• Title/Summary/Keyword: inhibitory compounds

검색결과 1,634건 처리시간 0.026초

Isoquinolines: Are they possible candidate for $Ca^{2+}$ blockers\ulcorner

  • 장기철;윤용진;조수동;정원석
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1994년도 춘계학술대회 and 제3회 신약개발 연구발표회
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    • pp.217-217
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    • 1994
  • Calcium entry blockers, capable of inhibiting transmembrane influx of extracellular calcium through specific calcium channels, are useful drugs in the treatment of angina pectoris, hypertension, cardiac arrythmia, and various cardiovascular disorders. Compounds having isoquinoline structures have recently been reported to possess calcium antagonistic action. Therefore, in the present study, we have attempted to synthesize some isoquinoline and related compound.; in order to search for potentially effective chemicals acting on cardiovascular system, and evaluated their pharmacological properties focusing on calcium antagonistic actions. Almost all of the compounds so far synthesized, had inhibitory action against phenylephrine or high potassium-induced contraction in vascular smooth muscle with different degrees of potencies depending on their structures, However, some of tetrahydroisoquinoline analogs showed directly inhibit calcium current in isolated rabbit cardiac myocytes examined by patch clamp techniques. The pharmacological properties of these compounds need more intensive investigation as to whether these chemicals may have developed as a new cardiovascular active drugs. Therefore, we are now under investigation of the mechanism of action of these compounds.

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수종식물의 분비물질이 종자 발아와 균류 생장에 미치는 알레로파시 효과 (Allelopathic Effects on Seed Germination and Fungus Growth from the Secreting Substances of Some Plants)

  • 이호준;김용옥;장남기
    • The Korean Journal of Ecology
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    • 제20권3호
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    • pp.181-189
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    • 1997
  • Phenolic compounds from 7 species of naturalized invader species and Korean wild plants were analyzed by high performance liquid chromatography. Eleven phenolic compounds including benzoic acid were identified. The extract of naturalized plants was significantly more inhibitory to seed germination and seedling growth of the both naturalized and Korean wild plants. The content of total phenolic compounds in each extract were 43.5 mg/l in Ailanthus altissima as the maximum amount and 25.5 mg/l in Phytolacca americana as the minimum. Phytotoxic substances of ethanol extracts was investigated for antifungal activity against 23 selected fungus species. The antifungal activity of Phytolacca americana showed the greatest clear zone of 23 mm in Aspergillus awamori and its activity had an effect against 6 fungus species. Ailanthus altissima formed the greatest clear zone of 26 mm in Erwinia carotovora sub. sp. carotovora and had an effect agsinst 2 fungus species.

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Antioxidant compounds from the stem bark of Sorbus commixta

  • Na, Min-Kyun;An, Ren-Bo;Lee, Sang-Myung;Min, Byung-Sun;Kim, Young-Ho;Bae, Ki-Hwan;Kang, Sam-Sik
    • Natural Product Sciences
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    • 제8권1호
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    • pp.26-29
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    • 2002
  • The MeOH extract of Sorbus commixta (Rosaceae) exhibited strong DPPH radical scavenging activity, and through activity-guided fractionation two antioxidant compounds were isolated and identified as $catechin-7-O-{\beta}-D-xylopyranoside$ (1) and $catechin-7-O-\;{\beta}-D-apiofuranoside$ (2) by physicochemical and spectrometric methods. To evaluate the antioxidant effect of these compounds, some in vitro tests, such as the DPPH radical scavenging activity test, the superoxide radical scavenging activity test and the lipid peroxidation inhibitory activity test, were performed. Compounds 1 and 2 showed stronger activities than both a-tocopherol and butylated hydroxy anisole (BHA) in each assay.

Substituted Benzothiazolyl Urea 유도체의 합성 및 항균작용에 관한 연구 (Studies on the Syntheses and Antimicrobial Activity of Substituted Benzothiazolyl Urea Derivatives)

  • 강회양
    • 한국환경보건학회지
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    • 제7권2호
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    • pp.113-117
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    • 1981
  • Twelve benzothiazolyl and 6-substituted benzothiazoly phenyl and chlorophenyl ureas have been newly synthesized by reacting 2-amino benzothiazole and 2-amino-6-substituted benzothazole with three or four phenyl and chlorophenyl isocyanate, respectively. The structures of these compounds were determined by measurement of the molecular weights and elementary analysis as well as IR spectrophotometry. The compounds generally exhibited antibacterial activity against Staphylococcus aureus and Escherichia coli in the concentration of $50\mu g/ml$. The compounds containing chloro group exhibited stronger antibacterial activity than those containing methyl group against Eschichia coli. The difference in the antibacterial activity according to the substituted group (phenyl, o-, m-, and p-chlorophenyl) was also noted. The compounds containing o-chlorophenyl group, on the whole, exhibited more potent growth-inhibitory activity againsts staphylococcus aureus.

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데침조건에 따른 감태의 생리활성 성분 및 항산화 활성의 변화 (The Changes of Biologically Functional Compounds and Antioxidant Activities in Ecklonia cava with Blanching Times)

  • 김진아;이종미
    • 한국식생활문화학회지
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    • 제19권4호
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    • pp.369-377
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    • 2004
  • This study was performed to investigate the change of biologically functional compounds and antioxidant activities in Ecklonia cava with blanching times. As biologically functional compounds, the contents of minerals(K, Ca, Na, Mg, Fe, Cu, Mn and Zn), vitamins($vitamin\;C,\;{\beta}-carotene\;and\;{\alpha}-tocopherol$) and total polyphenol were analyzed. And antioxidant activity was determined through free radicals(DPPH radical, superoxide anion radical, hydroxyl radical and hydrogen peroxide) scavenging activity and linoleic acid peroxidation inhibitory activity. As the blanching time increased, the contents of minerals, vitamin C, ${\beta}-carotene$ and total polyphenol were decreased however ${\alpha}-tocopherol$ was not affected by blanching time, and antioxidant activities were decreased with blanching time.

Biological Activities of Larix kaempferi Needles

  • Kwon, Dong-Joo;Bae, Young-Soo
    • Journal of Forest and Environmental Science
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    • 제23권2호
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    • pp.87-91
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    • 2007
  • The needles of L. kaempferi was extracted with 95% ethanol and successively partitioned with n-hexane, $CH_2Cl_2$ and EtOAc. Repeated column chromatography on the EtOAc and $H_2O$ soluble fractions gave three flavan-3-ols, one flavone glycoside, six flavonol glycosides and one lignan derivative. Their structures were elucidated on the basis of chemical and spectroscopic evidences. The antioxidant activities of the isolated compounds were evaluated by DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging method. Flavan compounds indicated good antioxidative potentials compared with BHT (butylated hydroxytoluene) and ${\alpha}$-tocopherol as controls. In the anti-inflammatory test on most of the isolated compounds, NO (nitric oxide) assay against the RAW 264.7 (Mouse Macrophage) showed similar inhibitory potentials to NO production of the control. The cytotoxicity was determined by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay and most of the isolated compounds indicated no toxicity in various concentration.

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건조방법에 따른 해조류(톳)의 생리활성 성분 및 항산화 활성의 변화 (The Change of Biologically Functional Compounds and Antioxidant Activities in Hizikia Fusiformis with Drying Methods)

  • 이종미;김진아
    • 한국식생활문화학회지
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    • 제19권2호
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    • pp.200-208
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    • 2004
  • This study was performed to investigate the change of biologically functional compounds and antioxidant activities in Hizikia fusiformis with drying methods. As biologically functional compounds, the contents of minerals(K, Ca, Ma, Mg, Fe, Cu, Mn and Zn), vitamins(vitamin C, ${\beta}-carotene\;and\;{\alpha}-tocopherol$) and total polyphenol were analyzed. And antioxidant activity was determined through free radicals(DPPH radical, superoxide anion radical, hydroxyl radical and hydrogen peroxide) scavenging activity and linoleic acid peroxidation inhibitory activity. The contents of minerals were not affected by drying methods however vitamins and total polyphenol were lost more by sun-drying than other drying methods studies. Total polyphenol was preserved by freezing-drying than other drying methods studies, resulting in high antioxidant activities.

Antioxidant compounds from the twig of the Morus alba L

  • Jin, Wen-Yi;Na, Min-Kyun;Bo, An-Ren;Lee, Hyun-Yong;Bae, Ki-Hwan
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.377.2-377.2
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    • 2002
  • The MeOH extract of the twig of Marus alba L. (Moraceae) inhibited strong lipid peroxidation activity. Five antioxidative compounds were isolated through activity-guided fractionation. and identified as 6-geranylapigenin (1). 6-geranylnorartocarpetin(2). resveratrol (3). oxyresveratrol (4). quercetin (5) by physicochemical and spectrometric methods. In order to evaluate the antioxidant effect of these compounds. the lipid peroxidation inhibitory activity test were performed. Compounds 1-5 showed greater activity than tocopherol. (omitted)

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산사(Crataegi Fructus) 추출물로부터 ${\alpha}-amylase$${\alpha}-glucosidase$ 저해 물질 분리 및 동정 (Isolation and Identification of Inhibitory Compound from Crataegi Fructus on ${\alpha}-amylase$ and ${\alpha}-glucosidase$)

  • 김명욱;조영제;김정환
    • Applied Biological Chemistry
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    • 제50권3호
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    • pp.204-209
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    • 2007
  • 산사 추출물로부터 ${\alpha}-amylase$, ${\alpha}-glucosidase$ 저해활성을 탐색하고 Sephadex LH-20($5{\times}45$ cm)와 MCI-gel CHP-20를 이용하여 저해활성 물질을 정제하고 구조분석을 하였다. 산사 추출물의 페놀화합물의 함량은 물 추출물에서 22.5 mg/g, 60% ethanol 추출물에서 19.2 mg/g으로 나타났으며, 산사 물 추출물 (200 ${\mu}g/ml$)에서 ${\alpha}-amylase$, ${\alpha}-glucosidase$ 저해활성이 각각 100%와 82.6%로 나타났으나, 60% ethanol 추출물(200 ${\mu}g/ml$)에서는 ${\alpha}-glucosidase$ 저해활성이 12%로 낮은 저해활성을 나타내어 산사 물 추출물을 Sephadex LH-20를 이용하여 분획한 결과 I, II, III, IV의 4가지 분획물을 획득하고 다시 Sephadex LH-20과 MCI-gel을 이용하여 nomal phase type인 $EtOH{\rightarrow}H_2O$와 reverse phase type인 $H_2O{\rightarrow}MeOH$로 유기용매의 농도를 증가 시키며 용출하여 A, B, C, D의 compounds를 얻었다. 4가지 compound 중 compound C(200 ${\mu}g/ml$)가 ${\alpha}$-amylase, ${\alpha}$-glucosidase 저해활성이 각각 97.6%, 97.7%로 가장 높게 나타났으며, FAB-MS, NMR과 IR spectrum을 분석한 결과 chlorogenic acid로 동정되었다.

추출방법에 따른 참취(Aster scaber Thunb.)의 페놀화합물 함량과 생리활성 및 소화효소 저해 효과 (Polyphenolic Compounds, Physiological Activities, and Digestive Enzyme Inhibitory Effect of Aster scaber Thunb. Extracts According to Different Extraction Processes)

  • 김재원;윤광섭
    • 한국식품영양과학회지
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    • 제43권11호
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    • pp.1701-1708
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    • 2014
  • 참취의 활용 및 생리활성을 증가시킬 수 있는 적정 추출방법을 알아보고자 상온교반, 환류냉각, 가압가열, 저온고압 및 초음파 추출법을 이용하여 추출한 두벌 째 수확 참취 추출물의 생리활성을 비교하였다. 추출 수율은 환류냉각추출, 초음파추출, 가압가열추출, 상온추출, 저온고압추출 순으로 높았다. 폴리페놀, 플라보노이드 함량은 저온고압추출에서 유의적으로 높았고, 상압가열, 고온고압, 초음파추출에서는 대등한 함량을 나타내었다. 페놀화합물 정량의 경우 chlorogenic acid 함량은 가압가열추출에서 유의적으로 높았으며 cynarin 함량의 경우 환류냉각, 저온고압 및 초음파 추출에서 유의적으로 높았고, astragalin 함량의 경우 저온고압추출에서 높은 함량이 검출되었다. Xanthine oxidase(XO), angiotensin I-converting enzyme(ACE), HMG-CoA reductase 저해활성의 경우 저온고압추출 및 초음파 추출물에서 우수한 활성을 나타내었으며, 소화효소 저해활성(${\alpha}$-amylase, trypsin, lipase)에서도 유사한 경향을 나타내었다. 이러한 결과를 종합해 볼 때 저온고압 및 초음파 추출물에서 소재 활용가치가 높을 것으로 사료되며 천연 항산화제 및 기능성 증진을 위한 소재로 이용 가능할 것으로 판단된다.