The effect and mechanisms of Myristica fragrans on blood clotting were evaluated by evaluating blood coagulation time and the fibrinolytic system. The compounds 2 and 5 were isolated from the herbal extract and their activities were assessed for the first time. None of the tested compounds had fibrinolytic activity, but could inhibit the fibrinolytic activity of urokinase. Compound 2 showed the highest inhibitory activity (IC50 = 1.747 mg·mL-1) followed by compounds 4 (IC50 = 1.818 mg·mL-1) and 1 (IC50 = 2.407 mg·mL-1), which were higher than that of the compound in Danshen drug tablets (IC50 = 6.577 mg·mL-1) used in China. Moreover, compounds 1 and 2 showed strong α-glucosidase inhibitory activity in a dose-dependent manner with IC50 values 21.76 ± 0.59 and 21.31 ± 0.00 μg·mL-1, respectively. These results demonstrated that the compounds are promising candidates as procoagulant and antidiabetic agents.