울금(Curcuma longa L.)의 생리활성 및 지질과산화 저해능에 미치는 영향을 확인하고 기능성 식품 소재로 활용 가치를 검토하기 위하여 연구를 수행하였다. 총 카로티노이드(total carotenoid) 함량은 1.581±0.005 mg β-carotene equivalents (BCE)/g dry weight으로 관찰되었다. 70% 메탄올, chloroform:methanol (CM, 2:1, v/v), 에틸 아세테이트(ethyl acetate, EA) 3가지 용매를 사용한 추출 수율은 70% 메탄올(16.54%), CM (5.64%), EA (4.14%) 순으로 나타났다. 총 페놀 함량은 EA, CM 및 70% 메탄올에서 각각 106.287, 90.614 및 18.527 mg gallic acid equivalents (GAE)/g의 함량으로 나타났으며, 추출 용매 별 항산화능은 0.2, 0.4, 0.6, 0.8 mg/mL의 농도로 측정하였고, 양성대조구로 사용된 BHA (butylated hydroxyanisole) 및 trolox 보다는 낮은 항산화능을 보였다. Nitric oxide (NO) 라디칼 소거능은 70% 메탄올에서 28.65~48.43%, CM 18.86~55.10%, EA에서 15.68~56.25%로 관찰 되었다. Nitrite (NO2) 소거능은 70% 메탄올, CM 및 EA 순으로 나타나 EA 추출물에서 유의적인 차이를 보이며 강한 NO2 소거능을 나타내었다(p<0.05). β-carotene 탈색 저해능은 70% 메탄올, CM 및 EA에서 각각 1.64~23.79%, 6.99~41.16% 및 10.20~48.52%로 관찰되었다. 한편, 지질과산화 저해능은 70% 메탄올, CM 및 EA 추출물에서 높게 측정되었다. 이상의 결과로 미루어 볼 때, 울금은 기능성 식품 소재로서 활용 가치가 있을 것으로 판단된다.

본 연구에서는 α-glucosidase 저해활성이 우수한 천연 자원을 개발하기 위하여 개똥쑥으로부터 천연 물질을 분리·동정하고 분리된 물질에 대하여 α-glucosidase 저해활성을 측정하였다. 개똥쑥 잎과 줄 기의 chloroform층과 ethyl acetate층으로부터 각각 6개와 5개의 화합물을 분리하였다. 분리한 화합물 중 chloroform층으로부터 분리된 ArteCA(M.W. 316g/mol, C16H12O7)는 isorhamnetin, ArteCB(M.W. 360g/mol, C18H16O8)는 chrysosplenol D, ArteCC(M.W. 316 g/mol, C16H12O7)는 rhamnetin, ArteCD (M.W. 374g/mol, C18H16O8)는 chrysosplenetin, ArteCE(M.W. 284g/mol, C21H20O12)는 acacetin 그리 고 ArteCF(M.W. 270g/mol, C16H14O4)는 imperatorin으로 확인되었다. 한편 EtOAc층으로부터 분리된 ArteEAA(M.W. 178g/mol, C9H6O4)는 6,7-dihydroxy coumarin, ArteEAB (M.W. 192g/mol, C10H8O4) 는 scopoletin, ArteEAC (M.W. 448g/mol, C21H20O11)는 kaempferol-3-O-b-D-glucoside, ArteEAD (M.W. 464 g/mol, C21H20O12)는 quercetin-3-O-b-D-glucoside 및 ArteEAE(M.W. 318g/mol, C15H10O8)는 myricetin으로 확인되었다. 이 중에서 ArteEAE(myricetin)는 α-glucosidase에 대하여 97.3%의 높은 저해활성을 가지고 있었으므로, 혈당조절용 건강식품 또는 치료제 개발을 위한 물질로 활용될 수 있을 것으로 판단되었다.

This study was designed to determine the biological activities of Chionanthus retusus flower extracts. Water and 90% ethanol extracts of C. retusus flower were prepared. The inhibitory activities of water and ethanol extracts with a phenolic content of 200 μg/mL against xanthine oxidase were 25.60% and 15.92%, respectively. Further, the water extract did not show any inhibitory activity against α-glucosidase whereas the ethanol extract showed 100.00% inhibition of α-glucosidase. The inhibitory activities of the extracts against tyrosinase were 17.27% (water extract) and 36.13% (ethanol extract), which suggest that the extracts may have a whitening effect. The water extract did not inhibit elastase activity but showed a collagenase-inhibitory activity of 20.21%. On the contrary, the ethanol extract showed 96.26% and 35.93% inhibition of collagenase and elastase, respectively. These findings suggest that the extracts may have an anti-wrinkle effect. Lastly, the extracts showed a hyaluronidase inhibitory activity of 36.96% (water extract) and 88.70% (ethanol extract), suggesting that they may have an anti-inflammatory effect. The results indicate that C. retusus flower extracts containing phenolic compounds can be used as functional resources because they have anti-gout, carbohydrate degradation-inhibitory, whitening, anti-wrinkle, and anti-inflammatory effects.

In this study, the anti-inflammatory effect of hyaluronidase (HAase) inhibition was determined from 92 species of oriental herbal medicine extracted with water and ethanol solvents because of their non-toxicity in the human body. The water extracts of Evodia officinalis (86.8%), Thuja orientalis (80.8%), Carthami semen (66.5%), Melia azedarach (74.7%), Siegesbeckia pubescens (61.3%), Saururus chinensis (49.15%) showed a relatively greater anti-inflammatory activity. The ethanol extracts of Ailanthus altissima and Saururus chinensis demonstrated the highest anti-inflammatory effect at above 90%. Saururus chinensis was selected for its high anti-inflammatory effect in both water and ethanol extract. Ethanol was more effective than water and optimal extraction conditions for phenolic compounds was determined to be extraction with 50% ethanol for 12 hours. The extracts from Saururus chinensis in optimal condition showed 70~80% anti-inflammatory effect when 100~250 μg/mL phenolic concentration was treated. Concentration of above 500 μg/mL decreased the inhibitory effect. The anti-inflammatory effect and extraction yield were increased by ultra-fine grind technology, indicating that this method can be used to increase the extraction yield of phenolic compounds from medicinal plants.

We evaluated the inhibitory effects of extracts and components of Geranium thunbergii on aldose reductase (AR) and galactitol formation in rat lenses with high levels of galactose as a part of our ongoing search of natural sources for therapeutic and preventive agents for diabetic complications. The inhibitory effects of water, methanol and ethanol extracts of G. thunbergii on rat lens AR (RLAR) were determined. Comparing inhibitory effects of various solvent extracts, ethanol extract showed RLAR inhibitory activity (IC50 values, 5.24 and 6.39μg/ml, respectively). The ethanol extract was fractionated to chloroform, ethyl acetate and water. Of these, the ethyl acetate fraction from ethanol extract of G. thunbergii exhibited RLAR inhibitory activity (IC50 value, 2.64μg/ml). In order to identify the bioactive components of ethyl acetate soluble fraction of ethanol extract from G. thunbergii, eight compounds, namely gallic acid (1), protocatechuic acid (2), p-hydroxybenzoic acid (3), brevifolin carboxylic acid (4), geraniin (5), ellagic acid (6), kaempferol-3-O-arabinofuranosyl-7-O-rhamnopyranoside (7), kaempferitrin (8) were isolated. The isolates were subjected to in vitro bioassays to evaluate their inhibitory activity on RLAR and galactitol formation in rat lenses. The ellagic tannins (5, 6) and flavonoid (7) exhibited strong inhibitory effects on RLAR. Also, these three compounds (5, 6 and 7) suppressed galactitol accumulation in rat lens under high galactose conditions, demonstrating the potential to prevent galactitol accumulation exo vivo. These results suggest that the extracts and components of G. thunbergii are a promising agent in the prevention or treatment of diabetic complications.

ROS have been associated with pathogenic processes including carcinogenesis through direct effect on DNA and play an important role in the pathogenesis of inflammation. Because of many types of phenolic acid derivatives and flavonoids, apples have been one of the human diet since ancient times and are one of the most commonly consumed fruits in worldwide. In this study, catechin, chlorogenic acid and phlorizin dihydrate were purified and identified by HPLC and GC/MS. The contents of catechin, chlorogenic acid and phlorizin dihydrate were 1.01 mg, 7.01 mg and 3.67 mg/ kg wet weight, respectively. Catechin and phlorizin dihydrate were found to significantly inhibit oxidative DNA damage, while chlorogenic did not affect. Also, catechin inhibits NO and PGE2 production via suppressing iNOS and COX-2 expression. However, chlorogenic acid and phlorizin dihydrate did not affect. Our results show that catechin may be the most active phenolic compound in anti-oxidative damage and anti-inflammatory effect.

신규 미백 소재 개발을 위하여 tyrosinase의 활성을 억제하는 천연물과, alpha-melanocyte stimulating hormone (α-MSH)을 저해하는 펩타이드를 결합한 소재를 고체상 합성법으로 제조하였다[1,2]. Tyrosinase 활성 억제 효능이 있는 천연유래물질을 기존 연구를 바탕으로 선정하였으며, 이중에서 상업화 된 물질 17종에 대해 Mushroom Tyrosinase 활성 억제 효과를 측정하여, 그 중 caffeic acid, coumaric acid를 선별하였다. 펩타이드는 α-MSH 분비를 억제하며, tyrosinase활성을 억제하는 것으로 알려진 melanostatin을 선정하였으며[3-5], PLG-NH2 (Proline-Leucine-Glycine-NH2) 중에서 유도체화 수율의 저하 원인으로 예상되는 Proline (Pro)의 서열을 다른 아미노산으로 변경하면서 선별된 천연물인 coumaric acid와 caffeic acid에 도입하였다. 또한 최종물질의 원가를 고려하여 acid-amide 형태를 acid형태로 전환한 유도체를 합성하였다. 이들 펩타이드 유도체들에 대해서 B16F1 melanoma cell에서의 멜라닌 생성 억제 효능을 평가하여 유도체화된 물질이 기존의 천연유래물질이나 펩타이드에 비하여 높은 저해효과를 가지는 것을 확인하였다.

Compounds of isolated from roots extract of Pueraria thunbergiana were tested their inhibitory effects on α-glucosidase and α-amylase. Inhibitory activity of methylene chloride (MC) fraction and ethyl acetate (EA) fraction against α-glucosidase showed more than 60% at a concentration of 500μg/ml. Among the nine compounds tested on α-glucosidase, biochanin A, (-)-tuberosin and calycosin from MC fraction and daidzein from EA fraction were stronger inhibitors than acarbose (IC50=530μg/ml), and their IC50 were 9, 144, 328 and 20μg/ml, respectively. Biochanin A and (-)-tuberosin also inhibited α-amylase activity as like as acarbose IC50=20.5μg/ml), and their IC50 were 22 and 348μg/ml, respectively. Although daidzein was already known α-glucosidase inhibitory effects, it was newly evaluated that biochanin A and (-)-tuberosin inhibited α-glucosidase as well as α-amylase, and that calycosin did α-glucosidase.

기질 화합물로써 3β-hydroxy-12-oleanen-28-oic acid 유도체들의 치환기(R₁ ∼ R₄)가 변화함에 따른 protein tyrosine phosphatase (PTP)-1B의 저해활성에 관한 비교 분자장 분석(CoMFA) 모델을 유도하고 정량적으로 검토하였다. 최적의 CoMFA F1 모델은 가장 높은 예측성과 상관성(r²cv.=0.654 및 r²ncv.=0.995)을 나타내었다. 저해활성에 관한 CoMFA장 기여비율(%)의 순서는 입체장(53.0 %), 정전기장(36.2 %) 및 소수성장(10.8 %) 이었다. 등고도 분석 결과로부터 저해활성은 기질 분자 내 R4-치환기에 의존적이었으며 특히 melanin 저해활성이 높은 새로운 화합물(P1 및 P2)이 예측되었다.

국내산 인삼의 부위별 quercetin, p-coumaric acid, maltol, esculetin의 함량을 측정한 결과 잎에서는 quercetin과 esculetin이 주근에서는 p-coumaric acid가 다량 함유되어 있었다. 이중잎의 EA 분획물은 melan-a 세포주에서 뛰어난 멜라닌 생성억제 활성을 보였으며, 이의 주요성분인 quercetin과 esculetin이 tyrosinase 활성억제도, melan-a 세포주에서의 멜라닌 생성억제도, UV-흡수도 측정에서 모두 우수한 활성을 나타내는 결과로 미루어 인삼의 잎은 피부미백을 목적으로 하는 기능성 소재로 이용될 수 있는 가능성을 가지는 것으로 사료된다.