• Archives of Pharmacal Research
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• v.26 no.11
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• pp.925-928
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• 2003

Four guaia-12,6-olide type sesquiterpene lactones, aguerin B (1), 8$\alpha$-acetoxyzaluzanin C (2), cynaropicrin (3), and deacylcynaropicrin (4), were isolated from the flowers of Hemisteptia Iyrata Bunge. It is the first report on the isolation of compounds 1-4 from Hemisteptia species. All the isolates (1-4) were examined for their cytotoxic activity against SK-OV-3, LOX-IMVI, A549, MCF-7, PC-3, and HCT-15 human cancer cell lines.

• Archives of Pharmacal Research
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• v.24 no.5
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• pp.397-401
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• 2001

In the search for new naturally occurring angiogenic inhibitory we found that culture broths from two unidentified fungal strains exerted potent inhibitory activities on capillary-like tube formation of human umbilical vein endothelial cells (HUVEC) in vitro. Two active compounds were isolated by bioassay-guided separation and their structures were identified as gliotoxin (1) and its derivative methylthiogliotoxin (2) by spectroscopic analyses. These compounds significantly inhibited the migration of HUVEC assessed by in vitro wounding migration assay and exhibited at least 10 times more potent inhibition of proliferation of HUVECs as compared with that of cancer cell lines such as HeLa, MCF-7, and KB 3-1 cells. Especially, gliotoxin having disulfide group exerted more potent activities than methylthiogliotoxin, suggesting that gliotoxin could be a useful compound for further study as an anti-angiogenic agent.

• Macromolecular Research
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• v.17 no.1
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• pp.19-25
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• 2009

In order to enhance the gene delivery efficiency and decrease the cytotoxicity of polyplexes, we synthesized Solutol-g-PEI by conjugating polyethyleneimine (PEI) to Solutol (polyoxyethylene (10) stearate), and evaluated its efficiency as a possible nonviral gene carrier candidate. Structural analysis of synthesized polymer was performed by using $^1H$-NMR. Gel retardation assay, particle sizes and zeta potential measurement confirmed that the new gene carrier formed a compact complex with plasmid DNA. The complexes were smaller than 150 nm, which implicated its potential for intracellular delivery. It showed lower cytotoxicity in three different cell lines (Hela, MCF-7, and HepG2) than PEI 25 kDa. pGL3-lus was used as a reporter gene, and the transfection efficiency was in vitro measured in Hela cells. Solutol-g-PEI showed much higher transfection efficiency than unmodified PEI 25 kDa.

• Journal of Integrative Natural Science
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• v.5 no.1
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• pp.46-52
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• 2012

Mulberry extracts can be incorporated into skin-whitening products. The compound attributed to lighten the skin is arbutin, a form of hydroquinone that inhibits melanin release by suppressing the tyrosinase enzyme. For the cosmetic applications, the physiological effects of mulberry (Morus alba) extracts were investigated. The water soluble fraction of mulberry contains higher amount of protein (16.28~4.47%) in contrast to fat (1.55~1.41%). In addition, the fraction abundantly contains succinic acid (972.4-275.8 mg/g) and phosphoric acid (1,628.4-121.9 mg/g) in different parts of mulberry. The free radical scavenging ability in water soluble fraction was found to display remarkable effects in comparison with methanol and ethyl acetate fraction. The ethyl acetate-soluble of root and leaf showed remarkable tyrosinase inhibition activity by IC 50 (${\mu}g/ml$). The anticancer activity of methanol fraction obtained from mulberry using human cancer cell lines showed growth inhibition effect (270.14 mg/ml in Calu-6 cells, 295.29 mg/ml in HCT-116, and 332.29 mg/ml in MCF-7 cells, respectively). Based on the results, Morus alba extracts include cosmetic ingredients with antioxidizing and whitening properties.

• Journal of Microbiology and Biotechnology
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• v.34 no.2
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• pp.240-248
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• 2024

In cancer treatment, multi-target approach has paid attention to a reasonable strategy for the potential agents. We investigated whether (E)-2-methoxy-4-(3-(4-methoxyphenyl) prop-1-en-1-yl) phenol (MMPP) could exert an anticancer effect by dual-regulating VEGFR2 and PPARγ. MMPP showed modulating effects in TNBC type (MDA-MB-231 and MDA-MB-468) and luminal A type (MCF7) breast cancer cell lines. MMPP enhanced PPARγ transcriptional activity and inhibited VEGFR2 phosphorylation. MMPP-induced signaling by VEGFR2 and PPARγ ultimately triggered the downregulation of AKT activity. MMPP exhibited anticancer effects, as evidenced by growth inhibition, inducement of apoptosis, and suppression of migration and invasion. At the molecular level, MMPP activated pro-apoptotic proteins (caspase3, caspase8, caspase9, and bax), while inhibiting the anti-apoptotic proteins (bcl2). Additionally, MMPP inhibited the mRNA expressions of EMT-promoting transcription factors. Therefore, our findings showed molecular mechanisms of MMPP by regulating VEGFR2 and PPARγ, and suggested that MMPP has potential to treat breast cancer.

• Journal of Applied Biological Chemistry
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• v.52 no.4
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• pp.180-186
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• 2009

Whole plants of Vitex rotundifolia were extracted for 2 days with methylene chloride ($CH_2Cl_2$) followed by extraction of the residue for an additional 2 days. The same procedure was also applied using methanol (MeOH). The two crude extracts were combined and partitioned between $CH_2Cl_2$ and $H_2O$. The organic layer was further partitioned between n-hexane and 85% aq. MeOH, and the aqueous layer was also further fractionated with n-BuOH and $H_2O$, successively. From the 85% aq. MeOH fraction, one compound was isolated through the repeated HPLC. According to the results of physicochemical data including NMR and MS, the chemical structure of the compound was determined as artemetin (1). The antiproliferative effects of the crude extracts, fractions, and compound against HT1080, AGS, MCF-7 and HT-29 human cancer cells were compared with the control by using MTT assay. In the comparative analysis, the 85% aq. MeOH fraction exhibited the strongest antiproliferative effects on human cancer cell lines in a dose-dependent manner (p<0.05). In addition, exposure of compound 1 isolated from 85% aq. MeOH fraction led to strong antiproliferative effect in HT1080 cancer cell lines. These results suggest that the extracts and compound isolated from V. rotundifolia may be used as potential chemopreventive and chemotherapeutic agents.

• Korean Journal of Medicinal Crop Science
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• v.11 no.1
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• pp.53-61
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• 2003

Cirsium japonicum var. ussuriense were extracted with methanol and then fractionated with nhexane, EtOAc and BuOH to get active fractions. And their antioxidant and antimicrobial activities in each fraction were determined. Ethyl acetate and butanol fraction of Cirsium japonicum var. ussuriense showed strong antioxidant activities, but hexane fraction did not show any activities. But in the antimicrobial test, Ethyl acetate fraction showed strong antimicrobial activities except to Aspergillus awamori, Asperigillus niger. Especially, Ethyl acetate fraction showed the strongest activities against Bacillus subtilis. And aqueous fraction showed the strongest activities against Cladosporium herbarum, Hypocrea nigricans. This study was performed to determine the antimutagenic and cytotoxic effect of Cirsium japonicum var. ussuriense methanol extract on Salmonella typhimurium TA98, TA100 and cancer cell lines using Ames test and cytotoxicity assay, respectively. Cancer cell lines include human lung carcinoma(A549), human breast adenocarcinoma(MCF-7) and human hepatocellular carcinoma (Hep3B). Futher fractionations with hexane, ethyl acetate, butanol and water from methanol extract of Cirsium japonicum var. ussuriense were performed to obtain effective fraction, methanol extract showed 60.14% inhibition effect on the mutagenesis induced by MNNG against TA100, while 77% and 72.5% inhibition was observed on the mutagenesis induced by 4NQO against TA98 and TA100, respectively. and methanol extract showed 82.25% and 73.7% inhibitory effect on the mutagenesis induced by Trp-P-1 against TA98 and TA100, respectively. methanol extract showed the strongest effect against A549, MCF-7 and Hep3B at the same concentration compared to those of other fration.

• Korean Journal of Medicinal Crop Science
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• v.14 no.1
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• pp.1-7
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• 2006

This research was conducted to investigate the possibilities of usage of germinated-buckwheat (Fagopyrum esculentum $M{\ddot{o}}ench$) by examining antioxidative, antimicrobial and cytotoxic effects of extracts from different germinated root length of buckwheat. Antioxidant activity $(RC_{50})$ was shown higher in extracts of non-germinated seed $(50.41\;{\mu}g/mL)$ and root length 10 mm $(80.57\;{\mu}g/mL)$, 2 mm $(93.77\;{\mu}g/mL)$, 5 mm $(107.09\;{\mu}g/mL)$ than BHT $(163.96\;{\mu}g/mL)$ as a synthetic antioxidant. In antimicrobial activity, non-germinated and germinated seeds were formed inhibitory zone against S. aureus $(4{\sim}10\;mm)$, P. aeruginosa $(2{\sim}9\;mm)$ at the concentrations of $10{\sim}40\;mg/mL$ but B. subtilis, E. coli and S. typhimurium were not apparent antimicrobial activity. Extracts of germinated seed also decreased their antimicrobial activity compared to non-germinated seed extract. In addition, the growth of Calu-6 was inhibited of both 5 mm root length germinated and non-germinated seeds $(800\;{\mu}g/mL)$ as 95.12% and 87.15%, respectively, but these did not show any influence on cytotoxic effect against MCF-7 and Caco-2 cell lines. Extracts of 2 mm and 5 mm germinated seeds were also inhibited against Calu-6 and SNU-601 cell lines.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2018.04a
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• pp.94-94
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• 2018

The gold (LC-AuNPs) and silver (LC-AgNPs) nanoparticles were rapidly synthesized by fruit extract of Lycium chinense within 1.15 and 25 min respectively in an eco-friendly way. The synthesized nanoparticles confirmed by relevant surface plasmon resonance peaks for gold and silver nanoparticles at 536 and 480 nm, respectively. FE-TEM results revealed that LC-AuNPs were 20-50 nm and LC-AgNPs were 50-100 nm. The maximum distribution of gold, silver elements and the crystallographic nature of synthesized were confirmed using EDX, elemental mapping and XRD. LC-AgNPs showed inhibitory activity against pathogenic microorganisms such as E. coli and S. aureus, whereas LC-AuNPs did not show inhibitory activity. The LC-AgNps nanoparticles exhibited significant cytotoxicity to human breast cancer MCF7 cell line and less cytotoxicity to non-diseased RAW264.7 (murine macrophage) cells whereas LC-AuNps showed minimal toxicity to both cell lines. In-depth research on this rapid, facile and greenery nanoparticles may play a potential role in biomedical applications.

• Journal of Microbiology and Biotechnology
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• v.32 no.5
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• pp.551-563
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• 2022

L-asparaginase (E.C. 3.5.1.1) purified from bacterial cells is widely used in the food industry, as well as in the treatment of childhood acute lymphoblastic leukemia. In the present study, the Burkholderia pseudomallei L-asparaginase gene was cloned into the pGEX-2T DNA plasmid, expressed in E. coli BL21 (DE3) pLysS, and purified to homogeneity using Glutathione Sepharose chromatography with 7.26 purification fold and 16.01% recovery. The purified enzyme exhibited a molecular weight of ~33.6 kDa with SDS-PAGE and showed maximal activity at 50℃ and pH 8.0. It retained 95.1, 89.6%, and 70.2% initial activity after 60 min at 30℃, 40℃, and 50℃, respectively. The enzyme reserved its activity at 30℃ and 37℃ up to 24 h. The enzyme had optimum pH of 8 and reserved 50% activity up to 24 h. The recombinant enzyme showed the highest substrate specificity towards L-asparaginase substrate, while no detectable specificity was observed for L-glutamine, urea, and acrylamide at 10 mM concentration. THP-1, a human leukemia cell line, displayed significant morphological alterations after being treated with recombinant L-asparaginase and the IC₅₀ of the purified enzyme was recorded as 0.8 IU. Furthermore, the purified recombinant Lasparaginase improved cytotoxicity in liver cancer HepG2 and breast cancer MCF-7 cell lines, with IC₅₀ values of 1.53 and 18 IU, respectively.