• Title/Summary/Keyword: Drug Discovery

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A New Triterpenoid Saponin from Pulsatilla cernua

  • Fan, Wenhao;Liu, Jianyu;Gong, Yixia;Ma, Jing;Zhou, Nan;Xu, Yongnan
    • Natural Product Sciences
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    • v.19 no.2
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    • pp.150-154
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    • 2013
  • A new oleanane-type triterpenoid saponin together with six known saponins were isolated from the roots of Pulsatilla cernua. Their structures were elucidated on the basis of spectroscopic data, including 2D NMR spectra and chemical evidence. Compounds 1 and 6 are reported from this genus for the first time.

Genetically Engineered Mouse Models for Drug Development and Preclinical Trials

  • Lee, Ho
    • Biomolecules & Therapeutics
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    • v.22 no.4
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    • pp.267-274
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    • 2014
  • Drug development and preclinical trials are challenging processes and more than 80% to 90% of drug candidates fail to gain approval from the United States Food and Drug Administration. Predictive and efficient tools are required to discover high quality targets and increase the probability of success in the process of new drug development. One such solution to the challenges faced in the development of new drugs and combination therapies is the use of low-cost and experimentally manageable in vivo animal models. Since the 1980's, scientists have been able to genetically modify the mouse genome by removing or replacing a specific gene, which has improved the identification and validation of target genes of interest. Now genetically engineered mouse models (GEMMs) are widely used and have proved to be a powerful tool in drug discovery processes. This review particularly covers recent fascinating technologies for drug discovery and preclinical trials, targeted transgenesis and RNAi mouse, including application and combination of inducible system. Improvements in technologies and the development of new GEMMs are expected to guide future applications of these models to drug discovery and preclinical trials.

Intercellular Lipid Mediators and GPCR Drug Discovery

  • Im, Dong-Soon
    • Biomolecules & Therapeutics
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    • v.21 no.6
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    • pp.411-422
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    • 2013
  • G-protein-coupled receptors (GPCR) are the largest superfamily of receptors responsible for signaling between cells and tissues, and because they play important physiological roles in homeostasis, they are major drug targets. New technologies have been developed for the identification of new ligands, new GPCR functions, and for drug discovery purposes. In particular, intercellular lipid mediators, such as, lysophosphatidic acid and sphingosine 1-phosphate have attracted much attention for drug discovery and this has resulted in the development of fingolimod (FTY-720) and AM095. The discovery of new intercellular lipid mediators and their GPCRs are discussed from the perspective of drug development. Lipid GPCRs for lysophospholipids, including lysophosphatidylserine, lysophosphatidylinositol, lysophosphatidylcholine, free fatty acids, fatty acid derivatives, and other lipid mediators are reviewed.

Minor Phenolic Constituents of the Anemarrhenae Rhizoma

  • Youn, Ui-Joung;Lee, Ye-Seul;Jeong, Ha-Na;Nam, Joo-Won;Lee, Yoo-Jin;Son, Young-Min;Hwang, Eun-Sook;Seo, Eun-Kyoung
    • Natural Product Sciences
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    • v.15 no.4
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    • pp.203-207
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    • 2009
  • A homoisoflavanone, 7,4'-dihydroxyhomoisoflavanone (1) and a flavanone, (2S)-7,4'-dihydroxy-5-methoxyflavanone (2), were isolated from the rhizomes of Anemarrhena asphodeloides, together with 4,4'-dihydroxychalcon (3), 2'-O-methylphlorethin (4), 1,3-bis-di-p-hydroxyphenyl-4-penten-1-one (5), and 2,4'-dihydroxy-4-methoxybenzophenone (6) on the basis of spectroscopic and physicochemical analyses including 1Dand 2D- NMR techniques as well as by comparison of their data with the published values. Compounds 1 - 4 were isolated for the first time from this plant source. Among isolates, compound 2 exhibited moderate inhibitory effect on the differentiation of pre-adipocyte 3T3-L1 cells.

A Synthesis of New Fluorine-containing Phenylformamidines and Their Insecticidal Activities (새로운 불소함유 Phenylformamidine 유도체의 합성과 살충활성)

  • Lee, Dong-Guk;Chung, Kun-Hoe;Ko, Young-Kwan;Ryu, Jae-Wook;Woo, Jae-Chun;Koo, Dong-Wan;Choi, Yong-Ho;Park, No-Joong;Hong, Mi-Sook;Kim, Tae-Joon
    • The Korean Journal of Pesticide Science
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    • v.12 no.3
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    • pp.295-301
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    • 2008
  • Phenylformamidines are well known as insecticides for their specific activity against the insects. It has now been established that they show insecticidal activity as agonists on the octopamine receptor which is located in the synapse membrane. In this study we tried to test the effect of fluorine substituted aromatic formamidines and 1,3,5-triazapenta-1,4-dienes. Among the compounds, 2h, 2k, 21, 3g, 3h, 3k showed good activity against mite and aphid and 4f and 4g showed high activity against mite.