Garlic is a natural source which has abundant organosulfur constituents. Garlic is divided into water-soluble organosulfur constituents mainly SAC (S-allylcystein), NAC (N-acetylcysteine) and oil soluble organosulfur constituents such as DATS (diallyl trisulfide), DADS (diallyl disulfide), DAS (diallyl sulfide). The aim of this research was to compare the bioactive constituents and antioxidant activity between garlic water-soluble and garlic oil. Garlic water-soluble constituents were identified by Liquid Chromatography-Mass Spectrometry (LC-MS) and five constituents were found, namely N-acetylcysteine (NAC), cysteinyl-alanine, phenol-2-2-benzoxazolyl and two unknown constituents. The GC-MS chromatogram also showed three main constituents present in garlic oil as diallyldisulphide (DADS), diallyltrisulphide (DATS) and D-limonene. Interestingly, garlic water-soluble extract had higher antioxidant activity 70 % ± 0.02 % in comparison with garlic oil 58 % ± 0.07 %. This study conducts a novel preparation of garlic water-soluble for enhancing antioxidant properties on garlic novel preparation.