• 한국미생물·생명공학회지
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• 제45권3호
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• pp.209-217
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• 2017

In the enduring investigation of the bioactive microbes, Pseudomonas aeruginosa strain (referred to as CGK-KS-1 (ICTB-315)), isolated from Chumathang hot spring, Ladakh, and India, was identified to possess a major bioactive fraction with antimicrobial and anti-biofilm properties. This bioactive metabolite was purified through bioactivity-guided fractionation. The chemical structure of this major compound was elucidated as phenazine-1-carboxamide (PCN) based on $^1H$ and $^{13}C$ NMR, FT-IR, EI-HR-MS and 2D NMR spectroscopic techniques. In the current study, PCN exhibited antimicrobial activity with MIC values ranging between $1.9-3.9{\mu}g/ml$ against various test human pathogens and Xanthomonas spp. PCN showed the anti-biofilm property with the $IC_{50}$ values ranging from 17.04 to $60.7{\mu}M$ against different test pathogens. The in silico docking studies showed PCN strongly interacted with various proteins of different Xanthomonas spp. with high binding energies. We report herein for the first time the anti-biofilm property and the docking studies of PCN. The extrolite from P. aeruginosa strain CGK-KS-1 showed promising bioactivities and may be considered as a potential candidate for application in various biocontrol strategies.

• 한국지능시스템학회논문지
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• 제26권5호
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• pp.383-389
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• 2016

본 논문은 선박의 외벽 청소를 위하여 영상기반의 용접부 인식기능을 탑재한 선체 블라시팅 로봇을 제시하였다. 본 로봇제작의 목표로서 선체 청소로봇의 설계 및 제작과정과 영상을 이용한 용접 비드 인식에 따른 성능 결과를 제시하였다. 그리고, 로봇제작에 따른 메카니즘과 로봇시스템의 제어기 제작 과정과 수직상승 메카니즘, 영상 시스템, 원격제어 기능을 갖는 선체 청소 특성에 대해서 기술하였다. 이러한 선체 청소로봇은 선박이 정박하는 동안에 청소를 수행하게 되므로 재도킹을 할 필요가 없는 장점이 있다. 따라서, 개발된 청소작업은 시간과 비용을 절감할 수 있고, 선체의 수직벽면의 주행이 가능하므로 부유물질 등을 수집할 수 있는 필러장치를 장착하고 있다. 개발된 로봇시스템의 동작 및 통신 성능테스트 결과를 통하여 성능평가 결과를 제시하였다.

• Bulletin of the Korean Chemical Society
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• 제33권11호
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• pp.3772-3776
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• 2012

Mitogen-activated protein kinase phosphatase 4 (MKP4) has proved to be a promising target for the development of therapeutics for the treatment of diabetes and the other metabolic diseases. Here, we report an example for a successful application of the structure-based virtual screening to identify three novel inhibitors of MKP4. These inhibitors have desirable physicochemical properties as a drug candidate and reveal a moderate potency with $IC_{50}$ values ranging from 4.9 to $32.3{\mu}M$. Therefore, they deserve consideration for further development by structure-activity relationship studies to optimize the inhibitory and antidiabetic activities. Structural features relevant to the stabilization of the newly identified inhibitors in the active site of MKP4 are discussed in detail.

• 로봇학회논문지
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• 제18권3호
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• pp.233-240
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• 2023

In this paper, we proposed a hybrid type robot that simultaneously surveillance and reconnaissance on the ground and in the air. It was possible to expand the surveillance and reconnaissance range by expanding the surveillance and reconnaissance area of the ground robot and quickly moving to the hidden area through the drone. First, ground robots go to mission areas through drones and perform surveillance and reconnaissance missions for urban warfare or mountainous areas. Second, drones move ground robots quickly. It transmits surveillance and reconnaissance images of ground robots to the control system and performs reconnaissance missions at the same time. Finally, in order to secure the interoperability of these hybrid robots, basic performance and environmental performance were verified. The evaluation method was tested and verified based on the KS standards.

• 대한화학회지
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• 제55권5호
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• pp.765-775
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• 2011

Novel analogs of bortezomib were designed, synthesized and in vitro biological evaluation was carried out using human tumor cell lines A549 and PC3. Docking studies of these analogs of bortezomib was discussed. According to biological investigations, the inhibitors 4, 6, and 8 were found to be more potent than reference drug candidate bortezomib. A549 cell line showed significant sensitivity towards 4, 6, and 8 with $IC_{50}$ values 14.03, 18.5, and 12.4 nM, respectively, and PC3 cell line showed IC50 values 26.1, 37.0, and 21.2 nM, respectively. The $IC_{50}$ values of bortezomib in these cell lines are 27.3 nM and 42.0 nM.

• Genomics & Informatics
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• 제19권1호
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• pp.7.1-7.13
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• 2021

Levodopa (L-DOPA) therapy is normally practised to treat motor pattern associated with Parkinson disease (PD). Additionally, several inhibitory drugs such as Entacapone and Opicapone are also cosupplemented to protect peripheral inactivation of exogenous L-DOPA (~80%) that occurs due to metabolic activity of the enzyme catechol-O-methyltransferase (COMT). Although, both Entacapone and Opicapone have U.S. Food and Drug Administration approval but regular use of these drugs is associated with high risk of side effects. Thus, authors have focused on in silico discovery of phytochemicals and evaluation of their effectiveness against human soluble COMT using virtual screening, molecular docking, drug-like property prediction, generation of pharmacophoric property, and molecular dynamics simulation. Overall, study proposed, nine phytochemicals (withaphysalin D, withaphysalin N, withaferin A, withacnistin, withaphysalin C, withaphysalin O, withanolide B, withasomnine, and withaphysalin F) of plant Withania somnifera have strong binding efficiency against human COMT in comparison to both of the drugs i.e., Opicapone and Entacapone, thus may be used as putative bioenhancer in L-DOPA therapy. The present study needs further experimental validation to be used as an adjuvant in PD treatment.

• Reproductive and Developmental Biology
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• 제33권1호
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• pp.1-5
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• 2009

To search a new pig pheromonal odorant, the $N^1$-allyl-$N^2$-(tetrahydrofuran-Z-ylmethyl)oxalamide molecule predicted by ligand based approach and molecular docking method was synthesized by nucleophilic addition-elimination reaction ($Ad_{NU-E}$) between N-allyloxalamic acid ethylester and tetrahydrofurlmethylamine. According to the evaluation results for efficiency of pig estrus control, the synthesized pig pheromonal $N^1$-allyl-$N^2$-(tetrahydrofuran-2-ylmethyl)oxalamide molecule advanced the estrus by 11.3 days (p<0.05) compared with the non-pheromone group. And from these results, it is predicted that the synthesized pig pheromonal compound will be able to increase the reproduction efficiency of pig.

• Asian Pacific Journal of Cancer Prevention
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• 제17권3호
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• pp.1571-1576
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• 2016

Alteration of the acetylation status of chromatin and other non-histone proteins by HDAC inhibitors has evolved as an excellent epigenetic strategy in treatment of cancers. The present study was sought to identify compounds with positive pharmacological profiles targeting HDAC1. Analogues of Vorinostat synthesized by Cai et al, 2015 formed the test compounds for the present pharmacological evaluation. Hydroxamte analogue 6H showed superior pharmacological profile in comparison to all the compounds in the analogue dataset owing to its better electrostatic interactions and hydrogen bonding patterns. In order to identify compounds with even better high affinity and pharmacological profile than 6H and Vorinostat, virtual screening was performed. A total of 83 compounds similar to Vorinostat and 154 compounds akin to analogue 6H were retrieved. SCHEMBL15675695 (PubCid: 15739209) and AKOS019005527 (PubCid: 80442147) similar to Vorinostat and 6H, were the best docked compounds among the virtually screened compounds. However, in spite of having good affinity, none of the virtually screened compounds had better affinity than that of 6H. In addition SCHEMBL15675695 was predicted to be a carcinogen while AKOS019005527 is Ames toxic. From, our extensive analysis involving binding affinity analysis, ADMET properties predictions and pharmacophoric mappings, we report Vorinostat hydroxamate analogue 6H to be a potential candidate for HDAC inhibition in treatment of cancers through an epigenetic strategy.

• 한국항해학회지
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• 제18권4호
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• pp.33-47
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• 1994

On developing port system, the performance tests of system in relation to ship maneuver generally consists of the three parts: the channel transit, the manoeuvring in a turning basin and the docking/undocking. The quantifications of risk of an accident has priviously been difficult due to the low occurrence of accidents relative to the number of transits. Additionally, accident statistics could not be related port system because of the large number of factors contributing to the accident. such as human error, equipment failure, visibility, light, traffic. etc. In case of the channel transit, "Relative Risk Factor(RRF)" or "Relative Risk Factor for Meeting Traffic" was proposed as the as the measures derived to quantify the relative risk of accident by M.W.Smith. This factor measure the tracking performance, the turning performance and the passing performance at meeting traffic. On the other hand, the safety of berthing maneuver is not measured with a few evaluating factors as controlled due to complex controllabilites such as steering, engine, side thrusters or tugs. This work, therefore, aims to propose the evaluating measure by the Analytic Hierarchy Process(AHP). Six experimental scenarios were establised under the various environmental conditions as independent variables. In every simulation, the difficulty of maneuver was scored by captain and compared with AHP scores. The results show almost same and from which the weights of eight evaluating factors could be fixed. Additionally, the limit value of relative factor in berthing safety to six scenarios could be estimated to 0.11.e estimated to 0.11.

• Natural Product Sciences
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• 제25권3호
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• pp.215-221
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• 2019

Inflammation is the crucial biological process of immune system which acts as body's defense and protective response against the injuries or infection. However, the systemic inflammation devotes the adverse effects such as multiple inflammation associated diseases. One of the best ways to treat this entity is by blocking the tumor necrosis factor alpha ($TNF-{\alpha}$) and TNF-related apoptosis-inducing ligand (TRAIL) to avoid the proinflammation cytokines production. Thus, this study aims to evaluate the potency of Sambucus bioactive compounds as anti-inflammation through in silico approach. In order to assess that, molecular docking was performed to evaluate the interaction properties between the $TNF-{\alpha}$ or TRAIL with the ligands. The 2D structure of ligands were retrieved online via PubChem and the 3D protein modeling was done by using SWISS Model. The prediction results of the study showed that caffeic acid (-6.4 kcal/mol) and homovanillic acid (-6.6 kcal/mol) have the greatest binding affinity against the $TNF-{\alpha}$ and TRAIL respectively. This evidence suggests that caffeic acid and homovanillic acid may potent as anti-inflammatory agent against the inflammation associated diseases. Finally, this study needs further examination and evaluation to validate the potency of Sambucus bioactive compounds.