bakuchiol and Osteoporosis

Bakuchiol (BAK), [(1E,3S)-3-ethenyl-3,7-dimethyl-1,6-octadien-1-yl]phenol is a prenylated phenolic monoterpene extracted from the fruit of Psoralea corylifolia L., which belongs to the Leguminosae plant family. Previous research has shown that BAK exerts a variety of pharmacological effects, including antioxidant, antibacterial, anti-inflammatory, antiaging and estrogen-like effects. In addition, recent studies have indicated that BAK exerts protective effects in the heart, liver, skin and other organs. BAK treatment protects the heart against ischemia-reperfusion injury through modulating cardioprotective pathways. BAK also inhibits liver fibrosis via promoting myofibroblast apoptosis and relieves the hepatotoxicity of multiple toxicants by suppressing oxidative stress and inflammatory changes. BAK inhibits the proliferation of various cancer cells, including stomach, breast and skin cancer cells, thereby exerting anticancer effects. Further, BAK effectively slows skin aging by preserving skin collagen. BAK treatment can protect against bone loss and delay osteoporosis by exerting estrogen-like effects. In addition, BAK remarkably reduces blood glucose and triglycerides and might be a potential pharmacological agent that can be used to protect against pancreatic beta-cell damage and diabetes progression. In this review, the pharmacological mechanisms and protective effects of BAK in human diseases are discussed, with a focus on the protective effects of BAK in the heart, liver and other important organs.

Topics: Animals; Diabetes Mellitus; Heart; Humans; Liver; Liver Cirrhosis; Myocardial Reperfusion Injury; Neoplasms; Osteoporosis; Phenols; Protective Agents

Estrogen replacement therapy (ERT) is utilized as a major regime for treatment of postmenopausal osteoporosis at present. However, long-term supplement of estrogen may cause uterine hyperplasia and hypertension leading to a high risk of endometrial cancer and breast cancer. Psoralea corylifolia L. has long been used as tonic and food additives in many countries. Previous studies had found two ingredients in P. corylifolia L.: bavachin and bakuchiol exhibited osteoblastic activity. The present study was designed to investigate the protective effect of bakuchiol and bavachin on ovariectomy-induced bone loss and explore the possible mechanism. In vivo, bakuchiol and bavachin could prevented estrogen deficiency-induced bone loss in ovariectomized rats without uterotrophic activity. In vitro studies suggested that bakuchiol and bavachin induced primary human osteoblast differentiation by up-regulating the Wnt signalling pathway. This study suggests that such a bone-protective role makes them a promising and safe estrogen supplement for the ERT.

Topics: Animals; Cell Differentiation; Cells, Cultured; Disease Models, Animal; Female; Flavonoids; Humans; Osteoblasts; Osteoclasts; Osteoporosis; Ovariectomy; Phenols; Plant Extracts; Psoralea; Rats; Up-Regulation; Wnt Signaling Pathway

The aim of the present study was to investigate whether ethanol extracts of Psoralea corylifolia L. (PCE) and its active component protect against bone loss in ovariectomised rats. We screened oestrogenic activities of the main extract fractions using in vitro assays and identified bakuchiol as the most active oestrogenic component by HPLC and LC/MS, and then demonstrated that bakuchiol had strong binding affinity for oestrogen receptor (ER) alpha. Seventy female Sprague-Dawley rats were assigned to either a sham-operated group (n 10) or an ovariectomised group (n 60). The ovariectomised group was subdivided into six groups, each containing ten rats: vehicle group, two bakuchiol-treated groups (dose of 15 mg/kg per d or 30 mg/kg per d; ten rats for each group), two PCE-supplemented groups (0.25 % or 0.5 % extracts of diets; ten rats for each group) and a 17beta-oestradiol (E2)-treated group (20 microg/kg per d). We recorded weight and feed intake every week, and killed all animals after 6 weeks. Blood was collected, and the uterus, kidneys and livers were removed. Bakuchiol has a three-fold higher binding affinity for ERalpha than for ERbeta. Bakuchiol and PCE treatments had no uterotrophic activity even though they demonstrated oestrogenic activity in the in vitro assays. Bakuchiol and PCE treatments reduced postmenopausal bone loss by increasing alkaline phosphatase, Ca concentrations, serum E2 concentration and bone mineral density, and by decreasing the inorganic P level. The present study indicated that bakuchiol and PCE treatments could protect against bone loss.

Topics: Alkaline Phosphatase; Animals; Bone Density; Calcium; Estradiol; Female; Models, Animal; Organ Size; Osteoporosis; Ovariectomy; Phenols; Phosphorus; Phytotherapy; Plant Extracts; Protein Binding; Psoralea; Rats; Rats, Sprague-Dawley; Receptors, Estrogen; Seeds; Uterus; Weight Gain