• Bulletin of the Korean Chemical Society
• /
• v.34 no.5
• /
• pp.1349-1354
• /
• 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.

• Restorative Dentistry and Endodontics
• /
• v.18 no.1
• /
• pp.95-102
• /
• 1993

Two functions of root canal medicaments and irrigants are to reduce microorganisms and to encourge the repair of apical tissues. The biocompatibility of endodontic materials has been tested using in vitro cell culture techniques. The purpose of this study Was to evaluate and compare the cytotoxic effects of 2 root canal irrigation solutions and 4 antiseptics on HEp-2 and McCoy cells. Two irrigation solutions were sodium hypochlorite. $H_2O_2$ and 4 antiseptics were povidone, ethanol, glutaraldehyde and benzalkonium chloride. Each solutions were serially diluted to 1:1, 1:10, 1:$10^2$, 1:$10^3$, 1:$10^4$, 1:$10^5$, 1:$10^6$. And each diluted solutions were added to the cells and cytotoxic effects were measured with the absorbance of formazan formed cells by ELISA READER. The results were as follows : 1. Benzalkonium chloride was the most cytotoxic on HEp-2 cell. (P<0.05) 2. $H_2O_2$ was the most cytotoxic on McCoy cell. (P<.05) 3. Povidone and ethanol showed mild cytotoxic effect on HEp-2 and McCoy cell. (P<0.05).

• Toxicological Research
• /
• v.26 no.2
• /
• pp.117-121
• /
• 2010

The crude ethanol extract of B. repanda showed the cytotoxic activity against Polio virus (25% activity at $150{\mu}g$/disk) and the minor cytotoxic activity against BSC cells (African green monkey kidney). However, the crude ethanol extract of B. repanda was non-toxic to murine leukaemia cells CCL 46 P388D1 ($IC_{50}$, > 62,500 ng/ml). Cytotoxic and antifungal activities were strongly shown by Fr. 64-3 which was eluted with 90% $CH_3CN/H_2O$, 100% $CH_3CN$, and 50% $CH_3CN/H_2O$(SM 2 at $150{\mu}g$/disk). The fraction 64-3 also showed the most cytotoxic activity against murine leukaemia cells (128 mg, $IC_{50}$ 10,051 ng/ml at $75{\mu}g$/disk). These results suggest that this fraction has a potent antifungal activity against the dermatophytic fungus Trichophyton mentagrophytes ATCC 28185.

• Natural Product Sciences
• /
• v.24 no.4
• /
• pp.219-224
• /
• 2018

During the screening for cytotoxic compounds from plants grown in Korea, Betula platyphylla (BP) showed potent activity against the adenocarcinomic human alveolar basal epithelial A549 cell line. To identify the cytotoxic components from BP, the $CH_2Cl_2$ fraction with the most significant cytotoxic effect was applied to the column chromatographies. Seven compounds were isolated: lupeol (1), betulinic acid (2), (-)-rhododendrol (3), platyphyllenone (4), platyphyllone (5), (-)-centrolobol (6), and oleanolic acid (7). Among them, three diarylheptanoids (4 - 6) exhibited cytotoxicity toward A549 cells. Especially, $50{\mu}M$ of 4 reduced A549 cell viability to $18.93{\pm}0.82%$ compared to control ($100.00{\pm}21.48%$). Lactate dehydrogenase (LDH) leakage and intracellular reactive oxygen species (ROS) production were also induced by $50{\mu}M$ 4. This is the first report on the cytotoxic effect of BP-derived diarylheptanoids 4-6 against A549 cells. The compound 4 may be useful for the development of early hit compounds for non-small cell lung carcinoma, but the consideration about selectivity of 4 is required since 4 also showed the cytotoxicity in the human normal lung epithelial BEAS-2B cell line.

• Proceedings of the Plant Resources Society of Korea Conference
• /
• 2020.12a
• /
• pp.16-44
• /
• 2020

Cancer is the second leading cause of death in the world. According to the 2018 reports, one in six people worldwide is reported to die as a result of cancer. The discovery of anticancer drugs has been utilized extensively, but there has been no report on excellent selective activity in cancer cells. The discovery of bioactive substances from marine sponges has been the limelight in the pharmaceutical field over the past decade owing to the production of many bioactive compounds from the sponges to protect themselves against the environment. On top of that, marine sponges also produced cytotoxic compounds such as terpenoids, alkaloids, steroids, and peptides which suggests that marine sponges have high potential in the development of anticancer drugs. Thus, this study aimed to obtain new cytotoxic compounds from S. siphonella in Egypt and Arenoscelra sp. and Gelliodes sp. in Vietnam, and further investigation of the extract from these marine sponges led to isolation of ten new compounds and 21 known compounds. Chapter 1 will discuss about the isolation and structure elucidation of eight new polyacetylene derivatives from S. siphonella and their cytotoxic activities. The isolation and structural elucidation of one new polybrominated iododiphenyl ether from Arenosoclea sp. as well as cytotoxic activities of the isolated compounds will be reported in chapter 2. Finally, isolation and structure elucidation of new compounds from the marine sponge Gelliodes sp. and their cytotoxic activities will be discussed in chapter 3.

• Korean Journal of Pharmacognosy
• /
• v.23 no.4
• /
• pp.264-267
• /
• 1992

The cytotoxic activity of medicinal plants was screened using A549 human lung cancer cell line. Plant materials were extracted with 80% methanol and fractionated to chloroform and water layers. Each methanol, chloroform, and water extract of thirty-two medicinal plants was tested for cytotoxic activity in A549 cell culture system and the cell viability was measured by SRB assay.

• Korean Journal of Pharmacognosy
• /
• v.19 no.4
• /
• pp.251-255
• /
• 1988

A cytotoxic sesquiterpene against L1210 cell, named pubetalin. was isolated from the herb of Siegesbeckia pubescens Makino. Its structure was identified as $6-formyl-2,\;3,\;3{\alpha},\;4,\;5,\;8,\;9,\;11{\alpha}-octahydro-10-hydroxymethyl-5-methoxy-3-methylene-2-oxocyclodeca[{\beta}]\;furan-4-ylester$ of 2-methyl-2-propenoic acid.

• Proceedings of the PSK Conference
• /
• 2003.04a
• /
• pp.215.2-216
• /
• 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)

• Archives of Pharmacal Research
• /
• v.26 no.4
• /
• pp.270-274
• /
• 2003

A series of new 3-alkyl-1-(1-methyl-2-phenylethyl)ureas related to ceramide was synthesized and evaluated for their in vitro cytotoxic activity against five human tumor cell lines. The urea analogue (2b) of 813 showed comparable or slightly more potent cytotoxic activity as compared to B13, indicating that urea does appear to serve as a bioisostere of amide.

• Proceedings of the Korean Society of Toxicology Conference
• /
• 2001.10a
• /
• pp.105-105
• /
• 2001

A wide array of natural products have been identified to possess potenital cancer chemopreventive properties. Of particular interest is Polyporus umbellatus frs.. that exhibits antimutagenic and cytotoxic effects. The crud drug "chorei" prepared from the dried fruit body of Polyporus umbellatus is used for kidney and other such disease. In the study, we are isolating the minor components of Chorei and examined their antimutagenic and cytotoxic effects.(omitted)