• Title/Summary/Keyword: $IC_{50}$ values

Search Result 1,075, Processing Time 0.036 seconds

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
    • /
    • v.28 no.5
    • /
    • pp.534-540
    • /
    • 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.

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

  • Ha, Hyekyung;Lee, Sion;Kim, Dong-Hyun;Seo, Chang-Seob;Shin, Hyeun-kyoo
    • The Journal of Korean Medicine
    • /
    • v.42 no.3
    • /
    • pp.44-55
    • /
    • 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.

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

  • Hwang, Keum-Hee;Kim, Hyun-Ku;Han, Yong-Nam
    • Korean Journal of Food Science and Technology
    • /
    • v.29 no.2
    • /
    • pp.194-197
    • /
    • 1997
  • Dopamine ${\beta}-hydroxylase\;(DBH)$ catalyses the enzymatic reaction of dopamine to norepinephrine. For the purpose of screening DBH inhibitory activity from edible mushrooms, Ganoderma lucidum, Agaricus bisporus and Lentinus edodes were examined by tracing inhibitory activities against bovine adrenal DBH, utilizing tyramine as a substrate. Among the three edible mushrooms tested, Ganoderma lucidum showed potent enzyme inhibitory activilies above 100% against DBH in chloroform fraction. Lentinus edodes and Agaricus bisporus showed inhibitory activities in ethylacetate fraction on 79.7% and 64.7%, respectively. Each solvent fraction of these mushrooms were assessed in the aspects of their inhibitory activities against DBH, and their $IC_{50}$ values were calculated. $IC_{50}$ value of chloroform fraction of Ganoderma lucidum was $1.60{\times}10^{-4}\;g$, and those of ethylacetate fractions of Agaricus bisporus and Lentinus edodes were $5.50{\times}10^{-4}\;g\;and\;2.35{\times}10^{-4}\;g$, respectively.

  • PDF

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

  • Gwak, Mi-Kyung;Choi, Hee-Sun;Manochai, Benya;Hong, Jeong-Hwa
    • Korean Journal of Medicinal Crop Science
    • /
    • v.19 no.1
    • /
    • pp.38-46
    • /
    • 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.

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

  • Yim, Chi-Hye;Cho, Jae-Seung;Kim, Hyo-Soo;Kwon, Seung-Man;Kim, Shin;Kim, Il-Hwan;Park, Hye-Sun
    • Journal of Sasang Constitutional Medicine
    • /
    • v.19 no.2
    • /
    • pp.170-178
    • /
    • 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.

  • PDF

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

  • Yang, Hye-Jung;Park, Mi-Jung;Lee, Heum-Sook
    • Korean Journal of Food Science and Technology
    • /
    • v.43 no.1
    • /
    • pp.51-57
    • /
    • 2011
  • From the total methanolic extract of Gardenia jasminoides (Rubiaceae), various antioxidative characteristics were identified in terms of nitrite scavenging ability, 2,2'-azino-bis (3-ethylbenzthiazoline-6-sulphonic acid) (ABTS) radical cation inhibition, superoxide dismutase (SOD)-like activity, and elongation effect of lipid peroxidation using Rancimat. After successive partitioning with n-hexane, chloroform, n-butanol, and water, potent nitrite scavenging abilities were shown in the n-butanol fraction and water fraction, and $IC_{50}$ values were 183 ppm and 194 ppm, respectively. As for ABTS radical cation inhibition, the chloroform fraction was most potent and its $IC_{50}$ was 159 ppm. SOD-like activity was slightly low in all of the fractions. The elongation effect of lipid peroxidation also increased dose-dependently and the antioxidative index (AI) of the total methanolic extract was 2.93 in 1000 ppm, which was more effective than 1.66 of butylated hydroxy anisol in the same concentration. The compounds I and II were isolated through silica gel column chromatography of the active fractions, and identified as geniposide and crocin, respectively, by $^1H-NMR$ spectral data. The $IC_{50}$ values for the nitrite scavenging abilities of geniposide and crocin were 940 ppm and 77 ppm, respectively. In ABTS radical cation inhibition, the $IC_{50}$ values of geniposide and crocin were 684 ppm and 549 ppm, respectively. And the $EC_{50}$ value for SOD-like activity of crocin was 259 ppm, which was much smaller than 453 ppm by the positive control, chlorogenic acid. The $EC_{50}$ value of geniposide could not be identified.

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

  • Lee, Sang-Seon;Kim, Young-Ho;Bae, Ki-Hwan;Kim, Hack-Seang;Lee, Myung-Koo
    • Korean Journal of Pharmacognosy
    • /
    • v.29 no.4
    • /
    • pp.271-276
    • /
    • 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.

  • PDF

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
    • /
    • v.18 no.4
    • /
    • pp.233-238
    • /
    • 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
    • /
    • v.25 no.5
    • /
    • pp.625-627
    • /
    • 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
    • /
    • v.21 no.4
    • /
    • pp.478-480
    • /
    • 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 $\mu\textrm{M}$.

  • PDF