• Title/Summary/Keyword: Natural source

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Chemical Genomics with Natural Products

  • Jung, Hye-Jin;Ho, Jeong-Kwon
    • Journal of Microbiology and Biotechnology
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    • v.16 no.5
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    • pp.651-660
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    • 2006
  • Natural products are a rich source of biologically active small molecules and a fertile area for lead discovery of new drugs [10, 52]. For instance, 5% of the 1,031 new chemical entities approved as drugs by the US Food and Drug Administration (FDA) were natural products between 1981 and 2002, and another 23% were natural product-derived molecules [53]. These molecules have evolved through millions of years of natural selection to interact with biomolecules in the cells or organisms and offer unrivaled chemical and structural diversity [14, 37]. Nonetheless, a large percentage of nature remains unexplored, in particular, in the marine and microbial environments. Therefore, natural products are still major valuable sources of innovative therapeutic agents for human diseases. However, even when a natural product is found to exhibit biological activity, the cellular target and mode of action of the compound are mostly mysterious. This is also true of many natural products that are currently under clinical trials or have already been approved as clinical drugs [11]. The lack of information on a definitive cellular target for a biologically active natural product prevents the rational design and development of more potent therapeutics. Therefore, there is a great need for new techniques to expedite the rapid identification and validation of cellular targets for biologically active natural products. Chemical genomics is a new integrated research engine toward functional studies of genome and drug discovery [40, 69]. The identification and validation of cellular receptors of biologically active small molecules is one of the key goals of the discipline. This eventually facilitates subsequent rational drug design, and provides valuable information on the receptors in cellular processes. Indeed, several biologically crucial proteins have already been identified as targets for natural products using chemical genomics approach (Table 1). Herein, the representative case studies of chemical genomics using natural products derived from microbes, marine sources, and plants will be introduced.

Inhibitors of Adipogenesis in 3T3-L1 Cells Isolated from Wheat Bran (밀겨 유래의 3T3-L1 세포 지방생성 억제물질)

  • Jeong, Won-Sik;Hong, Seong-Su;Lee, Jung-A;Ahn, Eun-Kyung;Oh, Joa-Sub
    • Korean Journal of Pharmacognosy
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    • v.42 no.4
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    • pp.302-308
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    • 2011
  • As a part of our ongoing program on finding biologically active components from natural source we found three known constituents from the EtOH extract of the wheat bran. The known compounds were identified as tachioside (1), pinellic acid (2) and tryptophan (3). The structure and relative stereochemistry were determined from MS, 1D and extensive 2D NMR techniques as well as by comparison of their data with the published values. All isolates were tested their inhibitory effects on the adipogenesis in 3T3-L1 cells. The effect of compounds from wheat bran on 3T3-L1 adipocyte differentiation were measured by Oil Red O staining. These results demonstrate that tachioside (1) and pinellic acid (2) decreased lipid content in 3T3-L1 adipocytes by inhibiting lipogenesis. These compounds had shown antiobesity activities.

Fungi-rice bran based Fermentation of Coptis Chinensis and Curcuma Longa Root and its Influence of Silk Dyeing

  • Park, Young Mi;Choi, Jae Hong
    • Fashion & Textile Research Journal
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    • v.15 no.4
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    • pp.635-641
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    • 2013
  • This study examined the dye-properties of natural fabrics dyed with Coptis chinensis and Curcuma longa root fermented with fungi. The optimum culture conditions for the fermentation of microorganisms, the relationship between natural dye color and fermentation conditions were investigated. Two different medical herbs (ground to 80-100 mesh in size) were used as a natural dyeing source. Phellinus linteus (P. linteus), which can grow in different media, such as Agarmedium (only agar containing medium), maltose extract agar (MA) and potato dextrose extract agar (PDA) culture media, were isolated from the medium. P. linteus was confirmed to be the optimum microorganism for the fermentation of Coptis chinensis and Curcuma longa, and the MA medium was confirmed to be the best for culturing. When using the microorganism as the fermenting agent, $32^{\circ}C$ was found to be the optimum fermenting temperature for both natural colorants. Regarding the dyeing property of the fermented natural dye, silk was dyed quite darkly in an appearance by naked eye estimation and the K/S value in the color strength of silk reached a high level of 16 after the fermenting process. The washing fastness of dyed silk after treatment washing was reduced from 4 to under4 and indicates that dyed silk with fermented plant was not unsubstantial. The light fastness was 1 to 2, showing intended to maintain due to the fermentation process.

Elucidating Molecular Interactions of Natural Inhibitors with HPV-16 E6 Oncoprotein through Docking Analysis

  • Kumar, Satish;Jena, Lingaraja;Galande, Sneha;Daf, Sangeeta;Mohod, Kanchan;Varma, Ashok K.
    • Genomics & Informatics
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    • v.12 no.2
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    • pp.64-70
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    • 2014
  • Human papillomavirus (HPV) infection is the leading cause of cancer mortality among women worldwide. The life-threatening infection caused by HPV demands the need for designing anticancerous drugs. In the recent years, different compounds from natural origins, such as carrageenan, curcumin, epigallocatechin gallate, indole-3-carbinol, jaceosidin, and withaferin, have been used as a hopeful source of anticancer therapy. These compounds have been shown to suppress HPV infection by different researchers. In the present study, we explored these natural inhibitors against E6 oncoprotein of high-risk HPV-16, which is known to inactivate the p53 tumor suppressor protein. A robust homology model of HPV-16 E6 was built to anticipate the interaction mechanism of E6 oncoprotein with natural inhibitory molecules using a structure-based drug designing approach. Docking analysis showed the interaction of these natural compounds with the p53-binding site of E6 protein residues 113-122 (CQKPLCPEEK) and helped the restoration of p53 functioning. Docking analysis, besides helping in silico validation of natural compounds, also helps understand molecular mechanisms of protein-ligand interactions.

Anti-oxidant Effect of Agastache rugosa on Oxidative Damage Induced by $H_2O_2$ in NIH 3T3 Cell

  • Hong, Se-Chul;Jeong, Jin-Boo;Park, Gwang-Hun;Kim, Jeong-Sook;Seo, Eul-Won;Jeong, Hyung-Jin
    • Korean Journal of Plant Resources
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    • v.22 no.6
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    • pp.498-505
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    • 2009
  • The plant Agastache rugosa Kuntze has various physiological and pharmacological activities. Especially, it has been regarded as a valuable source for the treatment of anti-inflammatory and oxidative stress-induced disorders. However, little has been known about the functional role of it on oxidative damage in mammalian cells by ROS. In this study, we investigated the DPPH radical, hydroxyl radical, hydrogen peroxide and intracellular ROS scavenging capacity, and $Fe^{2+}$ chelating activity of the extracts from Agastache rugosa. In addition, we evaluated whether the extract can be capable of reducing $H_2O_2$-induced DNA and cell damage in NIH 3T3 cells. These extracts showed a dose-dependent free radical scavenging capacity and a protective effect on DNA damage and the lipid peroxidation causing the cell damage by $H_2O_2$. Therefore, these results suggest that Agastache rugosa is useful as a herbal medicine for the chemoprevention against oxidative carcinogenesis.

In Silico Docking to Explicate Interface between Plant-Originated Inhibitors and E6 Oncogenic Protein of Highly Threatening Human Papillomavirus 18

  • Kumar, Satish;Jena, Lingaraja;Sahoo, Maheswata;Kakde, Mrunmayi;Daf, Sangeeta;Varma, Ashok K.
    • Genomics & Informatics
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    • v.13 no.2
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    • pp.60-67
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    • 2015
  • The leading cause of cancer mortality globally amongst the women is due to human papillomavirus (HPV) infection. There is need to explore anti-cancerous drugs against this life-threatening infection. Traditionally, different natural compounds such as withaferin A, artemisinin, ursolic acid, ferulic acid, (-)-epigallocatechin-3-gallate, berberin, resveratrol, jaceosidin, curcumin, gingerol, indol-3-carbinol, and silymarin have been used as hopeful source of cancer treatment. These natural inhibitors have been shown to block HPV infection by different researchers. In the present study, we explored these natural compounds against E6 oncoprotein of high risk HPV18, which is known to inactivate tumor suppressor p53 protein. E6, a high throughput protein model of HPV18, was predicted to anticipate the interaction mechanism of E6 oncoprotein with these natural inhibitors using structure-based drug designing approach. Docking analysis showed the interaction of these natural inhibitors with p53 binding site of E6 protein residues 108-117 (CQKPLNPAEK) and help reinstatement of normal p53 functioning. Further, docking analysis besides helping in silico validations of natural compounds also helped elucidating the molecular mechanism of inhibition of HPV oncoproteins.

A Study on the Characteristics of Heat Source Temperature for Two-Well Geothermal System Using Numerical Simulation (수치 시뮬레이션을 이용한 복수정(Two-Well) 개방형 지열 시스템의 열원수 온도 변화 검토)

  • Cho, JeongHeum;Nam, YuJin
    • Korean Journal of Air-Conditioning and Refrigeration Engineering
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    • v.27 no.4
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    • pp.207-212
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    • 2015
  • The use of groundwater and ground_heat is one of the ways to use natural and renewable energy, and it has been considered as a technology to reduce greenhouse gas emissions and increase energy-saving. There are a few researches on the optimum design for the open-loop geothermal system. In this study, to develop the optimal design method numerical simulation of the open-loop geothermal system with two-wells was performed by a groundwater and heat transfer model. In this paper, a study was performed to analyze the system performance according to well distance and pumping flow rate. In the result, average heat exchange rate and heat source temperature were calculated and it was found that they were dependent on the pumping rate.

A study on determining the optimum mixing ratio of carbon source for anaerobic treatment (혐기성처리를 위한 탄소원의 최적 혼합비율 결정에 관한 연구)

  • 김은호;장성호
    • Journal of environmental and Sanitary engineering
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    • v.14 no.3
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    • pp.31-38
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    • 1999
  • The purpose of this study were to determine the optimum mixing ratio of sewage sludge and papermill sludge as carbon source required to SRB in treating abandoned mine drainage with natural purification wetland. If mixing sewage sludge/papermill sludge 2.0 SO42- reduced 46.2%, and then 30% in mixing ratio 0.5.Because sewage sludge was faster biodegradability than papermill sludge, effluent SCOD was 40mg/L in mixing ratio 0.5, and after that was all but regular. pH and ORP were almost neutral and -160mV, but after that was all but regular and it indicated that SRB activity was suitable. Fe removal rate was 60% in mixing ratio 2.0, and 54% in mixing ratio 0.5. In point of carbon source supply, It indicated that mixing ration 0.5 was considered as the most appropriate, because degradability of swewage sludge under short time was higher than that of papermill sludge.

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Radiation Activity of Safety-Related Fission Products of DUPIC Fuel

  • Ryu, Ho-Jin;Park, Chang-Je;Park, Hangbok;Song, Kee-Chan
    • Proceedings of the Korean Radioactive Waste Society Conference
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    • 2004.06a
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    • pp.397-398
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    • 2004
  • It is important to estimate the radiation activity of the nuclear fuel which is a source term of the loss of coolant accident. The purpose of this study is to identify the most important parameters of the source term calculation based on three fuel types: typical natural uranium CANDU fuel, slightly enriched uranium and DUPIC fuel. The characteristics of the radiation source term were analyzed through sensitivity calculations of the linear power, fuel turnup, and the power shape.(omitted)

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High Efficiency DC-DC Converter for Fuel Cell System (연료전지 계통 연계형 고효율 DC-DC 컨버터)

  • Oh, Eun-Tae;Yoon, Soo-Young;Lee, Yoon-Jae;You, Gwang-Min;Chae, Hyung-Jun;Han, Byung-Moon;Lee, Jun-Young
    • The Transactions of The Korean Institute of Electrical Engineers
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    • v.58 no.12
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    • pp.2410-2415
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    • 2009
  • Studying for environmental friendly and efficient energy source is now actively under way on because problems like environmental pollution and exhaust of natural resources are in issue. Fuel Cell which is an alternative energy source has low voltage and high current characteristic, therefore boost up voltage converter and DC-AC converter is required to use as a common power source. In this paper, DC-DC converter which has high efficient and high power density is proposed and verified by experimental result.