Limited uptake of [C]Gardenia Blue administered orally in male and female rats and mice.

Gardenia blue (GB), a widely used plant-derived food color is prepared by reaction of genipin, the aglycone of geniposide, with protein hydrolysate. Recent animal studies investigating GB toxicity have indicated blue coloration in the gastrointestinal tract, kidneys and mesenteric lymph nodes in rodents following dietary administration. This study investigated the uptake and disposition of [C]GB in male and female rats and mice administered 100 or 1000 mg/kg by gavage.

Synthesis of C-labeled 5-aminoimidazole-4-carboxamide-1-β-D-[ C ] ribofuranosyl 5'-monophosphate.

5-Aminoimidazole-4-carboxamide-1-β-D-[ C ] ribofuranosyl 5'-monophosphate ([ C ribose] AICAR-PO H ) (6) has been synthesized from [ C ]adenosine. Incorporation of the mass-label into [ C ribose] AICAR-PO H provides a useful standard to aid in metabolite identification and quantification in monitoring metabolic pathways. A synthetic route to the C-labeled compound has not been previously reported.

Characterization of the isomeric configuration and impurities of (Z)-endoxifen by 2D NMR, high resolution LC⬜MS, and quantitative HPLC analysis.

(Z)-Endoxifen (4-hydroxy-N-desmethyltamoxifen), an active metabolite generated via actions of CYP3A4/5 and CYP2D6, is a more potent selective estrogen receptor modulator (SERM) than tamoxifen. In the MCF-7 human mammary tumor xenograft model with female athymic mice, (Z)-endoxifen, at an oral dose of 4⬜8 mg/kg, significantly inhibits tumor growth. (Z)-Endoxifen's potential as an alternative therapeutic agent independent of CYP2D6 activities, which can vary widely in ER+ breast cancer patients, is being actively evaluated.

LC/MS characterization of impurities and degradation products of a potent antitumor peptidic dimer, CU201.

Compound CU201 [SUIM-(d-Arg-Arg-Pro-Hyp-Gly-Igl-Ser-d-Igl-Oic-Arg)(2), where SUIM=suberimidyl; Hyp=trans-4-hydroxyproline; Igl=alpha-(2-indanyl)-glycine; Oic=octahydroindole-2-carboxylic acid], is a dimeric analog of the potent bradykinin antagonist peptide B9430. It blocks the G(alphaq,11) signal of the heterotrimeric G proteins, stimulates c-Jun kinases, and induces apoptosis in lung cancer cells with neuroendocrine features. CU201 shows potent inhibition for small-cell lung cancer cells in vitro (ED(50)=0.