Discovery and Delivery of Bioactive Natural Products

dc.contributor.authorDu, Yongleen
dc.contributor.committeechairKingston, David G. I.en
dc.contributor.committeememberGandour, Richard D.en
dc.contributor.committeememberCarlier, Paul R.en
dc.contributor.committeememberSantos, Webster L.en
dc.contributor.departmentChemistryen
dc.date.accessioned2018-06-26T08:00:45Zen
dc.date.available2018-06-26T08:00:45Zen
dc.date.issued2018-06-25en
dc.description.abstractAs a part of search for bioactive natural products from the plants in collaboration with the Natural Products Discovery Institute (NPDI), ten plant extracts were investigated for their antiplasmodial activity against Plasmodium falciparum Dd2 strain. Twenty-eight compounds were isolated, and twelve of them were new compounds. The structures of all these compounds were determined by analysis of their mass spectrometric, 1D and 2D NMR, and ECD spectrum. Among these natural products, there were three compounds with good antiplasmodial activity, trichospirolide A with an IC50 value of 1.5 μM, malleastrumolide A with an IC50 value of 2.7 μM, and (+)-lariciresinol with an IC50 value of 3.7 μM. In addition to the studies of drug delivery of bioactive natural product, doxorubicin, a novel thiolated doxorubicin analog were designed and synthesized. Its analogs and PEG stabilizing ligands were then conjugated to gold nanoparticles and the resulting Au-Dox constructs were evaluated by TEM. The release of native drug can be achieved by the action of reducing agents, and that reductive drug release gave the cleanest drug release.en
dc.description.degreePh. D.en
dc.format.mediumETDen
dc.identifier.othervt_gsexam:15423en
dc.identifier.urihttp://hdl.handle.net/10919/83762en
dc.publisherVirginia Techen
dc.rightsIn Copyrighten
dc.rights.urihttp://rightsstatements.org/vocab/InC/1.0/en
dc.subjectNatural Productsen
dc.subjectAntiplasmodialen
dc.subjectAntiproliferativeen
dc.subjectSesquiterpenoiden
dc.subjectNeolignanen
dc.subjectDiterpenoiden
dc.subjectCoumarinen
dc.subjectButanolideen
dc.titleDiscovery and Delivery of Bioactive Natural Productsen
dc.typeDissertationen
thesis.degree.disciplineChemistryen
thesis.degree.grantorVirginia Polytechnic Institute and State Universityen
thesis.degree.leveldoctoralen
thesis.degree.namePh. D.en
Files
Original bundle
Now showing 1 - 1 of 1
Loading...
Thumbnail Image
Name:
Du_Y_D_2018.pdf
Size:
14.9 MB
Format:
Adobe Portable Document Format