Cimicifugae Rhizoma: From Origins, Bioactive Constituents to Clinical Outcomes

Abstract

Cimicifugae Rhizoma, mainly originated from C. acerina, C. dahurica, C. foetida, C. heracleifolia, C. racemosa and C. simplex, has long been used in traditional medicine system. During the past 45 years, a lot of efforts have been dedicated to the studies on their bioactive constituents, pharmacological effects and clinical uses, and a variety of biological activities including relief of hot flash, anti-osteoporosis, anti-human immunodeficiency virus (HIV), antiinflammatory, antidiabetes, antimalaria and vasoactive property have been discovered. Although C. racemosa is widely applied to relieve menopause symptoms in clinic for its hormonal-like action, meaningfully, no estrogenic effect was confirmed up to date. The purpose of this paper is to systematically highlight these achievements and the further therapeutic potential. The origins and distributions of the rhizome are simply listed and phytochemical aspects including over 200 compounds mainly belonging to cycloartane-type triterpenoids have been summarized. The pharmacological characterizations, especially, as a clinically effective phytomedicine, the effects of the rhizoma on menopause symptoms and the clinical applications including possible mechanism have been reviewed in detail. Various in vivo, in vitro studies on the anti-bone resorption effects of the triterpenoids, together with structure-activity relationships are also incorporated to explore the therapeutic potential on osteoporosis, a major public health threat for postmenopausal women.

Synergistic cytotoxic effects of tamoxifen and black cohosh on MCF-7 and MDA-MB-231 human breast cancer cells: an in vitro studyThis article is one of a selection of papers published in this special issue (part 2 of 2) on the Safety and Efficacy of Natural Health Products.

“…In fact, several placebocontrolled clinical trials, mainly in Germany, conducted with healthy women, suggest that black cohosh alleviates somatic and psychological symptoms associated with menopause (Foster 1999). The results of the most recent studies confirm the absence of any estrogenic effect of black cohosh (Li and Yu 2006); (Zhang et al 2003); (Bodinet and Freudenstein 2002); (Liske et al 2002). Black cohosh does not change levels of estradiol (E 2 ), follicle-stimulating hormone (FSH), or luteinizing hormone (LH) and does not affect vaginal maturation (changes in vaginal epithelial cell morphology) (Liske 1998).…”

Nitrogen-Containing Constituents of Black Cohosh: Chemistry, Structure Elucidation, and Biological Activities

“…Triterpene glycosides represent the major constituents of all hydroalcoholic black cohosh extracts and have been extensively studied from both the phytochemical and biological side. More than 40 triterpenes have been isolated and structurally characterized to date [21, 22]. They represent a particular analytical challenge due to their close structural similarities and overall complexity of distinguishing these structures, which include numerous stereocenters.…”

Three New Cycloartenol Triterpenoid Saponins from the Roots of Cimicifuga simplex Wormsk

“…This herb has also been used for the treatment of human immunodeficiency virus (HIV), and its more general analgesic, antipyretic, antidiabetes, antimalaria and vasoactive properties [3,4,5]. Its chemical constituents have been extensively investigated and the main constituents are 9,19-cyclolanostane triterpenoid glycosides, flavonoids, alkaloids, and chromones [6,7,8,9]. More than 200 uncommon cycloartane-type triterpenoid saponins have been isolated from Cimicifuga plants [6].…”

“…Its chemical constituents have been extensively investigated and the main constituents are 9,19-cyclolanostane triterpenoid glycosides, flavonoids, alkaloids, and chromones [6,7,8,9]. More than 200 uncommon cycloartane-type triterpenoid saponins have been isolated from Cimicifuga plants [6]. Genjiro and his team have isolated more than fifty cycloartane-type triterpenoids from C. simplex grown in Japan [10,11,12,13,14,15,16,17,18,19,20,21,22].…”