Ephedra Herb is a crude drug for the treatment of headache, bronchial asthma, nasal in‰ammation, and the common cold. Although it has been considered that ephedrine alkaloids (EAs) are the principal active ingredients of Ephedra Herb, EAs are known to induce palpitations, hypertension, insomnia, and dysuria as major side eŠects. Therefore, the administration of EAs-containing drugs to patients with cardiovascular-related diseases is strongly contraindicated. Previously, we isolated herbacetin 7-O-neohesperidoside from Ephedra Herb. In addition, we found that herbacetin, a ‰avonoid aglycone in Ephedra Herb, had antiproliferative and analgesic eŠects. Therefore, the prospect of preparing safer natural medicines without the adverse eŠects associated with EAs was appealing. In this symposium review, to achieve the aim of producting a clinically useful Ephedra Herb extract with none of the adverse eŠects associated with EAs, I present an e‹cient preparation method of EAs-free Ephedra Herb extract, together with its chemical composition, antiproliferative eŠects, and a putative marker for quality control.