• Archives of Pharmacal Research
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• v.26 no.10
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• pp.778-784
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• 2003

N'-(1-alkyl-2,3-dihydro-2-oxo-1H-3-indolyliden)-4-pyridinecarboxylic acid hydrazide derivatives, 3(a-g), were synthesized in a trial to overcome the resistance developed with the therapeutic uses of isoniazid (INH). The lipophilicity of the synthesized derivatives supersedes that of the INH as expressed by Clog p values. The synthesized compounds and INH were tested against bovin, human sensitive and human resist strains of Mycobacterium tuberculosis. Compounds 3a, 3d, 3f and 3g with 1-unsubstituted, 1-propyl, 1-propynyl and 1-benzyl groups respectively exhibited equipotent growth inhibitory activity (MIC 10 $\mu$mol) against the tested strains as compared with INH however the later has no activity against human resist strain. Pharmacokinetic study revealed that the rate and extent of absorption of the tested derivatives (3d and 3f) significantly higher than that of INH (p＜0.05). The relative bioavailabilities ($F_R%$) were 183.15 and 443.25 for 3f and 3d respectively as compared to INH. These results preliminary indicate the possible use of the prepared derivatives for treatment of tuberculosis infections in order to overcome the resistance developed with INH.

• YAKHAK HOEJI
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• v.49 no.2
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• pp.174-179
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• 2005

The human skin is constantly exposed to environmental irritants such as ultraviolet, smoke, chemicals. Free radicals and reactive oxygen species (ROS) caused by these environmen tal facts play critical roles in cellular damage. These irritants are in themselves damaging to the skin structure but they also participate the immensely complex inflammatory reaction. The purpose of this study was to investigate the skin cell protective effect of Campsis grandiflora extract on the UVB-irradiated human dermal fibroblasts (HDFs). We tested free radical and superoxide scavenging effect in vitro. C. grandiflora extracts had potent radical scavenging effect by 82% at $100{\mu}g/ml$, respectively. For testing intracellular ROS scavenging activity the cultured HDFs were analyzed by increase in DCF fluorescence upon exposure to UVB 20 $MJ/cm^2$ after treatment of C.grandiflora extracts. The results showed that oxidation of CM-DCFDA was inhibited by C.grandiflora extracts effectively and C.grandiflora extracts has a potent free radical scavenging activity in UVB- irradiated HDFs. In ROS imaging using confocal microscope we visualized DCF fluorescence in HDFs directly. In conclusion, our results suggest that C.grandiflora can be effectively used for the prevention of UV-induced adverse skin reactions such as radical production, and skin cell damage.

• Korean Journal of Acupuncture
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• v.25 no.4
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• pp.89-104
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• 2008

Objectives : This study was undertaken to determine the in vitro antioxidant activity of the extract of Chilgitang herb-acupuncture solution (CHAS). Methods : The radical scavenging capacity was tested by 2,2-diphenyl-1-picryl-hydrazyl (DPPH), hypoxanthine-xanthine oxidase system, DCFH-DA assay, nitric oxide and peroxynitrite generating system. In addition, antioxidant activity on copper and AAPH mediated human low-density lipoprotein (LDL) oxidation was measured by using TBARS assay and relative electrophoretic mobility assay. The amount of total phenolic compounds was assayed by the Folin-Ciocalteu method. Results : CHAS revealed a potent scavenging activity on DPPH radical(82%), superoxide anions(73%), hydroxyl radical(63%), nitric oxide (99%) and peroxynitrite (99%). Moreover, CHAS showed a strong inhibitory effect (59%) on $FeCl_2$-ascorbic acid induced lipid peroxidation of rat liver homogenate. CHAS also markedly inhibited copper(81%) and AAPH(56%)-mediated LDL oxidation, and effectively suppressed the electrophoretic mobility during exposure of human LDL to copper ions. CHAS (82 mg/g) contained higher concentration of total phenolic compounds than that of water extract (45 mg/g) obtained from Chilgitang. Conclusions : These results indicate that CHAS may protect against ROS- or RNS involved diseases, including cardiovascular diseases.

• Molecules and Cells
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• v.21 no.2
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• pp.213-217
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• 2006

Although AIMP1 (previously known as p43) is one of three auxiliary proteins bound to a macromolecular aminoacyl tRNA complex, it is also secreted as a cytokine controlling both angiogenesis and immune responses. Here we show that systemically administered purified recombinant human AIMP1 had anti-tumor activity in mouse xenograft models. In Meth A-bearing Balb/c mice, tumor volume increased about 28 fold in the vehicle treatment group, while an increase of about 16.7 fold was observed in the AIMP1-treated group. We also evaluated the anti-tumor activity of AIMP1 in combination with a sub-clinical dose of the cytotoxic anti-tumor drug, paclitaxel. The growth of NUGC-3 human stomach cancer cells was suppressed by 84% and 94% by the combinations of 5 mg/kg paclitaxel + 25 mg/kg AIMP1 (p = 0.03), and 5 mg/kg paclitaxel + 50 mg/kg AIMP1 (p = 0.02), respectively, while 5 mg/kg paclitaxel alone suppressed growth by only 54% (p = 0.02). A similar cooperative effect of AIMP1 and paclitaxel was observed in a lung cancer xenograft model. These results suggest that AIMP1 may be useful as a novel anti-tumor agent.

• KSBB Journal
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• v.18 no.1
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• pp.19-24
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• 2003

A purified substance was separated from marine alga, Chlorella capsulate. Immuno-stimulatory activity was measured by observing the growth of human immune T and B cells. The growth of human T and B cells was enhanced by up to about 1.4 times by adding the fraction from C. capsulata, compared with commercially available CGF extracts from the fresh water alga, C. vulgaris. The secretion of TNF-a and IL-6 was also enhanced up to about 1.5 times by adding the separated fraction. Adding 0.4 g/L of the extract increased the production of nitric oxide from macrophages by 1.6 fold. 50% of the AGS cell growth was inhibited by adding 0.4 g/L of the water extracted sample.

• Korean Journal of Food Science and Technology
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• v.51 no.4
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• pp.393-397
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• 2019

Proteasome inhibitors can promote apoptosis and cell cycle arrest in cancer cells by inhibition of nuclear factorkappaB ($NF-{\kappa}B$) activation. The purpose of this study was to investigate the effects of persimmon leaf extract (PSE) on proteasome activity in HepG2 human liver cancer cells. PSE treatment inhibited the proteasome activity and $NF-{\kappa}B$ activation in a dose-dependent manner in HepG2 human liver cancer cells (p<0.05). PSE treatment increased the population of cells in G2/M and sub-G1 phases. The results suggested that PSE is one of the candidate substances that may be developed into a proteasome inhibitor.

• Korean Journal of Pharmacognosy
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• v.51 no.4
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• pp.264-269
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• 2020

The study aimed to characterize chemical composition and anticancer property of the n-hexane fraction derived from Asiasari Radix et Rhizoma. The anticancer activity was evaluated on a panel of cancer cell lines including HN22, HSC2, HSC3, and HSC4 cells (human oral cancer), HCC827 and HCC827GR cells (human lung cancer), and KYSE30 and KYSE450 (human esophageal cancer) by MTS assay. As a result, The least polar subfraction from n-hexane-soluble layer displayed notable cytotoxicity on the tumor cell lines with IC50 ranging from 1.20 to 17.0 ㎍/ml. The chemical composition of constituents in the active subfraction was determined by gas chromatography-mass spectrometry (GC-MS). The essential oils comprised of sesquiterpenes including β-gurjunene (7.45%), γ-amorphene (6.61%), guaia-6,9-diene (6.40%), δ-guaiene (5.21%) and a phenylpropanoid, safrole (0.49%) were mainly identified in addition to long-chain hydrocarbons including n-heptadecane (24.60%), 7-hexadecene (4.44%) and a diterpenoid, ent-kaur-16-ene (6.57%).

• Journal of Korea Multimedia Society
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• v.24 no.3
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• pp.416-422
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• 2021

Due to the large differences in human activity within classes, the large similarity between classes, and the problems of visual angle and occlusion, it is difficult to extract features manually, and the detection rate of human behavior is low. In order to better solve these problems, an improved Faster R-CNN-based detection algorithm is proposed in this paper. It achieves multi-object recognition and localization through a second-order detection network, and replaces the original feature extraction module with Dense-Net, which can fuse multi-level feature information, increase network depth and avoid disappearance of network gradients. Meanwhile, the proposal merging strategy is improved with Soft-NMS, where an attenuation function is designed to replace the conventional NMS algorithm, thereby avoiding missed detection of adjacent or overlapping objects, and enhancing the network detection accuracy under multiple objects. During the experiment, the improved Faster R-CNN method in this article has 84.7% target detection result, which is improved compared to other methods, which proves that the target recognition method has significant advantages and potential.

• Journal of Marine Bioscience and Biotechnology
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• v.14 no.2
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• pp.93-101
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• 2022

Hizikia fusiforme, a type of brown algae, is widely used in Asian cuisine. It has been reported to have various pharmacological effects. In this study, the effects of the ethanol extract from H. fusiforme (EAHF) on the proliferation of human colon carcinoma cells were investigated. The effect on the survival of human hepatocarcinoma and colon carcinoma cells was examined, and results revealed that the anti-proliferative effects of EAHF were higher in colon carcinoma cells than in hepatocarcinoma cells. The inhibition of proliferation of HT29 colon carcinoma cells by EAHF treatment was closely related to the induction of apoptosis. EAHF treatment also increased caspase activity and poly(ADP-ribose) polymerase degradation, induced mitochondrial dysfunction, altered Bcl-2 family protein expression, and increased the rate of cytochrome c released from the mitochondria into the cytoplasm. Furthermore, the production of reactive oxygen species (ROS) was markedly stimulated by EAHF treatment, and when ROS production was blocked, EAHF-induced cytotoxicity was significantly attenuated. These results indicate that the anticancer activity of EAHF in HT29 colon carcinoma cells was induced by ROS-dependent mitochondrial impairment. While EAHF exhibited potent anticancer activity in colon carcinoma cells in this study, further studies on the active components of EAHF and their efficacy should be performed.

• Analytical Science and Technology
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• v.36 no.2
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• pp.70-79
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• 2023

The synthesis of the Mannich base as a ligand (L) N-(morpholino (phenyl) methyl) acetamide is the subject of this study. Elemental analyses, FT-IR spectra, UV-vis, ¹H-NMR, and magnetic measurements were used to confirm the synthesis of the [Ni(L)₂]Cl₂ complex, thermal analysis (TG/DTG), atomic absorption, and scanning, and structurally explained as electron microscopy (SEM), and X-ray powder diffraction (XRD) methods. The melting point of the complex and its molar conductivity were also measured. The suggested geometries of the complexes formed have a tetrahedral structure, according to the data acquired using various techniques. Theoretical approaches to the complex formation have been investigated. For molecular mechanics and semi-empirical calculations, the HYPERCHEM6 program had been used. The effect of the novel Ni(II) complex on the cancer cell Hepa-2 (human hepatocellular ademocarcinoma), that is the human laryngeal cancer, was studied. It has been found that these ligand and complex have potent effects on the cancer cell. The antibacterial activity of the free ligand and its complex was evaluated against two kinds of human pathogenic bacteria. The first category is Gram-positive (Staphylococcus aureas, epiderimids), whereas the second group is Gram-negative (Psedamonas aeruginosa, Escherichia coli) (from the diffusion method). Finally, it was discovered that various chemicals had varied growth-inhibiting effects on bacteria.