• Title/Summary/Keyword: active compound

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A New Compound Isolation and Structure Analysis from Phellodendron Amurense Fruit Extract (황벽나무 열매 추출물로부터 신규 화합물의 분리 및 구조분석)

  • Kim, Young-Hee;Choi, Jung Eun;Hong, Jin-Young;Jo, Chang Wook;Lee, Jeung-Min;Kim, Soo Ji
    • Journal of the Korean Wood Science and Technology
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    • v.41 no.4
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    • pp.269-275
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    • 2013
  • Antifungal and insecticidal activity of Korean traditional medicinal plants was carried out to develop natural material for the development of organic cultural heritage conservation. As a result, Phellodendron amurense fruit was finally selected as a candidate of antifungal and insecticidal natural material. An novel active compound was purified from the ethylacetate fraction of Phellodendron amurense fruits using silica gel and Sephadex LH-20 column chromatography and PTLC. The compound was obtained as yellow oil form; UV ${\lambda}_{max}$(MeOH): 260 nm. The chemical structure of novel compound was determined as (4'-ethyl-2'-methylfuranyl)-6-methoxy-7-methylnona-2E,4E,6Z,8E-tetraenoic acid on the basis of various NMR experiments including $^1H$- and $^{13}C$-NMR, HMQC, HMBC and ESI-mass spectrum.

Etch Rate Dependence of Differently Doped Poly-Si Films on the Plasma Parameters (플라즈마 변수에 의한 불순물주입 다결정실리콘 박막의 식각율 변화)

  • Park, Sung-Ho;Kim, Youn-Tae;Kim, Jin-Sup;Kim, Bo-Woo;Ma, Dong-Sung
    • Journal of the Korean Institute of Telematics and Electronics
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    • v.25 no.11
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    • pp.1342-1349
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    • 1988
  • The dependence of the etch rates of differently doped poly-Si films on the gas composition, the chamber pressure and the RF power was investigated in detail. The highest anisotropy and the lowest CD loss were achieved at the $SF_6$-rich compositions, i.e., $Cl_2:SF_6$=17:33 (SCCM), in the $POCl_3$-doped poly-Si. The etch rates increased for n-type dopant (phosphorus), while decreased for p-type (boron) with increasing the doping levels irrespective of plasma parameters. And from the results of the activation of doped poly-Si films the active carrier concentrations as well as the doping concentrations were found to be responsible for the increase of the etch rate of the phosphorus-doped poly-Si.

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Design of a High Performance 32$\times$32-bit Multiplier Based on Novel Compound Mode Logic and Sign Select Booth Encoder (새로운 복합모드로직과 사인선택 Booth 인코더를 이용한 고성능 32$\times$32-bit 곱셈기의 설계)

  • Kim, Jin-Hwa;Song, Min-Gyu
    • Journal of the Institute of Electronics Engineers of Korea SD
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    • v.38 no.3
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    • pp.205-210
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    • 2001
  • In this paper, a novel compound mode logic based on the advantage of both CMOS logic and pass-transistor logic(PTL) is proposed. From the experimental results, the power-delay products of the compound mode logic is about 22% lower than that of the conventional CMOS logic, when we design a full adder. With the proposed logic, a high performance 32$\times$32-bit multiplier has been fabricated with 0.6um CMOS technology. It is composed of an improved sign select Booth encoder, an efficient data compressor based on the compound mode logic, and a 64-bit conditional sum adder with separated carry generation block. The Proposed 32$\times$32-bit multiplier is composed of 28,732 transistors with an active area of 1.59$\times$1.68 mm2 except for the testing circuits. From the measured results, the multiplication time of the 32$\times$32-bit multiplier is 9.8㎱ at a 3.3V power supply, and it consumes about 186㎽ at 100MHz.

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Isolation and Characterization of Constituent Compounds from Leaves and Stems of Chrysanthemum boreale Makino (산국 잎과 줄기의 유효성분 분리 및 특성 연구)

  • Park, Sook Jahr;Park, Moon Ki;Lee, Jong Rok
    • Journal of Environmental Science International
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    • v.28 no.11
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    • pp.993-1004
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    • 2019
  • Chrysanthemum boreale Makino (C. boreale) is widely distributed in Asian countries, and has traditionally been used to treat various inflammatory diseases including bronchitis. In this study, we aimed to isolate biologically active compounds from leaves and stems of C. boreale. Chemical components were purified by column chromatograpy and recyclic HPLC, and characterized from their spectral data (IR, MS, NMR). Biological activity experiments were conducted for Farnesyl-protein transferase (FPTase) activity, apoptosis and nitirc oxide (NO) release. As a results, three sesquiterpene lactones were isolated. Compound 1 (4-methoxy-8-O-acetyl-10-hydroxy-2,11(13)-guaiadiene-12,6-olide) showed strong cytotoxic activities having an average growth inhibition of 50% ($GI_{50}$) value of $1.89{\mu}g/m{\ell}$ against human colon adenocarcinoma cells. Compound 1 also showed a low half maximal inhibitory concentration ($IC_{50}$) value of $10{\mu}g/m{\ell}$ for NO release. In the caspase 3 activity, compound 1 and compound 2 (8-O-(2-carbonyl-2-butyl)-3,10-dihydroxy-4,11(13) -guaiadiene-12,6-olide) exhibited 94% and 90% apoptosis inhibition activity, respectively. Compound 3 (4,8-O-diacetyl -10-hydroxy-2(3),11(13)-guaiadiene-12,6-olide) showed a strong inhibitory effect on FPTase activity with 90% inhibitory activity at a concentration of $100{\mu}g/m{\ell}$. These results clearly show the presence of lactone compounds in the leaves and stems, which may partially contribute to the pharmacological activity of C. boreale.

Discovery of Chitin Deacetylase Inhibitors through Structure-Based Virtual Screening and Biological Assays

  • Liu, Yaodong;Ahmed, Sibtain;Fang, Yaowei;Chen, Meng;An, Jia;Yang, Guang;Hou, Xiaoyue;Lu, Jing;Ye, Qinwen;Zhu, Rongjun;Liu, Qitong;Liu, Shu
    • Journal of Microbiology and Biotechnology
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    • v.32 no.4
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    • pp.504-513
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    • 2022
  • Chitin deacetylase (CDA) inhibitors were developed as novel antifungal agents because CDA participates in critical fungal physiological and metabolic processes and increases virulence in soil-borne fungal pathogens. However, few CDA inhibitors have been reported. In this study, 150 candidate CDA inhibitors were selected from the commercial Chemdiv compound library through structure-based virtual screening. The top-ranked 25 compounds were further evaluated for biological activity. The compound J075-4187 had an IC50 of 4.24 ± 0.16 µM for AnCDA. Molecular docking calculations predicted that compound J075-4187 binds to the amino acid residues, including active sites (H101, D48). Furthermore, compound J075-4187 inhibited food spoilage fungi and plant pathogenic fungi, with minimum inhibitory concentration (MIC) at 260 ㎍/ml and minimum fungicidal concentration (MFC) at 520 ㎍/ml. Therefore, compound J075-4187 is a good candidate for use in developing antifungal agents for fungi control.

Molecular docking of bioactive compounds derived from Moringa oleifera with p53 protein in the apoptosis pathway of oral squamous cell carcinoma

  • Rath, Sonali;Jagadeb, Manaswini;Bhuyan, Ruchi
    • Genomics & Informatics
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    • v.19 no.4
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    • pp.46.1-46.11
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    • 2021
  • Moringa oleifera is nowadays raising as the most preferred medicinal plant, as every part of the moringa plant has potential bioactive compounds which can be used as herbal medicines. Some bioactive compounds of M. oleifera possess potential anti-cancer properties which interact with the apoptosis protein p53 in cancer cell lines of oral squamous cell carcinoma. This research work focuses on the interaction among the selected bioactive compounds derived from M. oleifera with targeted apoptosis protein p53 from the apoptosis pathway to check whether the bioactive compound will induce apoptosis after the mutation in p53. To check the toxicity and drug-likeness of the selected bioactive compound derived from M. oleifera based on Lipinski's Rule of Five. Detailed analysis of the 3D structure of apoptosis protein p53. To analyze protein's active site by CASTp 3.0 server. Molecular docking and binding affinity were analyzed between protein p53 with selected bioactive compounds in order to find the most potential inhibitor against the target. This study shows the docking between the potential bioactive compounds with targeted apoptosis protein p53. Quercetin was the most potential bioactive compound whereas kaempferol shows poor affinity towards the targeted p53 protein in the apoptosis pathway. Thus, the objective of this research can provide an insight prediction towards M. oleifera derived bioactive compounds and target apoptosis protein p53 in the structural analysis for compound isolation and in-vivo experiments on the cancer cell line.

Structural Analysis and Biological Activities of Sesquiterpene Lactones Isolated from the Leaves and Stems of Chrysanthemum boreale Makino (산국의 잎과 줄기에서 분리한 Sesquiterpene Lactone들의 구조규명 및 생리활성)

  • Lee, Jong Rok;Park, Moon Ki
    • Journal of Environmental Science International
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    • v.26 no.11
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    • pp.1285-1295
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    • 2017
  • Chrysanthemum boreale Makino is widely distributed in Korea, China, Japan and Southeast Asian countries. C. boreale is one of the herbs used for treating various inflammatory diseases in oriental medicine. The present study was conducted to identify biologically active compounds from the leaves and stems of C. boreale. We isolated two sesquiterpene sactones from the leaves and stems of C. boreale using silica gel column chromatography and recyclic high perfomance liquid chromatography. The lactones were characterized by their spectroscopic data (NMR, IR, MASS). These compounds were subjected to Farnesyl Protein Transferase (FPTase) inhibition, Nitric Oxide (NO) release inhibition and apoptosis inhibition. The structur of the following isolated compound were elucidated 8,10-${\small{O}$-Acetyl-2-methoxy-10-hydroxy-3,11(13)-guaiadiene-12,6-olide and 4,10-dihydroxy-8-${\small{O}$-Acetyl-2,11(13)-guaiadiene-12,6-olide. In the NO release inhibition assay, compound 2 showed strong activities, with an $IC_{50}$ value of $7{\mu}g/mL$, whereas compound 1 did not exhibit significant activity with an $IC_{50}$ value of over $14{\mu}g/mL$ against murine macrophage.

Inhibition of CDK4 activity by 7-chloro-4-nitro-benzo[1,2,5]oxadiazole 1-oxide (7-Chloro-4-nitro-benzo[1,2,5]oxadliazole 1-oxide의 CDK4 활성저해)

  • Jeon Yong-Jin;Ko Jong Hee;Yeon Seung Woo;Kim Tae-Yong
    • YAKHAK HOEJI
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    • v.50 no.1
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    • pp.52-57
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    • 2006
  • The activation of cyclin dependent kinase 4 (CDK4) is found in more than half of all human cancers. Therefore CDK4 is an attractive target for the development of a novel anticancer agent. For mass screening of CDK4 inhibitor, we set up in vitro kinase assay for CDK4 activity using a cyclin D1-CDK4 fusion protein, which is constitutively active and exhibits enhanced stability. From the screening of representative compound library of Korea Chemical Bank, we found that 7-chloro-4-nitro-benzo[1,2,5]oxadiazole 1-oxide (FBP-1248) selectively inhibited CDK4 activity in vitro by ATP competitive manner. This compound prevented the phosphorylation of retinoblatsoma tumor suppressor protein, Rb, and inhibited cell growth through cell cycle arrest. In summary, we developed an efficient assay system for CDK4 activity in vitro and identified the CDK4 inhibitory compound, FBP-1248.

Polyacetylene Compound from Cirsium japonicum var. ussuriense Inhibited Caspase-1-mediated IL-$1{\beta}$ Expression

  • Shim, Hong;Moon, Jung Sun;Lee, Sookyeon;Yim, Dongsool;Kang, Tae Jin
    • IMMUNE NETWORK
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    • v.12 no.5
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    • pp.213-216
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    • 2012
  • Our previous report showed that polyacetylene compound, 1-Heptadecene-11, 13-diyne-8, 9, 10-triol (PA) from the root of Cirsium japonicum var. ussuriense has anti-inflammatory activity. In this study we investigated the role of the PA as inhibitor of caspase-1, which converts prointerleukin-$1{\beta}$ (proIL-$1{\beta}$) to active IL-$1{\beta}$ and is activated by inflammasome involved in the inflammatory process. We tested the effect of PA on the production of pro-inflammatory cytokines, IL-$1{\beta}$ in murine macrophage cell line, RAW264.7. PA inhibited lipopolysaccharide (LPS)-induced IL-$1{\beta}$ production by macrophages at a dose dependent manner. PA also suppressed the activation of caspase-1. The mRNA level of ASC (apoptosis-associated spec-like protein containing a CARD), an important adaptor protein of inflammasome, was decreased in the PA treated group. Therefore our results suggest that the anti-inflammatory effect of PA is due to inhibit the caspase-1 activation.

Isolation of epi-Oleanolic Acid from Korean Mistletoe and Its Apoptosis-Inducing Activity in Tumor Cells

  • Jung, Myung-Ju;Yoo, Yung-Choon;Lee, Kyung-Bok;Kim, Jong-Bae;Song, Kyung-Sik
    • Archives of Pharmacal Research
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    • v.27 no.8
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    • pp.840-844
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    • 2004
  • A triterpene was isolated as a cytotoxic principle from the dichloromethane extract of Korean mistletoe (KM; Viscum album colora turn) by repeated silica gel chromatography and recrystalli-zation. In in vitro analysis of cytotoxic activity using various human and murine tumor cell lines, the dichloromethane extract of KM was highly cytotoxic against these cells. We isolated the most active compound, referred to VD-3, from the dichloromethane extract of KM. The VD-3 was shown to be less cytotoxic to normal cells (murine splenocytes). From the identification of the chemical structure of VD-3 by spectral data and chemical synthesis, the compound was proven to be epi-oleanolic acid. Tumor cells treated with VD-3 showed a typical pattern of apo-ptotic cell death, such as apparent morphological changes and DNA fragmentation. These results indicate that epi-oleanolic acid is an important compound responsible for antitumor activity of KM.