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Preparation And Activitiy Studies Of Different Alginates And Their Series Derivaties

Posted on:2014-01-14Degree:MasterType:Thesis
Country:ChinaCandidate:X C SunFull Text:PDF
GTID:2254330401984484Subject:Medicinal chemistry
Abstract/Summary:PDF Full Text Request
In this paper, eight kinds of alginates were extracted by hot extraction andalkaline extraction from the three kinds of seaweeds: Durvillaea Antarctica, Lessonianigrescence, Lessonia trabeculata, and also, basic physical and chemical propertiesand structural analysis were carried out.. NMR showed that among the guluronic acidcontent of TCA1was over than90%, the mannuronic acid content of AWA1was morethan80%, and12kinds of alginates from degradation by acid drop and microwaveacid drop;20kinds of alginates with molecular weight from3-110kDa, M/G valuefrom the0.1-9were obtained; it has the highest mechanical strength, minimumshrinkage and a high G content of more than70%when the alginate porosities aswell as in the monovalention solution has a higher stability characteristics, TCA1(MW=80KDa; FG=91%) was used to produce a package microorganismsmicrospheres prepared microcapsule particle size0.5-5.0mm (particle size of themicrocapsules can be controlled), a larger size of the particle diameter of themicrocapsules had a greater advantage in terms of large-scale preparation andrecovery, and during the preparation of the capsules prepared in full physiologicalconditions, to ensure that the cells’activity.Five membered nitrogen containing heterocyclic compounds with a wide range ofphysiological activities, such as anti-viral, anti-bacterial, anti-inflammatory, andanti-tumor, often concerned in new drug research as a pharmacophore, the antiviraldrug ribavirin and antifungal fluconazole as azole compounds are successfully used inclinical nitrogen. In this paper,20kinds of prepared alginate triazole ring weremodified to40alginate triazole ring derivative eventually. Firstly, by using of EDCand NHS to prepare alginate-PEG-N3b, the amount of EDC in this reaction is animportant reason to affect the yield, when the mass ratio of EDC and alginate was 117/50, the degree of substitution was about11%, the optimal reaction conditions:room temperature,60min, pH=4-6.Then alginate-PEG-N3b with propiolate and3–Ethynylthiophene by clickingreaction to prepare the carboxymethyl triazolylazo-PEG-alginate c and3-thiophentriazolo-PEG-alginate d, compared with these two methods, which werethe conventional method and microwave synthesis method, for the first method, at70℃for12h, the production rate was100%, however, microwave synthesis onlyin the100W, under80°C reaction15min yield can reach100%, the efficiency getimproved greatly.In this paper, also, series of alginate derivatives c, d were conducted to theevaluation of the anti-aquatic Vibrio and the anti-viral activities. The results showedthat the carboxy group promoted the antiviral activity, the introduction of the triazolering can enhanced the activities, when3-thiophentriazolo-PEG-alginate d with whichpresented three nitrogen azole group corporation and also thiazolylthiophene group,the activity get further improved, which descripted that the thiophene ring was alsothe promotion group corporation to antiviral activity; alginates’ molecular weight andM/G value also effect on the anti-viral activity, the alginate contents high M, and inthe molecular weight at4KDa had the strongest anti-viral activity, the inhibition rateof M3d reached70%; Evaluation of antibacterial activity of derivatives: three aquaticpathogens:V. anguillarum, V. alginolyticus, V.Parahaemolyticus, Characterizations ofanti-bacterial activities by flatting punch measured inhibition zone, the minimuminhibitory concentration (MIC) was measured by Fold dilution method. The studyfound that different degrees of polymerization and M/G, the power of antibacterialwas different, where in the molecular weight of3KDa of high G alginate derivativesG2G2d had the highest anti-bacterial activity, the modifying group of the triazolegroup and thienyl group had a better resistance to the three Vibrio produced and thealginate derivatives3-thiophentriazolo-PEG-alginate d slightly higher thananti-bacterial activity. because the derivatives safty, non-toxic characteristics, whichwas expected to be a feed or drugs used in aquaculture.20series of heparin-like derivatives E were made by using the traditional sulfur trioxide-pyridine method and the non-traditional aqueous phase intermediate sulfatedsulfated sulphonated, and its results showed that the APTT of these derivatives MG1E,MG5E, MG2E, G2E can reach to220s, which were over the ocean drugs PSS. Plus,derivatives E played the anticoagulant effects roles by impacting the intrinsticpathway and common coagulation pathway, with a molecular weight of20KDa,haing a larger potential anticoagulants.
Keywords/Search Tags:alginate, chemical modification, antibacterial activity, anticoagulantactivity, antiviral activity
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