• Journal of Physiology & Pathology in Korean Medicine
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• v.18 no.5
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• pp.1343-1346
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• 2004

Cornis fructus were extracted by successive extractions and then fractionated with chloroform extract to get active fractions. This study was performed to determine the cytotoxic effect of chloroform extract from Corn is fructus on NIH 3T3 fibroblasts and cancer cell lines using MTT assay. All extracts did not exhibit cytotoxicity in NIH 3T3 fibroblasts. Chloroform extract exhibited antitumor activity in A549, MDA-MB-123, B16 melanoma and SNU-C4 cells. Futher fractionation with chloroform extract was performed to obtain effective fractions. 3 fraction showed the strongest cytotoxic effect against A549, MDA-MB-123, B16 melanoma and SNU-C4 cells. These results suggest that 3 fraction of the chloroform extract from Cornis fructus possessed bioactive material of antitumorous agents.

• The Korean Journal of Physiology and Pharmacology
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• v.13 no.6
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• pp.511-516
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• 2009

A series of substituted 2-arylnaphthyridin-4-one analogues, which were previously synthesized in our laboratory, were evaluated for their in vitro cytotoxic activity against human lung cancer A549 and human renal cancer Caki-2 cells using MTT assay. Some compounds (11, 12, and 13) showed stronger cytotoxicity than colchicine against both tumor cell lines, and compound 13 exhibited the most potent activity with $IC_{50}$ values of 2.3 and $13.4\;{\mu}M$, respectively. Three-dimensional quantitative structure activity relationship (3D-QSAR) studies of comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) were performed. Predictive 3D-QSAR models were obtained with $q^2$ values of 0.869 and 0.872 and $r^2_{ncv}$ values of 0.983 and 0.993 for CoMFA and CoMSIA, respectively. These results demonstrate that CoMFA and CoMSIA models could be reliably used in the design of novel cytotoxic agents.

• Archives of Pharmacal Research
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• v.24 no.5
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• pp.390-396
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• 2001

Synthesized 6-arylamino-5,8-quinolinediones 4a-4j and 6-chloro-7-arylamino-5,8-isoquinolinediones 5a-5g were evaluated for effects on NAD(P)H quinone oxidoreductase (NQOl ) activity with the cytosolic fractions derived from cultured human lung cancer cells and their cytotoxicity in cultured several human solid cancer cell lines. The 5,8-quinolinediones 4 and 5,8-isoquinolinediones 5 affected the reduction potential by NQO1 activity and showed a potent cytotoxic activity against human cancer cell lines. The tested compounds 4a, 5c, 5f, and 5g were considered as more potent cytotoxic agents. The compounds 4d, 5b, 5c, 5e and 5g were comparable modulators of NQO1 activity.

• Journal of Physiology & Pathology in Korean Medicine
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• v.17 no.5
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• pp.1288-1292
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• 2003

This study was carried out to evaluate cytotoxic effects of Houttuynia cordata T/sub HUNB/ extracts on A549 (lung cancer), MDA-MB231 (breast cancer), SNU-C4 (colon cancer) and B16 (mouse melanoma) cell lines. We have determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazoliumbromide (MTT) assay. The 150 ㎍/㎖ concentration of methanol extract (63.81 %) of Houttuynia cordata T/sub HUNB/ was shown significantly antitoxic activity on A549 cell lines. The order of cytotoxicity fractions of methanol from Houttuynia cordata T/sub HUNB/ extracts against cancer cell lines in vitro is as follows : hexane fraction layer > chloroform fraction layer > ethyl acetate fraction layer > buthanol fraction layer > water fraction layer. These results suggest that the hexane fraction of methanol extract from Houttuynia cordata T/sub HUNB/ extract may be a valuable choice for the development of antitumor agents.

• Natural Product Sciences
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• v.8 no.4
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• pp.170-172
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• 2002

In continuous efforts for discovery of novel potent antitumor agents from natural products, fifty-seven methanolic extracts derived from indigenous Korean plants were primarily evaluated for in vitro cytotoxic activity in cultured human lung (A549) and colon (Col2) cancer cells. As a result, 16 plant extracts were found to be active against A549 cells and 15 extracts were active against Col2 cells in the criteria of $IC_{50}$<$50\;{\mu}g/ml$. In particular, the extracts of Calystegia soldanella $(IC_{50}$<$8.0\;{\mu}g/ml\;in\;A549;IC_{50}=27.4\;{\mu}g/ml\;in\;Col2)$, Heloniopsis orientalis $(IC_{50}=4.6\;{\mu}g/ml\;in\;A549; IC_{50}=4.5\;{\mu}g/ml\;in\;Col2)$, and Thuja koraiensis $(IC_{50}=1.2\;{\mu}g/ml\;in\;A549;IC_{50}=0.6\;{\mu}g/ml\;in\;Col2)$ showed a potent cytotoxic activity. Further study for the identification of active compounds from these lead extracts might be warranted.

• Archives of Pharmacal Research
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• v.25 no.4
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• pp.550-555
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• 2002

The discovery and development of the taxane class of antitumor compounds represent significant advances in the treatment of patients with a variety of malignancies. These drugs are effectively used in the treatment of breast cancer. In this study we evaluated the efficacy of fractionated usage of both paclitaxel and docetaxel as a single agent in the breast cancer cell line MCF-7. It has been shown that the cytotoxic effect of paclitaxel was increased when the divided $IC_{50}$ concentrations were used sequentially and in contrast to paclitaxel, cytotoxic effect of docetaxel was decreased with the same schema and the single dose of $IC_{50}$ concentration was optimal. The cause of the difference between the cytotoxic effects of two agents with this schedule is obscure. Demonstrating mechanisms, which are responsible for these differences, will be important for more rational use of taxoids and to provide basis for the following clinical trials.

• Archives of Pharmacal Research
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• v.21 no.6
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• pp.749-752
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• 1998

Six 3-dialkylaminomethyl-1-azaanthraquinones and five 4-dialkylaminomethyl-1-azaanthraquinones were synthesized and evaluated in vitro cytotoxicity against four human can cer cell lines. The compounds retained much of their cytotoxic activity against the multi-drug-resistant cell line (KB-V-1) as shown by resistance index.

• Biomedical Science Letters
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• v.12 no.4
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• pp.451-455
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• 2006

It is demonstrated that inorganic mercury has cytotoxic effect on glial cells. Recently, oxygen radicals is involved in methylmercuric chloride (MMC)-induced cytotoxicity. But, the toxic mechanism of MMC is left unknown. The purpose of this study was to examine the cytotoxicity of MMC on $C_6$ glioma cells. The cytotoxicy was measured by cell viability using XTT assay in $C_6$ glioma cells. Colorimetric assay is regarded as a very sensitive screening method for the determination of the cell viability on various agents. In this study, MMC decreased cell viability according to the dose- and time dependent manners after $C_6$ glioma cells were grown with various concentrations of MMC for 48 hours. In the protective effect of allopurinol on MMC-induced cytotoxicity, allopurinol was effective in the prevention of MMC-induced cytotoxicity in these cultures. These results suggest that MMC has highly cytotoxic effect on $C_6$ glioma cells by the decrease of cell viavility, and free radical scavenger such as allopurinol was effective on organic mercury-induced cytotoxicity in these cultures.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.18
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• pp.7505-7513
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• 2014

Several toxic substances have been detected in plants which are responsible for animal and human diseases. Bracken fern (Pteridium aquilinum) is one example, widely distributed in many parts of the world. It is known to cause cancer in humans and other animals. In fact, man can be directly or indirectly exposed to the danger by consuming fern, contaminated water, milk, meat, and spore inhalation. Experimental studies have shown an association between bracken exposure and gastric cancer, and research has shown genotoxic and cytotoxic effects in vitro. This paper describes and reviews toxic, carcinogenic, genotoxic/cytotoxic, and immunomodulatory effects of bracken and included possible toxic agents. The chemistry of Ptaquiloside (PT) reactions is emphasized, along with bracken problems in livestock, possible pathways of exposure in man, and control for human health.

• Proceedings of the Korean Society of Applied Pharmacology
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• 2000.04a
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• pp.8-9
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• 2000

Despite the advances made in the past few decades in cancer chemotherapy, many conventional anticancer drugs display relatively poor selectivity for cancer cells. The nonselectivity of anticancer drugs and the development of anticancer drug resistance have been recognized as serious limitations in their clinical usefulness. Therefore, a major challenge in cancer chemotherapy is the development of new anticancer agents with improved selectivity for tumor cells as well as the prevention of the host cell resistance, both of which result in the improvement of therapeutic effect against cancer cells. Cyclophosphamide (CP), a widely used anticancer agent, is a prodrug that is activated by hepatic microsomal mixed-function oxidase (MFO) catalyzed C$_4$- hydroxylation. The resulting 4-hydroxycyclophosphamide (4-OH-CP) is converted to the ring-opened tautomer to aldophosphamide (Aldo) which subsequently undergoes a base- catalyzed ${\beta}$-elimination to generate cytotoxic phosphoramide mustard (PDA) and acrolein. The cytotoxic activity of CP is attributed to the aziridinium ion species derived from PDA that cross-links interstrand DNA.