• Journal of Pharmacopuncture
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• v.22 no.2
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• pp.115-121
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• 2019

Objectives: The objective of this study was to evaluate antidiabetic activity of Chaturmukha rasa based on streptozotocin induced diabetes model, alpha amylase inhibitory activity, alpha Glucosidase inhibitory activity and inhibition of sucrase. Methods: Chaturmukha rasa was prepared as per Ayurvedic formulary. Antidiabetic activity was measured in experimentally streptozotocin induced rats. The dose was taken as 45 mg/kg, i.p. The antidiabetic activity of Chaturmukha rasa was compared Triphala Kwatha, a marketed formulation. Further In vitro $\acute{\alpha}$- Amylase Inhibitory Assay, In vitro salivary amylase Inhibitory Assay, In vitro ${\alpha}-Glucosidase$ Inhibitory Assay and In vitro Sucrase Inhibitory Assay was performed with respect to Chaturmukha rasa. The IC50 value was calculated for all the above activity. Results: Streptozotocin with Acarbose showed significant decrease in blood glucose level whereas streptozotocin with Triphala kwatha showed more decrease in blood glucose level than Streptozotocin with Acarbose. The combination of Streptozotocin + Triphala kwatha + Chaturmukha rasa showed a significant decrease in blood glucose level on 21st day. In vitro $\acute{\alpha}$- Amylase Inhibitory Assay the Chaturmukha rasa showed IC50 value $495.94{\mu}l$ when compared with Acarbose $427.33{\mu}l$, respectively. In the ${\alpha}-Glucosidase$ Inhibitory Assay Chaturmukha rasa showed IC50 value $70.93{\mu}l$ when compared with Acarbose $102.28{\mu}l$, respectively. In vitro Sucrase Inhibitory Assay Chaturmukha rasa showed IC50 value $415.4{\mu}l$ when compared with Acarbose $371.43{\mu}l$, respectively. Conclusion: This study supports that Chaturmukha rasa may inhibit diabetes by inhibition of salivary amylase or alpha Glucosidase or sucrase. This may be the mechanism by which Chaturmukha rasa inhibits diabetes. Further this study supports the usage of Chaturmukha rasa for the management of diabetes.

• Genomics & Informatics
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• v.19 no.1
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• pp.10.1-10.7
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• 2021

Although many models have been proposed to accurately predict the response of drugs in cell lines recent years, understanding the genome related to drug response is also the key for completing oncology precision medicine. In this paper, based on the cancer cell line gene expression and the drug response data, we established a reliable and accurate drug response prediction model and found predictor genes for some drugs of interest. To this end, we first performed pre-selection of genes based on the Pearson correlation coefficient and then used ElasticNet regression model for drug response prediction and fine gene selection. To find more reliable set of predictor genes, we performed regression twice for each drug, one with IC₅₀ and the other with area under the curve (AUC) (or activity area). For the 12 drugs we tested, the predictive performance in terms of Pearson correlation coefficient exceeded 0.6 and the highest one was 17-AAG for which Pearson correlation coefficient was 0.811 for IC₅₀ and 0.81 for AUC. We identify common predictor genes for IC₅₀ and AUC, with which the performance was similar to those with genes separately found for IC₅₀ and AUC, but with much smaller number of predictor genes. By using only common predictor genes, the highest performance was AZD6244 (0.8016 for IC₅₀, 0.7945 for AUC) with 321 predictor genes.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.35 no.3
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• pp.243-250
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• 2009

To develop a new natural whitening agent for cosmetics, we investigated the inhibitory effects of Poria cocos Bark extracts (PCBE) and its active compound on melanogenesis. PCBE showed ROS scavenging activities in 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and xanthine/xanthine oxidase system with the $IC_{50}$ values of $19.4{\pm}2.21{\mu}g$/mL and $IC_{50}=103{\pm}3.33{\mu}g$/mL, respectively. PCBE reduced intracellular tyrosinase activity about 34 % at concentration of $50{\mu}g$/mL. And PCBE reduced melanin contents of B16 melanoma cells about 51 % at concentration of $50{\mu}g$/mL without cell cytotoxicity (below $100{\mu}g$/mL). We purified one active compound from PCBE and identified its structure. It was identified as 3-$\beta$-hydroxylanosta-7,9(11),24-trien-4-oic acid, triterpene family, by $^1H$-NMR, $^{13}C$-NMR and Mass analysis. 3-$\beta$-hydroxylanosta-7,9(11),24-trien-4-oic acid showed ROS scavenging activities in DPPH radical and xanthine/xanthine oxidase system with the $IC_{50}$ values of $4.3{\pm}0.15{\mu}g$/mL and $54{\pm}1.67{\mu}g$/mL, respectively. Also, it was shown that 3-$\beta$-hydroxylanosta-7,9(11),24-trien-4-oic acid reduced intracellular tyrosinase activity about 43 % at concentration of $10{\mu}g$/mL. And it inhibited melanin synthesis in a dose dependent manner ($IC_{50}=3.6{\mu}g$/mL) without cell cytotoxicity (below $100{\mu}g$/mL). 3-$\beta$-hydroxylanosta-7,9(11),24-trien-4-oic acid inhibited tyrosinase, TRP-1 and TRP-2 expression at protein level. These results suggest that PCBE and 3-$\beta$-hydroxylanosta-7,9(11),24-trien-4-oic acid reduced melanin formation by the inhibition of tyrosinase activity and expression in B16 melanoma cells. Therefore, we suggest that PCBE could be used as a useful whitening agent.

• Korean Journal of Environmental Agriculture
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• v.35 no.1
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• pp.79-86
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• 2016

BACKGROUND: This study was initiated to quantitatively evaluate the effects of five heavy metals on the growth and P removal efficiencies of Alcaligenes sp., known as the Phosphorus Accumulating Organisms (PAOs). It was cultivated in the batch system with five heavy metals, such as Cd, Cu, Zn, Pb and Ni, added in single and binary mixtures, respectively.METHODS AND RESULTS: IC₅₀ (half of inhibition concentration of bacterial growth) and EC₅₀ (half of effective concentration of phosphorus removal Efficiencies) were used to quantitatively evaluate the effects of heavy metals on the growth and phosphorus removal Efficiencies of Alcaligenes sp. In addition, Additive Index Value (A.I.V.) method was used to evaluate the interactive effects between Alcaligenes sp. and heavy metals. As a result, as the five heavy metals were singly added to Alcaligenes sp., the greatest inhibitory effects on the growth and P removal efficiencies of each bacteria was observed in the cadmium (Cd). In the binary mixture treatments of heavy metals, the treatments of lowest IC₅₀ and EC₅₀ were the Cd + Cu treatment. Based on the IC₅₀ and EC₅₀ of the binary mixtures of heavy metals treatments, most interactive effects between the heavy metals were found to be antagonistic.CONCLUSION: Based on the results obtained from this study, it appears that they could provide the basic information about the toxic effects of the respective treatments of single and binary mixtures of heavy metals on the growth and P removal efficiencies of Alcaligenes sp. through further study about the characterization of functional proteins involved in toxic effects of heavy metals.

• KOREAN JOURNAL OF CROP SCIENCE
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• v.57 no.1
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• pp.22-28
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• 2012

This experiment was conducted to find out high antioxidant activity varieties of chinese matrimony from the 131 accessions which conserved at Cheongyang Gugija Experiment Station. The status of the 131 accessions were composed 21 of local varieties, 20 of introduced species and 90 of improved races. The anti-oxidant activity using DPPH and $IC_{50}$, 45 accessions out of 90 showed high activity in free radical scavenging ability as less than $200{\mu}g/m{\ell}$ in improved races, while nine and six accessions from the introduced species and local varieties, respectively. At the stem part, the highest three anti-oxidant varieties among 131 accessions are "C0148-94", "D0148-72" and "Cheongdae", while China collection 1 in leaf part. Since "Cheongdae" is the progeny from the "Cheongyang Jaerae 5" and "Myungan" and those two varieties, "C0148-94" and "D0148-72" are from the Myungan and Cheongdae, high anti-oxidant activity can be inherited in Chinese matrimony vine.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.15
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• pp.6581-6589
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• 2015

Background: Previously, stingless bee (Trigona spp.) products from East Kalimantan, Indonesia, were successfully screened for in vitro antiproliferative activity against human cancer derived cell lines. It was established that propolis from T. incisa presented the highest in vitro cytotoxicity against the SW620 colon cancer cell line (6% cell survival in $20{\mu}g/mL$). Materials and Methods: Propolis from T. incisa was extracted with methanol and further partitioned with n-hexane, ethyl acetate and methanol. The in vitro cytotoxicity of the extracts was assessed by the MTT assay against human colon (SW620), liver (Hep-G2), gastric (KATO-III), lung (Chago) and breast (BT474) cancer derived cell lines. The active fractions were further enriched by silica gel quick column, absorption and size exclusion chromatography. The purity of each fraction was checked by thin layer chromatography. Cytotoxicity in BT-474 cells induced by cardanol compared to doxorubicin were evaluated by MTT assay, induction of cell cycle arrest and cell death by flow cytometric analysis of propidium iodide and annexin-V stained cells. Results: A cardol isomer was found to be the major compound in one active fraction (F45) of T. incisa propolis, with a cytotoxicity against the SW620 ($IC_{50}$ of $4.51{\pm}0.76{\mu}g/mL$), KATO-III (IC50 of $6.06{\pm}0.39{\mu}g/mL$), Hep-G2 ($IC_{50}$ of $0.71{\pm}0.22{\mu}g/mL$), Chago I ($IC_{50}$ of $0.81{\pm}0.18{\mu}g/mL$) and BT474 (IC50 of $4.28{\pm}0.14{\mu}g/mL$) cell lines. Early apoptosis (programmed cell death) of SW620 cells was induced by the cardol containing F45 fraction at the $IC_{50}$ and $IC_{80}$ concentrations, respectively, within 2-6 h of incubation. In addition, the F45 fraction induced cell cycle arrest at the G1 subphase. Conclusions: Indonesian stingless bee (T. incisa) propolis had moderately potent in vitro anticancer activity on human cancer derived cell lines. Cardol or 5-pentadecyl resorcinol was identified as a major active compound and induced apoptosis in SW620 cells in an early period (${\leq}6h$) and cell cycle arrest at the G1 subphase. Thus, cardol is a potential candidate for cancer chemotherapy.

• Food Science and Preservation
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• v.21 no.3
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• pp.421-426
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• 2014

In this study, the antioxidant and pancreatic lipase inhibitory activities of aqueous methanolic (70% methanol) extract from the roots of Anemarrhena asphodeloides were investigated. The extracts of four solvent fractions (the n-hexane layer, EtOAc layer, n-BuOH layer, and $H_2O$ layer) of the 70% methanol extract were also investigated. Furthermore, the total phenolic content was quantified using a spectrophotometric method. All the tested samples showed dose-dependent radical scavenging and pancreatic lipase inhibitory activities. In particular, the pancreatic lipase inhibitory activity of the ethyl acetate soluble portion (the EtOAc layer) from the rhizomes of the A. asphodeloides was higher than that of the other solvent-soluble portions. The antioxidant property of the extracts was evaluated using radical scavenging assays with DPPH and $ABTS^+$ radicals. 1000 mg/ml of the n-BuOH layer extract showed 91.2% DPPH radical scavenging activity. The EtOAc layer extract and the n-BuOH layer extract showed $IC_{50}=20.5{\pm}1.7mg/ml$ and $IC_{50}=50.5{\pm}0.7mg/ml$ $ABTS^+$ radical scavenging activities, respectively. The anti-obesity efficacy of the A. asphodeloides extract was tested via porcine pancreatic lipase assay. A pancreatic lipase inhibitory activity ($IC_{50}$) of $31.3{\pm}0.1mg/ml$ was obtained from the EtOAc layer extract. These results suggest that A. asphodeloides can be considered a new potential source of natural antioxidant and anti-obesity agents.

• Korean Journal of Food Science and Technology
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• v.46 no.6
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• pp.665-670
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• 2014

We isolated twelve lignans and three terpenoids were isolated from the n-hexane fraction of Schisandra chinensis extract. Using spectroscopic data and comparison with available literature, the following compounds were identified: (1) wuweizisu C, (2) gomisin N, (3) deoxyschisandrin, (4) gomisin A, (5) schisandrin, (6) chamigrenal, (7) schisanlactone D, (8) methylgomisin O, (9) angeloylgomisin O, (10) (-)-gomisin $L_2$, (11) schisandronic acid, (12) (-)-gomisin $L_1$, (13) (+)-gomisin $K_3$, (14) gomisin J, and (15) tigloylgomisin H. Notably, this was the first finding that compound (8) was isolated from this plant. Each compound was evaluated for its in vitro cytotoxic activities toward HL-60 (human leukemia), HeLa (human cervical carcinoma), and MCF-7 (breast cancer) cell lines. Compounds (7), (8), and (9) exhibited strong cytotoxic effects on HL-60 ($IC_{50}$ 7.37, 6.60, and $8.00{\mu}M$, respectively), whereas compound (6) exhibited weak cytotoxicity towards MCF-7 ($IC_{50}$ $30.50{\mu}M$). In addition, compound (8) showed the strongest activity towards HeLa cells ($IC_{50}$ $1.46{\mu}M$).

• Journal of Life Science
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• v.21 no.11
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• pp.1558-1564
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• 2011

Cytochrome P450 2J2 (CYP2J2) plays important roles in the metabolism of endogenous metabolites such as arachidonic acid as well as therapeutic drugs. CYP2J2 is overexpressed in human cancer tissues and cancer cell lines, as well as in epoxyeicosatrienoic acids (EETs) and CYP2J2-mediated metabolites, and prevent apoptosis of cancer cells. This study aimed to screen marketed drugs for inhibitory potential on CYP2J2 isoforms using human liver microsomes. The initial screen isolated 4 compounds, from 120 marketed drugs, that inhibited the CYP2J2-mediated astemizole O-demethylation more than 50% in the following the order: haloperidol (75%) > terfenadine (56%) > aripiprazole (55%) > miconazole (52%). Miconazole strongly inhibited CYP2J2-mediated ebastine hydroxylation ($IC_{50}$=11.2 ${\mu}M$) and terfenadine hydroxylation ($IC_{50}$=2.2 ${\mu}M$), and terfenadine also inhibited CYP2J2-mediated ebastine hydroxylation ($IC_{50}$=13.6 ${\mu}M$) in a dose dependent manner. The present data suggest that these drugs are potential candidates for further evaluation for their anti-cancer activities.

• Korean Journal of Radiology
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• v.24 no.1
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• pp.39-50
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• 2023

Objective: To assess the contrast-enhanced CT and ultrasonography (US) findings of intracholecystic papillary neoplasm (ICPN) and determine the imaging features predicting ICPN associated with invasive carcinoma (ICPN-IC). Materials and Methods: In this retrospective study, we enrolled 119 consecutive patients, including 60 male and 59 female, with a mean age ± standard deviation of 63.3 ± 12.1 years, who had pathologically confirmed ICPN (low-grade dysplasia [DP] = 34, high-grade DP = 35, IC = 50) and underwent preoperative CT or US. Two radiologists independently assessed the CT and US findings, focusing on wall and polypoid lesion characteristics. The likelihood of ICPN-IC was graded on a 5-point scale. Univariable and multivariable logistic regression analyses were performed to identify significant predictors of ICPN-IC separately for wall and polypoid lesion findings. The performances of CT and US in distinguishing ICPN-IC from ICPN with DP (ICPN-DP) was evaluated using the area under the receiver operating characteristic curve (AUC). Results: For wall characteristics, the maximum wall thickness (adjusted odds ratio [aOR] = 1.4; 95% confidence interval [CI]: 1.1-1.9) and mucosal discontinuity (aOR = 5.6; 95% CI: 1.3-23.4) on CT were independently associated with ICPN-IC. Among 119 ICPNs, 110 (92.4%) showed polypoid lesions. Regarding polypoid lesion findings, multiplicity (aOR = 4.0; 95% CI: 1.6-10.4), lesion base wall thickening (aOR = 6.0; 95% CI: 2.3-15.8) on CT, and polyp size (aOR = 1.1; 95% CI: 1.0-1.2) on US were independently associated with ICPN-IC. CT showed a higher diagnostic performance than US in predicting ICPN-IC (AUC = 0.793 vs. 0.676; p = 0.002). Conclusion: ICPN showed polypoid lesions and/or wall thickening on CT or US. A thick wall, multiplicity, presence of wall thickening in the polypoid lesion base, and large polyp size are imaging findings independently associated with invasive cancer and may be useful for differentiating ICPN-IC from ICPN-DP.