyphenol mixture of a native Korean variety of Artemisia argyi H. (Seomae mugwort) and its anti-inflammatory effects

  • Seong Min Kim;Soo Jung Lee;Venu Venkatarame;Gowda Saralamma;Sang Eun Ha;Preethi Vetrivel;Kebede Taye Desta;Jin Young Choi;Won Sup Lee;Sung Chul Shin;Gon-Sup Kim
    • International Journal of Molecular Medicine
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    • v.44 no.5
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    • pp.1741-1752
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    • 2019
  • In the present study, a polyphenolic mixture was isolated from Seomae mugwort (SM; a native Korean variety of Artemisia argyi H.) via extraction with aqueous 70% methanol followed by the elution of ethyl acetate over a silica gel column. Each polyphenolic compound was analyzed using high-performance liquid chromatography coupled with tandem mass spectrometry, and compared with the literature. In addition to the 14 characterized components, one hydroxycinnamate, six flavonoids, and one lignan were reported for the first time, to the best our knowledge, in Artemisia argyi H. The anti-inflammatory properties of SM polyphenols were studied in lipopolysaccharide-treated RAW 264.7 macrophage cells. The SM polyphenols attenuated the activation of macrophages via the inhibition of nitric oxide production, nuclear factor-κB activation, the mRNA expression of inducible nitric oxide synthase, tumor necrosis factor α and interleukin-1β, and the phosphorylation of mitogen-activated protein kinase. Our results suggested that SM polyphenols may have therapeutic potential for the treatment of inflammatory-related diseases.

Medicinal Components in Bupleurum Species (시호의 약리성분 특성)

  • Kim, Kwan-Su;Lee, Seung-Tack;Chae, Young-Am
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.41 no.spc1
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    • pp.123-144
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    • 1996
  • This review deals briefly with the various medicinal components(mainly saikosaponins), their biological activities and the variation of their contents by different cultivation environment and plant parts in Bupleurum species. Bupleuri radix, a crude drug, is the root of Bupleurum falcatum L. (Korea, Japan), B. chinense(China), and their related species (Umbelliferae). There are over 120 species in Bupleurum genus throughout world, mainly Asian area, and over 5 species in Korea, investigated up to now. These plants contain many physiological active compounds and the principal components are saikosaponins. Major activities of this crude drug and saikosaponins are the anti-inflammatory and antihepatotoxic activities. Saikosaponins and their derivatives in Bupleurum spp. have been chemically studied, isolated and identified over 70 compounds in over 50 species. Other components, physiologically active ones, also have been investigated, which are the groups of lignan, flavonoid, essential oil, polyacetylene, polysaccharide, etc. Saikosaponins belong to the group of triterpenoid saponin chemotaxonomically and occur the accumulation and turnover in plant tissues through secondary metabolism, mevalonic acid pathway. The contents and kinds of saikosaponins and other components in Bupleurum spp. plants are various due to different species and growing environments, as the plant growth characters and yield are various. Most of medicinal plants as well as Bupleurum species are very useful as agricultural products and traditional medicines, and also are very valuable as genetic resources and natural products. So we need to collect, evaluate, preserve, and utilize various medicinal plants, and also to under-stand secondary metabolism and improve the breeding and cultivation techniques for the safe production of crude drugs with high quality and yielding.

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Hepatoprotective Activities of Gomisin A and Gomisin N (Gomisin A 및 Gomisin N의 간독성 보호작용)

  • Heo Jeong-Haing;Park Jin-Gu;Cheon Ho-Jun;Kim Yeong-Shik;Kang Sam-Sik;Hung Tran Manh;Bae Ki-Hwan;Lee Sun-Mee
    • Korean Journal of Pharmacognosy
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    • v.37 no.4 s.147
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    • pp.294-301
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    • 2006
  • The aim of this study was to investigate the protective activity of gomisin A and gomisin N, bioactive lignan components isolated from Schizandae Fructus, on hepatocyte injury induced by carbon tetrachloride($CCl_4$, 10 mM), t-butyl hydroperoxide(TBH, 0.5 mM), and D-galactosamine(GalN, 30 mM). Primary cultures of rat hepatocyte(18 h culture) were treated with $CCl_4$, TBH or GalN and various concentrations(0.1, 1, 10, $100{\mu}M$) of gomisin A or gomisin N. $CCl_4$ significantly increased the levels of lactate dehydrogenase(LDH), alanine aminotransferase(ALT), and aspartate aminotransferase(AST). These increases were inhibited by gomisin N. TBH significantly increased the level of AST; an increase that was inhibited by gomisin N. GalN markedly increased the levels of LDH and ALT, and these increases was significantly inhibited by both gomisin A and gomisin N. These results suggest that gomisin A and gomisin N have the hepatoprotective activity.

Antioxidant and Synergistic Effect of Sesame Oil Cake Extract Treated from $\beta$-Glucosidase ($\beta$-Glucosidase 처리된 참깨박 추출물의 항산화 및 상승효과)

  • 손종연;강동우;신길만
    • The Korean Journal of Food And Nutrition
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    • v.14 no.6
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    • pp.591-595
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    • 2001
  • The antioxidant and synergistic effects of sesame oil cake extract treated with $\beta$ -glucosidase were examined. The sesamin and sesamolin were identified from the 80% ethanol extract of seame oil cake treated with $\beta$ -glucosidase, which suggested the presence of the active substances as their glycosides in sesame seed. The contents of sesamin and sesamolin in sesame oil cake extract were about 8.32% (8,315.4 mg/100g) and 0.28% (2,824.5mg/100g) , respectively. Sesame oil cake extract showed antioxidant activity at concentrations of 50ppm, 100ppm and 200ppm, and the effect was Increased with the addition of sesame oil cake extract. The antioxidant effect of sesame oil cake extract was stronger than that of $\alpha$-tocopherol or ascorbyl palmitate, but weaker than of BHT Also, when the sesame oil cake extract(50ppm) was used in combination with $\alpha$-tocopherol(50 ppm), the sesame oil cake showed very strong synergistic effect.

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The Study of Pytoestrogen Intake and Bone Mineral Density of Vegetarian and Nonvegetarian Postmenopausal Women (채식과 일반식 폐경 후 여성의 식물성 에스트로겐 섭취와 골밀도와의 관련성)

  • 김미현;최미경;승정자
    • Korean Journal of Community Nutrition
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    • v.9 no.1
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    • pp.66-72
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    • 2004
  • There is some evidence that phytostrogen plays an important role in bone metabolism in postmenopausal women. In this study, we investigated the phytoestrogen intake levels and the relation between dietary phytoestrogens intake and bone mineral density of vegetarian (n = 77) and omnivore postmenopausal women (n = 122 . Vegetarian women, all of them were seven day adventists, who had been on vegetarian diet (almost lacto-ovo vegetarians;a few vegans) oyer 20 yrs. The average age of vegetarians and omnivores were 62.3 yrs and 60.2 yrs, respectively and, there was no significant difference. However, body weight (p < 0.001), body mass index (p < 0.001) of vegetarians were significantly lower than those of omnivores. The mean daily energy intake of vegetarians and omnivores were 1386.1 kcal (76.3% of RDA) and 1424.5 kcal (76.9% of RDA), respectively. The mean calcium intake of vegetarians (456.7 mg, 66.3 % of RDA) was not significantly different from that of omnivores (453.5 mg, 65.2 % of RDA). The mean daily isoflavones (daidzein +genistein) intake of vegetarians and omnivore were 33.9 mg and 23.9 mg, respectively. The vegetarians consumed significantly greater quantities of isoflavones (p < 0.05) and lignans precursor (p < 0.05). In the vegetarians, intake of isoflavones was significantly positively correlated with BMD of femoral neck, after adjusted for age and BMI. Also lignan precursor intake of vegetarians was significantly positively correlated with BMD of spine, after adjusted for age and BMI. In conclusion, in omnivore post menopausal women, intake of phytoestrogen such as isoflavones and lignans was little low, and it is not clear that positive association with bone mineral density. But in vegetarian postmenopausal women, phytoestrogen intakes be important factors related to bone mineral density.

Intake of dietary phytoestrogen and indices of antioxidant and bone metabolism of pre- and post-menopausal Korean women

  • Jang, Jeong-Hee;Yoon, Ji-Young;Cho, Sung-Hee
    • Nutrition Research and Practice
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    • v.1 no.4
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    • pp.305-312
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    • 2007
  • A group of 101 women, aged 40-65 years consisted of 48 premenopausal subjects and 53 postmenopausal ones living in Daegu and Gyeongbuk area in Korea were evaluated with their general characteristics, lifestyle factors, nutrient and phytoestrogen intakes, blood and urinary indices concerning antioxidant status and bone metabolism. Body mass index (BMI), waist hip ratio (WHR) and systolic blood pressure (SBP) of the postmenopausal women were significantly higher (23.8, 0.86, and 126.9 mmHg, respectively) than those of the premenopausal women (22.6, 0.82, and 115.9 mmHg; respectively). Nutrient intakes of the postmenopausal and premenopausal groups were not different except lower fat intake and higher dietary fiber and iron intakes in the postmenopausal group. Daily total phytoestrogen intake was significantly higher in the postmenopausal group (48.54 mg) than the premenopausal (31.41 mg) and was resulted mostly from higher intakes of daidzein and genistein from soy and soy products (45.42 mg vs 28.91 mg). Serum genistein level and excretion of enterolactone, major lignan metabolite, were not very different between the two groups. Serum retinal and ${\alpha}$- tocopherol levels were higher in the postmenopausal group but TBARS levels were not different between the two groups. Serum osteocalcin (7.18 ng/mL) and urinary deoxypyridinoline (7.15 nmol/mmol creatinine), in the postmenopausal group were significantly higher than those in the premenopausal group (4.80 ng/mL, 5.95 nmol/mmol creatinine). Urinary excretion of enterolactone was positively correlated with serum osetocalcin in premenopausal women and serum genistein negatively correlated with the urinary DPD in postmenopausal women. Dietary phytoestrogen intake was negatively correlated with serum level of TBARS in all subjects. It is concluded that the effect of total phytoestrogen intake is beneficial on body antioxidant status in all middle-aged women regardless of menopause but the effect on bone metabolism appears different by the type of the phytoestrogen and the menopausal state.

Correlation among Growth Characteristics according to the Cultivated Years of Saururus chinensis BAILL. (재배년수에 따른 삼백초(三白草)의 생육형질간 상관관계)

  • Nam Sang-Young;Kim Min-Ja;Yun Tae;Kim Hong-Sig;Jong Seung-Keun;Kim In-Jae
    • Korean Journal of Plant Resources
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    • v.19 no.2
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    • pp.248-251
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    • 2006
  • The growth of stem and leaves in Saururus chinensis. in the 2nd year was markedly increased comparing to that in the 1st year, however the growth in the 3rd you was not increased significantly. The growth in the 1st yew was greater in low planting density, while the growth in the 3rd year decreased in higher planting densities. The num- ber of leaves and stems per unit area increased in higher planting densities and later years. The weight of stem and leaves in Saururus chinensis was higher at the highest planting density in the 1st yew, at $40{\times}10cm$ planting in the 2nd year and at $40{\times}20cm$ planting in the 3rd year. The weight of rhizome in Saururus chinensis increased greatly in the 2nd you comparing to that in the 1st year, but the increase was insignificant in the 3rd year. The weight of rhizomes in Saururus chinensis showed significant interaction between planting densities and years showed highly significant difference.

Inhibitory Effects of Phylligenin on the Proliferation of Cultured Rat Neural Progenitor Cells

  • Lee, Sung-Hoon;Go, Hyo-Sang;Choi, Chang-Soon;Cheong, Jae-Hoon;Han, Sun-Young;Bae, Ki-Hwan;Ko, Kwang-Ho;Park, Seung-Hwa
    • Biomolecules & Therapeutics
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    • v.18 no.1
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    • pp.48-55
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    • 2010
  • Neural progenitor cells (NPCs) differentiate into astrocytes, neurons and oligodendrocytes, which is controlled by various factors in brain. Recent evidences suggest that small molecules modulating the proliferation and differentiation of NPCs may have therapeutic value as well as the potential use as chemical probes. Phylligenin is a lignan with anti-inflammatory activity that is isolated from the fruits of Forsythia koreana. We investigated effects of phylligenin on proliferation and differentiation of NPCs. Treatment of phylligenin decreased the number of proliferating NPCs in culture without effects on the differentiation and survival of neural cells such as neurons and astrocytes. To examine the mechanism of the decreased NPCs number, we performed cell cycle analysis. Proliferation of NPCs was decreased via G1-S transition block by phylligenin treatment, and it was mediated by the increase of p21 level. However, phylligenin did not induce apoptosis of NPCs as determined by TUNEL assay and PARP cleavage. We also found that viability of glioma cell lines such as C6 and U87MG glioma cells, but not that of primary neuron and astrocyte, was inhibited by phylligenin. These results suggest that phylligenin selectively inhibits proliferation of rapidly growing cells such as neural stem cells and glioma cells. Given that the possible role of brain tumor stem cells in the pathology of brain cancers, the inhibitory effects of phylligenin might be useful in the development of new therapeutic agents against brain cancers.