Artemisia integrifolia L (Compositae) is a medicinal and edible plant. To investigate its antihyperlipidemic effect, a crude lipophilic extract and the composing compounds were isolated and fractioned from the petroleum ether extract of aerial parts of A. integrifolia using column chromatography on silica gel. The anti-hyperlipidemia effect was studied in a rat model of acute hyperlipidemia, which was induced by triton WR-1339. A new compound, integrinol (4), together with nine known compounds, namely chamazulene (1), acetylenes (E)-2 (2), acetylenes (E)-3 (3), eugenol (5), palmitic acid (6), oleic acid (7), linoleic acid (8), linolenic acid (9) and 12,13-epoxylinolenic acid were isolated from the crude lipophilic extract of A. integrifolia. The LD50 value of the crude extract was more than 4g/kg. In Triton WR-1339-induced acute hyperlipidemia model, the crude lipophilic extract (200 mg/kg) significantly reduced total cholesterol (TC) by 70% (p ≤ 0.01) and triglycerides (TGs) by 94% (p ≤ 0.001). The fractioned compounds, such as chamazulene (1), acetylene-2 (2), and linolenic acid (9), used at 4 mg/kg dose, also significantly decreased the concentrations of TC (32%, 33% and 64%, respectively) and TGs (48%, 33% and 93%, respectively). These compounds (i.e., chamazulene, acetylenes (E)-2, and linolenic acid) were considered to be responsible for the bioactive antihyperlipidemic effect. In conclusion, the crude lipid extract of Artemisia integrifolia L could be used as a potential treatment to avert hyperlipidemia. Further studies to confirm these results in other models of hyperlipidemia (e.g., diet-induced obesity) are warranted.