• Natural Product Sciences
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• v.20 no.4
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• pp.227-231
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• 2014

Cimicifuga heracleifolia extract (CHE) was investigated for its effects on the release of nitric oxide (NO) and at the level of inducible nitric oxide synthase (iNOS) gene expression in mouse macrophages. We found that C. heracleifolia elicited a dose-dependent increase in NO production and the level of iNOS mRNA. Since, iNOS transcription has been shown to be under the control of the transcription factor $NF-{\kappa}B$, the effects of CHE on $NF-{\kappa}B$ activation were examined. Transient expression assays with $NF-{\kappa}B$ binding sites linked to the luciferase gene revealed that the increased level of iNOS mRNA, induced by CHE, was mediated by the $NF-{\kappa}B$ transcription factor complex. By using DNA fragments containing the $NF-{\kappa}B$ binding sequence, CHE was shown to activate the protein/DNA binding of $NF-{\kappa}B$ to its cognate site, as measured by electrophoretic mobility shift assay. These results demonstrate that C. heracleifolia stimulates NO production and is able to up-regulate iNOS expression through $NF-{\kappa}B$ transactivation.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.9
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• pp.3753-3758
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• 2015

Background: Polymeric nanoparticles are attractive materials that have been widely used in medicine for drug delivery, with therapeutic applications. In our study, polymeric nanoparticles and the anticancer drug, chrysin, were encapsulated into poly (D, L-lactic-co-glycolic acid) poly (ethylene glycol) (PLGA-PEG) nanoparticles for local treatment. Materials and Methods: PLGA: PEG triblock copolymers were synthesized by ring-opening polymerization of D, L-lactide and glycolide as an initiator. The bulk properties of these copolymers were characterized using 1H nuclear magnetic resonance spectroscopy and Fourier transform infrared spectroscopy. In addition, the resulting particles were characterized by scanning electron microscopy. Results: The chrysin encapsulation efficiency achieved for polymeric nanoparticles was 70% control of release kinetics. The cytotoxicity of different concentration of pure chrysin and chrysin loaded in PLGA-PEG ($5-640{\mu}M$) on T47-D breast cancer cell line was analyzed by MTT-assay. Conclusions: There is potential for use of these nanoparticles for biomedical applications. Future work should include in vivo investigation of the targeting capability and effectiveness of these nanoparticles in the treatment of breast cancer.

• Journal of Veterinary Science
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• v.24 no.3
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• pp.44.1-44.17
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• 2023

Background: Antibiotic resistance is a significant public health concern around the globe. Antimicrobial peptides exhibit broad-spectrum and efficient antibacterial activity with an added advantage of low drug resistance. The higher water content and 3D network structure of the hydrogels are beneficial for maintaining antimicrobial peptide activity and help to prevent degradation. The antimicrobial peptide released from hydrogels also hasten the local wound healing by promoting epithelial tissue regeneration and granulation tissue formation. Objective: This study aimed at developing sodium alginate based hydrogel loaded with a novel antimicrobial peptide Chol-37(F34-R) and to investigate the characteristics in vitro and in vivo as an alternative antibacterial wound dressing to treat infectious wounds. Methods: Hydrogels were developed and optimized by varying the concentrations of crosslinkers and subjected to various characterization tests like cross-sectional morphology, swelling index, percent water contents, water retention ratio, drug release and antibacterial activity in vitro, and Pseudomonas aeruginosa infected wound mice model in vivo. Results: The results indicated that the hydrogel C proved superior in terms of cross-sectional morphology having uniformly sized interconnected pores, a good swelling index, with the capacity to retain a higher quantity of water. Furthermore, the optimized hydrogel has been found to exert a significant antimicrobial activity against bacteria and was also found to prevent bacterial infiltration into the wound site due to forming an impermeable barrier between the wound bed and external environment. The optimized hydrogel was found to significantly hasten skin regeneration in animal models when compared to other treatments in addition to strong inhibitory effect on the release of pro-inflammatory cytokines (interleukin-1β and tumor necrosis factor-α). Conclusions: Our results suggest that sodium alginate -based hydrogels loaded with Chol-37(F34-R) hold the potential to be used as an alternative to conventional antibiotics in treating infectious skin wounds.

• Journal of Pharmaceutical Investigation
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• v.30 no.3
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• pp.151-158
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• 2000

Gel and cream containing 5% and 10% ketonic fraction (KF) of Leptospermum scoparium, respectively were formulated. Antimicrobial activity, stability, anti-inflammatory effect, rheological properties, drug release and acute toxicity for these topical efficacy were evaluated. Gel and cream containing neomycin or gentamycin in combination with KF has potent antimicrobial activity. Gel and cream were physically stable and did not show any creaming for 6 months storage. Gel showed plastic flow with yield value and cream showed pseudoplastic flow with hysteresis loop. The gel and cream containing KF showed higher viscosity than control or commercial one. The viscosity increased as the concentration of KF increased. Both 10% gel and cream showed a significant decrease in swelling when applied to the carrageenan- injected paw, suggesting local antiinflammatory activity. Particularly, 10% gel preparation showed similar antiinflammatory activity when compared with commercially available drugs. Percent of drug released and diffusion coefficient were in the order of 5% gel, 10% gel, 5% cream, and 10% cream, respectively. There were no significant changes of body weight in rats percutaneously administered with 10% cream and gel when compared with control. There were no induced acute toxicity when 10% cream or gel was applied to rats. Leptospermum scoparium could be practicaly used in topical preparations.

• The Korean Journal of Physiology and Pharmacology
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• v.28 no.3
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• pp.275-284
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• 2024

Worldwide, cardiovascular disease is the main cause of death, which accordingly increased by hyperlipidemia. Hyperlipidemia therapy can include lifestyle changes and medications to control cholesterol levels. Statins are the medications of the first choice for dealing with lipid abnormalities. Rosuvastatin founds to control high lipid levels by hindering liver production of cholesterol and to achieve the targeted levels of low-density lipoprotein cholesterol, another lipid lowering agents named ezetimibe may be used as an added therapy. Both rosuvastatin and ezetimibe have low bioavailability which will stand as barrier to decrease cholesterol levels, because of such depictions, formulations of this combined therapy in nanotechnology will be of a great assistance. Our study demonstrated preparations of nanoparticles of this combined therapy, showing their physical characterizations, and examined their behavior in laboratory conditions and vivo habitation. The mean particle size was uniform, polydispersity index and zeta potential of formulations were found to be in the ranges of (0.181-0.72) and (-13.4 to -6.24), respectively. Acceptable limits of entrapment efficiency were affirmed with appearance of spherical and uniform nanoparticles. In vitro testing showed a sustained release of drug exceeded 90% over 24 h. In vivo study revealed an enhanced dissolution and bioavailability from loaded nanoparticles, which was evidenced by calculated pharmacokinetic parameters using triton for hyperlipidemia induction. Stability studies were performed and assured that the formulations are kept the same up to one month. Therefore, nano formulations is a suitable transporter for combined therapy of rosuvastatin and ezetimibe with improvement in their dissolution and bioavailability.

• Applied Chemistry for Engineering
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• v.28 no.4
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• pp.404-409
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• 2017

Natural polymer chitosan has been widely applied to medical fields due to its biochemical activities such as anticancer, antibacterial and lowering cholesterol in addition to biocompatibility and biodegradability. Currently, researches are being actively conducted to develop various drug-encapsulated chitosan nanoparticles for curing different diseases by applying chitosan to a drug delivery system. The free amine ($-NH_2$) group present in chitosan can bind to various hydrophobic groups by physical and chemical modification and the chitosan with hydrophobic groups can form shell-core nanoparticles by self-assembly when dispersed in water. In addition, an insoluble drug can increase the solubility against water when it was encapsulated in the core of chitosan nanoparticles. Also, the therapy effect can be maximized by minimizing side effects of drugs such as proteins, anticancer drugs and vaccines when they were encapsulated in the core of chitosan nanoparticles. Moreover, it is possible to control the particle size and release rate according to the hydrophobic group introduced to chitosan, so that it can be applied to a wide range of medical fields. The purpose of this review is to discuss the preparation and property of chitosan nanoparticles modified with various hydrophobic groups, and the application to drug delivery systems according to their property.

• The Korean Journal of Medicine
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• v.93 no.6
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• pp.509-517
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• 2018

A small number of viable tuberculosis bacilli can reside in an individual with latent tuberculosis infection (LTBI) without obvious clinical symptoms or abnormal chest radiographs. Diagnosis and treatment of LTBI are important for tuberculosis (TB) control in public and private healthcare facilities, particularly in high-risk populations. The updated 2017 Korean guidelines for TB recommend that tuberculin skin tests, interferon-gamma release assays, or a combination of them can be used for the diagnosis of LTBI, depending on the age and immune status of the patient as well as their TB contact history. For diagnosis of LTBI, exclusion of active TB is essential, and the possibility of healed TB in those without a history of treatment for TB but at risk of its development must be considered. The treatment options for LTBI include isoniazid, rifampicin, isoniazid/rifampicin, and isoniazid/rifapentine. The benefits and risks of these agents based on the age of the patient and their hepatotoxicity must be considered when selecting the appropriate drug. Standardized diagnosis and treatment of LTBI based on the updated 2017 guidelines will contribute to the control of TB in Korea as well as to further revisions of the guidelines.

• Polymer(Korea)
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• v.32 no.3
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• pp.193-198
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• 2008

Sibutramine is a highly crystalline and poorly water soluble drug as the appetite depressant for obesity treatment. In order to increase water solubility of sibutramine, microspheres including sibutramine were prepared by solid dispersion method using a spray dryer. The crystallinity and morphology of the prepared microspheres were confirmed by SEM and XRD. The morphology of micro spheres has gradually changed into spherical shape as increasing evaporation rate of solvent. According to XRD analysis, crystallinity of sibutramine in micro spheres was decreased by below 10%. Release behavior of microspheres was investiaged at pH 1.2, pH 6.8, and solubility of the sibutramine was significantly different depending on pH. The hard capsule showed fast release of sibutramine comparing with the tablet. These results demonstrated that the pharmaceutical preparation is able to control the release behaviors.

• Polymer(Korea)
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• v.31 no.3
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• pp.215-220
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• 2007

The control of the surface energy by electrohydrodynamic force provides electrospraying with various potential advantages such as simple particle size control, mono-dispersity, high recovery, and mild processing conditions. The advantages are quite helpful to improve the stability of protein drug and control its release. Herein, the nano-encapsulation of protein drugs using electrospraying was investigated. Albumin as a model protein was processed using uniaxial and co-axial electrospraying, and chitosan, polycaporlactone (PCL), and poly (ethylene glycol) (PEG) were used as encapsulation materials. The major processing parameters such as the conductivity of spraying liquids, flow rate, the distance of electrical potential gradient, etc were measured to obtain the maximum efficiency. In the chitosan systems, mean particles size decreases as flow rate and the distance between nozzle and the collecting part decreases. In the uniaxial technique of the PCL systems, mean particles size decreases as flow rate decreases. In the coaxial technique of the PCL systems, it was found that the particles size gets larger under the application of the higher ratio of inner-to-outer liquid flow rates. The primary particles formed out of an electrospraying nozzle showed narrow particle size distribution, but once they arrived to the collecting part, aggregation behavior was observed obviously. Efficient nano-encapsulation of albumin with PCL, PEG, and chitosan was conveniently achieved using electrospraying at above 12 kV.

• Journal of Oriental Neuropsychiatry
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• v.14 no.1
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• pp.85-106
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• 2003

Studies have shown that both the psychomotor stimulant effects and rewarding properties of addictive drugs, including morphine, are sensitized by repeated drug administration and it is suggested that both of these effects are mediated by the same or closely overlapping dopamine systems. Specifically, the mesolimbic dopamine system has been implicated in the reinforcing and sensitizing properties of morphine. In oriental medicine, Shenmen (HT7) point on the heart channel has been used to treat mental and psychosomatic disorders. This study was designed to investigate the effect of acupuncture on acute and repeated morphine-induced changes in extracellular dopamine levels using in vivo microdialysis and morphine-induced behavioral changes. In the morphine sensitization experiment, male Sprague-Dawley rats were treated twice a day for three days with increasing doses of morphine (10, 20 and 40 mg/kg, s.c.) or with saline. After 15 days of withdrawal, rats were challenged with morphine hydrochloride (5mg/kg, s.c.). Acupuncture was applied at bilateral Shenmen (HT7) points for 1 min after the morphine challenge. In the acute experiment, rats also received acupuncture for 1 min after an injection of morphine hydrochloride (5 mg/kg, s.c.). Results showed that acupuncture at the specific acupoint HT7, but not at control points (tail) significantly decreased both dopamine release and behavior induced by a systemic morphine challenge or a single sc morphine injection in the acute animals. These results suggest that reduction in sensitization may be one mechanism whereby acupuncture alleviates morphine craving in addicts.