SummaryThe aim of the present study was to follow the dynamics of potential antihypertensive (angiotensin‐converting enzyme (ACE)) and antidiabetogenic (dipeptidyl peptidase IV (DPP‐IV)) inhibitory activities during artisanal fermentation of Mexican cocoa beans. Almendra Blanca, Criollo and Forastero cocoa beans were sampled after 0, 48, 72, 96 and 120 h of fermentation and roasting (140 °C) and subjected to simulated gastrointestinal digestion. Subsequently, proteolytic activity (OPA method), peptide abundance (RP–HPLC), ACE and DPP‐IV inhibitory activities and IC50 were determined. The results showed that proteolytic activity, peptide abundance and ACE and DPP‐IV inhibition were higher (P < 0.05) at the final stages of fermentation (96 and 120 h). However, IC50 values in partially fermented (48 to 96 h) cocoa beans were the lowest (P < 0.05) of all. In conclusion, a partially fermented cocoa bean may be desirable for its use as a functional ingredient with potential antihypertensive and antidiabetogenic effects.