• Title, Summary, Keyword: cytotoxic activity

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Antibacterial, cytotoxic and neuropharmacological activities of Cerbera odollam seeds

  • Ahmed, F;Amin, R;Shahid, IZ;Sobhani, MME
    • Oriental Pharmacy and Experimental Medicine
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    • v.8 no.4
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    • pp.323-328
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    • 2008
  • The MeOH extract of seeds of Cerbera odollam Gaertn. (Apocynaceae) was screened for its antibacterial, cytotoxic and neuropharmacological activities. The extract showed moderate anti-bacterial activity against Salmonella typhi, Streptococcus saprophyticus, and Streptococcus pyogenes. It exhibited high level cytotoxicity against brine shrimp ($LC_{50}$: $3\;{\mu}g/ml$). The extract potentiated pentobarbital induced sleeping time in mice which was further supported by the exploratory behavior test at dose of 25 mg/kg. The overall results tend to suggest the antibacterial, cytotoxic and CNS depressant activities of the extract.

Compounds from the Aerial Parts of Aceriphyllum rossii and Their Cytotoxic Activity

  • Tran, Thi Thu Trang;Nguyen, Thi Yen;Tran, Manh Hung;Weon, Kwon-Yeon;Woo, Mi Hee;Min, Byung Sun
    • Natural Product Sciences
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    • v.20 no.3
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    • pp.146-151
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    • 2014
  • The purification of the MeOH extracts from the aerial parts of Aceriphyllum rossii Engler (Saxifragaceae) using column chromatography furnished fourteen compounds (1 - 14). The chemical structures of the isolated compounds were determined using mainly nuclear magnetic resonance spectra and mass spectrometry. All the isolated compounds were tested for their cytotoxic activity against LH-60, MCF-7 and HeLa cancer cells in vitro using a MTT assay method. Compounds possessing an olean-triterpenoid skeleton entirely exhibit dose dependent cytotoxic activity. These findings partially confirmed the anticancer effect of this medicinal plant, suggesting a further study on the anticancer potential of the triterpenoid structure in compounds from this plant.

Cytotoxic Evaluation of the Ethyl Acetate Soluble Fraction of Perilla frutescens (소엽 Ethyl acetate 분획의 세포독성 평가)

  • Kim Sung-Eun;Chun Hyun-Ja;Kim Il-Kwang;Han Du-Seok;Lee Hyun-Ok;Ahn Jong-Woong;Lee Mee-Hee;Baek Seung-Hwa
    • Journal of Society of Preventive Korean Medicine
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    • v.5 no.2
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    • pp.106-113
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    • 2001
  • The Cytotoxic activity of the ethyl acetate soluble fraction of Perilla frutescens on human oral epithelioid carcinoma cell lines was evaluated by 3-(4,5-dimethylthiazol- 2-yl)-2,5-diphenyl-2H-tetrazalium bromide (MTT) colorimetric method. The light microscopic study was carried out to observe the morphological changes of cultured human oral epitheloid carcinoma cell lines (KB) These results were obtained as follows; 1. subfraction 1 of the ethyl acetate soluble fraction of perilla frutescens was shown significant cytotoxic activity (p<0.001) at 10-2 mg/ml concentration, this concentration was decreased the cytotoxic activity of 70.3% . 2. The comparison of IC50 values of various subfractions in human oral epithelioid carcinoma cell lines was exhibited that their susceptibility to these subfractions decreased in the following order ; subfraction 5 > subfraction 4 > subfraction 3 > subfraction 2 > subfraction 1 by MTT assay. In light microscopy, the subfraction 1 of the ethyl acetate soluble fraction of Perilla frutescens showed the highest cytotoxic activity. These findings suggest that subfraction 1 possessed the most cytotoxic constituents.

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Chemical Modification of Alisol B 23-acetate and Their Cytotoxic Activity

  • Lee, Sang-Myung;Min, Byung-Sun;Bae, Ki-Hwan
    • Archives of Pharmacal Research
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    • v.25 no.5
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    • pp.608-612
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    • 2002
  • The twelve-protostane analogues were synthesized from alisol B 23-acetate and assessed for their in vitro antitumor activity against six different human and murine tumor cell lines. Of the compounds synthesized, 23S-acetoxy-24R(25)-epoxy-11$\beta$,23S-dihydroxyprotost-13(17)-en-3-hy-droxyimine (12) exhibited significant cytotoxic activities against A549, SK-OV3, B16-F10, and HT1080 tumor cells with $ED_{50}/$ values of 10.0, 8.7 ,5.2, and 3.1 ${\mu}g$/ml, respectively. Furthermore, 23S-acetoxy-13(17),24R(25)-diepoxy-11$\beta$-hydroxyprotost-3-one (5), 13(17),24R(25)-diepoxy-11$\beta$, 23S-dihydroxyprotostan-3-one (6), 24R,25-epoxy-11$\beta$,23S-dihydroxyprotost-13(17)-en-3-one (7), and 11$\beta$,23S,24R,25-tetrahydroxyprotost-13(17)-en-3-one (9) showed moderate cytotoxic activities against 816-F10 and HT1080 tumor cells. These results mean that a hydroxyimino group at C-3 position in the protostane-type terpene enhances cytotoxic activity.

Chemical Constituents from the Leaf and Twig of Acer okamotoanum Nakai and their Cytotoxicity

  • Jin, Wen-Yi;Min, Byung-Sun;Youn, Ui-Jung;Hung, Tran-Manh;Song, Kyung-Sik;Seong, Yeon-Hee;Bae, Ki-Hwan
    • Korean Journal of Medicinal Crop Science
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    • v.14 no.2
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    • pp.77-81
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    • 2006
  • As a result of cytotoxic compounds against cancer cell lines from natural sources, senven compounds were isolated from the leaf and twig of Acer okamotoanum Nakai. The compounds (1-7) were identified as ethyl gallate (1), methyl gallate (2), gallic acid (3), trans $resveratrol-3-O-{\beta}-D-glucopyranoside$ (4), acertannin (5), nikoenoside (6), and fraxin (7) by physicochemical and spectroscopic data (including mp, UV, IR, MS, $^1H-NMR,\;^{13}C-NMR$, DEPT, and HMBC) in comparison with those of published papers. All the compounds were tested for their cytotoxic activity against L1210, HL-60, K562, and B16F10 cancer cell lines in vitro by MTT assay method. Compounds 1-3 and 5 showed cytotoxic activity against all tested cell lines with $IC_{50}$ values ranged from 12.5 to $72.2\;{\mu}M$. Of the compounds, methyl gallate (2) exhibited the most potent cytotoxic activity against L1210, HL-60, K562, and B16F10 tumor cells with $IC_{50}$ values of 12.5, 48.3, 22.8, and $22.8\;{\mu}M$, respectively. Other compounds did not show any cytotoxic activity against four cancer cell lines.

Cytotoxic Triterpenoids from the Fruiting Bodies of Ganoderma lucidum

  • Tung, Nguyen The;Trang, Tran Thi Thu;Cuong, To Dao;Thu, Nguyen Van;Woo, Mi Hee;Min, Byung Sun
    • Natural Product Sciences
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    • v.20 no.1
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    • pp.7-12
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    • 2014
  • Twelve triterpenoids (1 - 12) were isolated from $CHCl_3$-soluble fraction of fruiting bodies of Ganoderma lucidum. Extensive spectroscopic and chemical studies established the structures of these compounds as butyl lucidenate P (1), butyl lucidenate $E_2$ (2), butyl lucidenate $D_2$ (3), butyl lucidenate Q (4), ganoderiol F (5), methyl ganoderate H (6), methyl ganoderate J (7), lucidumol B (8), ganodermanondiol (9), methyl lucidenate N (10), methyl lucidenate A (11) and butyl lucidenate N (12). All of the compounds were examined for their cytotoxic activity against HL-60, HeLa, and MCF-7 cancer cell lines. Among them, compounds 4 and 8 showed cytotoxic activity with $IC_{50}$ values of 6.6 and 1.6 ${\mu}M$ against HL-60, respectively. In addition, compound 8 also showed cytotoxic activity with $IC_{50}$ values of 2.0 ${\mu}M$ against HeLa cancer cell line, other compounds were moderate or inactive.

Novel 5-Fluorouracil Derivatives: Synthesis and Cytotoxic Activity of 2-Butoxy-4-Substituted 5-Fluoropyrimidines

  • Sun, Jian;Zhang, Shi-Jie;Li, Hai-Bo;Zhou, Wei;Hu, Wei-Xiao;Shan, Shang
    • Bulletin of the Korean Chemical Society
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    • v.34 no.5
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    • pp.1349-1354
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    • 2013
  • Twenty two new 5-fluorouracil (5-FU) derivatives, 2-butoxy-4-substituted 5-fluoropyrimidines, were synthesized and characterized by IR, $^1H$ NMR, MS, HRMS. All compounds were preliminarily evaluated by MTT assay on human liver BEL-7402 cancer cell line in vitro. Ten compounds were selected to test their cytotoxic activity against A549, HL-60 and MCF-7 cancer cell lines in vitro. These compounds were more sensitive to BEL-7402 than other cell lines, particularly, cytotoxic activity of compounds 6b, 6d-f, 6p, 6s-u were in sub-micromolar scale. The highest cytotoxic potency against A549, HL-60 and MCF-7 was shown by 2-butoxy-4-chloro-5-fluoropyrimidine (5) with $IC_{50}$ values of 0.10, 1.66 and $0.59{\mu}M$, respectively. Compounds 6d and 6e were effective against MCF-7 with $IC_{50}$ $9.73{\mu}M$ and HL-60 with $IC_{50}$ $8.83{\mu}M$, respectively.

Cytotoxic Effects of Strawberry, Korean Raspberry, and Mulberry Extracts on Human Ovarian Cancer A2780 Cells

  • Lee, Dahae;Kang, Ki Sung;Lee, Sanghyun;Cho, Eun Ju;Kim, Hyun Young
    • Preventive Nutrition and Food Science
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    • v.21 no.4
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    • pp.384-388
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    • 2016
  • Reactive oxygen species are tumorigenic by their ability to increase cell proliferation, survival, and cellular migration. The purpose of the present study was to compare the antioxidant activity and cytotoxic effects of 3 berry extracts (strawberry, Korean raspberry, and mulberry) in A2780 human ovarian carcinoma cells. Except for raspberry, the ethyl acetate or methylene chloride fractions of berries containing phenolic compounds exerted dose dependent free radical scavenging activities. In the raspberry fractions, the hexane fraction also exhibited potent antioxidant activity. The cytotoxic effects of berries extracts in A2780 human ovarian carcinoma cells were measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Surprisingly, co-treatment with n-butanol (BuOH) fractions of berries showed stronger cytotoxic effects compared to the other fractions. These findings suggest that potent anticancer molecules are found in the BuOH fractions of berries that have stronger cytotoxic activity than antioxidants.

The Cytotoxic Activity of 3,4,5-Trihydroxybenzoic Acid Methylester and Related Compounds against Skin and Oral Cancer Cell Lines (3,4,5-Trihydroxybenzoic Acid Methylester와 관련 화합물의 피부암 및 구강암 세포주에 대한 세포독성)

  • Lee, Jae-Sug;Han, Du-Seok;Kang, Jeong-Il;Baek, Jong-Min;Baek, Seung-Hwa
    • YAKHAK HOEJI
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    • v.54 no.2
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    • pp.112-121
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    • 2010
  • The cytotoxic activity of 33,4,5-trihydroxybenzoic acid methylester and related compounds on the growth of normal cell lines, human skin melanoma cells and human oral epithelioid cell line were evaluated by the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) and 2,3-bis-[2-methoxy-4-nitro-5-sulfo-phenyl]-2-H-tetrazolium-5-caboxanilide (XTT) methods. 3,4,5-Trihydroxybenzoic acid methylester decreased the cell viability of human skin melanoma cells and human oral epithelioid cells shown by the MTT method and the cell adhesion activity of human skin melanoma cells and human oral epithelioid cells shown by the XTT method. In light microscopy, 100 ${\mu}M$ 3,4,5-trihydroxybenzoic acid methylester showed the highest cytotoxic activity. These results suggest that 3,4,5-trihydroxybenzoic acid methylester has a potential anticancer activity.

In vitro Biological Activity of Germacranolide sesquiterpene lactones

  • Kim, Myung-Ju;Lee, Jae-Sug;Baek, Seung-Hwa
    • Oriental Pharmacy and Experimental Medicine
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    • v.9 no.2
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    • pp.192-199
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    • 2009
  • Bioactivity-directed isolation has led to the isolation of (-)-ent-costunolide (1) as the major active compound from Hepatostolonophora paucistipula. This compound (1) was determined by spectroscopic data interpretation. This sesquiterpene lactone (1) inhibited the growth of the dermatophytic fungus Trichophyton mentagrophytes ATCC 28185, (4 mm inhibition zone at $15{\mu}g$/disc), cytotoxic activity to murine leukaemia cell lines ATCC CCL 46 P 388D1 ($IC_{50}$ 687 ng/ml, at $0.075{\mu}g$/disk), BSC monkey kidney cell lines (100% of well at $15{\mu}g$/disk) and antiviral activity to Herpes simplex virus (0.25 mg/ml, 100% of well at $7.5{\mu}g$/disk) and Polio virus (0.125 mg/ml, 100% of well at $3.75{\mu}g$/disk). These results suggest that (-)-ent-costunolide (1) has potential antimicrobial and cytotoxic agents.