• 제목/요약/키워드: farnesyl protein transferase (FPTase)

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Inhibitory Effect of Acetylshikonin from Roots of Lithospermum erythrorhizon on LDL Oxidation and FPTase Activity (지치뿌리로부터 분리한 Acetylshikonin의 LDL 산화 저해활성과 FPTase 저해활성)

  • Kim, Geum-Soog;Jeong, Tae-Sook;Kwon, Byoung-Mok;Kim, Young-Ok;Cha, Seon-Woo;Song, Kyung-Sik;Bek, Nam-In
    • Journal of Applied Biological Chemistry
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    • v.52 no.4
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    • pp.221-225
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    • 2009
  • Lithospermum erythrorhizon has been known well as one of traditional medicine for fever reduction, detoxication, and blood circulation improvement. This study was carried out to isolate biological active compounds from roots of Lithospermum erythrorhizon and to investigate their low density lipoprotein (LDL) antioxidant and anticancer activities. The hexane extract of Lithospermi Radix has been separated on silica gel chromatography and a naphthoquinone pigment compound 1 has been isolated. The structure of the compound 1 has been identified by spectroscopic technique, including MS and NMR, as acetylshikonin (1). Acetylshikonin showed significantly inhibitory activity on $Cu^{2+}$-induced human LDL oxidation with $IC_{50}$ value of $8.8\;{\mu}M$ and obvious anticancer effect by inhibiting farnesyl:protein transferase (FPTase) activity with $IC_{50}$ value of $23\;{\mu}M$, which suggested that acetylshikonin might be useful for the treatment of atherosclerosis and cancer.

Development of Biologically Active Compounds from Edible Plant Sources-XXIV. - Anti-cancer Activity of Alcohol Extracts from Edible Plants - (식용 식물자원으로부터 활성물질의 탐색-XXIV. - 식용 식물 추출물의 항암 활성 -)

  • Kwak, Ho-Young;Kwon, Byoung-Mog;Song, Myoung-Chong;Lee, Jin-Hee;Yang, Hye-Joung;Kim, Dae-Keun;Ahn, Eun-Mi;Baek, Nam-In
    • Korean Journal of Pharmacognosy
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    • v.38 no.4
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    • pp.312-320
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    • 2007
  • The screening of anti-cancer activity for the MeOH extracts of 163 natural sources, which were registered as edible plants by Korea Food & Drug Administration, exhibited 9 extracts to have significant inhibitory effects on farnesyl-protein transferase (FPTase) and phosphatase of regenerating liver-3 (PRL-3). In order to confirm the inhibitory activity of these active extracts, the activity assay was repeated for some fractions obtained from the active extracts using Medium Pressure Liquid Chromatography (MPLC). Some fractions of Carya illinoensis, Chlorella vulgaris, Panicum miliaceum, Perilla frutescens, Rosmarinus officinalis showed over 50% inhibitory activity on FPTase as well as those of Capsella bursa-pastoris, C. illinoensis, C. vulgaris, Coix lacrymajobi, Myristica fragrans, P. miliaceum, R. officinalis did over 50% inhibitory activity on PRL-3.

Inhibitory Activity of Edible Plant Extracts on Proliferation of Human Umbilical Vein Endothelial Cells (HUVECs)

  • Song, Myoung-Chong;Kim, Sung-Hoon;Kwak, Ho-Young;Yang, Hye-Joung;Bang, Myun-Ho;Chung, In-Sik;Lee, Youn-Hyung;Baek, Nam-In
    • Journal of Applied Biological Chemistry
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    • v.50 no.4
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    • pp.249-253
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    • 2007
  • Thirteen edible plants previously reported to show inhibitory activities on farnesyl protein transferase (FPTase) and phosphatase of the regenerating liver-3 (PRL-3) were evaluated for inhibitory activity on the proliferation of human umbilical vein endothelial cells (HUVECs). Four plant extracts, Oenothera erythrosepala, Perilla frutescens, Panicum miliaceum, and Quercus acutissima, significantly inhibited the proliferation of HUVECs induced by the basic fibroblast growth factor (bFGF) without cytotoxicity at 100 ${\mu}g/mL$. Myristica fragrans, Rosmarinus officinalis, and Syringa patula also showed inhibitory activity on the proliferation with only mild cytotoxicity.

Anticoagulation and Anticancer Constituents from Eugenia caryophyllata Thunb

  • Han, Kyung-Min;Kim, Dong-Hyun;Ahn, Eun-Mi;Lee, Youn-Hyung;Chung, In-Sik;Kim, Dae-Keun;Kwon, Byoung-Mog;Kim, Sung-Hoon;Baek, Nam-In
    • Korean Journal of Medicinal Crop Science
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    • v.15 no.2
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    • pp.82-88
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    • 2007
  • From the EtOAc fraction of Eugenia caryophyllata, four compounds were isolated through activity-guided silica gel column chromatography, From the result of spectroscopic data including NMR, MS and IR, the chemical structures of the compounds were determined as 1-allyl-4-hydroxy-3-methoxybezene acetate (eugenol acetate, 1), 1-allyl-4-hydroxy-3-methoxybezene (eugenol, 2), $3{\beta}-hydroxyolean-12-en-28-oic$ acid (oleanolic acid, 3) and $2{\alpha}$, $3{\beta}-dihydroxyolean-12-en-28-oic$ acid (maslinic acid, 4). Compounds 3 and 4 were isolated for the first time from this plant. Also, compounds 1, 2 and 3 exhibited relatively high platelet aggregation inhibitory activity with the $IC_{50}$ values of 0.24, 0.09 and 0.07 mM, respectively. Compound 2 significantly prolonged activated partial thromboplastin time (aPTT) with the value of $124{\pm}11.2$ seconds as compared to the control with the value of $37.5{\pm}2.2$ seconds at the concentration of 50 ${\mu}g/ml$. Compounds 1 and 3 revealed inhibitory activity on farnesyl protein transferase (FPTase) with the $IC_{50}$ values of 0.49 and 0.24 mM and compounds 1 and 2 highly inhibited the growth of rat-H-ras cells with the $Gl_{50}$ values of 6.63 and 5.70 ${\mu}M$, respectively.

Screening of Biologically Active Compound from Edible Plant Sources-IX. Isolation and Identification of Sesquiterpene Lactons Isolated from the Root of Ixeris dentata forma albiflora; Inhibition Effects on ACAT, DGAT and FPTase Activity (식용식물자원으로부터 활성물질의 탐색-IX. 흰씀바귀(Ixeris dentata forma albiflora)뿌리에서 Sesquiterpene Lactone 화합물의 분리 및 구조 동정; ACAT, DGAT 및 FPTase 효소 활성의 저해)

  • Bang, Myun-Ho;Jang, Tae-O;Song, Myoung-Chong;Kim, Dong-Hyun;Kwon, Byoung-Mog;Kim, Young-Kuk;Lee, Hyun-Sun;Chung, In-Sik;Kim, Dae-Keun;Kim, Sung-Hoon;Park, Mi-Hyun;Baek, Nam-In
    • Applied Biological Chemistry
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    • v.47 no.2
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    • pp.251-257
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    • 2004
  • The root of lxeris dentata forma albiflora was extracted with 80% aqueous MeOH and solvent fractionated with EtOAc, n-BuOH and water, successively. From the EtOAc and n-BuOH fractions, four sesquiterpene compounds were isolated through the repeated silica gel and ODS column chromatographies. The chemical structures were determined as zaluzanin C (1), $9{\alpha}-hydroxyguaian-4(l5),10(14),11(13)-triene-6,12-olide$ (2), $3{\beta}-O-{\beta}-D-glucopyranosyl-8{\alpha}-hydroxyguaian-4(15),10(14 )-diene-6,12-olide$ (3), and $3{\beta}-O-{\beta}- D-glucopyranosyl-8{\beta}hydroxyguaian-10(14)-ene-6,12-olide$ (4) through the interpretation of several spectral data including 2D-NMR. Some showed the inhibitory effects on DGAT (Diacylglycerol acyltransferase), ($IC_{50}$ values of 1, 2: 0.13, 0.10 mM), the catalyzing enzymes of the intracellular esterification of diacylglycerol and FPTase (Famesyl-protein transferase), ($IC_{50}$ values of 1, 2: 0.15, 0.18 mM), the farnesylation enzyme for Ras protein charge of cancer promotion.