Ligustilide, a major bioactive component of Angelica sinensis, promotes bone formation via the GPR30/EGFR pathway

Abstract

Angelica sinensis ( Oliv .) Diels is a widely-used traditional Chinese herbal medicine in treating osteoporosis. Ligustilide (LIG) is the main component of A . sinensis and is considered to be the most effective biologically active ingredient in this plant. LIG has been found to have multiple pharmacological activities, such as anti-atherosclerosis, neuroprotection, anticancer, anti-inflammatory and analgesic. However, little is known regarding its anti-osteoporotic effects. The aims of this study were to investigate any protective effect of LIG on bone formation. The results showed that LIG significantly ameliorated inhibition of bone formation in zebrafish caused by prednisolone. LIG promoted osteoblast differentiation, including that of the pre-osteoblastic cell line MC3T3-E1 and bone marrow mesenchymal stem cells. LIG greatly improved the viability of MC3T3-E1 cells exposed to H 2 O 2 , attenuated H 2 O 2 -induced apoptosis and increased the expression of Bcl-2. Furthermore, LIG treatment lead to marked activation of phosphorylated EGFR and ERK1/2. These effects could be obviously inhibited by blocking GPR30 signaling with the specific inhibitor G15. Collectively, the results reveal that GPR30 is a positive switch for LIG to increase bone formation via regulation of EGFR, and these results provide evidence for the potential of LIG to treat osteoporosis.

G Protein-Coupled Estrogen Receptor Mediates Cell Proliferation through the cAMP/PKA/CREB Pathway in Murine Bone Marrow Mesenchymal Stem Cells

“…In this study, we further showed it is also expressed in rat and mice osteogenic cells. GPER-1 has been suggested to play a role in bone development [7,12,27], and mediate the effect of chemicals, such as rutin and ligustilide, on osteogenic differentiation [28,29]. A study showed that GPER-1 activation promotes osteogenesis on the pre-osteoblast cells, MC3T3E1, through the AMPK/anti-acetyl-CoA carboxylase (ACC) pathway [30].…”

Chemical Fingerprint Analysis and Ultra-Performance Liquid Chromatography Quadrupole Time-of-Flight Mass Spectrometry-Based Metabolomics Study of the Protective Effect of Buxue Yimu Granule in Medical-Induced Incomplete Abortion Rats

“…Diels has been considered to be “female’s ginseng” mainly because of its excellent therapeutic effect for gynecological diseases, such as dysmenorrhea, irregular menstruation, premenstrual, and menopausal symptoms ( Huntley and Ernst, 2003 ; Haines et al, 2008 ; Hook, 2014 ). Ferulic acid, ligustilide and angelica polysaccharide are considered to be the main bioactive substances of Angelica ( Wei and Huang 2015 ; Yang et al, 2019 ) Studies have confirmed that Angelica sinensis (Oliv.) Diels extract can be developed for the treatment of endometriosis by inhibiting inflammatory reactions ( Xiong et al, 2020 ) and could significantly decrease NF-kB/β-actin and IL-6/β-actin mRNA expression in the uterus of rats with pelvic inflammation ( Huang et al, 2012 ).…”

Effect of Watering of Selected Seasoning Herbs with Water Treated with Low-Temperature, Low-Pressure Glow Plasma of Low Frequency

“…Four components, trans-ligustilide, α-terpinyl acetate, cis-ligustilide and β-phellandrene, constituted almost 95% of the total yield of isolated oil. Ligustilide, a phthalide, is efficient for treating osteoporosis and exhibits other pharmacological activities, such as anti-atherosclerosis, neuroprotection, anticancer, anti-inflammatory and analgesic activities [30,31]. On watering with LPGPA, the content of its trans-and cis-isomers increased and decreased by 6 and 5%, respectively.…”