• Molecular & Cellular Toxicology
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• v.3 no.4
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• pp.222-230
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• 2007

Some drugs may be limited in their clinical application due to their propensity towards their adverse effects. Toxicogenomic technology represents a useful approach for evaluating the toxic properties of new drug candidates early in the drug discovery process. Nitrofurantoin (NF) is clinical chemotherapeutic agent and antimicrobial and used to treatment of urinary tract infections. However, NF has been shown to result in pulmonary toxic effects. In this research, we revealed the changing expression gene profiles in BEAS-2B, human bronchial epithelial cell line, exposed to NF by using human oligonucleotide chip. Through the clustering analysis of gene expression profiles, we identified 136 up-regulated genes and 379 down-regulated genes changed by more than 2-fold by NF. This study identifies several interesting targets and functions in relation to NF-induced toxicity through a gene ontology analysis method including biological process, cellular components, molecular function and KEGG pathway.

• BMB Reports
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• v.36 no.3
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• pp.269-274
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• 2003

In the fight against cancer, novel chemotherapeutic agents are constantly being sought to complement existing drugs. Various studies have presented evidence that the apoptosis that is induced by these anticancer agents is implicated in tumor regression, and Bcl-2 family genes play a part in apoptosis following treatment with various stimuli. Here, we present data that a styrylpyrone derivative (SPD) that is extracted from the plant Goniothalamus sp. showed cytotoxic effects on the human breast cancer cell line MCF-7. SPD significantly increased apoptosis in MCF-7 cells, as visualized by phase contrast microscopy and evaluated by the Tdt-mediated dUTP nick end-labeling assay and nuclear morphology. Western blotting and immunostaining revealed up-regulation of the proapoptotic Bax protein expression. SPD, however, did not affect the expression of the anti-apoptotic protein, Bcl-2. These results, therefore, suggest SPD as a potent cytotoxic agent on MCF-7 cells by inducing apoptosis through the modulation of Bax levels.

• Plant Resources
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• v.4 no.3
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• pp.192-195
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• 2001

Human immunodeficiency virus (HIV), the causative agent of AIDS, still continues to spread rapidly in the world population, especially in Africa and Southeast Asia. At present, two kinds of therapeutic approaches are used for treatment of AIDS. One is to target HIV reverse transcriptase, which is responsible for the viral genome transcription. The other is to inhibit HIV pretense PR, which is essential for the processing of viral proteins. Drug combinations based on these approaches can reduce the blood virus to an undetectable level. However, a small amount of virus may lurk inside the immune cells in a dormant state. Another major obstacle of long-term treatment of the disease is remarkable mutation in HIV. Most of the clinical chemotherapeutic agents have one or more of these problems. High cost and harmful side-effects further reduced the desirability of these drugs. In the course our studies on development of anti-HIV agents from natural products, we investigated various crude drugs for their inhibitory activity against HIV-induced cytopathic effects (CPE) in culture cells, HIV-pretense (PR), HIV-reverse transcriptase (RT) including ribonuclease H (RNase H), and HIV integrase (INT). In the present paper, some inhibitory substances relating to the development of anti-HIV agents are reported.

• Journal of Korean Neurosurgical Society
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• v.39 no.2
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• pp.148-151
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• 2006

Dermatofibrosarcoma protuberans[DFSP] is an uncommon fibrohistiocytic tumor characterized by aggressive local invasion and consequent local recurrence rather than distant metastasis. We present a case of a 51-year-old male patient with a typical cutaneous DFSP, which showed local recurrences and distant metastasis to the central nervous system[CNS] and the lung after 15 years from the initial diagnosis. CNS metastatic lesions recurred in 5 months after surgical resection of the first CNS lesion. These metastatic tumors were treated by open surgery and gamma-knife radiosurgery. Despite continuous medication of oral chemotherapeutic agent, the patient died during 1-year follow-up period.

• Biomolecules & Therapeutics
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• v.6 no.3
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• pp.303-311
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• 1998

The general pharmacological properties of new platinum (II) coordination complexes, SA : [Pt(trans-ι-DACH)(DPPE)] . 2NO$_3$, SB : [Pt(cia-DACH)(DPPP)] 2NO$_3$ and SC : [Pt(cia-DACH)(DPPE)] 2NO$_3$on central nervous, respiratory, cardiovascular and digestive systems were studied in various experimental animals. These platinum (II) anticancer agents had no effects on analgesia, thiopental-induced sleeping time, body temperature, strychnine-induced convulsion, inflammation and local anesthetic action in mice and rats. Intestinal motility, stomach-ulcer induced by serotonin and bile-secretion of rats were not influenced by the dose of 30 mg/kg. However SB and SC induced a mild decrease in heart rate in anesthetized rats. Based on these results, these new platinum (II) complexes may be regarded as a valuable lead compound in the development of new anticancer chemotherapeutic agents with marked antitumor activity and low toxicity.

• Korean Journal of Microbiology
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• v.29 no.6
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• pp.353-360
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• 1991

5-substituted uridine(I,Br,Cl), 5'-amino-5'-deoxyuridine conjugates of amino acid, peptide and penicillin G, 5'-monophosphate uridine derivatives and 5'-monophosphate-fatty acid detrivatives were chemically synthesized. Their biological activities were determined as MIC and IC/sub 50/ unit against various pathogenic microorganisms in vitro. 5'-amino-5'-deoxyuridine-cyclo(Phe-Asp)(23), 5-iodo-5'-amino-deoxyuridine-penicillin G(26) were the most efficient; their IC/sub 50/ against L5178Y murine lymphoma cell was 6.5 h/ml, MIC against S. aureus (+) and E. coli (-) was 6.25 g/ml. MIC of 5-bromo-2', 3'-O-isopropylideneuridine(6) against Trichophyton rubrum was 0.2 g/ml. And 5'-monophosphate derivatives are more active than simple uridine derivatives, suggesting other modified nucleoside 5'-phosphate may be worthwhile examing further as a new prodrugs.

• BMB Reports
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• v.29 no.6
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• pp.489-492
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• 1996

A number of anticancer-chemotherapeutic agents induce cell death through the process of apoptosis. Effects of echinomycin, an anticancer agent on cancer progression, were investigated in P388 murine leukemia cells. First, according to the results of cytotoxicity measurement. $IC_{50}$ of echinomycin was 1.12 nM, a relatively lower value than the other examined anticancer agents, mitomycin-C and etoposide Second, the DNA fragmentation assay for echinomycin-treated cells exhibited that echinomycin was able to induce apoptosis in a shorter period of time and with a lower dose than mitomycin-C or etoposide. The data of DNA fragmentation were quite comparable to those of cytotoxicity measurement. Finally we showed that mitogen-activated protein (MAP) kinase, a key protein in cell mitosis, was translocated into the nucleus from the cytosol after treatment with echinomycin. These findings suggest that a MAP kinase-related process may be involved in apoptosis induced by echinomycin.

• Archives of Pharmacal Research
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• v.29 no.5
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• pp.363-368
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• 2006

EGCG [(-)-epigallocatechin-3-gallate], a major component of green tea has been considered as a major antioxidant constituent. In addition to having been considered for cancer treatment as a chemopreventive and chemotherapeutic agent, EGCG has recently been attributed an anti-proliferative effect. We re-examined the latter finding in this study and added specific focus on the ability of EGCG to induce apoptosis in human osteogenic sarcoma (HOS) cells. Antiproliferative action of EGCG $(IC_{50}=35.3{\pm}6.0{\mu}g/mL)$ appeared to be linked to apoptotic cell death based on morphological changes, chromosomal DNA degradation, and an increase in the $sub-G_1$ apoptotic cell population. Treatment of HOS cells with EGCG gradually activated caspase-3, an established inducer of apoptotic cell death.

• Archives of Pharmacal Research
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• v.5 no.2
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• pp.61-70
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• 1982

Sulfisoxazole, a chemotherapeutic agent, was microencapsulated with ethylcellulose by means of phase separation form cyclohexane by temperatture change. The size distribution was determined by use of standard sieves and the effect of core to wall ratio was noted. To examine their shapes and usrface characteristics, the microcapsules were observed with a scanning electron microscope. Release of the drug from microcapsules into pH 7.5 buffer medium was studied. The release pattern was found to have similar properties to the release of a drug from an insoluble porous matrix reported. The apparent diffusion coefficient of sulfisoxazole was measured for the transport of the drug from the core of microcapsules into the surronding sink condition. The apparent diffusion coefficient increased with increasing capsule size.

• Molecules and Cells
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• v.44 no.5
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• pp.356-362
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• 2021

An increasing number of studies have revealed an interaction between gut microbiota and tumors. The enrichment of specific bacteria strains in the intestines has been found to modulate tumor growth and influence the mechanisms of tumor treatment. Various bacteria are involved in modulating the effects of chemotherapeutic drugs currently used to treat patients with cancer, and they affect not only gastrointestinal tract tumors but also distant organ tumors. In addition, changes in the gut microbiota are known to be involved in the antitumor immune response as well as the modulation of the intestinal immune system. As a result, the gut microbiota plays an important role in modulating the efficacy of immune checkpoint inhibitors. Therefore, gut microbiota could be considered as an adjuvant treatment option with other cancer treatment or as another marker for predicting treatment response. In this review, we examine how gut microbiota affects cancer treatments.