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영남대학교 약품개발연구소> 약품개발연구소 연구업적집> A new 9,11-secisterik with a 1,4-quinone from a Korean marine sponge Ircinia sp.

A new 9,11-secisterik with a 1,4-quinone from a Korean marine sponge Ircinia sp.

Inho Yang , Hyukjae Choi , Sang Jip Nam , Heonjoong Kang
  • : 영남대학교 약품개발연구소
  • : 약품개발연구소 연구업적집 26권0호
  • : 연속간행물
  • : 2016년 09월
  • : 2-2(1pages)

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An intensive investigation of chemical com-ponents for Ircinia sp. Ied to the isolation of a new 9,11-secosterol. The chemical structure of this compound was elucidated based on the interpretation of NMP and MS spectrosopic data. The isolated compound exhibited an-tibacterial activities against Staphylococcus epidermidis and Bacillus subtilis with MIC values of 6.3 and 25 μg Mi-1, respectively.

UCI(KEPA)

I410-ECN-0102-2017-510-000515786

간행물정보

  • : 의약학분야  > 약품제제
  • :
  • :
  • : 연간
  • : 1225-2816
  • :
  • : 학술지
  • : 연속간행물
  • : 1991-2016
  • : 1478


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15-Hydroxy-7-azaindolin-2-one, a novel hybrid of pyridinol and sunitinib: design, synthesis and cytotoxicity against cancer cells

저자 : Sajita Shah , Chaemin Lee , Hyukjae Choi , Jaya Gautam , Hyeonjin Jang , Geum Jin Kim , Yu Jeong Lee , Chhabi Lal Chaudhary , Sang Won Park , Tae Gyu Nam , Jung Ae Kim , Byeong Seon Jeong

발행기관 : 영남대학교 약품개발연구소 간행물 : 약품개발연구소 연구업적집 26권 0호 발행 연도 : 2016 페이지 : pp. 1-1 (1 pages)

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Angiogenesis plays important roles in tumor growth and metastasis. Sunitinib (sutent®) is an antitumor agent targeting receptor tyrosme kmases which are Involved in angiogenesis as well as cancer cell growth and survival. Using the pyridin-3-01 scaffold. which was previously reported as an excellent antioxidant and antiangiogenic platform, we have synthesized sunitinb mimics 6 by hybridizing bicyclic pyridlnol4 as a key scaffold and pyrrole-2-carbaidehydes 7 as side chains, Cytotoxicity assays showed that compounds: 6 have comparable to better anticancer activity than sunltll1lb against five different cancer cell lines. In addition. compounds 6 showed even lower levels of cytotoxicity against normal cells. resulting in up to 26-fold better safety Windows, than sunitinib, Signaling pathway-associated transcription factor reporter assay and western blot analyses revealed that apoptosis induction In MDA-MB-231 human breast cancer cells by 6F is mall1ly mediated through the pS3 increase and down-regulation of phospho-signal transdu-cer and activator of transcription 3 (STAT3) and its target gene products, cyclin D, Bcl-2. and survivin. The data strongly suggest that our hybrid compounds can provide a novel anticancer scaffold with Improved and safer cytotoxicity profiles than sunitinib.

2A new 9,11-secisterik with a 1,4-quinone from a Korean marine sponge Ircinia sp.

저자 : Inho Yang , Hyukjae Choi , Sang Jip Nam , Heonjoong Kang

발행기관 : 영남대학교 약품개발연구소 간행물 : 약품개발연구소 연구업적집 26권 0호 발행 연도 : 2016 페이지 : pp. 2-2 (1 pages)

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An intensive investigation of chemical com-ponents for Ircinia sp. Ied to the isolation of a new 9,11-secosterol. The chemical structure of this compound was elucidated based on the interpretation of NMP and MS spectrosopic data. The isolated compound exhibited an-tibacterial activities against Staphylococcus epidermidis and Bacillus subtilis with MIC values of 6.3 and 25 μg Mi-1, respectively.

3A new series of 2-phenol-4-aryl-6-chlorophenyl pyridine derivatives as dual topoisomerase I/II inhibitors: Synthesis, biological evalution and 3D-QSAR study

저자 : Radha Karki , Kyu Yeon Jun , Tara Man Kadayat , Somin Shin , Til Bahadur Thapa Magar , Ganesh Bist , Aarajana Shrestha , Younghwa Na , Youngjoo Kwon , Eung Seok Lee

발행기관 : 영남대학교 약품개발연구소 간행물 : 약품개발연구소 연구업적집 26권 0호 발행 연도 : 2016 페이지 : pp. 3-3 (1 pages)

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As a continuous effort to develop novel antitumor agents, a new series of forty-five-2phenol-4-aryl-6-chlorophenyl pyridine compounds were synthesized and evaluated for cytotoxicity against four different human cancer cell lines(DU145, HCT15, T47D, and HeLa), and topoisomerase I and II inhibitory activity, Several compounds(10-15, 20, 22, 24, 28, 42, and 49) displayed strong to moderate dual topoisomerase I and II inhibitory activity at 100 μM. It was observed that hydroxyl and chlorine moiety at meta or para position of phenyl ring is favorable for dual topoisomerase inhibitory activity and cytotoxicity. Most of the compounds displayed stronger cytotoxicities than those of all positive controls against the HCT15 and T47D cell lines. For investigation of the structure-activity relationships, a 3D-QSAR analysis using the method of comparative molecular field analysis (CoMFA) was performed. The generated 3D contour maps can be used for further rational design of novel terpyridine derivatives as highly selective and potent cytotoxic agents.

4Anti-Inflammatory Activity of a Novel Acetylene Isolated from the Roots of Angelica tenuissima NAKAI

저자 : Hyun Gyu Choi , Hyunkjae Choi , Jeong Hyung Lee , Byung Sun Min , Jeong Ah Kim

발행기관 : 영남대학교 약품개발연구소 간행물 : 약품개발연구소 연구업적집 26권 0호 발행 연도 : 2016 페이지 : pp. 4-4 (1 pages)

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Three polyacetylenes, one novel and two known. were isolated from the root of Angelica tenuissima. U ing 1H- and13C_NMR, COSY. HMBC, and HMQC, their truciure were found to be (3R,8S)-heptadeca-1-en-4.6-diyne-3,8-diol (1), falcarindiol (2). and oplopandiol (3). Absolute configuration of compound 1 were established using Mosher`s esterification. In addition. the polyacetylenes (1 - 3) were evaluated for their anti-inflammatory activity. Compounds 1 and 3 showed potent inhibitory activity against lipopolysaccharide-induced nitric oxide (N0) production in RAW267.7 macrophage cell with IC50 value of 4.31 and 5.06 μM. respectively. Compound 1. strongly inhibited inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2 in a concentration-dependent manner.

5A Novel Bromoindole Alkaloid from a Korean Colonial Tunicate Didemnum sp.

저자 : Dongyup Hahn , Geum Jin Kim , Hyukjae Choi , Henjoong Kang

발행기관 : 영남대학교 약품개발연구소 간행물 : 약품개발연구소 연구업적집 26권 0호 발행 연도 : 2016 페이지 : pp. 5-5 (1 pages)

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Chemical investigation on a colonial marine tunicate, Didemnum sp. led to the isolation of a series of indole alkaloids including a new (1) and two known metabolites (2-3). Based on the spectroscopic analysis including 1D and 2D NMR along with MS spectra, the structure of 1 (16-epi-18-acetyl herdmanine D) was elucidated as a new amino acid derivative. The absolute configuration of 1 was determined by comparison of specific rotation with the known compound. The structures of compounds 2 and 3 were also identified as bromoindole containing compounds N-(6-bromo-IH-indole- 3-carbonyl)-L-arginine and (6-bromo-IH-indol- 3-yl) oxoacetamide, respectively, based on 1H and 13C NMR data, MS data and specific rotation value. Their pharmacological potentials as antibacterial agents and FXR antagonists were investigated, but no significant activity was found. However, the structural similarity of compound 1 to compound 4 suggested the anti-inflammatory potential of compound 1.

6Bioautography with TLC-MS/NMR for Rapid Discovery of Anti-tuberculosis Lead Compounds from Natural Sources

저자 : Edyta M. Grzelak , Changhwa Hwang , Geping Cai , Joo Won Nam , Mary P Choules , Wei Gao , David C Lankin , James B Mcalpine , Surafel G Mulugeta , Jose G Napolitano , Joo Won Suh , Seung Hwan Yang , Jinhua

발행기관 : 영남대학교 약품개발연구소 간행물 : 약품개발연구소 연구업적집 26권 0호 발행 연도 : 2016 페이지 : pp. 6-6 (1 pages)

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While natural products constitute an established source of lead compounds, the classical iterative bioassay-guided isolation process is both time- and labor-intensive and prone to failing to identify active minor constituents. (HP)TLC.bioautography.MS/NMR, which combines cutting-­edge microbiological, chromatographic, and spectrometric technologies, was developed 10 accelerate anti-tuberculosis (TB) drug discovery from natural sources by acquiring structural information at a very early stage of the isolation process, Using the avirulent, bioluminescent Mtb strain mc27000 luxABCDE, three variations of bioautography were evaluated and optimized for sensitivity in detecting anti-T``B agent , including established clinical agents and new lead with novel mechanisms of action. Several exemplary applications of this approach to microbial extracts demonstrate its potential as a routine method in anti-TB drug discovery from natural sources.

7Bromo-honaucin A inhibits osteoclastogenic differentiation in RAW 264.7 cells via Akt and ERK signaling pathways

저자 : Mahesh Sapkota , Liang Li , Hyukjae Choi , William H Gerwick , Yunjo Soh

발행기관 : 영남대학교 약품개발연구소 간행물 : 약품개발연구소 연구업적집 26권 0호 발행 연도 : 2016 페이지 : pp. 7-7 (1 pages)

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Osteoclasts are unique bone remodeling cells derived from multinucleated myeloid progenitor cells. They play homeostatic vital roles in skeletal modeling and remodeling but also destroy bone masses in many pathological conditions such as osteoporosis and rheumatoid arthritis. Receptor activation of NF-KB li-gand (RANKL) is essential osteclastogenesis. In this study, we investigated the effects of bromo-honaucin A (Br-H A) isolated from Leptolyngbya crossbyana (cyanobacterium). To investigate the me-chanism of the inhibitory effect of Br-H A on osteoclstogenesis. we employed Br-H Ain RANKL-treated murine monocyte/macrophage RAW 264.7 cells for osteoclastic differentiation in-vitro. The inhibitory effects on in-vitro osteoclastogenesis was evaluated by counting the number of Tartarate resistant acid phospatase (TRAP) positive multinucleated cells and by measuring the expression level of osteoclast-specific genes like matrix metalloproteinase 9 (MMP9). cathepsin K (CATH K), GRB2-associated-binding protein 2 (GAB2), c-terminal myc kinase (C-MYC). C-terminal Src kinase (C-SRC) and Microphthalmia-associated transcription factor (MITF). Moreover, Br-H A blocked the resorbing capacity of RAW 264.7 cells on calcium phosphate-coated plates. Finally, Br-H A clearly decreased the expression of Akt and also decreased the activation of ERK. Thus, the study identifies Br-H A as potent inhibitor potentialin the treatment of diseases involving abnormal bone lysis such as osteoporosis. rheumatoid arthritis, and periodontal bone degradation.

8Chondroprotective and anti-inflammatory effects of ChondroT, a new complex herbal medication

저자 : Jung Up Park , Seon Jong Kim , Chang Su Na , Chan Hun Choi , Chang Seob Seo , Jong Keon Son , Bok Yun Kang , Young Ran Kim

발행기관 : 영남대학교 약품개발연구소 간행물 : 약품개발연구소 연구업적집 26권 0호 발행 연도 : 2016 페이지 : pp. 8-8 (1 pages)

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Background: Ganghwaljetongyeum (GHJTY) is a complex herbal decoction comprising 18 plants; it is used to treat arthritis. In order to develop a new anti-arthritic herbal medication, we selected 5 out of 18 GHJTY plants by using bioinformatics analysis. The new medication, called ChondroT. comprised water extracts of Osterici Radix, Lonicerae Folium, Angelicae Gigantis Radix, Clematidis Radix, and Phellodendri Cortex. This study was designed to investigate its chondroprotective and anti-inflammatory effects to develop an anti-arthritic herb medicine. Methods: ChondroT was validated using a convenient and accurate high-performance liquid chromatography-photodiode array (HPLC-PDA) detection method for simultaneous determination of its seven reference components. The concentrations of the seven marker constituents were in the range of 0.81-5.46 mg/g. The chondroprotective effects were evaluated based on SW1353 chondrocytes and matrix metalloproteinase 1 (MMP1) expression. In addition, the anti-inflammatory effects of ChondroT were studied by Western blotting of pro-inflammatory enzymes and by enzyme-linked immunosorbent assay (ELISA) of inflammatory mediators in lipopolysaccharides (LPS)-induced RAW264.7 cells. Results: ChondroT enhanced the growth of SW1353 chondrocytes and also significantly inhibited IL-1 ~-induced MMP-1 expression. However, ChondroT did not show any effects on the growth of HeLa and RAW264.7 cells The expression of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) was induced by LPS in RAW264.7 cells, which was significantly decreased by pre-treatment with Chondro]. In addition, ChondroT reduced the activation of NF-kB and production of inflammatory mediators, such as IL-1~, IL-6, PGE2, and nitric oxide (NO) in LPS-induced RAW264.7 cells. Conclusions: These results show that ChondroT exerted a chondroprotective effect and demonstrated multi-target mechanisms related to infiammation and arthritis. In addition, the suppressive effect was greater than that exhibited by GHJTY, suggesting that Chondrof. a new complex herbal medication, has therapeutic potential for the treatment of arthritis.

9Considerations of the chemical biology of microbial natural products provide an effective drug discovery strategy

저자 : Hyukjae Choi , Dong Chan Oh

발행기관 : 영남대학교 약품개발연구소 간행물 : 약품개발연구소 연구업적집 26권 0호 발행 연도 : 2016 페이지 : pp. 9-9 (1 pages)

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Conventional approaches to natural product drug discovery rely mainly on random searches for bioactive compounds using bioassays. These traditional approaches do not incorporate a chemical biology per-spective. Searching for bioactive molecules using a chemical and biological rationale constitutes a powerful search paradigm. Here, the authors review recent examples of the discovery of bioactive natural products based on chemical and biological interactions between hosts and symbionts, and propose this method provides a more effective means of exploring natural chemical diversity and eventually of discovering new druge.

10Design and synthesis of conformationally constrained hydroxylated 4-phenyl-2-ary chromenopyridines as novel and selective topoisomerase II-targeted antiproliferative agents

저자 : Pritam Thapa , Kyu Yeon Jun , Tara Man Kadayat , Chanmi Park , Zhi Zheng , Til Bahadur Thapa Magar , Ganesh Bist , Aarajana Shrestha , Younghwa Na , Youngjoo Kwon , Eung Seok Lee

발행기관 : 영남대학교 약품개발연구소 간행물 : 약품개발연구소 연구업적집 26권 0호 발행 연도 : 2016 페이지 : pp. 10-10 (1 pages)

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To develop novel selective topoisomerase II inhibitors, we designed and synthesized a series of conforma-tionally constrained hydroxylated 4-phenyl-2-aryl chromenopyridines and evaluated their to poi so-merase inhibitory activity and cytotoxicity against three human cancer cell lines (DU145, HCn5, and T47D) and a normal cell line (MCF10A). All of the prepared compounds displayed stronger or similar topoisomerase II inhibitory activity as well as cytotoxicity against three human cancer cell lines com-pared to etoposide. Compounds 10., 109, 11., 11f, 11g, 12., 12f, and 12g especially showed stronger topoisornerase II inhibitory activity as compared to etoposide at both 100 μM and 20 μM. A structure-ac-tivity relationship study revealed that hydroxyphenyl moiety at 4-position of pyridine and ortho-hydrox-yphenyl or thienyl moiety at 2-position of pyridine has an important role in displaying selective topoisomerase II inhibition. The compound 12b with para-hydroxyphenyl and meta-hydroxyphenyl at 4- and 2-position of pyridine. respectively, showed the most significant cytotoxicity against all three can-cer cell lines, whereas less cytotoxicity to a normal cell line as compared to adriamycin.

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