• Archives of Pharmacal Research
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• v.27 no.12
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• pp.1226-1232
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• 2004

Extracts from seventeen seaweeds were determined for tyrosinase inhibitory activity using mushroom tyrosinase with L-tyrosine as a substrate. Only one of them, Ecklonia stolonifera OKAMURA (Laminariaceae) belonging to brown algae, showed high tyrosinase inhibitory activity. Bioassay-guided fractionation of the active ethyl acetate (EtOAc) soluble fraction from the methanolic extract of E. stolonifera, led us to the isolation of phloroglucinol derivatives [phloroglucinol (1), eckstolonol (2), eckol (3), phlorofucofuroeckol A (4), and dieckol (5)]. Compounds 1~5 were found to inhibit the oxidation of L-tyrosine catalyzed by mushroom tyrosinase with $IC_{50}$ values of 92.8, 126, 33.2, 177, and 2.16 ${\mu}g$ /mL, respectively. It was compared with those of kojic acid and arbutin, well-known tyrosinase inhibitors, with $IC_{50}$ values of 6.32 and 112 ${\mu}g$ / mL, respectively. The inhibitory kinetics analyzed from Lineweaver-Burk plots, showed compounds 1 and 2 to be competitive inhibitors with $K_i$ of $2.3{\times}10^{-4}\;and\;3.1{times}10^{-4}$ M, and compounds 3~5 to be noncompetitive inhibitors with $K_i$ of $1.9{\times}10^{-5},\;1.4{\times}10^{-3}\;and\;1.5{\times}10^{-5}$ M, respectively. This work showed that phloroglucinol derivatives, natural compounds found in brown algae, could be involved in the control of pigmentation in plants and other organisms through inhibition of tyrosinase activity using L-tyrosine as a substrate.

• Biomolecules & Therapeutics
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• v.31 no.2
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• pp.176-182
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• 2023

Among 14 subtypes of serotonin receptors (5-HTRs), 5-HT_2AR plays important roles in drug addiction and various psychiatric disorders. Agonists for 5-HT_2AR have been classified into three structural groups: phenethylamines, tryptamines, and ergolines. In this study, the structure-activity relationship (SAR) of phenethylamine and tryptamine derivatives for binding 5-HT_2AR was determined. In addition, functional and regulatory evaluation of selected compounds was conducted for extracellular signal-regulated kinases (ERKs) and receptor endocytosis. SAR studies showed that phenethylamines possessed higher affinity to 5-HT_2AR than tryptamines. In phenethylamines, two phenyl groups were attached to the carbon and nitrogen (R³ ) atoms of ethylamine, the backbone of phenethylamines. Alkyl or halogen groups on the phenyl ring attached to the β carbon exerted positive effects on the binding affinity when they were at para positions. Oxygen-containing groups attached to R³ exerted mixed influences depending on the position of their attachment. In tryptamine derivatives, tryptamine group was attached to the β carbon of ethylamine, and ally groups were attached to the nitrogen atom. Oxygen-containing substituents on large ring and alkyl substituents on the small ring of tryptamine groups exerted positive and negative influence on the affinity for 5-HT_2AR, respectively. Ally groups attached to the nitrogen atom of ethylamine exerted negative influences. Functional and regulatory activities of the tested compounds correlated with their affinity for 5-HT_2AR, suggesting their agonistic nature. In conclusion, this study provides information for designing novel ligands for 5-HT_2AR, which can be used to control psychiatric disorders and drug abuse.

• Biomolecules & Therapeutics
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• v.32 no.4
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• pp.442-450
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• 2024

The type-1 cannabinoid receptor (CB₁R) is a potential therapeutic target in several pathological conditions, including neuropsychological disorders and neurodegenerative diseases. Owing to their structural diversity, it is not easy to derive general structure-activity relationships (SARs) for CB₁R ligands. In this study, CB₁R ligands were classified into six structural families, and the corresponding SAR was determined for their affinities for CB₁R. In addition, we determined their functional activities for the activation of extracellular signal-regulated kinases (ERKs). Among derivatives of indol-3-yl-methanone, the highest ligand affinity was observed when a pentyl and a naphthalenyl group were attached to the N1 position of the indole ring and the carbon site of the methanone moiety, respectively. In the case of adamantane indazole-3-carboxamide derivatives, the presence of fluorine in the pentyl group, the substituent at the N1 position of the indazole ring, strongly increased the affinity for CB₁R. For (naphthalen-1-yl) methanone derivatives, the presence of 4-alkoxynaphthalene in the methanone moiety was more beneficial for the affinity to CB₁R than that of a heterocyclic ring. The functional activities of the tested compounds, evaluated through ERK assay, were correlated with their affinity for CB₁R, suggesting their agonistic nature. In conclusion, this study provides valuable insight for designing novel ligands for CB₁R, which can be used to control psychiatric disorders and drug abuse.

• 제어로봇시스템학회:학술대회논문집
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• 1996.10b
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• pp.1087-1090
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• 1996

The objective of this paper is to present a new input torque shaping method for slewing and vibration suppression of flexible structure based on Fourier series expansion. Vibration energy of the structure with shaped control input is investigated with respect to the shaping parameter of the reference torque, maneuver time and the number of trigonometric functions to be included in the series. Analytic expressions of the performance indices and their derivatives are derived in the modal coordinates. Numerical results show the effectiveness of the proposed approach to design the open-loop control law that modifies the shape of input torque for simultaneous slewing and vibration suppression.

• Bulletin of the Korean Chemical Society
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• v.35 no.11
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• pp.3232-3238
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• 2014

Mollugin has been reported to have various biological activities including antineoplastic, antitumor, antiviral against the hepatitis B virus, anti-aging and antimutagenic activities. An effective and concise synthesis of mollugin in two steps including kinetic control from the cheap starting material 1,4-naphthoquinone has been introduced, and mollugin derivatives thus prepared are screened for their inhibition ability against the hepatitis C virus (HCV) and the dihydrobenzochromene structure might be an additional anti-HCV agent as a new leading compound.

• Journal of Institute of Control, Robotics and Systems
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• v.5 no.2
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• pp.237-247
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• 1999

Flight parameters of a light aircraft in normal category named ChangGong-91 we identified from flight tests. Modified Maximum Likelihood Estimation (MMLE) is used to produce aerodynamic coefficients, stability and control derivatives. A Flight Training Device (FTD) has been developed based on the identified flight parameters. Flat earth, rigid body, and standard atmosphere are assumed in the FTD model. Euler angles are adapted for rotational state variables to reduce computational load. Variations in flight Mach number and Reynolds number are assumed to be negligible. Body, stability and inertial axes allow 6 second-order linear differential equations for translational and rotational motions. The equations of motion are integrated with respect to time, resulting in good agreements with flight tests.

• Proceedings of the KIEE Conference
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• 2006.04a
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• pp.219-221
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• 2006

The recently developed autopilot controller can make the input-output (I/O) dynamic characteristics of the nonlinear missile dynamics linear and independent of flight conditions. However, significant fin actuator dynamics can degenerate the I/O dynamic performance of the overall system. In this paper, we propose a singular perturbation-like method to compensate the effect of significant fin actuator dynamics in nonlinear missile control. The proposed compensation method does not require the time derivatives of fin angles but can maintain the linear I/O dynamic characteristics provided by the recently developed autopilot controller.

• Journal of Institute of Control, Robotics and Systems
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• v.4 no.1
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• pp.76-81
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• 1998

This paper presents an on-line scheme for parameter estimation of continuous-time systems, based on the model adjustment technique and the genetic algorithm technique. To deal with the initialisation and unmeasurable signal problems in on-line parameter estimation of continuous-time systems, a discrete-time model is obtained for the linear differential equation model and approximations of unmeasurable states with the observable output and its time-delayed values are obtained for the nonlinear state space model. Noisy observations may affect these approximation processes and degrade the estimation performance. A digital prefilter is therefore incorporated to avoid direct approximations of system derivatives from possible noisy observations. The parameters of both the model and the designed filter are adjusted on-line by a genetic algorithm, A set of simulation works for linear and nonlinear systems is carried out to demonstrate the effectiveness of the proposed method.

• Proceedings of the KIEE Conference
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• 2001.07d
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• pp.2470-2472
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• 2001

This paper describes the application of a fuzzy-tuning PID controller to a 3-DOF attitude control of a small model helicopter in hover for the compensation of coupling effects between each axis and system uncertainties due to the variation of engine RPM. A Low-level PID controller is designed by Ziegler-Nichols method and its gains are tuned by a high-level fuzzy system based on error states and its time derivatives. The experimental results show that the attitude control performance of fuzzy-tuning PID controller is improved comparing with that of a Ziegler-Nichols PID controller and fuzzy controller.

• 제어로봇시스템학회:학술대회논문집
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• 1996.10b
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• pp.359-362
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• 1996

The guidance system which uses the line-of-sight(LOS) rate to guide the missile towards its target has been used to the conventional differential game, such as the pursuer-evader game. Proportional navigation guidance and its derivatives have been shown to be an effective LOS rate guidance system. In this paper, we have used the genetic algorithm to construct the guidance system for the pursuer-evader type differential game. Also we have proposed the prediction model to obtain the informations about the intention of future actions of the pursuer and the evader.