PURIFICATION OF SYNTHETIC PEPTIDES

Most of the synthetic peptides prepared by the LMAP are free of other peptide contaminants.  This is documented by the mass spectral analysis and the amino acid analysis.  The peptides can usually be used as is for antigen preparation.  However, you may wish to clean up additional peptide for other experiments, such as for use in tissue culture.  The simplest purification procedure is a simple desalting column.  This will remove the small molecule scavengers used to protect the amino acid side chains during cleavage of the peptide from its resin.  If you wish to HPLC purify your peptide for other experimental purposes and do not have an instrument in your laboratory, we can train you to use the LMAP preparative Rainin HPLC.  LMAP staff can also do this for you.  If you have any problems with peptide solubility, desalting, or HPLC separations, we will be glad to answer your questions.  

Desalting of Synthetic Peptides:  Desalting of peptides is performed on short columns of Sephadex G-10/G-25 or BioGel P-4/P-10 in a volatile solvent which can later be removed by lyophilization or SpeedVac concentration.  Most soluble peptides can be desalted in 20% acetic acid.  If you are not certain of the solubility of your peptide, place small amounts of the peptide in several microcentrifuge tubes.  Try to dissolve the peptide in several of the following solvents:  5% acetic acid, 20% acetic acid, 5% formic acid, 25 mM ammonium bicarbonate.  Choose the most effective solvent for your peptide. 

A large amount of peptide can be desalted on a column of Sephadex G-10 (2.5 x 15 cm).  Wash the column with 5 bed volumes of the selected solvent.  Dissolve up to 250 mg of peptide in 10 ml of solvent.  Load the peptide gently onto the surface of column.  After absorption, add 3 ml of solvent, gently washing the walls without disturbing the column bed.  Then elute with the solvent, collecting 2 ml fractions.  The peptide should elute at the void volume of the column.  Monitor the absorbance at 220 nm (for peptide bonds) or 280 nm (for Trp or Tyr).  Alternatively, use one of the peptide quantitation assays described in the next section to locate your peptide. 

If you do not have experience with packing gel filtration columns, prepacked columns are available from BioRad Laboratories or Pierce Chemical Co.  These columns will be shorter, but the sample may be as much as 1/3 of the column volume.  Resolution is best if the sample is no more than 20% of the column volume. 

HPLC Purification of Synthetic Peptides:  A simple linear gradient from 0.1% trifluoracetic acid (TFA, Pierce, Sequenal Grade) to 70% acetonitrile (+ 0.1% TFA) will purify most peptides on reversed phase columns.  A very soluble peptide can be separated on a C-18 column.  However, longer or more hydrophobic peptides are more effectively eluted from C-4 or C-8 columns.  Many peptides are not soluble in dilute TFA solution, making them difficult to prepare for injection onto an HPLC column.  Instead, peptides can be dissolved in 6 M guanidine hydrochloride (Pierce, Sequenal grade) containing 0.1% TFA [1g guanidine + 1 ml water yields a 6 M solution].  The guanidine salts will elute in the breakthrough of the column, while the peptide will bind.  Monitor the column effluent at 220 nm.  The major peak will be your peptide.  There will be minor ultraviolet absorbing peaks, which are the scavenger reagents. 

Please note that cysteine-containing peptides may sometimes give split peaks, representing both oxidized and reduced forms of the peptide.   However, because of the large amounts of reducing agents and scavengers present during cleavage from the resin, most peptides are in the fully reduced state.

Sep-Pak Cartridges for Peptide Desalting (Solid Phase Extraction):  Small, disposable cartridges containing reversed phase resin are available from several manufacturers.  These operate on the same principles as HPLC-type separations, but do not involve pumping systems, just disposable syringes.  Instructions are available with these inexpensive packages.  The peptides are eluted in either methanol or acetonitrile containing a small amount of trifluoracetic acid.  These solutions can be used as stocks, or can be easily dried down in a vacuum concentrator.  Extra drying time is needed to remove trifluoracetic acid. 

FPLC Columns:  Many laboratories at AECOM have FPLC systems.  There are several prepacked FPLC columns which are useful for peptide cleanup.  The PepSep column is a reversed phase column run under conditions similar to those described above for HPLC reversed phase.  The Fast Desalting column is a gel filtration column which can desalt your peptide in 10-15 minutes.  Although these FPLC columns are somewhat expensive, Pharmacia now sells a set of  5 HiTrap Desalting columns.  These inexpensive columns can be run with either a syringe, a peristaltic pump, or an FPLC pump.  They can even be used in series, if the sample to be desalted exceeds the capacity of a single column.  

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