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Four pesticidal botanicals were isolated (two from, Simmondsia chinensis and two from Artemisia judaica) and identified as simmondsin, simmondsin 2`ferulate, piperitone and trans-ethyl cinnamate, respectively. Oral administration of single doses each of 250 or 500 mg/kg from each compound did not show any signs of toxicity or mortality to male albino rats after two days of treatment. The in vivo effects of these compounds on activities of alkaline phosphatase (ALP), gamma-glutamyl transferase (GGT), lactate dehydrogenase (LDH) and creatinine phosphokinase (CPK) in the serum of treated rats and concentrations of testosterone, follicle stimulation hormone (FSH) and triiodothyronine hormone (T3) were evaluated. Simmondsin 2´-ferulate displayed significant decrease in the activity of ALP enzymes at the two tested doses. Simmondsin caused decrease in the activity of the enzymes at 250 mg/kg and increase in the enzymes activity at 500 mg/kg. Piperitone and trans-ethyl cinnamate increased the activity of the enzymes at two tested doses. The tested compounds showed no significant effect on the activity of GGT except for trans-ethyl cinnamate at 500 mg/kg. Simmondsin and simmondsin 2´-ferulate displayed significant decrease in the activity of both LDH and CPK, while piperitone and trans-ethyl cinnamate caused increase in the activity of these enzymes. The tested compounds lowered the concentration of FSH. Simmondsin and simmondsin 2´-ferulate decreased the concentration of T3 and testosterone. Piperitone and trans-ethyl cinnamate increased the concentration of these enzymes.