• Applied Biological Chemistry
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• 제43권2호
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• pp.148-152
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• 2000

뽕나무(Morus alba) 및 꾸지뽕나무(Cudrania tricuspidata)의 잎과 줄기 껍질의 수용성 추출물에 대하여 in vitro 실험계에서 항산화 활성을 비교 검토하였다. 성장기 마우스의 간장 microsome을 이용한 생체막 지질 과산화 억제정도는 꾸지뽕나무 줄기 껍질(53%)>뽕나무 줄기 껍질(43%)>꾸지뽕나무 잎(38%)>뽕나무 및(34%) 순으로 나타났다. Linoleic acid산화 실험계에서는 꾸지뽕나무 줄기 껍질과 뽕나무 잎의 추출물이 강한 항산화 활성을 나타내었으며, 꾸지뽕나무 줄기 껍질의 추출물은 반응 8일째까지 강한 활성을 보였다. TBA method에서는 뽕나무 줄기 껍질이 다른 것에 비해 약간 강한 활성을 보였으며, 또한 DPPH에 의한 수소공여능은 각 시료첨가 0.05%에서 뽕나무 잎>꾸지뽕나무 잎>통나무 줄기 껍질>꾸지뽕나무 줄기 껍질 순으로 나타나 및 추출물에서 비교적 수소공여 작용이 강하였다. 이들 추출물의 총 폴리페놀 화합물의 함량을 측정한 결과 뽕나무 잎(1.32%), 뽕나무 줄기 껍질(1.28%), 꾸지뽕나무 잎(1.34%), 꾸지뽕나무 줄기 껍질(1.30%)로 큰 차이가 없었다.

• 한국염색가공학회지
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• 제26권1호
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• pp.45-52
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• 2014

Red pine (Pinus densiflora) is widely used traditional medicine, pharmacological and nutritional values from which the phytochemical compounds are derived. The present study was aimed to examine the antibacterial effects in the absence and presence of a immature red pine cone extract against 13 microorganisms. The components in the aqueous extract from immature red pine cone were identified by GC-MS. About 1.4% of total polyphenolic compound was measured in aqueous extract collected from immature red pine cone. Also, the high concentration of ${\beta}$-phellenandrene, ${\alpha}$-pinene, limonene, bornyl acetate and aldehyde was detected in total ion chromatograms. Of total 13 microorganisms, 4 microorganisms including Pseudomonas aeruginosa, Vibrio cholera, Listeria monocytogenes, Klebsiella pneumonia were effectively killed by aqueous extract of immature red pine cone. The highest anti-bacterial effect was detected in P. aeruginosa, followed by V. cholera, L. monocytogenes and K. pneumonia. In case of P. aeruginosa, the largest diameter of inhibition zone was maintained to 1/2 solution treated cells and slightly decreased at 1/4 and 1/8 solution treated cells. Also, in test used V. cholera and L. monocytogenes, the inhibition zone was strongly formed in only 1 and 1/2 solution treated cells, while K. pneumonia showed the very small diameter of inhibition zone in all concentrations. Therefore, these results suggested that the aqueous extracts of immature red pine cone should be considered as a new and potentially important anti-bacterial substrate to effectively prevent the microbial infection and penetration.

• Asian Pacific Journal of Cancer Prevention
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• 제17권4호
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• pp.2291-2295
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• 2016

Small molecule tyrosine kinase inhibitors targeting HER 2 receptors have emerged as an important therapeutic approach in inhibition of downstream proliferation and survival signals for the treatment of breast cancers. Recent drug discovery efforts have demonstrated that naturally occurring polyphenolic compounds like delphinidin have potential to inhibit proliferation and promote apoptosis of breast cancer cells by targeting HER2 receptors. While delphinidin may thus reduce tumour size, it is associated with serious side effects like dysphonia. Owing to the narrow therapeutic window of delphinidin, the present study aimed to identify high affinity compounds targeting HER2 with safer pharmacological profiles than delphinidin through virtual screening approaches. Delphinidin served as the query parent for identification of structurally similar compounds by Tanimoto-based similarity searching with a threshold of 95% against the PubChem database. The compounds retrieved were further subjected to Lipinski and Verber's filters to obtain drug like agents, then further filtered by diversity based screens with a cut off of 0.6. The compound with Pubchem ID: 91596862 was identified to have higher affinity than its parent. In addition it also proved to be non-toxic with a better ADMET profile and higher kinase activity. The compound identified in the study can be put to further in vitro drug testing to complement the present study.

• The Korean Journal of Physiology and Pharmacology
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• 제20권3호
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• pp.269-277
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• 2016

Ellagic acid (EA), an antioxidant polyphenolic constituent of plant origin, has been reported to possess diverse pharmacological properties, including anti-inflammatory, anti-tumor and immunomodulatory activities. This work aimed to clarify the skin anti-photoaging properties of EA in human dermal fibroblasts. The skin anti-photoaging activity was evaluated by analyzing the reactive oxygen species (ROS), matrix metalloproteinase-2 (MMP-2), total glutathione (GSH) and superoxide dismutase (SOD) activity levels as well as cell viability in dermal fibroblasts under UV-B irradiation. When fibroblasts were exposed to EA prior to UV-B irradiation, EA suppressed UV-B-induced ROS and proMMP-2 elevation. However, EA restored total GSH and SOD activity levels diminished in fibroblasts under UV-B irradiation. EA had an up-regulating activity on the UV-B-reduced Nrf2 levels in fibroblasts. EA, at the concentrations used, was unable to interfere with cell viabilities in both non-irradiated and irradiated fibroblasts. In human dermal fibroblasts, EA plays a defensive role against UV-B-induced oxidative stress possibly through an Nrf2-dependent pathway, indicating that this compound has potential skin antiphotoaging properties.

• Asian Pacific Journal of Cancer Prevention
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• 제17권8호
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• pp.3865-3869
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• 2016

Curcumin, a polyphenolic compound isolated from the rhizomes of an herbaceous perennial plant, Curcuma longa, is known to possess anticancerous activity. However, the mechanism of apoptosis induction in cancers differs. In this study, we have (1) investigated the anticancerous activity of curcumin on REH and RS4;11 leukemia cells and (2) studied the chemo-sensitizing potential of curcumin for doxorubicin, a drug presently used for leukemia treatment. It was found that curcumin induced a dose dependent decrease in cell viability because of apoptosis induction as visualized by annexin V-FITC/ PI staining. Curcumin-induced apoptosis of leukemia cells was mediated by PARP-1 cleavage. An increased level of caspase-3, apoptosis inducing factor (AIF), cleaved PARP-1 and decreased level of Bcl2 was observed in leukemia cells after 24h of curcumin treatment. In addition, curcumin at doses lower than the $IC_{50}$ value significantly enhanced doxorubicin induced cell death. Therefore, we conclude that curcumin induces apoptosis in leukemia cells via PARP-1 mediated caspase-3 dependent pathway and further may act as a potential chemo-sensitizing agent for doxorubicin. Our study highlights the chemo-preventive and chemo-sensitizing role of curcumin.

• Preventive Nutrition and Food Science
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• 제13권4호
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• pp.299-305
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• 2008

This study compared the physicochemical properties of root hair of white ginseng (WG), root hair of tissue cultured mountain ginseng (MG), root hair of red ginseng (RG) and extruded ginseng samples. The comparison of crude ash and total sugar resulted insignificant differences between extruded and raw samples. MG had a higher content of crude ash, crude protein, amino acids and polyphenolic compound than WG and RG; the total sugar and reducing sugar were highest in RG. Crude fat and acidic polysaccharide in RG and WG were similar to and higher than MG. Crude saponin of treated samples WG1 (moisture content 25%, barrel temperature $110^{\circ}C$) and WG3 (moisture content 35%, barrel temperature $110^{\circ}C$) were 9.80% and 9.73%, respectively, which were the highest among ginseng samples. In conclusion, the extrusion process can be applied to red ginseng manufacturing, and some characteristics of MG were higher than in RG and WG.

• Biomolecules & Therapeutics
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• 제22권1호
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• pp.35-40
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• 2014

Resveratrol is a polyphenolic compound found in various natural products such as grapes and berries and possesses anti-cancer, anti-hyperlipidemia, and anti-aging properties. Recently, it has been reported that resveratrol inhibits ${\alpha}$-melanocyte-stimulating hormone signaling, viability, and migration in melanoma cells. However, these effects have not been confirmed in vivo, specifically brownish guinea pigs. To evaluate the potential of resveratrol as a regulator of melanin for hyperpigmentation therapy, the influence of resveratrol on pigmentation was investigated by ultraviolet B-induced hyperpigmentation in brownish guinea pig skin. We found that resveratrol reduced the expression of melanogenesis-related proteins tyrosinase, tyrosinase-related proteins 1 and 2, and microphthalmia-associated transcription factor in melanoma cells. Furthermore, topical application of resveratrol was demonstrated to significantly decrease hyperpigmentation on ultraviolet B-stimulated guinea pig skin in vivo. Based on our histological data, resveratrol inhibits melanin synthesis via a reduction in tyrosinase-related protein 2 among the melanogenic enzymes. This study is the first to provide evidence supporting resveratrol as a depigmentation agent, along with further clinical investigation of resveratrol in ultraviolet B-induced skin disorders such as hyperpigmentation and skin photoaging.

• Biomolecules & Therapeutics
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• 제21권4호
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• pp.258-263
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• 2013

We demonstrate herein that silibinin, a polyphenolic flavonoid compound isolated from milk thistle (Silybum marianum), inhibits LPS-induced activation of macrophages and production of nitric oxide (NO) in RAW 264.7 cells. Western blot analysis showed silibinin inhibits iNOS gene expression. RT-PCR showed that silibinin inhibits iNOS, TNF-${\alpha}$, and $IL1{\beta}$. We also showed that silibinin strongly inhibits p38 MAPK phosphorylation, whereas the ERK1/2 and JNK pathways are not inhibited. The p38 MAPK inhibitor abrogated the LPS-induced nitrite production, whereas the MEK-1 inhibitor did not affect the nitrite production. A molecular modeling study proposed a binding pose for silibinin targeting the ATP binding site of p38 MAPK (1OUK). Collectively, this series of experiments indicates that silibinin inhibits macrophage activation by blocking p38 MAPK signaling.

• Animal cells and systems
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• 제13권4호
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• pp.357-362
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• 2009

Hesperidin, the most abundant polyphenolic compound found in citrus fruits, has been known to possess neuroprotective, sedative, and anticonvulsive effects on the nervous system. In a recent electrophysiological study, it was reported that hesperidin induced biphasic change in population spike amplitude in hippocampal CA1 neurons in response to both single spike stimuli and theta-burst stimulation depending on its concentration. However, the precise mechanism by which hesperidin acts on neuronal functions has not been fully elucidated. Here, using whole-cell patch-clamp recording, we revealed that hesperidin did not affect excitatory synaptic activities such as basal synaptic transmission and theta-burst LTP. Moreover, in a current injection experiment, spike number, resting membrane potential and action potential threshold also remained unchanged. Taken together, these results indicate that the effects of hesperidin on the neuronal functions such as spiking activity might not be attributable to either modification of excitatory synaptic transmissions or changes in membrane excitability in hippocampal CA1 neuron.

• 한국식품영양학회지
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• 제29권3호
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• pp.347-356
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• 2016

This study analyzed the antioxidant properties of Equisetum arvense and its effects on serum factor levels in mice fed a high-fat diet. The aim was to establish a new effective resource for biologically active materials. E. arvense stem and root extracts were obtained using deionized water at $95^{\circ}C$, and 70.5% ethanol at $85^{\circ}C$. These extracts were used to analyze the total phenolic compounds and antioxidant (ABTS, DDPH, and FRAP) activities. The effects of prepared ground samples were evaluated by feeding them to mice. E. arvense extracts showed strong antioxidant effects. The caffeic acid content was highest in the 70.5% ethanol extract of the vegetative stem, as determined by high-performance liquid chromatography. The blood concentrations of insulin and leptin were significantly lower in mice fed a high-fat diet supplemented with extracts of the root, reproductive stem, and vegetative stem of E. arvense than in mice fed only a high-fat diet. These results suggest that the polyphenolic compounds in E. arvense extracts exert various antioxidant effects. The stems and root of E. arvense can lower the blood levels of insulin and leptin, even after consumption of a high-fat diet.