• Title/Summary/Keyword: inhibition activities

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Inhibition of Various Proteases by MAPI and Inactivation fo MAPI by Trypsin

  • Lee, Hyun-Sook;Kho, Yung-Hee;Lee, Kye-Joon
    • Journal of Microbiology and Biotechnology
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    • v.10 no.2
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    • pp.181-186
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    • 2000
  • MAPI (microbial alkaline protease inhibitor) was isolated from cultrue broth of Streptomyces chromofuscus SMF28. The Ki values of MAPI for the representative serine proteases such as chymotrypsin and proteinase K were 0.28 and $0.63{\;}\mu\textrm{M}$, respectively, and for the cysteine proteases cathepsin B and papain were 0.66 and $0.28{\;}\mu\textrm{M}$, respectively. These data indicate that MAPI is not a potent selective inhibitor of serine or cysteine proteases. Progress curves for the inhibition of three proteases by MAPI exhibithe characteristic patterns; MAPI exhibited slow-binding inhibition of cathepsin B. It was rapidly associated with chymotrypsin before the addition of substrate and then reactivation of MAPI-inhibited enzyme was investigated in the presence of substrate. On the other hand, MAPI-proteinase K interaction was typical for those classical inhibitors. When MAPI was incubated with trypsin, there was an extensive reduction in the ingibitory activities of MAPI corresponding to 66.5% inactivation of MAPI, indicating that trypsin-like protease may play a role in the decrease of the inhibitory activity during cultivation.

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Study on DPPH Free Radical Scavenging and Lipid Peroxidation Inhibitory Activities of Vietnamese Medicinal Plants

  • Phan, Thi Anh Dao;Nguyen, Xuan Hai;Nguyen, Trung Nhan;Tran, Le Quan;Nguyen, Thi Thanh Mai
    • Natural Product Sciences
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    • v.18 no.1
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    • pp.1-7
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    • 2012
  • Among 90 Vietnamese medicinal plant extracts investigated for their antioxidant activity by DPPH assay at various concentrations from $10-100{\mu}g/mL$, 67 showed an inhibition rate over 50% at $100{\mu}g/mL$; 47 had greater than 50% inhibition at $50{\mu}g/mL$; 17 showed over 50% inhibition at $25{\mu}g/mL$. 8 extracts which exhibited strong inhibitory activity more than 50% inhibition at $10{\mu}g/mL$ were further tested for lipid peroxidation inhibition by TBA assay. They displayed activity with $IC_{50}$ values from 30.6 to $158.9{\mu}g/mL$. Until now, this is the first report on antioxidant activity of the female flower of Borassus flabellifer, and the stem of Combretum latifolium, Embelia ribes, Spatholobus parviflorus, and Tetrastigma erubescens. Fractionations of the EtOAc extract prepared from S. parviflorus led to the isolation of protocatechuic acid (1), ferulic acid (2), epicatechin (3), and gallic acid (4). These compounds showed significant DPPH inhibitory activity with $IC_{50}$ values from 6.5 to $23.6{\mu}M$.

Inhibition of the Activity of Phosphoinositide-Specific Phospholipase C Isozymes by Antipsychotics and Antidepressants

  • Joo, Yeon-Ho;Park, Eun-Sil;Park, Joo-Bae;Suh, Pann-Ghill;Kim, Yong-Sik;Ryu, Sung-Ho
    • Biomolecules & Therapeutics
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    • v.1 no.1
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    • pp.121-124
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    • 1993
  • To elucidate the effect of antipsychotics and antidepressants on phosphoinositide(Pl) second massenger system, we studied the dose-dependent inhibition of the phosphoinositide-specific phospholipase C(PLC) isozymes, ${\beta}_1,\;{\gamma}_1$ and${\delta}_1,$ by fluphenazine and haloperidol as antipsychotics, and amitriptyline, maprotiline and mianserin as antidepressants. All the antipsychotics and antidepressants tested showed inhibition on at least one of the PLC isozymes with $IC_{50}$ at the concentration between 25 and $250 {\mu}M.$ Maprotiline, mianserin and amitriptyline inhibited 80 to 90% of the activities of all three PLC isozymes at the concentration of $250{\mu}M,$ while haloperidol and fluphenazine inhibited PLC ${\beta}_1$ and${\gamma}_1$ But baclofen didn't inhibit any PLC isozyme. These results suggested that PLC isozymes are inhibited by antipsychotics and antidepessants even though the concentration is high, and these drugs may affect PI signal transduction system by direct inhibition of PLC isozymes.

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Melanin synthesis and skin wrinkle inhibitory effects of the medicinal mushroom Ganoderma applanatum

  • Yoon, Ki Nam;Lee, Tae Soo
    • Journal of Mushroom
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    • v.19 no.3
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    • pp.150-159
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    • 2021
  • Anti-melanogenesis and skin anti-wrinkle effects of methanol (ME) and hot water (HE) extracts from the fruiting bodies of Ganoderma applanatum were investigated in this study. The total phenolic contents of the ME and HE of the mushroom were 11.68 and 3.15 ㎍ GAEs/mg, respectively, whereas the total flavonoid contents of the ME and HE were 21.82 and 2.69 ㎍ QEs/mg, respectively. The survival rate of B16-F10 murine melanoma cells treated with 750 ㎍ ME and HE were 83.46% and 85.54%, respectively, thereby suggesting that mushroom extracts were slightly cytotoxic at the tested concentration. The in vitro tyrosinase inhibition by ME (83.15%) and HE (83.44%) was significantly lower than that of kojic acid (99.61%), the positive control, at 2.0 mg/mL. Although the inhibition of cellular melanin synthesis in B16-F10 melanoma cells by 2.0 mg/mL of ME (50.24%) and HE (51.24%) was lower than that of arbutin (64.84%), the inhibition by both ME and HE was higher than 50%. Collagenase inhibition by HE was comparable to 2.0 mg/mL epigallocatechin (EGCG), the positive control; however, elastase inhibition by ME and HE was lower than that of EGCG at the concentration tested. The results showed that the fruiting bodies of G. applanatum had good anti-tyrosinase, good anti-collagenase, and moderate anti-elastase activities, which might be useful for developing novel skin-whitening and anti-wrinkle agents.

Physicochemical Characteristics and Physiological Activities of Naturally Fermented Glasswort (Salicornia herbacea L.) Juice (자연발효 함초액의 이화학적 특성 및 생리활성)

  • Park, Sun-Young;Cho, Jeong-Yong;Chung, Dong-Ok;Ham, Kyung-Sik
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.40 no.11
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    • pp.1493-1500
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    • 2011
  • We investigated the physicochemical properties and physiological activities of glasswort juice fermented naturally for different periods of time. Glasswort juice fermented for six years (LFGJ) showed higher crude fiber and lower NaCl content than glasswort juice fermented for two years (SFGJ). Fermented glasswort juice contained K, Mg, and Ca as the main minerals, and the mineral content in both SFGJ and LFGJ were similar. The main free amino acids of fermented glasswort juice were determined to be alanine, proline, aspartic acid, and lysine. The leucine and aspartic acid content in LFGJ was higher than that in SFGJ. SFGJ had higher 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS$^+$) radical-scavenging activities than LFGJ. Fermented glasswort juice showed high ACE inhibition and ${\alpha}$-glucosidase inhibition activities regardless of how long it was fermented. An oral glucose tolerance test was carried out in rats fed diets containing 4% NaCl (control) or 4% NaCl+2% LFGJ (LFGJ). The LFGJ group showed enhanced glucose tolerance compared to the control group.

Potent Inhibition of Monoamine Oxidase B by a Piloquinone from Marine-Derived Streptomyces sp. CNQ-027

  • Lee, Hyun Woo;Choi, Hansol;Nam, Sang-Jip;Fenical, William;Kim, Hoon
    • Journal of Microbiology and Biotechnology
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    • v.27 no.4
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    • pp.785-790
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    • 2017
  • Two piloquinone derivatives isolated from Streptomyces sp. CNQ-027 were tested for the inhibitory activities of two isoforms of monoamine oxidase (MAO), which catalyzes monoamine neurotransmitters. The piloquinone 4,7-dihydroxy-3-methyl-2-(4-methyl-1-oxopentyl)-6H-dibenzo[b,d]pyran-6-one (1) was found to be a highly potent inhibitor of human MAO-B, with an $IC_{50}$ value of $1.21{\mu}M$; in addition, it was found to be highly effective against MAO-A, with an $IC_{50}$ value of $6.47{\mu}M$. Compound 1 was selective, but not extremely so, for MAO-B compared with MAO-A, with a selectivity index value of 5.35. Compound 1,8-dihydroxy-2-methyl-3-(4-methyl-1-oxopentyl)-9,10-phenanthrenedione (2) was moderately effective for the inhibition of MAO-B ($IC_{50}=14.50{\mu}M$) but not for MAO-A ($IC_{50}$ > $80{\mu}M$). There was no time-dependency in inhibition of MAO-A or -B by compound 1, and the MAO-A and -B activities were almost completely recovered in the dilution experiments with an excess amount of compound 1. Compound 1 showed competitive inhibition for MAO-A and -B, with $K_i$ values of 0.573 and $0.248{\mu}M$, respectively. These results suggest that piloquinones from a microbial source could be potent reversible MAO inhibitors and may be useful lead compounds for developing MAO enzyme inhibitors to treat related disorders, such as depression, Parkinson's disease, and Alzheimer's disease.

Antimicrobial Activities of Viscous Substance from Chongkukjang Fermented with different bacillus spry. (청국장 발효 세균의 종류에 따른 청국장 정절물의 항 미생물 활성에 관한 연구)

  • 윤호경;최희선;허성호;홍정화
    • Journal of Food Hygiene and Safety
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    • v.16 no.3
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    • pp.188-193
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    • 2001
  • To evaluate antimicrobial activities of chongkukjang slime fermented by different strains, growth characteristics were compared using various standard microorganisms with addition of chongkykjang slime. Chonghkjang slime was prepared by fermenting cooked soybean after inoculating with Bacillus circulans K-1, Baciilus spp N-1 and Bacillus subtilis CH-1, respectively. Significant antimicrobial activity was observed by chongkukjang slime on gram positive bacteria (Staphylococcus aureus, Bacillus cereus, Bacillus subtilis, Micrococcus luteus), gram negative bacteria(Escherichia coli O157:H7, Salmonella Typhimurium, Pseudomonas fluorescens), and yeast (Pichia membranaefaciens, Saccharomyces cerevisiae, Candida albicans). In case of B. cereus growth inhibition of 80% was achieved by the addition of chongkukjang slime; on the contrary, to Escherichia coli O157:H7 only 20% inhibition was observed. Slime from Bacillus subtilis CH-1, in particular, inhibition of 40% toward bacteria and yeast, whereas slime from Bacillus circulans K-1, Bacillus spp N-1 showed only 20% inhibition.

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Screening of Biological Activity of Solvent Extract from Styela clava Tunic for Fishery Waste Recycling (수산폐기물 재활용을 위한 미더덕껍질 용매 추출물의 생리활성 탐색)

  • Lee, Sang-Mee;Kang, Eun-Jin;Go, Tae-Hun;Jeong, Seong-Yun;Park, Geun-Tae;Lee, Hee-Sup;Hwang, Dae-Youn;Jung, Young-Jin;Son, Hong-Joo
    • Journal of Environmental Science International
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    • v.23 no.1
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    • pp.89-96
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    • 2014
  • Styela clava tunic is generated in large amounts as a waste from S. clava processing plants and causes environmental problem. Although biological activities of S. clava were reported by many investigators, study on S. clava tunic was little. In this study, therefore, tyrosinase inhibition and antioxidative activities of extracts from S. clava tunic using different solvent were investigated for recycling of the fishery waste. Among extraction methods tested, autoclaved extraction (25.7%) and hot water extraction (18.2%) appeared to be effective for extraction. The highest total phenolic content was 46.6 mg/g in autoclaved extract while the highest flavonoid content was 23.0 mg/g in chloroform extract. All extracts possessed tyrosinase inhibition activity and the inhibition activity was concentration-dependent. Inhibition concentration ($IC_{50}$) against tyrosinase activity was $0.36{\times}10^4$ mg/ml in ethanol extract, $0.11{\times}10^3$ mg/ml in acetone extract and 0.27 mg/ml in n-butanol extract. Among extracts tested, hot water and autoclaved extracts displayed higher antioxidative activity than organic solvent extracts. Therefore, our data suggest that extract from S. clava tunic may potential candidate for cosmetic product with whitening effect and medicine for diseases caused by various oxidative stresses.

Biological Activity of Methanolic Extract from Ganoderma lucidum, Momordica charantia, Fagopyrum tataricum, and Their Mixtures (영지버섯, 여주, 쓴메밀 및 혼합 시료의 메탄올 추출물의 생리활성)

  • Cha, Jae-Young;Jin, Jong-Sung;Cho, Young-Su
    • Journal of Life Science
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    • v.21 no.7
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    • pp.1016-1024
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    • 2011
  • The concentrations of bioactive material (polyphenolics and flavonoids) and the biological activities of antioxidative (DPPH [${\alpha},{\alpha}'$-diphenyl-${\beta}$-picrylhydrazyl] free radical scavenging activity, peroxidation of rat liver microsome, and Fe/Cu reducing power), ${\alpha}$-glucosidase inhibition, tyrosinase inhibition, and fibrinolytic activity were tested by in vitro experimental models using 70% methanolic extract from Ganoderma lucidum, Momordica charantia, Fagopyrum tataricum and their mixtures. The highest yield and the concentrations of polyphenolics and flavonoids were shown in the mixture extract. Mixture extract was shown to have the highest activities of ${\alpha}$-glucosidase inhibition and tyrosinase inhibition, fibrinolytic, DPPH free radical scavenging, and Fe/Cu reducing power in a concentration-dependent manner. From these results, mixture methanol extract was shown to have the most potent bioactive properties and to contain large amounts of biological materials such as polyphenolics and flavonoids. This mixture could be a good dietary supplement material candidate, such as for antidiabetic functional foods.

Growth Inhibitory Effects of Chloride Salts and Organic Acid Salts Against Food-Borne Microorganisms (Chloride염 및 유기산 칼슘염의 식중독 미생물에 대한 증식 억제 효과)

  • 이나영;김용석;신동화
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.32 no.8
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    • pp.1233-1238
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    • 2003
  • The growth inhibitory effects of chloride salts and organic acid salts against six food-borne microorganisms (Bacillus cereus ATCC 11778, Escherichia coli O157:H7 ATCC 43894, Listeria monocytogenes ATCC 19111, Salmonella Typhimurium ATCC 14028, Staphylococcus aureus ATCC 25923, Vibrio parahaemolyticus ATCC 17802) were determined using Bioscreen C in broth medium. The growth inhibitory concentrations of sodium chloride and potassium chloride on B. cereus were 7 and 9%, respectively. E. coli O157:H7 and S. aureus were inhibited by treatment of 3% calcium chloride. Magnesium chloride showed growth inhibitory effect on B. cereus, S. Typhimurium, and S. aureus at 5%. The order of growth inhibition effects by organic acid salts was calcium propionate>calcium acetate>calcium lactate. Calcium chloride (3%) with 0.01% lactic acid showed strong inhibition on the growth of S. Typhimurium and exhibited stronger growth inhibition than calcium chloride alone (5%). We concluded that calcium chloride and calcium propionate had strong growth inhibitory activities and that calcium chloride and sodium chloride in combination with lactic acid had stronger inhibitory activities than that of chloride salts alone.