• 제목/요약/키워드: $IC_{50}values$

검색결과 1,076건 처리시간 0.027초

In Vitro Free Radical and ONOO- Scavengers from Sophora flavescens

  • Jung, Hee-Jin;Kang, Sam-Sik;Hyun, Sook-Kyung;Choi, Jae-Sue
    • Archives of Pharmacal Research
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    • 제28권5호
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    • pp.534-540
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    • 2005
  • Activity-guided fractionation of the CH$_2Cl_2$-soluble fraction of the roots of Sophora flavescens furnished five 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scaveng ers: trans-hexadecyl ferulic acid (1) cis-octadecyl ferulic acid (2), trans-hexadecyl sinapic acid (3), (-)-4-hydroxy-3-methoxy-(6aR,11aR)-8, 9-methylenedioxypterocarpan (4) and desmethylanhydroicaritin (8), along with nine known inactive compounds: (-)-maackiain (5), xanthohumol (6), formononetin (7), (2S)-2'-methoxykurarinone (9), (2S)-3${\beta}$,7,4'-trihydroxy-5-methoxy-8-(${\gamma},{\gamma}$- imethylallyl )-flavanone (10), (2S)-7,4'-dihydroxy-5-methoxy-8- (${\gamma},{\gamma}$-dimethylallyl ) -flavanone (11), umbelliferone (12), kuraridin (13), and trifolirhizin (14). Compounds 1-4 and 8 exhibited DPPH free radical scavenging effects at IC$_{50}$ values of 33.01 ${\pm}$ 0.20, 57.06 ${\pm}$ 0.16, 39.84 ${\pm}$ 0.36, 35.83 ${\pm}$ 0.47, and 18.11 ${\pm}$ 0.04${\mu}$M, respectively. L-Ascorbic acid, when used as a positive control, exhibited an IC$_{50}$ value of 7.39 ${\pm}$ 0.01 ${\mu}$M. Compounds 1-4 and 8 also appeared to exert significant scavenging effects on authentic ONOO-, with IC$_{50}$ values of 5.76 ${\pm}$ 1.19, 15.06 ${\pm}$ 1.64, 8.17 ${\pm}$ 4.97, 1.95 ${\pm}$ 0.29 and 4.06 ${\pm}$ 2.41 ${\mu}$M, respectively. Penicillamine (IC$_{50}$= 2.36 ${\pm}$ 0.79${\mu}$M) was used as a positive control. In addition, compounds 2,4,6,8, and 10 were isolated from this plant for the first time.

한약재 13종의 hERG 채널 관련 심장독성 평가 (hERG Channel-Related Cardiotoxicity Assessment of 13 Herbal Medicines)

  • 하혜경;이시온;김동현;서창섭;신현규
    • 대한한의학회지
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    • 제42권3호
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    • pp.44-55
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    • 2021
  • Objectives: As the use of herbal medicinal products (HMPs) increases worldwide, systematic verification of the safety of HMPs is required. The induction of cardiotoxicity is one of the major factors in post-approval withdrawal of medicinal products, and drug-induced cardiotoxicity assessment is emerging as an important step in drug development. In the present study, we evaluated human ether-à-go-go-related gene (hERG) potassium channel-related cardiotoxicity to predict the risk of cardiac arrhythmia in thirteen herbal medicines known to have cardiac toxicity. Methods: We measured the inhibition rate of hERG potassium channel activity of 13 medicinal herbal extracts in hERG-expressing HEK 293 cells using an automated patch-clamping system. Quinidine was used as a positive control for inhibition of hERG activity. Results: Extracts of Evodiae Fructus, Strychni Semen, and Corydalis Tuber potently inhibited the activity of hERG, and IC50 values were 3.158, 19.87, and 41.26 ㎍/mL, respectively. Cnidi Fructus, Ephedra Herba, Lithospermi Radix, Polygoni Multiflori Radix, Visci Ramulus et Folium, Asiasari Radix et Rhizoma, and Scolopendra weakly inhibited hERG activity, and the IC50 value for each herbal medicine was more than 400 ㎍/mL. Aconiti Kusnezoffii Tuber and two types of Aconiti Lateralis Radix Preparata (Po and Yeom) had weak inhibitory activity against hERG, and the IC50 values were more than 700 ㎍/mL. The IC50 value of quinidine against hERG was 1.021 𝜇M. Conclusion: Evodiae Fructus, Strychni Semen, and Corydalis Tuber acted as potent inhibitors against hERG. These herbal medicines may cause cardiac arrhythmia through QT prolongation, so care should be taken when taking them.

식용 버섯류의 도파민 베타 수산화효소에 대한 저해활성 검색 (Screening of Inhibitory Activity of Edible Mushrooms on Dopamine ${\beta}-Hydroxylase$)

  • 황금희;김현구;한용남
    • 한국식품과학회지
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    • 제29권2호
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    • pp.194-197
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    • 1997
  • 식용버섯류 중 국내에서 재배되고 있는 식용버섯류에 대한 생리활성 검색의 일환으로 영지, 양송이, 표고 등 3종의 버섯을 대상으로 dopamine ${\beta}-hydroxylase(DBH)$에 대한 저해활성을 tyramine을 기질로 하여 검색하였다. 각 버섯들의 DBH에 대한 저해활성은 영지버섯은 클로로포름 분획에서 100% 이상의 현저한 저해활성을 나타내었으며 표고와 양송이는 에틸아세테이트 분획에서 각각 79.7%라 64.7%의 저해활성을 나타내었다. 한편, 이들 버섯류의 각 용매분획에 대하여 DBH 저해활성을 검색하여 각 분획의 $IC_{50}$을 구하고 용매분획 총량의 specific activity를 비교한 결과, 영지버섯의 클로로포름분획의 $IC_{50}$$1.60{\times}10^{-4}\;g$으로 DBH에 대한 저해활성을 나타내었고 양송이와 표고버섯의 경우 에틸아세테이트 분획의 $IC_{50}$$5.50{\times}10^{-4}\;g,\;2.35{\times}10^{-4}\;g$으로 각각 검색되었다.

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노니 과실에 함유된 항산화물의 추출 공정 (Extraction Procedures for Free Radical Scavenging Activity from Noni Fruit (Morinda citrifolia))

  • 곽미경;최희선;;홍정화
    • 한국약용작물학회지
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    • 제19권1호
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    • pp.38-46
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    • 2011
  • In this study, we investigated maximum yield of radical scavenging activity (RSA) using each of various extraction solvents and procedure from noni friut (Morinda citrifolia). Noni fruits were either sun-dried (FS) or hot-air dried (FO) at $60^{\circ}C$ after steam blanching. For optimum aqueous extraction, noni fruits should be sun dried and autoclave extraction time should not be over 30 min to produce extraction with high RSA with low cost. In case of 50% ethanol extraction, reflux extracts of FS and FO resulted in $IC_{50}$ of 1.92 mg/mL and 3.06 mg/mL at 8 hr. When $IC_{50}$ values were lower than 5 mg/mL, coefficient of correlation was 0.71 indicating that 71% of the phenolic antioxidants in noni fruits were accounted for the activity by scavenging free DPPH. However, coefficient of correlation significantly decreased to 0.63 over $IC_{50}$ values of 5 mg/mL. Autoclave extraction contained chlorogenic acid of $14.69 \;{\mu}g/mL$ and scopoletin of $3.86 \;{\mu}g/mL$. Reflux extraction showed all three compounds, chlorogenic acid ($26.19 \;{\mu}g/mL$), quercetin ($19.59 \;{\mu}g/mL$), and scopoletin ($17.4 \;{\mu}g/mL$). Therefore, the result of this study indicated that the potential antioxidant activities and functional values were obtained significantly with reflux extraction from noni fruit.

지모(知母) 추출물이 L-1210 및 S-180 암세포주 성장 억제에 미치는 영향 (The Growth Inhibition Effect of L-1210 and S-180 Cancer Cell Lines by the Extract from Anemarrhena Asphodeloides)

  • 임치혜;초재승;김효수;권승만;김신;김일환;박혜선
    • 사상체질의학회지
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    • 제19권2호
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    • pp.170-178
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    • 2007
  • 1. Objective This study was aimed to screen the potential antitumor activity of one kinds of Korean medicinal herb extracts against cancer cell lines and to evaluate the growth inhibition effect of L-1210 and S-180 cancer cell lines. 2. Methods It confirmed Anemarrhena asphodeloides extracts to screen the potential antitumor activity. Then, it was extracted with 4 kinds of solvents ; hexane, ethyl acetate, butanol and $H_2O$, and the Growth inhibition effect of these extracts were determined against cancer cell and normal cell. The results were as follows : The IC50(50% inhibitory concentration) values of Anemarrhena asphodeloides extracts were shown to be $253{\mu}g/ml$ against L-1210 cell lines. The IC50 values of ethyl acetate extracts were shown to be $915{\mu}g/ml$ against L-1210 cell lines. The IC50 values of butanol extracts were shown to be $52.3{\mu}g/ml$, $485{\mu}g/ml$ against L-1210, S-180 cell lines, respectively. The butanol extracts were more selectively effective than other extracts to cancer cell lines. 3. Conclusion From these data, it could be concluded that the Anemarrhena asphodeloides extracts to the Growth inhibition effect of L-1210 and S-180 cancer cell lines.

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치자의 항산화 활성 및 활성성분의 분리 (Antioxidative Activities and Components of Gardenia jasminoides)

  • 양혜정;박미정;이흠숙
    • 한국식품과학회지
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    • 제43권1호
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    • pp.51-57
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    • 2011
  • 치자의 항산화 활성과 유지산화 지연효과를 측정하고 활성을 보인 분획에서 주성분인 geniposide와 crocin을 분리하고 그 구조를 확인하였다. 여러 분획 중 부탄올 분획과 물 분획의 항산화성이 가장 우수함을 확인하고 그 분획의 주성분으로 분리된 geniposide와 crocin의 단일물질로서의 항산화력을 측정 비교한 결과, crocin의 항산화력이 더 강함을 알 수 있었다. 특히 SOD 유사활성 시험에서 여러 분획의 활성이 총 메탄올 추출물보다도 낮음에 비하여 crocin 단일 물질은 양성 대조군 cholorogenic acid의 $EC_{50}$ 값 453 ppm에 비하여 절반정도 낮은 $EC_{50}$값 259 ppm으로 매우 높은 활성을 보였다. 유지 산화 지연효과도 치자의 총 메탄올 추출물 250 ppm 이상의 농도에서의 AI값은 BHA 1000 ppm에서의 AI값 1.66 보다 큰 1.81 이상임을 보여 유지 산화 지연효과가 우수함을 나타내었다. 이 논문의 연구결과로 치자의 항산화 기능성 식품 및 첨가제로서의 개발가능성이 확인되었다고 사료된다.

수종의 생약추출물이 Monoamine Oxidase 활성에 미치는 영향 (제1보) (Effects of Herbal Medicines on Monoamine Oxidase Activity (I))

  • 이상선;김영호;배기환;김학성;이명구
    • 생약학회지
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    • 제29권4호
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    • pp.271-276
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    • 1998
  • The inhibitory effects of MeOH extracts of 100 medicinal herbs on monoamine oxidase (MAO) activity were investigated. MAO was purified from mouse brain and its activity was determined by fluorospectrophotomer using kynuramine as a substrate. Nine kinds of MeOH extracts of herbs including Artemisia iwayomogi showed a mild inhibitory effect with ${100}-{200}\;{\mu}/ml$ in their $IC_{50}$ values on MAO activity. Seventeen MeOH extracts including Juglans mandshurica exhibited a weak inhibition of MAO activity with ${200}-{300}\;{\mu}/ml$ in their $IC_{50}$ values.

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Cholinesterase Inhibitory Constituents from Capsosiphon fulvescens

  • Fang, Zhe;Jeong, Su Yang;Choi, Jae Sue;Min, Byung Sun;Min, Bo Kyung;Woo, Mi Hee
    • Natural Product Sciences
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    • 제18권4호
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    • pp.233-238
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    • 2012
  • Nine compounds (1 - 9), ${\alpha}$-linolenic acid (1), cis-5,8,11,14,17-elcosapentaenoic acid (2), phytol (3), loliolide (4), uridine (5), thymidine (6), deoxyadenosine (7), adenine (8), and adenosine (9), were isolated from the n-hexane, methylene chloride, ethyl acetate and n-butanol fractions of Capsosiphon fulvescens. The structures of these compounds were elucidated on the basis of spectroscopic evidence. Compounds 1 - 9 exhibited acetylcholinesterase (AChE) inhibitory activities with $IC_{50}$ values ranging from 114.91 to $252.40{\mu}M$, whereas 2 - 4 showed butyrylcholinesterase (BChE) inhibitory activities with $IC_{50}$ values ranging from 251.18 to $499.16{\mu}M$.

Further Isolation of Peroxynitrite and 1, 1-Diphenyl-2-picrylhy-drazyl Radical Scavenging Isorhamnetin 7-Ο-glucoside from the Leaves of Brassica juncea L.

  • Choi, Jae-Sue;Jung, Mee-Jung;Park, Hye-Jin;Chung, Hae-Young;Kang, Sam-Sik
    • Archives of Pharmacal Research
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    • 제25권5호
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    • pp.625-627
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    • 2002
  • From the leaves of Brassica juncea, an radical scavenging isorhamnetin 7-Ο-glucoside on peroxynitrite and 1,1-diphenyl-2-picrylhydrazyl (DPPH) was isolated and characterized based on the spectroscopic evidence. The compound showed the peroxynitrite and DPPH scavenging activities with $IC_{50}$ values of 2.07$\pm$0.17 and 13.3 $\mu$M, respectively. Penicillamine and L-ascorbic acid as positive control exhibited radical scavenging activities with $IC_{50}$ values of 3.17$\pm$0.39 and 12.78 $\mu$M, respectively.

Studies of Structure Activity Relationship of Flavonoids for the Anti-allergic Actions

  • Cheong, Ho;Ryu, Shi-Yong;Oak, Min-Ho;Cheon, Seung-Hoon;Yoo, Gyurng-Soo;Kim, Kyeong-Man
    • Archives of Pharmacal Research
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    • 제21권4호
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    • pp.478-480
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    • 1998
  • The structure activity relationship of flavonoids for anti-allergic actions was studied by determining the $IC_{50}$ values for the degranulation. The hexosaminidase release from RBL-2H3 cells (degranulation marker) was employed as an estimate for the anti-allergic actions. Among 22 flavonoid compounds tested, luteolin, apigenin, diosmetin, fisetin, and quercetin were found to be most active with $IC_{50}$ values less than 10 $\mu\textrm{M}$.

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