Analytical assay development for costatolide (NSC661122) and 7,8-dihydrocostatolide (NSC661123), potential anti-HIV agents (Meeting abstract). NLM AIDSLINE Important note: Information in this article was accurate in 1995. The state of the art may have changed since the publication date.

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Analytical assay development for costatolide (NSC661122) and 7,8-dihydrocostatolide (NSC661123), potential anti-HIV agents (Meeting abstract).

Proc Annu Meet Am Assoc Cancer Res; 35:A2526 1994. Unique Identifier : AIDSLINE ICDB/95604211
Newman RA; Costa M; Fuentes A; Dept. of Clinical Investigation, UT M.D. Anderson Cancer Center,; Houston, TX 77030

Abstract: Costatolide and dihydrocostatolide, structural analogs of the rain forest-derived natural product calanolide A, have demonstrated potent anti-HIV activity in in vitro screens. As part of their preclinical development at NCI, we developed an HPLC-based analytical assay for these compounds in biological fluids. Costatolide was found to be stable in mouse, dog and human plasma for up to 24 hr at 37 C and for up to 1 month at -70 C. Costatolide was greater than 99% protein bound in plasma from all three species. Drug can be extracted from plasma using a C18 solid phase cartridge. Eluted compound is chromatographed using a Spherisorb ODS 5 mu HPLC column and a mobile phase consisting of 80:20 acetonitrile:water (v/v). The assay is linear from 12.5 to 600 ng/ml plasma when dihydrocostatolide is used as an internal standard. The method had excellent between- and within-day reproducibility as well as accuracy. An assay for dihydrocostatolide using costatolide as the internal standard is under development. Pharmacokinetic data derived from mice for each compound using these analytical assays will be presented.
Keywords: Animal Antiviral Agents/*BLOOD/PHARMACOLOGY Chromatography, High Pressure Liquid Dogs Human HIV/*DRUG EFFECTS Mice Reproducibility of Results ABSTRACTKWDanimalantiviralagents/KWDblood/pharmacologychromatography,highpressureliquiddogshumanhiv/KWDdrugeffectsmicereproducibilityofresultsabstract
950330
M9530844

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