• Biomolecules & Therapeutics
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• 제23권3호
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• pp.275-282
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• 2015

In the present study, we synthesized a series of novel 7-methoxy-N-(substituted phenyl)benzofuran-2-carboxamide derivatives in moderate to good yields and evaluated their neuroprotective and antioxidant activities using primary cultured rat cortical neuronal cells and in vitro cell-free bioassays. Based on our primary screening data with eighteen synthesized derivatives, nine compounds (1a, 1c, 1f, 1i, 1j, 1l, 1p, 1q and 1r) exhibiting considerable protection against the NMDA-induced excitotoxic neuronal cell damage at the concentration of $100{\mu}M$ were selected for further evaluation. Among the selected derivatives, compound 1f (with $-CH_3$ substitution at R2 position) exhibited the most potent and efficacious neuroprotective action against the NMDA-induced excitotoxicity. Its neuroprotective effect was almost comparable to that of memantine, a well-known NMDA antagonist, at $30{\mu}M$ concentration. In addition to 1f, compound 1j (with -OH substitution at R3 position) also showed marked anti-excitotoxic effects at both 100 and $300{\mu}M$ concentrations. These findings suggest that $-CH_3$ substitution at R2 position and, to a lesser degree, -OH substitution at R3 position may be important for exhibiting neuroprotective action against excitotoxic damage. Compound 1j was also found to scavenge 1,1-diphenyl-2-picrylhydrazyl radicals and inhibit in vitro lipid peroxidation in rat brain homogenate in moderate and appreciable degrees. Taken together, our structure-activity relationship studies suggest that the compound with $-CH_3$ substitution at R2 and -OH substitution at R3 positions of the benzofuran moiety might serve as the lead exhibiting potent anti-excitotoxic, ROS scavenging, and antioxidant activities. Further synthesis and evaluation will be necessary to confirm this possibility.

• 한국약용작물학회지
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• 제18권4호
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• pp.255-265
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• 2010

The extent of growth L. plantarum (LP), L. delbrueckii subsp. bulgaricus (LD), L. fermentum (LF), S. thermophilus (ST), B. longum (BI) and S. cerevisiae (SA) was generally good with the lower concentration of the ginseng extract. Total sapogenin content was slightly different with kinds of a fermentation microorganism and the time of fermentation process, and generally reduced compare to before fermentation. The content of ginsenoside Rb1, Rb2, Rb3, Re and Rf were decreased with the fermentation but ginsenoside Rd was increased by the E, LF and SA fermented extract. The content of compound K increased in the order of not-fermented extrac < enzyme fermented extract < enzyme and microorganism fermented extract, and as the fermented time get longer, the content of compound K was sightly increased. Especially, the content of compound K of the SA fermented extract was the most increased, also it of the BI, LD and LF fermented extract was increased, so these extract were considered a high valuable. Polyphenol content of the BI, LD, LP and ST fermented extract indicated $9.18{\pm}0.39{\sim}15.68{\pm}0.54$ mg/10 g which was lower than it of a not-fermented extract ($11.92{\pm}0.26{\sim}28.41{\pm}0.39$ mg/10 g). Flavonoid content of a ginseng fermented extract indicated $26.93{\pm}0.17{\sim}156.45{\pm}1.29$ mg/10 g, it was higher than a not-fermented extract ($18.06{\pm}0.90$ mg/10 g). As the fermented time get longer, the flavonoid content tendency to increase. DPPH radical scavenging activity of a fermented ginseng extract was $24.11{\pm}1.41{\sim}55.62{\pm}0.33%$, it was slightly lower compared to a natural antioxidant, vitamin C. But it of the LF and ST fermented extract was similar to a natural antioxidant, vitamin C. It has not a concerned in a fermentation. Nitrite scavenging ability of a 24 hr fermented extract was above 80% at pH 2.5 and 4.2, it was similar to an artificial antioxidant, BHT ($84.76{\pm}0.13%$; pH2.5, $84.98{\pm}0.11%$; pH 4.2). It has not a concerned in a fermentation. SOD-like activity of a fermented extract was lower than that of a not-fermented extract ($19.22{\pm}0.51%$), but it of the E and LP-fermented extract was a very highly notable value. As the fermented time get longer, the SOD-like activity tendency to increase.

• 한국식품영양과학회지
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• 제40권3호
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• pp.470-474
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• 2011

열처리한 양파 착즙액의 ethyl acetate 분획물로부터 항산화물질을 분리 동정하기 위하여 1, 2차 silica gel column chromatography, preparative TLC 및 HPLC를 이용하여 항산화활성 물질을 분리 정제하였다. GC/MSD, $^1H$-NMR 및 $^{13}C$-NMR spectrum 결과로부터 구조 동정한 결과 분리된 물질은 2,3-dihydro-3,5-dihydroxy-6-methyl-4H-pyran-4-one(DDMP)으로 확인되었다. DDMP의 항산화활성의 $IC_{50}$값은 241.6 ${\mu}g/mL$이었으며, vitamin E의 69.2 ${\mu}g/mL$와 C의 45.3 ${\mu}g/mL$보다는 낮은 활성을 보였고 BHT의 268.0 ${\mu}g/mL$보다는 높은 활성을 보였지만 유의적인(p>0.05) 차이는 나타나지 않았다. 추후 DDMP를 기능성물질로 활용하기 위하여 다양한 생리활성 평가가 필요할 것으로 생각된다.

• 대한화장품학회지
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• 제46권4호
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• pp.329-337
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• 2020

본 연구는 willamette 품종의 동결건조라즈베리분말, n-hexane 및 ethyl acetate를 이용하여 라즈베리 추출물(Rubus idaeus (Raspberry) fruit extract, RIFE)을 제조한 다음 페놀 화합물 함량, 철 이온 환원능력, 그리고 라디칼 소거 능력의 측정을 수행하였다. Willamette 품종 라즈베리추출물은 10% 농도까지 세포독성을 보이지 않았다. 해당 농도로 실험을 수행한 결과 총 페놀 화합물 함량은 375.3 ppm, 총 플라보노이드 함량은 43.46 ppm이 포함된 것을 확인하였고, ferric reducing antioxidant power (FRAP) reagent를 이용한 철 이온 환원능력은 FeSO4 0.532 mM에 해당하는 환원능력을 가졌음을 확인하였다. 이를 바탕으로 항산화 소재의 대표적 원료인 L-ascorbic acid와 비교하는 라디칼 소거능 실험을 실시하였다. 그 결과 1,1-diphenyl- 2-picrylhydrazyl (DPPH) 라디칼 소거능력은 94.5 ± 0.7%를 나타냈고, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) 라디칼 소거능은 99.4 ± 2.82%를 나타냈으며, nitric oxide (NO) 라디칼소거능은 88.5 ± 0.4%를 나타냈다. 표준인 L-ascorbic acid 용액과 비교할 때 25 - 50 ppm 사이의 효능을 지닌 DPPH 라디칼 소거능 / 100 ppm에 근접한 효능을 지닌 ABTS 라디칼 소거능 / 1,000 ppm 이상의 효능을 지닌 NO 라디칼 소거능을 가졌음을 확인하였다. 이러한 결과들은 willamette 품종 라즈베리추출물이 항산화 활성을 가지는 효과적인 화장품 소재로 적용 가능하다는 것을 시사한다.

• 한국식품영양과학회지
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• 제45권4호
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• pp.510-517
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• 2016

본 연구는 싸리나무 잎에서 분리한 flavonoid 화합물인 eriodictyol의 항산화 활성을 평가하기 위해 hydrogen peroxide로 산화적 스트레스를 유도한 HepG2 세포에서 eriodictyol 화합물의 처리가 SOD-1, SOD-2, CAT 및 GPx의 유전자 발현에 미치는 영향을 분석하였으며, 또한 간 기능 지표효소인 GOT, LDH 및 GGT 활성을 분석하였다. 그리고 세포 내 활성산소종 생성 억제 효능을 분석하기 위하여 DCFH-DA assay를 실시하여 eriodictyol 화합물의 기능성 소재로서의 가능성을 알아보고자 본 실험을 하였다. Eriodictyol 화합물의 세포독성을 확인하기 위하여 HepG2 세포주를 이용하여 실시한 결과 eriodictyol 화합물을 $10{\sim}50{\mu}g/mL$의 농도로 처리한 모든 실험군에서 약 98% 이상의 세포생존율을 나타내었다. 항산화 효소 유전자 발현량을 통한 산화스트레스 억제 효과를 분석하기 위하여 HepG2 세포주에 hydrogen peroxide를 처리하여 산화스트레스가 증가시킨 조건에서 eriodictyol 화합물을 처리하여 SOD-1, SOD-2, CAT 및 GPx 발현량을 분석한 결과 eriodictyol 화합물의 처리 농도가 증가할수록 hydrogen peroxide 처리에 의해 감소한 SOD-1, SOD-2, CAT 및 GPx 발현량이 유의적으로 증가하는 것을 확인할 수 있었다. 간 기능 지표효소 활성을 측정하기 위해 GOT, LDH 및 GGT 활성을 분석한 결과 hydrogen peroxide로 단독 처리한 대조군과 eriodictyol 화합물을 처리한 군을 비교하였을 때 eriodictyol 화합물을 처리한 군에서 hydrogen peroxide 처리에 의해 증가한 GOT, LDH 및 GGT 활성이 유의적으로 감소하였다. HepG2 세포주에 eriodictyol 화합물을 처리하여 세포 내 활성산소종 생성에 미치는 영향을 DCFH-DA assay로 확인한 결과 eriodictyol 화합물의 농도가 증가함에 따라 세포내 활성산소종의 생성을 억제하는 것을 확인할 수 있었다. 따라서 본 실험을 통하여 eriodictyol 화합물은 산화적 스트레스로부터 항산화 효소 활성을 증가시키며, 활성산소종의 생성을 억제하는 효과를 확인할 수 있었다. 또한 간 기능 지표효소의 활성을 감소시켜 세포 보호 효과를 나타내어 항산화 활성 및 세포 보호 효과를 나타내는 기능성 소재로써 이용 가능성이 높을 것으로 판단되며, 후속연구를 통해 싸리나무 유래 eriodictyol 화합물의 세포 내 항산화 단백질 발현에 미치는 영향 및 동물실험을 통한 항산화 효과를 검증하는 것이 필요할 것으로 생각된다.

• 동아시아식생활학회지
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• 제16권2호
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• pp.199-206
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• 2006

This study was designed to investigate the effect of medicinal herb extract on the antioxidant and antimicrobial activities against Helicobacter pylori, which is known as a ulcerogenic pathogen. The concentration of total phenolic compound of Scutellaria baicalensis(13.14%) was highest among water extracts and that of Ulmus parvifolia(15.12%) was highest among the ethanol extracts. The antioxidant activity of the water extract of Scutellaria baicalensis and of the ethanol extract of Ulmus parvifolia were 91.00% and 65.03%, respectively, in DPPH assay. The antioxidant activity of the water extract of Scutellaria baicalensis and of the ethanol extract of Ulmus parvifolia were 32.90% and 27.70%, respectively, in SOD assay. The antioxidant activity of the water extract of Ulmus parvifolia and of the ethanol extract of Glycyrrhiza uralensis Fischer was 2.15 and 2.17, respectively, in TBARS assay. In disc method, Scutellaria baicalensis showed the highest anti-microbial activity against H. pylori, followed by Glycyrrhiza uralensis Fischer among the water extracts and Glycyrrhiza uralensis Fischer showed the highest anti-microbial activity followed by Radix puerariae among ethanol extract.

• Ocean and Polar Research
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• 제33권3호
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• pp.255-263
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• 2011

The aim of this investigation was to evaluate antioxidant activity of crude extracts from the halophyte Vitex rotundifolia, their solvent fractions, and isolated compounds (1-3). Antioxidant capacity was determined by measuring DPPH radical, and authentic $ONOO^-$ and $ONOO^-$ generated from 3- morpholinsydnonimine (SIN-1) in vitro as well as degree of occurrence of intracellular ROS, NO and GSH in mouse macrophage Raw 264.7 cells. From comparative analysis, MeOH extract, n-BuOH, and 85% aq. MeOH solvent fractions showed significant antioxidant effect in DPPH radical and $ONOO^-$ assay systems. Activity-guided purification of n-BuOH and 85% aq. MeOH fractions led to the isolation of flavonoids 1-3. Among them, compound 1 exhibited excellent antioxidant effect in all bioassay systems tested. On the other hand, compounds 2 and 3 revealed potent inhibitory effect against $ONOO^-$ generated from SIN-1, comparable with the positive control penicillamine.

• Natural Product Sciences
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• 제24권2호
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• pp.119-124
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• 2018

Two triterpenoids, arjunolic acid (1), belleric acid (2), five phenylethanoids, martynoside (3), orobanchoside (4), 3,4-dihydroxyphenethylalcohol-6-O-caffeoyl-${\beta}$-$\text\tiny{D}$-glucoside (5), leucosceptoside B (6), lunariifolioside (7), four phenolic acids, ferulic acid (8), syringic acid (9), vanillic acid (10), 4-hydroxybenzoic acid (11), and one lignan, (+)-syringaresinol-${\beta}$-$\text\tiny{D}$-glucoside (12), were isolated from the roots of P. umbrosa. All isolated compounds were explored for their antioxidant potential in the DPPH and ABTS assays. In DPPH assay, compound 5 showed high antioxidant capacity. Compounds 3, 4, 6, and 7 displayed considerable antioxidant activities. In addition, compounds 5-7 exhibited potential antioxidant capacities in the ABTS assay.

• 한국축산식품학회지
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• 제33권6호
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• pp.689-695
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• 2013

This study was conducted to investigate the effects of in vitro human digestion on the antioxidant activity of blueberry leaf extracts (BLE) in emulsion-type sausages (ETS). Leaves from four cultivars of blueberries (Bluecrop, Bluegold, Duke, and Northland) collected from a wild blueberry farm were extracted with 80% ethanol. ETS were prepared with 0.2% BLE. The samples were then passed through an in vitro human digestion system which simulates the composition of the mouth, stomach, and small intestine juice. Only one phenolic compound (chlorogenic acid) was detected in the BLE. Northland BLE had appreciably higher amounts of chlorogenic acid than that of other BLE, both before and after in vitro human digestion. Antioxidant activity of any BLE was not influenced by in vitro human digestion, whereas the antioxidant activity of chlorogenic acid standard increased in response to in vitro human digestion in both 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) and ferric-reducing ability of plasma (FRAP). In the present study, the antioxidant activities of the BLE were not strongly influenced by in vitro human digestion, and the antioxidant activity depended on the chlorogenic acid content of ETS. Thus, compounds from blueberry leaves may have important applications in the future as natural antioxidants for meat products.

• 한국식품영양학회지
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• 제29권3호
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• pp.347-356
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• 2016

This study analyzed the antioxidant properties of Equisetum arvense and its effects on serum factor levels in mice fed a high-fat diet. The aim was to establish a new effective resource for biologically active materials. E. arvense stem and root extracts were obtained using deionized water at $95^{\circ}C$, and 70.5% ethanol at $85^{\circ}C$. These extracts were used to analyze the total phenolic compounds and antioxidant (ABTS, DDPH, and FRAP) activities. The effects of prepared ground samples were evaluated by feeding them to mice. E. arvense extracts showed strong antioxidant effects. The caffeic acid content was highest in the 70.5% ethanol extract of the vegetative stem, as determined by high-performance liquid chromatography. The blood concentrations of insulin and leptin were significantly lower in mice fed a high-fat diet supplemented with extracts of the root, reproductive stem, and vegetative stem of E. arvense than in mice fed only a high-fat diet. These results suggest that the polyphenolic compounds in E. arvense extracts exert various antioxidant effects. The stems and root of E. arvense can lower the blood levels of insulin and leptin, even after consumption of a high-fat diet.