• Title/Summary/Keyword: FPTase 활성 억제

Search Result 5, Processing Time 0.018 seconds

Effects of Polyacetylenes in Ginseng on Activity of Enzymes Related to Post-translational Modification of Ras Protein and Effects of Petroleum Ether Extract of Ginseng on Progression of Cell Cycle (인삼의 polyacetylene 계 성분이 Ras 단백질 변형 효소의 활성에 미치는 영향과 인삼의 석유에텔 추출물이 세포주기에 미치는 영향)

  • 김동청;이지영;인만진;채희정;황윤경;황우익
    • Journal of Ginseng Research
    • /
    • v.25 no.4
    • /
    • pp.156-161
    • /
    • 2001
  • We investigated the effects of polyacetylenes of ginseng on farnesyl protein transferase (FPTase) and carboxyl methyl transferase (CMTase) activities related to post-translational modification of Ras protein. We also investigated the effect of petroleum ether extract (PEE) of ginseng on progression of cell cycle. FPTase activity was respectively inhibited 16.2% by 10mM panaxynol and 21.3% by 10mM panaxydol, whereas CMTase activity was not inhibited by panaxynol or panaxydol. Treatment of PEE significantly reduced the numbers and size of human colon cancer cell (HT-29) and human liver cancer cell(HepG2) cultured, respectively. To investigate the mechanism of growth inhibition by PEE of ginseng, we analyzed the cell cycle progressions of PT-29 and HepG2 cells, respectively. We found that PEE significantly inhibited progression of cell cycle from G1 to S phase. These results suggest that anticancer effects of PEE were derived from the arrest of G1 phase in cell cycle progression.

  • PDF

FPTase Inhibition Effect of Protostanes from Alismatis Rhizoma and Derivatives from Alisol B 23-acetate (택사 (Alismatis Rhizoma)에서 분리한 Protostane계 화합물과 그 유도체의 FPTase 억제활성)

  • Lee, Sang-Myung;Kwon, Byoung-Mog;Min, Byung-Sun
    • Korean Journal of Pharmacognosy
    • /
    • v.42 no.3
    • /
    • pp.218-222
    • /
    • 2011
  • The purpose of this research is to study of inhibitory activity of protostane type triterpens against farnesyl-protein transferase (FPTase). The ingredients of Alismatis Rhizoma, alisol B 23-acetate, C 23-acetate, alisols B and A 24-acetate, and thirteen synthetic analogues from alisol B 23-acetate exhibited inhibition activity against FPTase by scintillation proximity assay method. As a result, alisol C 23-acetate, one of the constituents of Alismatis Rhizoma, the synthetic analogues carboxylated and hydroxylated on branch chain of protostane exhibited a significant inhibitory activity. However, the compounds significantly lowered the inhibitory activity, when there is no 3 position keto on protostane skeletone.

Development of Biologically Active Compounds from Edible Plant Sources-X. -Isolation of Lipids from the Flower of Campsis grandiflora K. Schum. and their Inhibitory Effect on FPTase- (식용 식물자원으로부터 활성물질의 탐색-X. -능소화(Campsis grandiflora K. Schum.)로부터 지질화합물의 분리 및 FPTase 저해 효과 측정-)

  • Kim, Dong-Hyun;Song, Myoung-Chong;Han, Kyung-Min;Bang, Myun-Ho;Kwon, Byoung-Mog;Kim, Sung-Hoon;Kim, Dae-Keun;Chung, In-Sik;Park, Mi-Hyun;Baek, Nam-In
    • Applied Biological Chemistry
    • /
    • v.47 no.3
    • /
    • pp.357-360
    • /
    • 2004
  • The flower of Campsis granudiflora K. Schum. was extracted with 80% aqueous MeOH, and the concentrated extract was partitioned with EtOAc, n-BuOH and $H_2O$. From the EtOAc fraction, four compounds were isolated through the repeated silica gel and ODS column chromatographies. From the result of physico-chemical data including NMR, MS and IR, the chemical structures of the compounds were determined as linolenic acid methyl ester, linoleic acid methyl ester, ${\beta}-sitosterol$ and daucosterol. Daucosterol inhibited FPTase activity with $IC_{50}$ values of $14{\pm}0.04\;{\mu}M$.

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
    • /
    • v.47 no.2
    • /
    • pp.251-257
    • /
    • 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.

Anti-cancer Activity of Flavonoids from Aceriphyllum rossii (돌단풍(Aceriphyllum rossii)에서 분리한 플라보노이드의 항암활성)

  • Ahn, Eun-Mi;Han, Jae-Taek;Kwon, Byoung-Mog;Kim, Sung-Hoon;Baek, Nam-In
    • Applied Biological Chemistry
    • /
    • v.51 no.4
    • /
    • pp.309-315
    • /
    • 2008
  • The methanol extract from the aerial parts of Aceriphyllum rossii was fractionated into ethyl acetate, n-BuOH and $H_2O$ layers through solvent fractionation. Repeated silica gel column chromatography of EtOAc and n-BuOH layers afforded five flavonol glycosides. They were identified as astragalin (1), kaempferol 3-O-${\alpha}$-L-rhamnopyranosyl (1${\rightarrow}$6)-${\beta}$-D-glucopyranoside (2), rutin (3), kaempferol 3-O-${\alpha}$-L-rhamnopyranosyl (1${\rightarrow}$4)-${\alpha}$-L-rhamnopyranosyl 1${\rightarrow}$6)-${\beta}$-D-glucopyranoside (4), and quercetin 3-O-${\alpha}$-L-rhamnopyranosyl (1${\rightarrow}$4)-${\alpha}$-L-rhamnopyranosyl (1${\rightarrow}$6)-${\beta}$-D-glucopyranoside (5) on the basis of spectroscopic data. All of them showed an inhibition in farnesyl protein tranferase (FPTase) activity, and rutin (3) inhibited the growth of rat H-ras cell and the cell migration of human umbilical vein endothelial cells (HUVECs).