Cytoprotective effects and mechanisms of quercetin, quercitrin and avicularin isolated from Lespedeza cuneata G. Don against ROS-induced cellular damage

이건수,박수남 한국공업화학회 2019 Journal of Industrial and Engineering Chemistry Vol.71 No.-

The purpose of this study was to compare the anti-oxidative and cytoprotective effects of quercitrin andavicularin isolated from Lespedeza cuneata G. Don extract to those of quercetin, an aglycone of quercitrin,and avicularin. Quercetin had higher antioxidative activity and cell penetration ratio than its glycosides,resulting in greater cytoprotective effects against 1O2. The cytoprotective effects against cell damageseems to reflect 1O2 quenching rate, free radical and ROS scavenging activity, and cell permeability. Among them, cell permeability to block free radical initiation and chain reactions in cell membranes isconsidered to be the most important feature of cytoprotective activity.

Antioxidant and cytoprotective effects of enzyme‐extracted constituents of Protaetia brevitarsis seulensis powder

Choi In‐Hag,Choi Sung‐Up,Son Jin‐Sung,Jang Woo‐Whan,Chung Tae‐Ho 한국곤충학회 2021 Entomological Research Vol.51 No.2

This study was aimed to compare the antioxidant and cytoprotective effects of hot‐water and enzyme‐extracted constituents of Protaetia brevitarsis seulensis powder. The products of enzymatic extraction had 1,1‐diphenyl‐2‐picrylhydrazyl (DPPH)‐radical‐scavenging activity, cytotoxic effects, and provided cytoprotection against H2O2 and intracellular reactive oxygen species. Enzymatic extraction improved DPPH‐radical‐scavenging activity relative to hot‐water extraction (P < 0.05), with inhibition rates of 33% at 500 μg/mL and 35% at 1000 μg/mL. Cell viability ranged from 100 to 122%, and was higher for hot‐water than for enzymatic extraction (P > 0.05). Hot‐water extraction achieved greater cytoprotection against H2O2 than enzymatic extraction. However, enzymatic extraction achieved greater antioxidant and cytoprotective activity against reactive oxygen species than hot‐water extraction. These results provide evidence of the antioxidant and cytoprotective effects produced by enzymatic extraction of the active ingredients from Protaetia brevitarsis seulensis powder.

페놀 화합물의 Hexavalent Chromium독성에 대한 세포 보호효과

한두석,강정일,백승화,Han, Du-Seok,Kang, Jeong-Il,Baek, Seung-Hwa 대한예방한의학회 2009 대한예방한의학회지 Vol.13 No.2

Objectives : In order to evaluate the cytotoxicity of hexavalent chromium, the cytoprotective effect of phenolic compounds against hexavalent chromium-induced cytotoxicity, cell viability, cell adhesion ability, lactate dehydrogenase(LDH) activity, and morphological changes of cells were examined. Methods : We measured the cytotoxicity of hexavalent chromium with 3-[4,5-dimethyl-thiazol-2-yl]-2,5-diphenyltetrazolium bromide(MTT), 2,3-bis-[2-methoxy-4-nitro-5-sulfophenyl]-2H-tetrazolium-5-caboxanilide (XTT), LDH and DPPH methods. Results : The cytotoxicity of hexavalent chromium($IC_{50}$, $44.0-51.0{\mu}M$) was high according to the toxic criteria. Cytoprotective effect of phenolic compounds against $IC_{50}$ value of hexavalent chromium in cell morphology increased in a concentration-dependent manner. Conclusions : These results suggest that 3,4,5-trihydroxybenzoic acid may be used as a cytoprotective agent against chromium(IV)-mediated cytotoxicity.

갈근탕 추출물의 카드뮴 독성에 대한 세포 보호효과

박소윤(So Yun Park),백종민(Jong Min Baek),백승화(Seung Hwa Baek) 대한약학회 2010 약학회지 Vol.54 No.3

Cytotoxicity of cadmium on NIH 3T3 fibroblasts was utilized in order to discover antitoxic compound in Galgeuntang extract in this study. Treatment groups were chosen as follows; control (medium only), MTT50 group and five experimental groups. MTT {3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazoliumbromide} method was performed to evaluate the cytotoxicity of cell organelles and IC50 was also measured. Accordingly we have examined the detoxification effects of Galgeuntang extract on cadmium-treated NIH 3T3 fibroblasts to observe morphological changes by the light microscopy. Galgeuntang extract showed cytoprotective effects on cadmium-induced cytotoxicity. Furthermore, Galgeuntang showed a dose-dependency in detoxication. The phenolic content of Galgeuntang ethanol extract was higher than that of water content. These results suggest that Galgeuntang extract may be used as a cytoprotective agent against cadmium (II)-mediated cytotoxicity.

Cytoprotective Effects of Sulfuretin from Rhus verniciflua through Regulating of Heme Oxygenase-1 in Human Dental Pulp Cells

이동성,오현철,김경수,Samell Keo,정길생,김윤철 한국생약학회 2013 Natural Product Sciences Vol.19 No.1

Rhus verniciflua Stokes (Anacadiaceae) is a plant that is native to East Asian countries, such as Korea, China, and Japan, and it has been found to exert various biological activities including antioxidative, anti-aggregatory, anti-inflammatory, anti-mutagenic, and apoptotic effects. Sulfuretin is one of the major flavonoid component isolated from the heartwood of R. verniciflua. Reactive oxygen species (ROS), produced via dental adhesive bleaching agents and pulpal disease, can cause oxidative stress. In the present study, we isolated sulfuretin from R. verniciflua and demonstrated that sulfuretin possesses cytoprotective effects against hydrogen peroxide (H2O2)-induced dental cell death. H2O2 is a representative ROS and causes cell death through necrosis in human dental pulp (HDP) cells. H2O2-induced cytotoxicity and production of ROS were blocked in the presence of sulfuretin, and these effects were dose dependent. Sulfuretin also increased heme oxygenase-1 (HO-1) protein expression. In addition, to determine whether sulfuretin-induced HO-1 expression mediated this cytoprotective effect, HDP cells were cotreated with sulfuretin in the absence or presence of SnPP, an inhibitor of HO activity. Sulfuretin-dependent HO-1 expression was required for suppression of H2O2-induced HDP cell death and ROS generation. These results indicate that sulfuretin-dependent HO-1 expression was required for the inhibition of H2O2-induced cell death and ROS generation. In addition, sulfuretin may be used to prevent functional dental cell death and thus may be useful as a pulpal disease agent.

Antioxidant and Cytoprotective Activities of Enzymatic Extracts from Rhizoid of Laminaria japonica

Jae-Young Je,Soo Yeon Park,Chang-Bum Ahn 한국식품영양과학회 2017 Preventive Nutrition and Food Science Vol.22 No.4

Rhizoid of Laminaria japonica was hydrolyzed with proteases and carbohydrases to obtain antioxidant materials. Oxygen radical absorbance capacity (ORAC) of the enzymatic extracts was evaluated and the Protamex extract (PE) exhibited the highest ORAC value. PE also potently scavenged 2,2-diphenyl-1-picrylhydrazyl radical, 2,2’-azino-bis(3-ethylbenzthiazoline-6-sulphonic) acid cation radical, and hydrogen peroxide (H2O2) and had good reducing power. PE inhibited hydroxyl radical-induced DNA scission by measuring the conversion of supercoiled pBR322 plasmid DNA to the open circular form. The cytoprotective effect of PE against H2O2-induced hepatic cell damage was also investigated. PE showed a dose-dependent cytoprotective effect in cultured hepatocytes by inhibiting intracellular reactive oxygen species scavenging activity. In addition, PE up-regulated the expression of heme oxygenase-1, which is a cytoprotective enzyme, by activating translocation of nuclear factor-erythroid 2-related factor 2. Taken together, the enzymatic extract of rhizoid of L. japonica, particularly PE, may be useful for antioxidant additives.

하수오 추출물, 분획물 및 주성분의 항산화, 세포 보호 및 항균 활성에 관한 평가

신혁수 ( Hyuk Soo Shin ),김민우 ( Minwoo Kim ),송제리 ( Jerry Song ),이준석 ( Junseok Lee ),하윤정 ( Yoonjeong Ha ),전영희 ( Young Hee Jeon ),김지웅 ( Ji Woong Kim ),이윤주 ( Yun Ju Lee ),박수남 ( Soo Nam Park ) 대한화장품학회 2018 대한화장품학회지 Vol.44 No.4

본 연구에서는 하수오를 이용하여 50% 에탄올 추출물과 에틸아세테이트 분획물을 제조하고, 추출물 및 분획물의 항산화, 세포 보호 및 항균 효능을 평가하여 기능성 소재로서의 가능성을 확인하였다. 또한, 하수오에 주요하게 존재하는 성분의 활성도 검증하였다. HPLC-DAD, LC-EIS-MS를 통해 분석한 결과, 하수오의 주성분은 2, 3, 5, 4'-tetrahydroxystilbene 2-O-β-D-glucoside (THSG)이었다. 페놀류 및 THSG 함량은 에틸아세테이트 분획물이 에탄올 추출물 보다 각각 11.1 및 3.0배 높게 나타났다. DPPH 자유 라디칼 및 Fe³⁺-EDTA/H₂O₂ 시스템에서 생성된 ROS에 대한 소거 활성 평가에서, 에틸 아세테이트 분획물은 에탄올 추출물 보다 뛰어난 소거 활성을 나타냈다. 특히 ROS 소거 활성 평가에서 에틸 아세테이트 분획물과 THSG은 L-ascorbic acid와 동등한 소거 활성을 나타냈다. 이러한 결과를 바탕으로 수행된 광증감 반응으로 유도된 적혈구의 산화적 손상에 대한 세포 보호 활성은 에틸아세테이트 분획물, 에탄올 추출물, THSG 순서로 나타났으며, 모든 실험군이 양성 대조군으로 사용한 (+)-α-tocopherol보다 우수한 활성을 나타냄을 확인하였다. 항균 활성 평가는 S. aureus, E. coli, P. aeruginosa, C. albicans 균주를 대상으로, disc diffusion assay와 broth microdilution assay를 이용하여 수행하였다. 그 결과 추출물, 분획물 및 THSG 모두 모든 균주에 대해 항균 활성을 나타냈으며, 특히 그람 양성균인 S. aureus에 대해 methyl paraben보다 우수한 항균력을 나타냄을 확인하였다. 본 연구의 결과는 하수오가 항산화, 세포 보호 및 항균력에 관한 천연 소재로의 활용될 수 있는 가능성을 시사한다. In this study, the antioxidant, cytoprotective and antimicrobial activities of 50% ethanol extract of Polygoni multiflori Radix (PMR) and its ethyl acetate fraction were evaluated to confirm the applicability as a functional ingredient. The activities of the major constituent of PMR were verified and 2, 3, 5, 4′-tetrahydroxystilbene 2-O-β-D-glucoside (THSG) was confirmed to be the main component of extract and fraction using HPLC-DAD, LC-EIS-MS analysis. The phenolic and THSG contents of the ethyl acetate fraction were 11.1- and 3.0-folds higher than those of the ethanol extract, respectively. As a result of the DPPH assay and that of luminol dependent chemiluminescence assay in Fe³⁺-EDTA/H2O2 system. the ethylacetate fraction was superior to the ethanol extract in free radical and ROS scavenging activities. Especially, the ethyl acetate fraction and THSG exhibited the similar scavenging activity like L-ascorbic acid in ROS scavenging activity. The ethyl acetate fraction perceived the most potent cytoprotective effect against oxidative damage of erythrocytes induced by photosensitization reaction, followed by the ethanol fraction, THSG and that of (+)-α-tocopherol, which was used as a positive control. Antimicrobial activities were evaluated by disc diffusion and broth microdilution assay against S. aureus, E. coli, P. aeruginosa and C. albicans. In particular, the antibacterial activity of the extract and fraction against S. aureus was superior to that of methyl paraben. Taken together, our results suggest that PMR could be used as a natural ingredient for antioxidant, cytoprotective and antimicrobial activities.

니파야자(Nypa fruticans Wurmb) 싹 추출물 및 분획물의항산화, 세포 보호 및 항균 효과에 관한 평가

신혁수,이윤주,김지웅,송바름,이상래,박수남 한국생약학회 2018 생약학회지 Vol.49 No.2

Nypa fruticans Wurmb is a species of palm, which is widely distributed in the mangrove forest of Southeast Asia. Various parts of N. fruticans has been used as a traditional medicinal plant. However, the physiological activities of N. fruticans has not yet been clarified well. Therefore, in this study, the 50% ethanol extract and its aqueous and ethyl acetate fractions of young shoots of N. fruticans were investigated for their antioxidant, cytoprotective effect, and antimicrobial activities. Every sample possessed very high free radical and various ROS scavenging capacities assessed by employing different in vitro assays such as DPPH∙, O2∙-, ∙OH, and 1O2 scavenging activities. Based on these results, the cytoprotective effect was investigated using the oxidative hemolysis of erythrocyte. We found that the extract and fractions provide a greater protective effect compared with (+)-a-tocopherol. Furthermore, antimicrobial activities were confirmed against skin pathogens by broth microdilution assay. The ethyl acetate fraction had much higher antimicrobial activities than methyl paraben against Staphylococcus aureus, Bacillus subtilis, Pseudomonas aeruginosa, and Candida albicans. Taken together, our results indicated that the young shoots of N. fruticans may have the potential role as a natural active ingredient through their antioxidant, cytoprotective effect, and antimicrobial activities.

인동덩굴 추출물과 분획물의 항산화 활성 및 산화적 스트레스에 대한 세포 보호 효과

이예슬 ( Ye Seul Lee ),윤믿음 ( Mid Eum Yun ),이윤주 ( Yun Ju Lee ),박영민 ( Young Min Park ),이상래 ( Sang Lae Lee ),박수남 ( Soo Nam Park ) 한국미생물생명공학회(구 한국산업미생물학회) 2018 한국미생물·생명공학회지 Vol.46 No.1

DPPH를 이용한 인동덩굴 추출물의 자유라디칼 소거활성(FSC50) 측정 결과, 인동덩굴 에틸아세테이트 분획물 (77.25μg/ml)이 50% 에탄올 추출물(152.00 μg/ml)보다 약 2배 높은 활성을 나타내었다. Luminol 발광법을 이용한 인동덩굴 추출물의 활성산소 소거활성(총 항산화능, OSC₅₀) 측정 결과, 인동덩굴 에틸아세테이트 분획물(0.33 μg/ml) > 인동덩굴 50% 에탄올 추출물(1.12 μg/ml) > L-ascorbic acid (4.95μg/ml) 순서로 높게 나타났다. ¹O₂으로 유도된 적혈구 파괴에 대한 세포 보호 효과(τ₅₀) 측정 결과, 인동덩굴 추출물의 농도에 의존적으로 세포 보호 효과가 나타났으나, 고농도에서는 세포 보호 효과가 감소하는 경향을 나타내었다. 인동덩굴 50% 에탄올 추출물은 10 μg/ml의 농도(46.0 min)에서, 인동덩굴 에틸아세테이트 분획물은 1 μg/ml의 농도(52.3min)에서 가장 높은 세포 보호 효과를 나타내었다. 인동덩굴 추출물 및 분획물의 세포 독성 평가 결과, 본 실험에서는 0.4-12.5 μg/ml의 농도 범위를 설정하여 세포 보호 효과를 평가하였다. 과산화수소로 유도된 각질 형성 세포인 HaCaT세포 보호 효과는 인동덩굴 50% 에탄올 추출물 및 에틸아세테이트 분획물 12.5 μg/ml의 농도에서 각각 70.0, 78.6%의 세포 생존율을 나타냈으며, 대조군(65%)과 비교하여 유의한 세포 보호 효과를 가지고 있음을 확인하였다. UVB를 조사한 HaCaT 세포의 세포 내 ROS 소거 활성에서 인동덩굴 50% 에탄올 추출물 및 에틸아세테이트 분획물 모두 농도 의존적으로 ROS를 소거하였으며, 12.5 μg/ml 농도에서 각각 45.2, 63.3%의 ROS 소거율을 나타내었다. 이를 통해 인동덩굴 에틸아세테이트 분획물이 50% 에탄올 추출물보다 높은 세포 내 ROS 억제능이 있음을 확인하였다. TLC와 HPLC 크로마토그램을 이용한 인동덩굴의 에틸아세테이트 분획물의 성분 분석을 통해 caffeic acid, luteolin, apigenin, coumaric acid를 확인하였다. Caffeic acid와 luteolin의 뛰어난 환원력과 킬레이팅 작용이 인동덩굴 추출물의 활성산소 소거활성과 세포 보호 효과에 크게 기인했을 것으로 사료된다. 인동덩굴 50% 에탄올 추출물과 에틸아세테이트 분획물의 총 페놀성 화합물 및 총 플라보노이드 함량 측정 결과를 통해, 인동덩굴 에틸아세테이트 분획물이 50% 에탄올 추출물보다 많은 페놀성 화합물, 플라보노이드를 함유하고 있기 때문에 더욱 우수한 항산화 활성을 나타내었음을 확인하였다. 본 연구에서는 자외선에 의해 생성되는 다양한 ROS에 대한 인동덩굴 추출물 및 분획물의 항산화 활성을 평가하였고 이상의 결과를 통해 인동덩굴 추출물이 식물유래 천연 항산화제로서 가치가 있음을 시사하였다. 뿐만 아니라, 인동덩굴의 항산화 기능성 화장품 소재로서의 개발 가능성을 확인하였다. In this study, the antioxidant activities and cytoprotective effects against oxidative stress of Lonicera japonica Thunb. 50% ethanol extract and ethyl acetate fraction were investigated. Using the 1,1-diphenyl- 2-picrylhydrazyl assay, the free radical scavenging activity (FSC50) of L. japonica Thunb. 50% ethanol extract and ethyl acetate fraction was determined as 152.00 and 77.25 μg/ml, respectively. To measure the reactive oxygen species (ROS) scavenging activity, the total antioxidant capacity (OSC50) was determined by using a luminol-dependent chemiluminescence assay. The antioxidant activity of the ethyl acetate fraction (0.33 μg/ml) was approximately four times stronger than that of the 50% ethanol extract (1.12 μg/ml). The protective effect against ¹O₂-induced cellular damage of human erythrocytes (τ₅₀) was 46.0 min at 10 μg/ml of the 50% ethanol extract and 52.3 min at 1 μg/ml of the ethyl acetate fraction. We also investigated the cytoprotective effects against oxidative stress induced by H₂O₂ and the intracellular ROS scavenging activity in response to UVB irradiation and found that the extract and fraction protected human skin cells from damage and reduced ROS. These results confirmed that L. japonica Thunb. was a valuable plant-derived natural antioxidant with potential for development as an antioxidative functional ingredient.

Antioxidant Flavone Glycosides from the Leaves of Sasa borealis

Hae-Suk Park,임주희,Hyun Jung Kim,최현진,이익수 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.2

Sasa borealis (Poaceae) is a perennial medicinal plant which is a major source of bamboo leaves in Korea. The n-BuOH extract of S. borealis leaves exhibited significant antioxidant activity against the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and a cytoprotective effect against oxidative damage in HepG2 cells. Bioactivity-guided fractionation by column chromatography led to the isolation of two antioxidative flavonoid C-glycoside derivatives, isoorientin (2) and isoorientin 2''-O-α-L-rhamnoside (4) along with tricin 7-O-β-D-glucopyranoside (1) and apigenin 6-C-β-D-xylopyranosyl-8-C-β-D-glucopyranoside (3). Their structures were identified on the basis of chemical and spectroscopic methods. The radical scavenging activity and cytoprotective effect against oxidative damage of all the isolated compounds were also evaluated. Isoorientin (2) and isoorientin 2-O-α-L-rhamnoside (4) showed potent free radical scavenging activity with IC50 values of 9.5 and 34.5 µM, respectively, and strong cytoprotective effects against t-BOOH-induced oxidative damage in HepG2 cells, at very low concentrations of 1.1 µM isoorientin and 0.8 µM isoorientin 2-O-α-L-rhamnoside. This is the first report of the isolation and antioxidant activity of compounds 2 and 4 from S. borealis.