Black Cohosh (Actaea racemosa, Cimicifuga racemosa) Behaves as a Mixed Competitive Ligand and Partial Agonist at the Human μ Opiate Receptor
- 1 December 2006
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Agricultural and Food Chemistry
- Vol. 54 (26), 9852-9857
- https://doi.org/10.1021/jf062808u
Abstract
Black cohosh is a commonly used botanical dietary supplement for the treatment of climacteric complaints. Because the opiate system in the brain is intimately associated with mood, temperature, and sex hormonal levels, the activity of black cohosh extracts at the human μ opiate receptor (hMOR) expressed in Chinese hamster ovary cells was investigated. The 100% methanol, 75% ethanol, and 40% 2-propanol extracts of black cohosh effectively displaced the specific binding of [3H]DAMGO to hMOR. Further studies of the clinically used ethanol extract indicated that black cohosh acted as a mixed competitive ligand, displacing 77 ± 4% [3H]DAMGO to hMOR (Ki = 62.9 μg/mL). Using the [35S]GTPγS assay, the action of black cohosh was found to be consistent with an agonist, with an EC50 of 68.8 ± 7.7 μg/mL. These results demonstrate for the first time that black cohosh contains active principle(s) that activate hMOR, supporting its beneficial role in alleviating menopausal symptoms. Keywords: Black cohosh; menopause; hot flashes; opiate; botanical dietary supplementKeywords
This publication has 53 references indexed in Scilit:
- Targeted drug delivery crossing cytoplasmic membranes of intended cells via ligand-grafted sterically stabilized liposomesJournal of Controlled Release, 2006
- Black Cohosh and St. John’s Wort for Climacteric ComplaintsObstetrics & Gynecology, 2006
- Cimipronidine, a Cyclic Guanidine Alkaloid from Cimicifuga racemosaJournal of Natural Products, 2005
- Efficacy ofCimicifuga racemosaon climacteric complaints: A randomized study versus low-dose transdermal estradiolGynecological Endocrinology, 2005
- Pathophysiology and Treatment of Hot FlashesMayo Clinic Proceedings, 2002
- Risks and Benefits of Estrogen Plus Progestin in Healthy Postmenopausal Women: Principal Results From the Women's Health Initiative Randomized Controlled TrialJAMA, 2002
- Flavones in Extracts ofCimicifuga racemosaPlanta Medica, 1997
- Opioid control of luteinizing hormone secretion in humansJournal of Steroid Biochemistry, 1989
- Similarities between morphine withdrawal in the rat and the menopausal hot flushLife Sciences, 1983
- Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reactionBiochemical Pharmacology, 1973