• Journal of Life Science
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• v.33 no.1
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• pp.15-24
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• 2023

To examine the antitumor effect of proso millet grains, whether proso millet grains exert apoptotic activity against human cancer cells was investigated. When the cytotoxicity of 80% ethanol (EtOH) extract of proso millet grains was tested against various cancer cells using MTT assay, more potent cytotoxicity was observed against human breast cancer MDA-MB-231 cells than against other cancer cells. When the EtOH extract was evaporated to dryness, dissolved in water, and then further fractionated by sequential extraction using four organic solvents (n-hexane, methylene chloride, ethyl acetate, and n-butanol), the BuOH fraction exhibited the highest cytotoxicity against MDA-MB-231 cells. Along with the cytotoxicity, TUNEL-positive apoptotic nucleosomal DNA fragmentation and several apoptotic responses including BAK/BAX activation, mitochondria membrane potential (Δψm) loss, mitochondrial cytochrome c release into the cytosol, activation of caspase-8/-9/-3, and degradation of poly (ADP-ribose) polymerase (PARP) were detected. However, human normal mammary epithelial MCF-10A cells exhibited a significantly lesser extent of sensitivity compared to malignant MDA-MB-231 cells. Irrespective of Fas-associated death domain (FADD)-deficiency or caspase-8-deficiency, human T acute lymphoblastic leukemia Jurkat cells displayed similar sensitivities to the cytotoxicity of BuOH fraction, excluding an involvement of extrinsic apoptotic mechanism in the apoptosis induction. These results demonstrate that the cytotoxicity of BuOH fraction from proso millet grains against human breast cancer MDA-MB-231 cells is attributable to intrinsic apoptotic cell death resulting from BAK/BAX activation, and subsequent mediation of mitochondrial damage-dependent activation of caspase cascade.

• Korean Journal of Medicinal Crop Science
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• v.13 no.4
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• pp.199-205
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• 2005

This study was carried out to investigate the effect of 70% ethanol extract and each fraction from Rhododendron brachycarpum D. Don leaves on cytotoxicity, anticancer, genotoxicity and immunological activity in vitro bioassay. Cytotoxicity for human normal cells (HEL299 and Chang) of the samples was shown below 35% in 0.5 mg/ml concentration of samples except aqueous fraction by SRB assay. DNA damage on the Chang cell of the samples alone in comet assay was observed very weak damage activity even in high concentration (1 mg/ml) of the samples. The anticancer effect of the samples on human cancer cell lines (A549, AGS, Hep3B, MCF7) was indicated that the cancer cells were inhibited gradually in proportion to the increase of the concentration of the samples by MTT assay. The growth of the Raji and Jurkat cells were hastened by adding butanol fraction among the samples. In the genotoxicity on $H_2O_2-induced$ DNA damage in Chang cells using alkaline comet assay, most of samples were shown a strong protective activity from DNA OTM values.

• Korean Journal of Medicinal Crop Science
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• v.26 no.1
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• pp.42-54
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• 2018

Background: Allergic diseases like such as atopic dermatitis, asthma, and rhinitis have recently increased both domestically and globally. The present study was undertaken to select candidates with anti-allergic activity from plant resources. Methods and Results: Fifty-six plant extracts at $20{\mu}g/m{\ell}$ were screened against ${\beta}$-hexosaminidase production and interleukin (IL)-4 release in degranulated rat basophilic leukemia (RBL)-2H3 cells. The anti-allergy activity of three plant extracts selected from the preliminary screening experiment, Polygonatum sibiricum F. Delaroche (root), Pyrus pytifolia var. culta (Makino) Nakai (leaf), and Rehmannia glutinosa (Gaertn.) Libosch. ex Steud (root) were measured at concentrations of $2-250{\mu}g/m{\ell}$ in three cell lines as RBL-2H3, HaCaT and Jurkcat T cells. The assay showed the root extract of R. glutinosa to have an inhibitory activity of 4.2% - 28.6% on ${\beta}$-hexosaminidase production from IgE-sensitized RBL-2H3 cells. Each extract of P. sibiricum and R. glutinosa reduced IL-4 release in IgE-sensitized RBL-2H3 cells, respectively. The leaf extract of P. pyrifolia var. culta showed a significantly potent suppressive effect of 10.2% - 74.7% on the mRNA expression of tumor necrosis factor (TNF)-${\alpha}$ in HaCaT cells sensitized with TNF-a and INF-g, and showed inhibitory effect of -8.6% - 90.9% on the mRNA expression of IL-2 in Jurkat T cells sensitized with PMA and A23187. Conclusions: The results showed that the root of R. glutinosa and leaf of P. pyrifolia var. culta could be useful candidates as antiallergy materials.

• Biomolecules & Therapeutics
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• v.27 no.5
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• pp.492-501
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• 2019

Nitrogen-containing heterocycles such as quinoline, quinazolinones and indole are scaffolds of natural products and have broad biological effects. During the last years those structures have been intensively synthesized and modified to yield new synthetic molecules that can specifically inhibit the activity of dysregulated protein kinases in cancer cells. Herein, a series of newly synthesized isoquinolinamine (FX-1 to 8) and isoindoloquinazolinone (FX-9, FX-42, FX-43) compounds were evaluated in regards to their anti-leukemic potential on human B- and T- acute lymphoblastic leukemia (ALL) cells. Several biological effects were observed. B-ALL cells (SEM, RS4;11) were more sensitive against isoquinolinamine compounds than T-ALL cells (Jurkat, CEM). In SEM cells, metabolic activity decreased with $10{\mu}M$ up to 26.7% (FX-3), 25.2% (FX-7) and 14.5% (FX-8). The 3-(p-Tolyl) isoquinolin-1-amine FX-9 was the most effective agent against B- and T-ALL cells with IC50 values ranging from 0.54 to $1.94{\mu}M$. None of the tested compounds displayed hemolysis on erythrocytes or cytotoxicity against healthy leukocytes. Anti-proliferative effect of FX-9 was associated with changes in cell morphology and apoptosis induction. Further, influence of FX-9 on PI3K/AKT, MAPK and JAK/STAT signaling was detected but was heterogeneous. Functional inhibition testing of 58 kinases revealed no specific inhibitory activity among cancer-related kinases. In conclusion, FX-9 displays significant antileukemic activity in B- and T-ALL cells and should be further evaluated in regards to the mechanisms of action. Further compounds of the current series might serve as templates for the design of new compounds and as basic structures for modification approaches.

• Microbiology and Biotechnology Letters
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• v.28 no.2
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• pp.97-104
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• 2000

Screening of Biologically Active Essential Oils from Ligusticum tenuissimum. Kim, Min-Hae, Young-Gil Kim, Jin-Ha Lee, Keo-Pyo Hong, Jung-Ki Hong, Young-Joon Kong, and Hyeon-Yong Lee*. Division of Food and Biotechnology, Kangwon National University, Chunchon 200-701, Korea, 1 Regional Crop Development Station, Kangwon Agricultural Research & Extension Services, Chunchon 200-150, Korea-The biological activities of the crude essential oils from Ligusticum tenuissimum and the control(phthalic anhydride) were compared. About 60% of the growth of MCF7, A549, and Rep3B cells were inhibited by adding 1.0 mg/ml of the crude essential oils and below 40% was observed by the control. Cytotoxicity on human normal lung cell(IMR90) was scored as 34.4% for the crude oil and 26.4% for control, respectively. It was found that the crude essential oils were more effective than the control in anti mutagenecity tested by both Rec-assay and CRG V79 cells. The growth of human T-cell(Jurkat) was enhanced up to 1.21 times by adding the crude essential oil compared with the control. 50% of a-glucosidase activity was inhibited by both the crude essential oil and the control. ACE activities were inhibited 80.1 % and 65.3% by adding 1.0 mg/ml of the crude oil and the control, respectively. The higher enhancement of glutathione-S-transferase activity was observed in the crude oil than those in the control: 301 % v.s 234% at 1.0 mg/ml of the treatment. Thrombolytic activity was measured as 42.9% and 28.6% for the crude oil and the standard, respectively. The effect of the oil on the nerve cells PCI2, was observed as follows: the neurite of PCl2 cells was lengthened up to 255 /-lm longer than 205 /-lm of control. The number of neurite-bearing cells were about two times higher than control. The survival ratio of the crude essential oil was also increased up to 56.4% which was about two fold higher than in control.