• 제목/요약/키워드: inhibitory compounds

검색결과 1,642건 처리시간 0.03초

추출방법에 따른 참취(Aster scaber Thunb.)의 페놀화합물 함량과 생리활성 및 소화효소 저해 효과 (Polyphenolic Compounds, Physiological Activities, and Digestive Enzyme Inhibitory Effect of Aster scaber Thunb. Extracts According to Different Extraction Processes)

  • 김재원;윤광섭
    • 한국식품영양과학회지
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    • 제43권11호
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    • pp.1701-1708
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    • 2014
  • 참취의 활용 및 생리활성을 증가시킬 수 있는 적정 추출방법을 알아보고자 상온교반, 환류냉각, 가압가열, 저온고압 및 초음파 추출법을 이용하여 추출한 두벌 째 수확 참취 추출물의 생리활성을 비교하였다. 추출 수율은 환류냉각추출, 초음파추출, 가압가열추출, 상온추출, 저온고압추출 순으로 높았다. 폴리페놀, 플라보노이드 함량은 저온고압추출에서 유의적으로 높았고, 상압가열, 고온고압, 초음파추출에서는 대등한 함량을 나타내었다. 페놀화합물 정량의 경우 chlorogenic acid 함량은 가압가열추출에서 유의적으로 높았으며 cynarin 함량의 경우 환류냉각, 저온고압 및 초음파 추출에서 유의적으로 높았고, astragalin 함량의 경우 저온고압추출에서 높은 함량이 검출되었다. Xanthine oxidase(XO), angiotensin I-converting enzyme(ACE), HMG-CoA reductase 저해활성의 경우 저온고압추출 및 초음파 추출물에서 우수한 활성을 나타내었으며, 소화효소 저해활성(${\alpha}$-amylase, trypsin, lipase)에서도 유사한 경향을 나타내었다. 이러한 결과를 종합해 볼 때 저온고압 및 초음파 추출물에서 소재 활용가치가 높을 것으로 사료되며 천연 항산화제 및 기능성 증진을 위한 소재로 이용 가능할 것으로 판단된다.

선씀바귀 추출물의 항산화 및 항당뇨 효과 (Antioxidant and anti-diabetic effects of Ixeris strigosa extract)

  • 지윤정;이은영;이지연;서경혜;김동휘;박춘근;김형돈
    • Journal of Nutrition and Health
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    • 제53권3호
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    • pp.244-254
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    • 2020
  • 본 연구는 선씀바귀의 항산화 및 탄수화물 소화효소 억제 효과를 평가하여 제 2형 당뇨환자에게 중요한 항산화제 및 혈당 상승 억제제로서의 가능성을 타진하고자 하였다. 선씀바귀 추출물의 총 폴리페놀, 플라보노이드 함량과 in vitro 항산화 활성 및 소화효소 저해 활성을 조사한 결과 ISE가 ISW보다 총페놀과 플라보노이드 함량이 높았고 항산화 활성 및 소화효소 저해 활성 또한 높았다. ISE의 계통분획물 중에 에틸아세테이트 분획물과 부탄올 분획물의 소화효소 저해 활성이 가장 우수하고, 추출물의 항산화활성과 탄수화물 소화효소 억제효과가 총 페놀 및 플라보노이드함량과 높은 상관성을 가지는 것으로 볼 때, ISW에 비해 상대적으로 높은 ISE의 항산화 및 소화효소 저해 활성은 페놀 화합물, 특히 플라보노이드 화합물 때문임을 알 수 있었다. 따라서 ISE와 에틸아세테이트 그리고 부탄올 분획물은 우수한 항당뇨 기능성 소재라고 판단된다.

Assessment of Antioxidant and Phenolic Compound Concentrations as well as Xanthine Oxidase and Tyrosinase Inhibitory Properties of Different Extracts of Pleurotus citrinopileatus Fruiting Bodies

  • Alam, Nuhu;Yoon, Ki-Nam;Lee, Kyung-Rim;Kim, Hye-Young;Shin, Pyung-Gyun;Cheong, Jong-Chun;Yoo, Young-Bok;Shim, Mi-Ja;Lee, Min-Woong;Lee, Tae-Soo
    • Mycobiology
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    • 제39권1호
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    • pp.12-19
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    • 2011
  • Cellular damage caused by reactive oxygen species has been implicated in several diseases, thus establishing a significant role for antioxidants in maintaining human health. Acetone, methanol, and hot water extracts of Pleurotus citrinopileatus were evaluated for their antioxidant activities against ${\beta}$-carotene-linoleic acid and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals, reducing power, ferrous ion-chelating abilities, and xanthine oxidase inhibitory activities. In addition, the tyrosinase inhibitory effects and phenolic compound contents of the extracts were also analyzed. Methanol and acetone extracts of P. citrinopileatus showed stronger inhibition of ${\beta}$-carotene-linoleic acid compared to the hot water extract. Methanol extract (8 mg/mL) showed a significantly high reducing power of 2.92 compared to the other extracts. The hot water extract was more effective than the acetone and methanole extracts for scavenging DPPH radicals. The strongest chelating effect (92.72%) was obtained with 1.0 mg/mL of acetone extract. High performance liquid chromatography analysis detected eight phenolic compounds, including gallic acid, protocatechuic acid, chlorogenic acid, ferulic acid, naringenin, hesperetin, formononetin, and biochanin-A, in an acetonitrile and hydrochloric acid (5 : 1) solvent extract. Xanthine oxidase and tyrosinase inhibitory activities of the acetone, methanol, and hot water extracts increased with increasing concentration. This study suggests that fruiting bodies of P. citrinopileatus can potentially be used as a readily accessible source of natural antioxidants.

Differential Effects of Tautomycetin and Its Derivatives on Protein Phosphatase Inhibition, Immunosuppressive Function and Antitumor Activity

  • Niu, Mingshan;Sun, Yan;Liu, Bo;Tang, Li;Qiu, Rongguo
    • The Korean Journal of Physiology and Pharmacology
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    • 제16권2호
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    • pp.145-151
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    • 2012
  • In the present work, we studied the structure-activity relationship (SAR) of tautomycetin (TMC) and its derivatives. Further, we demonstrated the correlation between the immunosuppressive fuction, anticancer activity and protein phosphatase type 1 (PP1) inhibition of TMC and its derivatives. We have prepared some TMC derivatives via combinatorial biosynthesis, isolation from fermentation broth or chemical degradation of TMC. We found that the immunosuppressive activity was correlated with anticancer activity for TMC and its analog compounds, indicating that TMC may home at the same targets for its immunosuppressive and anticancer activities. Interestingly, TMC-F1, TMC-D1 and TMC-D2 all retained significant, albeit reduced PP1 inhibitory activity compared to TMC. However, only TMC-D2 showed immunosuppressive and anticancer activities in studies carried out in cell lines. Moreover, TMC-Chain did not show any significant inhibitory activity towards PP1 but showed strong growth inhibitory effect. This observation implicates that the maleic anhydride moiety of TMC is critical for its phosphatase inhibitory activity whereas the C1-C18 moiety of TMC is essential for the inhibition of tumor cell proliferation. Furthermore, we measured $in$ $vivo$ phosphatase activities of PP1 in MCF-7 cell extracts treated with TMC and its related compounds, and the results indicate that the cytotoxicity of TMC doesn't correlate with its $in$ $vivo$ PP1 inhibition activity. Taken together, our study suggests that the immunosuppressive and anticancer activities of TMC are not due to the inhibition of PP1. Our results provide a novel insight for the elucidation of the underlying molecular mechanisms of TMC's important biological functions.

Development of Cholinesterase Inhibitors using 1-Benzyl Piperidin-4-yl (α)-Lipoic Amide Molecules

  • Lee, Seung-Hwan;Kim, Beom-Cheol;Kim, Jae-Kwan;Lee, Hye Sook;Shon, Min Young;Park, Jeong Ho
    • Bulletin of the Korean Chemical Society
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    • 제35권6호
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    • pp.1681-1686
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    • 2014
  • A series of hybrid molecules between (${\alpha}$)-lipoic acid (ALA) and 4-amino-1-benzyl piperidines were synthesized and their in vitro cholinesterase (acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)) inhibitory activities were evaluated. Even though the parent compounds did not exhibit any inhibitory activity against cholinesterase (ChE) with the exception of compound 14 ($IC_{50}=255.26{\pm}4.41$ against BuChE), all hybrid molecules demonstrated BuChE inhibitory activity. Some hybrid compounds also displayed AChE inhibitory activity. Specifically, compound 17 was shown to be an effective inhibitor against both AChE ($IC_{50}=1.75{\pm}0.30{\mu}M$) and BuChE ($IC_{50}=5.61{\pm}1.25{\mu}M$) comparable to galantamine ($IC_{50}=1.7{\pm}0.9{\mu}M$ against AChE and $IC_{50}=9.4{\pm}2.5{\mu}M$ against BuChE). Inhibition kinetic studies using compound 17 indicated a mixed inhibition type for AChE and a noncompetitive inhibition type for BuChE. Its binding affinity ($K_i$) values to AChE and BuChE were $3.8{\pm}0.005{\mu}M$ and $7.0{\pm}0.04{\mu}M$, respectively.

Phenyl-2,2'-methylenebis(cyclohexane-1,3-dione) 유도체의 Tyrosinase 저해활성에 관한 HQSAR 분석 (HQSAR Analyses on the Tyrosinase Inhibitory Activity of Phenyl-2,2'-methylenebis(cyclohexane-1,3-dione) Analogues)

  • 김상진;김영옥;조윤기;최원석;성낙도
    • 대한화장품학회지
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    • 제36권3호
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    • pp.199-205
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    • 2010
  • 기질 화합물로써 일련의 phenyl-2,2'-methylenebis(cyclohexane-1,3-dione) 유도체(1-22)들의 치환기($R_1$$R_2$)가 변화함에 따른 tyrosinase 활성저해에 대한 분자 홀로그래피적인 정량적 구조-활성관계(HQSAR) 모델을 유도하였다. 그리고 tyrosinase 저해활성에 미치는 구조상 요소들의 분석결과에 근거하여 높은 tyrosinase 저해활성을 보이는 새로운 tyrosinase 저해활성 분자를 설계하였다. 또한, 통계적으로 양호한 E-2 모델(상관성; $r_2$ = 0.929 및 예측성; $q_2$ = 0.564)을 유도하였으며 설계된 화합물, P1 ($Pred.pI_{50}$ = 5.48)는 기준물질로 사용된 kojic acid에 비하여 약 13.4배 높은 저해활성을 나타낼 것으로 예측되었다.

Inhibition of Klebsiella pneumoniae ATCC 13883 Cells by Hexane Extract of Halimeda discoidea (Decaisne) and the Identification of Its Potential Bioactive Compounds

  • Supardy, Nor Afifah;Ibrahim, Darah;Sulaiman, Shaida Fariza;Zakaria, Nurul Aili
    • Journal of Microbiology and Biotechnology
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    • 제22권6호
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    • pp.872-881
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    • 2012
  • The inhibitory effect of the Klebsiella pneumoniae ATCC 13883 strain caused by the hexane extract of Halimeda discoidea (Nor Afifah et al., 2010) was further evaluated by means of the microscopy view and its growth curves. The morphological changes of the K. pneumoniae ATCC 13883 cells were observed under the scanning electron microscope (SEM) and transmission electron microscope (TEM) after they were treated at minimum inhibitory concentration (MIC; 0.50 mg/ml) (Nor Afifah et al., 2010) for 12, 24, and 36 h. The results showed the severity of the morphological deteriorations experienced by the treated cells. The killing curve assay was performed for 48 h at three different extract concentrations (1/2 MIC, MIC, and 2 MIC). An increase in the extract concentration of up to 2 MIC value did significantly reduce the number of cells by approximately 1.9 $log_{10}$, as compared with the control. Identification of the potential compounds of the extract responsible for the antibacterial activity was carried out through the gas chromatography-mass spectrum (GC-MS) analysis of the active subfraction, and the compound E-15-heptadecenal was identified and suggested as the most potential antibacterial compound of this extract. The subsequent cellular degenerations showed by the data might well explain the inhibitory mechanisms of the suggested antibacterial compound. All of these inhibitory effects have further proven the presence of an antibacterial compound within H. discoidea that can inhibit the growth of K. pneumoniae ATCC 13883.

열처리에 따른 돼지감자 Methanol 추출물의 항산화 및 α-glucosidase 저해 효과 (Antioxidant Activity and α-Glucosidase Inhibitory Effect of Jerusalem Artichoke (Helianthus tuberosus) Methanol Extracts by Heat Treatment Conditions)

  • 정현주;김주성;사여진;김명옥;양금봉;김명조
    • 한국약용작물학회지
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    • 제19권4호
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    • pp.257-263
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    • 2011
  • This study investigated the changes of antioxidant activity and ${\alpha}$-glucosidase inhibitory effect of Jerusalem artichoke (Helianthus tuberosus) 100% methanol extracts by various heat treatment. The contents of total phenolic and flavonoid compounds in methanol extract tended to increased gradually with the rise of temperature to 180$^{\circ}C$. The maximum yield of gallic acid (51.52 ${\pm}$ 2.17mg/g extract weight) and quercetin (13.39 ${\pm}$ 0.03mg/g extract weight) were obtained with extraction temperature of 180$^{\circ}C$ for 120min. In addition, the improving extraction efficiency resulted in the increased biological activities, such as electronic donation ability (EDA, 90.36${\pm}$ 0.57%), reducing power (Abs 1.14) and ${\alpha}$-glucosidase inhibitory effect (92.14 ${\pm}$ 1.14%). Overall, the results of this study indicate that the optimum conditions for the extraction process were an extraction temperature at 180$^{\circ}C$ for 120 min, and will provide the basis for future research on the improving extraction yield of phenolic and flavonoid compounds.

Biological Properties of Different Types and Parts of the Dandelions: Comparisons of Anti-Oxidative, Immune Cell Proliferative and Tumor Cell Growth Inhibitory Activities

  • Lee, Sung-Hyeon;Park, Jae-Bok;Park, Hong-Ju;Cho, Soo-Muk;Park, Young-Ja;Sin, Jeong-Im
    • Preventive Nutrition and Food Science
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    • 제10권2호
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    • pp.172-178
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    • 2005
  • Dandelions have been reported to have medicinal properties and bioactive components that impact human health. However, the precise biological properties of dandelions and the parts of the plants possessing bioactive components remain uncertain. In this study, we evaluated 3 different types of dandelions based on their cultivation origin (Songpa, Uiryung, and native Uiryung types) as well as their 4 different plant parts (leaf, flower, root, skin). Each sample was extracted with $80\%$ methanol and then compared for the biological activities (anti-oxidative, immune cell proliferative and tumor cell growth inhibitory activities). All 3 types of dandelions possessed a degree of biological functions including the hydroxyl radical scavenger activity, immune cell proliferative activity and tumor cell growth inhibitory activity. However, there was no significant difference in these activities between the 3 dandelion types. Leaves of all three dandelion types showed the highest levels of all biological activities. To a lesser degree, the flower and root parts displayed biological activities. In the skin parts, anti-oxidative activity was also detected only at higher doses of dandelion extracts. Heating the dandelion leaf extract did not affect the biological activity, suggesting a heat-stable nature of the biological compounds. Taken together, these collective data suggest that dandelions, in particular their leaves, possess a high concentration of heat-resistant biological compounds, which are responsible for anti-oxidative, immune cell proliferative and tumor cell growth-inhibitory activities.

율무근의 식물화학적 성분 연구 및 Tyrosinase 저해 활성 (Phytochemical constituents of Coix lachryma-jobi var. ma-yuen roots and their tyrosinase inhibitory activity)

  • 최윤혁;최춘환;이재연;안은경;오좌섭;홍성수
    • Journal of Applied Biological Chemistry
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    • 제60권1호
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    • pp.49-54
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    • 2017
  • 본 연구는 천연 미백소재 탐색을 위하여 율무(C. lachryma-jobi var. ma-yuen) 부산물 추출물의 tyrosinase 저해활성을 검증하였으며, 그 중에서 뿌리 추출물은 $159.3g/{\mu}mL$$IC_{50}$ 값을 나타내었다. 율무 뿌리 추출물의 순차적 용매 분획에 대한 활성 검증 후 가장 활성이 우수한 EtOAc 분획물에 대하여 Diaion HP-20 column chromatography, MPLC및 preparative HPLC를 수행해 율무근으로부터 여섯 개의 화합물을 정제하였고, 이 물질들의 구조 분석은 LC-MS와 NMR 데이터 해석을 바탕으로 진행하여 각각 (+)-icariol $A_2$ (1), zhepiresionol (2), 4-hydroxybenzaldehyde (3), trans-${\rho}$-coumaric acid (4), N-(2-hydroxy-4-methoxyphenyl)-2-hydroxyacetamide (5), coixol (6)로 구조를 규명하였다. 화합물 1은 이 식물에서 처음으로 분리되었으며, 화합물 5는 자연계로부터 처음으로 분리된 화합물로 확인하였다. 이들 화합물 중 4-hydroxybenzaldehyde (3), trans-${\rho}$-coumaric acid (4)와 coixol (6)은 순서대로 707.4, 6.5, $62.4{\mu}M$$IC_{50}$ 값을 나타내어 대조군으로 사용한 arbutin ($IC_{50}=618.7{\mu}M$)과 비교시 유사하거나 우수한 활성을 확인하였다. 이로 미루어 보아, 율무근 추출물과 활성물질의 tyrosinase 저해활성을 확인할 수 있었으며, 율무근 추출물의 미백소재로서의 적용 가능성을 확인할 수 있었다.