• Title/Summary/Keyword: $IC_50$

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Screening for Cytotoxicity of Crude Extracts from Fruit on Leukaemia Cells in Citrus and Related Genera

  • Soo
    • Korean Journal of Plant Resources
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    • v.10 no.3
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    • pp.213-220
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    • 1997
  • The present study has been undertaken to characterize availability of citrus as a medicinal plant with antineoplastic property. The crude extracts from 40 species of fruits with 12 species of the local Citrus in Cheju island were evaluated on their potential activities against mouse P388 lymphocytic leukaemia in vitro. The percent cytotoxicity varied from 25.40 to 97.94% at a concentration of $100{\mu}g/mL$. Among 40 spp., 8 species showed high toxicity more than 90% against P388 cells and Cheongkyool(C. nippokoreana) exhibited the most cytotoxicity as 97.94%($IC_{50}=20.2{\mu}g/mL$). Nine varieties of C. junos were showed insiginicant cytotoxicity. In trifoliate orange, immature fruit was stronger than mature and peel extract showed higher cytotoxicity($IC_{50}=18{\mu}g/mL$) than the other tissues. Hexane fraction from methanol(MeOH) extract of trifoliate orange showed highly significant inhibition of cell growth($IC_{50}=3.9{\mu}g/mL$). In addition, its cytotoxicity increased remarkably from 3.95 to $0.40{\mu}g/mL$ as exposure time legthened. Cytotoxic activities of crude extracts were decreased considerably during a six months storage period. It was apparent that there is considerable variation in cytotoxicity, depending upon species, maturity and storage time of extracts. There was no meaningful cytotoxic difference between archicitrus and metacitrus in the genus Citrus.

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Cytotoxic Saponins from the Root of Dipsacus asper Wall

  • Hung Tran Manh;Jin WenYi;Thuong Phuong Thien;Song Kyung Sik;Seong Yeon Hee;Bae KiHwan
    • Archives of Pharmacal Research
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    • v.28 no.9
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    • pp.1053-1056
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    • 2005
  • Cytotoxic activitiy of seven hederagenin saponins isolated from the root of Dipsacus asper were investigated in vitro against L1210, HL-60 and SK-OV-3 tumor cell lines by the MTT method. $3-O-\alpha-L-rhamnopyranosyl-(1{\rightarrow}2)-\alpha-L -arabinopyranosyl$ hederagenin (2),\;$3-O-\beta-D­xylopyranosyl-( 1{\rightarrow}3)-\alpha-L-Rhamnopyranosyl-(1{\rightarrow}2)-\alpha-L -arabinopyranosyl$ hederagenin (6) and $3-O-\beta-D-glucopyranosyl-(1{\rightarrow}3)-\alpha-L-rhamnopyranosyl-( 1{\rightarrow}2)-\alpha-L-arabinopyranosyl$ hederagenin (7) exhibited the potent cytotoxicity against the three tumor cell lines with $IC_{50}$ values ranging from 4.7 to 8.7 ${\mu}g/mL$, with the exception of compound 7, which exhibited weak cytotoxic activity against SK-OV-3 $(IC_{50}\;22.5\;{\mu}g/mL)$. Other compounds did not exhibit any cytotoxic activity $(IC_{50}>30{\mu}g/mL)$.

Monoamine Oxidase Inhibitory Coumarins from the Aerial Parts of Dictamnus albus

  • Jeong, Seon-Hwa;Han, Xiang Hua;Hong, Seong-Su;Hwang, Ji-Sang;Hwang, Ji-Hye;Lee, Dong-Ho;Lee, Myung-Koo;Ro,, Jai-Seup;Hwang, Bang-Yeon
    • Archives of Pharmacal Research
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    • v.29 no.12
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    • pp.1119-1124
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    • 2006
  • The methanol extract from the aerial parts of Dictamnus albus was active in inhibiting monoamine oxidase (MAO) from the mouse brain. Activity-guided fractionation led to the isolation of four known coumarins, 7-(6'R-hydroxy-3', 7'-dimethyl-2'E, 7'-octadienyloxy) coumarin (1), auraptene (2), umbelliferone (3), and xanthotoxin (4), as active compounds along with an inactive alkaloid, skimmianine (5). Compounds 1 and 2 inhibited MAO activity in a concentration-dependent manner with $IC_{50}$ values of 0.7 and $1.7\;{\mu}M$, respectively. Compounds 1 and 2 showed a slight and potently selective inhibitory effect against MAO-B ($IC_{50}\;0.5\;and\;0.6\;{\mu}M,\;respectively$) compared to MAO-A ($IC_{50}\;1.3\;and\;34.6\;{\mu}M,\;respectively$). According to kinetic analyses derived by Lineweaver-Burk reciprocal plots, compounds 1 and 2 exhibited a competitive inhibition to MAO-B.

Anticancer Effects of Natural Medicinal Plant Extracts on Oral Carcinoma Cells (천연 약용식물 추출물의 구강상피세포암 세포주에 대한 항암효과)

  • 김정희;현진원;김여갑
    • Biomolecules & Therapeutics
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    • v.7 no.2
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    • pp.153-157
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    • 1999
  • The anticancer effect of medicinal plants against two oral carcinoma cells, A253 and SCC-25 were investigated in this study. Methanol extracts from 63 medicinal plants, which have anticancer activities against other cancers such as stomach, hepatocellular or colon carcinomas, were prepared and screened for their anti- oral cancer activity by using MTT assay. Thirty one samples showed anti-oral cancer activity against either cell line used, however, other 32 samples had no anti-oral cancer activity. Among these samples methanol extract of Caesalpinia sappan revealed the strongest anti-oral cancer activity. The $IC_{50}$/ values of this extract against A253 and SCC-25 cells were 16 and 25 $\mu$g/m1, respectively. Fractions of n-hexane, dichloromethane, ethylacetate, n-buthanol and water were prepared from methanol extracts of Caesalpinia sappan, Anthriscus sylvestris, Rhus japonica, Curcuma arowatica, Inula helenium, Sinoarnudinaria reticulata, and Polygonum cuspidatum, respectively. Among these 35 fractions the n-hexane fraction of Inula helenium showed the strongest anti-oral cancer activity, the $IC_{50}$/ value was 1.6$\pm$0.3 $\mu\textrm{g}$/ml. Ten other fractions showed $IC_{50}$/ values lower than 10 $\mu\textrm{g}$/ml.

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Physiological Functionalities and Anti-oxidant activity of heated radish extract

  • Kim, Hyun-Kyoung
    • International journal of advanced smart convergence
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    • v.7 no.2
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    • pp.38-46
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    • 2018
  • This study proceeded an experiment that can increase such physiological properties of heated radish extract. During the extraction of radish, including the byproduct, an increase in antioxidant properties of radish according the heating temperature was performed. Upon the extracts of radish bark and radish green extract(mucheong), the physiological functionalities and antioxidant activity were investigated. As a result, the color of radish ethanol extract in dependence of heating temperature, showed light brown color at low heating temperature and black color from $150^{\circ}C$. The total polyphenol content significantly increased as a result of heat treatment; 6.7 times and 22 times higher than the control at $110^{\circ}C$ and $150^{\circ}C$, respectively. DPPH radical scavenging ability and antioxidant property increased with increasing heating temperature; in comparison to heat-treated radish at $110^{\circ}C$ and $150^{\circ}C$, $IC_{50}$ decreased by 1/22 times. $IC_{50}$ of the control was 23times higher than $150^{\circ}C$ heat treated radish (Control $IC_{50}$:130.305). According to the graph that represents ABTS activity, antioxidant activity increased in dependence of heat treatment likewise to the total polyphenol content and DDPH radical scavenging activity. Upon heat treatment at $150^{\circ}C$, antioxidant activity in consequence of ABTS assay increased 23 times higher than the control.

Anti-Proliferative Activity and Apoptosis Induction of an Ethanolic Extract of Boesenbergia pandurata (Roxb.) Schlecht. against HeLa and Vero Cell Lines

  • Listyawati, Shanti;Sismindari, Sismindari;Mubarika, Sofia;Murti, Yosi Bayu;Ikawati, Muthi
    • Asian Pacific Journal of Cancer Prevention
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    • v.17 no.1
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    • pp.183-187
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    • 2016
  • Rhizomes of Boesenbergia pandurata (Roxb.) Schlecht have been reported to contain active compounds with anticancer properties. This research was carried out to examine anti-proliferative and apoptotic induction against HeLa and Vero cells-line. Dried powder of B. pandurata rhizomes was extracted by a maceration method using 90% ethanol. Cytotoxic assays to determine $IC_{50}$ and anti-proliferative effects were carried out by MTT methods. Observation of apoptosis was achieved with double staining using acridine orange and ethidium bromide. The results showed that ethanolic extract of B. pandurata was more cytotoxic against HeLa cells ($IC_{50}$ of $60{\mu}g/mL$) than Vero cells ($IC_{50}$ of $125{\mu}g/mL$). The extract had higher anti-proliferative activity as well as apoptotic induction in HeLa than Vero cells. Therefore, it was concluded that the ethanolic extract of B. pandurata had anti-proliferative as well as apoptosis induction activity dependent on the cell type.

Extracts and Essential Oil of Ledum palustre L. Leaves and Their Antioxidant and Antimicrobial Activities

  • Kim, Dong-Myong;Nam, Bong-Woo
    • Preventive Nutrition and Food Science
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    • v.11 no.2
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    • pp.100-104
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    • 2006
  • The in vitro antimicrobial and antioxidant activities of the essential oil and methanol extracts of Ledum palustre L. were investigated. Using GC-MS analysis, we identified 37 compounds in the essential oil, constituting 87.58% of the total oil. There are several monoterpenes, of which sabinene is the major compound ($16{\sim}17%$). There are several oxygenated monoterpenes of which terpinen-4-ol(7.6%) and myrtenal (3.5%) are the main constituents. $\beta$-Selinene, a-selinene, $\gamma$-elemene, a-caryophyllene are the main sesquiterpenes ($2{\sim}6%$ range). The oil strongly reduced the diphenylpicrylhydrazyl radical ($IC_{50}=1.56{\mu}g/mL$) formation and exhibited a hydroxyl radical scavenging effect in the $Fe^{3+}-EDTA-H_2O_2$ deoxyribose system ($IC_{50}=2.7{\mu}g/mL$), and also inhibited the nonenzymatic lipid peroxidation of rat liver homogenate ($IC_{50}=13.5{\mu}g/mL$). The polar phase of the extract showed antioxidant activity. The oil showed antimicrobial activity against Streptococcus pneumoniae, Clostridium perfringens, Candida albicans, Mycobacterium smegmatis, Acinetobacter lwoffii and Candida krusei while the water-insoluble parts of the methanolic extracts exhibited slight or no activity. This study confirms that the essential oil of Ledum palustre L. possesses antioxidant and low antimicrobial properties in vitro.

Evaluation of ${\mu}$-Calpain Inhibitory Activity of Korean Indigenous Marine Organism Extracts

  • Lee, Yoo-Jin;Lee, Eun-Young;Han, Ah-Reum;Song, Jun-Im;Kwon, Young-Joo;Seo, Eun-Kyoung
    • Natural Product Sciences
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    • v.18 no.2
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    • pp.102-105
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    • 2012
  • Marine organism extracts were prepared from 26 species of Korean indigenous marine organisms, including 25 species belonging in class Anthozoa of phylum Cnidaria and a species belonging to subphylum Urochordata of phylum Chordata, and screened their inhibitory effects against ${\mu}$-calpain. As a result, the thirteen extracts were found to be active in the criteria of $IC_{50}$ < 100 ${\mu}g/ml$. Among them, the MeOH extracts of Plexauroides praelonga and Alveopora japonica showed remarkable ${\mu}$-calpain inhibitory activity with $IC_{50}$ values of $4.62{\pm}0.22$ and $4.82{\pm}0.07{\mu}g/ml$, respectively. In addition, chemical investigation of A. japonica led to the isolation of an active compound, hexadecyl tetradecanoate, as a selective cathepsin B inhibitor ($IC_{50}=9.05{\pm}2.45{\mu}M$). This compound was isolated as constituent of A. japonica for the first time in the present study.

혈소판 분리 방법에 따른 혈소판 응집 억제 효능 검색법

  • 고석태;정진호;류근호
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1993.04a
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    • pp.152-152
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    • 1993
  • 혈전 등에 의한 혈행 장애 예방 및 치료 약물의 개발을 목적으로 혈소판 기능에 대한 약물의 영향을 연구하는데 있어, 효율적인 실험 조건의 선택은 중요하다. 본 연구에서는 마늘 메탄올 추출물의 혈소판 응집 억제능을 platelet rich plasma(PRP), washed platelet (Ca$^2$비첨가), washed platelet(Ca$_{2+}$ 첨가) 등 세가지 분리 조건을 사용하여 실험하였다. 그 결과 마늘 추출물의 $IC_{50}$/이 각각 2348 $\mu\textrm{g}$/ml, 221 $\mu\textrm{g}$/ml, 851 $\mu\textrm{g}$/ml로서, washed platelet(Ca$_{2+}$ 비첨가)가 마늘 추출물의 혈소판 응집 억제 작용에 가장 민감한 것으로 나타났다. 또한 마늘 추출물과는 다른기전으로 혈소판 응집 억제 효과를 나타내는 menadione과 propranolol도 이와 동일한 결과를 보였다. 실험 조건에 따른 이러한 차이가 PRP 중에 존재하는 알부민 등과의 단백 결합에 의한 약물의 유효농도 감소에 기인한다고 추정되어, washed platelet에 여러 농도의 알부민을 첨가하여 혈소판 응집 억제 실험을 실시한 결과 약물의 $IC_{50}$/은 알부민 농도 의존적으로 증가하였다. 혈소판 응집과 함께 혈소판 기능 변화를 측정하는 지표인 혈소판 분비능을 분비된 ATP를 Luciferin-Luciferase로 측정하여 알아보았다. 그 결과 thrombin에 의한 혈소판의 ATP 유리에 미치는 마늘 추출물의 영향을 위의 세 실험 조건에서 실험하여 $IC_{50}$/을 비교한 결과 그 값이 washed platelet에서 가장 낮고 PRP에서 가장 높아, 혈소판 응집 억제 실험과 동일한 결과를 나타내었다. 이상의 결과는 세가지 혈소판 분리 조건 중 washed platelet(Ca$_{2+}$ 비첨가)가 약물에 의한 혈소판 기능 억제실험에 가장 효율적임을 제시하고 있으며, 그 주요한 원인은 알부민 등 단백 결합에 의한 유효 약물 농도 감소 때문이라고 추정된다.

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Antioxidant and Antiproliferative Activities of Methanolic Extract from Celandine

  • Hu, Weicheng;Wang, Myeong-Hyeon
    • Food Science and Biotechnology
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    • v.18 no.1
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    • pp.207-212
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    • 2009
  • Celandine (Chelidonium majus, family Papaveraceae) is an herb used extensively in traditional Korean medicine. To investigate its antioxidant and antiproliferative activities, the methanolic extract of celandine was introduced. The antioxidant properties of the extract were tested using various in vitro systems, including hydroxyl radical scavenging assay, DNA damage protection assay, 1,1-diphenyll-2-2-pricylhydrazyl (DPPH) free radical scavenging activity, metal chelating activity, and reducing power assay. The extract exhibited stronger antioxidant activity ($IC_{50}=7.92{\mu}g/mL$) against hydroxyl radicals in the Fenton system than butylated hydroxyanisole ($IC_{50}=51.46{\mu}g/mL$) and $\alpha$-tocopherol ($IC_{50}=67.48{\mu}g/mL$). Likewise, damage to the plasmid pBR 322 induced by hydroxyl radicals was found to be protected by the extract at a concentration of $400{\mu}g/mL$. Cellular proliferation and the induction of apoptosis were also examined by a cellular proliferation assay, flow cytometry, and mRNA expression analysis. Taken together, the extract significantly inhibited the growth of HT-29 cells in a concentration- and time-dependent manner, and gradually increased both the proportion of apoptotic cells and the expression of caspase-3. Overall, our research suggests that celandine possesses antioxidant and antiproliferative properties.