• Archives of Pharmacal Research
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• 제27권5호
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• pp.478-484
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• 2004

The novel 1-(1-benzoylindoline-5-sulfonyl)-4-phenyl-4,5-dihydroimidazolones 2 shows highly potent and broad cytotoxicities. Their cytotoxicities against human lung carcinoma A549, human chronic myelogenous leukemia K562, and human ovarian adenocarcinoma SK-OV-3 are compatible with doxorubicin. Compound 2p (1-[(4-aminobenzoyl)indoline-5-sulfonyl])-4-phenyl-4,5-dihydroimidazolone) exhibits a cytotoxicity that is far more potent than doxorubicin and also exhibits highly effective antitumour activities against murine (3LL, Colon 26) and human xenograft (NCI-H23, SW620) tumor models.

• Journal of Pharmaceutical Investigation
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• 제25권4호
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• pp.365-369
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• 1995

The acute cytotoxicities of chloroquine sulfate, propranolol, ascorbic acid, acetylsalicylic acid and acrylamide on cultured adult rat hepatocytes were evaluated by the use of LDH leakage and NR uptake test. On the basis of $IC_{50}$ values, the rank order of cytotoxicities of these drugs in both tests was chloroquine sulfate > propranolol > acetylsalicylic acid > ascorbic acid. The $IC_{50}$ of LDH test was very similar to that of NR uptake test. Thus, we concluded that both tests are reliable and sensitive methods in detecting toxicity in adult cultured rat hepatocytes.

• 약학회지
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• 제33권2호
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• pp.118-123
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• 1989

A new polyacetylene compound which has strong cytotoxic activity against L1210 cell, was isolated from Korean ginseng roots. The structure was determined to be heptadeca-1-ene-4,6-diyne-3,9-diol-10-acetate (10-acetyl panaxytriol, $ED_{50}\;=\;1.2\;{\mu}g/ml$). The cytotoxicities of this compound and acetyl panaxydol lower than their starting substances, panaxytriol and panaxydol. The presence of one for the decreases in the cytotoxicities.

• Archives of Pharmacal Research
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• 제24권4호
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• pp.300-306
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• 2001

A novel and two known bioactive mono-tetrahydrofuran (THF) annonaceous acetogenins, annomocherin (1), annonacin (2) and annomontacin (3), have been isolated from the fractionated ethanolic extracts of the seeds of Annona cherimolia, guided by the brine shrimp lethality test (BST). Their structures were elucidated on the basis of spectroscopic and chemical methods. All compounds have a relative stereochemistry of threo/trans/threo for the mono-THF ring with two flanking hydroxyls. Compound 1 has a double bond at C-23/ 24 of aliphatic chain. Compound 1 was isolated from natural sources for the first time, and was named annomocherin. Two known Compounds 2 and 3 which have never been isolated from this species before, were obtained. Compound 1 exhibited potent and selective cytotoxicities against the breast carcinoma (MCF-7) and kidney carcinoma (A-498) cell lines with 100 to 1,000 times the potency of adriamycin. In brine shrimp lethality test (BST), 1-3 exhibited cytotoxicity.

• 대한약학회:학술대회논문집
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• 대한약학회 2000년도 NEW STRATEGY FOR DRUG DEVELOPMENT IN POST-GENOMIC ERA(대한약학회)
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• pp.212.1-212.1
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• 2000

• 한국산업보건학회지
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• 제23권2호
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• pp.50-56
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• 2013

Objectives: The present study investigated cytotoxicity and DNA damage in human lung cells in vitro. Methods: Neodymium oxide and lanthanum oxide were dispersed by ultrasonic treatments. The assay was performed with MRC-5 (Human male fetus lung cell). Cytotoxicity and comet assay of lanthanum oxide and neodymium oxide were measured after 24 and 48 hours incubation. Results: After 24 hours of exposure to rare earth metals, the cytotoxicities of lanthanum oxide in more than $1{\mu}M$ concentration groups were significantly increased when compared to the control group, but the cytotoxicities of neodymiun oxide in more than $100{\mu}M$ concentration groups were statistically increased. After 48 hours exposure, cytotoxicities of both materials were statistically increased in $100,000{\mu}M$ concentration groups. Olive tail moments of the lanthanum oxide treated group were significantly increased when compared to the control group. Conclusions: The cytotoxicity of lanthanum oxide was higher than that of neodymium oxide. The DNA of MRC-5 cells treated with lanthanum oxide for 48 hours were significantly damaged.

• 한국산학기술학회논문지
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• 제9권6호
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• pp.1787-1794
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• 2008

Coenzyme $Q_{10}$과 그 유도체 coenzyme $Q_n$ 6종을 합성하고, 이들 유도체에 대하여 상피세포(LLC-PK1 cell)를 이용한 항산화 효과와 NIH/3T3 세포를 이용한 세포독성 실험을 실시하였다. 그 결과, 합성한 coenzyme $Q_n$ 유도체들이 coenzyme $Q_{10}$에 비해 우수한 항산화 효과를 나타내었으며, 그 중 coenzyme $Q_3$-C가 모든 농도에서 $107.7{\sim}135.9%$로 가장 우수한 효과를 나타내었다. 또한, 모든 coenzyme $Q_n$ 유도체들이 Coenzyme $Q_{10}$과 유사한 세포독성을 나타내었다. Coenzyme $Q_n$의 n수에 따른 항산화 효과 및 세포독성 실험에서 isoprene unit의 수가 적은 유도체들에서 우수한 효과를 나타내었다.

• The Korean Journal of Physiology and Pharmacology
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• 제15권6호
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• pp.423-429
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• 2011

B13 analogues are being considered as therapeutic agents for cancer cells, since B13 is a ceramide analogue and inhibits ceramidase to promote apoptosis in cancer cells. B13 sulfonamides are assumed to have biological activity similar to B13, since they are made by bioisosterically substituting the carboxyl moiety of B13 with sulfone group. Twenty B13 sulfonamides were evaluated for their in vitro cytotoxicities against human colon cancer HT-29 and lung cancer A549 cell lines using MTT assays. Replacement of the amide group with a sulfonamide group increased cytotoxicity in both cancer cell lines. The sulfonamides with long alkyl chains exhibited activities two to three times more potent than that of B13 and compound (15) had the most potent activity with $IC_{50}$ values of 27 and $28.7{\mu}M$ for HT-29 and A549, respectively. The comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) were used to carry out QSAR molecular modeling of these compounds. The predictive CoMSIA models for HT-29 and A549 gave cross-validated q2 values of 0.703 and 0.830, respectively. From graphical analysis of these models, we suppose that the stereochemistry of 1,3-propandiol is not important for activity and that introduction of a sulfonamide group and long alkyl chains into B13 can increase cytotoxicity.

• Toxicological Research
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• 제19권1호
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• pp.45-50
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• 2003

The purpose of this study was to determine the role of substituted groups in phenolic compounds to develop an anticancer agent having strong cytotoxicity against cancer cells but weak against normal cells. The phenolic compounds used in this study were gallic acid and ferulic acid with hydroxyl and carboxyl groups, syringic acid with hydroxyl, carboxyl and methoxy groups, and pyre-gallol with hydroxyl groups. Cytotoxicities of these compounds were evaluated by MTT assay for cell viability and XTT assay for cell adhesion activity in normal human skin fibroblast (Detroit 551) and human skin melanoma (SK-MEL-3) cells. Syringic acid, gallic acid and ferulic acid decreased the cell viability and cell adhesion activity in SK-MEL-3 cells but not in Detroit 551 cells while pyrogallol decreased in both cells. The susceptibility of cell viability based on the $IC_{50}$ values of MTT assay in Detroit 551 cells was in the following order: pyrogallol > gallic acid > ferulic acid > syringic acid, while it was in SK-MEL-3 cells: Syringic acid > progallol > ferulic acid > gallic acid. These results suggest that carboxyl and methoxy groups of these compounds play an important role in selectivity of cytotoxicity in normal and cancer cells.

• Archives of Pharmacal Research
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• 제21권5호
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• pp.599-609
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• 1998

In search for new antitumor agents, twelve 6-aziridinylbenzimidazole derivatives were synthesized and their cytotoxicities were tested against three cancer cell lines (mouse lymphocytic leukemia P388 and B16, and human gastric carcinoma SNU-16). From 4-amino-3-nitrotoluene as the starting material, 2-(acetoxymethyl)benzimidazoles (5a-d) were obtained by Phillips reaction. These benzimidazoles were then reacted with Fremy's salt to give a mixture of three 2-(acetoxymethyl) (8a-c) and four 2-(hydroxymethyl)benzimidazole-4,7-diones (9a-d). Addition of these quinones with aziridine afforded 6-aziridinyl-2-(acetoxymethyl) (10a-c) and 6-aziridinyl-2-(hydroxymethyl)benzimidazole-4,7-diones (11a-d). Utilizing 2-(hydroxymethyl)benzimidazole-4,7-diones (9b,d), esters 10d and 13e-h were prepared by the sequential reactions of esterification and addition. The synthesized compounds show potent cytotoxicity against all of three cell lines tested. The cytotoxicities of 10a-d or 11a-d against SNU-16 were wuperior to those of 13e-h, and were equal to or slightly higher than that of mitomycin C. compounds 11a-d were slightly more cytotoxic than 10a-d in all cell lines tested.