• Mycobiology
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• 제51권4호
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• pp.246-255
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• 2023

Genus Penicillium comprising the most important and extensively studied fungi has been well-known as a rich source of secondary metabolites. Our study aimed to analyze and investigate biological activities, including in vitro anti-cancer, anti-inflammatory and anti-diabetic properties, of metabolites from a marine-derived fungus belonging to P. levitum. The chemical compounds in the culture broth of P. levitum strain N33.2 were extracted with ethyl acetate. Followingly, chemical analysis of the extract leaded to the isolation of three ergostane-type steroid components, namely cerevisterol (1), ergosterol peroxide (2), and (3β,5α,22E)-ergosta-6,8(14),22-triene-3,5-diol (3). Among these, (3) was the most potent cytotoxic against human cancer cell lines Hep-G2, A549 and MCF-7 with IC₅₀ values of 2.89, 18.51, and 16.47 ㎍/mL, respectively, while the compound (1) showed no significant effect against tested cancer cells. Anti-inflammatory properties of purified compounds were evaluated based on NO-production in LPS-induced murine RAW264.7 macrophages. As a result, tested compounds performed diverse inhibitory effects on NO production by the macrophages, with the most significant inhibition rate of 81.37±1.35% at 25 ㎍/mL by the compound (2). Interestingly, compounds (2) and (3) exhibited inhibitory activities against pancreatic lipase and α-glucosidase enzymes in vitro assays. Our study brought out new data concerning the chemical properties and biological activities of isolated steroids from a P. levitum fungus.

• 한국식품영양학회지
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• 제25권3호
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• pp.447-453
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• 2012

Various types of tea are consumed as a popular beverage worldwide particularly in Asian countries such as Korea, China, and Japan. The purpose of this study was to investigate the mineral contents, antioxidant properties and anticancer activity of Yak-Sun tea that is prepared by six oriental medicinal herbs. The results of the mineral contents were as follows; Ca, Mg, and Na contents were higher than those of green tea, whereas Fe, P, and K contents were lower than those of green tea. The total phenolics and flavonoid content of the Yak-Sun tea were higher than those of green and black teas. The $IC_{50}$ values of DPPH radical, hydroxyl radical, hydrogen peroxide radical scavenging of Yak-Sun tea were 0.78, 1.58, and 2.04 $mg/m{\ell}$, respectively, whereas the radical scavenging values of ${\alpha}$-tocopherol was 0.06, 0.05, and 0.09 $mg/m{\ell}$, respectively. When cancer cells were treated with Yak-Sun tea, the anticancer activity increased in a dose dependent manner. HCT116 colon cancer cell lines were dramatically increased, as compared to other cancer cell lines, such as MCF-7, H460, and MKN45 cell lines. The results of this study demonstrated that Yak-Sun tea could function as a tea to enhance health conditions for antioxidant and anticancer activity.

• 한국축산식품학회지
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• 제42권4호
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• pp.609-624
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• 2022

Tenebrio molitor larvae, as known as edible insects, has advantages of being rich in protein, and has been recognized as a suitable alternate protein source for broiler and pig feed. Moreover, given their ability to biodegrade polystyrene, a major pollutant, Tenebrio molitor larvae has been proposed as an innovative solution to environmental problems. In the present study, we investigated the toxicity of Tenebrio molitor larvae powder (TMlp) ingested with expanded-polystyrene (W/ eps) through in vitro and in vivo experiments. The objective of this study was to determine whether TMlp W/ eps can be applied as livestock alternative protein source. For in vitro experiments, cytotoxicity test was performed to investigate the effects of TMlp-extract on the viability of estrogen-dependent MCF-7 cells. The possibility of estrogen response was investigated in two groups: Expanded-polystyrene-fed (W/ eps) TMlp group and without expanded-polystyrene-fed (W/o eps) TMlp group. For in vivo experiments, The male Sprague-Dawley rats were divided based on the dosage of TMlp administered and oral administration was performed to every day for 5 weeks. A toxicological assessments were performed, which included clinical signs, food consumption, body and organ weights, hematology, serum chemistry, and hematoxylin and eosin staining of liver and kidney. There were no specific adverse effect of TMlp W/ eps-related findings under the experimental conditions of this study, but further studies on both sexes and animal species differences should be investigated. In conclusion, TMlp W/ eps was considered non-toxic and observed to be applicable as an alternative protein source for livestock feed.

• 대한한방부인과학회지
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• 제26권1호
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• pp.1-24
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• 2013

Objectives: The object of this study was to observe the protective effect of Gamijipaesan aqueous extracts(GJS), which has been traditionally used in Korean medicine in obstetrics & gynecological fields as anti-infectious and anti-inflammatory agents, against mastitis induced by Staphylococcus aureus infection in a rat model through antibacterial, antiinflammatory, immunomodulatory, and anti-oxidant effects. Methods: Antibacterial activities of GJS against S. aureus were detected using standard agar microdilution methods, with the effects on the bacterial invasion and intracellular killing of individual test materials in human mammary gland carcinoma cell(MCF-7) and murine macrophages(Raw 264.7) at MIC1/2, MIC and MIC2 concentration levels. In addition, the effects on the cell viability, nitric oxide(NO), tumor necrosis factor(TNF)-${\alpha}$ and interleukin (IL)-6 productions of LPS activated Raw 264.7 cells. The changes on the mammary tissue viable bacterial numbers, myeloperoxidae(MPO), inducible nitric oxide synthetase(iNOS), TNF-${\alpha}$ and IL-6 contents were observed in the S. aureus in vivo intramammary infectious rat model. The anti-bacterial and anti-inflammatory effects were compared with ciprofloxacin and piroxicam, respectively in the present study. Results: MIC of GJS and ciprofloxacin against S. aureus were detected as $0.860{\pm}0.428$ (0.391-1.563) mg/ml and $0.371{\pm}0.262$(0.098-0.782) ${\mu}g/ml$, respectively. In addition, GJS and ciprofloxacin were also showed marked dosage-dependent inhibition of the both bacterial invasion and intracellular killing assays using MCF-7 and Raw 264.7 cells at MIC1/2, MIC and $MIC{\times}2$ concentrations, respectively. $ED_{50}$ against LPS-induced cell viabilities and NO, TNF-${\alpha}$ and IL-6 releases of GJS were detected as 0.72, 0.04, 0.08 and 0.11 mg/ml, and as 19.04, 4.18, 5.37 and 4.27 ${\mu}g/ml$ in piroxicam, respectively. 250 and 500 mg/kg of GJS also inhibit the intramammary bacterial growth, MPO, iNOS, TNF-${\alpha}$ and IL-6 contents in S. aureus in vivo intramammary infected rats, respectively. GJS 500 mg/kg showed quite similar antibacterial and anti-infectious effects as compared with ciprofloxacin 40 mg/kg and also showed similar anti-inflammatory effects as piroxicam 10 mg/kg, in S. aureus in vivo intramammary infectious models. Conclusions: The results obtained in this study suggest that over 250 mg/kg of GJS showed favorable anti-infectious effects against S. aureus infection in a rat model through their antibacterial, anti-inflammatory, immunomodulatory and anti-oxidant effects and therefore expected that GJS can be used as alternative therapies, having both anti-inflammatory and anti-infectious activities. However, more detail mechanism studies should be conducted in future with the efficacy tests of individual herbal composition of GJS and the screening of the biological active compounds in individual herbs. In the present study, GJS 500 mg/kg showed quite similar anti-infectious effects were detected as compared with ciprofloxacin 40 mg/kg treated rats, and also GJS shows quite similar anti-inflammatory effects as compared with piroxicam 10 mg/kg in S. aureus in vivo intramammary infectious rats, but ciprofloxacin did not showed any anti-inflammatory effects, and piroxicam did not showed anti-infectious effects in this study.

• Journal of Ginseng Research
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• 제44권5호
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• pp.690-696
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• 2020

Background: As the main metabolites of ginsenosides, 20(S, R)-protopanaxadiol [PPD(S, R)] and 20(S, R)-protopanaxatriol [PPT(S, R)] are the structural basis response to a series of pharmacological effects of their parent components. Although the estrogenicity of several ginsenosides has been confirmed, however, the underlying mechanisms of their estrogenic effects are still largely unclear. In this work, PPD(S, R) and PPT(S, R) were assessed for their ability to bind and activate human estrogen receptor α (hERα) by a combination of in vitro and in silico analysis. Methods: The recombinant hERα ligand-binding domain (hERα-LBD) was expressed in E. coli strain. The direct binding interactions of ginsenosides with hERα-LBD and their ERα agonistic potency were investigated by fluorescence polarization and reporter gene assays, respectively. Then, molecular dynamics simulations were carried out to simulate the binding modes between ginsenosides and hERα-LBD to reveal the structural basis for their agonist activities toward receptor. Results: Fluorescence polarization assay revealed that PPD(S, R) and PPT(S, R) could bind to hERα-LBD with moderate affinities. In the dual luciferase reporter assay using transiently transfected MCF-7 cells, PPD(S, R) and PPT(S, R) acted as agonists of hERα. Molecular docking results showed that these ginsenosides adopted an agonist conformation in the flexible hydrophobic ligand-binding pocket. The stereostructure of C-20 hydroxyl group and the presence of C-6 hydroxyl group exerted significant influence on the hydrogen bond network and steric hindrance, respectively. Conclusion: This work may provide insight into the chemical and pharmacological screening of novel therapeutic agents from ginsenosides.

• 한국식품저장유통학회:학술대회논문집
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• 한국식품저장유통학회 2003년도 춘계총회 및 제22차 학술발표회
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• pp.22-39
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• 2003

Biological activity of phenolic compounds in seeds and leaves of safflower (Carthamu tinctorius L.) were evaluated using several in vitro and in vivo assays. Six phenolic constituents were isolated from the seeds and identified as N-feruloylserotonia, N- (p-coumaroyl)serotonin, matairesinol, 8′-hydroxyarctigenin, acacetin 7-O-$\beta$-D-glucoside (tilianine) and acacetin. Six phenolic compounds exhibited considerable antioxidative activity, and especially two serotonins showed potent DPPH radical scavenging activity and antiperoxidative activity against rat liver microsomal lipid peroxidation induced by the hydroxyl radical generated via a Fenton-type reaction. Additionally, six phenolic compounds possessed comparable cytotoxicity against three cancer cells, Hela cell, MCF-7 and HepG2 cell, and particularly acacetin and its glycosides had the most potent cytotoxicity. Moreover, we found that feeding safflower seeds attenuated bone loss, and lowered levels of plasma and liver lipids in ovariectomized rats. Serotonins, lignans and flavones stimulated proliferation of the osteoblast-like cells in a dose-dependent manner (10$^{-15}$ ~10$^{-6}$ M), as potently as E$_2$ (17$\beta$-estradiol). Particularly, serotonins were mainly responsible for bone-protecting and lipid lowering effects in ovariectomized rats. Meanwhile, eight flavonoids, including a novel quercetin-7-O-(6"-O-acetyl)-$\beta$-D-glucopyranoside and seven kown flavonoids, luteolin quercetin, luteolin 7-O-$\beta$-D-glucopyranoside, luteolin-7-O-(6"-O-acetyl)-$\beta$-D-gluco-pyranoside, quercetin 7-O- -glucopyranoside, acacetin 7-O-$\beta$-D-glucuronide and apigenin-6-C-$\beta$-D-glucopyranosyl-8-C-$\beta$-D-glucopyranoside were first isolated and identified from safflower leaf. Among these flavonoids, luteolin-acetyl-glucoside and $\beta$quercetin- acetyl-glucoside showed potent antioxidative activities against 2-deoxyribose degradation and lipid peroxidation in rat liver microsomes. Luteolin, quercetin and their corresponding glycosides also exhibited strong antioxidative activity, while acacetin glucuronide and apigenin-6, 8-di-C-glucoside were relatively less active. Finally, changes in phenolic compositions were also determined by HPLC in the safflower seed and leaf during growth stages and roasting process to produce standardized supplement powerds. These results suggest that phenolic compounds in the roasted safflower seed and leaf may be useful as potential sources of therapeutic agents against several pathological disorders such as carcinogenesis, atherosclerosis and osteoporosis.

• 한국수산과학회지
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• 제39권4호
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• pp.318-325
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• 2006

Ultrasonified extracts from seawater-based cultures of the microalga Spiyulina platensis were obtained using water and ethanol at 60 and 100$^{\circ}C$. The yield of the aqueous fraction of S. platensis extracted using ultrasonification was about 33.46%. The cytotoxicity against HEK293 and inhibition ratios of the cancer cell lines A549, AGS, MCF7, and Hep3B were measured using the sulforhodamine-B (SRB) assay. The cytotoxicity of all extracts at 1.0 mg/mL was below 26%. The cytotoxicity of the ultrasonified extracts from the seawater-based culture of the microalga Spirulina platensis was about 4% less than that of Spirulina platensis without ultrasonification. The inhibition ratio of cancer cell growth was approximately 80% for 1.0 mg/mL extracts. The inhibitory effect on cancer cell growth was greater for seawater containing ultrasonified Spirulina platensis extracts than for extracts without ultrasonification. The differentiation ratio of HL-60 cells was 160.9%. Densitometric analysis of Bcl-2 revealed that the ultrasonified extracts had greater anticancer activity than the extracts without ultrasonification.

• BMB Reports
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• 제43권1호
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• pp.17-22
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• 2010

In this study, a novel member of BTB-kelch proteins, named KBTBD7, was cloned from a human embryonic heart cDNA library. The cDNA of KBTBD7 is 3,008 bp long and encodes a protein product of 684 amino acids (77.2 kD). This protein is highly conserved in evolution across different species. Western blot analysis indicates that a 77 kD protein specific for KBTBD7 is wildly expressed in all embryonic tissues examined. In COS-7 cells, KBTBD7 proteins are localized to the cytoplasm. KBTBD7 is a transcription activator when fused to GAL4 DNA-binding domain. Deletion analysis indicates that the BTB domain and kelch repeat motif are main regions for transcriptional activation. Overexpression of KBTBD7 in MCF-7 cells activates the transcriptional activities of activator protein-1 (AP-1) and serum response element (SRE), which can be relieved by siRNA. These results suggest that KBTBD7 proteins may act as a new transcriptional activator in mitogen-activated protein kinase (MAPK) signaling.

• 대한암한의학회지
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• 제20권2호
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• pp.13-21
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• 2015

Objective : The objective of this study was to investigate the experimental efficacy of anti-tumor activity of the complexed herbal formula, Onbaekwon (OBW), which was derived from the literature of Traditional Korean Medicine, Dongeuibogam. Methods : Nine Cancer cell lines, LoVo, MCF-7, HepG2, AGS, A549, NCI-H69, HL-60, Sarcoma 180, LL/2, were prepared and the cytotoxicity was assessed by 3-(4,5-dimethylthiazol-2yl)-2,5-dephenyl tetrazolium bromide (MTT) assay. Four of them, NCI-H69, HL-60, Sarcoma 180, and LL/2, showed strong cytotoxic activities and they were additionally undergone flow cytometry to find out their effects on apoptosis. ICR male mice were implanted with Sarcoma 180 intraperitoneally and divided into 8 species for each group. Control group was treated with normal saline, positive control group was treated with cyclophosphamide 8mg/kg, and experimental group was treated with OBW 1 g/kg. Results : Among 9 cancer cell lines, NCI-H69, HL-60, Sarcoma 180, and LL/2, expressed less than 0.10 mg/ml of $IC_{50}$ under 0.1~1mg/ml of OBW. NCI-H69, HL-60, Sarcoma 180, and LL/2, showed dose-dependent efficacy of apoptosis. When Sarcoma 180 cancer cell was implanted in ICR male mice and treated with the OBW, they prolonged the median overall survival for 0.8 days, from 17.5 to 18.3. Conclusion : OBW showed strong cytotoxicity to some cancer cells, which are NCI-H69, HL-60, Sarcoma 180, and LL/2, and its apoptotic activity was dose-dependent. OBW prolonged the median survival of mice implanted with Sarcoma 180. Further researches would be expected to support the efficacy of OBW.

• Journal of Microbiology and Biotechnology
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• 제28권6호
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• pp.1007-1021
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• 2018

Cancer represents one of the most significant threats to human health on a global scale. Hence, the development of effective cancer prevention strategies, as well as the discovery of novel therapeutic agents against cancer, is urgently required. In light of this challenge, this research aimed to evaluate the effects of several potent bioactive peptides and proteins contained in crocodile white blood cell extract (cWBC) against LU-1, LNCaP, PC-3, MCF-7, and CaCo-2 cancer cell lines. The results demonstrate that 25, 50, 100, and $200{\mu}g/ml$ cWBC exhibits a strong cytotoxic effect against all investigated cell lines ($IC_{50}$ $70.34-101.0{\mu}g/ml$), while showing no signs of cytotoxicity towards noncancerous Vero and HaCaT cells. Specifically, cWBC treatment caused a significant reduction in the cancerous cells' colony forming ability. A remarkable suppression of cancerous cell migration was observed after treatment with cWBC, indicating potent antimetastatic properties. The mechanism involved in the cancer cell cytotoxicity of cWBC may be related to apoptosis induction, as evidenced by typical apoptotic morphology features. Moreover, certain cWBC concentrations induced significant overproduction of ROS and significantly inhibited the $S-G_2/M$ transition in the cancer cell. The molecular mechanisms of cWBC in apoptosis induction were to decrease Bcl-2 and XIAP expression levels and increase the expression levels of caspase-3, caspase-8, and p53. These led to a decrease in the expression level of the cell cycle-associated gene cyclin-B1 and the arrest of cell population growth. Consequently, these findings demonstrate the prospect of the use of cWBC for cancer therapy.