• Title/Summary/Keyword: inhibiting activity

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알데히드 옥시다제의 활성에 미치는 리도카인 및 프로카인아미드의 영향 (The Effect of Lidocaine and Procainamide on the Hepatic Aldehyde Oxidase Activity)

  • 허근;김진숙;김대경;하은필;이상일;용철순
    • 약학회지
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    • 제43권6호
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    • pp.756-761
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    • 1999
  • Lipid peroxidation mediated by hydroxyl radicals which are generated during myocardial ischermia has suggested as a possible mechanism of ischemic myocardial damage. Recently, it has been reported that anti-arrhythmic action of lidocaine, a local anesthetic, is attributed to its "membrane-stabilizing" properties through scavenging free radicals, thus, inhibiting lipid peroxidation. Aldehyde oxidase and xanthine oxidase which catalyze the oxidation of many purine, pyrimidine and pteridine derivatives are known as free radical generating systems. In this experiment, we studied the effect of lidocaine and procainamide on the hepatic aldehyde and xanthine oxidase activity and antioxidative activities. It was found that lidocaine and procainamide inhibited both NADPH-dependent and independent lipid peroxidation. Both of tested compounds were found to be ineffective in inhibiting xanthine oxidase. Lidocaine and procainamide, however, inhibited aldehyde oxidase activity in vitro as well as in vivo. Based on the above results, lidocaine and procainamide could be employed as a therapeutic agent for aldehyde oxidaserelated disease.d disease.

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국내자생식물 메탄올추출물의 Wnt/β-catenin 신호전달체계에 대한 효과 (Effect on Wnt/β-catenin Pathway of Methanol Extracts from Native Plants in Korea)

  • 김보라;김현수
    • 한국자원식물학회지
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    • 제29권5호
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    • pp.620-624
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    • 2016
  • 본 연구에서 국내 자생식물 추출물중 비만관련 특허가 없는 식물원료를 대상으로 지방세포의 분화억제 효과를 Wnt/β-catenin 신호전달계 활성측정방법으로 탐색하여 비만치료를 위한 기능성소재 응용가능성을 검토하였다. HEK 293-TOP세포의 luciferase 리포터 상대적인 활성은 무 처리 대조군에 비하여 지유(전초), 측백나무(줄기)가 각각 152%, 130%로 높은 활성을 나타내었으며, 피마자(전초)는 약 90%대의 활성을, 해당화(줄기), 괴화(전초)의 경우는 약 80%, 초피나무(줄기), 칡(줄기), 까마중(전초)은 약 70%대의 높은 활성을 나타내었다. 또한, 신경줄기 세포에 대한 어떠한 독성도 보이지 않음으로써 안전한 물질인 것으로 사료되었다. 이 결과는 Wnt/β-catenin 신호전달 활성 측정방법이 향후 High throughput screening 기반기술로 활용될 수 있을 것으로 판단되며, 지방세포 분화 억제활성 후보로 선별된 식물추출물들에 대한 추가적인 실험을 통하여 항비만 소재 개발 응용 가능성을 타진할 것이다.

비타민나무(Seabuckthorn, Hippophae rhamnoides L.) 부위별 추출물의 생리활성 비교 (Comparison of Biological Activities of Extracts from Different Parts of Seabuckthorn (Hippophae rhamnoides L.))

  • 박유화;임상현;함헌주;정햇님;이광재;김경희;김성문
    • 한국식품영양과학회지
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    • 제39권7호
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    • pp.975-979
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    • 2010
  • 국내에서 재배된 비타민나무(Hippophae rhamnoides L.)의 생리활성을 부위별(줄기, 잎, 뿌리, 열매), 용매별(물, 에탄올)로 시험한 결과는 다음과 같다. $\alpha$-Glucosidase 활성 억제 실험에서, 비타민나무의 저해활성은 줄기의 에탄올 추출물이 93%로 가장 높았고, 다음이 잎의 에탄올 추출물이 88.7% 순으로서 대조구 acarbose의 20.2%보다 훨씬 높았다. Pancreatin 기원의 $\alpha$-amylase 억제 활성 측정 실험에서는 잎의 물 추출물이 54.7%로 다른 추출물에 비해 가장 높았다. HT-29 cell과 DU-145 cell의 암세포에 대한 항암효과 시험 결과 뿌리의 물 추출물에서 각각 47.1%, 32.3%의 항암효과가 나타났다. 또한 항균활성 실험 결과 잎의 에탄올 추출물에서 위해균주인 Clostridium butyricum, Proteus mirabilis, Shigella flexneri에 대한 저해활성이 나타났다. 향후 연구에서는 생리활성 효과가 나타난 물질에 대한 분리, 정제 등의 연구가 계속 수행되어져야할 것으로 생각된다.

평간개울지혈탕(平肝開鬱止血湯)의 항염증, 항산화 및 항노화에 미치는 영향 (Effects of Pyeonggangaeuljihyeol-tang(PGJT) Extract on Anti-inflammatory, Antioxidant and Anti-aging)

  • 이경원;송영채;김희택
    • 한방안이비인후피부과학회지
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    • 제37권1호
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    • pp.29-41
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    • 2024
  • Objectives : The purpose of this study is to confirm the anti-inflammatory, antioxidant and anti-aging efficacy of Pyeonggangaeuljihyeol-tang(PGJT) extract. Methods : In order to confirm the anti-inflammatory activity of PGJT extract, the inhibitory effect on NO PGE2 production were evaluated and the expression level of iNOS, COX-2 and IL-6 mRNA were measured through qRT-PCR, Antioxidant activity was evaluated for radical scavenging activity using DPPH and ABTS, anti-aging activity was evaulated for collagenase, elastase, tyrosinase and L-DOPA oxidation inhibitory activity. Results : PGJT extract shows anti-inflammatory effect by inhibiting the production of NO and PGE2 by reducing the expression level of iNOS, COX-2 and IL-6 mRNA, antioxidant effect by increasing DPPH and ABTS scavenging abillity in a concentration dependent manner. In addition, the anti-aging effect was confirmed by inhibiting collagenase, elastase, tyrosinase production and L-DOPA oxidation. Conclusion : This suggests that PGJT showed an overall excellent anti-inflammatory effect and an inhibitory effect on the activity of antioxidant and anti-aging related enzymes.

사과 과실로부터 분리한 polygalacturonase-inhibiting protein(PGIP)의 생화학적 특성 (Characterization of an Apple Polygalacturonase-inhibiting Protein (PGIP) from Apple Fruits)

  • 이동훈;강상구;강인규;이윤경;최철;변재균
    • 생명과학회지
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    • 제16권4호
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    • pp.653-658
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    • 2006
  • 사과 겹무늬썩음병균이(Botryosphaeria dothidea) 생성하는 세포벽 분해효소인 endopolygalaturonase를 억제하는 polygalacturonase-inhibiting protein (PGIP)를 사과 과실로부터 분리하였다. 분리되어진 사과 PGIP는 사과 겹무늬썩음병균이 생성하는 PG에 대하여 혼합형의 저해를 나타내었다. PGIP의 반응 최적온도는 $40^{\circ}C$이며 최적 pH는 5.0이었다. 이 효소는 $60^{\circ}C$까지는 비교적 안정하였으나 $70^{\circ}C$에서는 효소의 활성이 완전히 억제되었으며 pH 4.0에서 8.0까지는 안정하였다. PGIP는 $K^+$, $Cu^{2+}$, $Mg^{2+}$, $Ca^{2+}$$Zn^{2+}$ 등의 금속이온과 SDS 그리고 CDTA에 의해 효소의 활성이 저해되었다.

The Effect of Chinese Herbs on Acne Pathogens

  • Tseng, Wen-Kai;Lin, Shiann-Tsai;Chen, Yi-Shyan;Kwan, Chang-Chin
    • 대한화장품학회:학술대회논문집
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    • 대한화장품학회 2003년도 IFSCC Conference Proceeding Book II
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    • pp.1-11
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    • 2003
  • Chinese herbs have been used for a long period of time and less side effects than synthesized chemical drugs. Therefore, using Chinese herbs as natural additives in cosmetics becomes popular in recent years. The methanol extracts of Scutellariae Radix, Lithospermi Radix, Lonicerae Flos, Andrographitis. Herba, Angelicae Dahuricae Radix, Ligustici Rhizoma et Radix, Hedyotis Diffusae Herba, Isatidis Folium, Magnoliae Liliflorae Flos, Forsythiae Fructus, Anmarrhenae Rhizoma, Spirodelae Herba, Gardeniae Fructus, Sophorae Flavescentis Radix, Coptidis Rhizoma, Prunellae Spica, Equiseti Hiemalis Herba, Gentianae Radix, Moutan Radicis Cortex, Fraxini Cortex, Lycii Radicis Cortex, Violae Herba, Lophatheri Herba, Matricariae chamomillae Flos, Taraxaci Herba and Scutellariae Barbatae Herba are used to test the efficiency of inhibiting acne pathogens. Twenty-six Chinese herbs are extracted by methanol, and then condensed to dried powder. These extracts are divided into water-soluble part and DMSO soluble part. These two type solutions are tested for the effect on acne pathogens by paper disc diffusion method. The results show that the substances of water soluble part which are Coptidis Rhizoma, Moutan Radicis Cortex, Scutellariae Barbatae Herba have medium to high activity of inhibiting acne pathogents, and the substances of DMSO soluble part which are Coptidis Rhizoma, Ligustici Rhizoma et Radix, Sophorae Flavescentis Radix, Moutan Radicis Cortex, Scutellariae Radix, Scutellariae Barbatae Herba also have medium to high activity of inhibiting acne pathogens. Using Chinese herbs as natural additives in cosmetics is convenience and valuable application in cosmetceutical research and development. Therefore, it is worth that re-investigation and find out the potential of Chinese herbs being use in cosmetics.

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Anti-neuroinflammatory Effects of 12-Dehydrogingerdione in LPS-Activated Microglia through Inhibiting Akt/IKK/NF-κB Pathway and Activating Nrf-2/HO-1 Pathway

  • Zhao, Dong;Gu, Ming-Yao;Xu, Jiu Liang;Zhang, Li Jun;Ryu, Shi Yong;Yang, Hyun Ok
    • Biomolecules & Therapeutics
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    • 제27권1호
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    • pp.92-100
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    • 2019
  • Ginger, one of worldwide consumed dietary spice, is not only famous as food supplements, but also believed to exert a variety of remarkable pharmacological activity as herbal remedies. In this study, a ginger constituent, 12-dehydrogingerdione (DHGD) was proven that has comparable anti-inflammatory activity with positive control 6-shogaol in inhibiting LPS-induced interleukin (IL)-6, tumor necrosis factor $(TNF)-{\alpha}$, prostaglandin (PG) $E_2$, nitric oxide (NO), inducible NO synthase (iNOS) and cyclooxygenase (COX)-2, without interfering with COX-1 in cultured microglial cells. Subsequent mechanistic studies indicate that 12-DHGD may inhibit neuro-inflammation through suppressing the LPS-activated $Akt/IKK/NF-{\kappa}B$ pathway. Furthermore, 12-DHGD markedly promoted the activation of NF-E2-related factor (Nrf)-2 and heme oxygenase (HO)-1, and we demonstrated that the involvement of HO-1 on the production of pro-inflammatory mediators such as NO and $TNF-{\alpha}$ by using a HO-1 inhibitor, Zinc protoporphyrin (Znpp). These results indicate that 12-DHGD may protect against neuro-inflammation by inhibiting $Akt/IKK/I{\kappa}B/NF-{\kappa}B$ pathway and promoting Nrf-2/HO-1 pathway.

Isolation and Biological Activities of an Alkaloid Compound (3-methylcanthin-5, 6-dione) from Picrasma quassiodes (D. Don) Benn.

  • Yin, Yu;Lee, Seok-Ki;Wang, Myeong-Hyeon
    • Natural Product Sciences
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    • 제17권1호
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    • pp.5-9
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    • 2011
  • An alkaloid, 3-methylcanthin-5, 6-dione, was isolated from the stem of Picrasma quassioides (D. Don) Benn. and characterized by comprehensive analyses of its 1D and 2D NMR spectra. It was also evaluated for its cytotoxic activity in vitro against three human cancer cell lines (MDA-MB-231, HT-29 and NCI-N87), using MTT assays. We found that 3-methylcanthin-5, 6-dione exhibited significant anti-inflammatory activity via inhibiting NO production induced in LPS-stimulated murine macrophage RAW264.7 cells. The antioxidant activity of 3-methylcanthin-5, 6-dione was measured by DPPH free radical scavenging assays, hydroxyl radical scavenging assays and reducing power assays. Our results showed that 3-methylcanthin-5, 6-dione has significant biological activities.

생쥐에서 사간 추출물의 기억력 감퇴에 대한 개선 효과 (Belamcandae Rhizoma Extract Improves Memory Impairment in Mice)

  • 정지욱
    • 생약학회지
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    • 제52권1호
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    • pp.55-60
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    • 2021
  • Belamcandae Rhizoma (BR), the rhizome of Belamcanda chinensis (L.) DC., possesses various biological properties such as anti-inflammatory activity, antioxidant activity and antimutagenic activity. However, there have been no studies on the anti-amnesic effect of BR. In this study, we assessed the improvement effect of BR extract on scopolamine-induced amnesia in mice. ICR mice were administrated with BR (50, 100 or 200 mg/kg, p.o.) and were subsequently injected of scopolamine (1 mg/kg, i.p.) 30 min before behavioral tasks (Y-maze, passive avoidance and Morris water maze tasks). To further assess the possible mechanisms of BR, the ex vivo acetylcholinesterase (AChE) activity was also evaluated. BR could ameliorate scopolamine-induced memory impairment and could regulate the cholinergic function by inhibiting the AChE activity. These data demonstrated that BR exert candidate extract against amnesia by restoring the cholinergic activity.

대두와 약콩의 Acetylcholinesterase 활성 억제효과와 항산화 효과 (Acetycholinesterase Inhibiting Effect and Free Radical Scavenging Effect of Soybean(Glycine max) and Yak-Kong(Rhynchosia nolubilis))

  • 강순아;한진아
    • 동아시아식생활학회지
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    • 제14권1호
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    • pp.64-69
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    • 2004
  • 본 연구에서는 이미 항산화 효과로 알려져 있는 대두와 약성이 탁월한 약콩에서 AChE 활성 억제효과와 Free radical scavenger 효과를 노화로 인한 질병 예방효과에 대한 기초자료를 제공하고자 수행하였다. 1. 대두 열탕 추출물의 경우 저농도인 1, 0.1 mg/$m\ell$에서는AChE의 활성 억제 효과가 메탄을 추출물보다 높았다. (P<0.001) 2. 대두, 약콩 메탄올 추출물에서는 고농도인 5 mg/$m\ell$에서 각 시료의 효과가 62.0$\pm$2.43%, 65.0$\pm$3.29%로 비슷했으나 저농도인 0.1 mg/$m\ell$에서는 약콩의 경우 25.5$\pm$0.94%로 약콩이 대두에 비해 유의적인 AChE 억제효과를 나타냈다. (p<0.001) 3. 시간에 따른 Free radical scavenger효과는 비타민 C의 경우 시간에 따라 비슷한 효과를 보였으나 대두와 약콩은 incubating 시간에 따라 free radical 억제효과가 증가해 높은 항산화 효과를 볼 수 있었다. 4. 대두, 약콩 메탄올 추출물에서는 약콩이 고농도인 5mg/$m\ell$에서 약4배 정도의 효과를 보였으며 Free radical scavenger의 50%효과를 나타내는 $IC_{50}$/에서는 약 10배 정도로 높은 Free radical scavenger 효과를 나타내 약콩이 대두에 비해 유의적으로 높은 효과를 나타내었다. 결론적으로, 대두와 약콩의 추출물은 AChE 활성억제효과에 있어서 좋은 효과를 나타내며 또한 노화의 원인과 질병의 원인이 되는 free radical을 억제하는 효과를 가지고 있어 노인성 치매를 비롯하여 파킨슨씨병, 뇌허혈 및 뇌졸중과 같은 각종 노인성 질환예방에 도움이 될 것으로 보인다.

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