• 제목/요약/키워드: product inhibition

검색결과 647건 처리시간 0.025초

Ethnopharmacological Evaluation of Peristrophe bicalyculata Nees. for Anti-inflammatory and Analgesic Activity

  • Rathi, Anshu;Rao, Ch.V.;Khatoon, S.;Mehrotra, S.
    • Natural Product Sciences
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    • 제9권3호
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    • pp.195-199
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    • 2003
  • The ethanolic (50% v/v) extracts of Peristrophe bicalyculata Nees. (Acanthaceae) were examined for anti-inflammatory and analgesic activities in experimental animals. P. bicalyculata in doses of 50, 100 and 200 mg/kg caused a dose dependent inhibition of swelling caused by carrageenin equivalent to 12.25-24.49% protection and 16.62-39.44% in cotton pellet induced granuloma in rats. There was a significant increase in the tail-flick reaction time in mice (18.05-76.43% protection) and analgesy-meter induced pain in rats (14.49-56.85%) protection). The extract of P. bicalyculata resulted in an inhibition of stretching episodes and the protection range of 14.49-56.85% respectively in acetic acid induced writhing.

Lignan Derivatives from Fraxinus rhynchophylla and Inhibitory Activity on Pancreatic Lipase

  • Ahn, Jong-Hoon;Shin, Eun-Jin;Liu, Qing;Kim, Seon-Beom;Choi, Kyeong-Mi;Yoo, Hwan-Soo;Hwang, Bang-Yeon;Lee, Mi-Kyeong
    • Natural Product Sciences
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    • 제18권2호
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    • pp.116-120
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    • 2012
  • Pancreatic lipase digests dietary fats by hydrolysis, which is a key enzyme for lipid absorption. Therefore, reduction of fat absorption by the inhibition of pancreatic lipase is suggested to be a therapeutic strategy for obesity. We previously reported coumarins and secoiridoids of Fraxinus rhynchophylla as inhibitory constituents on adipocyte differentiation. Further investigation on F. rhynchophylla led to the isolation of lignan derivatives such as lignans (1 - 10), sesquilignans (11 - 14) and coumarinolignans (15 - 17). Among them, coumarinolignans and sesquilignans were first reported from Fraxinus species. Among the constituents isolated, sesquilignans showed the significant inhibition on pancreatic lipase, whereas lignans and coumarinolignans exerted weak effects.

Influence of Food Ingredients on the Formation of Heterocyclic Aromatic Amine in Cooked Pork Patties

  • Shin, Han-Seung
    • Food Science and Biotechnology
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    • 제14권5호
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    • pp.572-575
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    • 2005
  • The effects of cooking method, cooking time and various food ingredients on the formation/ inhibition of heterocyclic aromatic amines (HAAs) in pork products were investigated. Three HAAs, 2-amino-3,8-dimethylimidazo [4,5-f] quinoxaline ($MeIQ_x$), 2-amino-3,4,8-trimethylimidazo [4,5-f] quinoxaline ($DiMeIQ_x$) and 2-amino-1-methyl-6-phenylimidazo [4,5-b] pyridine (PhIP) were measured in pork products using solid-phase extraction and HPLC. Pork patties were boiled, oven-broiled and pan-fried to internal temperatures of 71, 77 and $88^{\circ}C$. Generally, HAA concentrations increased with increasing internal temperature, and HAA formation was greatest with pan-fried. Selected food ingredients (vitamin E, sodium nitrite, sodium tripolyphosphate, sodium ascorbate, Nanking cherry tissue and cherry tissue extract) inhibited HAA formation in pork patties fried at $225^{\circ}C$ for 10 min/side, with the greater inhibition provided by cherry tissue and its methanolic extract.

아미노산류가 들깨잎 폴리페놀 옥시다제 활성저해에 미치는 영향 (Effects of Amino Acids on the Inhibition of Polyphenol Oxidase Activity from Perillae Folium)

  • 박수선;김안근;손은수
    • 약학회지
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    • 제40권1호
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    • pp.65-71
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    • 1996
  • Characterization of Polyphenol oxidase (PPO) in Perillae Folium, particullarly inhibitor studies were investigated. This enzyme was stable at pH 5.0 and the residual activity of PPO at ${\geq}$ ph 5.5 was estimated to be very low. PPO activity was decreased slightly by adding amino acid with catechol as a substrate, particullary PPO activity was inhibited markedly by cystein, histidine, lysine and arginine. In the absorption spectra of the product formed when catechol was oxidized by PPO, with a ${\lambda}_{max}$ at 410nm, the peak shifted toward ${\lambda}_{max}$ 520nm by addition of L-proline. At relatively low concentrations($10^{-3}M$), sulfite and dithiothreithol completely inhibited PPO activity. Inhibition of PPO activity by amino acids and inhibitors increased or decreased depending on the pH used to measure it.

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Synthesis of Flavokawain Analogues and their Anti-neoplastic Effects on Drug-resistant Cancer Cells Through Hsp90 Inhibition

  • Seo, Young Ho;Park, Sun You
    • Bulletin of the Korean Chemical Society
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    • 제35권4호
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    • pp.1154-1158
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    • 2014
  • Hsp90 is an ubiquitous molecular chaperone protein, which plays an important role in regulating maturation and stabilization of many oncogenic proteins. Due to its potential to simultaneously disable multiple signaling pathways, Hsp90 represents great promise as a therapeutic target of cancer. In this study, we synthesized flavokawain analogues and evaluated their biological activities against drug-resistant cancer cells. The study indicated that compound 1i impaired the growth of gefitinib-resistant non-small cell lung cancer (H1975), down-regulated the expression of Hsp90 client proteins including EGFR, Her2, Met, Akt and Cdk4, and upregulated the expression of Hsp70. The result strongly suggested that compound 1i inhibited the proliferation of cancer cells through Hsp90 inhibition. Overall, compound 1i could serve as a potential lead compound to overcome the drug resistance in cancer chemotherapy.

Cytotoxic and Antibacterial Activities of Gossypin

  • Chamundeeswari, D.;Sukumar, Ethirajan;Amar, K.;Reddy, N. Brahmananda;Kumar, I. Anil;Chowdry, B.V.;Samatha, K.
    • Natural Product Sciences
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    • 제13권4호
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    • pp.300-303
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    • 2007
  • Gossypin, a naturally occurring polyhydroxy flavonoid, when subjected to in vitro cytotoxic screening against vero cell lines exhibited 68.75% inhibition at a concentration of $1000{\mu}g$. When tested against five bacteria and five fungi, the flavone derivative showed a moderate activity against Staphylococcus aureus and Escherichia coli, mild inhibition against Pseudomonas aerugenosa and Salmonella typhi and no activity against any of the tested fungi, in the concentrations studied.

2가 양이온이 Thiamine Pyrophosphate에 의한 Group I Intron Ribozyme의 Splicing 억제에 미치는 영향 (Effects of Divalent Cations on the Self-splicing Inhibition of Group I Intron by the Coen-zyme Thiamine Pyrophosphate)

  • 안성준;박인국
    • 미생물학회지
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    • 제38권1호
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    • pp.13-18
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    • 2002
  • 2가 양이온($Mg^{2+}$, $Mn^{2+}$, $Zn^{2+}$)이 조효소 thiamine pyrophosphate에 의한 T4파지 티민생합성 유전자 (td) 인트론 RNA의 splicing에 미치는 영향을 조사하였다. $Mg^{2+}$를 30 mM까지 증가시켰을 때 splicing 활성은 농도에 비례하여 증가하였다. 그러나 $Mg^{2+}$이 존재하지 않는 상태에서 0.1-4 mM 농도에 걸쳐 $Zn^{2+}$를 사용한 결과 약 20% 정도의 splicing이 일어났다. 이때 대부분의 splicing product는 인트론-엑손2 및 엑손2였고 엑손1-엑손2는 검출되지 않았다. 그리고 4 mM 농도에서는 RNA가 대부분 가수분해되는 현상이 나타났다. $Mn^{2+}$ 이온은 사용한 농도 범위 (0.1-8 mM)에서 $Zn^{2+}$ 보다는 전반적으로 약간 증가된 splicing 활성을 보였으며 8 mM 농도에서도 약 30% 정도의 splicing 활성을 보였다. $Zn^{2+}$ 이온처럼 splicing product는 인트론-엑손2 및 엑손2였고 엑손1-엑손2는 검출되지 않았 다. 반면에 splicing반응에 10 mM $Mg^{2+}$ 를 첨가했을 때 $Zn^{2+}$$Mn^{2+}$ 이온은 평균 약 35-40% 정도 splicing활성을 촉진시키는 것으로 나타났다. 실험한 2가 양이온 중에서 특히 $Mg^{2+}$ 은 가장 낮은 농도에서 thiamine pyrophosphate 에 의한 억제반응을 극복하는 최고의 활성효과를 나타냈다. 이와 같은 억제 회복 효과는 $Mg^{2+}$에 의한 리보자임의 td intron 구조적 안정성에 기인하는 것으로 추정된다.

Hypolipidemic effect of Salicornia herbacea in animal model of type 2 diabetes mellitus

  • Hwang, Ji-Yeon;Lee, Soo-Kyung;Jo, Ja-Rim;Kim, Mi-Eun;So, Hyun-Ah;Cho, Chang-Woo;Seo, Young-Wan;Kim, Jung-In
    • Nutrition Research and Practice
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    • 제1권4호
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    • pp.371-375
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    • 2007
  • To control blood glucose level as close to normal is a major goal of treatment of diabetes mellitus. Hyperglycemia and hyperlipidemia are the major risk factors for cardiovascular complications, the major cause of immature death among the patients with type 2 diabetes. The purpose of this study is to determine the hypoglycemic and hypolipidemic effects of Salicornia herbacea in animal model of type 2 diabetes and to investigate the possible mechanisms for the beneficial effects of S. herbacea. S. herbacea was extracted with 70% ethanol and desalted with 100% ethanol. Three week-old db/db mice (C57BL/KsJ, n=16) were fed AIN-93G semipurified diet or diet containing 1% desalted ethanol extract of S. herbacea for 6 weeks after 1 week of adaptation. Fasting plasma glucose, triglyceride, and total cholesterol were measured by enzymatic methods and blood glycated hemoglobin ($HbA_{1C}$) by the chromatographic method. Body weight and food intake of S. herbacea group were not significantly different from those of the control group. Fasting plasma glucose and blood glycated hemoglobin levels tended to be lowered by S. herbacea treatment. Consumption of S. herbacea extract significantly decreased plasma triglyceride and cholesterol levels (p<0.05). The inhibition of S. herbacea extract against yeast ${\alpha}$-glucosidase was 31.9% of that of acarbose at the concentration of 0.5 mg/mL in vitro. The inhibitory activity of ethanol extract of S. herbacea against porcine pancreatic lipase was 59.0% of that of orlistat at the concentration of 0.25 mg/mL in vitro. Thus, these results suggest that S. herbacea could be effective in controlling hyperlipidemia by inhibition of pancreatic lipase in animal model of type 2 diabetes.

밤나무잎의 항주름 효과 (Anti-wrinkle Effect of Chestnut Leaf)

  • 장민정;전동하;김세현;한상익;이진태
    • 생명과학회지
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    • 제23권6호
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    • pp.751-756
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    • 2013
  • 본 연구는 노령목의 산림의 경제적 가치를 증진하고자 밤나무 잎에 함유된 물질의 기능성화장품 원료로의 기능을 규명하여 화장품 산업에 적용하기 위하여 천연소재로써의 이용 가능성을 살펴보았다. 항산화능 측정을 위한 실험으로 DPPH radical 소거능과 ABTS cation radical 소거능을 실시하였으며, 양성 대조군으로는 항산화 작용이 있는 것으로 알려진 BHA를 이용하여 밤잎 추출물의 항산화 효과를 비교하였다. 그 결과 아세톤 추출물의 경우 시료 농도에 따라 DPPH radical 및 ABTS radical 소거 증가 정도가 컸으며, 열수 추출물은 10 ug/ml의 농도에서 50% 이상의 소거활성을 나타내었다. 이러한 결과로 미루어 볼 때 밤잎 추출물은 항산화 작용이 높고 피부에서 흔히 일어나는 활성산소에 대한 노화 방지에 도움이 될 것으로 사료된다. 주름개선 효과 측정으로 elastase 저해활성을 측정한 결과 아세톤과 열수 추출물에서는 그 효과가 없었으나 에탄올 추출물 100 ug/ml에서 64.6%의 우수한 elastase 저해활성을 나타내었으며, collagenase 저해활성을 측정한 결과 3가지 추출물은 100 ug/ml에서 열수 추출물 18.0%, 아세톤 추출물 14.3%, 에탄올 추출물 5.3%의 순으로 collagenase 저해활성능을 나타내었으며, 다른 천연물질을 이용한 연구결과와 비교 시 밤잎 추출물은 주름개선에 우수함을 확인 할 수 있었다. 주름개선 원료로의 이용가치가 있을 것으로 보인다. 이상의 연구 결과로 보아 밤잎은 항산화 및 항노화 효소 활성을 갖는 천연소재로서 주름개선 소재로 활용 될 수 있을 것으로 사료되며, 임삼 효능 평가 등의 계속적인 연구를 통해 기능성 화장품 소재로 개발된 가능성이 매우 높다고 사료된다.

Biotransformation of benzyle trans-2-phenylcyclopropanecarbamate to tranylcypromine in rats

  • Il, Kang-Gun;Chung, Soon-Young
    • Archives of Pharmacal Research
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    • 제7권2호
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    • pp.141-143
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    • 1984
  • A metabolic study was performed in order to characterize the in vivo MAO-inhibitory activity of benzyl trans-2-phenylcylopropanecarbamate which was reported to be twice as potent as the tranylcypromine. In the rat urine which was obtained after the administration of the benzyl trans-2-pheny-lcyclopropanecarbamate (40mg/kg) through oral route, a metabolic product, tranylcypromine as well as the intact drug was detected by GC/MS.

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