• 제목/요약/키워드: $IC_{50}$ values

검색결과 1,077건 처리시간 0.026초

Cytotoxic Effect of Hexavalent Chromium on C6 Glioma Cells

  • Suk Seung-Han
    • 대한의생명과학회지
    • /
    • 제12권3호
    • /
    • pp.261-265
    • /
    • 2006
  • Toxic effect of Hexavalent chromium $(CrO_3)$ on various cells and organs has been well recognized. However, the mechanism and degree of cytotoxicity of $CrO_3$ remain unclear. This study was performed to examine the cytotoxicity of $CrO_3$ on $C_6$ glioma cells by measuring cell viability. The XTT assay, one of the sensitive methods to determine the cell viability, was taken to examine the viability of glioma cells treated with $CrO_3$. In this study, not only decreased the number of glioma cells but morphologic changes of them were noted and cell viability decreased in a time and dose-dependent manner after treated with various concentrations of $CrO_3$ for 48hours. $IC_{90}\;and\;IC_{50}$ values in XTT assay were determined at $25{\mu}M\;and\;55{\mu}M$ $CrO_3$, respectively. These results suggest that Hexavalent chromium has a highly cytotoxic effect and has a time and dose-dependent cytotoxicity on $C_6$ glioma cells.

  • PDF

Cap-Modified Hydroxamate Analogues as Histone Deacetylases Inhibitors and Antitumor Agents

  • Zhang, Qing-Wei;Feng, Juan;Li, Jian-Qi
    • Bulletin of the Korean Chemical Society
    • /
    • 제35권1호
    • /
    • pp.129-134
    • /
    • 2014
  • Two series of SAHA-liked hydroxamate analogues were designed, synthesized and evaluated for their biological activities against nuclear HDACs. Compounds of Series I were found to be very effective inhibitors of cancer cell growth in the PC-3, Hut78, K562 and Jurkat E6-1 cancer cell lines with mean $IC_{50}$ values from $0.54{\mu}M$ (Ic, Jurkat E6-1) to $7.73{\mu}M$ (Ib, K562), indicating that they are cell permeable and the benzimidazolyl-based ligands are flexible enough to occupy the binding site of HDAC.

In vitro Cytotoxicity of Sambutoxin

  • Kim, Jin-Cheol;Park, Jeng-Bae;Kim, Gye-Won;Kim, Won-Bae;Lee, Yin-Won
    • Applied Biological Chemistry
    • /
    • 제41권4호
    • /
    • pp.273-274
    • /
    • 1998
  • In vitro cytotoxicity of sambutoxin was measured by using various human and murine tumor cells and $IC_{50}$ values of sambutoxin ranged from 46.2 to 1,425.6 ng/ml.

  • PDF

Revision of Structures of Flavanoids from Scutellaria indica and Their Protein Tyrosine Phosphatase 1B Inhibitory Activity

  • Min, Byung-Sun
    • Natural Product Sciences
    • /
    • 제12권4호
    • /
    • pp.205-209
    • /
    • 2006
  • The structures of flavonoids, 2(S)-5,7-dihydroxy-8,2'-dimethoxyflavanone (1), wogonin (2), 2(S)-5,7, 2'-trihydroxy-8-methoxyflavanone (3), and 2(S)-5,2',5'-trihydroxy-7,8-dimethoxyflavanone (4), isolated from Scutellaria indica were revised on the basis of 2D NMR spectroscopy, including to gCOSY, gHSQC, and gHMBC. Compounds 1-4 were tested in vitro protein tyrosine phosphatase 1B (PTP1B) inhibitory activity. Compounds 2 and 4 exhibited weak PTP1B inhibitory activity with $IC_{50}$ values of 208 and $337{\mu}M$, respectively.

Inhibitory Constituents against HIV-1 Protease from Agastache rugosa

  • Min, Byung-Sun;Masao-Hattori;Lee, Hyeong-Kyu;Kim, Young-Ho
    • Archives of Pharmacal Research
    • /
    • 제22권1호
    • /
    • pp.75-77
    • /
    • 1999
  • Two diterpenoid compounds, agastanol (1) and agastaquinone (2), were isolated from the roots of Agastache rugosa (Labiatae). Compound 1 and 2 showed significant inhibitory effects against human immunodeficiency virus type 1 (HIV-1) protease activity with $IC_{50}$ values of 360 and $87{\mu}M$, respectively.

  • PDF

Antioxidative Constituents from Lycopus lucidus

  • Woo, Eun-Rhan;Piao, Mei-Shan
    • Archives of Pharmacal Research
    • /
    • 제27권2호
    • /
    • pp.173-176
    • /
    • 2004
  • Three phenolic compounds, rosmarinic acid (1), methyl rosmarinate (2), ethyl rosmarinate (3), and two flavonoids, luteolin (4), luteolin-7-O-$\beta$-D-glucuronide methyl ester (5) were isolated from the aerial part of Lycopus lucidus (Labiatae). Their structures were determined by chemical and spectral analysis. Compounds 1-5 exhibited potent antioxidative activity on the NBT superoxide scavenging assay. The $IC_{50}$ values for compounds 1-5 were 2.59, 1.42, 0.78, 2.83, and 3.05 $\mu\textrm{g}$/mL respectively. In addition, five compounds were isolated from this plant for the first time.

Anti-oxidant activities of the extracts from the herbs of Artemisia apiacea

  • Kim, Kyoung-Soon;Lee, Sang-Hyun;Lee, Yeon-Sil;Jung, Sang-Hoon;Park, You-Mie;Shin, Kuk-Hyun;Kim, Bak-Kwang
    • 대한약학회:학술대회논문집
    • /
    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
    • /
    • pp.288.2-288.2
    • /
    • 2003
  • The anti-oxidant activities of the various fractions from the herbs of Artemisia apiacea were investigated. The n-hexane and n-butanol fractions were found to cause significant free radical scavenging effects on DPPH, their scavenging potencies as indicated in IC50 values, being 230.1 and 183.7 mg/$m\ell$, respectively. (omitted)

  • PDF

Antioxidant Activities of Phenolic Derivatives from Dipsacus asper Wall. (II)

  • Hung, Tran Manh;Thuong, Phuong Thien;Youn, Ui-Joung;Zhang, Xin Feng;Min, Byung-Sun;Woo, Mi-Hee;Lee, Hyeong-Kyu;Bae, Ki-Hwan
    • Natural Product Sciences
    • /
    • 제14권2호
    • /
    • pp.107-112
    • /
    • 2008
  • The six phenolic compounds isolated from the root of Dipsacus asper, 3,4-di-O-caffeoylquinic acid (1), methyl 3,4-di-O-caffeoyl quinate (2), 3,5-di-O-caffeoylquinic acid (3), methyl 3,5-di-O-caffeoyl quinate (4), 4-5-di-O-caffeoylquinic acid (5), methyl 4,5-di-O-caffeoyl quinate (6) were continuously evaluated for their antioxidant activity using superoxide radical scavenging and AAPH-mediated (LDL) oxidation assay. The results demonstrated that compounds 1 - 6 had remarkable antioxidant activities with the $IC_50$ values ranging from 12.0 to $2.8{\mu}M$ in superoxide radical scavenging. They also inhibited AAPH-mediated low-density lipoprotein LDL oxidation by the generation of thiobarbituric acid reactive substances (TBARS) with $IC_50$ ranging from 6.7 to $8.7{\mu}M$.

Development of Selective Butyrylcholinesterase Inhibitors Using (R)-Lipoic Acid-Polyphenol Hybrid Molecules

  • Woo, Yeun-Ji;Lee, Bo-Hyun;Yeun, Go-Heum;Kim, Hyun-Ju;Ko, Jang-Myoun;Won, Moo-Ho;Lee, Bong-Ho;Park, Jeong-Ho
    • Bulletin of the Korean Chemical Society
    • /
    • 제32권spc8호
    • /
    • pp.2997-3002
    • /
    • 2011
  • A series of hybrid molecules between (R)-lipoic acid (ALA) and the acetylated or methylated polyphenol compounds were synthesized and their in vitro cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibition activities were checked. The $IC_{50}$ values of all hybrid molecules for a BuChE inhibition were lower than those of the single parent compounds. Specifically, ALA-acetyl protected caffeic acid (11, ALA-AcCA) was shown as an effective inhibitor of BuChE ($IC_{50}=0.5{\pm}0.2\;{\mu}M$) and also had a great selectivity for BuChE over AChE (more than 800 fold). Inhibition kinetic study indicated that 11 is a mixed inhibition type. Its binding affinity ($K_i$) value to BuChE is $1.52{\pm}0.18\;{\mu}M$.

돼지혈액으로부터 항고혈압물질의 분리 (Isolation of Angiotensin Converting Enzyme Inhibitors from Pig Blood)

  • 박은희;송경빈
    • Applied Biological Chemistry
    • /
    • 제40권1호
    • /
    • pp.39-42
    • /
    • 1997
  • 돼지혈액의 혈장으로부터 ACE 저해제들을 분리 정제하였다. 돼지 도축혈액을 먼저 혈액응고방지제를 첨가한후 원심분리에 의해 혈장과 혈구로 분리한 다음 혈장단백질을 최종농도 4% TCA로 침전시켰다. ACE 저해제들은 TCA 상등액과 혈장단백질 가수분해물로부터 한외여과, 겔여과크로마토그라피, 역상고속액체크로마토그라피 방법으로 분리되었는데 $IC_{50}4값들이 각각 $2\;{\mu}M,\;23\;{\mu}M$로 측정되었다.

  • PDF