• Title/Summary/Keyword: Inhibitory Activity

Search Result 7,150, Processing Time 0.035 seconds

Inhibitory effect of Capparis zeylanica Linn. on acetylcholinesterase activity and attenuation of scopolamine-induced amnesia

  • Chaudhary, Amrendra Kumar;Solanki, Ruchi;Singh, Vandana;Singh, Umesh Kumar
    • CELLMED
    • /
    • v.2 no.2
    • /
    • pp.19.1-19.6
    • /
    • 2012
  • $Capparis$ $zeylanica$ Linn. a 'Rasayana' drug is used for its memory enhancing effects in the traditional Ayurvedic system of medicine. The aim of this study was to evaluate acetylcholinesterase (AChE) inhibitory and memory enhancing activities of $Capparis$ $zeylanica$ Linn. The$in-vitro$ and $ex-vivo$ models of AChE inhibitory activity were used along with Morris water maze test to study the effect on memory in rats. The anticholinesterase effect of methanolic and aqueous extracts of $Capparis$ $zeylanica$ was measured by spectrophotometric Ellman method at 0.1, 0.3, 1.0, 3.0, 10 and 30 mg/ml and brain monoamine oxidase (MAO-A and MAO-B) activity was assessed by Naoi's method. The results $in-vitro$ and $ex-vivo$ AChE assay revealed that methanolic and aqueous extracts of $Capparis$ $zeylanica$ inhibit AChE activity, whereas these extracts did not alter MAO activity at any concentration tested as compared to moclobemide and L-deprenyl. The results indicate that $Capparis$ $zeylanica$ improves scopolamine-induced memory deficits through inhibition of AChE activity, and not by direct MAO inhibition.

Comparison of the Physiological Activity of Extracts of Bark and Cork Layer from Prunus sargentii (산벚나무 수피 및 코르크층 추출물의 생리활성 비교)

  • Lee, Kyoung-In;Yang, Sun-Ah;Pyo, Byoung-Sik;Kim, Sun-Min
    • Korean Journal of Pharmacognosy
    • /
    • v.42 no.2
    • /
    • pp.169-174
    • /
    • 2011
  • In this study, we investigated on antioxidative activity, antibacterial activity and tyrosinase inhibitory activity in 75% ethanol extracts of bark and cork layer from Prunus sargentii. The total polyphenol content of cork and bark extract was found to be 217.4 mg/g and 184.3 mg/g. And flavonoid content was found to be 31.9 mg/g and 58.6 mg/g respectively. In DPPH radical scavenging ability, cork extract was exhibited stronger scavenging ability than bark extract. Moreover, cork extract was showed higher inhibitory activity than bark extract in tyrosinase inhibitory activity. In antibacterial activity, bark extract was showed higher growth inhibition effect than cork extract against tested bacterial strains. In measurement of cytotoxicity by MTT assay, bark and cork extract showed fine cell viabilities(95.7~120.9%) against RAW 264.7 cell.

Inhibitory Effect of Metabolites isolated from Streptococcus mutas sp. M-20 on Glucosyltransferase Activity from Streptococcus mutans (Streptomyces sp. M-20 균의 대사물에 의한 Streptococcus mutans의 Glucosyltransferase 활성 억제 효과)

  • Kim, Kyoung-Ja
    • YAKHAK HOEJI
    • /
    • v.49 no.2
    • /
    • pp.122-127
    • /
    • 2005
  • Dental caries is one of the most common oral diseases in the world. Glucosyltransferase (Gtase) of Streptococcus mutans (S. mutans) plays an important role in the develo pment of dental caries. For the purpose to develop anti- caries, we examined the effect of metabolites isolated from Streptomyces sp. M-20 on Gtase and the growth of S. mutans. Streptomyces sp. M-20 isolated from Mongolian soil showed 95~96% sequence homology with that of Streptomyces lin- colnensis. The metabolites of Streptomyces sp. M-20 were partially purified by extraction with ethyl acetate, silica gel column chromatography and preparative TLC. Partially purified metabolite, red colored component (MR-20) in ethyl acetate fraction showed potent antibacterial activitiy against S. mutans and inhibitory activity against Gtase purified from S. mutans, while another isolated yellow component (MY-20) showed no activity against S. mutans. The inhibitory activity of MR-20 against Gtase was confirmed by activity staining on SDS-polyacrylamide gel electrophoresis. The concentration of MR-20 for 50% inhibition $(IC_{50})$ against Gtase activity was $60{\mu}g/ml$. These results suggest that MR-20 can be developed for antibacterial agent and anticaries.

EFFECT OF ZIZYPHI FRUCTUS EXTRACT ON THE BIOLOGICAL ACTIVITY OF GINGIVAL FIBROBLAST (대조 추출물분획이 치은 섬유아세포의 생물학적 활성화에 미치는 영향)

  • Yang, Chang-Ho;Lee, Yong-Moo;Cho, Ki-Yeong;Bae, Ki-Hwan;Chung, Chong-Pyoung
    • Journal of Periodontal and Implant Science
    • /
    • v.24 no.1
    • /
    • pp.144-154
    • /
    • 1994
  • Final goal of periodontal treatment is to reconstruct the destructed periodontal tissue as well as to remove the necrotic pathologic elements. The purpose of this study is to investigate on the effect of Zizyphi extract to the inhibitory ability on collagenolytic activity of P gingivalis, biologic activity of gingival fibroblasts, and on the collagen and protein synthesis of gingival fibroblasts. Gingival fibroblast from giniva of first bicuspids from patient for orthodontic treatment were used and cultured. For the measurement of inhibitory ability of collagenolytic activity, crude enzyme was extracted and used on the basis of modified Ono's method. On the inhibition of collagenolytic enzyme from herbal extracts, collagenokit CLN-100 were used. The cellular activity of gingival fibroblast, were studied using MTT solution and measured optical density on 570mm by ELISA reader. To measure the effects on the ability of whole protein and collagen synthesis, cell membrane was destructed with ultrasonic grinder after culturing, centrifuged and counted by liquid scintilation counter. The inhibitory effects on producing of $IL-l{\beta}$ by monocyte, after promotion of producing $IL-l{\beta}$ by LPS, were compared with the mixture of herbal extracts and other drugs using thymocyte stimulation assay. About inhibitory effects of $PGF_2$. by gingival fibroblasts, herbal extract was compared with the addition of the other control groups using enzyme imunoassay. On the inhibition of collagenolytic activity by P. gingivalis, benzene extracts showed the most efficient inhibitory effects among the $19{\mu}g/ml$ of the compared extracts and 40.5% by Tetracycline. On the cellular activity promoting effects, compared extracts showed a bit of more effects than PDGF of $100{\mu}g/ml$ concentration and IGF of $20{\mu}g/ml$ concentration. All of the PDGF, IGF, Zizyphi Fructus extract should increase in collagen synthesis, but especially 70% ethylalcohol extracts of Zizyphi Fructus showed comparably high effects among the compared extracts. Effects on whole protein synthesis were slightly increased on every extract but especially 70% ethylalcohol extract showed significantly effective than any other estract. On the inhibitory effects of Zizyphi Fructus $IL-l{\beta}$ production by monocyte, compared extracts showed 70% of highly inhibitory effect than that of 60% inhibition effects on controlled group and each extracts showed no significant difference. In $PGF_2$ production inhibitroy effect of Zizyphi Fructus gingival fibroblasts, Herbal extracts showed 70% of inhibition comparing with tat of 90.2% of controlled group, but each extracts showed similar effects excluding the $H_2O$ extracts. These results suggested that Zizyphi Fructus might be useful medicine for inhibition of inflammatory mediator including $IL-l{\beta}$ and $PGF_2$.

  • PDF

Antioxidant Activity and Inhibitory Activities of Xanthine Oxidase and Tyrosinase of Yeasts from Wild Flowers in Korea (우리나라 야생화에서 분리한 효모의 항산화 활성과 Xanthine Oxidase 및 Tyrosinase 저해활성)

  • Han, Sang-Min;Hyun, Se-Hee;Kim, Na-Mi;Lee, Jong-Soo
    • The Korean Journal of Mycology
    • /
    • v.43 no.2
    • /
    • pp.99-103
    • /
    • 2015
  • We prepared supernatants and cell-free extracts of yeasts isolated from wild flowers in Korea, and their antioxidant activity and inhibitory activities of xanthine oxidase and tyrosinase were investigated. Among them, cell-free extracts of Kuraishia capsulata UL40-2 and Sporobolomyces ruberrimus 121-Z-3 showed significantly high xanthine oxidase inhibitory activity of 46.4% and 48.3%, respectively. Starmerella bombicola 80-J-1 also showed tyrosinase inhibitory activity of 36.2% in the cell-free extract. Other antioxidant activities and tyrosinase inhibitory activities were not detected or were below 20%. Maximal production of the xanthine oxidase inhibitors were observed when Kuraishia capsulate UL40-2 and Sporobolomyces ruberrimus 121-Z-3 were cultured in the yeast extract-peptone-dextrose media at $30^{\circ}C$ for 24 hour, respectively.

In vitro Inhibitory Activity on Rat Intestinal Mucosa ${\alpha}-glucosidase$ by Rice Hull Extract (왕겨추출물의 쥐소장점막 ${\alpha}-glucosidase$에 대한 in vitro에서의 저해효과)

  • Kim, Hye-Young
    • Korean Journal of Food Science and Technology
    • /
    • v.29 no.3
    • /
    • pp.601-608
    • /
    • 1997
  • In order to search for the way to utilize rice hull as a renewable resource, the inhibition on ${\alpha}-glucosidase$ and the fractionation of rice hull extract was investigated. An ethanol extract of rice hull from Japonica-type rice seeds exhibited 30% inhibitory activity on rat intestinal brush border ${\alpha}-glucosidase$ (1.4 mU/mL) in vitro at the concentration of 0.8 mg/mL using 6 mM p-nitrophenyl ${\alpha}-D-glucopyranoside$ as a substrate $(IC_{50}\;162\;mg/mL)$. Among the fractions obtained by partitioning the ethanol extract successively with solvents, the ethyl acetate fraction at the concentration of 0.8 mg/mL was found to exhibit the most potent inhibitory activity i.e. 65% inhibition of ${\alpha}-glucosidase\;(IC_{50}\;0.14\;mg/mL)$. Silica gel column chromatography of the ethyl acetate fraction exhibited slightly higher (90%) inhibitory activity, and its subsequent fractionation by Sephadex LH-20 column chromatography did not improve inhibitory activity. Considering the inhibitory activity and yield, the ethyl acetate fraction obtained by the solvent-partitioning process would be a candidate for the hypoglycemic food if it has in vivo effectiveness.

  • PDF

Inhibitory Effect of the Phenolic Compounds from Geranium thunbergii on Rat Lens Aldose Reductase and Galactitol Formation (현초에서 분리된 페놀성 화합물들의 흰쥐 수정체 유래 알도즈 환원효소 및 갈락티톨 생성 억제 효과)

  • Choi, Se-Jin;Kim, Jin-Kyu;Jang, Jai-Man;Lim, Soon-Sung
    • Korean Journal of Medicinal Crop Science
    • /
    • v.20 no.4
    • /
    • pp.222-230
    • /
    • 2012
  • We evaluated the inhibitory effects of extracts and components of Geranium thunbergii on aldose reductase (AR) and galactitol formation in rat lenses with high levels of galactose as a part of our ongoing search of natural sources for therapeutic and preventive agents for diabetic complications. The inhibitory effects of water, methanol and ethanol extracts of G. thunbergii on rat lens AR (RLAR) were determined. Comparing inhibitory effects of various solvent extracts, ethanol extract showed RLAR inhibitory activity ($IC_{50}$ values, 5.24 and $6.39{\mu}g/m{\ell}$, respectively). The ethanol extract was fractionated to chloroform, ethyl acetate and water. Of these, the ethyl acetate fraction from ethanol extract of G. thunbergii exhibited RLAR inhibitory activity ($IC_{50}$ value, $2.64{\mu}g/m{\ell}$). In order to identify the bioactive components of ethyl acetate soluble fraction of ethanol extract from G. thunbergii, eight compounds, namely gallic acid (1), protocatechuic acid (2), p-hydroxybenzoic acid (3), brevifolin carboxylic acid (4), geraniin (5), ellagic acid (6), kaempferol-3-O-arabinofuranosyl-7-O-rhamnopyranoside (7), kaempferitrin (8) were isolated. The isolates were subjected to in vitro bioassays to evaluate their inhibitory activity on RLAR and galactitol formation in rat lenses. The ellagic tannins (5, 6) and flavonoid (7) exhibited strong inhibitory effects on RLAR. Also, these three compounds (5, 6 and 7) suppressed galactitol accumulation in rat lens under high galactose conditions, demonstrating the potential to prevent galactitol accumulation exo vivo. These results suggest that the extracts and components of G. thunbergii are a promising agent in the prevention or treatment of diabetic complications.

Separation and Purification of Angiotensin Converting Enzyme Inhibitory Peptides Derived from Goat's Milk Casein Hydrolysates

  • Lee, K.J.;Kim, S.B.;Ryu, J.S.;Shin, H.S.;Lim, J.W.
    • Asian-Australasian Journal of Animal Sciences
    • /
    • v.18 no.5
    • /
    • pp.741-746
    • /
    • 2005
  • To investigate the basic information and the possibility of ACE-inhibitory peptides for antihypertension materials, goat's caisin (CN) was hydrolyzed by various proteolytic enzymes and ACE-inhibitory peptides were separated and purified. ACE-inhibition ratios of enzymatic hydrolysates of goat's CN and various characteristics of ACE-inhibitory peptides were determined. ACE-inhibition ratios of goat's CN hydrolysates were shown the highest with 87.84% by pepsin for 48 h. By Sephadex G-25 gel chromatograms, Fraction 3 from goat's CN hydrolysates by pepsin for 48 h was confirmed the highest ACE-inhibition activity. Fraction 3 g and Fraction 3 gh from peptic hydrolysates by RP-HPLC to first and second purification were the highest in ACE-inhibition activity, respectively. The most abundant amino acid was leucine (18.83%) in Fraction 3 gh of ACE-inhibitory peptides after second purification. Amino acid sequence analysis of Fraction 3 gh of ACE-inhibitory peptides was shown that the Ala-Tyr-Phe-Tyr, Pro-Tyr-Tyr and Tyr-Leu. IC$_{50}$ calibrated in peptic hydrolysates at 48 h, Fraction 3, Fraction 3 g and Fraction 3 gh from goat's CN hydrolysates by pepsin for 48 h were 29.89, 3.07, 1.85 and 0.87 g/ml, respectively. Based on the results of this experiment, goat's CN hydrolysates by pepsin were shown to have ACE-inhibitory activity.

Anti-melanogenesis Effect of Phenolic Compounds Isolated from Gastrodia elata (천마(Gastrodia elate) 추출물로부터 분리된 페놀성 물질의 멜라닌 생성 억제작용)

  • 김경태;김진국;박선희;이정하;이수희;김기호;박수남
    • Journal of the Society of Cosmetic Scientists of Korea
    • /
    • v.30 no.1
    • /
    • pp.33-38
    • /
    • 2004
  • Melanin pigmentation in human skin is a major defense mechanism against ultraviolet light of the sun, but abnormal pigmentation such as freckles, liver spot could be a serious aesthetic problem. Nearly all studies are mainly concentrated on searching for the materials that have inhibitory activities on tyrosinase. In this work, to isolate phenolic compounds from Gastrodia elata, we purified the extract through solvent fractionation, column chromatography, and recrystallization. They were identified as 4-hydroxybenzyl alcohol 1, bis(4-hydroxyphenyl)methane 2, gastrodin (4-${\beta}$-D-glucopyranosyloxybenzyl alcohol) 3 on the base of spectroscopic evidences. In order to investigate their depigmentation effect, inhibitory activity against mushroom tyrosinase and inhibitory activity of melanin synthesis in B16 melanoma cells were evaluated in vitro. We have found that 4-hydroxybenzyl alcohol 1 and gastrodin (4- ${\beta}$-D-glucopyranosyloxybenzyl alcohol) 3 have no tyrosinase inhibitory activity, but inhibit the melanin synthesis in B16 melanoma cells. Tyrosinase inhibitory activities of bis(4-hydroxyphenyl)methane 2 (IC$\_$50/ = 400 $\mu\textrm{g}$/mL) and butanol fraction (IC$\_$50/ = 46 $\mu\textrm{g}$/mL) were lower/higher than that of arbutin (IC$\_$50/ = 114 $\mu\textrm{g}$/mL), but inhibitory activities of melanin synthesis in B16 melanoma cells were much higher than that of arbutin. Especially, tyrosinase inhibitory activities of isolated phenolic fraction (IC$\_$50/ = 2.37 $\mu\textrm{g}$/mL) from butanol fraction was very higher than that of arbutin (IC$\_$50/ = 114 $\mu\textrm{g}$/mL). Therefore, these results suggest that isolated phenolic compounds from Gastrodia elata have inhibitory activity against mushroom tyrosinase and inhibitory activity of melanin synthesis in 816 melanoma cells in vitro.

Applications of Extracellular Polysaccharide p-m10356

  • Park, Hee-Jung;Kim, Hyong-Ju;Lee, Chang-Moon;Kim, Jin;Lee, Hong-Kum;Yim, Joung-Han;Lee, Ki-Young
    • 한국생물공학회:학술대회논문집
    • /
    • 2005.04a
    • /
    • pp.566-569
    • /
    • 2005
  • The extracellular polysaccharide...(EPS) has been used in a wide variety of industrial applications because of gel formation, emulsion stability, control of the surface tension, water absorption and film formation etc. In this study, inhibitory activity on tyrosinase and inhibitory activity on angiotensin converting enzyme...(ACE) are determined. UV adsorption wavelength, beads formation of EPS were investigated. In the result, in 1%(w/v) EPS concentration, EPS had inhibitory activity of 71.8% on tyrosinase and inhibitory activity of 61.5% on angiotensin converting enzyme in 1.5% EPS concentration. Adsorption wavelength of EPS was UV-B,C . Beads based on EPS were prepared by w/o emulsion method and the shape of EPS beads observed by SEM was spherical and uniform.

  • PDF