• Macromolecular Research
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• v.15 no.7
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• pp.646-655
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• 2007

To achieve targeted drug delivery for chemotherapy, a ligand-mediated nanoparticulate drug carrier was designed, which could identity a specific receptor on the surfaces of tumor cells. Biodegradable poly(ethylene oxide)/poly$({\varepsilon}-caprolactone)$ (PEG/PCL) amphiphilic block copolymers coupled to biotin ligands were synthesized with a variety of PEG/PCL compositions. Block copolymeric nanoparticles harboring the anticancer drug paclitaxel were prepared via micelle formation in aqueous solution. The size of the biotin-conjugated PEG/PCL nanoparticles was determined by light scattering measurements to be 88-118 nm, depending on the molecular weight of the block copolymer, and remained less than 120 nm even after paclitaxel loading. From an in vitro release study, biotin-conjugated PEG/PCL nanoparticles containing paclitaxel evidenced sustained release profiles of the drug with no initial burst effect. The biotin-conjugated PEG/PCL block copolymer itself evidenced no significant adverse effects on cell viability at $0.005-1.0{\mu}g/mL$ of nanoparticle suspension regardless of cell type (normal human fibroblasts and HeLa cells). However, biotin-conjugated PEG/PCL harboring paclitaxel evidenced a much higher cytotoxicity for cancer cells than was observed in the PEG/PCL nanoparticles without the biotin group. These results showed that the biotin-conjugated nanoparticles could improve the selective delivery of paclitaxel into cancer cells via interactions with over-expressed biotin receptors on the surfaces of cancer cells.

• Journal of Physiology & Pathology in Korean Medicine
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• v.17 no.3
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• pp.711-718
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• 2003

Wanpae-tang is suggested to have antitumor activity on lung cancer. This study was performed to investigate antitumor, immune response, and apoptotic effects by Wanpae-tang in the cancer cell lines and C57BL/6 mice. Experimental studies were progressed through the anticancer activities such as, survival time, cell cytotoxicity, natural killer cell activity, productivity of interleukins and apoptotio effects. The results were summarized as follows: 1. Median survival time of Wanpae-tang treated group was prolonged to 4.1%, as compared with control group, but was not significant. 2. On the MTT assay, half-maximal inhibitory concentration(IC50) of Wanpae-tang was 15.00 ㎎/㎖ in HeLa cell, and 4.158 ㎎/㎖ in HRT-18 cell. 3. Natural killer cell activity in Wanpae-tang treated group was decreased in case of 100:1 and 10:1 effect cell/target cell ratio. 4. Production of interleukin-2, 4, 12 in Wanpae-tang treated group were significantly increased. 5. On the studies of Wanpae-tang induced apoptosis, a DNA fragmentation patterns were not appeared.

• The Journal of the Korea Contents Association
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• v.21 no.11
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• pp.518-527
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• 2021

This study verifies the polyphenol and flavonoid contents of a dried extract, as well as its antioxidant effect and growth inhibitory effect on cancer cells to investigate the potential of yellow cherry tomatoes as a physiologically active food material. The polyphenol and flavonoid contents were determined as 10.96 ± 1.57 and 4.12 ± 0.41 mg/g, respectively. The antioxidant activity was confirmed by measuring DPPH and ABTS radical scavenging ability, and RC50-the concentration that reduces free radicals by 50%-were determined as 490.83 ± 17.35 ㎍/mL and 355.90 ± 0.79 ㎍/mL, respectively. The dried extract showed no cytotoxicity with respect to normal hepatocytes (Chang) and no growth inhibitory activity with respect to A549 lung cancer cells, whereas dried extract showed growth inhibitory activities of 15.2% and 18.4% with respect to human cervical adenocarcinoma (HeLa) and human hepatocellular carcinoma (HepG2) cells, respectively, when treated with a concentration at 100㎍/mL. The results of this study confirm the potential of yellow cherry tomatoes as a physiologically active food material by verifying their antioxidant activity and their growth inhibitory activity with respect to cervical and liver cancer cells.

• Journal of Apiculture
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• v.34 no.3
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• pp.245-254
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• 2019

We investigated the anti-tumor effects and molecular mechanism of Brazil, China and Korean regional propolis on HeLa ovarian cancer cell line. Each propolis extracts was prepared by ethanol extraction method. Cytotoxicity of propolis extracts was determinated by EZ-cytox cell viability assay. To necessity of anti-tumor effect and molecular mechanism of propolis, we must be adjusting propolis concentration. Due to 100 ㎍/mL of propolis extract were reduced cell viability to less than 50%, we adjusted all of propolis concentration to 100 ㎍/mL. By Western blotting analysis, we confirmed that anti-tumor mechanism of Brazil, China and Korea regional propolis has significantly difference. All of propolis was activated apoptosis related molecules such as PARP, caspase-3. However, cell proliferation signaling molecules including Akt1, ERK and Bcl-2 were reduced the protein expression level. Especially, the expression of tumor suppressor protein p53 was significantly increased in propolis-treated group such as Gyeonggi, Chungbuk, Chungnam, Jeonbuk, Gyeongnam and China. The phosphorylation of Bax which as apoptosis indicator was appeared in propolis-treated group such as Gyeonggi, Gangwon, Chungnam, Gyeongbuk, China. In this results showed that the regional propolis has completely different mechanism in anti-tumor. Thus, propolis extracts may be useful source of functional materials on anti-cancer and it will be able to choose the suitable propolis for cancer therapy by analyzing individual characteristics.

• Journal of Nutrition and Health
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• v.38 no.7
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• pp.503-511
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• 2005

In this study we investigated the biological activity of Chondria Crassicaulis (CC) on the human cancer cells. CC was extracted with methanol and further fractionated into four different types: hexane (CCMH), methanol (CCMM), butanol (CCMB), and aqueous (CCMA) partition layers. We determined the cytotoxic effect of these layers on human cancer cells by MTT assay. Among various partition layers of CC, the CCMM and CCMB showed the strong cytotoxic effects at 150 ${\mu}g$/ml which resulted $98.91\%$, $92.96\%$ on HeLa cell lines and $95.47\%$, $77.05\%$ on MCF-7 cell lines. And, the anti-proliferative effect of CC was accompanied by a marked inhibition of cyclooxygenase (COX-2), Caspase-3 and IAP (cIAP-1, cIAP-2 and XIAP) protein and concomitant induction of p53, p21 and Survivin protein. However, CC did not affect the level of Bax, Bcl-2 and Bcl-XL- protein. Also, we observed quinone reductase (QR) induced effects in all fraction layers of CC on HepG2 cells. The QR induced effects of the CCMH and CCMM on HePG2 cells at 120 ${\mu}g$/mL concentration indicated 3.73 and 2.45 with the control value of 1.0. Although further studies are needed, the present work suggests that CC may be a chemopreventive agent for the treatment of human cancer cells.

• Journal of Nutrition and Health
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• v.38 no.4
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• pp.307-312
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• 2005

We investigated the growth inhibitory effects of Atrina pecitinata (AP) on the proliferation in human cancer cell lines in vitro. AP was extracted with methanol which was further fractionated into four different types: methanol (APMM), haxane (APMH), butanol (APMB), and aquous layers (APMA). Among various partition layers, the APMM showed the strongest cytotoxic effects on all cancer cell lines which we used. In the MTT assay of AP fractions, the growth inhibitory effects was increased in proportion to its concentration. We observed quinone reductase (QR) induced effects in all fraction layers of AP on HepG2 cells. The QR induced effects of APMM on HepG2 cell at 80 $\mu$g/mL concentration indicated 2.0 with a control value of 1.0.

• Journal of the Korean Society of Food Science and Nutrition
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• v.37 no.4
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• pp.416-421
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• 2008

This study was performed to determine the antimutagenic and anticytotoxic effects of soybean paste (doenjang) added deep sea water salt and see tangle in Salmonella Typhimurium TA98, TA100 and human cancer cell lines. In the Ames test, methanol extract of doenjang did not exhibit any mutagenicity but showed substantial inhibitory effects against mutation induced by N-methyl-N'-nitro-N-nitrosoguanidine (MNNG) and 4-nitroquinoline-1-oxide (4NQO). The methanol extracts of doenjang ($200{\mu}g$/plate) added deep sea salt and see tangle (doenjang C) showed approximately 89.1% and 70% inhibitory effect on the mutagenesis induced by MNNG and 4NQO against TA100 strain, whereas 84.4% inhibitions were observed on the mutagenesis induced by 4NQO against TA98 strain. The cytotoxic effects of doenjang methanol extracts against the cell lines with human cervical adenocarcinoma (HeLa), human hepatocellular carcinoma (Hep3B), human gastric carcinoma (AGS), human lung carcinoma (A549) and human breast adenocarcinoma (MCF-7) were inhibited with the increase of the extract concentration. The treatment of 1.0 mg/mL doenjang C of methanol extracts showed strong cytotoxicities of 71%, 74.4%, 66.2%, 77.3%, and 71.2% against HeLa, Hep3B, AGS, A549, and MCF-7, respectively. In contrast 1 mg/mL treatment of doenjang C methanol extracts had only $10{\sim}40%$ cytotoxicity on normal human embryonal kidney cell (293). Doenjang methanol extract inhibited significantly the tumor growth in mice injected sarcoma-180 cells. Especially, doenjang C methanol extract showed an inhibition of tumor cell activity of 33% by the administration of 25 mg/kg methanol extracts.

• BMB Reports
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• v.41 no.5
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• pp.369-375
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• 2008

Polygonatum cyrtonema Lectin (PCL), which is classified as a monocot mannose-binding lectin, has received great regards for its uniquely biological activities and potentially medical applications in cancer cells. This paper was initially aimed to study apoptosis of PCL on Hela cells. Thus, 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) method was carried out. Through observation of cell morphologic changes and Lactate dehydrogenase (LDH) activity-based cytotoxicity assays, PCL induced HeLa cell apoptosis in a dose-dependent manner. To further gain structural basis, multiple alignments, homology modeling and docking experiments were performed to analyze the correlation between its biological activities and mannose-binding sites. Eventually, considering docking data, chemical modification properties on the three mannose-binding sites were analyzed by a series of biological experiments (e.g., hemagglutinating and mitogenic activity assays, fluorescence and Circular Dichrosim (CD) spectroscopy) to profoundly identify the role of some key amino acids in the structure-function relationship of PCL.

• Journal of Microbiology and Biotechnology
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• v.29 no.1
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• pp.171-177
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• 2019

Parasitic infections have remained a significant burden on human and animal health. In part, this is due to lack of clinically-approved, novel antimicrobials and a lack of interest by the pharmaceutical industry. An alternative approach is to modify existing clinically-approved drugs for efficient delivery formulations to ensure minimum inhibitory concentration is achieved at the target site. Nanotechnology offers the potential to enhance the therapeutic efficacy of drugs through modification of nanoparticles with ligands. Amphotericin B, nystatin, and fluconazole are clinically available drugs in the treatment of amoebal and fungal infections. These drugs were conjugated with gold nanoparticles. To characterize these gold-conjugated drug, atomic force microscopy, ultraviolet-visible spectrophotometry and Fourier transform infrared spectroscopy were performed. These drugs and their gold nanoconjugates were examined for antimicrobial activity against the protist pathogen, Acanthamoeba castellanii of the T4 genotype. Moreover, host cell cytotoxicity assays were accomplished. Cytotoxicity of these drugs and drug-conjugated gold nanoparticles was also determined by lactate dehydrogenase assay. Gold nanoparticles conjugation resulted in enhanced bioactivity of all three drugs with amphotericin B producing the most significant effects against Acanthamoeba castellanii (p < 0.05). In contrast, bare gold nanoparticles did not exhibit antimicrobial potency. Furthermore, amoebae treated with drugs-conjugated gold nanoparticles showed reduced cytotoxicity against HeLa cells. In this report, we demonstrated the use of nanotechnology to modify existing clinically-approved drugs and enhance their efficacy against pathogenic amoebae. Given the lack of development of novel drugs, this is a viable approach in the treatment of neglected diseases.

• Journal of the Korean Society of Food Science and Nutrition
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• v.37 no.4
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• pp.410-415
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• 2008

This study was performed to observe the antimutagenic and cytotoxic activities of methanol extract of kochujang added with sea tangle and deep sea water salts (SDK) and kochujang added with sea tangle (SK) using the Ames test and SRB assay, respectively. The direct antimutagenic effect of SDK and SK methanol extracts were examined by Ames test using Salmonella Typhimurium TA98 and TA100. In the Ames test, methanol extract of SDK and SK alone did not exhibit mutagenicity and most of the samples showed high antimutagenic effects against mutation induced by N-methyl-N'-nitro-N-nitrosoguanidine (MNNG) and 4-nitroquinoline-1-oxide (4NQO). Methanol extract of SDK ($200{\mu}g$/plate) showed approximately 71.4% inhibitory effect on the mutagenesis induced by 4NQO against TA98 strain; whereas 56.1% and 83.6% inhibitions were observed on the mutagenensis induced by 4NQO and MNNG against TA100 strain. The cytotoxic effects of SDK and SK increased with increasing sample concentration against human cervical adenocarcinoma (HeLa), human hepatocellular carcinoma (Hep3B), human breast adenocarcinoma (MCF-7), human stomach adenocarcinoma (AGS), and human lung carcinoma (A549). The SDK at the concentration of 1 mg/ml showed cytotoxicities of 61.5%, 61.3%, 51.4%, 57.9% and 77.7% against HeLa, Hep3B, MCF-7, AGS and A549, respectively. In contrast 1 mg/ml treatment of SDK and SK methanol extract had only $2{\sim}38%$ cytotoxicity on human transformed primary embryonal kidney cell (293).