• Journal of Ginseng Research
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• v.45 no.1
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• pp.48-57
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• 2021

Background: Ginsenoside Rh2 is well known for many pharmacological activities, such as anticancer, antidiabetes, antiinflammatory, and antiobesity properties. Glycosyltransferases (GTs) are ubiquitous enzymes present in nature and are widely used for the synthesis of oligosaccharides, polysaccharides, glycoconjugates, and novel derivatives. We aimed to synthesize new ginsenosides from Rh2 using the recombinant GT enzyme and investigate its cytotoxicity with diverse cell lines. Methods: We have used a GT gene with 1,224-bp gene sequence cloned from Lactobacillus rhamnosus (LRGT) and then expressed in Escherichia coli BL21 (DE3). The recombinant GT protein was purified and demonstrated to transform Rh2 into two novel ginsenosides, and they were characterized by nuclear magnetic resonance (NMR) techniques and evaluated by 3-(4, 5-dimethylthiazol-2-yl)-2-5-diphenyltetrazolium bromide assay. Results: Two novel ginsenosides with an additional glucopyranosyl (6→1) and two additional glucopyranosyl (6→1) linked with the C-3 position of the substrate Rh2 were synthesized, respectively. Cell viability assay in the lung cancer (A549) cell line showed that glucosyl ginsenoside Rh2 inhibited cell viability more potently than ginsenoside Rg3 and Rh2 at a concentration of 10 μM. Furthermore, glucosyl ginsenoside Rh2 did not exhibit any cytotoxic effect in murine macrophage cells (RAW264.7), mouse embryo fibroblasts cells (3T3-L1), and skin cells (B16BL6) at a concentration of 10 μM compared with ginsenoside Rh2 and Rg3. Conclusion: This is the first report on the synthesis of two novel ginsenosides, namely, glucosyl ginsenoside Rh2 and diglucosyl ginsenoside Rh2 from Rh2 by using recombinant GT isolated from L. rhamnosus. Moreover, diglucosyl ginsenoside Rh2 might be a new candidate for treatment of inflammation, obesity, and skin whiting, and especially for anticancer.

• Korean Journal of Medicinal Crop Science
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• v.13 no.4
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• pp.154-160
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• 2005

This study was performed to compare anticancer and immune activities between natural Artemisia capillaris Thunb. extract and tissue cultured plant extract (hairy root, in vitro culture, callus). The inhibitory effect of cancer cell growth, human B cell growth and productivity of cytokines were examined. Furthermore, HPLC analysis was performed to confirm the components. The anticancer activities increased by more than 55% with the cultured callus of Artemisia capillaris T. for four cancer cell lines(Lung carcunoma, Stomach adenocarcinoma, Hepatocillular carcinoma, Breast adenocarcinoma), showing higher effect than natural Artemisia capillaris T. The extracts from hairy root and in vitro culture of Artemisia capillaris T. significantly increased the immune B cell growth. The immune B cell growth effect of natural Artemisia capillaris T. was higher than that of the tissue culture plants such as hairy root, in vitro culture and callus. Both natural and tissue cultured plants showed similar effects on cytokine secretion. The similar peak size was observed between natural Artemisia capillaris T. and cultured callus in HPLC analysis. As a results, the biological activities were not observed the difference between natural Artemisia capillaris T. and cultured callus. Thus, the cultured callus will be altered natural Artemisia capillaris T. in the environmental side and the resources preservative side

• Journal of Environmental Science International
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• v.16 no.8
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• pp.995-999
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• 2007

This study assessed the characteristics of emission and cell toxicology of Methylethylketone(MEK) in ambient air of industrial area. MEK is produced by the oxidation of sec-butyl alcohol and used as the solvent for making ink, printing, coating of film, bonding material and drug extraction. The MEK concentrations in the ambient-air of industrial area in Gimhae City was detected in the range of $25.4{\sim}1,580{\mu}g/m^3$ with an average $297.4{\mu}g/m^3$. The concentration of MEK showed a descending tendency from April to August followed by its increased tendency since then. The effects of MEK on the human lung cancer A549 cells was examined by the generation of Reactive Oxygen Species(ROS) and cytotoxicity. The range of MEK concentration detected in the area induced ROS generation affecting the oxidation state with a little effects on the viability of the cells.

• Bulletin of the Korean Chemical Society
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• v.32 no.7
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• pp.2397-2404
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• 2011

Variable selection k nearest neighbor QSAR modeling approach was applied to a data set of 80 3-arylisoquinolines exhibiting cytotoxicity against human lung tumor cell line (A-549). All compounds were characterized with molecular topology descriptors calculated with the MolconnZ program. Seven compounds were randomly selected from the original dataset and used as an external validation set. The remaining subset of 73 compounds was divided into multiple training (56 to 61 compounds) and test (17 to 12 compounds) sets using a chemical diversity sampling method developed in this group. Highly predictive models characterized by the leave-one out cross-validated $R^2$ ($q^2$) values greater than 0.8 for the training sets and $R^2$ values greater than 0.7 for the test sets have been obtained. The robustness of models was confirmed by the Y-randomization test: all models built using training sets with randomly shuffled activities were characterized by low $q^2{\leq}0.26$ and $R^2{\leq}0.22$ for training and test sets, respectively. Twelve best models (with the highest values of both $q^2$ and $R^2$) predicted the activities of the external validation set of seven compounds with $R^2$ ranging from 0.71 to 0.93.

• Herbal Formula Science
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• v.10 no.2
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• pp.243-249
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• 2002

This study was performed to investigate the effects of fermented extract of Pinus densiflora (FPD) on oxygen radicals and $H_2O_2$-induced damage. The results are as follows: 1. The 1.1-diphenyl-2-picrylhydrazyl (DPPH) free radicals were considerably reduced by FPD and $IC_{50}$ value was showed the concentration of 20 ㎍／㎖. 2. The cytotoxicity did not observe by FPD treatment in A548 cells. 3. The $H_2O_2$-induced cell damage was recovered by FPD pretreatment in A549 cells. These results suggest that FPD, as a natural antioxidant, has scavenging effect of free radicals and protection effect from $H_2O_2$-induced cytotoxicity.

• Korean Journal of Medicinal Crop Science
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• v.17 no.2
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• pp.102-108
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• 2009

This study was performed to enhance anticancer activities of E. sinica, and A. gigas by ultra high pressure extraction process. The cytotoxicity of E. sinica and A. gigas on human kidney cell (HEK293) was as low as 24.94% and 25.3% in adding 1.0 $mg/m{\ell}$ of the sample extracted at 500 Mpa for 15 minute. Generally, the inhibition of cancer cell growth on A549 and MCF-7 was increased over 20% in the ultra high pressure samples, compared to the conventional extraction process. Under the extracts from ultra high pressure process showed not only the strongest anticancer activities, but also had better stability than normal extracts. It was also found that the extracts of A. gigas reduced the hypertrophy of the internal organs, such as adrenal and spleen caused stresses in several mouse models.

• KSBB Journal
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• v.14 no.5
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• pp.543-549
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• 1999

For development of an integrated calorimetric bio-reactor to measure the metabolic heat dissipated during cell growth, a 5 liter jar fermenter was modified to measure the pulse length of automatic temperature control signals to set heater on and off, and the to send them to computer to calculate the cumulative heat supplied. Cumulative heats for the calorimetric reactor in the absence of cell growth, were measured with varying conditions. The heat loss by the aeration was 30.9 kJ/vvm and the loss to ambient air was 10.5 kJ/L/hr/$^{\circ}C$. Cumulative heat was measued within $\pm$0.2% when testing with a small electri heater submerged in the reactor. Metabolic heat was measured to be 0.76 and 0.76 and 11.4kJ per g consumption of glucose during cultivation of S. cerevisiae and E. coli, respectively.

• Korean Journal of Pharmacognosy
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• v.34 no.4 s.135
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• pp.308-313
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• 2003

A bioassay-guided fractionation of the stem bark extract of Eucommia ulmoides Oliver (Eucommiaceae) led to the isolation of three iridoid constituents, genipin (1), geniposide (3), geniposidic acid (4) as well as $({\pm})-guaiacylglycerol$ (2) and fatty acid mixtures as active ingredients of the extract responsible for the antitumoral property. The EtOAc soluble part and BuOH soluble part of the extract demonstrated a potent inhibition on the proliferation of cultured human tumor cells such as A549 (non small cell lung), SK-OV-3 (ovary), SK-MEL-2 (melanoma), XF498 (central nerve system) and HCT-15 (colon) in vitro, whereas the remaining water soluble part exhibited a poor inhibition. The intensive investigation of the EtOAc soluble part and BuOH soluble part of the extract yielded genipin, guaiacylglycerol, geniposide, geniposidic acid and large amounts of fatty acid mixtures as active components.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.2
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• pp.611-616
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• 2014

Objectives: Dendritic cell (DC)-based tumor immunotherapy needs an immunogenic tumor associated antigen (TAA) and an effective approach for its presentation to lymphocytes. In this study we explored whether transduction of DCs with lentiviruses (LVs) expressing the human interleukin-12 gene could stimulate antigen-specific cytotoxic T cells (CTLs) against human lung cancer cells in vitro. Methods: Peripheral blood monocyte-derived DCs were transduced with a lentiviral vector encoding human IL-12 gene (LV-12). The anticipated target of the human IL-12 gene was detected by RT-PCR. The concentration of IL-12 in the culture supernatant of DCs was measured by ELISA.Transduction efficiencies and CD83 phenotypes of DCs were assessed by flow cytometry. DCs were pulsed with tumor antigen of lung cancer cells (DC+Ag) and transduced with LV-12 (DC-LV-12+Ag). Stimulation of T lymphocyte proliferation by DCs and activation of cytotoxic T-lymphocytes (CTL) stimulated by LV-12 transduced DCs pulsed with tumor antigen against A549 lung cancer cells were assessed with methyl thiazolyltetrazolium (MTT). Results: A recombinant lentivirus expressing the IL-12 gene was successfully constructed. DC transduced with LV-12 produced higher levels of IL-12 and expressed higher levels of CD83 than non-transduced. The DC modified by interleukin -12 gene and pulsed with tumor antigen demonstrated good stimulation of lymphocyte proliferation, induction of antigen-specific cytotoxic T lymphocytes and antitumor effects. Conclusions: Dendritic cells transduced with a lentivirus-mediated interleukin-12 gene have an enhanced ability to kill lung cancer cells through promoting T lymphocyte proliferation and cytotoxicity.

• Journal of Physiology & Pathology in Korean Medicine
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• v.19 no.4
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• pp.950-954
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• 2005

Phellinus linteus (Berk. & M.A. Curtis) Teng, commonly referred to as Sangwhang in Korea, is a well-known species of the genus Phellinus, which attracts great attention due to its phamarcological values. P. linteus has been reported to produce anti-tumor, anti-angiogenic, anti-mutagenic and immunomodulatory activities in vivo and in vitro. However, despite extensive biochemical studies on P. linteus, the wine produced by P. linteus fermentation (WPLF) has poorly investigated. In the present study, it was compared the in vitro cytotoxic effects of WPLF with ethanol as positive control. WPLF as well as ethanol induced the inhibition of cell proliferation and morphological changes in both HepG2 and A549 cells in a concentration-dependent manner, however, WPLG treatment has less cytotoxic effects than ethanol treatment. These cytotoxic effects were associated with the induction of apoptotic cell death, but, WPLG treatment has less apoptotisis inducing effects than ethanol treatment.