<p>α-Amylase inhibitors play a critical role in managing blood sugar levels by hindering the enzymatic breakdown of carbohydrates, slowing glucose absorption, and contributing to metabolic health. These inhibitors are found in various natural sources, including plants, animals, and microbes, each offering unique bioactive compounds with potential therapeutic benefits. Plant-based inhibitors, such as those found in white kidney beans (<i>Phaseolus vulgaris</i>), bitter melon (<i>Momordica charantia</i>), fenugreek (<i>Trigonella foenum-graecum</i>), and cinnamon, have demonstrated significant α-amylase inhibitory activity and are associated with improved glucose regulation and potential antidiabetic properties. Animal-derived inhibitors like ovoinhibitors and milk proteins also contribute to enzyme regulation, although their use is more limited in dietary interventions. Microbial sources, such as <i>Streptomyces</i> and <i>Bacillus</i> species, offer promising avenues for biotechnological applications due to their high efficacy and easy production. The various mechanisms of action include competitive and non-competitive inhibition, which impact enzyme activity and ultimately influence postprandial glucose levels. This review synthesizes current knowledge on the sources, active compounds, and potential health implications of α-amylase inhibitors, emphasizing their relevance in developing functional foods and nutraceuticals aimed at metabolic disease prevention and management.</p>