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Cimicifugoside H1 is biogenetically key compounds of Cimicifugae Rhizoma. In China, the rhizomes of C. foetida L. are used to treat some symptoms, such as headache, toothache, mouth ulcers, and sore throat. Cimicifugoside H1 is a major constituent of Cimicifuga foetida L. extract with 23-epi-26-deoxyactein, cimigenolxyloside, and 25-O-acetylcimigenoside present at lower levels (the percentage 21.2%, 1.6%, 2.9% and 1.1%) but systemic exposure to 23-epi-26-deoxyactein, cimigenolxyloside, and 25-O-acetylcimigenoside following oral administration of the extract of Cimicifuga foetida L. was significantly greater than to Cimicifugoside H1. The low oral bioavailability of Cimicifugoside H1 is probably the result of its poor membrane permeability leading to poor intestinal absorption.