PMID- 23441686 OWN - NLM STAT- MEDLINE DCOM- 20130813 LR - 20231104 IS - 1520-6025 (Electronic) IS - 0163-3864 (Print) IS - 0163-3864 (Linking) VI - 76 IP - 4 DP - 2013 Apr 26 TI - Comparative study of chromatographic medium-associated mass and potential antitumor activity loss with bioactive extracts. PG - 642-7 LID - 10.1021/np300858c [doi] AB - Natural product drug discovery programs often rely on the use of silica (Si) gel, reversed-phase media, or size-exclusion resins (e.g., RP-C18, Sephadex LH-20) for compound purification. The synthetic polymer-based sorbent Diaion HP20SS (cross-linked polystyrene matrix) is used as an alternative to prepare purified natural product libraries. To evaluate the impact of chromatographic media on the isolation of biologically active, yet chromatographically unstable natural products, Diaion HP20SS was evaluated side-by-side with normal-phase sorbents for irreversible binding of extract constituents and their effects on bioactivity. An array of chemically diverse natural product-rich extracts was selected as a test panel, and a cell-based reporter assay for hypoxia-inducible factor-1 (HIF-1) was employed to monitor potential change(s) in bioactivity. Silica gel caused significant irreversible binding of three out of 10 extracts. Curcuma longa, Saururus cernuus, and Citrus reticulata extracts showed decreased HIF-1 inhibitory activity after elution through Si gel. An additional nonpolar column wash of HP20SS with EtOAc retained considerable bioactivities of active extracts. In general, Si gel produced the greatest loss of bioactivity. However, HP20SS elution reduced significantly HIF-1 inhibitory activity of certain extracts (e.g., Asimina triloba). FAU - Datta, Sandipan AU - Datta S AD - Department of Pharmacognosy, School of Pharmacy, University of Mississippi, Mississippi 38677, United States. FAU - Zhou, Yu-Dong AU - Zhou YD FAU - Nagle, Dale G AU - Nagle DG LA - eng GR - C06 RR-14503/RR/NCRR NIH HHS/United States GR - C06 RR014503/RR/NCRR NIH HHS/United States GR - CA98787/CA/NCI NIH HHS/United States GR - R01 CA098787/CA/NCI NIH HHS/United States GR - R56 CA098787/CA/NCI NIH HHS/United States PT - Journal Article PT - Research Support, N.I.H., Extramural PT - Research Support, U.S. Gov't, Non-P.H.S. DEP - 20130226 PL - United States TA - J Nat Prod JT - Journal of natural products JID - 7906882 RN - 0 (Biological Products) RN - 0 (Dextrans) RN - 0 (Hypoxia-Inducible Factor 1) RN - 0 (Plant Extracts) RN - 60650-90-0 (Silica Gel) RN - 9014-76-0 (sephadex) SB - IM MH - Asimina/chemistry MH - Aspalathus/chemistry MH - Biological Products MH - Chromatography MH - Citrus/chemistry MH - Curcuma/chemistry MH - Cyclopia Plant/chemistry MH - Dextrans MH - Female MH - Humans MH - Hypoxia-Inducible Factor 1/*antagonists & inhibitors MH - Lythraceae/chemistry MH - Plant Extracts/analysis/*chemistry MH - Podophyllum/*chemistry MH - Saururaceae/chemistry MH - Silica Gel MH - Vaccinium macrocarpon/chemistry PMC - PMC3683388 MID - NIHMS449870 COIS- The authors declare no competing financial interests. EDAT- 2013/02/28 06:00 MHDA- 2013/08/14 06:00 PMCR- 2014/04/26 CRDT- 2013/02/28 06:00 PHST- 2013/02/28 06:00 [entrez] PHST- 2013/02/28 06:00 [pubmed] PHST- 2013/08/14 06:00 [medline] PHST- 2014/04/26 00:00 [pmc-release] AID - 10.1021/np300858c [doi] PST - ppublish SO - J Nat Prod. 2013 Apr 26;76(4):642-7. doi: 10.1021/np300858c. Epub 2013 Feb 26.