• Journal of information and communication convergence engineering
• /
• v.14 no.1
• /
• pp.40-44
• /
• 2016

The device coupling between the stacked top/bottom field-effect transistors (FETs) in two types of monolithic 3D inverter (M3INV) with/without a metal layer in the bottom tier is investigated, and then the regime of the thickness T_ILD and dielectric constant ε_r of the inter-layer distance (ILD), the doping concentration N_d (N_a), and length L_g of the channel, and the side-wall length L_SW where the stacked FETs are coupled are studied. When N_d (N_a) < 10¹⁶ cm^-3 and L_SW < 20 nm, the threshold voltage shift of the top FET varies almost constantly by the gate voltage of the bottom FET, but when N_d (N_a) > 10¹⁶ cm^-3 or L_SW > 20 nm, the shift decreases and increases, respectively. M3INVs with T_ILD ≥ 50 nm and ε_r ≤ 3.9 can neglect the interaction between the stacked FETs, but when T_ILD or ε_r do not meet the above conditions, the interaction must be taken into consideration.

• Proceedings of the PSK Conference
• /
• 2003.10b
• /
• pp.91.2-91.2
• /
• 2003

Cyclin-dependent kinases (CDKs) regulate the cell division cycle, apoptosis, transcription and differentiation. Inhibition of CDK is a promising target in development of anti-cancer agents. An indirubin analog (AGM01l), a CDK inhibitor, is a synthetic compound that inhibits human cancer cell growth in vitro. AGM01l showed a potent cytotoxicity in cultured human cancer cell lines (IC$\sub$50/ = 5.43 ${\mu}$M for A549, human colon cancer cell; IC$\sub$50/ = 1.21 ${\mu}$M for SNU-638, human stomach cancer cell; IC$\sub$50/ 9.23 ${\mu}$M for HL-60, human leukemia cell). (omitted)

• The Journal of Korean Medicine
• /
• v.43 no.1
• /
• pp.33-41
• /
• 2022

Objectives: Drug-induced blockade of the human ether-à-go-go related gene (hERG) potassium ion channel causes acquired long QT syndrome, which is known to cause cardiac arrhythmias and be fatal. To establish safety evidence of herbal formulae, we evaluated the effects of 31 herbal formulae on hERG channel activity. Methods: The current through hERG channel was measured by changing the membrane voltage before and after treatment with 31 herbal formulae in HEK 293 cell overexpressing hERG channel using a whole-cell patch clamp system. The current-voltage curves and the activity curves were fitted, and the hERG activity and 50% inhibitory concentration (IC₅₀) according to each herbal formula were calculated. Results: Chokyungjongok-tang, Oncheong-eum, and Cheongsangbangpung-tang strongly inhibited the hERG activity, with IC₅₀ values of 67.67, 141.2, and 296.3 ㎍/mL, respectively. Yeonkyopaedok-san, Eunkyo-san, Ukgan-san gajinphibanha, Daegunjoong-tang (except Oryzae gluten), Insamyangyoung-tang, Banhahubak-tang, SokyungHwalhyul-tang, Jodeung-san, Hyeonggaeyeongyo-tang, and Bangkeehwangkee-tang weakly inhibited hERG activity, with IC₅₀ values ranging from 400 to 1000 ㎍/mL. The other 18 herbal formulae showed very weak hERG activity inhibition of less than 50% at the highest concentration (1000 ㎍/mL). Conclusion: This study provided safety information on cardiotoxicity by cardiac arrhythmia risk assessment of herbal formulae, and is expected to be a reference data for predicting the safety and risk of herbal formulae.

• Herbal Formula Science
• /
• v.31 no.1
• /
• pp.11-19
• /
• 2023

Objectives : The purpose of this study was to examine the effects of herbal medicines on pacemaker potentials of large intestinal interstitial Cells of Cajal (ICC) in mice. Methods : We made the ICC culture in large intestine in mice and used the electrophysiological method to record pacemaker potentials. Also we used MTT assay to check cell viability and examined the ICC protein expression by western blot. Results : 1.Glycyrrhiza uralensis Fischer (GF) (50-150 ㎍/ml) induced pacemaker depolarization and decreased frequency with concentration-dependent manners. EC₅₀ is 58.95 ㎍/ml. Angelica gigas (AG) (50-200 ㎍/ml) induced pacemaker depolarization and decreased frequency with concentration-dependent manners. EC₅₀ is 77.22 ㎍/ml. Poncirus fructus (PF) (10-100 ㎍/ml) induced pacemaker depolarization and decreased frequency with concentration-dependent manners. EC₅₀ is 13.39 ㎍/ml. Citrus unshiu S. Marcov. (CU) (10-500 ㎍/ml) induced pacemaker depolarization and decreased frequency with concentration-dependent manners. EC₅₀ is 139.80 ㎍/ml. Gardenia jasminoides J. Ellis (GJ) (100-500 ㎍/ml) induced pacemaker depolarization and decreased frequency with concentration-dependent manners. EC₅₀ is 78.70 ㎍/ml. Coptis chinensis (CC) (100-1000 ㎍/ml) induced pacemaker depolarization and decreased frequency with concentration-dependent manners. EC₅₀ is 138.10 ㎍/ml. Scutellaria baicalensis (SB) (10-100 ㎍/ml) had no effects on pacemaker potentials and decreased frequency with concentration-dependent manners. IC₅₀ is 18.34 ㎍/ml. Atractylodes macrocephala koidzumi (AM) (10-100 ㎍/ml) induced pacemaker hyperpolarizations and decreased frequency with concentration-dependent manners. IC₅₀ is 18.54 ㎍/ml. 2. PF, SB and AM had no effects on cell death in large ICC. 3. PF increased the ANO1 and c-kit protein expression and SB and AM increased the c-kit protein expression in large ICC. Conclusions : These results suggest that PF, SB, and AM are likely to be the optimal combination of herbal medicines that can be used to treat diseases such as gastrointestinal motility disorders such as irritable bowel syndrome.

• Korean Journal of Pharmacognosy
• /
• v.50 no.4
• /
• pp.245-252
• /
• 2019

This study was initially explored to procure biomaterials capable of inhibiting cancer cell growth from nine Persicaria species (Polygonaceae). The extract of P. nepalensis that was selected from the initial screenings was further fractionated to identify bioactive compounds. The ethyl acetate (EtOAc) fraction was shown to be the most active in the inhibition of cell growth against six cancer cell lines (IC₅₀ value of 3.77-12.87 ㎍/ml). Phytochemical study led to the isolation of two galactolipids of 1,2-di-O-linolenoyl-3-O-β-D-galactospyranosyl-sn-glycerol (1) and 1-O-linolenoyl-3-O-β-D-galactospyranosyl-sn-glycerol (2) from the hexane fraction and three phenylpropanoyl sucroses of lapathoside A (3), vanicoside B (4) and lapathoside C (5) from the EtOAc fraction. These isolated compounds have not been reported from this plant. Compounds 3 and 4 exhibited the effective growth inhibition against a panel of cancer cell lines (IC₅₀ value of 6.90-18.09 μM). In addition, the anti-inflammatory activity was evaluated to determine lipopolysaccharide (LPS)-induced nitric oxide (NO) formation in RAW264.7 mouse macrophage cells. The EtOAc fraction (IC₅₀; 34.14 ㎍/ml) and its constituents, 3 (8.55 μM) and 4 (7.83 μM) were shown to be effective in the inhibition of LPS-induced NO production. Therefore, compounds 3 and 4 were considered to be active constituents for anti-inflammatory and antitumor activity from P. nepalensis.

• Journal of Korean Neurosurgical Society
• /
• v.64 no.6
• /
• pp.864-872
• /
• 2021

Objective : The aim of our study is to investigate the cytotoxic, antioxidant, and antimicrobial effects of newly synthesized boron compounds in U87MG glioblastoma cell treatment. Methods : We synthesized boron glycine monoester (BGM) and boron glycine diester (BGD) structures containing boron atoms and determined their cytotoxic activities on glioblastoma by the MTT method. The inhibitory concentration 50 (IC₅₀) value was calculated with GraphPad Prism 5.0 program. The IC₅₀ values were administered 48 hours on U87MG glioblastoma cell. Catalase (CAT), acid phosphatase (ACP) and alkaline phosphatase (ALP) enzyme activity, malondialdehyde (MDA), total glutathione (GSH), and total protein levels were detected using spectrophotometric methods. We determined the antimicrobial activities of BGM and BGD with the disc diffusion method. Results : After 48 hours of BGM and BGD application to U87MG glioblastoma cells, we found the IC₅₀ value as 6.6 mM and 26 mM, respectively. CAT and ACP enzyme activities were decreased in BGM and BGD groups. MDA which is a metabolite of lipid peroxidation was increased in both boron compounds groups. GSH level was reduced especially in BGD group. BGM and BGD have been found to be antimicrobial effects. Conclusion : Boron compounds, especially the BGM, can provide a new therapeutic approach for the treatment of glioblastoma with their anticancer, antioxidant, and antimicrobial effects.

• Biomolecules & Therapeutics
• /
• v.30 no.6
• /
• pp.520-528
• /
• 2022

Mast cells are an effector cell that plays a pivotal role in type I hypersensitive immune responses. Mast cells exist in connective tissues, such as skin and mucosal tissue, and contain granules which contain bioactive substances such as histamine and heparin in cells. The granules of mast cells are secreted by antigen stimulation to cause the type I allergic hypersensitivity. In addition, stimulated by antigen, mast cells synthesize and secrete various eicosanoids and cytokines. While AT9283 is known to have anticancer effects, the therapeutic effect of AT9283 on allergic disorders is completely unknown. In this study, it was found that AT9283 reversibly inhibited antigen-IgE binding-induced degranulation in mast cells (IC₅₀, approx. 0.58 μM) and suppressed the secretion of the inflammatory cytokines IL-4 (IC₅₀, approx. 0.09 μM) and TNF-α (IC₅₀, approx. 0.19 μM). For a mechanism of mast cell inhibition, while not inhibiting Syk phosphorylation, AT9283 suppressed the activation of LAT, a downstream substrate protein of Syk, in a dose-dependent manner. As expected, AT9283 also inhibited the activation of PLCγ1 and Akt, downstream signaling molecules of Syk/LAT, and MAP kinases such as JNK, Erk1/2, and P38. In an in vitro protein tyrosine kinase assay, AT9283 directly inhibited Syk activity. Next, AT9283 dose-dependently inhibited passive cutaneous anaphylaxis (PCA), an IgE-mediated allergic acute response, in mice (ED50, approx. 34 mg/kg, p.o.). These findings suggest that AT9283 has potential to use as a new drug for alleviating the symptoms of IgE-mediated allergic disorders.

• Journal of the Korean Society of Industry Convergence
• /
• v.26 no.1
• /
• pp.47-57
• /
• 2023

In this study, the bioactive activities (antioxidant activity, whitening activity, and anti-wrinkle effect) of dried tapioca-unhulled barley grain residue (TUDDG) obtained after alcohol fermentation, were measured. In the case of DPPH radical scavenging activity, the 50% ethanol extract of TUDDG showed the highest level of about 83% at the concentration of 100 mg/ml, and the ABTS radical scavenging activity was also about 98% of the 50% ethanol extract of TUDDG even at the concentration of 10 mg/mL. In the case of mushroom tyrosinase inhibitory activity, the 50% ethanol extract of TUDDG showed the highest activity at 100 mg/ml concentration of 37%. As a result of collagenage activity inhibition and elastase analysis, the 50% ethanol extract of TUDDG showed high activity with 4.2 mg/mL (IC₅₀) and 26.1 mg/mL (IC₅₀), respectively. Therefore, considering the physiological activity as well as the extraction efficiency of physiologically active substances, the 50% ethanol extract of TUDDG is judged to be highly effective.

• Natural Product Sciences
• /
• v.28 no.3
• /
• pp.115-120
• /
• 2022

Ten compounds, consisting of neoflavonoids (1-5), isoflavonoids (6 and 7), flavanone (8), and chalcones (9 and 10) were isolated from the ethyl acetate and n-butanol-soluble fractions of the heartwood of Dalbergia melanoxylon. The chemical structures were identified on the basis of spectroscopic evidence and compared to previously reported spectra. Compounds 1-10 were evaluated for cytotoxicity against HCT116 human colorectal cancer, MDA-MB-231 human metastatic breast cancer, and A2058 human melanoma cell lines. Among them, compounds 3 and 10 showed the strongest cytotoxic activity with IC₅₀ values of 11.92±1.07 μM, 10.83±1.02 μM, and 14.37±1.02 μM, 13.62±1.09 μM against HCT116 and MDA-MB-231 cell lines, respectively. Compounds 9 and 10 also had cytotoxic activity with IC₅₀ values of 13.49±1.18 μM and 9.82±0.91 μM against A2058 cell lines, respectively. To the best our knowledge, compounds 2 and 5-10 were isolated from this source for the first time.

• Journal of Microbiology and Biotechnology
• /
• v.30 no.6
• /
• pp.893-902
• /
• 2020

Propolis is a resinous substance that is collected by Apis mellifera from plant sources and is used in traditional medicine. To study the phytochemical constituents and apoptotic potential of Jordanian propolis extract against different cancer cell lines, propolis was extracted using methanol, hexane, and ethyl acetate and was fractionated using chromatographic methods. Cytotoxicity was assessed using MTT and LDH assays. The apoptotic potential was investigated using florescence microscopy, multicaspase assay, Annexin-V and dead cell assay, and cell cycle assay. The phytochemical constituents were analyzed using GC-MS. The methanol extract of propolis exhibited cytotoxic potential against all cell lines tested. The IC₅₀ values of the methanol extract were 47.4, 77.8, 91.2, and 145.0 ㎍/ml for HepG2, LoVo, MDAMB231, and MCF7 cell lines, respectively. The IC₅₀ values of the F1 fraction were 31.6 (MDAMB231), 38.9 (HepG2), 36.7 (LoVo) and 75.5 (MCF7) ㎍/ml. On further purification using thin-layer chromatography, the IC₅₀ values of the F1-3 fraction were found to be 84.31(HepG2), 79.2 (MCF7), 70.4 (LoVo), and 68.9 (MDAMB231) ㎍/ml, respectively. The anticancer potential of the F1 fraction was confirmed through the induction of apoptosis and cell cycle arrest at the G0/G1 phase. The GC-MS analysis of the F1 fraction revealed the presence of 3-methyl-4-isopropylphenol (29.44%) as a major constituent. These findings indicate the potential of propolis extract as a cancer therapy. However, further investigation is required to assess the acute and subacute toxicity of the most active fraction.