• 한국미생물학회:학술대회논문집
• /
• 한국미생물학회 2003년도 International Meeting of the Microbiological Society of Korea
• /
• pp.77-79
• /
• 2003

Current therapeutic strategies far anthrax have had no significant impact on anthrax mortality over the last several decades. This study used a matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF MS) discovery platform to generate protein expression profiles in search of overexpressed proteins in murine macrophage cells (RAW264.7) which infected with Bacillus anthracis spores as potentially novel molecular targets. Two differentially expressed proteins were identified in infected murine macrophage cells as Syndapin and CDC46, respectively. Syndapins are potential links between the cortical actin cytoskeleton and endocytosis. Other two proteins were identified from murine macrophage cells infected with avirulent spores as ITBG-2 (CD18) and HSPA5, respectively. These data demonstrate the feasibility of using a MALDI-TOF platform to generate protein expression profiles and identify potential molecular targets for anthrax therapeutics.

• Advances in Traditional Medicine
• /
• 제8권4호
• /
• pp.365-373
• /
• 2008

Murraya koenigii leaves commonly known as 'curry patta' are routinely added to Indian gravy and vegetarian dishes by south Indian as a favourate condiment. The present study was undertaken to investigate the effects of Murraya koenigii leaves (MKL) on memory in rats. Elevated plus-maze and Hebb-Williams maze served as the exteroceptive behavioral models for testing memory. Diazepam-, scopolamine- and ageing-induced amnesia served as the interoceptive behavioral models. MKL fed orally to various groups of young and aged rats with diet containing 2, 4 and 8% w/w of MKL for 30 days consecutively were investigated. The MKL diets produced a significant dose-dependent improvement in memory scores of young and aged rats and significantly reduced the amnesia induced by scopolamine (0.4 mg/kg, i.p.) and diazepam (1 mg/kg, i.p.). Therefore, it would be worthwhile to specifically investigate the therapeutic potential of MKL in the management of dementia patients.

• Bulletin of the Korean Chemical Society
• /
• 제34권12호
• /
• pp.3782-3786
• /
• 2013

Non-small cell lung cancer (NSCLC) is the most common type of lung cancer and that accounts for 85% of lung cancer patients. Although several EGFR-targeted drugs have been developed in the treatment of NSCLC, the clinical efficacy of EGFR-targeted drugs in NSCLC is limited by the occurrence of drug resistance. In this regard, Hsp90 represents great promise as a therapeutic target of cancer due to its potential to simultaneously disable multiple signaling pathways. In this study, we discovered that a natural product, flavokawain B disrupted Hsp90 chaperoning function and impaired the growth of gefitinib-resistant non-small cell lung cancer (H1975). The result suggested that flavokawain B could serve as a potential lead compound to overcome the drug resistance in cancer chemotherapy.

• Asian Pacific Journal of Cancer Prevention
• /
• 제14권8호
• /
• pp.4635-4639
• /
• 2013

Multi-drug resistance (MDR) is an essential aspect of human lung cancer chemotherapy failure. Recent studies have shown that vinorelbine is involved in underlying processes in human tumors, reversing the MDR inseveral types of cancer cells. However, the roles and potential mechanism are not fully clear. In this study, we explored effects of vinorelbine in multi-drug resistance reversal of human lung cancer A549/DDP cells. We found that vinorelbine increased drug sensitivity to cisplatin and intracellular accumulation of rhodamine-123, while decreasing expression of P-glycoprotein (P-gp), multi-drug resistance-associated protein (MRP1) and glutathione-S-transferase ${\pi}$ (GST-${\pi}$) in A549/DDP cells. At the same time, we also established downregulation of p-Akt and decreased transcriptional activation of NF-${\kappa}B$ and twist after vinorelbine treatment. The results indicated that vinorelbine might be used as a potential therapeutic strategy in human lung cancer.

• Biomolecules & Therapeutics
• /
• 제14권1호
• /
• pp.36-39
• /
• 2006

Some flavones/flavonols were previously found to inhibit collagenase. To establish a therapeutic potential for skin inflammation, twenty-three synthetic flavone derivatives were examined for their inhibitory potential against collagenase from Clostridium histolyticum. From the results, it was found that most of them having various hydroxyl, methoxyl, methylsulfuryl and/or chloro substitution(s) on A- and B-rings were not efficient collagenase inhibitors. Among the synthetic flavones tested, only two synthetic derivatives, 3',4'-dihydroxyflavone and 5-hydroxy-4'-methoxyflavone, weakly inhibited bacterial collagenase (13-29% inhibition at 50-100 ${\mu}M$).

• 한국응용약물학회:학술대회논문집
• /
• 한국응용약물학회 2008년도 Proceedings of the Convention
• /
• pp.23-30
• /
• 2008

Mitochondria biogenesis requires a coordination of two genomes, nuclear DNA (nDNA) and mitochondrial DNA (mtDNA). Disruption of mitochondria function leads to a loss of mitochondrial membrane potential and ATP generating capacity and consequently results in chronic degenerative diseases including insulin resistance, metabolic syndrome and neurodegenerative diseases. Although PPAR-${\gamma}$ coactivator-$1{\alpha}$ (PGC-$1{\alpha}$) was discovered as a central regulator of mitochondria biogenesis and a transcriptional co-activator of nuclear respiratory factor (NRF) and mitochondrial transcription factor A (Tfam), the expressions of PGC-$1{\alpha}$, NRF and Tfam were not significantly altered in tissues showing abnormal mitochondria functions. This observation suggests that there should be another regulator(s) for mitochondria function. Here, we demonstrate microRNAs (miRNAs) can modulate mitochondria function. Overexpression of microRNA dissipated mitochondrial membrane potential and increased ROS production in vitro and in vivo. It will be discussed the target of microRNA and its role in metabolic syndrome.

• 통합자연과학논문집
• /
• 제4권4호
• /
• pp.255-265
• /
• 2011

Marine ecosystems are often characterized by a high biological diversity, and it corresponds to a high chemical diversity. Up to present, more than 20,000 new bioactive substances have been isolated from marine organisms, where considerable numbers of these naturally occurring derivatives are developed as potential candidates for pharmaceutical application. In this process, screening of natural products from marine organisms that could potentially inhibit the expression of metalloproteinases has gained a huge popularity. Cancer is considered as one of the deadliest diseases in the medical field. Matrix metalloproteinase (MMPs) can degrade extracellular matrix (ECM) components and play important roles in a variety of biological and pathological processes. Matrix metalloproteinase inhibitors (MMPIs) have been identified as potential therapeutic candidates for metastasis, arthritis, chronic inflammation and wrinkle formation.

• 통합자연과학논문집
• /
• 제10권1호
• /
• pp.20-26
• /
• 2017

Chemerin receptor, which predominantly expressed in immune cells as well as adipose tissue, was found to stimulate chemotaxis of dendritic cells and macrophages to the site of inflammation. Chemerin is a widely distributed multifunctional secreted protein implicated in immune cell migration, adipogenesis, osteoblastogenesis, angiogenesis, myogenesis, and glucose homeostasis. Recent studies suggest chemerin may play an important role in the pathogenesis of obesity and insulin resistance and it becomes a potential therapeutic target for treating type II diabetes. The crystal structure of chemerin receptor has not yet been resolved. Therefore, in the present study, homology modelling of CMKLR1 was done utilizing the crystal structure of human angiotension receptor in complex with inverse agonist olmesartan as the template. Since the template has low sequence identity, we have incorporated both threading and comparative modelling approach to generate the three dimensional structure. 3D models were generated and validated. The reported models can be used to characterize the critical amino acid residues in the binding site of CMKLR1.

• Bulletin of the Korean Chemical Society
• /
• 제35권4호
• /
• pp.1154-1158
• /
• 2014

Hsp90 is an ubiquitous molecular chaperone protein, which plays an important role in regulating maturation and stabilization of many oncogenic proteins. Due to its potential to simultaneously disable multiple signaling pathways, Hsp90 represents great promise as a therapeutic target of cancer. In this study, we synthesized flavokawain analogues and evaluated their biological activities against drug-resistant cancer cells. The study indicated that compound 1i impaired the growth of gefitinib-resistant non-small cell lung cancer (H1975), down-regulated the expression of Hsp90 client proteins including EGFR, Her2, Met, Akt and Cdk4, and upregulated the expression of Hsp70. The result strongly suggested that compound 1i inhibited the proliferation of cancer cells through Hsp90 inhibition. Overall, compound 1i could serve as a potential lead compound to overcome the drug resistance in cancer chemotherapy.

• 생물정신의학
• /
• 제25권2호
• /
• pp.21-30
• /
• 2018

Attention deficit hyperactivity disorder (ADHD) is a common childhood psychiatric disorder. Recently, it has been suggested that brain-derived neurotropic factor (BDNF) may play a role in the pathogenesis of ADHD. Our aim of this review is to understand the physiological functions of BDNF and its potential relationship with ADHD and therapeutic approaches of ADHD. Searches were conducted in Pubmed and Research Information Service System (RISS). In this review, we summarized important literatures for the physiological functions of BDNF in neurodevelopment, change of serum BDNF level in ADHD, association of BDNF polymorphism and ADHD and potential association of treatment of ADHD with serum BDNF level. Further studies are required to more clearly understand the source and the role of BDNF in ADHD and to develop BDNF based-ADHD treatement.