• Title/Summary/Keyword: enzyme inhibitory activity

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Screening of Inhibitory Activity of Medicinal Plants against Heparinase (수종 생약의 Heparinase 저해활성 검색)

  • Ahn, Soon-Cheol;Kim, Bo-Yeon;Oh, Won-Keun;Lee, Myung-Sun;Bae, Eun-Young;Kang, Dae-Wook;Ahn, Jong-Seog
    • Korean Journal of Pharmacognosy
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    • v.33 no.2 s.129
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    • pp.144-150
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    • 2002
  • The methanol extracts of 132 herbal medicines were screened for the inhibitory activity against heparinase enzyme from Flavobacterium heparinum. Eleven medicinal plants, Amomum xanthiodides, Agrimonia pilosa, Paeonia lactiflora, Rubia cordifolia, Sanguisorba officinalis, Torrega grandis, Morus alba, Gleditsia sinensis, Crataegus pinnatifida, Cornus officinalis, Paeonia japonica showed potent inhibition on heparinase activity. The active substituents of those herbal medicine could be extracted into butanol fraction and the inhibitory compounds of Morus alba are now isolating.

Anti-HIV and Antihepatotoxic Constituents from Medicinal Plant Resources

  • Park, Jong-Cheol;Park, Ju-Gwon;Hur, Jong-Moon;Hwang, Young-Hee;Jung, Deuk-Young
    • Plant Resources
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    • v.4 no.3
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    • pp.196-199
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    • 2001
  • Medicinal plants were screened for the inhibitory effects on human immunodeficiency virus type 1 pretense. Of the extracts tested, the strong inhibitory effects were observed in the acetone extracts of the pericarp of Camellia japonica. Camelliatannin H from the pericarp of C. japonica showed a potent inhibitory activity on HIV-1 pretense. Effects of the extract and compound from leaves of Zanthoxylum piperitum on the enzyme activities were investigated in the liver of bromobenzene-treated rats. The methanol extract and protocatechuic acid isolated from Z. pipetitum reduced the activity of aniline hydroxylase that increased by bromobenzene, while did not affect the activities of aminopyrin N-demethylase and glutathione S-transferase. The extract and protocatechuic acid recovered significantly the activity of epoxide hydrolase decreased by bromobenzene.

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Anti-HIV and Antihepatotoxic Constituents from Medicinal Plant Resources

  • Park, Jong-Cheol;Park, Ju-Gwon;Hur, Jong-Moon;Hwang, Young-Hee;Jung, Deuk-Young
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2001.11a
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    • pp.68-73
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    • 2001
  • Medicinal plants were screened for the inhibitory effects on human immunodeficiency virus type 1 pretense Of the extracts tested, the strong inhibitory effects were observed in the acetone extracts of the pericarp of Camellia japonica. Camelliatannin H from the pericarp of C. japonica showed a potent inhibitory activity on HIV- 1 pretense. Effects of the extract and compound from leaves of Zanthoxylum piperitum on the enzyme activities were investigated in the liver of bromobenzene-treated rats. The methanol extract and protocatechuic acid isolated from Z. piperitum reduced the activity of aniline hydroxylase that increased by bromobenzene, while did not affect the activities of aminopyrin N-demethylase and glutathione S-transferase The extract and protocatechuic acid recovered significantly the activity of epoxide hydrolase decreased by bromobenzene.

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Effect of Vitamin A and $B_2$ Derivatives on Aminopyrine Demethylase Activity (비타민 A 및 $B_2$ 유도체의 Aminopyrine Demethylase 활성도에 대한 영향)

  • 이향우
    • YAKHAK HOEJI
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    • v.28 no.1
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    • pp.53-59
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    • 1984
  • Drug-metabolizing system which has the important role in drug metabolism is localized in smooth endoplasmic reticulum of hepatocytes and is composed of NADPH, NADPH-cytochrome $P_{450}$ reductase, cytochrome $P_{450}$ and others. It is well known that the enzyme system is induced by phenobarbital and methylcholanthrene. Lipid peroxidation is reaction of oxidative deterioration of polyunsaturated lipids. Formation of lipid peroxides in liver microsome has been found to produce degradation of phospholipid, which are major components of microsomal membrane. The relationship between the formation of lipid oxides and the activities of drug-metabolizing enzyme in the liver of rats was reported by several investigators. In this study the effect of riboflavin tetrabutylate, an antioxidant on lipid peroxidation, specially the relationship between lipid peroxidation and drug-metabolizing enzyme system was investigated. In addition the effect of vitamin A derivatives, such as retinoic acid and retinoid on the enzyme was also observed. Results are summarized as followings. 1) The pretretment with riboflavin tetrabutylate inhibited completely the lengthened sleeping time due to $CCl_{4}$ treatment. 2) The increase of TBA value was prevented by the pretreatment with riboflavin tetrabutylate. 3) The pretreatment with riboflavin tetrabutylate also prevented the decrease of drug-metabolizing enzyme caused by $CCl_{4}$. 4) Both retinoic acid and retinoid remarkably decreased the activity of aminopyrine demethylase. Pretreatment of riboflavin tetrabutylate, however, prevented inhibitory effect of retinoic acid on the enzyme activity.

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Studies on the Epitope of Neuronal Growth Inhibitory Factor (GIF) with Using of the Specific Antibody

  • Pang, Li-Yan;Ru, Bing-Gen
    • BMB Reports
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    • v.38 no.6
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    • pp.646-649
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    • 2005
  • Human neuronal growth inhibitory factor (GIF), a metalloprotein classified as metallothionein-3, is specifically expressed in mammal central nervous system (CNS). In these Studies the specific antibody to human GIF was prepared and used to search the epitope of human GIF by enzyme-linked immunosorbent assay (ELISA) and sequence comparison. The result of ELISA showed the epitope of human GIF may locate on a octapeptide (EAAEAEAE) in the $\alpha$-domain of human GIF, and the result of nerve cell culture indicated that the biological activity of GIF may be affected by the specific antibody.

Screening of Chinese Herbal Medicines with Inhibitory Effect on Aldose Reductase (X) (중국 약용식물 추출물의 알도즈 환원 효소 억제 효능 검색(X))

  • Choi, So-Jin;Kim, Young Sook;Kim, Joo Hwan;Kim, Jin Sook
    • Korean Journal of Pharmacognosy
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    • v.45 no.4
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    • pp.359-365
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    • 2014
  • Aldose reductase (AR) is the key enzyme of the polyol pathway in the development of the diabetic complications. Sixty seven Chinese herbal medicines have been investigated for inhibitory activities on AR. Among them, 7 herbal medicines, Buddleja crispa (twigs and leaves), Taiwania flousiana (twigs and leaves), Sloanea hemsleyana (fruits), Euphorbia nemetocypha (whole plants), Photinia glomerata (twigs and leaves), Vitex yunnanensis (twigs and leaves) exhibited a significant inhibitory activity against AR. Particularly, S. hemsleyana and V. yunnanensis showed 1.2-4.5 times more potent inhibitory activity than the positive control, 3,3-tetramethyleneglutaric acid (TMG).

Antioxidant and Anticholinesterase Potential of Two Nigerian Bitter Yams Using a Simulated Gastrointestinal Digestion Model and Conventional Extraction

  • Salawu, Sule Ola;Ajiboye, Praise Blessing;Akindahunsi, Akintunde Afolabi;Boligon, Aline Augusti
    • Preventive Nutrition and Food Science
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    • v.22 no.2
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    • pp.107-117
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    • 2017
  • The purpose of this study was to evaluate the antioxidant and anticholinesterase activities of yellow and white bitter yams from South Western Nigeria using methanolic extraction and simulated gastrointestinal digestion models. The phenolic compounds in the bitter yam varieties were evaluated by high performance liquid chromatography with a diode array detector (HPLC-DAD). The total phenolic content of the bitter yams was measured by the Folin-Ciocalteu method, reductive potential by assessing the ability of the bitter yam to reduce $FeCl_3$ solution, and the antioxidant activities were determined by the 2,2-diphenyl-1-picrylhydrazyl radical ($DPPH^{\cdot}$) scavenging activity, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical cation ($ABTS^{{\cdot}+}$) scavenging activity, nitric oxide radical ($NO^{\cdot}$) scavenging ability, hydroxyl radical scavenging ability, and ability to inhibit $Fe^{2+}$-induced lipid oxidation. The HPLC-DAD analysis revealed the presence of some phenolic compounds in the studied bitter yam varieties, with varying degree of quantitative changes after cooking. The antioxidant indices (total phenolic content, total flavonoid content, reducing power, $DPPH^{\cdot}$ scavenging activity, $ABTS^{{\cdot}+}$ scavenging activity, and $NO^{\cdot}$ scavenging activity) were higher in the simulated gastrointestinal digestion model compared to the methanolic extract, with the in vitro digested cooked white bitter yam ranking higher. Similarly, the in vitro digested yams had a higher inhibitory action against lipid oxidation compared to the methanolic extracts, with the cooked white bitter yam ranking high. The methanolic extracts and in vitro enzyme digests showed no acetylcholinesterase inhibitory abilities, while methanolic extracts and the in vitro enzyme digest displayed some level of butyrylcholinesterase inhibitory activities. Therefore the studied bitter yams could be considered as possible health supplements.

In vitro inhibitory activities of urea analogues on bacterial urease

  • Chang, Pan-Sup;Shu, Byung-Se;Nancy A.Strockbine;Kunin, Galvin M
    • Archives of Pharmacal Research
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    • v.9 no.3
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    • pp.163-167
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    • 1986
  • Twenty six urea analogues, most of which have already been approved for human use, were tested for their antiurease activity in vitro. Cell-free extracts obtained from a clinical isolate of Proteus mirabilis was used as the source of enzyme. Acetohydroxamic acid which is a proven potent urease inhibitor but not approved for human use was again shown to be the most active compound among the tested. Phenacemide, cycloserine, and deferoxamine were demonstrated to be moderate inhibitors. Oxtetracycline, trimethoprim, and cefamandole revealed a demonstrable antiruease activity, but only at very high concentrations. The antiurease activity of cycloserine, trimethoprim, and cefamandole was pH dependent-only active at acidic pH. The inhibitory activity of acetohydroxamic acid however was independent of change in pH. The inhibitory activity of acetohydroxamic acid however was independent of change in pH. Hydrogen ion concentration plays an important role in urease activity and acidification (pH 5. 5) alone eliminates approximately 65% of the enzymic activity. Adjustment of pH therefore appears to be an important adjunct in reducing unrease activity and should always be studied to maximize the effcacy of antiurease compounds under investigation.

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Antioxidant and Angiotensin Converting Enzyme I Inhibitory Activity on Different Parts of Germinated Rough Rice (발아 벼 부위별 추출물의 항산화활성과 Angiotensin Converting Enzyme I 저해활성)

  • Kim, Hyun-Young;Hwang, In-Guk;Kim, Tae-Myoung;Park, Dong-Sik;Kim, Jae-Hyun;Kim, Dae-Joong;Lee, Jun-Soo;Jeong, Heon-Sang
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.40 no.6
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    • pp.775-780
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    • 2011
  • We investigated the changes in antioxidant and angiotensin converting enzyme I (ACE) inhibitory activity in different parts of 'Ilpum' (Oryza sativa L.) rough rice before and after germination. Rough rice, either before or after germination, were separated into hull, brown rice, or sprout, and then extracted with distilled water and 70% ethanol. After germination, the total polyphenol contents of the distilled water extract of the brown rice was higher than before germination (5.84 and 1.67 mg/g, respectively). The DPPH radical scavenging activity on the unseparated rough rice ethanol extract increased from 22.95% before germination to 31.32% after germination, but it decreased in both the hull and brown rice extracts. The ABTS radical scavenging activity was highest in the sprout extract with a value of 4.41 mg AA eq/g. The reducing power of the brown rice ethanol extract increased from 0.32 before germination to 0.45 after germination. The ACE inhibitory activity of the in hull ethanol extract increased after germination. These results indicate that antioxidant capacity increases in the hull and sprout after germination could be considered having significant health benefits.

Factors that Influence the Activity of A Candida Lipase (Candida속(屬) Lipase의 활성(活性)에 영향(影響)을 미치는 제인자(諸因子)에 관한 연구(硏究))

  • Kim, S.Y.;Park, Y.J.;Lee, C.Y.
    • Applied Biological Chemistry
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    • v.14 no.3
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    • pp.207-212
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    • 1971
  • An enzyme preparation from a newly isolated Candida that showed a high lipase activity was subjected to examination of its reaction rate under various conditions. The original and a diluted enzyme solutions showed the zero order curve starting at the point of 50 minutes in time. When PVA was used as an emulsifyer more activity was observed than the case of gum arabic. The optimal temperature and pH were $37{\sim}40^{\circ}C$ and 7.0, respectively. Oleic acid as a fatty acid conferred on the enzyme an inhibitory action while calcium ion a positive one. Sodium cholate yielded an increase in reaction rate at the first stage.

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