• Journal of the Korea Academia-Industrial cooperation Society
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• v.16 no.11
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• pp.7575-7581
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• 2015

Corticotropin-releasing factor(CRF), one of the stress driven neuropeptides, was widely proposed to influence hair loss and re-growth. For the development of receptor antagonists, the screening system based on intracellular calcium signal process was developed and optimized. The aequorin parental cells were transfected with CRF1 receptor and alpha 16 promiscuous G protein cDNA to establish HEK293a16/hCRF1, a stable cell line for the human CRF1 receptor. In HEK293a16/hCRF1 cells, the range of sauvagine dose response was 12-fold higher($EC_{50}:15.21{\pm}1.83nM$) than in the transiently expressed cells, hence essential conditions for the antagonist screening experiments such as the robust signals and high solvent tolerance were secured. The standard antagonists for the CRF1 receptor, antalarmin and CP154526, resulted $IC_{50}$ values of $414.1{\pm}5.5$ and $290.7{\pm}1.9nM$, respectively. Similar results were presented with frozen HEK293a16/hCRF1 cells. Finally, our HEK293a16/hCRF1 cells with the aequorin based cellular functional assay can be a model system for the development of functional cosmetics and modulators that can have a clinical efficacy on hair re-growth.

• Carbon letters
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• v.13 no.3
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• pp.173-177
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• 2012

A drug delivery system (DDS) was prepared with a temperature and pH-responsive hydrogel. Poly(vinyl alcohol) (PVA)/poly(acrylic acid) (PAAc)/poly(N-isopropylacrylamide) (PNIPAAm)/multi-walled carbon nanotube (MWCNT) nanocomposites were prepared by radical polymerization for the temperature and pH-responsive hydrogels. MWCNTs were employed to improve both the thermal conductivity and mechanical properties of the PVA/PAAc/PNIPAAm/MWCNT nanocomposite hydrogels. Various amounts of MWCNTs (0, 0.5, 1 and 3 wt%) were added to the nanocomposite hydrogels. PVA/PAAc/PNIPAAm/MWCNT nanocomposite hydrogels were characterized with a scanning electron microscope. The mechanical properties were measured with a universal testing machine. Swelling and releasing properties of nanocomposite hydrogels were investigated at various temperatures and pHs. Temperature and pH-responsive release behavior was found to be dependent on the content of MWCNTs in nanocomposite hydrogels.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.15
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• pp.6343-6347
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• 2014

Multi-target drug design, in which drugs are designed as single molecules to simultaneously modulate multiple physiological targets, is an important strategy in the field of drug discovery. QT-011, a tamibarotene-furoxan derivative, was here prepared and proposed to exert synergistic effects on antileukemia by releasing nitric oxide and tamibarotene. Compared with tamibarotene itself, QT-011 displayed stronger antiproliferative effects on U937 and HL-60 cells and was more effective evaluated in a nude mice U937 xenograft model in vivo. In addition, QT-011 could release nitric oxide which might contribute to the antiproliferative activity. Autodocking assays showed that QT-011 fits well with the hydrophobic pocket of retinoic acid receptors. Taken together, these results suggest that QT-011 might be a highly effective derivative of tamibarotene and a potential candidate compound as antileukemia agent.

• Journal of Biomedical Engineering Research
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• v.38 no.1
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• pp.43-48
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• 2017

Chemotherapy, radiation therapy, and surgery are major methods to treat cancer. However, current cancer treatments report severe side effects and high recurrences. Recent studies about engineering nanoparticles as a drug carrier suggest possibilities in terms of specific targeting and spatiotemporal release of drugs. While many nanoparticles demonstrate lower toxicity and better targeting results than free drugs, they still need to improve their performance dramatically in terms of targeting accuracy, immune responses, and non-specific accumulation at organs. One possible way to overcome the challenges is to make precisely controlled nanoparticles with respect to size, shape, surface properties, and mechanical stiffness. Here, we demonstrate $500{\times}200nm$ discoidal polymeric nanoconstructs (DPNs) as a drug delivery carrier. DPNs were prepared by using a top-down fabrication method that we previously reported to control shape as well as size. Moreover, DPNs have multiple payloads, poly lactic-co-glycolic acid (PLGA), polyethylene glycol (PEG), lipid-Rhodamine B dye (RhB) and Salinomycin. In this study, we demonstrated a potential of DPNs as a drug carrier to treat cancer.

• Polymer(Korea)
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• v.38 no.1
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• pp.93-97
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• 2014

Biodegradable drug-eluting stent has dual functions of supporting the lumen and treating internal tumor preventing the restenosis by releasing drug. In this study, the polycaprolactone (PCL) based three dimensional (3D) mesh loaded with paclitaxel (PTX) was presented by rapid prototyping (RP) technique of solid freeform fabrication (SFF) for biodegradable drug-eluting stent application. PCL has many advantageous properties such as good biocompatibility, good mechanical properties, and good drug permeability. PTX is widely used in the cancer treatment by inhibiting tumor cell proliferation. Analytical methods of HPLC and NMR were used for simultaneous quantification of PTX. Scanning electron microscopy (SEM) was performed to observe the architecture and morphologies of 3D mesh. The cytotoxicity assay results indicated released PTX's biological activity. This study provided that PCL based 3D mesh loaded with PTX by RP technique has great potential for biodegradable drug-eluting stent application.

• Proceedings of the KSAR Conference
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• 2004.06a
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• pp.284-284
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• 2004

본 연구는 Elk 사슴에서 Magic Doctor(한경게놈텍)를 이용하여 발정동기화 인공수정 후 재발정 행동의 발현양상을 관찰하기 위해 실시하였다. 미경산록 7두와 경산록 13두를 공시하였고, 발종동기화 및 인공수정은 번식계절인 9월에 progesterone이 3 g 함유된 controlled intravaginal drug-releasing device(CIDR)를 14일간 질내에 삽입하고 제거한 후에 pregnant mare serum gonadotropin(PMSG) 250IU틀 근육 주사하여 발정동기화와 배란을 유도하였다. 인공수정은 CIDR제거 후 60∼62시간째에 실시하였고 인공수정 후 비임신 개체의 재발정 발현 양상을 관찰하였다. (중략)

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.303.2-304
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• 2003

For the purpose of obtaining high bone forming efficacy, chitosan microgranules were developed as bone substitutes. Chitosan has been applied to conduct the extracellular matrix (ECM) formation in tissue regenerative therapy. Microgranules designed in this study confer drug releasingcapacity in bone defect over long period to enhance bone regeneration. (omitted)

• Journal of Integrative Natural Science
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• v.11 no.1
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• pp.9-13
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• 2018

KiSS1-derived peptide receptor, a GPCR protein, binds with the hormone Kisspeptin plays a major role in the neuroendocrine regulation of reproduction. It is important in the onset of puberty and triggers the release of gonadotrophin-releasing hormone. It is a potential drug target for the disorders related to GnRH, hence, analysing the structural features of the receptor becomes important. The three dimensional of the receptor modelled in a previous study was utilised. In this study, we have analysed the protein - protein interaction of the receptor with Kisspeptin 10 and 15. The study revealed the important residues which are involved in the interaction. The result of this study could be helpful in understanding the mechanism of Kiss1 receptor activation and the pathophysiology of the disorders related to the receptor.

• Asian Pacific Journal of Cancer Prevention
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• v.14 no.8
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• pp.4853-4858
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• 2013

Objectives: To investigate whether hypoxia has an effect on regulation of multidrug resistance (MDR) to chemotherapeutic drugs in laryngeal carcinoma cells and explore the role of hypoxia-inducible factor-$1{\alpha}$ (HIF-$1{\alpha}$). Methods: Laryngeal cancer cells were cultured under normoxic and hypoxic conditions. The sensitivity of the cells to multiple drugs and levels of apoptosis induced by paclitaxel were determined by MTT assay and annexin-V/propidium iodide staining analysis, respectively. HIF-$1{\alpha}$ expression was blocked by RNA interference. The expression of HIF-$1{\alpha}$ gene was detected by real-time quantitative RT-PCR and Western blotting. The value of fluorescence intensity of intracellular adriamycin accumulation and retention in cells was evaluated by flow cytometry. Results: The sensitivity to multiple chemotherapy agents and induction of apoptosis by paclitaxel could be reduced by hypoxia (P<0.05). A the same time, the adriamycin releasing index of cells was increased (P<0.05). However, resistance acquisition subject to hypoxia in vitro was suppressed by down-regulating HIF-$1{\alpha}$ expression. Conclusion: HIF-$1{\alpha}$ could be considered as a key regulator for mediating hypoxia-induced MDR in laryngeal cancer cells via inhibition of drug-induced apoptosis and decrease in intracellular drug accumulation.

• The Korea Journal of Herbology
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• v.25 no.3
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• pp.35-41
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• 2010

Objectives : Allergy is an immune dysfunction caused by degranulation from mast cells in the early phase of allergic disease including allergic rhinitis (AR). The purpose of this study was to investigate the effects of Osterici Radix, roots of Ostericum koreanum Maximowicz in human mast cells and experimental allergic animal models. Methods : The anti-allergic effect of Osterici Radix water extract (NK-W) was investigated in human mast cell line, HMC-1 cells, and compound 48/80-induced systemic anaphylactic response in rats and ovalbumin (OVA)-induced AR in mice. Animals were orally administrated with NK-W (10 and 50 mg/kg) or anti-histamine drug, dosodium cromoglycate (50 mg/kg), and then intraperitoneally injected with compound 48/80 (8 mg/kg) or sensitized with 0.1% OVA into nasal. Animals were observed plasma histamine and histological changes of nasal mucosa. Also, mast cell degranulation and histamine production were determined in compound 48/80-stimulated HMC-1 cells. Results : NK-W inhibited compound 48/80-induced degranulation of mast cells and histamine releasing in HMC-1 cells. NK-W decreased mortality and serum histamine releasing in compound 48/80-induced anaphylatic rats in a dose-dependently manner. NK-W also inhibited serum histamine levels in OVA-induced AR mice and improved abnormal histological changes such as expansion of grandular cells and hypertrophy of epithelium in the nasal mucosa. These results indicate that Osterici Radix water extract suppress allergic response through downregulation of mast cell activation. Conclusions : This study suggests that a therapeutic potential of Osterici Radix as a source of anti-allergic agents for use in a number of allergic diseases.