The purpose of this study was to verify the effect of organic gallium on ovariectomized osteopenic rats. Thirty Wistar female rats used were divided into three groups: (1) sham-operation rats (control), (2) ovariectomized (OVX) rats with osteopenia, and (3) OVX rats with osteopenia treated with organic gallium. Treatments were performed over an 8-week period. At sacrifice, the fifth lumbar vertebral body, one tibia, one femur, and the fourth lumbar vertebrae were removed, subjected to micro-CT for determination of trabecular bone structure, and then processed for histomorphometry to assess bone turnover. The femoral neck was used for mechanical compression testing. Treatment with organic gallium increased bone volume in OVX animals. Organic gallium-treated animals had significant increases in trabecular and cortical thickness and bone strength. The plasma total calcium and inorganic phosphate concentrations in OVX rats decreased and bone mineral content in the lumbar vertebrae and femur increased after treatment with organic gallium. These data provide an important proof of concept that organic gallium may represent a powerful approach to treating or reversing severe osteoporosis in humans.
The purpose of the present study was to investigate the anti-inflammatory activity of Z-Ligustilide (LIG) in experimental ovariectomized (OVX) osteopenic rats. The anti-inflammatory potential of LIG in the regulation of nuclear factor kappa B (NF-κB), maleic dialdehyde (MDA), polymorphonuclear cells (PMN), interleukin-1β (IL-1β), inducible nitric oxide synthase (iNOS) and tumor necrosis factor-α (TNF-α), adhesion molecule (ICAM-1) and cyclooxygenase-2 (COX-2) was determined by ELISA. LIG significantly inhibited OVX-induced up-regulation of NF-κB activation and the production of IL-1β, TNF-α, iNOS, ICAM-1 and COX-2. Moreover, LIG suppressed MDA and infiltration of PMN. The results of the present study clearly demonstrate that there may be an inflammatory component in the etiology of osteoporosis. It revealed a significant anti-inflammatory effect of Z-Ligustilide in experimental OVX osteopenic rats.
The Z-ligustilide (LIG) was studied for its anti-inflammatory activities with prepared LIG nanoemulsions (LIGNE). Healthy male adult Wistar rats were used in the study. Endotoxin-induced uveitis (EIU) was induced by a footpad injection of 200 μg lipopolysaccharide. EIU rats were administered orally with saline, LIG (20 mg/kg/day), and LIGNE (20 mg LIG /kg/day), respectively. Twenty-four hours later, rats were euthanized, and blood was collected from either right marginal ear vein to estimate inflammatory cells and inflammatory mediators. The drug dissolution profiles of LIGNE in both phosphate buffer pH 6.8 and 0.1 N HCl showed complete dissolution within 20 min. Pharmacokinetic studies suggested a significant increase (P < 0.0001) in the C pmax and AUC0→24 h were observed in the LIGNE group when compared with the LIG group. LIGNE significantly reduced the levels of tumor necrosis factor alpha, interleukin 1 beta, vascular endothelial growth factor alpha, and interleukin-17. The anti-inflammatory animal testing revealed that LIGNE led to an improvement in oral bioavailability.
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