• Title, Summary, Keyword: cytotoxic activity

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The antioxidant and cytotoxic activities of Sonchus oleraceus L. extracts

  • Yin, Jie;Kwon, Gu-Joong;Wang, Myeong-Hyeon
    • Nutrition Research and Practice
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    • v.1 no.3
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    • pp.189-194
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    • 2007
  • This study investigated in vitro antioxidant activity of Sonchus oleraceus L. by extraction solvent, which were examined by reducing power, hydroxyl radical-scavenging activity(HRSA) and 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assays. 70% MeOH extract had the greatest reducing power while EtOH extract had the greatest HRSA. The antioxidant activity of S. oleraceus extracts was concentration dependent and its $IC_{50}$ values ranged from 47.1 to $210.5\;{\mu}g/ml$ and $IC_{50}$ of 70% MeOH, boiling water and 70% EtOH extracts were 47.1, 52.7 and $56.5\;{\mu}g/ml$, respectively. 70% MeOH extract of S. oleraceus contained the greatest amount of both phenolic and flavonoid contents. The extracts tested had greater nitrite scavenging effects at lower pH conditions. The cytotoxic activity showed that EtOH extract had the best activity against the growth of stomach cancer cell. These results suggest that S. oleraceus extract could be used as a potential source of natural antioxidants.

Cytotoxic Activity and Quantitative Structure Activity Relationships of Arylpropyl Sulfonamides

  • Hwang, Yu Jin;Park, Sang Min;Yim, Chul Bu;Im, Chaeuk
    • The Korean Journal of Physiology and Pharmacology
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    • v.17 no.3
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    • pp.237-243
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    • 2013
  • B13 is a ceramide analogue and apoptosis inducer with potent cytotoxic activity. A series of arylpropyl sulfonamide analogues of B13 were evaluated for their cytotoxicity using MTT assays in prostate cancer PC-3 and leukemia HL-60 cell lines. Some compounds (4, 9, 13, 14, 15, and 20) showed stronger activities than B13 in both tumor cell lines, and compound (15) gave the most potent activity with $IC_{50}$ values of 29.2 and 20.7 ${\mu}M$, for PC-3and HL-60 cells, respectively. Three-dimensional quantitative structure-activity relationship (3D-QSAR) analysis was performed to build highly reliable and predictive CoMSIA models with cross-validated $q^2$ values of 0.816 and 0.702, respectively. Our results suggest that long alkyl chains and a 1R, 2R configuration of the propyl group are important for the cytotoxic activities of arylpropyl sulfonamides. Moreover, the introduction of small hydrophobic groups in the phenyl ring and sulfonamide group could increase biological activity.

2- or 6-(1-Azidoalkyl)-5,8-Dimethoxy-1,4-Napyhthoquinone: Synthesis, Evaluation of Cytotoxic Activity, Antitumor Activity and Inhibitory Effect on DNA Topoisomerase-I

  • Chae, Gyu-Han;Song, Gyu-Yong;Kim, Yong;Cho, Hoon;Sok, Dai-Eun;Ahn, Byung-Zun
    • Archives of Pharmacal Research
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    • v.22 no.5
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    • pp.507-514
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    • 1999
  • 6-(1-azidoalkyl)-DMNQ derivatives compared to 2-(1-azidoalkyl)-DMNQ isomers, exhibited higher cytotoxic activity against L1210 mouse leukemia cells and stronger inhibition of DNA topoisomerase-I (TOPO-I), suggesting involvement of steric hindrance. However, similar antitumor activity against mice bearing S-180 cell was shown by 2-an 6-(1-azidoalkyl)-DMNQ derivatives.

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A Cytotoxic Monoterpene-Neolignan from the Stem Bark of Magnolia officinalis

  • Youn, Ui-Joung;Lee, Ik-Soo;Chen, Quan Cheng;Na, Min-Kyun;Jung, Hyun-Ju;Lee, Sang-Myung;Choi, Jae-Sue;Woo, Mi-Hee;Bae, Ki-Hwan;Min, Byung-Sun
    • Natural Product Sciences
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    • v.17 no.2
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    • pp.95-99
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    • 2011
  • A monoterpene-neolignan, piperitylmagnolol (1), was isolated from the stem bark of Magnolia officinalis, together with syringaresinol (2), caffeic acid (3), and sinapaldehyde (4). The isolated compounds were established on the basis of spectroscopic and physicochemical analyses including 1D- and 2D-NMR techniques, as well as on comparing the spectral data with those in the literature and of authentic samples. Compounds 1 - 4 were tested for their cytotoxic activity against the HeLa, K562, A549, and HCT116 cancer cell lines in vitro. Of the isolates, piperitylmagnolol (1) exhibited cytotoxic activity against the tested cancer cell lines with $IC_{50}$ values of 7.7 - 9.5 ${\mu}g/ml$.

Effect of Controlled Atmosphere Storage on the Antioxidative and Cytotoxic Activities of Fresh and Red Ginseng (CA저장이 수삼 및 대삼의 항산화 작용과 항암작용에 미치는 영향)

  • 전병선;정나미
    • Journal of Ginseng Research
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    • v.20 no.3
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    • pp.262-268
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    • 1996
  • 4-year-old fresh ginseng was stored for 12 weeks at 4$^{\circ}C$ under the CA storage and samples were withdrawn after every 1, 2, 3, 4, 6, 8 and 12 weeks for processing of red ginseng. Antloxidative and cytotoxic activities of steamed red ginseng for the quality evaluation are summarized as follows: Reducible activity of water extract to 1, 1-dipenyl-2-picryl hydrazyl increased with increasing storage period. Antioxldative activity of red ginseng did not change in petroleum ether fraction, while it had a tendency to increase In the fractions of ethyl ether and ethyl acetate with increasing storage period. in contrast to fresh ginseng, malonaldehyde formation In heparin mlcrosome of red ginseng processed from fresh ginseng stored In CO2:O2:Nl (6:4:90) with a 0.5% DF-100 immersion condition decreased but was not changed significantly by the period of storage. Cytotoxic activity against cancer cell at a 40 mg/ml concentration of red ginseng slightly increased with an increase in storage period but no effect was observed at the concentration less than 10 mg/ml.

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Pharmacological profiles of Holarhena antidysenterica (L.) Wall bark

  • Rahman, Shafiur;Ali, Eunus;Haque, Rubyat
    • Oriental Pharmacy and Experimental Medicine
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    • v.7 no.2
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    • pp.157-161
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    • 2007
  • We undertook the present study to evaluate different pharmacological as antioxidant, antibacterial and cytotoxic activities of the crude ethanolic extract of the stem bark of Holarhena antidysenterica (Family: Apocynaceae). The antioxidant property of the extract was assessed by 1,1-diphenyl-2-picryl hydrazyl free radical scavenging assay. The extract showed antioxidant activity ($IC_{50}$ about ${\sim}08$ ${\mu}g/ml$), which was comparable to standard drug ascorbic acid ($IC_{50}$ about ${\sim}10$ ${\mu}g/ml$). The extract showed a broad spectrum of antibacterial activity against all tested gram positive and gram negative bacteria most prominent against Enterococci, Staphylococcus pyogenase and Shigella sonnie. And the zones of inhibitions were ranging from 10 - 21 mm for all the tested bacteria. Its cytotoxic property was evaluated by brine shrimp lethality bioassay. The extract showed significant lethality and the $LC_{50}$, $LC_{90}$ values were 80 ${\mu}g/ml$, 320 ${\mu}g/ml$ respectively. The results tend to suggest that the extract might possess chemical constituent(s) that are responsible for antioxidant, antibacterial and cytotoxic activities.

Potentiation of TRAIL killing activity by multimerization through isoleucine zipper hexamerization motif

  • Han, Ji Hye;Moon, Ae Ran;Chang, Jeong Hwan;Bae, Jeehyeon;Choi, Jin Myung;Lee, Sung Haeng;Kim, Tae-Hyoung
    • BMB Reports
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    • v.49 no.5
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    • pp.282-287
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    • 2016
  • Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) is a homo-trimeric cytotoxic ligand. Several studies have demonstrated that incorporation of artificial trimerization motifs into the TRAIL protein leads to the enhancement of biological activity. Here, we show that linkage of the isoleucine zipper hexamerization motif to the N-terminus of TRAIL, referred as ILz(6):TRAIL, leads to multimerization of its trimeric form, which has higher cytotoxic activity compared to its native state. Size exclusion chromatography of ILz(6):TRAIL revealed possible existence of various forms such as trimeric, hexameric, and multimeric (possibly containing one-, two-, and multi-units of trimeric TRAIL, respectively). Increased number of multimerized ILz(6):TRAIL units corresponded with enhanced cytotoxic activity. Further, a high degree of ILz(6):TRAIL multimerization triggered rapid signaling events such as activation of caspases, tBid generation, and chromatin condensation. Taken together, these results indicate that multimerization of TRAIL significantly enhances its cytotoxic activity.

Modulation of NAD(P)H:Quinone Oxidoreductase (NQO1) Activity Mediated by 5-Arylamino-2-methyl -4,7-dioxobenzothiazoles and their Cytotoxic Potential

  • Ryu, Chung-Kyu;Jeong, Hyeh-Jean;Lee, Sang-Kook;Kang, Hye-Young;Ko, Kyung-Min;Sun, Yang-Jung;Song, Eun-Ha;Hur, Yeon-Hoe;Lee, Chong-Ock
    • Archives of Pharmacal Research
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    • v.23 no.6
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    • pp.554-558
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    • 2000
  • Synthesized 5-arylamino-2-methyl-4,7-dioxobenzothiazoles 3a-3o were evaluated for modulation of NAD(P)H: quinone oxidoreductase (NQOl) activity with the cytosolic fractions derived from cultured human lung cancer cells and their cytotoxicity in cultured several human solid cancer cell lines. The 4,7-dioxobenzothiazoles affected the reduction potential by NQOl activity and showed a potent cytotoxic activity against human cancer cell lines. The tested compounds 3a, 3b, 3g, 3h, 3n and 3o were considered as more potent cytotoxic agents, and comparable modulators of NQOl activity.

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2,3-Dibenzylbutyrolactones and 1,2,3,4-Tetrahydro-2-Naphthoic acid ${\gamma}-Lactones$: Structure and Activity Relationship in Cyto-toxic Activity

  • Kim, Yong;You, Young-Jae;Nam, Nguyen-Hai;Ahn, Byung-Zun
    • Archives of Pharmacal Research
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    • v.25 no.3
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    • pp.240-249
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    • 2002
  • Dibenzyl-g-butyrolactone and 1,2,3,4-tetrahydro-2-naphthoic acid $\gamma$-lactone (TNL) derivatives were synthesized and evaluated for cytotoxic activity against some cancer cell lines. It was found that TNL derivatives with a shorter distance between C-4 in ring A and C'-2 in ring C were more cytotoxic, while dibenzyl-${\gamma}$-butyrolactones with a longer one were nearly inactive. In TNL series, presence of 3,4-dioxy group in ring A and 2-methoxy group in ring C was essential for the enhancement of the activity.

The Study on the Effective Components in Various Parts of Luffa cylindrica and Development for Removal of the Flesh from its Fruits(III) -Cytotoxic Activity of Leaf, Stem and Seed Extracts against L1210 Cells and Antibacterial Activity against Streptococcus mutans OMZ176- (수세미오이의 부위별 유효성분 조사 및 사과락의 육질제거에 관한 연구(III) -잎, 줄기 및 종자의 L1210세포에 대한 세포독성과 충치균에 대한 항균작용-)

  • Bae, Ki-Hwan;Chi, Jong-Myung;Chang, Ki-Woon
    • Korean Journal of Pharmacognosy
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    • v.22 no.4
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    • pp.249-251
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    • 1991
  • The cytotoxic and antibacterial activities of the leaf, the stem and the seed extracts of Luffa cylindrica were evaluated against L1210 cells and Streptococcus mutans OMZ176, respectively. Among hexane, ether, butanol and water fractions, the ether fraction demonstrated the most potent cytotoxic activity, and the $ED_{50}$ values of the ether extract from the leaf, the stem and the seed were 3.5, 3.7 and $13.7{\mu}g/ml$, respectively. Meanwhile, the other fractions showed negligible effect. Separately, it was found that the antibacterial activity of the respective fraction from three parts was insignificant.

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