• Title/Summary/Keyword: betulinic acid

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Effect of Root Extract of Lythrum salicaria L. on Liver Function of Rat Acutely Administrated with Alcohol (털부처꽃 뿌리 추출물의 단회투여가 급성 알코올 투여 흰쥐의 간기능에 미치는 영향)

  • Lee, Seung-Eun;Lee, Jeong-Hoon;Kim, Geum-Soog;Hong, Yoon-Pyo;Noh, Hyung-Jun;Park, Chun-Geun;Kim, Seung-Yu
    • Korean Journal of Medicinal Crop Science
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    • v.20 no.5
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    • pp.345-352
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    • 2012
  • This experiment was conducted to verify whether one time feeding of Lythrum salicaria root crude extract (LSR extract) exhibits liver protecting activities in acutely ethanol administrated rat. Experiment groups were composed of normal, negative control (alcohol control), 2 positive control (Hovenia dulcis extract 900 mg/kg and milk thisle 100 mg/kg), betulinic acid (20 mg/kg), a compound separated from LSR, and 3 LSR (100, 300, 900 mg/kg) groups. LSR treated groups showed decrease (p < 0.05) in serum triglyceride by dose-dependent manner. The content of serum albumin and the activity of ADH and ALDH in LSR extract fed rats were increased (p < 0.05) dependently on the administration amounts. Our study indicated that one time supplement of LSR downregulates oxidative stress and shows liver protective activity in the acute alcohol-fed rats.

Topoisomerase I and II Inhibitory Activities and Cytotoxic Constituents from the Barks of Tilia amurnesis

  • Piao, Dong Gen;Lee, You-Jeong;Seo, Chang-Seob;Lee, Chong-Soon;Kim, Jae-Ryong;Chang, Hyun-Wook;Son, Jong-Keun
    • Natural Product Sciences
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    • v.17 no.3
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    • pp.245-249
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    • 2011
  • Eight compounds, squalene (1), friedelin (2), ${\beta}$-sitosterol (3), ${\beta}$-sitosterol-3-O-glucoside (4), ${\alpha}$-tocopherol (5), betulinic acid (6), trilinolein (7) and 1-O-(9Z,12Z-Octadecadienoyl)-3-nonadecanoyl glycerol (8), were isolated from the barks of Tilia amurensis. Their chemical structures were identified by comparing their physicochemical and spectral data with those published in the literature. These isolated compounds were examined for their inhibitory activities against topoisomerase I and II. Compound 7 showed significant inhibition of DNA topoisomerase I and II activities, with percent decreases in activity of 87 and 95%, respectively at a concentration of $100\;{\mu}M$. Compound 6 exhibited cytotoxicity against the human colon adenocarcinoma cell line (HT-29), the human breast adenocarcinoma cell line (MCF-7) and the human liver hepatoblastoma cell line (HepG-2), with $IC_{50}$ values of 20, 59 and $16\;{\mu}M$, respectively.

Cytotoxic and Antioxidant Compounds Isolated from the Cork of Euonymus alatus Sieb.

  • Jeong, Su Yang;Zhao, Bing Tian;Kim, Young Ho;Min, Byung Sun;Woo, Mi Hee
    • Natural Product Sciences
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    • v.19 no.4
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    • pp.366-371
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    • 2013
  • Seventeen compounds (1 - 17), ${\beta}$-sitosterone (1), lupenone (2), arborinone (3), ${\beta}$-sitosterol (4), lupeol (5), epi-lupeol (6), taraxerol (7), betulinic acid (8), 24R-methyllophenol (9), germanicol (10), hexatriacontane (11), nonacosan-1-ol (12), benzoic acid (13), tetradecyl(E)-ferulate (14), di(2-ethylhexyl) phthalate (15), trilinolein (16) and monopalmitin (17), were isolated from the methylene chloride-soluble fraction of the cork of Euonymus alatus Sieb. The structures of these compounds were elucidated on the basis of spectroscopic evidence. Compounds 6, 11, 13 and 14 were isolated for the first time from this plant. Compound 4 showed moderate cytotoxic activity with an $IC_{50}$ value of 6.22 ${\mu}M$ in HL-60 cell line. Compound 9 exhibited moderate cytotoxic activity with $IC_{50}$ values of 63.31, 15.45, 15.14 and 21.72 ${\mu}M$ in four kinds of human cancer cell lines, Jurkat T, HeLa, HL-60 and MCF-7, respectively. Compound 17 showed moderate cytotoxic activity with an $IC_{50}$ value of 70.71 ${\mu}M$ in Jurkat T cell line. In addition, compounds 2, 3, 14 and 16 exhibited weak antioxidant activity with $IC_{50}$ values of 151.76, 170.79, 137.46 and 139.37 ${\mu}M$, respectively.

Antioxidant value and Antiproliferative Efficacy of Mitragynine and a Silane Reduced Analogue

  • Goh, Teik Beng;Yian, Koh Rhun;Mordi, Mohd Nizam;Mansor, Sharif Mahsufi
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.14
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    • pp.5659-5665
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    • 2014
  • Background: To investigate the antioxidant value and anticancer functions of mitragynine (MTG) and its silane-reduced analogues (SRM) in vitro. Materials and Methods: MTG and SRM was analyzed for their reducing power ability, ABTS radical inhibition and 1,1-diphenyl-2-picryl hydrazylfree radicals scavenging activities. Furthermore, the antiproliferation efficacy was evaluated using MTT assay on K 562 and HCT116 cancer cell lines versus NIH/3T3 and CCD18-Co normal cell lines respectively. Results: SRM and MTG demonstrate moderate antioxidant value with ABTS assay (Trolox equivalent antioxidant capacity (TEAC): $2.25{\pm}0.02$ mmol trolox / mmol and $1.96{\pm}0.04$ mmol trolox / mmol respectively) and DPPH ($IC_{50}=3.75{\pm}0.04mg/mL$ and $IC_{50}=2.28{\pm}0.02mg/mL$ respectively). Both MTG and SRM demonstrate equal potency ($IC_{50}=25.20{\pm}1.53$ and $IC_{50}=22.19{\pm}1.06$ respectively) towards K 562 cell lines, comparable to control, betulinic acid (BA) ($IC_{50}24.40{\pm}1.26$). Both compounds showed concentration-dependent cytototoxicity effects and exert profound antiproliferative efficacy at concentration > $100{\mu}M$ towards HCT 116 and K 562 cancer cell lines, comparable to those of BA and 5-FU (5-Fluorouracil). Furthermore, both MTG and SRM exhibit high selectivity towards HCT 116 cell lines with selective indexes of 3.14 and 2.93 respectively compared to 5-FU (SI=0.60). Conclusions: These findings revealed that the medicinal and nutitional values of mitragynine obtained from ketum leaves that growth in tropical forest of Southeast Asia and its analogues does not limited to analgesic properties but could be promising antioxidant and anticancer or chemopreventive compounds.

Triptolide Inhibits Lipopolysaccharide-Induced MUC5AC/5B Expression via Nuclear Factor-Kappa B in Human Airway Epithelial Cells (사람 호흡기 상피세포에서 Triptolide의 Nuclear Factor-Kappa B를 통한 Lipopolysaccharide로 유도된 MUC5AC/5B 발현 억제 효과)

  • Seo, Bo Hyeon;Choi, Tae Yeong;Choi, Yoon Seok;Bae, Chang Hoon;Na, Hyung Gyun;Song, Si-Youn;Kim, Yong-Dae
    • Korean Journal of Otorhinolaryngology-Head and Neck Surgery
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    • v.61 no.12
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    • pp.674-680
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    • 2018
  • Background and Objectives The representative mucin genes in the human airway are MUC5AC and MUC5B, which are regulated by several inflammatory and anti-inflammatory substances. Triptolide (TPL), udenafil, betulinic acid, changkil saponin, and glucosteroid are some of the many anti-inflammatory substances that exist. TPL is a diterpenoid compound from the thunder god vine, which is used in traditional Chinese medicine for treatment of immune inflammatory diseases, such as rheumatoid arthritis, systemic lupus erythematosus, nephritis and asthma. However, the effects of TPL on mucin expression of human airway epithelial cells have yet to be reported. Hence, this study investigated the effect of TPL on lipopolysaccharide (LPS)-induced MUC5AC and MUC5B expression in human airway epithelial cells. Subjects and Method The NCI-H292 cells and the primary cultures of human nasal epithelial cells were used to investigate the effects of TPL on LPS-induced MUC5AC and MUC5B expression using real-time polymerase chain reaction, enzyme immunoassay, and Western blot. Results TPL significantly decreased the LPS-induced MUC5AC and MUC5B mRNA expression and protein production. TPL also significantly decreased the nuclear factor-kappa B (NF-kB) phosphorylation. Conclusion These results suggest that TPL down regulates MUC5AC and MUC5B expression via inhibition of NF-kB activation in human airway epithelial cells. This study may provide important information about the biological role of triptolide on mucus-secretion in airway inflammatory diseases and the development of novel therapeutic agents for controlling such diseases.