Material Basis and Mechanism of Epimedii Folium Against Osteoporosis Based on Spectrum-Effect Relationship and Network Pharmacology / 中国实验方剂学杂志

Objective:To study the material basis and potential molecular mechanism of Epimedii Folium against osteoporosis. Method:The chemical components in 14 batches of Epimedii Folium were analyzed by ultra-performance liquid chromatography-quadrupole-time of flight-tandem mass spectrometry （UPLC-Q-TOF-MS/MS）. With the activity of alkaline phosphatase （ALP） as the pharmacodynamic index，the partial least squares regression analysis （PLSR） was conducted to establish a model uncovering the spectrum-effect relationship between UPLC-Q-TOF-MS/MS spectral peak and ALP activity and screen the active components against osteoporosis. Online databases such as the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform （TCMSP），Comparative Toxicogenomics Database （CTD），Database for Annotation，Visualization，and Integrated Discovery （DAVID） and Cytoscape 3.6.1 were employed to predict the possible mechanism of action of Epimedii Folium against osteoporosis. Result:A total of 61 peaks and 56 compounds were identified by UPLC-Q-TOF-MS/MS. PLSR showed that icariin，baohuoside Ⅰ，epimedin A，sagittatoside A，and baohuoside Ⅱ might be the active components for Epimedii Folium to inhibit osteoporosis considering their strong correlation with ALP activity. As revealed by the network pharmacological analysis of the five components mentioned above，Epimedii Folium<italic> </italic>mainly regulated seven targets such as tumor necrosis factor （TNF），androgen receptor （AR），and estrogen receptor 1 （ESR1） and eight key pathways like endocrine and other factor-regulated calcium reabsorption，vascular endothelial growth factor （VEGF） signaling pathway，and transient receptor potential （TRP） channels to exert its anti-osteoporosis effect. Conclusion:The exploration of material basis and potential molecular mechanism of Epimedii Folium against osteoporosis based on UPLC-Q-TOF-MS/MS，spectrum-effect relationship，and network pharmacology has provided an experimental basis for the scientific explanation and clinical application of Epimedii Folium in treating osteoporosis.

Pharmacological aspects of fisetin

Over the past decades, epidemiological studies have concluded that a diet rich in plant-derived products plays a pivotal role in human health. Fisetin (3,3',4',7-tetrahydroxyflavone) is a hydrophobic polyphenolic compound primarily found in edible plants (e.g. strawberry, blueberry, apple, grape, persimmon, kiwi, and cucumber). Various preclinical studies have revealed that fisetin exhibits a wide range of pharmacological effects such as antioxidant, anti-inflammatory, anti-carcinogenic, anti-osteoporotic, antimicrobial, and anti-diabetic properties. Therefore, the pharmacological in vitro and in vivo studies on fisetin are discussed in this review. Additionally, this review would be useful for further study regarding the potential of natural products, notably fisetin, and its therapeutic potential for the prevention and treatment of diseases.

Pharmacological aspects of fisetin

Over the past decades, epidemiological studies have concluded that a diet rich in plant-derived products plays a pivotal role in human health. Fisetin (3,3',4',7-tetrahydroxyflavone) is a hydrophobic polyphenolic compound primarily found in edible plants (e.g. strawberry, blueberry, apple, grape, persimmon, kiwi, and cucumber). Various preclinical studies have revealed that fisetin exhibits a wide range of pharmacological effects such as antioxidant, anti-inflammatory, anti-carcinogenic, anti-osteoporotic, antimicrobial, and anti-diabetic properties. Therefore, the pharmacological in vitro and in vivo studies on fisetin are discussed in this review. Additionally, this review would be useful for further study regarding the potential of natural products, notably fisetin, and its therapeutic potential for the prevention and treatment of diseases.

Review on research progress of chemical constituents and pharmacological activities of Ligustrum / 中草药

Ligustrum plants are important ornamental plants and medicinal plants, with important ornamental value and medicinal value. Ligustrum plants are complicated in chemical constituents and extensive pharmacological activities. The review is to present an overview about studies on chemical constituents and pharmacological activities of the Ligustrum plants, which can provide some foundations and references for the further study.

Application progress on model organism zebrafish in screening of pharmacodynamic substances of Chinese materia medica / 中草药

Compared with mammals, zebrafish has unique advantages in screening pharmacoactive substance, and has been paid more and more attention in the field of medicine. In recent years, the exploration of zebrafish has been extended and extended to the field of Chinese materia medica (CMM), especially for the screening pharmacoactive substance of the single CMM, the CMM compound and Chinese patent medicines with multi-target, multi-channel and multi-link effects. As a complete animal model, zebrafish can carry out comprehensive and deep research on the effective chemical components that play a role in TCM, and then realize convenient, rapid and high-throughput screening of pharmacodynamics substances in CMM. Combined with the literature reports in recent five years at home and abroad, this paper reviews the latest research progress and unique advantages on the screening of pharmacodynamics substances in CMM in model organism zebrafish, mainly from the screening of cardiovascular drugs, lipid-lowering and liver-protecting drugs, anti-osteoporosis drugs, anti-tumor drugs, anti-inflammatory and other drugs, in order to provide a new idea for the application of model organism zebrafish in CMM and provide reference for the new drugs research of CMM.

Beneficial effects of Cuscuta chinensis extract on glucocorticoid-induced osteoporosis through modulation of RANKL/OPG signals

Cuscuta chinensis Lam. (Convolvulaceae) is an important herbal medicine widely used to improve sexual function, treat osteoporosis, and prevent aging, and has been reported to exhibit anti-osteoporotic effects in vitro. However, the activity of Cuscuta chinensis Lam. on glucocorticoid-induced osteoporosis still remains unclear. The present study aimed to assess the protective effect and the underlying mechanism of action of Cuscuta chinensis extract (CCE) against glucocorticoid-induced osteoporosis in vivo. Sprague-Dawley rats were randomly divided into four groups as follows: control group, osteoporosis group, and 2 CCE-treated osteoporosis groups (100 mg·kg-1·day-1). Blood samples and femur bones were collected for immunohistochemistry, biochemical, mRNA expression, and western blot analysis. HPLC analysis revealed that chlorogenic acid, quercetin, and hyperin were the major constituents of CCE. The results indicated that CCE increased bone length, bone weight, and bone mineral density and suppressed dexamethasone (DEX)-induced reduction in body weight. In addition, TRAP staining indicated that CCE reduced osteoclasts in DEX-induced osteoporosis rats. Mechanistically, CCE treatment alleviated the increase of bone resorption markers and the decline of osteogenic markers, which might be partially mediated by regulation of RANKL/OPG and RunX2 pathways. These results suggest that CCE showed promising effects in the protection against glucocorticoid-induced osteoporosis through protecting osteoblasts and suppressing osteoclastogenesis.

Spectrum-effect relationship of active fraction from Hedysarum polybotrys on osteoporosis / 中草药

Objective To study the correlation of anti-osteoporosis effect of Hedysarum polybotrys and HPLC fingerprint. Methods Osteoporosis model was established through ovary resection of female rats to select the best part after performing ig administration with different extracts of H. polybotrys. The fingerprints of ethanol extract of ten batches of H. polybotrys from different habitats were established by HPLC. The partial least squares regression (PLSR) analysis was used to explore the correlation between peak areas of HPLC fingerprints and efficacy. Moreover, the effects of active ingredient of H. polybotrys on the function of osteoblasts were observed. Results The ethanol extract of H. polybotrys was the most effective part. Nine common peaks of the active fraction were selected. Adenosine, calycosin and ononin in ethanol extract of H. polybotrys have been identified separately, among which adenosine and calycosin were positively correlated with the pharmacodynamic data, and ononin was negatively correlated with the effect of drug. Additionally, calycosin can increase osteoblast ALP activity. Conclusion The results indicate that anti-osteoporosis effect of H. polybotrys is related to various components, among which adenosine and calycosin have a certain contribution to this effect, and calycosin can also stimulate the differentiation of osteoblasts in vitro.

Anti-osteoporotic study on xanthohumol, an active ingredient in Humulus lupulus L / 药学实践杂志

Objective To evaluate the anti-osteoporotic effect of xanthohumol(XN)in animal and osteoblast.Methods The anti-osteoporotic study on XN was performed with ovariectomized mice model.Serum biochemical indexes,bone mineral density(BMD)and bone histomorphology were measured using Elisa kits and Micro-CT analysis.In vitro test,the effect of XN on osteoblastic proliferation,differentiation and mineralization were assayed.The expression of protein related to bone for-mation was measured by Western blot analysis.Results In vivo experiments,XN significantly increased the estrogen level, reduced the high bone turnover rate,improved the microenvironment and BMD in ovariectomized mice.In vitro experiments, XN protected bone loss not only by promoting osteoblastic proliferation,ALP activity and bone mineralization,but also through increasing the expression of osteopontin(OPN),bone sialoprotein(BSP)and bone morphogenetic protein-2(BMP-2). Conclusion This is the first report to confirm that XN has anti-osteoporotic effect,which provides a new approach for the clin-ical treatment of osteoporosis.

Effect of PKP combined with anti osteoporosis drugs on osteoporotic vertebral compression fractures / 中国生化药物杂志

Objective To investigate the clinical effect of PKP combined with anti osteoporosis drugs in the treatment of osteoporotic vertebral compression fractures.Methods 100 cases of osteoporotic vertebral compression fractures treated in our hospital from January 2014 to December 2016 were compression fracture as the research object in the course of the study, and were randomly divided into control group and experimental group,with 50 cases in each group.Patients in the control group were treated with PKP, while the experimental group was treated with PKP combined with anti osteoporosis drugs.The related clinical indicators of the two groups were compared and analyzed.Results After the corresponding treatment, there was no significant difference between the experimental group and the control group in the rate of cement leakage and the amount of bone cement injection.After operation, the ODI index and VAS scoreof the two groups were significantly better than before treatment, the difference was statistically significant(P<0.05), the patient's cone height was well recovered.After 14 to 24 months of follow-up found that, the fracture rate of the experimental group was 10.0%, significantly lower than the control group 24.0%, the difference was statistically significant(P<0.05).Conclusion PKP combined with anti osteoporosis drugs for the treatment of osteoporotic vertebral compression fractures has good clinical effect, can effectively reduce the adjacent segment cone fracture rate, improve the quality of life of patients, with further clinical promotion and application significance.

Clinical efficacy of percutaneous kyphoplasty combined with anti-osteoporosis drugs treatment of vertebral compression fracture with osteoporosis in elderly patients / 中国综合临床

Objective To investigate the clinical effect of percutaneous kyphoplasty(PKP) combined with anti-osteoporosis drug treatment of vertebral compression fracture with osteoporosis in elderly patients.Methods Fifty-three cases of elderly patients with thoracolumbar vertebral compression fracture due to osteoporosis were selected as subjects,who were hospitalized in the Central Hospital of Sujiatun District of Shenyang from October 2010 to December 2014.They were randomly divided into the observation group (27 cases) and control group(26 cases).All patients were treated with PKP.The patients in the observation group were given the anti-osteoporosis therapy.Before and after operarion,the visual analogue scale(VAS) score was estimated and Cobb's angle of the vertebrae were measured.Postoperative complications,bone mineral density in the first half year after operation were recorded.Results VAS of treatment and of control group before operation were 7.92± 1.00 and 7.89±0.99,higher than those of one week after operation(2.68± 1.01,2.73 ± ± 1.03).Two groups of treatment and control had no significant difference(P＞0.05),but before and one week after operation had significant difference(P=0.037,0.038).Cobb's angle of treatment and control group were (28.23±6.00) ° and (28.10±5.99) ° before operation,(10.90±2.99) ° and (11.09±3.00) ° one week after operation.Two groups of treatment and control had no significant difference(P＞0.05),but before and one week after operation had significant difference (P =0.027,0.029).The bone mineral density in observation group was (0.79±0.12) g/cm2,higher than that in control group((0.65±0.06) g/cm2,P=0.048) in sixth months after operation.The duration of follow up after operetion were 12 months.Recurrence rate of vertebral compression fracture in control group was 15.4％ (4/26),higher than that in observation group (0 (0/26)),and there was significant difference between two groups (P =0.041).Conclusion PKP combined with anti-osteoporosis treatment of vertebral compression fracture with osteoporosis can quickly relieve vertebral fracture pain and reduce the incidence of new vertebral fractures hair.The treatment with minimally invasive and orthopedic effect is worthy of clinical application.

Anti-osteoporotic and Antioxidant Activities by Rhizomes of Kaempferia parviflora Wall. ex Baker

In this report, we investigated the antioxidant (peroxyl radical-scavenging and reducing capacities) and anti-osteoporotic activities of extracts and isolated constituents (1 - 16) from the rhizomes of Kaempferia parviflora Wall. ex Baker on pre-osteoclastic RAW 264.7 cells. Compound 5 exhibited significant peroxyl radical-scavenging capacity, with TE value of 8.47 ± 0.52 µM, while compound 13 showed significant reducing capacity, with CUPRAC value of 5.66 ± 0.26 µM, at 10.0 µM. In addition, flavonoid compounds 2, 4, 6, 8, 10, 12, and terpene compound 15 showed significant inhibition of tartrate-resistant acid phosphatase (TRAP) in NF-κB ligand-induced osteoclastic RAW 264.7 cells, with values ranging from 16.97 ± 1.02 to 64.67 ± 2.76%. These results indicated that K. parviflora could be excellent sources for the antioxidant and anti-osteoporotic traditional medicinal plants.

The effects of senile osteoporosis on fracture healing / 中国综合临床

Objective To explore the fraction risk in patients with osteoporosis and effects of antiosteoporosis therapy on fracture healing.Methods All the recruited subjects were senile patients with fracture in lower extremity and were treated in the Department of Orthopaedics in Shandong Qianfoshan Hospital from Aug.2006 to Feb.2011.In the total 15 cases,10 were female and 5 were male,aged from 53 to 65 years (average 56.7 years old).After surgical reduction and internal fixation,all the 15 patients did free-weight and continous passive motion (CPM) functional exercise and received anti-osteoporosis treatment.X-ray was taken to show the preoperative and postoperative lumbar vertebrae and fracture position.Meanwhile,bone mineral density and blood calcium level and phosphate level were measured.Results Thirteen out of 15 patients were healed for bone fracture after a 3-month treatment,meeting the clinical standards of the fracture healing.The clinical fracture healing rate was 86.67％.Blood calcium level,phosphate level and the bone mineral density were significantly different between that before and after the treatment ( P ＜ 0.05 ).Conclusion Osteoporosis not only increases the risk of fracture,but also has an adverse effect on the bone healing.Anti-osteoporosis therapy has a positive role to the fracture healing in the senile patients with osteoporosis.

Non-anti-hyperlipemic effects of Monascus-fermented rice and its mechanism: Recent advances / 中华临床营养杂志

Monascus-fermented rice is a natural food and traditional Chinese medicine. Besides its wellknown effectiveness in lowering blood lipids, Monascus-fermented rice is also beneficial for decreasing blood pressure, preventing osteoporosis, and lowering blood sugar. This article reviews recent advances in its non-anti-hyperlipemic effects and their potential mechanisms.