• 대한약학회:학술대회논문집
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• 대한약학회 2001년도 Proceedings of the Pharmaceutical Society of Korea
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• pp.90-94
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• 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
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• 제30권1호
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• pp.70-73
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• 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.

• Natural Product Sciences
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• 제12권4호
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• pp.214-216
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• 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
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.367.1-367.1
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• 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
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• 제26권11호
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• pp.1285-1295
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• 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
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• 제50권4호
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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.

• Bulletin of the Korean Chemical Society
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• 제31권5호
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• pp.1355-1360
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• 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
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• 제38권4호
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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.

• Journal of Applied Biological Chemistry
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• 제52권4호
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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.

• Applied Biological Chemistry
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• 제45권4호
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• pp.223-227
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• 2002

그늘쑥(Artemisia sylvatica Max.)으로부터 분리된 sesquiterpene lactone계 화합물들의 구조적인 특성과 FPTase 저해활성을 나타내는 dehydromatricarin A, B 분자들 사이 biogenic Diels-Alder 반응의 경계분자 궤도함수 (FMO)상호작용에 대한 배향성을 검토하였다. 그 결과, 주 생성물이 얻어지는 반응은 B1(diene)의 HOMO와 A16(dienophile)의 LUMO간 hard-hard한 charge-control 반응이었다. 그리고 AO계수 분극간의 상호작용에 따른 배향성은 분리된 8-acetylarteminolide와 artanomaloide들이 모두 biogenic Diels-Alder 반응의 부 생성물들임을 시사하였다. 또한, 8-acetyl-arteminolide의 FPTase 저해활성($pI_{50}=3.75$ 및 logP=2.62)은 큰 반면에 artanomaloide 및 dehydromatricarin은 작았다.