Discovery of a Potent Antiosteoporotic Drug Molecular Scaffold Derived from and Its Bioinspired Total Synthesis.

, commonly known as Dong Quai in Europe and America and as Dang-gui in China, is a medicinal plant widely utilized for the prevention and treatment of osteoporosis. In this study, we report the discovery of a new category of phthalide from , namely falcarinphthalides A and B ( and ), which contains two fragments, (3,8)-falcarindiol () and ()-ligustilide (). Falcarinphthalides A and B ( and ) represent two unprecedented carbon skeletons of phthalide in natural products, and their antiosteoporotic activities were evaluated.

Genistein Modified with 8-Prenyl Group Suppresses Osteoclast Activity Directly via Its Prototype but Not Metabolite by Gut Microbiota.

Postmenopausal osteoporosis is a significant threat to human health globally. Genistein, a soy-derived isoflavone, is regarded as a promising anti-osteoporosis drug with the effects of promoting osteoblastogenesis and suppressing osteoclastogenesis. However, its oral bioavailability (6.

Eight new phenolic acids from the leaves of and their osteoprotective activities.

Eight previously unreported phenolic acids (1-8), including three new phenylpropenoid glycosides (1-3), and five undescribed shikimic acid derivatives (4-8), together with six known analogues (9-14), were obtained from the dried leaves of . The structures of these new compounds were elucidated by extensive spectroscopic analyses (1D, 2D-NMR, HRESIMS, IR, UV) and chemical methods. Compounds 1, 2, 4, and 5 were tested for their promotion effect on osteoblastogenesis of pre-osteoblastic MC3T3-E1 cells and inhibitory effect on osteoclastogenesis of RANKL-induced RAW264.

A new strategy for discovering effective substances and mechanisms of traditional Chinese medicine based on standardized drug containing plasma and the absorbed ingredients composition, a case study of Xian-Ling-Gu-Bao capsules.

Ethnopharmacological Relevance: The overall therapeutic effect of traditional Chinese medicine formulae (TCMF) was achieved by the interactions of multiple components with multiple targets. However, current pharmacology research strategies have struggled to identify effective substance groups and encountered challenges in elucidating the underlying mechanisms of TCMF.

Aim: In this study, a comprehensive strategy was proposed and applied to elucidate the interactions of the multiple components that underlie the functions of the famous TCMF: Xian-Ling-Gu-Bao (XLGB) capsule on bone metabolism in vivo and to elucidate the molecular mechanisms underlying the effects of XLGB on bone cells, especially on osteoblasts.

A novel strategy for exploring food originated anti-adipogenesis substances and mechanism by structural similarity evaluation, ADME prediction, network pharmacology and experimental validation.

Screening potential functional substances based on active compounds is still a challenge faced by researchers since hundreds and thousands of possible compounds exist in natural products (food, herb, etc.). In this study, an integrated strategy by a combination of structural similarity evaluation, ADME (absorption, distribution, metabolism, excretion) prediction, network pharmacology and experimental validation (SANE strategy) was proposed and applied to explore anti-adipogenesis substances.

Dissection of the potential pharmacological function of neohesperidin dihydrochalcone - a food additive - by in vivo substances profiling and network pharmacology.

Food additives are widely used in our daily life, and the side-effects caused by them have gained extensive attention around the world. Notably, constituent-oriented metabolites, in some sense, always contribute to pharmacological changes, inducing toxicity, therapeutic effects, etc. Characterization of the metabolites and their potential functions is of great importance to the practical applications.

8-prenylgenistein exerts osteogenic effects via ER α and Wnt-dependent signaling pathway.

8-prenylgenistein (8PG) was previously reported to exert stronger osteogenic activity than genistein, a well-known soy phytoestrogen. However, the molecular mechanism underlying the actions of 8PG on osteoblasts was far from clear. In the present study, the osteogenic effects and mechanisms of 8PG and genistein were studied using human BMSC and murine pre-osteoblast MC3T3-E1 cells.

Icariin, but Not Genistein, Exerts Osteogenic and Anti-apoptotic Effects in Osteoblastic Cells by Selective Activation of Non-genomic ERα Signaling.

Genistein and icariin are flavonoid compounds that exhibit estrogen-like properties in inducing bone formation and reducing bone loss associated with estrogen deficiency in both preclinical and clinical studies. However, the mechanisms that are involved in mediating their estrogenic actions in bone cells are far from clear. The present study aimed to study the signaling pathways that mediate the estrogenic actions of genistein and icariin in osteoblastic cells.

8-Prenylgenistein, a prenylated genistein derivative, exerted tissue selective osteoprotective effects in ovariectomized mice.

Our previous study reported that the osteogenic effects of 8-prenylgenistein (8PG) were more potent than its parent compound genistein. This study aimed to evaluate the osteoprotective effects of 8PG in ovariectomized (OVX) mice as well as to characterize its estrogenic effects in uterus. Mature OVX mice were treated with phytoestrogen-free diet containing 8PG or genistein.

New secoiridoids from the fruits of Ligustrum lucidum.

Three new secoiridoids, nuezhenelenoliciside (1), isojaslanceoside B (2), 6'-O-trans-cinnamoyl-secologanoside (3), were isolated from the dried fruits of Ligustrum lucidum. Their structures were elucidated by comprehensive spectroscopic analysis. Among them, 1 featured a rare rearrangement product of secoiridoid, which underwent the cleavage of chemical bond between C-1 and O-2, and the reformation of a new iridoid ring between C-8 and O-2.

Discovery of a New Class of Cathepsin K Inhibitors in Rhizoma Drynariae as Potential Candidates for the Treatment of Osteoporosis.

(RD), as one of the most common clinically used folk medicines, has been reported to exert potent anti-osteoporotic activity. The bioactive ingredients and mechanisms that account for its bone protective effects are under active investigation. Here we adopt a novel in silico target fishing method to reveal the target profile of RD.

Isolation and identification of metabolites of bakuchiol in rats.

Bakuchiol, the main active component of Psoralea corylifolia, showed a range of significant pharmacological activities, including antimicrobial, antiinflammatory, reduction of bone loss and estrogenic activities. In this research, 12 metabolites, including 11 new compounds, were isolated from the urine and feces of rats after oral administration of bakuchiol, and their structures were elucidated by extensive spectroscopic analysis. The possible metabolic pathways of bakuchiol in rats were proposed, and a rare bile acid conjugation reaction was found.