• Journal of Integrative Natural Science
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• v.13 no.4
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• pp.170-180
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• 2020

Abnormal regulation, hyperphosphorylation, and aggregation of the tau protein are the hallmark of several types of dementia, including Alzheimer's Disease. Increased activity of Glycogen Synthase Kinase-3β (GSK-3β) in the Central Nervous System (CNS), increased the tau hyperphosphorylation and caused the neurofibrillary tangles (NFTs) formation in the brain cells. Over the last two decades, numerous adenosine triphosphate (ATP) competitive inhibitors have been discovered that show inhibitory activity against GSK-3β. But these compounds exhibited off-target effects which motivated researchers to find new GSK-3β inhibitors. In the present study, we have collected the dataset of 31 C-Glycosylflavones derivatives that showed inhibitory activity against GSK-3β. Among the dataset, the most active compound was docked with the GSK-3β and molecular dynamics (MD) simulation was performed for 50 ns. Based on the 50 ns MD pose of the most active compound, the other dataset compounds were sketched, minimized, and aligned. The 3D-QSAR based Comparative Molecular Field Analysis (CoMFA) model was developed, which showed a reasonable value of q2=0.664 and r2=0.920. The contour maps generated based on the CoMFA model elaborated on the favorable substitutions at the R2 position. This study could assist in the future development of new GSK-3β inhibitors.

• Nutrition Research and Practice
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• v.8 no.5
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• pp.509-515
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• 2014

BACKGROUND/OBJECTIVES: The root of Vitis amurensis Ruprecht, a sort of wild-growing grape, has been used in oriental medicine for treatment of skin ailments; however, its dermatological activity is not sufficiently understood. The aim of this study was to investigate tyrosinase inhibitory and anti-melanogenic activities of V. amurensis Ruprecht root methanol extract (VARM) in B16F10 mouse melanoma cells and to attempt to isolate and identify the active compound issued from VARM. MATERIALS/METHODS: Anti-melanogenic activity of VARM was analyzed in ${\alpha}$-melanocyte stimulating hormone (MSH)-stimulated B16F10 cells through evaluation of antioxidative activity as well as inhibited tyrosinase activity and melanin contents compared with those of kojic acid and arbutin. After anti-melanogenic analysis of VARM, serial fractionation, nuclear magnetic resonance (NMR), and thin layer chromatorgraphy (TLC) were applied for identification of active compounds contained in VARM. RESULTS: VARM significantly inhibited oxidative stress and tyrosinase activity and attenuated ${\alpha}$-MSH-induced melanin production in B16F10 cells. For isolation of active compounds, VARM was fractionated using a series of organic solvents, including dichloromethane ($CH_2Cl_2$), ethyl acetate (EtOAc), and n-butanol (n-BuOH). Among fractions showing anti-melanogenic activity, the CH2Cl2 fraction induced the most potent attenuation of melanogenesis without cytotoxicity and the major compound in the $CH_2Cl_2$ fraction was identified as betulinic acid. Betulinic acid isolated from the $CH_2Cl_2$ fraction of VARM significantly attenuated ${\alpha}$-MSH-induced melanogenesis in a dose dependent manner, which was stronger than that of arbutin used as a positive control. CONCLUSIONS: These results indicate that VARM inhibits oxidative stress, tyrosinase activity, and ${\alpha}$-MSH-induced melanogenesis in B16F10 cells, due primarily to the active compound, betulinic acid, in the $CH_2Cl_2$ fraction.

• Archives of Pharmacal Research
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• v.21 no.6
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• pp.759-763
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• 1998

In connection with the development of new anticonvulsant agents with a broad spectrum, we found that N-Cbz-alpha-amino-alkylsuccinimides showed significant anticonvulsant activities, and the pharmacological activities of these compounds were dependent on their stereochemistry and N-substituted alkyl group. These results prompted us to define the effects of other functional group on the anticonvulsant activities of these compounds. Therefore a series of N-alkoxycarbonyl-alpha-amino-N-methylsuccinimide were prepared from N-Cbz-aspartic acid and were evaluated with their anticonvulsant activities againt the MES and PTZ tests, in order to define the effect of N-substituted alkoxy carbonyl group with the anticonvulsant activities. From these studies, it was found that all the tested N-alkoxycarbonyl-alpha-amino-N-methylsuccinimides exhibited significant anticonvulsant activities in the PTZ test and were not active in the MES test. The most active compound in the PTZ test was (S) N-ethoxycarbonyl-alpha-amino-N-methyl-succinimide. We found that the pharmacological activities in the PTZ test were dependent on their N-alkoxycarbonyl groups. They follow as such: The order of anticonvulsant activities for (R) series as evaluated by $ED_{50}$ was N-phenoxycarbonyl=N-4-nitrobenzyloxycarbonyl > N-ethoxycarbonyl > N-allyloxycarbonyl > N-tert. butoxycarbonyl compound: For the (S) series N-ethoxycarbonyl > N-phenoxycarbonyl > N-allyloxycarbonyl compound. From the above results, it was conceivable that N-substituted alkoxycarbonyl group had certain effects on the anticonvulsant activities of N-alkoxycarbonyl-${\alpha}$-amino-N-methylsuccinimides.

• The Plant Pathology Journal
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• v.20 no.1
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• pp.52-57
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• 2004

Sclerotinia sp. (isolate BWC98-105) causes stem blight and root rot in Leghum sp., and is presently being evaluated as a potential mycoherbicide for the control of Trifoliorium repens. Bioassays have shown that Sclerotinia sp. produces phytotoxic substance which is biologically active against T. repens. Two biologically active compounds, designated as compoundsI and II, were produced in vitro from the culture filtrate of BWC98-105 isolate Sclerotium sp. Compounds I and II were purified by means of liquid-liquid extraction and $C_{18}$ open column chromatography (300 ${\times}$ 30 mm, i.d). To determine the purity, the purified compounds were analyzed by RP-HPLC. The analytical RP-HPLC column was a TOSOH ODS-120T (150 ${\times}$ 4.6 mm i.d, Japan), of which the flow rate was set at 0.7 mL/min using the linear gradient solvent system initiated with 15 % methanol to 85 % methanol for 50 min with monitoring at 254 nm. Under these RP-HPLC conditions, compounds I and II eluted at 3.49 and 4.13 min, respectively. Compound II was found to be most potent and host specific. However, compound I had a unique antibiotic activity against phytopathogenic bacteria like bacterial leaf blight (Xanthomonas oryzae) on rice, where it played a less important role in producing toxicity on T. repens. No toxin activity was detected in the water fraction after partitioning with several organic solvents. However, toxin activity was detected in the ethyl acetate and butanol fractions. In the leaf bioassay using compound II, the disease first appeared within 4-5 h as water soaked rot, which subsequently developed into well-defined blight affecting the whole plant.

• Korean Journal of Food Science and Technology
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• v.30 no.3
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• pp.672-679
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• 1998

The ethanol extract and its chloroform fraction of Sophora flavescens Ait. exhibited growth inhibition on some food poisoning bacteria. The minimum inhibitory concentration of the above extracts were $50{\sim}500\;ppm$ and below 50 ppm Listeria monocytogenes (ATCC 19111, 19112, 19113, 19114, 15313). By silica gel column chromatography twice, antimicrobial active compound S-10-6 was isolated from chloroform fraction of Sophora flavescens Ait. The fraction S-10-6 showed strong growth inhibition at 10 ppm on 5 strains of L. monocytogenes, Bacillus subtilis ATCC 14593 and Staphylococcus aureus KFCC 11764 but Esherichia coli ATCC 25922 was not inhibited at 100 ppm and also confirmed bactericidal effect at 30 and 50 ppm on 5 strains of L. monocytogenes. The antimicrobial compound S-10-6 was identified as kushenol F, a kind of flavanone compound, by EI/MS, $^1H-NMR\;and\;^{13}C-NMR$.

• Journal of the Korean Institute of Illuminating and Electrical Installation Engineers
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• v.22 no.6
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• pp.141-147
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• 2008

This paper describes the design of frequency down converting Mixer in the receiver to use compound semiconductor and CMOS product process. The basic theory and structure of frequency down converting Mixer is surveyed, and we design mixer circuit with active balun which use the compound semiconductor and CMOS process. This mixer convert a single ended signal to differential signal at input port of RF and LO instead of matching circuit to get dual band balanced mixer structure and characteristic broadband. This designed mixer has a conversion gain $-1{\sim}-6[dB]$ at $2{\sim}6[GHz]$ bandwidths. However, the simulation of the designed mixer with active balun has the result of a 7[dB] conversion gain for -2[dBm] LO input power and -10[dBm] input P1[dB] at 5.8[GHz].

• Korean Journal of Pharmacognosy
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• v.46 no.2
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• pp.105-108
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• 2015

To establish the anti-diabetic(α-glucosidase inhibitory) activity of D. lotus leaf extract, isolate and identify the constituents responsible for the activity. The methanolic extract of leaves was partitioned between water, n-butanol and ethyl acetate. Bio-assay guided fractionation, based on inhibition of ;${\alpha}$-glucosidase, allowed isolation and identification of the active components. Liquid chromatography/mass spectrometry(LC/MS), ¹ H-NMR and ¹³ C-NMR spectra analyses demonstrated that the active compound was myricetin-3-O-;${\alpha}$-L-rhamnoside(1). Compound 1 demonstrated a strong inhibition on the α-glucosidase, in vitro and ;${\alpha}$-glucosidase inhibitory value was calculated as 98.08%, when that of a reference drug, acarbose was estimated as 83.03%. The present study indicates compound 1 could be considered as an ;${\alpha}$-glucosidase inhibitor and developed as an important antidiabetes agent for type II diabetes therapy.

• Journal of the Korean Society of Industry Convergence
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• v.7 no.3
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• pp.299-303
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• 2004

A systematic investigation for the reactivity and solvent effect was studied on the reaction of optical resolving agents with the optically active assistant compounds. The reaction rate constants of the nucleophillic substitution reactions were determined by means of conductometric method The linear solvent energy relationship based on the solvent parameters and the thermodynamic parameters was discussed on the reactions of various physiological active compounds and optical resolving agents The reaction mechanism was discussed from the kinetic results compared with the optical purity.

• Asian Journal of Turfgrass Science
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• v.8 no.3
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• pp.193-199
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• 1994

Effect pf rape seed oil cake compast (OM) active carbon(C) compound fertilizer (NPK) and magnesium sulfate (Mg) application on Zoysia koreana growth by lysimeter of 50cm soil column filled with a low fertility loam. Effect on growth was in order of OM>OM . NPK interaction> NPK . active carbon and Mg were not effective OM . NPK interaction effect was negative on leaf width and root dry matter yield. OM and OM . NPK interaction were most effective on rhizome growth. Their effect did not change the ratio of growth rates between aerial part and rhizome but change that between aerial part and root. Leaf width was most sensitive to the treatments.

• YAKHAK HOEJI
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• v.29 no.6
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• pp.375-379
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• 1985

The gas chromatographic behavior of optically active N-(N-benzoyl-L-valyl)-anilide used as stationary phase is described. N-(N-benzoyl-L-valyl)-anilide has been synthesized with good yield under mild condition via Schotten-Bauman process and coated on the Chromosorb W AW (80-100mesh) for the purpose of enantiomer separation. The behavior of this compound as optically active stationary phase for the separation of the enantiomers of N-TFA-D, L-amino acid isopropyl esters has been examined with respect to the correlation between the separation factors and column temperatures. All amino acid enantiomers examined were eluted within one hour and the elution pattern showed retention times increasing in the order of alanine, valine, leucine, threonine, proline and methionine.