114 research outputs found

    Tunnel Structure Analysis by the Operational Method First Report

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    Article信州大学工学部紀要 25: 13-20 (1968)departmental bulletin pape

    Finite Element Arch Analysis by the Operational Method

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    Article信州大学工学部紀要 25: 1-12 (1968)departmental bulletin pape

    Operational Finite Element Analysis of Circular Rings Surrounded with Elastic Foundation

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    Article信州大学工学部紀要 27: 37-46 (1969)departmental bulletin pape

    Direct Analysis of Continuous Beam-Columns

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    Article信州大学工学部紀要 23: 1-14 (1967)departmental bulletin pape

    SYNTHESIS, CHARACTERIZATION, AND IN VITRO ANTIMALARIAL ACTIVITY OF DIHYDROXYLATION DERIVATIVES OF TRICLOSAN

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    Objective: The emergence of malaria as a global health problem over the past few decades, accompanied by the rise of chemoresistant strains ofPlasmodium falciparum, has emphasized the need for the discovery of new therapeutic drugs against this disease. In this study, enantiomericallyenriched (enantioenriched) analogs of triclosan were synthesized and evaluated for antimalarial activity against P. falciparum cultures.Methods: Enantioselective dihydroxylation of the olefin in amide seven was performed efficiently using chiral quinine ligand (DHQ)2PHAL to yieldenantioenriched dihydroxy propionamide derivative (+)-1 in moderate yields. In a similar way, the chiral quinidine ligand (DHQD)2PHAL was used asstereoselectivity agent yielded the desired enantioenriched (−)-1. The enantioenriched products were used for further in vitro assay, and accordingly thepercent enantiomeric excess (% ee) was not determined. The structures of compounds were proven by spectral data (1H NMR, 13C NMR, and mass spectra).Results: The phenol moiety at the C1 position of triclosan was chemically substituted with a methoxy group, in conjunction with an introducedstereocenter in a 2,3-dihydroxy-propionamide group at C2’ position. Unmodified triclosan inhibited the P. falciparum cultures with an IC50 value of27.2 μM. By contrast, the triclosan analogs, compounds (+)-1 and (−)-1, inhibited the P. falciparum cultures with IC50 values of 0.034 and 0.028 μM,respectively.Conclusion: Collectively, our preliminary in vitro results suggest that these triclosan analogs have potent antimalarial activity and represent apromising new treatment strategy on further development

    Operational Method for Various Continuous Beams

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    Article信州大学工学部紀要 24: 1-22 (1968)departmental bulletin pape

    DESIGN, SYNTHESIS, AND CYTOTOXICITY EVALUATION OF NOVEL OPEN-CHAIN ANALOGUES OF ANTIMYCIN A 3 AS POTENTIAL ANTI-COLORECTAL CANCER AGENTS

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    Objective: Colorectal cancer is the third most common diagnosed cancer in the world. The aim of this work was to design, to synthesize, and toevaluate the novel open-chain analogues of antimycin A3 as highly potent anti-colorectal cancer agents.Methods: Our analogue synthesis was designed by modifying the nine-membered dilactone moiety of antimycin A with a simple open-chainmoiety, as well as introducing the stereocenter, and the hydroxyl groups on the side chain of the ester group. The synthesis was conducted through asequence of reactions from Boc-L-threonine by esterification, amidation, and sharpless asymmetric dihydroxylation. After completion the synthesis,cytotoxicities of the analogues were evaluated as inhibitors of colorectal HCT-116 cells by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide cell proliferation assay.Results: Novel open-chain analogues of antimycin A were successfully synthesized in a good yield. The analogues exhibited a greater anticanceractivity against colorectal HCT-116 cells than the original antimycin A3 with 50% inhibitory concentrations ranging of 35.0-47.0 µM. The resultsindicated that the presence of stereocenter and a hydroxylated open-chain moiety in the analogues were successfully improved its anti-colorectalcancer activity.3Conclusion: Our results clearly demonstrate that the opened-chain analogues of antimycin A as a promising candidates of new anti-colorectal canceragents.Keywords: Design, Synthesis, Open-chain, Analogue, Antimycin A, Anti-colorectal cancer.3

    DESIGN AND SCREENING OF GALLIC ACID DERIVATIVES AS INHIBITORS OF MALARIAL DIHYDROFOLATE REDUCTASE (DHFR) BY IN SILICO DOCKING

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    Objective: Malaria is an infection disease caused by plasmodium parasite with high prevalence in tropic and subtropic countries. The aim of this work was to design and screening of  gallic acid derivatives as inhibitors of malarial dihydrofolate reductase (DHFR) by in silico docking.Methods: The derivatives were designed by expanding the carboxyl group of gallic acid with open-chain moiety of L-threonine-allyl esters, as well as to modify the hydroxy groups on the aromatic ring of gallic acid with methoxyl group in the derivatives.  In silico approach has been utilized in finding the potential antimalaria of gallic acid derivatives. Fourteen Gallic acid derivatives (compound 2-15) were modeled into 3D structures by  ACD Labs software. Geometry optimization and minimization of energy 3D structure of gallic acid derivatives as ligands using the MOE software.  Docking process and amino acid analysis were executed by using MOE software. Results: In silico docking study resulted in the three top-ranked compounds, namely compound 5, 8 and 12. Among those three top-ranked compounds, compound 12 (octyl gallate), exhibited the strongest interaction and greatest inhibitory activity against the receptor of malarial DHFR.Conclusion Our results clearly demonstrated that compound 12 (octyl gallate) could be developed as a promising candidate for  the new anti-malarial agent.  Â

    Synthesis of Novel Temperature-responsive Polymer Gel of Poly(aspartic acid)s

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    Recently, thermo-responsive polymer gels have been studied in various research fields such as drug delivery system. One of represetative thermo-responsive polymer gels is poly(N-isopropylacrylamide) gel (PNIPAAm) that has a rapid and reversible volume phase transition. However, PNIPAAm is not biodegradable, resulting in limitation of its use in medical fields. Novel thermo-responsive polymer gel was prepared by closslinking of isopropylamine modified poly(succinimide) (IPA-PSI) (Poly[α,β -(DL-aspartate isopropyl amide)-co-(succinimide)]) with hexamethylenediamine. Because of peptide bonds in backbone, therefore, it is expected to possess biodegradability and biocompatibility. These gels changed their volume in response to change of environment such as temperature, pH and concentration of salt in water. Crosslinkage density and substitution degree of IPA-PSI affected volume phase transition bahavior of the gel

    イニュウシュオナジショウジョウバエ ノ トットリケン カラ ノ カクニン フロク:トットリケンサン ショウジョウバエ

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    外来種オナジショウジョウバエの鳥取県における生息を確認するため、2008年9月に鳥取市湖山の鳥取大構内の4カ所と鳥取市桂見の1カ所に合計9個のトラップを設置し、16種2,030個体のショウジョウバエを採集した。オナジショウジョウバエは設置したすべてのトラップから合計155個体採集され、鳥取県における定着が確認された。鳥取県における過去のショウジョウバエ調査と島根県からの最初のオナジショウジョウバエの記録から、本種の鳥取県への侵入時期は1990年前後と推定される。採集された種のうち、Drosophila kuntzei カクレポシショウウジョウバエとDrosophila annulipes ダンダラショウジョウバエも鳥取県新記録である。文献調査と今回のデータに基づき、鳥取県のショウジョウバエとして56種の記録を末尾に掲げる。 To confirm occurrence of Drosophila simulans, an exotic species of Drosophilidae (Diptera) in Japan, we collected drosophilid flies using nine bait (banana mixed with yeasts) traps in the campus of Tottori University and Katsurami, Tottori City in September 2008. We found a total of 155 adults of Drosophila simulans from all the traps among 2,030 flies of a total of 16 drosophilid species, and it confirmed settlement of the species in Tottori Prefecture. It is estimated that the species invaded Tottori Prefecture around 1990, since no flies of this species had been found in the faunal surveys of Drosophila conducted in the 1980s in Tottori City and the species was discovered in 193 in Matsue City of Shimane Prefecture, which is adjacent to Tottori Prefecture. Drosophila (Sophophora) kuntzei and D. (S.) annulipes were also new to fauna of Tottori Prefecture. On the basis of literature survey and the present data, a list of 56 drosophilid species of Tottori Prefecture is presented
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