한국환경과학회지 제28권 제11호 (p.993-1004)

|ORIGINAL ARTICLE|
산국 잎과 줄기의 유효성분 분리 및 특성 연구

Isolation and Characterization of Constituent Compounds from Leaves and Stems of Chrysanthemum boreale Makino
키워드 :
Chrysanthemum boreale Makino,Sesquiterpene lactone,Cytotoxicity,Farnesyl-protein transferase,Apoptosis,Nitric oxide

목차

Abstract
1. 서 론
2. 재료 및 방법
   2.1. 식물체 재료
   2.2. 시약 및 기기
   2.3. 화합물 1, 2, 3의 분리
   2.4. 암세포주에 대한 세포독성 실험
   2.5. FPTase의 활성 측정
   2.6. Apoptosis 저해 실험
   2.7. NO 방출 저해 실험
3. 결 과
   3.1. 산국의 잎과 줄기에서 분리한 화합물들의 구조동정: 화합물 1
   3.2. 산국의 잎과 줄기에서 분리한 화합물들의 구조동정: 화합물 2
   3.3. 산국의 잎과 줄기에서 분리한 화합물들의 구조동정: 화합물 3
   3.4. 산국에서 분리한 화합물들의 암세포주에 대한in vitro 세포독성실험
   3.5. 산국에서 분리한 화합물들의 farnesyl-proteintransferase (FPTase) 저해활성
   3.6. 산국에서 분리한 화합물들의 Apoptosis 저해활성
   3.7. 산국에서 분리한 화합물들의 Nitric Oxide (NO)방출 저해활성
4. 고 찰
5. 결 론
REFERNECES

초록

Chrysanthemum boreale Makino (C. boreale) is widely distributed in Asian countries, and has traditionally been used to treat various inflammatory diseases including bronchitis. In this study, we aimed to isolate biologically active compounds from leaves and stems of C. boreale. Chemical components were purified by column chromatograpy and recyclic HPLC, and characterized from their spectral data (IR, MS, NMR). Biological activity experiments were conducted for Farnesyl-protein transferase (FPTase) activity, apoptosis and nitirc oxide (NO) release. As a results, three sesquiterpene lactones were isolated. Compound 1 (4-methoxy-8-O-acetyl-10-hydroxy-2,11(13)-guaiadiene-12,6-olide) showed strong cytotoxic activities having an average growth inhibition of 50% (GI50) value of 1.89 ㎍/㎖against human colon adenocarcinoma cells. Compound 1 also showed a low half maximal inhibitory concentration (IC50) value of 10 ㎍/㎖ for NO release. In the caspase 3 activity, compound 1 and compound 2 (8-O-(2-carbonyl-2-butyl)-3,10-dihydroxy-4,11(13) -guaiadiene-12,6-olide) exhibited 94% and 90% apoptosis inhibition activity, respectively. Compound 3 (4,8-O-diacetyl -10-hydroxy-2(3),11(13)-guaiadiene-12,6-olide) showed a strong inhibitory effect on FPTase activity with 90% inhibitory activity at a concentration of 100 ㎍/㎖. These results clearly show the presence of lactone compounds in the leaves and stems, which may partially contribute to the pharmacological activity of C. boreale.