• Title/Summary/Keyword: Inhibitory Activity

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Inhibitory Aromatase Effects of Flavonoids from Ginkgo Biloba Extracts on Estrogen Biosynthesis

  • Park, Yong Joo;Choo, Wun Hak;Kim, Ha Ryong;Chung, Kyu Hyuck;Oh, Seung Min
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.15
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    • pp.6317-6325
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    • 2015
  • Ginkgo biloba extract (GBE) is a popular phytomedicine and has been used for disorders of the central nervous system, cardiovascular, renal, respiratory, and circulatory diseases. Although GBE is a complex mixture of over 300 compounds, its major components are 24% flavonoids and 6% terpene lactones. In this study, we tested the inhibitory effects of the three major flavonoids (kaempferol, quercetin, and isorhamnetin) from GBE, independently and as mixtures, on aromatase activity using JEG-3 cells (human placental cells) and recombinant proteins (human placental microsome). In both systems, kaempferol showed the strongest inhibitory effects among the three flavonoids; the flavanoid mixtures exerted increased inhibitory effects. The results of exon I.1-driven luciferase reporter gene assays supported the increased inhibitory effects of flavonoid mixtures, accompanied by suppression of estrogen biosynthesis. In the RT-PCR analysis, decreased patterns of aromatase promoter I.1 mRNA expressions were observed, which were similar to the aromatase inhibition patterns of flavonoids and their mixtures. The present study demonstrated that three flavonoids synergistically inhibit estrogen biosynthesis through aromatase inhibition, decrease CYP19 mRNA, and induce transcriptional suppression. Our results support the usefulness of flavonoids in adjuvant therapy for breast cancer by reducing estrogen levels with reduced adverse effects due to estrogen depletion.

Antioxidant and Cholinesterase Inhibitory Activities of the By-products of Three Pandalid Shrimps

  • Kim, Sang-Bo;Yoon, Na Young;Shi, Kil Bo;Lim, Chi-Won
    • Fisheries and Aquatic Sciences
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    • v.17 no.4
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    • pp.421-425
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    • 2014
  • The antioxidant and cholinesterase inhibitory activities of the acetone and dichloromethane ($CH_2Cl_2$) extracts of the by-products (heads, shells, and tails) of Pandalus borealis, Pandalus hypsinotus, and Pandalopsis japonica belonging to the family Pandalidae were investigated and their bioactivities were compared. The antioxidant and cholinesterase inhibitory activities of the organic solvent extracts of three shrimp by-products were evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-Azino-bis[3-ethylbenzothiazoline-6-sulfonic acid] ($ABTS^+$) radical scavenging activities, reducing power and xanthine oxidase (XO) inhibitory activity assays and Ellman's colorimetric method. The extracts of P. hypsinotus exhibited the highest antioxidant and cholinesterase inhibitory activities. The acetone extracts showed more potent activities toward antioxidant and cholinesterase inhibition compared with the $CH_2Cl_2$ extracts. Furthermore, the total carotenoid contents of the acetone extracts were higher than those of the $CH_2Cl_2$ extracts. Thus, the carotenoid contents may affect antioxidant and cholinesterase inhibition. Our results suggest that the shrimp by-products could act as a nutraceutical agent to prevent oxidative stress and Alzheimer's disease.

Antioxidant, anti-acetylcholinesterase and xanthine oxidase inhibitory activities of three extracts from Phellinus igniarius

  • Jin, Ga-Heon;Lee, Min Woong;Im, Kyung Hoan;Lee, Tae Soo
    • Journal of Mushroom
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    • v.12 no.1
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    • pp.1-7
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    • 2014
  • This study was initiated to investigate antioxidant, anti-acetylcholinesterase, and xanthine oxidase inhibitory activities and properties of fruiting bodies, mycelia, and fermentation culture filtrates from Phellinus igniarius. The contents of total phenols and flavonoid of fruit bodies, mycelia, and culture filtrate were 15.35-1.36 mg/g, 10.35-7.85 mg/g, and 8.25-5.36 mg/g. The 1,1-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging abilities of the extracts from the fruiting bodies, mycelia, and culture filtrates were 90.25-95.60%, 78.82-85.24%, and 76.32-82.50% at $50-400{\mu}g/mL$, respectively. The chelating ability of fruiting body extract on ferrous ions was higher than those of mycelia and culture filtrates tested. The anti-acetylcholinesterase inhibitory activity of the fruiting body extract at 400 ${mu}g/mg$ exhibited 91.10% on AChE, which is lower than that of positive control, galanthamine (94.82%). The xanthine oxidase inhibitory activities of the fruiting bodies, mycelia, and culture extract were 85.47%, 78.13%, and 72.49% at 400 ${\mu}g/mL$, respectively. Overall, the fruiting body extract has better anti-acetylcholinesterase, antioxidant and xanthine oxidase inhibitory activities than those from mycelia and culture filtrate.

A Study on the Tyrosinase Inhibitory and Antioxidant Effect of Microalgae Extracts

  • Ji, Keunho;Kim, Yeeun;Kim, Young Tae
    • Microbiology and Biotechnology Letters
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    • v.49 no.2
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    • pp.167-173
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    • 2021
  • Reactive oxygen species (ROS) disrupt the cellular redox balance, exert cytotoxic effects, and consequently promote the development of various diseases in humans. Previous studies have reported that antioxidants counteract the adverse effects of ROS. Several studies examine the whitening effects of various agents based on their ability to inhibit tyrosinase activity. Tyrosinase is a critical enzyme involved in the synthesis of melanin, which protects the skin against radiation. Various agents exhibiting antioxidant and tyrosinase inhibitory activities have been synthesized. However, these synthetic drugs are associated with toxicity, decreased safety, and poor skin penetration in vivo, which has limited the clinical application of synthetic drugs. This study examined the antioxidant and tyrosinase inhibitory activities of some microalgae. The methanol, dichloromethane, and ethyl acetate extracts of four microalgal species (Tetraselmis tetrathele, Dunaliella tertiolecta, Platymonas sp., and Chaetoceros simplex) were prepared. The physiological and whitening effects of microalgal extracts were investigated by measuring the antioxidant and tyrosinase inhibitory activities. The ethyl acetate extract of D. tertiolecta exhibited the highest antioxidant and tyrosinase inhibitory activities. Future studies must focus on examining the whitening effects of microalgae on cell lines to facilitate the development of microalga-based therapeutics for skin diseases, functional health foods, and whitening agents. Thus, microalgae have potential applications in the pharmaceutical, food, and cosmetic industries.

Beauty Food Activities of Isolated Phenolic Compounds from Ulmus pumila (유근피(Ulmus pumila)로부터 분리한 페놀성물질의 미용식품활성)

  • Kim, Kyung-Bum;Jo, Bun-Sung;Lee, Ju-Yeong;Park, Ki-Tae;An, Bong-Jeun;Lee, Sun-Ho;Cho, Young-Je
    • Journal of Applied Biological Chemistry
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    • v.55 no.4
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    • pp.207-215
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    • 2012
  • Phenolic compounds of $17.9{\pm}1.0mg/g$ were extracted from Ulmus pumila with 70% ethanol. The elastase inhibitory activity related with forming wrinkle was shown an excellent wrinkle improvement effect in 70% ethanol extracts as 55.5-69.5% at phenolic concentration of $50-200{\mu}g/mL$. The tyrosinase inhibitory activity related with skin-whitening was 24% in 70% ethanol extracts at phenolic concentration of $200{\mu}g/mL$. The astringent activity of 70% ethanol extracts was shown activity of 71% at phenolic concentration of $200{\mu}g/mL$ therefore it is judged that there is a high effect on pores reduction of the skin. The hyaluronidase inhibitory activity of U. pumila extracts was confirmed anti-inflammation effect of 80% at phenolic concentration of $50{\mu}g/mL$. Antimicrobial activity of U. pumila water extracts was shown each 8.7, 10.0, 11.1 and 11.8 mm clear zones on Propionebacterium acnes at phenolic concentration of $50-200{\mu}g/mL$. The stability of the multi-functional cosmetic (lotion) added U. pumila extracts was very stable for 28 days without changing of pH and viscosity also it's stable on temperature and sun lights. As the concentration of extracts was increased, the color of lotion was getting dark, but the sensory evaluation was high at score of 8.5.

Physiological activity of methanol extract and fractions from Citrus grandis Osbeck pericarp (당유자 과피 메탄올 추출물 및 분획물의 생리활성 검정)

  • Ko, Hyun Min;Kim, Ju-Sung
    • Journal of Plant Biotechnology
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    • v.45 no.3
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    • pp.279-286
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    • 2018
  • Citrus grandis Osbeck pericarp is used as tea, herbal medicine, etc., but is not commercialized in various ways. So, in this study, we identified potential for use of Citrus grandis Osbeck as health functional foods, cosmetics and food preservatives. Methanol extract of Citrus grandis Osbeck pericarp was fractionated with hexane, dichloromethane, ethyl acetate and butanol, to quantitatively analyze total phenol and flavonoid, and investigate antioxidative and enzyme inhibitory activities. Total phenol and flavonoid contents were highest in ethyl acetate fraction, FRAP and ORAC results also revealed highest activity in proportion to total phenol content. DPPH radical scavenging activity revealed that ethyl acetate, butanol and dichloromethane fraction manifested highest activity without significant difference. However, dichloromethane fraction revealed higher TEAC value and tyrosinase inhibitory activity than ethyl acetate fraction, and hexane fraction manifested best results with superoxide radical scavenging activity and ${\alpha}-glucosidase$ inhibitory activity. Antimicrobial activity also revealed best effect in dichloromethane and hexane fractions. So, based on the following results, use of dichloromethane fraction as material of natural functional cosmetics, ethyl acetate fraction for health functional foods, and hexane fractions for pharmaceuticals and food preservatives, would be most practical for product development.

Physiological Functionalities of Traditional Alaska Pollack Sik-hae (전통 명태식해(식해)의 기능성)

  • Cha, Yong-Jun;Lee, Cho-Eun;Jeong, Eun-Kyung;Kim, Hun;Lee, Jung-Suck
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.31 no.4
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    • pp.559-565
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    • 2002
  • The physiological functionalities such as antimicrobial activity, antioxidative activity, angiotensin-I converting enzyme (ACE) inhibitory activity and bile acid binding capacity were measured for the solvent-fractionated methanol extracts of Alaska pollack sik-hae at various time intervals during fermentation. Two temperature schemes of fermentation were studied: constant temperature of 2$0^{\circ}C$ (A) and stepwise change from 2$0^{\circ}C$ (10 days) to 5$^{\circ}C$ (B). The methanol extracts of Alaska pollack sik-hae showed antimicrobial activities against 9 kinds of micro-organisms including pathogenic and food poisoning strains. Among these, gram positive bacteria, in particular Staphylococcus aureus, showed more sensitivity to the extracts than gram negative bacteria and fungi. Antioxidative activity (EDA$_{50}$) increased until 15 days (A, 0.92 mg/$m\ell$) or 16 days of fermentation (B, 0.94 mg/$m\ell$), and then gradually decreased. ACE inhibitory activity was observed in all fermentation time except 0 day, and bile acid binding capacity at 15 days (A) and 16 days (B) only.

Inhibitory Effect of DPPH Radical Scavenging Activity and Hydroxyl Radicals (OH) Activity of Hydrocotyle sibthorpioides Lamarck (피막이풀의 DPPH 라디칼과 hydroxyl radicals (OH) 항산화 활성 및 리폭시게나아제 저해 효과)

  • Cho, Kyung-Soon
    • Journal of Life Science
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    • v.26 no.9
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    • pp.1022-1026
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    • 2016
  • In this study the hot water extract was prepared from Hydrocotyle sibthorpioides (Araliaceae) leaves and stems to study antioxidant activities and lipoxygenase inhibition. The extract showed the protective hydroxyl radical (-OH) which can damage virtually all types of macromolecules: carbohydrates, nucleic acids (mutations), lipids (lipid peroxidation), and amino acids. Hydroxyl radical scavenging activity of H. sibthorpioides was 78.6%. The extract showed strong activity against 1, 1- diphenyl 2-picrylhyorazyl (DPPH) which is a well-known radical and a trap (scavenger) for other radicals. DPPH scavenging activity of leaves of H. sibthorpioides was evaluated at 8.0 mg/ml was 86.0%. Lipoxygenases (LOXs) constitute a heterogeneous family of lipid peroxidizing enzymes capable of oxygenating polyunsaturated fatty acids to their corresponding hydroperoxy derivatives. The inhibitory effect of 15-LOX by H. sibthorpioides was assayed using a Morgan microplate assay. The extract of H. sibthorpioides was 55.5% inhibitory effects on the inhibition of LOX at 8.0 mg/ml. The IC50 values for OH activity, DPPH activity, and LOX inhibition from leaves 5.23 mg/ml, 6.44 mg/ml, and 3.71 mg/ml, respectively. Antioxidative activity assay showed that the water extracts from leaf and stem had a strong reducing power. These results show that H. sibthorpioides has some phytochemical constituents which may be active against the free radicals (OH and DPPH) and lipoxygenase enzyme.

Effect of Medicinal Herb Prepared through Traditional Antidiabetic Prescription on α-Glucosidase Activity and Evaluation Method for Anti-Melanogenesis Agents Using α-Glucosidase Activity (당뇨 처방에 근거한 생약재의 α-Glucosidase 활성 저해 효과 및 이를 활용한 미백 소재 평가법)

  • Kim, Mi Jin;Im, Kyung Ran;Yoon, Kyung-Sup
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.44 no.7
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    • pp.993-999
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    • 2015
  • For the purpose of investigating the in vitro antidiabetic activity of a medicinal herb and herb mixture extracts prepared through traditional antidiabetic prescription, this study examined ${\alpha}$-glucosidase inhibitory activity. Tyrosinase, a type I membrane glycoprotein, is synthesized and glycosylated in the endoplasmic reticulum (ER) and Golgi. The enzyme is subsequently transported to melanosomes, where it participates in melanogenesis. Previous studies showed that disruption of early ER N-glycan processing by an ${\alpha}$-glucosidase inhibitor suppresses tyrosinase enzymatic activity and melanogenesis. According to the results, most oriental medicinal herbal extracts were stronger than acarbose and N-butyldeoxynojirimycin, known as an ${\alpha}$-glucosidase inhibitor. Interestingly, ethyl acetate layer of enzyme hydrolyzed Cheongsimyeonjaeum had an inhibitory effect on melanin synthesis in B16F1 cells, although it did not inhibit tyrosinase activity directly. Together, ${\alpha}$-glucosidase inhibition activity could be used to evaluate anti-melanogenesis, although cross-checking with melanin inhibitory assay is recommended.

Biological activity of crude polyphenol fractions of Cedrela sinensis isolated using different extraction methods (참죽의 추출방법에 따른 폴리페놀 분획의 생리기능성)

  • Oh, Min Hui;Yoon, Kyung Young
    • Korean Journal of Food Science and Technology
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    • v.49 no.4
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    • pp.438-443
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    • 2017
  • The biological activity of crude polyphenol fractions (WphF, EphE, VphF, and SphF) extracted from Cedrela sinensis using hot water, ethanol, and enzymes such as Viscozyme and Shearzyme was examined in this study. The yield of VphF was the highest (43.44%) among all fractions. The total polyphenol and flavonoid content of the fractions were highest after ethanol extraction (447.98 and 337.49 mg/g, respectively). Fractions obtained after hot water and ethanol treatment showed high antioxidant activity. All fractions, except for WphF, showed a significantly higher ${\alpha}$-glucosidase inhibitory activity than the acarbose. EphF and WphF showed the high acetylcholinesterase inhibition activity. All fractions showed more than 50% tyrosinase inhibition activity at 2 mg/mL concentration. According to these results, the crude polyphenol fractions from C. sinensis showed high antioxidative, ${\alpha}$-glucosidase inhibitory, and tyrosinase inhibitory activities. This study suggests that crude polyphenol fractions from C. sinensis, especially the WphF and EphF fractions, are good sources of functional food.