• Title/Summary/Keyword: Inhibitory Activity

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Inhibitory Effect of Lactobacillus plantarum K11 on the Adhesion of Escherichia coli O157 to Caco-2 Cells

  • Lim, Sung-Mee;Ahn, Dong-Hyun;Im, Dong-Soon
    • Food Science and Biotechnology
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    • v.18 no.2
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    • pp.343-349
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    • 2009
  • Inhibitory effect of Escherichia coli O157 adhered to Caco-2 cells by the cells of Lactobacillus plantarum K11 and the cell-free culture supernatant (CFCS) and bacteriocin prepared from this strain was investigated. As the cell counts of viable L. plantarum K11 previously adhered to Caco-2 were increased, the rate of adhesion and adherent cell counts of E. coli O157 was lower. However, because the heated L. plantarum K11 rarely have the adhesion ability to Caco-2, the adhesion rate and adherent cell counts of E. coli O157 were high. In addition, the inhibitory effects of E. coli O157 adhesion by the CFCS and bacteriocin of L. plantarum K11 were dose-dependent manner. Therefore, the inhibition of adhesion of E. coli O157 to Caco-2 may result from the antimicrobial substances such as lactic acid and bacteriocin. Moreover the inhibitory activity of adhesion by the heated bacteriocin for 30 min at 100oC was similar to activity of non-treated bacteriocin, but the activity was disappeared by treatment with protease.

Development of Cholinesterase Inhibitors Using (a)-Lipoic Acid-benzyl Piperazine Hybrid Molecules

  • Kim, Beom-Cheol;Lee, Seung-Hwan;Jang, Mi;Shon, Min Young;Park, Jeong Ho
    • Bulletin of the Korean Chemical Society
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    • v.34 no.11
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    • pp.3322-3326
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    • 2013
  • A series of hybrid molecules between (${\alpha}$)-lipoic acid (ALA) and benzyl piperazines were synthesized and their in vitro cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibitory activities were evaluated. Even though the parent compounds did not show any inhibitory activity against cholinesterase (ChE), all hybrid molecules showed BuChE inhibitory activity. Some hybrid compounds also displayed AChE inhibitory activity. Specifically, ALA-1-(3-methylbenzyl)piperazine (15) was shown to be an effective inhibitor of both BuChE ($IC_{50}=2.3{\pm}0.7{\mu}M$) and AChE ($IC_{50}=30.31{\pm}0.64{\mu}M$). An inhibition kinetic study using compound 15 indicated a mixed inhibition type. Its binding affinity ($K_i$) value to BuChE is $2.91{\pm}0.15{\mu}M$.

Anti-proliferative and Anti-telomerase Activity of Curcuma Rhizome Extract on Oral Squamous Cell Carcinoma and Osteosarcoma Cells

  • Kim, Kyung-Jin;Kim, Jeong-Hee
    • International Journal of Oral Biology
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    • v.32 no.4
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    • pp.135-141
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    • 2007
  • Anti-proliferation of methanol extract of Curcuma rhizome on oral squamous cell carcinoma (KB) and osteosarcoma (HOS) cells were investigated. In order to elucidate the involvement of telomerase inhibitory activity as a part of anti-proliferative effect of Curcuma rhizome on cancer cells, we measured telomerase activity in Curcuma rhizome extract-treated cancer cells. The concentration inhibited cell proliferation to 50% $(IC_{50})$ of the methanol extract of Curcuma rhizome against oral squamous cell carcinoma (KB) cells and osteosarcoma (HOS) cells were 21.30 ${\mu}g/ml$ and 39.3${\mu}g/ml$, respectively. The methanol extract of Curcuma rhizome showed inhibitory telomerase inhibitory effect which is required for cancer cell immortality. Therefore, it seems that the anticancer effect of methanol extract of Curcuma rhizome is at least partially due to telomerase inhibitory effect. Five fraction samples were prepared according to its polarity differences and analyzed anti-proliferative effects of each fraction samples on oral squamous cell carcinoma and osteosarcoma cells. Anticancer effect was observed in dichloromethane, and ethylacetate fractions. The highest anticancer effect was found in dichloromethane fraction which had $IC_{50}$ value of 23.3 ${\mu}g/ml$ and 10.5${\mu}g/ml$ against oral squamous cell carcinoma (KB) cells and osteosarcoma (HOS) cells, respectively.

Inhibitory effects of Cnidium officinale extracts on $\alpha-MSH$ induced melanogenesis

  • Lee, Ghang-Tai;Lee, Jeong-No;Lee, Kwang-Sik;Jeong, Ji-Hean;Jo, Byoung-Kee
    • Proceedings of the SCSK Conference
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    • 2003.09b
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    • pp.44-49
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    • 2003
  • $\alpha$-MSH plays an important role in UV induced melanogenesis in human skin. It is believed to exert its effects by binding to $\alpha$-MSH receptor that in turn activates adenylate cyclase and increase melanocyte proliferation, dendricity and melanogenesis. In this study, we evaluated plant extracts showing the inhibitory activity on $\alpha$-MSH induced melanogenesis. The Cnidium officinale extracts showed high inhibitory activity on $\alpha$-MSH induced melanogenesis. It ($50{\mu}\textrm{g}$/ml) inhibited the melanin synthesis activated by $\alpha$-MSH in B-16 melanoma cells. Also, we isolated active compound from C. officinale extracts by Mass spectrophotometer, HPLC. It was identified as Senkyunolide A. It showed the same inhibitory activity as C. officinale extracts at the lower concentration. Finally, Senkyunolide A from Cnidium officinale extracts could playas $\alpha$-MSH antagonist and be used as a strong ingredient for skin whitening cosmetics.

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γ-Aminobutyric Acid (GABA) Production and Angiotensin-I Converting Enzyme (ACE) Inhibitory Activity of Fermented Soybean Containing Sea Tangle by the Co-Culture of Lactobacillus brevis with Aspergillus oryzae

  • Jang, Eun Kyeong;Kim, Nam Yeun;Ahn, Hyung Jin;Ji, Geun Eog
    • Journal of Microbiology and Biotechnology
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    • v.25 no.8
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    • pp.1315-1320
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    • 2015
  • To enhance the γ-aminobutyric acid (GABA) content, the optimized fermentation of soybean with added sea tangle extract was evaluated at 30℃ and pH 5.0. The medium was first inoculated with Aspergillus oryzae strain FMB S46471 and fermented for 3 days, followed by the subsequent inoculation with Lactobacillus brevis GABA 100. After fermentation for 7 days, the fermented soybean showed approximately 1.9 g/kg GABA and exhibited higher ACE inhibitory activity than the traditional soybean product. Furthermore, several peptides in the fraction containing the highest ACE inhibitory activity were identified. The novel fermented soybean enriched with GABA and ACE inhibitory components has great pharmaceutical and functional food values.

Evaluation of Antioxidant, Anti-cholinesterase, and Anti-inflammatory Effects of Culinary Mushroom Pleurotus pulmonarius

  • Nguyen, Trung Kien;Im, Kyung Hoan;Choi, Jaehyuk;Shin, Pyung Gyun;Lee, Tae Soo
    • Mycobiology
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    • v.44 no.4
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    • pp.291-301
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    • 2016
  • Culinary mushroom Pleurotus pulmonarius has been popular in Asian countries. In this study, the anti-oxidant, cholinesterase, and inflammation inhibitory activities of methanol extract (ME) of fruiting bodies of P. pulmonarius were evaluted. The 1,1-diphenyl-2-picryl-hydrazy free radical scavenging activity of ME at 2.0 mg/mL was comparable to that of butylated hydroxytoluene, the standard reference. The ME exhibited significantly higher hydroxyl radical scavenging activity than butylated hydroxytoluene. ME showed slightly lower but moderate inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase than galantamine, a standard AChE inhibitor. It also exhibited protective effect against cytotoxicity to PC-12 cells induced by glutamate ($10{\sim}100{\mu}g/mL$), inhibitory effect on nitric oxide (NO) production and inducible nitric oxide synthase protein expression in lipopolysaccharide-stimulated RAW 264.7 macrophages, and carrageenan-induced paw edema in a rat model. High-performance liquid chromatography analysis revealed the ME of P. pulmonarius contained at least 10 phenolic compounds and some of them were identified by the comparison with known standard phenolics. Taken together, our results demonstrate that fruiting bodies of P. pulmonarius possess antioxidant, anti-cholinesterase, and inflammation inhibitory activities.

The Inhibitory Constituents from the Ginger on a Drug Metabolizing Enzyme CYP3A4 (생강의 약물대사효소 CYP3A4 저해 성분)

  • 차배천;이은희;권준택
    • YAKHAK HOEJI
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    • v.48 no.5
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    • pp.266-271
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    • 2004
  • Ginger (Zingiber officinale Roscoe) is widely used as a common condiment for a variety of foods and beverages. In addition to its extensive utilization as a spice, the fresh or the processed rhizome is a useful crude drug in traditional Chinese medicine. It is considered to possess stomachic, carminative, stimulant, diuretic and antiemetic properties. Chemical studies on the pungent principles of ginger have been carried out by a number of investigators, and 6-gingerol and 6-shogaol as a major pungent substance have been isolated. In this study, the constituents inhibiting a drug metabolizing enzyme CYP3A4 from ginger were investigated. CYP3A4 is responsible for drug metabolism as heme-containing monooxygenases. As a result of experiment, 10-gingerol (lC$_{50}$ 5.75$\mu$M) isolated from EtOAc extract of ginger showed remarkable inhibitory activity compared to 6-gingerol ($IC_{50}$/ 14.56 $\mu$M) and zingerone ($IC_{50}$/ 379.63 $\mu$M). This paper describes the isolation, structure elucidation, and CYP3A4 inhibitory activity of these compounds. The structure of the compounds were identified by instrumental analysis such as LC-mass spectrometer and NMR.R.

Cytotoxic and COX-2 Inhibitory Constituents from the Aerial Parts of Aralia cordata

  • Lee, Ik-Soo;Jin, Wen-Yi;Zhang, Xin-Feng;Hung, Tran-Manh;Song, Kyung-Sik;Seong, Yeon-Hee;Bae, Ki-Hwan
    • Archives of Pharmacal Research
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    • v.29 no.7
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    • pp.548-555
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    • 2006
  • Three diterpenes (1, 8, and 9), three triterpenes (3, 4, and 7), one saponin (11), four sterols (2, 5, 6, and 12), and one cerebroside (10) were isolated from the EtOH extract of the aerial parts of Aralia cordata by repeated silica gel column chromatography. Their chemical structures were identified by comparing their physicochemical and spectral data with those published in literatures. All isolated compounds were evaluated for their cytotoxicity against L1210, K562, and LLC tumor cell lines using MTT assay. Of which, $3{\beta},5{\alpha}-dihydroxy-6{\beta}-methoxyergosta-7,22-diene$ (6) showed a potent cytotoxicity against all cell lines with $IC_{50}$ values of 11.7, 11.9, and $15.1\;{\mu}M$, respectively, while compounds 1, 5, and 11 showed a moderate or weak cytotoxicity. These isolates were also examined for their inhibitory activity against COX-1 and COX-2. Although most compounds, except for 2, 10, and 12, showed a strong inhibitory activity against COX-1, they exhibited a moderate or weak inhibitory activity against COX-2.

Anti-aging and Anti-dementia Activities of Different Solvent Extracts from Silvetia siliquosa (뜸부기(Silvetia siliquosa) 추출물의 항노화 및 항치매 활성)

  • Ji-Won Choi;Yeon-Ji Lee;Won-Suk Kim;Soo-Kyung Moon;Yong-Tae Kim
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.56 no.4
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    • pp.526-531
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    • 2023
  • This study investigated the ingredients, anti-aging and anti-dementia activities of the Korean marine algae Silvetia siliquosa. The S. siliquosa solvent extracts were prepared with 70% ethanol, 80% methanol, and distilled water. The extraction yield range of various solvent extracts was 15.82-49.98%. The ethanol and methanol extracts had higher tyrosinase and collagenase inhibitory activities than those of the water extract. Meanwhile, all extracts exhibited high elastase inhibitory activity. Conversely, the methanol and water extracts exhibited the highest acetylcholinesterase inhibitory activity (IC50, 0.40 mg/mL) and β-secretase inhibitory activity (IC50, 0.81 ㎍/mL), respectively. These results indicate that S. siliquosa may be useful in food and pharmaceutical materials as a cosmetic and functional.

Acetylcholinesterase Inhibitory and Antioxidant Properties of Aster yomena Extract (쑥부쟁이 추출물의 아세틸콜린에스테라제 저해 및 항산화 활성)

  • Bae, Jong-Sup;Kim, Tae-Hoon
    • The Korea Journal of Herbology
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    • v.24 no.4
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    • pp.121-126
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    • 2009
  • Objectives : To evaluate the radical scavenging and acetylcholinesterase (AChE) inhibitory activities of the ethylacetate (EtOAc)-soluble portion of a methanolic extract of Aster yomena, three different assay systems were performed. Methods : The antioxidant activity of A. yomena extract was tested as its capacity to scavenging free radicals of DPPH and $ABTS^+$, which has been widely used to evaluate the antioxidant activity of natural products from plant sources. AChE inhibitory activity was tested against mouse brain AChE by spectrophotometric method of Ellman using ELISA microplate reader. Results : The methanolic extract of A. yomena was fractionated and the EtOAc-soluble portion showed significant AChE inhibitory and free radical scavenging effects. Also the EtOAc-soluble portion revealed the highest phenolic contents as compared to the other extracts. Conclusions : These results indicate that phenolic compounds may be important constituents that give rise to the anti-AChE and antioxidative activities of A. yomena extract. Further phytochemical studies on this plant, for nutraceutical or pharmaceutical application, are warranted.