• 생약학회지
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• 제30권4호
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• pp.404-408
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• 1999

SH2 domains and their associated catalytic or noncatalytic proteins constitute critical signal transduction targets for drug discovery. Grb2 associates with phosphotyrosine sites of the activated receptors or Shc via their SH2 domain to link receptor tyrosine kinases to ras signalling. Blocking of the Grb2-Shc complex may be to intervene the oncogenic signal transduction pathways and to develop a new antitumor drug. In the search for blockers of Grb2 SH2-Shc interaction, Lutein, a family of carotenoids, was isolated from the extract of the leaf of Agastache rugosa O. Kuntze as SH2 domain antagonists. The $IC_{50}$ of Lutein against Grb2-Shc binding was $6.8\;{\mu}M$.

• 생약학회지
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• 제30권2호
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• pp.202-206
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• 1999

The MeOH extracts obtained from the leaves of Eucommia ulmoides were solvent-fractionated with EtOAc, n-BuOH, and $H_20$, successively. From the EtOAc extract showing Grab2-Shc inhibitory activity, a flavonol and a lignan compounds were isolated through repeated silica gel column chromatographies. By interpretation of several spectral data and adaptation of acetylation method, the chemical structures of the compounds were determined as 5,7,3',4'-tetrahydroxy-flavonol (quercetin), and 4,4',8',9-tetrahydroxy-3,3'-dimethoxy-7,9'-cyclolignan {(-)-olivil)}, respectively. The compounds exhibited $IC_{50}$ values in Grb2-Shc inhibitory activity to be 93 and $210\;{\mu}mole/l$, respectively.

• Applied Biological Chemistry
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• 제41권2호
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• pp.197-200
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• 1998

홍화 MeOH 추출물의 n-BuOH 분획으로부터 silica gel column chromatography를 반복하여 2종의 flavonoid 배당체를 분리, 정제하였다. 화합문의 화학구조를 HMBC를 포함한 NMR, MS, IR과 같은 기기분석 결과와 산가수분해반응을 이용하여 결정, 각각 $3-O-[{\beta}-D-glucopyranosyl(1{\rightarrow}2)\;{\beta}-D-glucopyranosyl]\;kaempferol$ 및 $3-O-[{\alpha}-L-rhamnopyranosyl(1{\rightarrow}6)\;{\beta}-D-glucopyranosyl]\;kaempferol$로 동정하였다. 각 화합물은 Grb2-Shc 결합저해활성$(IC_{50}:43,\;47\;{\mu}g/ml)$을 나타내었다.