February 2008 - 21 articles
Oral delivery is the most common and preferred route of drug administrationalthough the digestive tract exhibits several obstacles to drug delivery including motilityand intraluminal pH profiles. The gut milieu represents the largest mucosal surfacee...
The effects of anonaine, an aporphine isoquinoline alkaloid, on dopaminebiosynthesis and L-DOPA-induced cytotoxicity in PC12 cells were investigated. Anonaineat concentration ranges of 0.01-0.2 μM showed a significant inhibition of dopaminecontent at...
The first guaian-12-oic acid glucopyranosyl ester was isolated from the roots ofPicris rhagadioloides (L.) Desf. (Asteraceae), in addition to five costuslactone-typeguaianolides, four germacranolides and three phenolic compounds. This is the first ti...
Most cancer therapeutics (chemo, radiation, antibody-based, anti-angiogenic)are at best partially and/or temporarily effective. In general, the causes for failure can besummarized as: (i) poor diffusion and/or nonuniform distribution of drug/prodrugm...
Euphorbia wallichii of the family Euphorbiaceae yielded a new rearrangedpentacyclic triterpene of the multiflorane class which we have named spirowallichiione.The structure of this natural spirocompound was elucidated with the aid of modernspectrosco...
Mammalian carboxylesterases (CESs) comprise a multigene family whose geneproducts play important roles in biotransformation of ester- or amide-type prodrugs. Theyare members of an α,β-hydrolase-fold family and are found in various mammals. It has bee...
This paper describes an efficient synthesis and the antiparasitic evaluation ofcyclic β-amino acid-containing dipeptides 3.1-3.6 and 4.1-4.5. The antimalarial propertiesof all these dipeptides have been evaluated in vitro against Plasmodium falciparu...
1,1-Dimethyl-3-oxo-1,4-diazepan-1-ium chloride (1) and 1,1-dimethyl-1-carboxymethyl-3-aminopropyl ammonium hydrochloride (2) have been obtained by thereactions of 1,1-dimethyl-1,3-propylenediamine with ethyl chloroacetate and chloroaceticacid, respec...
The compound L-valine-3-{8-[(E)-2-[3-methoxyphenyl)ethenyl]-7-methyl-1-propargylxanthine-3-yl}propyl ester hydrochloride (MSX-4) was synthesized as an aminoacid ester prodrug of the adenosine A2A receptor antagonist MSX-2. It was found to bestable in...
Paclitaxel (1a), a well known antitumor agent adopted mainly for the treatmentof breast and ovarian cancer, suffers from significant disadvantages such as low solubility,certain toxicity and specific drug-resistance of some tumor cells. To overcome t...
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