• Title/Summary/Keyword: cytotoxic against L1210

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Isolation and Characterization of Antitumor Agents from Dictamnus albus

  • Kim, Se-Won;Yeo, Woon-Hyung;Ko, Young-Su;Kim, Si-Kwan
    • Korean Journal of Pharmacognosy
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    • v.28 no.4
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    • pp.209-214
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    • 1997
  • This study was carried out to find new antitumor agents from plant resource. Three cytotoxic agents were isolated from the root of Dictamnus albus by hexane extraction, silica gel column chromatography and HPLC. They were identified to be dictamnine $(C_{12}H_9NO_2)$, preskimmianine $(C_{17}H_{21}NO_4)$ and fraxinellone $(C_{14}H_{16}O_3)$ on the basis of spectroscopic evidences. In this study, it was newly found that these compounds possess a cytotoxic activity against lung lymphoma L1210 cell line. Among them. Preskimmianine was the most potent against the lymphoma L1210 with a $IC_{50}$ of $3.125\;{\mu}g/ml\;(10.3\;{\mu}M)$. Toxicity of preskimmianine against normal Iymphocyte was observed at the concentration of $50\;{\mu}g/ml\;(165\;{mu}M)$. These results support the pharmacological role of D. albus, a herb known as Paeksun in Korea and used as an anticancer agent in folk medicine.

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Synthesis and Evaluation of Antitumor Activity of 2- and 6-[(1,3- Benzothiazol-2-yl)aminomethyl]-5,8-dimethoxy-1,4-naphthoquinone Derivatives

  • Chung, Yong-Seog;Shin, Young-Kook;Zhan, Chang-Guo;Lee, Sung-Duck;Cho, Hoon
    • Archives of Pharmacal Research
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    • v.27 no.9
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    • pp.893-900
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    • 2004
  • 2- or 6-Substituted BZT-N derivatives were synthesized, and their cytotoxic activity against can-cer L1210 and SNU-1 cells was examined. The antitumor action was also assessed in mice bearing S-180 cells in peritoneal cavity. In a comparison, it was found that 6-substituted BZT-N derivatives exhibited higher potencies in both bioactivities than 2-substituted BZT-N derivatives against L1210 cells in in vitro and S-180 in vitro tests exception of compound 36. Interestingly, it was observed that 2-substituted compound 36, which has methyl group at RI position, exhib-ited a better antitumor activity than 6-substituted compounds against L1210 and SNU-1 in vitro. The EDso value of 2-substituted compound 36 against L1210 was found to be comparable to the EDso value of adriamycin and was even better against the solid cancer cell line SNU-1. It was also observed that 2-substituted compound 36 showed better antitumor activity in mice bearing S-180 cells in the peritoneal cavity. The T/C (%) value of 2-substituted compound 36 was simi-lar to that of adriamycin. Quantitative structure-activity relationship (QSAR) tests reveal that the experimental E $D_{50}$ values against SNU-1 closely correlate with both the calculated HOMO ener-gies ( $E_{HOMO}$) and the measured H-NMR chemical shift of 3-H ($\delta$$_{H}$). The results suggests that a compound having higher $E_{HOMO}$ and $\delta$$_{H}$ values usually should have a lower E $D_{50}$ (SNU-1) value.lue.lue.lue.

2-(1-Hydroxyiminoalkyl)-1,4-dimethoxy-9,10-anthraquinones: Synthesis and Evaluation of Cytotoxicity

  • Tam, Mai-Ngoc;Nam, Nguyen-Hai;Jin, Guang-Zhu;Ahn, Byung-Zun
    • Archives of Pharmacal Research
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    • v.23 no.4
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    • pp.283-287
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    • 2000
  • A series of 2-(1-hydroxyiminoalkyl)-1,4-dimethoxy-9,10-anthraquinones (oximes) was synthesized and evaluated for cytotoxicity against L1210 cells and A549 cells. These oximes showed a greater cytotoxic activity compared to those of 2-(1-hyd roxyalkyl)-1,4-dimethoxy-9,10-anthraquinones as the hydroxyalkyl bioisosteres. The enhanced cytotoxiciy assumed to be due to the improved water solubility of the hydroxyimino group. Moreover, it was found that the cytotoxicity of the oximes decreased with elongation of alkyl groups at the side chain. All of the synthesized compounds showed higher cytotoxicity against L1210 cells than A549 cells.

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Cytotoxic Compounds from the Roots of Pulsatilla koreana

  • Cuong, To Dao;Hung, Tran Manh;Lee, Mi-Kyoung;Thao, Nguyen Thi Phuong;Jang, Han-Su;Min, Byung-Sun
    • Natural Product Sciences
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    • v.15 no.4
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    • pp.250-255
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    • 2009
  • Seven compounds including hederagenin 3-[(O-${\alpha}$-L-rhamnopyranosyl-($1{\rightarrow}2$)-${\alpha}$-L-arabinopyranosyl) (1), $3{\beta}$-[(O-${\alpha}$-L-rhamnopyranosyl-($1{\rightarrow}2$)-${\alpha}$-L-arabinopyranosyl)oxy]olean-12-en-28-oic acid (2), caffeic acid methyl ester (3), ferulic acid (4), orebiusin A (5), latifonicinin C (6) and 5-(hydroxymethyl)-2-furfuraldehyde (7) were isolated from the ethyl acetate fraction of the roots of Pulsatilla koreana. Their chemical structures were established based on physicochemical and spectroscopic data analyses. All isolates were investigated for their cytotoxic activity against cancer cell lines. Among them, compound 1 showed inhibitory activity against A549, COLO 205, and L1210 cancer cell lines with $IC_{50}$ values of 15.8, 36.5, and 22.8 ${\mu}g$/mL, respectively.

Cytotoxic Effect of Aromatic and Aliphatic Compounds Produced by Streptomyces sp. Isolated in Korea (한국 Streptomyces SP.로부터 분리한 방향족 화합물과 지질 화합물의 세포독성 연구)

  • Shin, Suck-Woo;Ryeom, Kon
    • Biomolecules & Therapeutics
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    • v.5 no.2
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    • pp.215-221
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    • 1997
  • In an effort to screen new selective antitumor agents from the broth of soil microorganism, cytotoxicity oriented screening was performed against tumor cells and 3 compounds (Compound 1, 2 and 3) were isolated from Sreptomyces parvullus ISP 5048 and their chemical structures were determined. Among these compounds, Compound 2 showed the highest cytotoxicity against P388Dl and L1210. While the $IC_{50}$/ values of compound 2 against P388Dl and L1210 were 0.073$\mu$g/ml and 0.07$\mu$g/ml, respectively, and the $IC_{50}$/ value of Compound 3 was 0.17$\mu$g/ml against human lung cancer cells, A549, the cytotoxicity of Compound 2 and 3 against normal cell line, Vero E6 cell was about 4- and 8-fold lower than that of adriamycin. Based on the chemical analysis data, Compound 3 was octacosamicine A, a known antibiotic, which was reported by Dobasih et al. (1988). Taken together the results demonstrated that Compound 2 and Compound 3 has the possibility to be developed as antitumor agent because of its potent cytotoxicity as well as high selectivity against various cancer cell lines.

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Cytotoxic Anthraquinones and Stilbenes from Reynoutria sachalinensis (Fr. Schm.) Nakai

  • Jin, Wenyi;Na, Min-Kyun;Song, Gyu-Yong;Lee, Young-Mi;Bae, Ki-Hwan
    • Korean Journal of Medicinal Crop Science
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    • v.13 no.2
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    • pp.80-84
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    • 2005
  • Five known anthraquinones, physcion (1), I-O-methylemodin (2), emodin (3), $physcion-8-O-{\beta},-D-glucopyranoside$ (5), $emodin-8-O-{\beta},-D-glucopyranoside$ (6) and two known stilbenes, trans-resveratrol (4), $trans-resveratrol-3-O-{\beta},-D-glucopyranoside$ (7) were isolated from MeOH extract of Reynoutria sachalinensis (Polygonaceae). All structures were unambiguously established by 1D and 2D NMR and MS data and the compounds were evaluated for their cytotoxicity against L1210, HL-60, BI6F10 tumor cell lines in MTT assay. Among the compounds, trans-resveratrol (4) exhibited significant cytotoxic activity with $IC_{50}$ values of 9.2, 6.7 and $9.8\;{\mu}g/ml$, against the test cell lines respectively, but compounds 1-3 exhibited the moderate cytotoxic activity.

Antiproliferative and Antioxidative Activities of Methanol Extracts of Echinacea angustifolia (Echinacea angustifolia 메탄올 추출물의 암세포 증식억제 및 항산화 효과)

  • Lee Joon-Kyoung;Koo Seung-Ja
    • Korean journal of food and cookery science
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    • v.21 no.3 s.87
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    • pp.311-318
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    • 2005
  • Echinacea, also blown as the purple coneflower, is a herbal medicine that has been used for centuries, customarily as a treatment for the common cold, coughs, bronchitis, upper respiratory infections, and some inflammatory conditions. We investigated the effects of methanol extracts of Echinacea angustifolia on the cytotoxicity against cancer cells $(HepG_2,\;3LL,\;HL60,\;L1210)$ and antioxidative activity. From the test results, each part of Echinaceashowed a cytotoxic effect against the cancer cell lines, and this cytotoxic effect increased with increasing sample concentration. At 1.0 mg/mL concentration the relative cytotoxic activities of the flower bud, leaf, stern and root parts were $90.5\%,\;52.7\%,\;37.1\%\;and\;19.2\%$, respectively, in $HepG_2$ cells, and $75.5\%,\;93.3\%,\;81.2\%,\;and\;75.1\%$ respectively, in HL60 cells, as evaluated by MTT assay. $IC_{50}(50\%\;inhibitory\;concentration)$ of the methanol extracts of the Echinacea flower bud was 0.214 mg/mL on /$HepG_2$ cells, and that of the Echinacea leaf and root was 0.166 mg/mL and 0.210 mg/mL, respectively, on HL60 cells. After /$HepG_2$ cells were incubated for 6 days at $37^{\circ}C$ with various concentrations of each part, the cell number increased while the inhibition rate on the /$HepG_2$ cell growth decreased. The antioxidative activities of the flower bud, leaf, stem and root parts were $59.0\%$ (0.75 mg/mL), $80.76\%$ (0.5 mg/mL), $95.5\%$ (0.25mg/mL) and $98.15\%$ (0.25 mg/mL), respectively, as evaluated by electron donating ability. These results indicated that Echinacea angustifolia has strong anticancer and antioxidative effects in vitro.

Effect of Platycodon grandiflorum DC Extract on the Growth of Cancer Cell Lines (도라지(Platycodon grandiflorum DC) 추출 성분의 암세포 증식 억제효과)

  • Lee, Ji-Young;Hwang, Woo-Ik;Lim, Seung-Taik
    • Korean Journal of Food Science and Technology
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    • v.30 no.1
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    • pp.13-21
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    • 1998
  • To investigate the cytotoxic effect of Platycodon grandiflorum DC, petroleum ether extract of Platycodon grandiflorum DC was partially purified by a silica gel column chromatography. Among several fractions, fraction D which was obtained under the elution with a 7:3 mixture of petroleum ether and ethyl ether, showed patent cytotoxicity against mouse leukemia cell line (L1210), human rectum cancer cell line (HRT-18) and human colon cancer cell lint (HCT-48).

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Cytotoxic Constituents from the Roots of Bryonia alba L.

  • Baek, Nam-In;Lee, Dong-Wook;Lee, You-Hui;Kim, Shin-Il;Aprikian, Goorgen V.
    • Natural Product Sciences
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    • v.1 no.1
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    • pp.43-49
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    • 1995
  • Two cucurbitane-compounds were isolated from the roots of Bryonia alba L. and the chemical structures were established as 19-norlanost-5-ene-3,1l,22-trione-$2{\beta}$, $16{\alpha}$,$20{\beta}$,25-tetrahydroxy-9-methyl (23,24-dihydrocucurbitacin D) and 2-O-${\alpha}$-D-glucopyranosyl 19-norlanost-5-ene-3,11,22-trione-$2{\beta}$,$16{\alpha}$,$20{\beta}$,25-tetrahydroxy-9-methyl (arvenin IV), respectively, on the basis of chemical and spectral methods. Both of the compounds showed cytotoxic activity against cancer cell lines, A549, SK-MEL-2, COLO 205 and L1210.

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Synthesis and Antitumor Activity of 3'-hydroxydaunorubicin and 3'-hydroxydoxorubicin Derivatives Substituted with 4'-fluorine or 4'-azide in Sugar Moiety (당부분에서 4'-플루오린 또는 4'-아자이드로 치환된 3'-히드록시다우노루비신과 3'-히드록시독소루비신 유도체의 합성과 항암활성)

  • Ok, Kwang-Dae;Park, Jeong-Bae;Kim, Moon-Sung;Jung, Dong-Yoon;Yang, Junn-Ick
    • YAKHAK HOEJI
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    • v.40 no.2
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    • pp.117-125
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    • 1996
  • 3'-Deamino-3-hydroxy-4'-fluoro- or 3'-deamino-3'-hydroxy-4'-azido-daunorubicin(6,8) and -doxorubicin(7,9) have been synthesized, respectively. Compounds 7,8 and 9 were mo re cytotoxic than daunorubicin(1) and doxorubicin(2) against L1210 murine leukemic cell in vitro. When administered intraperitoneally for 9 days starting 1 day after tumor inoculation, compounds 7(T/C 605%) and 9(T/C 488%) showed significant antitumor activity for ip-inoculuated L1210 murine leukemia at wide range of doses.

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