• Proceedings of the Korean Society of Applied Pharmacology
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• 1999.04a
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• pp.1-4
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• 1999

The potential therapeutic benefit of nicotinic ligands in a variety of neurodegenerative pathologies involving the CNS has energized research efforts to develop nicotinic acetylcholine receptor (nAChR) subtype-selective ligands. In particular, there has been a concerted effort to develop nicotinic compounds with selectivity for CNS nAChRs as potential pharmacological tools in the management of these disorders. The characterization of other novel nicotinic ligands such as epibatidine. showing a marked increase in potency at nAChRs, has provided additional support for the development of potent, selective ligands at individual nAChR subtypes. We have developed and studied a number of nicotinic compounds to identify potential candidates exhibiting such selectivity. In the present study, we report the synthesis and biological evaluations of some azabicyclic and azatricyclic nicotine analogs to decipher the relationship among steric requirements of the nicotine's pyrrolidine ring system, binding affinity and subtype-selectivity.

• Archives of Pharmacal Research
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• v.13 no.4
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• pp.385-387
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• 1990

3-[(1-Methyl-1H-tetrazol-5-y)thiomethyl] is one of the most important side chains in cephaloporins. This side chain which occures in numerous antibacterial agents, suc as cefamandole, latamoxef, cefoperazone, and cefmenoxime, contributes remarkable potency and broad spectrum. For the continuous work of study on the development of broad spectrum cephalosporins, we become interested in the effect of structural modification of the substituent at the N-1 position of mercaptoterazole toward biological activity because our recent work had demonstraated that the arylsubstituted mercaptotetrazoles (Fig. 1) had favorable effect on the activity against gram-positive bacteria. The main focus of this report was to investigate the relationship between activity and functional groups in the mercaptotetrazole.

• Archives of Pharmacal Research
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• v.22 no.2
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• pp.184-188
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• 1999

A series of 4-amino Capsaincin anallogs 15, 17 and 19 were prepared to investigate the bioisosteric effect of 4-amino group, and all these compounds exhibited moderate or weak potency from their analgesic test. From our previous results and others, 4-hydroxyl group as well as 3-methoxy substituent could be crucial for high analgesic activity. This biological results also shows that the activity is sensitive to alkyl chain length in hydrophobic region and the phenylacetic amides 19 are more active than the corresponding urea derivatives 17.

• Archives of Pharmacal Research
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• v.15 no.2
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• pp.187-189
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• 1992

In the preceding paper, we reported the synthessis and biological properties of cephalosporins having quinoliniumthiomethyls at the C-3 position and demonstrated that quinoliniumthiomethylcephalosporins exhibited an extended antibacterial spectrum including antipseudomonal activity, especially strong antiGram-positive activity. With the aim of elaboration to optimize the antibacterial potency of the quaternary ammonium cephalosporins, we have studied the modification of substituents in the pyrrolidine ring of cefepime 1 which is characterized by its potent activity.

• The Sea:JOURNAL OF THE KOREAN SOCIETY OF OCEANOGRAPHY
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• v.26 no.3
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• pp.263-276
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• 2021

Marine benthic organisms have been used as the indicators for the environment assessment and recently considered as a very important component in the biodiversity and ecosystem restoration. In Korean waters, the quantitative data on marine benthos was used as one of major components for the marine pollution assessment for 50 years since 1970s. The species identification which is an important factor for the quantitative biological data was mainly performed by the marine benthic ecologists. This leads to the deterioration of the data quality on marine benthos from the misidentication of major taxonomic groups due to the lack of taxonomic expertise in Korea. This taxonomic problem has not been solved until now and remains in most data from national research projects on the marine ecosystems in Korean waters. Here we introduce the quality assurance and control (QA/QC) system for the marine biological data in UK, that is, NMBAQC (Northeast Atlantic Marine Biological Analytic and Quality Control) Scheme which has been performed by private companies to solve similar species identification problems in UK. This scheme asks for all marine laboratories which want to participate to any national monitoring programs in UK to keep their identification potency at high level by the internal quality assurance systems and provides a series of taxonomic workshops and literature to increase their capability. They also performs the external quality control for the marine laboratories by performing the Ring Test using standard specimens on various faunal groups. In the case of Korea, there are few taxonomic expertise in two existing national institutions and so they can't solve the taxonomic problems in marine benthic fauna data. We would like to provide a few necessary suggestions to solve the taxonomic problems in Korean marine biological data in short-terms and long-terms: (1) the identification of all dominant species in marine biological data should be confirmed by taxonomic expertise, (2) all the national research programs should include taxonomic experts, and (3) establishing a private company, like the Korea marine organism identification association (KMOIA), which can perform the QA/QC system on the marine organisms and support all Korean marine laboratories by providing taxonomic literature and species identification workshops to enhance their potency. The last suggestion needs more efforts and time for the establishment of that taxonomic company by gathering the detailed contents and related opinions from diverse stakeholders in Korea.

• The Korean Journal of Physiology and Pharmacology
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• v.2 no.5
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• pp.637-644
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• 1998

Previously, we have isolated authentic bombesin and another bombesin like peptide named bombesin like immunoreactivity (BLI)-K2 from the skin of Korean fire-bellied toad, Bombina orientalis. In the present study, we have newly purified three heterogeneous forms of BLI named BLI-K3, BLI-K4, and BLI-K5 from side fractions obtained in previous isolation of bombesin like peptide. The BLIs were separated into five peaks on a column of $C_{18}$ preparative HPLC. Among them, three minor peaks containing BLI-K3, K4, and K5 were purified by means of sequential chromatography on the columns of SP cation exchange HPLC and $C_{18}$ reverse phase HPLC. The purified BLI-K3 and K4 showed high binding affinity to an anti-bombesin serum (LBE 2G-2) with binding potency of 72 and 95%, respectively, relative to that of bombesin. However, they did not possess any distinctive biological activity of bombesin like peptide. On the contrary, the biological activity of BLI-K5 was similar to that of bombesin but its binding affinity to an anti-bombesin serum was low. The results indicate that three heterogeneous forms of BLI were coexpressed with bombesin and BLI-K2 in the skin of B. orientalis. All forms of the purified BLI in the present study were immunologically active but only BLI-K5 possessed the distinctive biological activity of bombesin like peptide.

• Journal of Embryo Transfer
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• v.23 no.2
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• pp.67-76
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• 2008

Since the birth of Dolly using fully differentiated somatic cells as a nuclear donor, viable clones were generated successfully in many mammalian species. These achievements in animal cloning demonstrate developmental potential of terminally differentiated somatic cells. At the same time, the somatic cell nuclear transfer (SCNT) technique provides the opportunities to study basic and applied biosciences. However, the efficiency generating viable offsprings by SCNT remains extremely low. There are several explanations why cloned embryos cannot fully develop into viable animals and what factors affect developmental potency of reconstructed embryos by the SCNT technique. The most critical and persuasive explanation for inefficiency in SCNT cloning is incomplete genomic reprogramming, such as DNA methylation and histone modification. Numerous studies on genomic reprogramming demonstrated that incorrect DNA methylation and aberrant epigenetic reprogramming are considerably correlated with abnormal development of SCNT cloned embryos even though its mechanism is not fully understood. The SCNT technique is useful in cloning farm animals because pluripotent stem cells are not established in farm animal species. Therapeutic cloning combined with genetic manipulation will help to control various human diseases. Also, the SCNT technique provides a chance to overcome excessive demand for the organs by production of transgenic animals as xenotransplantation resources. Here, we describe the factors affecting the efficiency of generating cloned farm animals by the SCNT technique and discuss future directions of animal cloning by SCNT to improve the cloning efficiency.

• Weed & Turfgrass Science
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• v.4 no.4
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• pp.321-329
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• 2015

The present study aimed to evaluate the phytotoxic potential of essential oils. For this purpose, 18 essential oil samples extracted from Korean plants and 64 commercial essential oils were screened for their phytotoxic potential against the seedling growth of Brassica napus L. (rapeseed). Among the 82 samples, 11 commercial oils (cinnamon, citronella, clove, cumin seed, geranium, jasmine, lemongrass, palmarosa, pimento, rose otto and spearmint) strongly inhibited the seedling growth with $GR_{50}$ value < $150{\mu}g\;mL^{-1}$. Major components from these effective essential oils were identified by solid phase microextraction/gas chromatography-mass spectrometry (SPME/GC-MS). GC-MS analyses revealed that the effective samples mainly consist of benzyl benzoate, carvone, citral, citronellol, eugenol, geraniol, D-limonene and terpinene. Subsequently, bioactivity of these individual components was evaluated against the seedling growth of B. napus, Echinochloa crus-galli and Aeschynomene indica. The components from different chemical groups exhibited different potency in inhibiting the seedling growth with varied $GR_{50}$ values ranged from $29{\mu}g\;mL^{-1}$ to > $1000{\mu}g\;mL^{-1}$. In the greenhouse experiment, citral and geraniol completely suppressed the growth of all the tested 10 plants at $100kg\;ha^{-1}$. In conclusion, the individual essential oil components geraniol and citral could be used as natural herbicides for weed management.

• YAKHAK HOEJI
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• v.51 no.6
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• pp.463-468
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• 2007

Chong Myung Tang is consisted of three medicinal herbs (Acori Graminei Rhizoma, Polygalae Radix and Hoelen cum Radix). It has been used as a medicine for the purpose of learning and memory improvement. In this paper, Chong Myung Tang was screened the biological activities for Alzheimer's disease. The extract (70% ethanol) of Acari Graminei Rhizoma (1 mg/ml) showed that acetylcholinesterase (AChE) and amyloid beta ($A{\beta}$) peptide aggregation inhibitory potency are 43.1% and 76.5%, respectively. The extract of Polygalae Radix showed inhibitory activity against $A{\beta}_{1-42}$ peptide aggregation (51.5%). To predict the drug-likeness, oral absorption ability; blood-brain barrier (BBB) penetraion rate, mutagenecity and carcinogenicity; in silico screening was performed against 16 compounds in the three medicinal herbs. According to the results, all compounds have appropriate chemical structures as medicines. The six compounds in Acori Graminei Rhizoma and the five compounds in Hoelen cum Radix showed excellent oral absorption rate and BBB penetration rate. The four compounds in Polygalae Radix showed excellent oral absorption rate, but their BBB penetration was presented low rate. And, the extract of Hoelen cum Radix didn't show AChE and $A{\beta}_{1-42}$ peptide aggregation inhibitory activities in vitro. Therefore, their activity in brain may be other mechanism. According to all of the results, in silico prediction technology is convenient and effective to determine biological active compounds in medicinal herbs.

• Journal of Applied Biological Chemistry
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• v.66
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• pp.29-38
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• 2023

Recent studies have highlighted the link between diseases and inflammation across our lifespan. Our sedentary lifestyle, high-calorie diet, chronic stress, chronic infections, and exposure to pollutants and xenobiotics, collectively intensify the course and recurrence of infections and inflammation in our bodies, promoting the prevalence of chronic diseases and aging. Given such phenomena and considering additional factors such as the frequency of prescription, and easy access to over-the-counter drugs, the need for anti-inflammatory therapeutics is ever-increasing. However, the readily available anti-inflammatory treatment option comes with a greater risk of side effects or high cost (biologics). Therefore in this growing competition of discovering and developing new potent anti-inflammatory drugs, we focused on utilizing the established knowledge of traditional medicine to find lead compounds. Since lead optimization is an indispensable step toward drug development, we applied this concept for the production of potent anti-inflammatory compounds achieved by structural modification of flavonoids. The derivative obtained through acetylation of myricetin, 3,3',4',5,5',7-hexaacetate myricetin, showed a greater inhibitory effect in the production of pro-inflammatory mediators such as nitric oxide, Prostaglandin E₂, and pro-inflammatory cytokines like interleukin-6, interleukin1β, in lipopolysaccharide-stimulated RAW264.7 mouse macrophage cells compared to myricetin. The increased potency of inhibition was in conjunction with an increased inhibitory effect on inducible nitric oxide synthase and cyclooxygenase-2 proteins. Through such measures, this study supports lead optimization for well-established lead compounds from traditional medicine using a simpler and greener chemistry approach for the purpose of designing and developing potent anti-inflammatory therapeutics with possibly fewer side effects and increased bioavailability.