Icariin, the main active compound of the traditional Chinese medicine, Epimedium, is commonly used for the clinical treatment of osteoporosis. However, the precise molecular mechanism of the therapeutic effect of icariin has not been elucidated. The aim of this study was to examine the effect of icariin on cell viability, alkaline phosphatase (ALP) activity, the amount of calcified nodules, and to delineate the molecular mechanism of icariin-enhanced bone formation by investigating the expression of bone morphogenic protein-2 (BMP-2), Smad4, Cbfa1/Runx2, osteoprotegerin (OPG), receptor activator of nuclear factor κ-B ligand (RANKL) and the OPG/RANKL ratio in the hFOB 1.19 human osteoblastic cell line. We found that icariin significantly increased the cell viability, the activity of ALP and the amount of calcified nodules in the hFOB 1.19 cells. Furthermore, we observed that icariin upregulated the expression of BMP-2, Smad4, Cbfa1/Runx2, OPG, RANKL and the OPG/RANKL ratio. Our results indicate that icariin can modulate the process of bone formation via the BMP-2/Smad4 signal transduction pathway in hFOB 1.19 cells.

Nuclear factor κB (NF‑κB) and mitogen‑activated protein kinase (MAPK) signaling pathways play a central role in inflammatory responses. Total flavonoids of Hedyotis diffusa Willd (TFHDW) are active compounds derived from Hedyotis diffusa Willd, which has been long used in Chinese traditional medicine for the treatment of various inflammatory diseases, including ulcerative colitis and bronchitis; however, the precise mechanisms underlying the effects of TFHDW are largely unknown. In the present study, the anti‑inflammatory effect of TFHDW was evaluated and the underlying molecular mechanisms were investigated in an in vitro inflammatory model comprising lipopolysaccharide (LPS)‑stimulated RAW 264.7 cells. The results indicated that TFHDW inhibited the inflammatory response as it significantly reduced the LPS‑induced expression of pro‑inflammatory nitric oxide, tumor necrosis factor (TNF)‑α, interleukin (IL)‑6 and IL‑1β in a concentration‑dependent manner, without causing cytotoxicity. In addition, the mRNA expression of inducible nitric oxide synthase, TNF‑α, IL‑6 and IL‑1β was suppressed by treatment with TFHDW in LPS‑stimulated RAW 264.7 cells. Moreover, TFHDW treatment significantly inhibited the LPS‑induced activation of NF‑κB via the suppression of inhibitor of κB (IκB) phosphorylation, and reduced the phosphorylation of MAPK signaling molecules (p38, c‑Jun N‑terminal protein kinase and extracellular signal‑regulated kinase 1/2), which resulted in the inhibition of cytokine expression. These findings suggest that TFHDW exerted anti‑inflammatory activity via suppression of the NF‑κB and MAPK signaling pathways.

AIM: To evaluate the efficacy and safety of the Xiaoyao pill for treatment of functional dyspepsia (FD) associated with perimenopausal depression. METHODS: This was a double-blind, randomized, controlled trial including 180 patients with FD accompanied by depression that were divided into two groups of 90. Patients in the treatment group received oral administration of the Xiaoyao pill for soothing the liver and activating the spleen, and patients in the control group received a placebo. This trial included an 8-wk therapy period with a follow-up period of 6 mo. The total efficacy and degree of depression, as assessed by the Hamilton Rating Scale for Depression (HRSD), were evaluated. Plasma levels of motilin and gastrin were measured and a gastric emptying test was conducted in each participant. RESULTS: The Xiaoyao pill had a good therapeutic effect and improved the symptoms in patients with perimenopausal FD as assessed by the HRSD score, motilin and gastrin levels, and rate of gastric emptying. The total effective rate of the Xiaoyao pill in the treatment group was significantly superior to that of the placebo in the control group. In the control group, the initial HRSD score was 12.12 ± 2.29 and decreased to 7.14 ± 1.67 after therapy (P < 0.01). In the treatment group, the initial HRSD score was 11.44 ± 2.15, which significantly decreased to 6.20 ± 2.08 after therapy (P < 0.01). Moreover, the HRSD score in the treatment group was significantly lower than in control group after 8 wk (P < 0.01). Motilin and gastrin levels in both groups were significantly increased after the 8-wk therapy (P < 0.05). The gastric emptying rate was also improved in both groups after therapy (P < 0.05), and the improvement was significantly better in the treatment group compared to the controls (P < 0.05). These results confirm the therapeutic effects of the Xiaoyao pill in perimenopausal FD patients and indicate that it is worthy of clinical promotion. CONCLUSION: The Xiaoyao pill is effective and safe for the treatment of perimenopausal women with FD associated with depression.