acid-phosphatase and icariin

Through researching the relationship among osteoporosis and inflammatory reaction besides angiogenesis, to compare pharmacological differences between icariin and genistein to inhibit bone loss.. 6 months old female SD rats were randomly divided into SHAM group, model group, ICA group, GEN group and E group. The bone mineral density of total, femur and lumbar, serum OC, TRACP 5b, IL-6 and VEGF, biomechanics of femur and tibia microarchitecture were analyzed.. Compared with SHAM group, model group of body weight, uterine weight, bone mineral density of total, femur and lumbar, serum OC, TRACP 5b, IL-6 and VEGF, biomechanics of femur and lumbar and tibia microarchitecture were significantly changed (P < 0.05). Compared with model group, ICA group of body weight, bone mineral density of total and femur, serum TRACP 5b and femural biomechanics were significantly changed (P < 0.05). GEN group of bone mineral density of total, femur and lumbar, serum OC, TRACP 5b, IL-6 and VEGF, biomechanics of femur and lumbar and tibia microarchitecture were significantly changed (P < 0.05).. Icariin inhibits bone loss on model rat through suppressing bone resorption. Genistein prevents bone loss on model rat by the pathway of inhibiting inflammatory reaction, activating angiogenesis, enhancing bone formation and inhibiting bone resorption. Moreover, pharmacological activity of genistein is more potential than icariin.

Topics: Acid Phosphatase; Administration, Oral; Angiogenesis Inducing Agents; Animals; Anti-Inflammatory Agents; Bone and Bones; Bone Density; Bone Density Conservation Agents; Bone Resorption; Epimedium; Fabaceae; Female; Flavonoids; Genistein; Interleukin-6; Isoenzymes; Osteocalcin; Osteoporosis; Ovariectomy; Random Allocation; Rats; Rats, Sprague-Dawley; Tartrate-Resistant Acid Phosphatase; Vascular Endothelial Growth Factor A

To investigate the effects of icariin on the streptozocin (STZ)-induced epididymis impair in rats.. The epididymis impair was induced by injection of streptozocin at dosage of 60 mg/kg ip in SD rats. Animals were randomly divided into six groups (n = 14): normal control, model group, three icariin treated group with different dosages (P.O, 20 mg/kg, 40 mg/kg, 80 mg/kg especially) and rosiglitazone group (P.O, 3 mg/kg), 12 weeks later, animals were sacrificed. The level of serum glucose, the activity of lactate dehydrogenase (LDH), acid phosphatase (ACP), gamma-glutamyltranspeptidase (gamma-GT), alpha-glucosidase activity as well as sialic acid (SA), fructose level in the epididymis were determined. The pathological examination was performed under microscope after the epididymis was fixed by 4% poly-formalin and stained by HE.. Compared with the normal control, the activity of LDH, ACP, gamma-GT and alpha-glucosidase in the epididymis revealed a decline, with lower level of SA and fructose. Histological examination showed that mature spermatocytes in the epididymis markedly decreased. These alterations were ameliorated in the groups with the treatment of icariin at 40 mg/kg and 80 mg/kg, but not at 20 mg/kg.. Icariin ameliorated the signs of epididymis in diabetic rats induced by streptozocin, this effect might carry out by promoting the elevation of special enzyme and energy metabolism in the epididymis.

Topics: Acid Phosphatase; alpha-Glucosidases; Animals; Blood Glucose; Diabetes Mellitus, Experimental; Epididymis; Flavonoids; Fructose; gamma-Glutamyltransferase; L-Lactate Dehydrogenase; Male; N-Acetylneuraminic Acid; Rats; Rats, Sprague-Dawley

Accumulating evidences suggest that Herba epimedii has the potential benefits against osteoporosis. However, previous studies were focused on the crude extract, total flavonoids (TF) and icariin (ICA), and the detailed molecular mechanisms of action and structure-activity relationship (SAR) remain unclear. Herein we aimed to systematically investigate the effects of Herba epimedii flavonoids (HEF) on the activity of osteoclasts, and explore the potential SAR. Both ICA and baohuoside-1 (BS) significantly inhibited the proliferation of RAW 264.7 cells (IC(50) 25 μM and 67 μM, respectively). Treatment of ICA resulted in G2/M arrest and apoptosis in RAW 264.7 cells as early as 12 h. Besides, HEF remarkably suppressed vitamin D-induced differentiation of osteoclasts in rabbit bone marrow cells and the bone resorption of rabbit mature osteoclasts in vitro. It is notable that the inhibitory effect of 100 μM ICA and BS on osteoclast formation is almost 90%; and the inhibition rate on bone resorption is 50% and 80%, respectively. Besides, RANKL-induced osteoclast formation from RAW 264.7 cells and the expression of TRAP, CA II, CTSK and MMP-9 was significantly reduced by the treatment of 25 μM HEF and 17β-estradiol (ES), and the inhibitory strength increases in the order TF < ES < ICA < BS, which was blocked by ICI182780 suggesting that the regulation of osteoclast activity might be ER dependent. Furthermore, the free hydroxyl group at C-7 of BS played an important role in the SAR for anti-osteoclast action. To conclude, HEF could regulate the formation and activity of osteoclasts by inhibiting the proliferation and differentiation, inducing apoptosis and cell cycle arrest and suppressing bone resorption of osteoclasts. Changes in osteoclast activity are probably mediated predominantly by interaction with nuclear estrogen receptors and via mitochondrial pathway. HEF, especially BS, has great potential for the prevention and treatment of osteoporosis.

Topics: Acid Phosphatase; Animals; Animals, Newborn; Apoptosis; Bone Resorption; Cell Cycle Checkpoints; Cell Differentiation; Cell Division; Cell Line; Cell Proliferation; Drugs, Chinese Herbal; Epimedium; Estradiol; Flavonoids; Fulvestrant; G2 Phase; Inhibitory Concentration 50; Isoenzymes; Matrix Metalloproteinase 9; Molecular Structure; Monocytes; Osteoclasts; Rabbits; RANK Ligand; Reverse Transcriptase Polymerase Chain Reaction; Tartrate-Resistant Acid Phosphatase

Icariin is a prenylated flavonol glycoside contained in the herb Epimedium, which has long been used to improve bone fracture healing or prevent osteoporosis because of the belief that the herb has bone-strengthening action. We have previously demonstrated that icariin enhances the osteogenic differentiation of rat bone marrow stromal cells, and partially explained the bone-strengthening mechanism of the herb. In the present study, the effect of icariin on osteoclastogenesis and bone resorption activity was investigated in mouse bone marrow culture. It was found that icariin dose-dependently inhibited the growth and differentiation of hemopoietic cells from which osteoclasts were formed. Far less TRAP+ multinuclear cells appeared in the 10 microM icariin group than in the control. The bone resorption pits formed in the 10 microM icariin group was also significantly less than that of the control. RT-PCR analysis showed that the gene expression of TRAP, RANK and CTR was obviously lower than that of the control. It can be concluded that icariin has the ability to inhibit the formation and bone resorption activity of osteoclasts, which suggests that icariin should be the effective component for the bone-strengthening action of herb Epimedium.

Topics: Acid Phosphatase; Animals; Biomarkers; Bone Marrow Cells; Bone Resorption; Cells, Cultured; Dose-Response Relationship, Drug; Epimedium; Flavonoids; Isoenzymes; Macrophage Colony-Stimulating Factor; Mice; Mice, Inbred BALB C; Microscopy, Phase-Contrast; Osteoclasts; Rabbits; RANK Ligand; Reverse Transcriptase Polymerase Chain Reaction; Tartrate-Resistant Acid Phosphatase

To observe the effects of Icariin on ovariectomized osteoporotic rats.. Female Wistar rats were ovariectomized and administered different dosage of Icariin and 17beta-estradiol for eight weeks. Bone mineral density (BMD), indexes of biomechanics and bone metabolism-associated biochemical markers were measured.. Icariin increased the BMD, maximum load and flexural rigidity in the osteoporotic rats. The activities of serum tartrate-resistant acid phosphatase (TRACP) and bone alkaline phosphatase (BALP) were decreased in the Icraiin-fed ovariectomized rats.. Icariin 225mg/kg per day could increase the BMD and improve indexes of bone biomechanics in ovariectomized osteoporotic rats. It was effective in preventing bone loss induced by ovariectomy.

Topics: Acid Phosphatase; Alkaline Phosphatase; Animals; Biomechanical Phenomena; Bone Density; Dose-Response Relationship, Drug; Drugs, Chinese Herbal; Female; Flavonoids; Isoenzymes; Osteoporosis; Ovariectomy; Rats; Rats, Wistar; Tartrate-Resistant Acid Phosphatase