• Bulletin of the Korean Chemical Society
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• v.35 no.8
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• pp.2375-2380
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• 2014

In the present investigation, a series of some novel 1,3-diaryl/heteroarylprop-2-en-1-one derivatives (3a-j) have been synthesized and evaluated for their in vitro cytotoxicity against three cancer cell lines, two hepatocarcinoma cell lines HUH-7, Hep-3b and one leukemia cancer cell line MOLT-4. Based on these results, structure-activity relationship (SAR) was studied on modification of $R^1$ and $R^2$ to identify the compound with maximum potency. Amongst the compounds, 3b and 3d strongly inhibited the growth of Hep-3b and MOLT-4 cells with $IC_{50}$ value of 3.39 and $3.63{\mu}M$ respectively. The results obtained from the inhibitory study had further been supported by the reactive oxygen species (ROS) measurement using flow cytometry in MOLT-4 cells. These observations collectively reveal that compounds comprising 1,3-diarylprop-2-en-1-one framework with pyrazole ring at position-3 and heteroaryl/aryl substituents at position-1 can be used as promising anticancer agents.

• Progress in Superconductivity and Cryogenics
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• v.15 no.2
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• pp.24-28
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• 2013

In this study, the homogeneity of critical current, $I_c$, along the lengthwise direction in the coated conductor (CC) tape under uniaxial tension was investigated using a multiple voltage tap configuration. Initially, a gradual and homogeneous $I_c$ degradation occurred in all subsections of the tape up to a certain strain value. This was followed by an abrupt $I_c$ degradation in some subsections, which caused scattering in $I_c$ values along the length with increasing tension strain. The $I_c$ degradation behaviour was also explained through n-value as well as microstructure analyses. Subsections showed $I_c$ scattering corresponding to damaged areas of the CC tape revealed that transverse cracks were distributed throughout the gauge length. This homogeneous $I_c$ degradation behaviour under tension is similar with the case under torsion strain but different with the case under hard bending which were previously reported. This behaviour is also different with the case using Bi-2223 HTS tapes under tension strain.

• Asian Pacific Journal of Cancer Prevention
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• v.13 no.5
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• pp.2095-2100
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• 2012

Sulforaphane (SFN) an isothiocyanate formed by hydrolysis of glucosinolates found in Brassica oleraceae is reported to possess anticancer and antioxidant activities. In this study, we isolated SFN from red cabbage (Brassica oleraceae var rubra) and evaluated the comparative antiproliferative activity of various fractions (standard SFN, extract and purified SFN) by MTT assay in human epithelial carcinoma HEp -2 and and Vero cells. Probable apoptotic mechanisms mediated through p53, bax and bcl-2 were also examined. The SFN fraction was collected by HPLC, enriched for its SFN content and confirmed. Expression of apoptosis-related proteins was detected by western blotting and RT PCR. Results showed that Std SFN and purified SFN concentration found to have closer $IC_{50}$ which is equal to 58.96 microgram/ml (HEp-2 cells), 61.2 microgram/ml (Vero cells) and less than the extract which is found to be 113 microgram/ml (HEp-2 cells) and 125 microgram/ml (Vero cells). Further studies on apoptotic mechanisms showed that purified SFN down-regulated the expression of bcl-2 (antiapoptotic), while up-regulating p53 and Bax (proapoptotic) proteins, as well as caspase-3. This study indicates that purified SFN possesses antiproliferative effects the same as Std SFN and its apoptotic mechanism in HEp-2 cells could be mediated through p53 induction, bax and bcl-2 signaling pathways.

• Korean Journal of Pharmacognosy
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• v.43 no.3
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• pp.239-242
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• 2012

This study was carried out to investigate the anti-malarial activity of Juniperus chinensis by in vitro and in vivo system using Plasmodium falciparum chloroquine-sensitive(3D7) and P. falciparum chloroquine-resistant(S20) strains. According to cytotoxicty test on NIH 3T3 cell, the ethanol extract(EtOH), ethylacetate(EtOAc) fraction and aqueous fraction possessed significant anti-malarial activity against both 3D7 and S20 strains at non-toxic concentrations(<100 /). In vitro assay, EtOAc fraction showed notable activity against 3D7 and S20 strains of P. falciparum with $IC_{50}$ values of $37{\pm}2{\mu}g/ml$ and $36{\pm}6{\mu}g/ml$. In animal test using P. falciparum infected human erythrocytes, the treatment of EtOAc fraction significantly inhibited parasitaemia in mice in a dose-dependent manner that is parasitaemia of 42%, 34% and 31% in doses of 10 mg/kg, 20 mg/kg and 40 mg/kg, respectively. The study provides data to support the medicinal importance of the J. chinensis.

• Journal of Ginseng Research
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• v.41 no.4
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• pp.496-502
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• 2017

Background: Ginsenosides are the major components of Panax ginseng Meyer, an herbal medicine used for the treatment of various diseases. Different ginsenosides contribute to the biological properties of ginseng, such as antimicrobial, anticancer, and immunomodulatory properties. In this study, we investigated the antiviral effects of 15 ginsenosides and compound K on gammaherpesvirus. Methods: The antiviral activity of ginsenosides was examined using the plaque-forming assay and by analyzing the expression of the lytic gene. Results: 20(R)-Ginsenoside Rh2 inhibited the replication and proliferation of murine gammaherpesvirus 68 (MHV-68), and its half-maximal inhibitory concentration ($IC_{50} $) against MHV-68 was estimated to be $2.77{\mu}M$. In addition, 20(R)-ginsenoside Rh2 inhibited 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced lytic replication of human gammaherpesvirus in the Kaposi's sarcoma-associated herpesvirus (KSHV)-positive cell line BC3. Conclusion: Our results indicate that 20(R)-ginsenoside Rh2 can inhibit the replication of mouse and human gammaherpesviruses, and thus, has the potential to treat gammaherpesvirus infection.

• JSTS:Journal of Semiconductor Technology and Science
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• v.5 no.4
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• pp.255-261
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• 2005

With the advent of sub-90nm technologies, the system-on-chip (SoC) and system-in-package (SiP) are becoming the trend in delivering low-cost, low-power, and small-form-factor consumer electronic systems running at multiple GHz. The shortened transistor channel length reduces the transistor switching cycles to the range of several picoseconds, yet the time-of-flights of the critical on-chip and off-chip interconnects are in the range of 10 picoseconds for 1.5mm-long wires and 100 picoseconds for 15mm-long wires. Designers realize the bottleneck today often lies at chip-to-chip interconnects and the industry needs a good model to compute the inductance in these parts of circuits. In this paper we propose a new method for extracting accurate equivalent inductance circuit models for SPICE-level circuit simulations of system-on-chip (SoC) and system-in-package (SiP) designs. In our method, geometrical meshes are created and numerical methods are used to find the solutions for the electromagnetic fields over the fine meshes. In this way, multiple-GHz SoC and SiP designers can use accurate inductance modeling and interconnect optimization to achieve high yields.

• Archives of Pharmacal Research
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• v.17 no.3
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• pp.135-138
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• 1994

Acyclonucleoside homologues of 1-$(\omega$-cyabnoalkyl)-and 1, 3-bis $(\omega$-cyanoalkyl) uracils were synthesized by the series of alkylation reactions of uracil with the $\omega$-chloroalkyl nitrile ${(Cl-(CH}_2)_n$-CN;n=1, 2, 3, 4) in DMSO under $50-70^circ{C}$ temperature. The 1-$(\omega$-cyanoalkyl)-and 1, 3-bis$(\omega$-cyanoalkyl) uracils were separated either by the fractional crystallization or column chromatography. The antitumor activities for these synthesized compounds were determined against four cell lines (J-82 cell, P388 cell, FM-3A cell and U-937 cell lines). These compounds failed to exhibit any significant antitumor activity.

• YAKHAK HOEJI
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• v.44 no.2
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• pp.149-154
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• 2000

Flavin mononucleotide (1,4-butanediamine) Pt(II) complex (7FMN) was synthesized and screened anticancer activity [J. Pharm. Soc. Korea 43(6),762-770 (1999)]. 7FMN have good water solubility and moderate anticancer activiy In this paper cell-cycle specificity and nephrotoxicity were studied. Interaction of DNA with cisplatin and synthesized 7FMN was analyzed by flow cytometry and showed G2 arrest in L1210 cell line. It means that cell-cycle on L1210 was inhibit in S phase by cisplatin and 7FMN. In order to biochemically analyze nephrotoxicity of cisplatin and 7FMN, after injecting each agent intraperitoneally, blood was exsanguinated after 6 hours, 1 day, 3 days and 7 days, respectively. Then, serum was separated from the blood. The serum level of BUN, creatinine and uric acid in cisplatin and 7FMN administated mice (25~35 g, ICR strain, a dose each 8,12 and 16 times of the $IC_{50}$/ value, cisplatin; 7 times) were determined by autochemistry analyzer. In cisplatinadministered mice group, BUN level was elevated than normal control group at 3rd day and repaired at 7th day. In 7FMN administrated group was not elevated. Creatinine and uric acid level were no difference with the normal control group. Therefore synthesized 7FMN is less toxic than cisplatin in nephrotoxiciaty.

• Archives of Pharmacal Research
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• v.22 no.2
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• pp.143-150
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• 1999

melatonin (MLT), N-acetyl-5-methoxytryptamine, is mainly secreted by the pineal gland. The ultraviolet (UV), infrared (IR) and 1H-NMR spectra of irradiated and non-irradiated MLT were measured, and phototoxicity tests of MLT, anthracence (positive control) and sodium lauryl sulfate (SLS, negative control) were performed. The methods employed include both in vitro test such as MTS assay using the human fibroblast cell and yeast growth inhibition assay using Candida albicans and in vivo method using the skin of guinea pig. UV absorption spectra and 1H-NMR spectra of MLT were changed by UVA (365 nm, 15 J/$\textrm{cm}^2$), but IR spectra of MLT were not changed. The fifty percent inhibitory concentration (IC50) ratio (UV-/UV+) of MLT was 10. The inhibition zone of irradiated-paper disks treated with MLT was not observed. According to the results of histophathological examination, no pathologic lesion was observed in the non-irradiated group, but slight degeneration of keratinocytes in the epidermis, homorrhage and vasodilation in dermis were observed in the irradiated group. These results indicated that the molecular structure of MLT is altered by UVA to unidentified photoproducts and a moderate phototoxicity of MLT is predicted.

• Archives of Pharmacal Research
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• v.27 no.7
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• pp.742-750
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• 2004

This paper for the first time reports the isolation of 5 compounds from Phellinus linteus. A sphingolipid (1) and two tyrosinase inhibitory compounds (2, 3) along with two carboxylic acids (4, 5), were isolated from the fruiting body of Phellinus linteus (Berk ＆ Curt) Aoshima. The structure of compound 1 was identified as 1-O-$\beta$-D-glucopyranosyl-(2S, 3R, 4E, 8E)-2-[(2R)-2-hydroxyhexadecanoylamino]-9-methyl-4,8-octadecadiene-1,3-diol, known as cerebroside B, based on spectroscopic methods such as 1D and 2D NMR as well as by acid hydrolysis. Compounds 2-5 were identified as protocatechualdehyde (2), 5-hydroxymethyl-2-furaldehyde (HMF) (3), succinic acid (4), and fumaric acid (5) based on the spectroscopic evidence. Compounds 2 and 3 inhibited the oxidation of L-tyrosine catalyzed by mushroom tyrosinase with an $IC_{50}$ of 0.40 and 90.8 $\mu\textrm{g}$/mL, respectively. The inhibitory kinetics, which were analyzed by the Lineweaver-Burk plots, were found to be competitive and noncompetitive inhibitors with a $K_{j}$ of 1.1 $\mu\textrm{m}$ and 1.4 mM, respectively.