Development of Biologically Active Compounds from Edible Plant Sources XXII. Isolation of Indoles from the Roots of Brassica campestris ssp rapa and their hACAT Inhibitory Activity

The roots of Brassica campestris ssp rapa were extracted with 80% aqueous MeOH, and the concentrated extract was partitioned with EtOAc, n-BuOH and $H_2O$. From the EtOAc fraction, three compounds were isolated through the repeated silica gel and octadecyl silica gel (ODS) column chromatography. From the results of spectroscopic data including NMR and MS, the chemical structures of the compounds were determined as caulilexin C (1), indoleacetonitrile (2) and arvelexin (3). The arvelexin (3) has been isolated from this plant for the first time. Compounds 1, 2 and 3 showed inhibitory activity on human Acyl CoA: cholesterol. transferase 1 (hACAT1) by $54.6{\pm}6.0%$, $69.2{\pm}4.7%$ and $68.6{\pm}3.7%$, and on human Acyl CoA: cholesterol transferase 2(hACAT2) by $4.8{\pm}13.4%$, $45.6{\pm}4.8%$ and $39.5{\pm}4.3%$, respectively, at 100 ${\mu}g/ml$.

식용식물자원으로부터 활성물질의 탐색 XXII. 순무(Brassica campestris ssp rapa) 뿌리로부터 인돌 화합물의 분리 및 hACAT 저해 활성

순무 뿌리로부터 80% MeOH 수용액으로 추출하고 이를 여과, 감압 농축하여 MeOH추출물을 얻었다. 이를 EtOAc 분획, n-BuOH분획, $H_2O$분획으로 나누었으며, EtOAc분획으로부터 silica gel 및 ODS column chromatography를 실시하여 3종의 화합물을 분리 정제하였다. 각각에 대하여 $^1H-NMR$, $^{13}C-NMR$, DEPT 스펙트럼 및 Mass 스펙트럼 데이터를 해석하여, caulilexin C (1), indoleacetonitrile (2) 및 arvelexin (3)로 구조를 결정하였다. 화합물 3는 순무에서는 이번에 처음 분리, 보고되었다. 또한 화합물 1, 2, 및 3은 100 ${\mu}g/ml$의 농도에서 hACATl의 활성을 각각 $54.6{\pm}6.0%$, $69.2{\pm}4.7%$ 및 $68.6{\pm}3.7%$ 억제하였고, hACAT2의 활성을 각각 $4.8{\pm}13.4%$, $45.6{\pm}4.8%$ 및 $39.5{\pm}4.3%$ 억제하였다.