• Natural Product Sciences
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• 제17권2호
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• pp.147-159
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• 2011

A high-performance liquid chromatography-electrospray ionization-tandem mass spectrometric method was developed to determine simultaneously eight marker constituents of Forsythiae fructus, and subsequently applied it to classify its two botanical origins. The marker compounds of Forsythia suspensa were phillyrin, pinoresinol, phillygenin, lariciresinol and forsythiaside; those of F.viridissima were arctiin, arctigenin and matairesinol. Separation of the eight analytes was achieved on a phenyl-hexyl column (150${\times}$2.0 mm i.d., 3 ${\mu}M$) using gradient elution with the mobile phase: (A) 10% acetonitrile in 0.5% acetic acid, (B) 40% aqueous acetonitrile. A few fragment ions specific to the types of lignans, among the product ions generated by collisonally induced dissociation (CID) of molecular ion clusters, such as [M-H]$^-$ or [M+OAc]$^-$ were used not only for fingerprinting analysis but for the quantification of each epimer by using multiple-reaction monitoring mode. It was shown good linearity ($r^2{\geq}$ 0.9998) over the wide range of all analytes; intra- and inter-day precisions (RSD, %) were within 9.14% and the accuracy ranged from 84.3 to 115.1%. The analytical results of 40 drug samples, combined with multivariate statistical analyses - principal component analysis (PCA) and hierarchical cluster analysis (HCA) - clearly demonstrated the classification of the test samples according to their botanical origins. This method would provide a practical strategy for assessing the authenticity or quality of the herbal drug.

• Journal of Microbiology and Biotechnology
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• 제15권2호
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• pp.269-273
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• 2005

Five dibenzylbutyrolactones were isolated from a methanol extract of Arctii fructus (Arctium lappa L.) by bioassay-guided isolation, using the interleukin-l $\beta$ converting enzyme (caspase-l, ICE) production inhibitory assay in vitro. These compounds were spectroscopically identified as lappaol E (1), lappaol A (2), matairesinol (3), arctigenin (4), and arctiin (5). Among the compounds tested, arctigenin (4) showed the strongest inhibitory activity for ICE production in IL-$\beta$-induced proliferation of D 1 OS cells. Western blot analysis demonstrated that the arctigenin suppressed the expression of ICE protein in a dose-dependent manner. To estimate the biotransformation of Arctii fructus in vivo by human intestinal bacteria, we carried out an anaerobic incubation of the Arctii fructus extract with a human fecal suspension. From the HPLC analysis of metabolites, Arctiin (IC$_{50}$=74.2$\mu$g/ml), a major component of Arctii fructus, was transformed to aglycone, arctigenin (IC$_{50}$=12.5$\mu$g/ml), by human intestinal bacteria. The ICE production inhibitory activity of Arctii fructus would be much stronger in vivo than in vitro due to the biotransformation by human intestinal bacteria.

• 한국식품저장유통학회:학술대회논문집
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• 한국식품저장유통학회 2003년도 춘계총회 및 제22차 학술발표회
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• pp.22-39
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• 2003

Biological activity of phenolic compounds in seeds and leaves of safflower (Carthamu tinctorius L.) were evaluated using several in vitro and in vivo assays. Six phenolic constituents were isolated from the seeds and identified as N-feruloylserotonia, N- (p-coumaroyl)serotonin, matairesinol, 8′-hydroxyarctigenin, acacetin 7-O-$\beta$-D-glucoside (tilianine) and acacetin. Six phenolic compounds exhibited considerable antioxidative activity, and especially two serotonins showed potent DPPH radical scavenging activity and antiperoxidative activity against rat liver microsomal lipid peroxidation induced by the hydroxyl radical generated via a Fenton-type reaction. Additionally, six phenolic compounds possessed comparable cytotoxicity against three cancer cells, Hela cell, MCF-7 and HepG2 cell, and particularly acacetin and its glycosides had the most potent cytotoxicity. Moreover, we found that feeding safflower seeds attenuated bone loss, and lowered levels of plasma and liver lipids in ovariectomized rats. Serotonins, lignans and flavones stimulated proliferation of the osteoblast-like cells in a dose-dependent manner (10$^{-15}$ ~10$^{-6}$ M), as potently as E$_2$ (17$\beta$-estradiol). Particularly, serotonins were mainly responsible for bone-protecting and lipid lowering effects in ovariectomized rats. Meanwhile, eight flavonoids, including a novel quercetin-7-O-(6"-O-acetyl)-$\beta$-D-glucopyranoside and seven kown flavonoids, luteolin quercetin, luteolin 7-O-$\beta$-D-glucopyranoside, luteolin-7-O-(6"-O-acetyl)-$\beta$-D-gluco-pyranoside, quercetin 7-O- -glucopyranoside, acacetin 7-O-$\beta$-D-glucuronide and apigenin-6-C-$\beta$-D-glucopyranosyl-8-C-$\beta$-D-glucopyranoside were first isolated and identified from safflower leaf. Among these flavonoids, luteolin-acetyl-glucoside and $\beta$quercetin- acetyl-glucoside showed potent antioxidative activities against 2-deoxyribose degradation and lipid peroxidation in rat liver microsomes. Luteolin, quercetin and their corresponding glycosides also exhibited strong antioxidative activity, while acacetin glucuronide and apigenin-6, 8-di-C-glucoside were relatively less active. Finally, changes in phenolic compositions were also determined by HPLC in the safflower seed and leaf during growth stages and roasting process to produce standardized supplement powerds. These results suggest that phenolic compounds in the roasted safflower seed and leaf may be useful as potential sources of therapeutic agents against several pathological disorders such as carcinogenesis, atherosclerosis and osteoporosis.

• 한국식품영양과학회지
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• 제37권9호
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• pp.1162-1167
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• 2008

홍화씨를 이용한 골다공증 및 고지혈증 예방용 건강기능식품을 개발하기 위한 연구의 일환으로 홍화씨의 소화성, 기능성 및 기호성을 증대시킬 수 있는 방안으로 발아홍화씨를 제조하여 일반성분 및 기능성성분(지방산, tocopherols, 수용성아미노산 및 페놀화합물)의 함량을 홍화씨와 비교 분석하였다. 홍화씨는 발아하면서 조단백질과 조지방은 감소한 반면, 가용성 무질소물, 조섬유소 및 회분은 다소 증가하는 경향을 나타내었으며, linoleic 및 oleic aicds가 약 80% 이상 거의 대부분을 차지하고 있었으며, 그 외 palmitic, stearic 및 arachidic acids가 주요 지방산으로 나타났고, 발아에 따른 지방산의 조성 비율은 거의 변화가 없었다. 홍화씨와 발아홍화씨의 $\alpha$-tocopherol 함량은 각각 744.7 및 809.0 mg%로서 발아 후 64.3 mg% 증가하였으며, 홍화씨의 주된 아미노산으로 asparagine, arginine, proline, glutamic acid가 차지하고 있었으며, 발아함에 따라 그들의 함량이 크게 증가하였고, 특히 threonine, valine, leucine, isoleucine, phenylalanine, lysine 및 histidine 등의 필수아미노산 함량이 크게 증가하였다. 홍화씨에는 3종의 리그난(8'-hydroxyarctigenin 4'-O-$\beta$-D-glucoside, 8'-hydroxyarctigenin 및 matairesinol)과 4종의 세로토닌유도체[N-feruloylserotonin 5-O-$\beta$-D-glucoside, N-feruloylserotonin, N-(pcoumaroyl)-serotonin 5-O-$\beta$-D-glucoside, N-(p-coumaroyl)serotonin] 그리고 2종의 플라보노이드(acacetin 7-O-$\beta$-D-glucuronide, acacetin) 화합물이 존재하였으며, 발아함에 따라 세로토닌유도체를 함유한 모든 페놀화합물의 함량은 다소 감소하는 경향을 나타내었다. 이와 같이 홍화씨를 발아함에 따라 섬유소 및 유용 기능성성분의 증가와 더불어 설사를 유발하는 고미성분의 감소 그리고 소화성 및 기호성을 떨어뜨리는 홍화씨 껍질의 분리 및 효율성 확대를 이룰 수 있기에 향후 발아홍화씨는 항골다공증 및 항고지혈증 건강기능식품 소재로서 개발 가능성이 높다고 사료된다.