• Title/Summary/Keyword: cytotoxic compound

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Bioactive Constituents from the n-Butanolic Fraction of Aruncus dioicus var. kamtschaticus

  • Vo, Quoc Hung;Nguyen, Phi Hung;Zhao, Bing Tian;Thi, Yen Nguyen;Nguyen, Duc Hung;Kim, Won Il;Seo, U Min;Min, Byung Sun;Woo, Mi Hee
    • Natural Product Sciences
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    • v.20 no.4
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    • pp.274-280
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    • 2014
  • Six compounds were isolated from the n-BuOH fraction of the aerial parts of Aruncus dioicus var. kamtschaticus including: sambunigrin (1), prunasin (2), aruncide A (3), aruncide C (4), 1-O-caffeoyl-${\beta}$-D-glucopyranose (5), and caffeic acid (6). Their structures were confirmed by comparing the spectral data with those reported in the literature. The isolated compounds (1 - 6) were then examined for their cytotoxic effects towards MCF-7, HL-60, and HeLa cancer cell lines, as well as their DPPH radical scavenging activity. The results indicated that compound 4 possessed the strongest inhibitory effect toward HeLa cell line with $IC_{50}$ value of $5.38{\pm}0.92{\mu}M$. Compound 3 possessed selective cytotoxic activity on HL-60 cells with $IC_{50}$ value of $6.27{\pm}0.17{\mu}M$, compound 5 was found as the best in inhibiting proliferation with $IC_{50}$ value of $2.25{\pm}0.09{\mu}M$, and the other compounds showed significant inhibition with $IC_{50}$ values ranging from 6.10 to $11.27{\mu}M$. Compound 5 also displayed the strongest cytotoxic effect toward MCF-7 cell line ($IC_{50}$ $4.32{\pm}0.15{\mu}M$). Both 5 and 6 demonstrated strong radical scavenging activity ($IC_{50}$ $6.87{\pm}0.03$ and $4.33{\pm}0.22{\mu}M$, respectively). Compounds 1 and 5 were isolated for the first time from this plant.

Antimicrobial and Cytotoxic Activity of Di-(2-ethylhexyl) Phthalate and Anhydrosophoradiol-3-acetate Isolated from Calotropis gigantea (Linn.) Flower

  • Habib, M. Rowshanul;Karim, M. Rezaul
    • Mycobiology
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    • v.37 no.1
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    • pp.31-36
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    • 2009
  • A phytochemical study on the flower of Calotropis gigantea (Linn.) using silica gel column chromatography and preparative thin layer chromatography, led to the first time isolation of Di-(2-ethylhexyl) phthalate (compound 1) and anhydrosophoradiol-3-acetate (compound 2). The structures of these compounds were confirmed by spectroscopic analyses (IR, HRTOFMS and NMR). The antibacterial and antifungal activities of ethyl acetate extract, compound 1 and compound 2 were measured using the disc diffusion method. Ethyl acetate extract and compound 1 presented better results than compound 2. The minimum inhibitory concentrations (MICs) of the extract and compounds were found to be in the range of $16{\sim}128{\mu}g/ml$. The cytotoxicity ($LC_{50}$) against brine shrimp nauplii (Artemia salina) were also evaluated and found to be 14.61 ${\mu}g/ml$ for ethyl acetate, 9.19 ${\mu}g/ml$ for compound 1 and 15.55 ${\mu}g/ml$ for compound 2.

New Cytotoxic Benzopyrans from the Leaves of Mallotus apelta

  • Kiem Phan Van;Dang Nguyen Hai;Bao Ha Viet;Huong Hoang Thanh;Minh Chau Van;Huong Le Mai;Lee Jung Joon;Kim Young Ho
    • Archives of Pharmacal Research
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    • v.28 no.10
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    • pp.1131-1134
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    • 2005
  • Two new benzopyrans 6-[1'-oxo-3'(R)-hydroxy-butyl]-5,7 -dimethoxy-2,2-dimethyl-2H-1-ben-zopyran (1) and 6-[1'-oxo-3'(R)-methoxy-butyl]-5,7 -dimethoxy-2,2-dimethyl-2H-1-benzopyran (2) were isolated from the leaves of Mallotus apelta Muell.-Arg., (Euphorbiaceae). Their chemical structures were elucidated by spectroscopic analyses, especially by 1D-, 2D-NMR and MS spectra. Compound 1 was found to have strong cytotoxic effect against two human cancer cell lines as human hepatocellular carcinoma (Hep-2, $IC_{50}\;:\;0.49\;{\mu}g/mL$) and rhabdosarcoma (RD, $IC_{50}\;:\;0.54\;{\mu}g/mL$), while compound 2 showed moderate activity against Hep-2 cell line ($IC_{50}\;:\;4.22\;{\mu}g/mL$) by in vitro assay.

Bioassay-guided Isolation of Deoxypodophyllotoxin, the Cytotoxic Constituent of Juniperus chinensis

  • Ali, A.M.;Intan-Safinar, I.;Mackeen, M.M.;El-Sharkawy, S.H.;Takahata, K.;Kanzaki, H.;Kawazu, K.
    • Natural Product Sciences
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    • v.4 no.3
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    • pp.180-183
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    • 1998
  • The ethanol extract from the leaves of Juniperus chinensis was found to be cytotoxic towards HeLa cells. Bioassay-guided fractionation of the EtOAc soluble faction directed by the microtitration cytotoxic assay revealed that the cytotoxic compound was deoxypodophyllotoxin. All the tumour cell lines tested (KU8112F-chronic mylogeneous leukemia, TK 10-renal carcinoma, UACC 62-melanoma and CEM-SS-T-lymphoblastic leukemia) were found to be susceptible to deoxypodophyllotoxin, however, the minimum effective concentration (MEC) required to reduce the cell population by 100 percent was different between cell lines.

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Bioactive Ginseng Yogurts Fermented with Bifidobacteria: The Transformation of Ginsenosides to Compound K

  • Kim, Na-Young;Han, Myung-Joo
    • Food Quality and Culture
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    • v.1 no.1
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    • pp.18-21
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    • 2007
  • The objective of this study was to prepare bioactive ginseng yogurts containing compound K, which is transformed from ginsenosides, and to investigate the compound's cytotoxicity against tumor cells. Milk containing ginseng was fermented by Bifidobacteria KK-I and KK-2, and their activities for transforming ginsenosides to compound K were measured. Among the tested concentrations of ginseng in the milk, compound K was effectively produced in the 3% and 6% ginseng yogurts fermented for 48 hrs. These fermented ginseng yogurts were extracted with BuOH, and their cytotoxicities against tumor cells were examined. The BuOH extract of the yogurt made from the 3% ginseng milk showed cytotoxic activity against P388 and HeLa tumor cells. However, the nonfermented ginseng milk did not exhibit cytotoxicity against these cells. Therefore, we deem that the ginseng yogurt, which contained compound K, could be developed as a potential fermented drink product.

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Biotransformation of Ginseng Extract to Cytotoxic Compound K and Ginsenoside $Rh_2$ by Human Intestinal Bacteria

  • Bae, Eun-Ah;Choo, Min-Kyung;Lee, Young-Churl;Kim, Dong-Hyun
    • Natural Product Sciences
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    • v.10 no.6
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    • pp.347-352
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    • 2004
  • When saponin extracts of dried ginseng and red ginseng were anaerobically incubated with human intestinal microflora, these extracts were metabolized to compound K and ginsenoside $Rh_2$, respectively. However, when these extracts were incubated with commercial lactic acid bacteria, these did not metabolize these ginsenosides to compound K or ginsenoside $Rh_2$. Among some intestinal bacteria isolated from human feces, Bacteroides C-35 and C-36 transformed these saponin extracts to compound K and ginsenoside $Rh_2$, respectively. These bacteria also transformed water extracts of dried ginseng and red ginseng to compound K and ginsenoside $Rh_2$, respectively, similarly with that of the saponin extracts. Among transformed ginsenosides, compound K and 20(S)-ginsenoside $Rh_2$ exhibited the most potent cyotoxicity against tumor cells.

Cytotoxic Activity of 13(E)-Labd-13-ene-8$\alpha$, 15-diol

  • Lim Jin A;Kwang Jung Sook;Yu Byung Soo;Baek Seung Hwa
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.18 no.4
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    • pp.1169-1172
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    • 2004
  • The cytotoxic activity of 13(E)-labd-13-ene-8α, 15-diol (1) was evaluated against tumor cell lines. A comparison of IC/sub 50/ values of this compound in cancer cell lines showed that their susceptibility to this compound decreased in the following order: P388>B16{F10>MDA-MB-231>A549>KB>SNU-C4 by the MTT method. 13(E}-Labd-13-ene-8α, 15-diol (1) was the most effective growth inhibitor of P388 murine leukaemia cell lines, producing approximately 8.3㎍/mL of IC/sub 50/ in the MTT method.

2,4-cis- and trans-isoannonacin: Cytotoxic Ketolactone Annonaceous Acetogenins from the Seeds of Asimina triloba (Asimina triloba 씨앗으로부터 세포독성 Annonaceous Acetogenin으로서의 2,4-cis- 및 trans-isoannonacin)

  • Kim, Dal-Hwan;Jung, Soon-Ja;Kim, Chong-Won;Woo, Mi-Hee
    • Korean Journal of Pharmacognosy
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    • v.29 no.4
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    • pp.331-337
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    • 1998
  • Most Annonaceous acetogenins are potently bioactive and offer exciting potential as new antitumor, pesticidal and other bioactivites. The major mode of action of the acetogenin is inhibition of electron transport in the mitochodria. Two known cytotoxic ketolactone Annonaceous acetogenins, (2,4-cis)-isoannonacin (compound 1) and (2,4-trans)-isoannonacin (compound 2), have been isolated from Asimina triloba (Annonaceae) by bioactivity directed fractionation. The structures were characterized on the basis of chemical and spectral data. Compounds 1 and 2, which are known but are first isolated from the seeds of this species, were ob-tained. In brine shrimp lethality test (BST), 1 and 2 exhibited cytotoxicity.

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Isolation and Properties of Antitumor Antibiotic YS-1649 from Penicillium sp. strain 1649

  • BOO-kIL PARK;YOO, SEONG-JAE
    • Journal of Microbiology and Biotechnology
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    • v.5 no.1
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    • pp.31-35
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    • 1995
  • An antitumor antibiotic named YS-1649 was isolated from the culture filtrate of a newly isolated fungus identified as Penicillium sp.. The fermentation yield reached about 40 mg per liter of the broth. YS-1649, a $\gamma$-Iactone - structured antibiotic, has the molecular fomular of $C_7H_6O_4$, Its structure was determined to be patulin by spectral analysis. It is active against some bacteria and showed cytotoxic effect on the proliferation of human breast cancer cell line, MCF-7, at concentrations of more than 0.048 $mu g/ml$. This compound also showed strong cytotoxic effect on the proliferation of human cancer cell lines, A549 and ACHN.

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Cytotoxic Constituents of Pilea mongolica

  • Kwon, Hak-Cheol;Lee, Kang-Ro;Zee, Ok-Pyo
    • Archives of Pharmacal Research
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    • v.20 no.2
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    • pp.180-183
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    • 1997
  • Bioassay-guided fractionation of the aerial parts of Pilea mongolica(Urticaceae) afforded two cytotoxic triterpenoids, epi-oleanolic acid (I) and oxo-oleanolic acid (II). The structures of the compounds were confirmed by spectral and synthetic evidences. Compound I and compound II exhibited cytotoxicity against cultured human tumor cell lines, A549 (non small cell lung adenocarcinoma), SK-OV-3 (ovarian), SK-MEL-2 (skin melanoma), XF498 (CNS) and HCT15 (colon) with $ED_{50}$ values of $3.2-8.1{\mu}g/ml$ and $0.7-6.8 {\mu}g/ml$, respectively.

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