• Bulletin of the Korean Chemical Society
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• 제34권5호
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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.

• Archives of Pharmacal Research
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• 제25권5호
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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.

• Preventive Nutrition and Food Science
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• 제21권4호
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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.

• Natural Product Sciences
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• 제20권1호
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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.

• 약학회지
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• 제54권2호
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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.

• Nutrition Research and Practice
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• 제1권3호
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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.

• Advances in Traditional Medicine
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• 제9권2호
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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.

• Archives of Pharmacal Research
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• 제25권3호
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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.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.215.2-216
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• 2003

Velutin and betulinic acid were isolated as a cytotoxic principle from the dichloromethane extract of Korean mistletoe (Viscum album var. coloratum) by repeated silicagel chromatography and recrystallization. In in vitro analysis of cytotoxic activity using NIH-3T3 cells, dichloromethane extract of Korean mistletoe was shown to be highly cytotoxic against tumor cells. And we obtained active compound (reffered to VD-2 and VD-6) from the dichloromethane extract. (omitted)

• Advances in Traditional Medicine
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• 제7권2호
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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.