• 대한약학회:학술대회논문집
• /
• 대한약학회 2001년도 Proceedings of the Pharmaceutical Society of Korea
• /
• pp.90-94
• /
• 2001

Wondonins A and B, aromatic alkaloids of an unprecedented skeletal class have been isolated form and association of the sponges Poecillastra wondoensis and Jaspis sp. In addition, four novel bromotyrosine-derived metabolites, psammaplins $A_1$ and $A_2$, aplysinellins A and B, have been isolated from the tropical sponge Aplysinella rhax. The structures of these compounds have been determined on the basis of combined chemical and spectral analyses. The new compounds exhibited significant cytotoxicity and antiangiogenic activity as well as inhibitory activities against farnesyl protein transferase and leucine aminopeptidase. In addition to these compounds, several bioactive metabolites have been isolated from sponges of Korean and tropical waters.

• 생약학회지
• /
• 제30권1호
• /
• pp.70-73
• /
• 1999

Nine sesquiterpene lactones, which were isolated from Hemisteptia lyrata Bunge. Chrysanthemum zawadskii Herbich var. latilobum Kitamura and Chrysanthemum boreale Makino were evaluated for the farnesyl-protein transferase (FPTase) inhibitor, conducted by the scintillation proximity assay (SPA). The angeloylcumambrin B and tigloylcumambrin B inhibited a recombinant rat FPTase with $IC_{50}$ value of $78\;{\mu}g/ml$ $(225\;{\mu}M)$ and $90\;{\mu}g/ml$ $(260 \;{\mu}M)$, respectively.

• 한국응용약물학회:학술대회논문집
• /
• 한국응용약물학회 1992년도 제1회 신약개발 연구발표회 초록집
• /
• pp.42-42
• /
• 1992

ras oncogene은 암조직이나 transformed human cell line에서 거의 공통적으로 발견되는 oncogene으로서 그 product인 p2l 단백질은 C-terminal 25개의 아미노산 외에는 거의 동일한 배열을 가지고 있는 매우 conservative한 단백질이며 C-terminal cysteine이 carboxy methylation되어 있고 또한 palmitic acid와 같은 long chain fatty acid도 결합되어 있다. 보고된 바에 의하면 p21 protein의 palmitation은 ras protein의 세포막에 대한 친화력을 유지시키며 이와 같은 친화력은 cell transforming activity의 기본요건으로 알려져 있다. 이와 같은 관점에서 볼때 p21 단백질의 C-terminal processing현상을 new drug target으로, 즉 p2l 단백질의 C-terminal processing을 억제하므로서 cell transforming activity를 저해 할 수 있을 것이므로 생체내에 존재하는 p21 단백질 C-terminal processing 억제제의 identification 및 purification은 항암제 연구와 밀접한 관계가 있다. 구체적으로 farnesyl-protein transferase inhibitor 혹은 carboxyl methyl inhibitor의 identification 및 purification은 이같은 목적을 달성 할 수 있는 가능성이 크다.

• Natural Product Sciences
• /
• 제12권4호
• /
• pp.214-216
• /
• 2006

Isorhamnetin from the aerial parts of Persicaria thunbergii has been reported to have anti-tumor activity mediated by the inhibition of farnesyl protein transferase. In this study, we investigated the anti-proliferation effects of isorhamnetin on NIH3T3, K-RAS, H-RAS and SW620 cells, and it showed anti-proliferative effects in a dose-dependent manner with $IC_{50}$ value 4.1, 7.9, 20.2, and $22.4{\mu}g/ml$, repectively.

• 대한약학회:학술대회논문집
• /
• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
• /
• pp.367.1-367.1
• /
• 2002

Flavo.no.ids are a diverse group of phytqchemicals that are produced by various plants in high quantities. Dietary flavonoids in edible plants can be further subdivided into. several structural groups. The large number of compounds arises from various combinations of multiple hydroxyl and methoxyl groups substituting the basic flavonoid skeleton. The chemopreentive activity of flavonoids is dependent on their structural features. (omitted)

• 한국환경과학회지
• /
• 제26권11호
• /
• pp.1285-1295
• /
• 2017

Chrysanthemum boreale Makino is widely distributed in Korea, China, Japan and Southeast Asian countries. C. boreale is one of the herbs used for treating various inflammatory diseases in oriental medicine. The present study was conducted to identify biologically active compounds from the leaves and stems of C. boreale. We isolated two sesquiterpene sactones from the leaves and stems of C. boreale using silica gel column chromatography and recyclic high perfomance liquid chromatography. The lactones were characterized by their spectroscopic data (NMR, IR, MASS). These compounds were subjected to Farnesyl Protein Transferase (FPTase) inhibition, Nitric Oxide (NO) release inhibition and apoptosis inhibition. The structur of the following isolated compound were elucidated 8,10-${\small{O}$-Acetyl-2-methoxy-10-hydroxy-3,11(13)-guaiadiene-12,6-olide and 4,10-dihydroxy-8-${\small{O}$-Acetyl-2,11(13)-guaiadiene-12,6-olide. In the NO release inhibition assay, compound 2 showed strong activities, with an $IC_{50}$ value of $7{\mu}g/mL$, whereas compound 1 did not exhibit significant activity with an $IC_{50}$ value of over $14{\mu}g/mL$ against murine macrophage.

• Journal of Applied Biological Chemistry
• /
• 제50권4호
• /
• pp.249-253
• /
• 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.

• Bulletin of the Korean Chemical Society
• /
• 제31권5호
• /
• pp.1355-1360
• /
• 2010

In order to search new inhibitors against farnesyl protein transferase (FPTase), a series of 2,3-bis-benzylidenesuccinaldehyde derivatives (1-29) were synthesized and their inhibition activities ($pI_{50}$) against FPTase were measured. From based on the reported results that the inhibitory activities of dimers 2,3-bis-benzylidenesuccinaldehydes were higher than those of monomers cinnamaldehydes, 3D-QSARs on FPTase inhibitory activities of the dimers (1-29) were studied quantitatively using comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) methods. The statistical qualities of the optimized CoMFA model II ($r^2{_{cv.}}$= 0.693 and $r^2{_{ncv.}}$= 0.974) was higher than those of the CoMSIA model II ($r^2{_{cv.}}$ = 0.484 and $r^2{_{ncv.}}$ = 0.928). The dependence of CoMFA models on chance correlations was evaluated with progressive scrambling analyses. And the inhibitory activity exhibited a strong correlation with steric factors of the substrate molecules. Therefore, from the results of graphical analyses on the contour maps and of predicted higher inhibitory active compounds, it is suggested that the structural distinctions and descriptors that contribute to inhibitory activities ($pI_{50}$) against FPTase will be able to applied new inhibitor design.

• 생약학회지
• /
• 제38권4호
• /
• pp.312-320
• /
• 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.

• Journal of Applied Biological Chemistry
• /
• 제52권4호
• /
• pp.221-225
• /
• 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.