• Journal of Marine Life Science
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• v.7 no.1
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• pp.15-20
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• 2022

Glioblastoma is one of the highly aggressive central nervous system tumors and it is difficult to treat owing its anatomical location. Peptides are novel class of drugs which has the potential to cross the blood brain barrier and exerts its anti-tumor activity. Here, we discovered a novel peptide from abalone (Haliotis discus hannai) next generation sequencing (NGS) data and tested its anticancer effect on glioblastoma cell line SNU-489. The anticancer activity was measured using a cytotoxicity assay in a time and dose-dependent manner. A concentration and time dependent increase in the cytotoxicity was seen in cells treated with the novel peptide. The highest cytotoxicity rate of about 67% was observed in SNU-489 cells treated with 200 µM peptide for 48 hrs. However, the cytotoxic effect was not or less observed in a normal skin cell line HaCaT at similar concentration, thus, evident of peptide's cell specific anticancer activity. In addition, the gene expression level of necroptosis-related genes was analyzed by qRT-PCR to elucidate the anticancer mechanism of the novel peptide. RIPK3 expression was significantly increased by 9.6-fold in 200 µM of novel peptide treatment group, and MLKL expression level was significantly elevated by 2-fold in 100 µM treated group compared to the control group. Therefore, this study confirmed that the novel abalone-derived peptide has anticancer potency, and it causes cancer cell death through the necroptosis mechanism. Collectively, these results suggest that the novel peptide could be candidate anticancer agent for the treatment of glioblastoma in the future.

• Biomolecules & Therapeutics
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• v.1 no.2
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• pp.226-235
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• 1993

DA-125, a new anthracycline antitumor antibiotic, was administered to Sprague-Dawley rats intravenously for 4 weeks to investigate the repeated dose toxicity Focal alopecia was noted in three female rats receiving 1.0mg/kg/day. In rats receiving 1.0 mg/kg/day, weight gain decreased in both sexes after first or second week. Hematological examination revealed lower counts of total leukocyte and increased numbers of platelet after second week. At terminal necropsy, atrophy of thymus and spleen was observed. Lymphocytic depletion of thymus and atrophy of white pulp in spleen were observed microscopically. A decrease in the number of hematopoietic cells in the bone marrow and degeneration of germinal epithelia in testes were also observed. These treatment-related effects were mainly confined to rats receiving 1.0 mg/kg/day. And toxic effects with microscopic changes were not observed in rats receiving 0.2 mg/kg/day or 0.04 mg/kg/day.

• Journal of Pharmaceutical Investigation
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• v.39 no.1
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• pp.13-18
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• 2009

Docetaxel is an anticancer agent with low aqueous solubility. More extensive clinical use of this drug is somewhat delayed due to lack of appropriate delivery vehicles. An attempt was made to adopt an o/w emulsion as the drug carrier which incorporated docetaxel in the propyleneglycerol stabilized by a mixed-emulsifier system. A suitable formulation was found in this study: 10 mg/mL docetaxel, 10% (w/v) oil blend, 4% (w/v) PG, 3% (w/v) Solutol HS 15 in 2.25% (w/v) glycerol solution. The formulated emulsion has very good stability when stored at $40^{\cird}C$, and the docetaxel containment efficiency can be maintained above 95% and the mean emulsion diameter around $10{\mu}m$ for at least 3 months. The formulated emulsion is a promising carrier for docetaxel and other lipophilic drugs.

• Proceedings of the Korean Society of Applied Pharmacology
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• 2001.11a
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• pp.79-79
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• 2001

Genotoxic chemotherapeutics are irreversible DNA targeting agents, which can act as anticancer and antiviral drugs. Natural antibacterial and anticancer enediynes function through the formation of free radicals formed by Bergman-type cycloaromatization and being capable of cleavage of DNA strand. They have been focused primarily on the design and syntheses of simple enediyne structures, which can be mimic their mechanistic feature. Recently. I have been reported the possible application of 4'-bromoacetophenone as a simple photoactivatable DNA cleaving agent, which could be readily prepared and exhibit potent and selective DNA cleaving activity. Herein, we further investigated the activity of 4'-bromoacetophenone-pyrrolecarboxamides, which consist of both DNA cleaving element and recognition unit under various conditions in order to get more understanding of the mechanism of the action and find a broad spectrum of application.

• Biomolecules & Therapeutics
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• v.1 no.1
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• pp.20-25
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• 1993

DA-125, a new anthracycline derivative, shows significant anticancer activities. We conducted a study to examine the local irritating effect of DA-125 using mice and rabbits. In the skin test in mice, intradermal injection of 0.4 mg of DA-125, compared to a dosage of 0.2 mg of adriamycin, had weak irritating potentials to induce skin ulceration and erythematous induration. A dosage of 0.6 mg of DA-125 produced similar degree of lesions in perivascular irritation model to that of 0.2 mg of adriamycin, but the healing time was shorter in the case of mice treated with DA-125. In ocular irritation study in rabbit, the highest M.O.I.(mean ocular irritation index) of 0.5% DA-125 solution was 0.67, therefore DA-125 could be considered as a practically non-irritating anticancer agent. These results suggest that substitution of DA-125 for Adriamycin would reduces the possibility of outbreaks of local irritation and the severity of the lesions.

• The Journal of the Korean dental association
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• v.15 no.9
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• pp.749-753
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• 1977

The author studied the effects of anticancer Endoxan to the rat's teeth. Two hundred pregnant rats were used. The experimental rats were given an intramuscular injection of Endoxan as nitrogen mustard derivatives 10mg. per 40gm of body weight. In order to investigate effects of Endoxan to the teeth of rats the control and experimental rats group wee sacrificed on 1,3,5,7 and 14days, and made preparation for histopathologic findings. The rusults were as follows: 1. In several days (about 5days) after injection of Endoxan, tooth germs of cap stage, bell stage, and dental lamina were irregular arranged form as compared with in the control group teeth. 2. Irregular arranged cell were recovered from 14days after injection of Endoxan.

• Asian Pacific Journal of Cancer Prevention
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• v.14 no.6
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• pp.3429-3436
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• 2013

Cervical cancer is a major health problem worldwide and is the most frequent cause of cancer in women in India. Early detection and affordable drugs with clinical efficacy have to go hand-in-hand in order to comprehensibly address this serious health challenge. Plant-based drugs with potent anticancer effects should add to the efforts to find a cheap drug with limited clinical side effects. Keeping this very purpose in mind, an attempt has been made in this review to explore the potential of plant extracts or constituents known to exhibit antitumorigenic activity or exert cytotoxic effect in human cervical carcinoma cells. Alkaloids such as those isolated from C. vincetoxicum and T. Tanakae, naucleaorals A and B, isolated from the roots of N. orientalis, (6aR)-normecambroline, isolated from the bark of N. dealbata appear promising in different human cervical carcinoma cells with the $IC_{50}$ of 4.0-8 ${\mu}g/mL$. However, other compounds such as rhinacanthone and neolignans isolated from different plants are not far behind and kill cervical cancer cells at a very low concentrations. Among plant extracts or its constituents that enhance the effect of known anticancer drugs, noni, derived from the plant M. citrifolia perhaps is the best candidate. The cytotoxic potency and apoptotic index of cisplatin was found to significantly enhanced in combination with noni in different human cervical carcinoma cells and it therefore holds significance as promising herbal-based anticancer agent. However, efficacy needs to be further investigated in various cervical cell lines and more importantly, in in vivo cervical cancer models for possible use as an alternative and safe anticancer drug.

• Journal of Ginseng Research
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• v.42 no.2
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• pp.133-143
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• 2018

Background: AD-2 (20(R)-dammarane-3b, 12b, 20, 25-tetrol; 25-OH-PPD) is a ginsenoside and isolated from Panax ginseng, showing anticancer activity against extensive human cancer cell lines. In this study, effects and mechanisms of 1C ((20R)-3b-O-(L-alanyl)-dammarane-12b, 20, 25-triol), a modified version of AD-2, were evaluated for its development as a novel anticancer drug. Methods: MTT assay was performed to evaluate cell cytotoxic activity. Cell cycle and levels of reactive oxygen species (ROS) were determined using flow cytometry analysis. Western blotting was employed to analyze signaling pathways. Results: 1C concentration-dependently reduces prostate cancer cell viability without affecting normal human gastric epithelial cell line-1 viability. In LNCaP prostate cancer cells, 1C triggered apoptosis via Bcl-2 family-mediated mitochondria pathway, downregulated expression of mouse double minute 2, upregulated expression of p53 and stimulated ROS production. ROS scavenger, N-acetylcysteine, can attenuate 1C-induced apoptosis. 1C also inhibited the proliferation of LNCaP cells through inhibition on $Wnt/{\beta}-catenin$ signaling pathway. Conclusion: 1C shows obvious anticancer activity based on inducing cell apoptosis by Bcl-2 family-mediated mitochondria pathway and ROS production, inhibiting $Wnt/{\beta}-catenin$ signaling pathway. These findings demonstrate that 1C may provide leads as a potential agent for cancer therapy.

• The Korean Journal of Ecology
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• v.17 no.4
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• pp.523-531
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• 1994

Optimal conditions for the seed germination and growth of Hedyotis diffusa were studied. As photoperiod was increased from 12 hr to 24hr, the germination rate of Hedyotis diffusa was gradually increased. The photoperiod and temperature inflenced on the fermination synergistically. After the growth of 20 weeks under the natural condition (June~Oct.), the length of H. diffusa was $38.9{\pm}4.2cm$ (15.5~52.5cm), and total dry weight per $3.3m^2$ was $316.7{\pm}10.3g$. It is considered that H. diffusa could be cultivated in a part of inland. The anticancer effect of H. diffusa extract was examined. F-344 rats aged 6 weeks were divided into 3 groups and were given an I.P. of diethylnitrosamine at 200mg/kg body weight as a promoter, initially. And in two weeks after the beginnign of the experiment, group 1 was supplied iwth feed containing 0.02% 2-AAG as a promoter for 6 weeks. Group 2 was supplied with feed containing extracts of H.diffusa (0.02%) for two weeks. Group3 was supplied with only basal diet. All rats were sacrificed for partial hepatectomu, and the antipromoting effect was examined by the number 문 area per $cm^2$ of foci in river. In group 1, the number of hyperplastic nodule was $18.5{\pm}7.7$, but in group2, it was drastically reduced to $10.3{\pm}1.8$ rather thn those of group1. The total area of nodules $(mm^2)$ /whole liver $(cm^2)$ of group 1 and group2 were $19.2{\pm}7.7$ and $5.0{\pm}3.2$, respectively. These results indicate that extract of H.diffusa act as an anticancer agent at statistically significant level (p<0.001).

• Asian Pacific Journal of Cancer Prevention
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• v.14 no.11
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• pp.6761-6767
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• 2013

The nuclear receptor, peroxisome proliferator-activated receptor gamma ($PPAR{\gamma}$), is expressed in various cancer cells including breast, prostate, colorectal and cervical examples. An endogenous ligand of $PPAR{\gamma}$, 15-deoxy-${\Delta}^{12,14}$ prostaglandin $J_2$ (PGJ2), is emerging as a potent anticancer agent but the exact mechanism has not been fully elucidated, especially in breast cancer. The present study compared the anticancer effects of PGJ2 on estrogen receptor alpha ($ER{\alpha}$)-positive (MCF-7) and $ER{\alpha}$-negative (MDA-MB-231) human breast cancer cells. Based on the reported signalling cross-talk between $ER{\alpha}$ and $ER{\alpha}$, the effect of the $ER{\alpha}$ ligand, $17{\beta}$-estradiol (E2) on the anticancer activities of PGJ2 in both types of cells was also explored. Here we report that PGJ2 inhibited proliferation of both MCF-7 and MDA-MB-231 cells by inducing apoptotic cell death with active involvement of mitochondria. The presence of E2 potentiated PGJ2-induced apoptosis in MCF-7, but not in MDA-MB-231 cells. The $ER{\alpha}$ antagonist, GW9662, failed to block PGJ2-induced activities but potentiated its effects in MCF-7 cells, instead. Interestingly, GW9662 also proved capable of inducing apoptotic cell death. It can be concluded that E2 enhances $ER{\alpha}$-independent anticancer effects of PGJ2 in the presence of its receptor.