In numerous nanomaterials, gold has been extensively developed as colloidal metal since early times in Europe. Due to relative simple preparation and high biocompatibility, gold nanoparticle is the most widely applied nanomaterials in biomedicine such as bio-chips, biosensing and bio-imaging using biomolecule- gold nanoparticle conjugates. These include ultrasensitive molecular-molecular interaction detection using SERS (Surface Enhanced Raman Spectroscopy) in vitro and vivo. Gold nanoparticles have been successfully used as a therapy for rheumatoid arthritis (RA) and for cancer treatment in disease animal models in recent years. Gold nanoparticles applied for tumor targeting with surface modification of peptide ligands or antibodies have been reported and thus may enable simultaneous diagnostics and therapeutics in one single platform-the theranotics concept. In this review we will introduce the various biomedical application based on native gold nanoparticles and their different modifications (DNA, peptide and enzyme). The potential for gold colloid and its derived functional nanoparticles is anticipated to play a critical role in future medicine.