Fructus Ligustri Lucidi in Osteoporosis: A Review of its Pharmacology, Phytochemistry, Pharmacokinetics and Safety

Abstract

Background: Fructus Ligustri Lucidi (FLL) has now attracted increasing attention as an alternative medicine in the prevention and treatment of osteoporosis. This study aimed to provide a general review of traditional interpretation of the actions of FLL in osteoporosis, main phytochemical constituents, pharmacokinetics, pharmacology in bone improving effect, and safety. Materials and Methods: Several databases, including PubMed, China National Knowledge Infrastructure, National Science and Technology Library, China Science and Technology Journal Database, and Web of Science were consulted to locate publications pertaining to FLL. The initial inquiry was conducted for the presence of the following keywords combinations in the abstracts: Fructus Ligustri Lucidi, osteoporosis, phytochemistry, pharmacokinetics, pharmacology, osteoblasts, osteoclasts, salidroside. About 150 research papers and reviews were consulted. Results: FLL is assumed to exhibit anti-osteoporotic effects by improving liver and kidney deficiencies and reducing lower back soreness in Traditional Chinese Medicine (TCM). The data from animal and cell experiments demonstrate that FLL is able to improve bone metabolism and bone quality in ovariectomized, growing, aged and diabetic rats through the regulation of PTH/FGF-23/1,25-(OH)2D3/CaSR, Nox4/ROS/NF-κB, and OPG/RANKL/cathepsin K signaling pathways. More than 100 individual compounds have been isolated from this plant. Oleanolic acid, ursolic acid, salidroside, and nuzhenide have been reported to exhibit the anti-osteoporosis effect. The pharmacokinetics data reveals that salidroside is one of the active constituents, and that tyrosol is hard to detect under physiological conditions. Acute and subacute toxicity studies show that FLL is well tolerated and presents no safety concerns. Conclusions: FLL provides a new option for the prevention and treatment of osteoporosis, which attracts rising interests in identifying potential anti-osteoporotic compounds and fractions from this plant. Further scientific evidences are expected from well-designed clinical trials on its bone protective effects and safety.

Intra-Articular Injection of Fructus Ligustri Lucidi Extract Attenuates Pain Behavior and Cartilage Degeneration in Mono-Iodoacetate Induced Osteoarthritic Rats

“…Bone and joint diseases, such as osteoarthritis and osteoporosis, are defined as “bone atrophy,” “bone loss,” or “bone rheumatism” in TCM, being attributed to the TCM syndrome of kidney-deficiency ( Guo et al, 2015 ). Meanwhile, FLL exerts bone-protective effect due to its kidney-tonifying activity against kidney deficiency, and has thereby been clinically used to treat osteoporosis and bone metabolic disorders ( Chen et al, 2017 ). Previous studies showed that FLL extract modulated the turnover of bone and the calcium balance in ovariectomized (OVX) rats ( Zhang et al, 2006 ).…”

“…It was originally recorded in the earliest existing Pharmacopeia “ Shennong Ben Cao Jing” ( Shennong’s Herbal ) during the East Han Dynasty of China (25-220 AD). It has been clinically used for over 1000 years, mainly to treat age-related diseases such as osteoporosis, arthritis, and bone pain ( Pang et al, 2015 ; Chen et al, 2017 ). In the Chinese Pharmacopeia, FLL is recognized as an edible herb with kidney-tonifying activity and is effective in treating soreness and weakness of waist and knees ( China Pharmacopeia Committee, 2015 ).…”

A rapid assay to screen adenosine deaminase inhibitors from Ligustri Lucidi Fructus against metabolism of cordycepin utilizing ultra‐high‐performance liquid chromatography–tandem mass spectrometry

“…These methods are less time‐consuming and have satisfactory selectivity. Ligustri Lucidi Fructus (LLF), the fruit of Ligustrum lucidum Ait., is a herbal medicine commonly used in clinical practice in China for nearly two thousand years (Chen et al, ). According to the Chinese Pharmacopoeia (2015 edition), the main function of LLF is to nourish the liver and kidney, brighten eyes, and make hair black (Chinese Pharmacopoeia Committee, ).…”

A validated LC–MS/MS method for the determination of specnuezhenide and salidroside in rat plasma and its application to a pharmacokinetic study

“…In the theory of traditional Chinese medicine, FLL belongs to the hepatic and nephritic meridian that has the effects of cultivating the spirit and nourishing the liver and kidney and it exhibits extensive bioactivities (Pang et al, ). A phytochemistry study suggested that iridoid glycosides were the main bioactive components (Chen et al, ). Among these, the content of specnuezhenide (SPN) was relatively high (Shi, Ma, & Cai, ).…”