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Kanokkarn Phromnoi Supachai Yodkeeree Komsak Pintha Sariya Mapoung Maitree Suttajit Chalermpong Saenjum Pornngarm Dejkriengkraikul 《Molecules (Basel, Switzerland)》2022,27(3)
Osteoporosis is the result of an imbalance in the bone-remodeling process via an increase in osteoclastic activity and a decrease in osteoblastic activity. Our previous studies have shown that Perilla frutescens seed meal has anti-osteoclastogenic activity. However, the role of perilla leaf hexane fraction (PLH) in osteoporosis has not yet been investigated and reported. In this study, we aimed to investigate the effects of PLH in osteoclast differentiation and osteogenic potential using cell-based experiments in vitro. From HPLC analysis, we found that PLH contained high luteolin and baicalein. PLH was shown to inhibit RANKL-induced ROS production and tartrate-resistant acid phosphatase (TRAP)-positive multi-nucleated osteoclasts. Moreover, PLH significantly downregulated the RANKL-induced MAPK and NF-κB signaling pathways, leading to the attenuation of NFATc1 and MMP-9 expression. In contrast, PLH enhanced osteoblast function by regulating alkaline phosphatase (ALP) and restoring TNF-α-suppressed osteoblast proliferation and osteogenic potential. Thus, luteolin and baicalein-rich PLH inhibits osteoclast differentiation but promotes the function of osteoblasts. Collectively, our data provide new evidence that suggests that PLH may be a valuable anti-osteoporosis agent. 相似文献
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Sujit Kootala Masahiro Tokunaga Jöns Hilborn Yasuhiko Iwasaki 《Macromolecular bioscience》2015,15(12):1634-1640
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外泌体是细胞分泌的微小具膜囊泡,作为重要媒介参与细胞间的信号传递,已在疾病的诊断和治疗中发挥独特作用。骨质疏松症是全身性骨代谢疾病,容易引起骨密度减少并导致骨折,在老年人群中发病率很高,目前急需发展特异性体液诊断技术。本论文采用超速离心的方法,对血清中的外泌体进行了分离富集和表征,并采用液相色谱-质谱进行了外泌体蛋白质组学分析,共鉴定到了179个外泌体蛋白质,主要参与防御响应和免疫应答等生物过程。针对来自正常对照组、骨量减少组和骨质疏松组的血清样本,分离富集其中的外泌体,通过免标记定量蛋白质组学分析,分别鉴定到188、224和185个蛋白质。定量分析显示17个蛋白质的表达量在骨质疏松组和骨量减少组有显著改变(p<0.05),包括Integrin β3、Integrin α2β1、Talin 1和Gelsolin等,说明人体骨质在衰变过程中发生了系统性变化,并体现在血清外泌体中。该研究可为骨质疏松研究提供潜在的分子标志物,有助于阐明其病变机制。 相似文献
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Ki-Shuk Shim Youn-Hwan Hwang Seon-A Jang Taesoo Kim Hyunil Ha 《Molecules (Basel, Switzerland)》2021,26(4)
In Asia, Amomum tsao-ko has long been used as a spice or seasoning in food to stimulate digestion. In the present study, we evaluated the effects of ethanol extract of Amomum tsao-ko (EEAT) on menopausal osteoporosis and obesity. After the administration of EEAT in ovariectomy (OVX) mice models for five weeks, microcomputed tomography and a histological analysis were performed to assess, respectively, the trabecular structure and the fat accumulation in adipose, liver, and bone tissues. We also examined the effects of EEAT on a bone marrow macrophage model of osteoclastogenesis by in vitro stimulation from the receptor activator of nuclear factor-kappa Β ligand (RANKL) through real-time PCR and Western blot analysis. In addition, ultrahigh performance liquid chromatography–tandem mass spectrometry (UHPLC–MS/MS) with authentic standards was applied to characterize the phytochemical profiling of EEAT. We found that EEAT significantly decreased OVX-induced body weight gain and fat accumulation, significantly prevented OVX-induced deterioration of bone mineral density and microstructure of trabecular tissues, and significantly inhibited osteoclast differentiation by downregulating NF-κB/Fos/NFATc1 signaling in osteoclasts. Furthermore, UHPLC–MS/MS identified eight beneficial phytochemicals in EEAT. Collectively, these results suggest that EEAT might be an effective nutraceutical candidate to attenuate menopausal osteoporosis by inhibiting osteoclastogenesis and to prevent obesity by suppressing fat accumulation. 相似文献
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Ki-Shuk Shim Dong-Ryun Gu Youn-Hwan Hwang Hyun Yang Jin-Ah Ryuk Hyunil Ha 《Molecules (Basel, Switzerland)》2022,27(1)
Fritillariae thunbergii bulbus has been widely used to treat symptoms of coughs and airway congestion in the chest due to pathological colds and damp phlegm in traditional Chinese medicine. Despite its long history of traditional use, its pharmacological activities on osteoclastogenesis and osteoporosis have not been evaluated. This study investigated the effects of the water extract of Fritillariae thunbergii bulbus (WEFT) on osteoclast differentiation in bone marrow-derived macrophage cells and on ovariectomy (OVX)-induced osteoporosis in mice. We found that WEFT significantly inhibited osteoclastogenesis by downregulating the receptor activator of the NF-κB ligand (RANKL) signaling-induced nuclear factor of activated T-cells cytoplasmic 1 (NFATc1) expression. In an OVX-induced osteoporosis model, WEFT significantly prevented the OVX-induced trabecular loss of femurs, accompanied by a reduction in fat accumulation in the bone marrow and liver. In addition, WEFT significantly prevented weight gain and gonadal fat gain without recovering uterine atrophy. Using ultrahigh-performance liquid chromatography-tandem mass spectrometry, seven alkaloids (peimisine glucoside, yibeissine, peiminoside, sipeimine-glucoside, peimisine, peimine, and peiminine) were identified in WEFT. The results of this study suggest that WEFT can be a potential pharmacological candidate to reduce menopausal osteoporosis and menopause-related symptoms, such as fat accumulation. 相似文献
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Background: Osteoporosis results from excessive bone resorption and reduced bone formation, triggered by sex hormone deficiency, oxidative stress and inflammation. Tanshinones are a class of lipophilic phenanthrene compounds found in the roots of Salvia miltiorrhiza with antioxidant and anti-inflammatory activities, which contribute to its anti-osteoporosis effects. This systematic review aims to provide an overview of the skeletal beneficial effects of tanshinones. Methods: A systematic literature search was conducted in January 2021 using Pubmed, Scopus and Web of Science from the inception of these databases. Original studies reporting the effects of tanshinones on bone through cell cultures, animal models and human clinical trials were considered. Results: The literature search found 158 unique articles on this topic, but only 20 articles met the inclusion criteria and were included in this review. The available evidence showed that tanshinones promoted osteoblastogenesis and bone formation while reducing osteoclastogenesis and bone resorption. Conclusions: Tanshinones modulates bone remodelling by inhibiting osteoclastogenesis and osteoblast apoptosis and stimulating osteoblastogenesis. Therefore, it might complement existing strategies to prevent bone loss. 相似文献
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Ammar Tahir Carina Kampleitner Theresa Wirglauer Ulrike Grienke Oskar Hoffmann Judith M. Rollinger 《Molecules (Basel, Switzerland)》2022,27(11)
(1) Background: Inhibition of osteoclast differentiation is the key approach in treating osteoporosis. However, using state-of-the-art treatments such as bisphosphonates and estrogen-based therapy is usually accompanied by many side effects. As opposed to this, the use of natural products as an osteoporotic remedy delivers promising outcomes with minimal side effects. (2) Methods: In the present study, we implemented a biochemometric workflow comprising (i) chemometric approaches using NMR and mass spectrometry and (ii) cell biological approaches using an osteoclast cytochemical marker (TRAP). The workflow serves as a screening tool to pursue potential in vitro osteoclast inhibitors. (3) Results: The workflow allowed for the selective isolation of two phenylpropanoids (coniferyl alcohol and sinapyl alcohol) from the fruits of neem tree (Azadirachta indica). These two isolated phenylpropanoids showed a very promising dose-dependent inhibition of osteoclast differentiation with negligible effects in terms of cell viability. (4) Conclusion: The presented workflow is an effective tool in the discovery of potential candidates for osteoclast inhibition from complex extracts. The used biochemometric approach saves time, effort and costs while delivering precise hints to selectively isolate bioactive constituents. 相似文献
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Chun Feng Zhaowei Xu Xiaojie Tang Haifei Cao Guilong Zhang Jiangwei Tan 《Molecules (Basel, Switzerland)》2022,27(13)
Bone homeostasis is maintained with the balance between bone formation and bone resorption, which is involved in the functional performance of osteoblast and osteoclast. Disruption of this equilibrium usually causes bone disorders including osteoporosis, osteoarthritis, and osteosclerosis. In addition, aberrant activity of bone also contributes to the bone metastasis that frequently occurs in the late stage of aggressive cancers. Orphan nuclear receptor estrogen-related receptor (ERRα) has been demonstrated to control the bone cell fate and the progression of tumor cells in bone through crosstalk with various molecules and signaling pathways. However, the defined function of this receptor in bone is inconsistent and controversial. Therefore, we summarized the latest research and conducted an overview to reveal the regulatory effect of ERRα on bone homeostasis and bone metastasis, this review may broaden the present understanding of the cellular and molecular model of ERRα and highlight its potential implication in clinical therapy. 相似文献
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Si-Jing Hu Gang Cheng Hao Zhou Qi Zhang Quan-Long Zhang Yang Wang Yi Shen Chen-Xia Lian Xue-Qin Ma Qiao-Yan Zhang Lu-Ping Qin 《Molecules (Basel, Switzerland)》2022,27(3)
As cannabinoid CB2 receptors (CB2R) possess various pharmacological effects—including anti-epilepsy, analgesia, anti-inflammation, anti-fibrosis, and regulation of bone metabolism—without the psychoactive side effects induced by cannabinoid CB1R activation, they have become the focus of research and development of new target drugs in recent years. The present study was intended to (1) establish a double luciferase screening system for a CB2R modulator; (2) validate the agonistic activities of the screened compounds on CB2R by determining cAMP accumulation using HEK293 cells that are stably expressing CB2R; (3) predict the binding affinity between ligands and CB2 receptors and characterize the binding modes using molecular docking; (4) analyze the CB2 receptors–ligand complex stability, conformational behavior, and interaction using molecular dynamics; and (5) evaluate the regulatory effects of the screened compounds on bone metabolism in osteoblasts and osteoclasts. The results demonstrated that the screening system had good stability and was able to screen cannabinoid CB2R modulators from botanical compounds. Altogether, nine CB2R agonists were identified by screening from 69 botanical compounds, and these CB2R agonists exhibited remarkable inhibitory effects on cAMP accumulation and good affinity to CB2R, as evidenced by the molecular docking and molecular dynamics. Five of the nine CB2R agonists could stimulate osteoblastic bone formation and inhibit osteoclastic bone resorption. All these findings may provide useful clues for the development of novel anti-osteoporotic drugs and help elucidate the mechanism underlying the biological activities of CB2R agonists identified from the botanical materials. 相似文献
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Gyeong Do Park Yoon-Hee Cheon So Young Eun Chang Hoon Lee Myeung Su Lee Ju-Young Kim Hae Joong Cho 《Molecules (Basel, Switzerland)》2021,26(9)
Osteoporosis is a systemic metabolic bone disorder that is caused by an imbalance in the functions of osteoclasts and osteoblasts and is characterized by excessive bone resorption by osteoclasts. Targeting osteoclast differentiation and bone resorption is considered a good fundamental solution for overcoming bone diseases. β-boswellic acid (βBA) is a natural compound found in Boswellia serrata, which is an active ingredient with anti-inflammatory, anti-rheumatic, and anti-cancer effects. Here, we explored the anti-resorptive effect of βBA on osteoclastogenesis. βBA significantly inhibited the formation of tartrate-resistant acid phosphatase-positive osteoclasts induced by receptor activator of nuclear factor-B ligand (RANKL) and suppressed bone resorption without any cytotoxicity. Interestingly, βBA significantly inhibited the phosphorylation of IκB, Btk, and PLCγ2 and the degradation of IκB. Additionally, βBA strongly inhibited the mRNA and protein expression of c-Fos and NFATc1 induced by RANKL and subsequently attenuated the expression of osteoclast marker genes, such as OC-STAMP, DC-STAMP, β3-integrin, MMP9, ATP6v0d2, and CtsK. These results suggest that βBA is a potential therapeutic candidate for the treatment of excessive osteoclast-induced bone diseases such as osteoporosis. 相似文献
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《Analytical letters》2012,45(1):46-55
Abstract A Chemiluminescence Enzyme‐Linked Immuno‐Sorbent Assay (CL‐ELISA) for determination and quantification of the fungicide thiram in honeybees was developed in an indirect competitive format. The assay was optimized by determining: the optimal coating conjugate concentration and anti‐thiram antiserum dilution, the effect of the incubation time on the competitive step, the tolerance to organic solvents. The IC50 and the limit of detection (LOD) values were 60 ng mL?1 and 9 ng mL?1, respectively, similar to those of colorimetric ELISA with a calibration range of 9–15,000 ng mL?1. Cross reactivity of some related compounds such as some dithiocarbamates, a thiocarbamate, the ethylenethiourea and the tetramethylthiourea were tested. The assay was then applied to honeybees sample extracts obtained by using the liquid‐liquid extraction or the graphitized carbon‐based solid phase extraction. The calibration curves in honeybee extracts from liquid‐liquid procedure gave an IC50 of 141 ng mL?1 and a LOD of 17 ng mL?1. In case of extracts obtained by SPE these values were 139 ng mL?1 and 15 ng mL?1, respectively. The average recovery value from honeybee extracts spiked with 75 ng mL?1 of thiram was 72% for SPE, higher than for liquid‐liquid extraction (60%). On the opposite, when the honeybees were directly spiked with 2 and 10 ppm the average recovery was higher for liquid‐liquid extraction (54%), than for SPE (31%). Finally, the assay was applied to honeybee samples collected during monitoring activities in Italy and Russia. 相似文献
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《Journal of Chemometrics》2018,32(3)
Human osteoclast‐stimulating factor (OSF) induces osteoclast formation and bone resorption in senile osteoporosis by recruiting multiple signaling complexes with cognate interacting partners through its N‐terminal Src homology 3 (SH3) peptide‐recognition domain. The domain can recognize and bind to the polyproline regions of its partner proteins, rendering a broad ligand specificity and cross‐reactivity. Here, the structural basis and physicochemical property of peptide affinity and cross‐reactivity to OSF SH3 domain were investigated systematically by using an integration of statistical analysis and molecular modeling. A structure‐based quantitative structure‐activity relationship method called cross‐nonbonded interaction characterization and statistical regression was used to characterize the intermolecular interactions involved in computationally modeled domain‐peptide complex structures and then to correlate the interactions with affinity for a panel of collected SH3‐binding peptide samples. Both the structural stability and generalization ability of obtained quantitative structure‐activity relationship regression models were examined rigorously via internal cross‐validation and external test, confirming that the models can properly describe even single‐residue mutations at domain‐peptide complex interface and give a reasonable extrapolation for the mutation effect on peptide affinity. Subsequently, the best model was used to investigate the promiscuity and cross‐reactivity of OSF SH3 domain binding to its various peptide ligands. It is found that few key residues in peptide ligands are primarily responsible for the domain affinity and selectivity, while most other residues only play a minor role in domain‐peptide binding affinity and stability. The peptide residues can be classified into 3 groups in terms of their contribution to ligand selectivity: key, assistant, and marginal residues. Considering that the key residues are very few so that many domain interacting partners share a similar binding profile, additional factors such as in vivo environments and biological contexts would also contribute to the specificity and cross‐reactivity of OSF SH3 domain. 相似文献
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Anne-Claire Martel Cosette Lair 《International journal of environmental analytical chemistry》2013,93(10):978-988
The validation of a multi-residue method for the determination of five neonicotinoid insecticides (imidacloprid, clothianidin, acetamiprid, thiacloprid and thiamethoxam) in honeybees is described. The method involves the extraction of pesticides using acetonitrile and liquid partitioning with n-hexane. One clean-up is then performed on a florisil cartridge (1?g, 6?mL) and the extract is analysed by liquid chromatography-electrospray ionisation-tandem mass spectrometry (LC-ESI-MS/MS). The recovery data were obtained by spiking honeybees samples free of pesticides at two concentration levels of the various neonicotinoids. The recoveries were in the range between 93.3 and 104.0% with relative standard deviation (RSD) less than 20%. The limit of quantification (LOQ) was 0.5?ng?g?1 (corresponding to 0.05?ng?bee?1) for all pesticides except for acetamiprid which was 1?ng?g?1 (corresponding to 0.1?ng?bee?1). 相似文献
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Salma Malihah Mohammad Nor-Khaizura Mahmud-Ab-Rashid Norhasnida Zawawi 《Molecules (Basel, Switzerland)》2021,26(4)
Stingless bee-collected pollen (bee bread) is a mixture of bee pollen, bee salivary enzymes, and regurgitated honey, fermented by indigenous microbes during storage in the cerumen pot. Current literature data for bee bread is overshadowed by bee pollen, particularly of honeybee Apis. In regions such as South America, Australia, and Southeast Asia, information on stingless bee bee bread is mainly sought to promote the meliponiculture industry for socioeconomic development. This review aims to highlight the physicochemical properties and health benefits of bee bread from the stingless bee. In addition, it describes the current progress on identification of beneficial microbes associated with bee bread and its relation to the bee gut. This review provides the basis for promoting research on stingless bee bee bread, its nutrients, and microbes for application in the food and pharmaceutical industries. 相似文献
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Abdelwahab Khalil Basem H. Elesawy Tarek M. Ali Osama M. Ahmed 《Molecules (Basel, Switzerland)》2021,26(16)
Insects of the order Hymenoptera have a defensive substance that contains many biologically active compounds. Specifically, venom from honeybees (Apis mellifera) contains many enzymes and peptides that are effective against various diseases. Different research papers stated the possibility of using bee venom (a direct bee sting or in an injectable form) in treating several complications; either in vivo or in vitro. Other reports used the active fractions of bee venom clinically or at labratory scale. Many reports and publications have stated that bee venom and its constituents have multiple biological activities including anti-microbial, anti-protozoan, anti-cancer, anti-inflammatory, and anti-arthritic properties. The present review aims to refer to the use of bee venom itself or its fractions in treating several diseases and counteracting drug toxicities as an alternative protocol of therapy. The updated molecular mechanisms of actions of bee venom and its components are discussed in light of the previous updated publications. The review also summarizes the potential of venom loaded on nanoparticles as a drug delivery vehicle and its molecular mechanisms. Finally, the products of bee venom available in markets are also demonstrated. 相似文献
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Shuang Wang Qinglin Cheng Yifan Gan Qibin Li Chao Liu Wei Sun 《Molecules (Basel, Switzerland)》2022,27(14)
To explore the influence of different wax components and the shear effect exerted by the pump and pipe wall in the process of crude oil pipeline transportation on the microbehavior of wax aggregation in crude oil at low temperatures, molecular dynamics models of binary and multivariate systems of crude oil with different wax components are established in this paper. The simulation results are compared with the existing experimental results and the NIST database to verify the rationality and accuracy of the models. By using the established binary model to simulate four crude oil systems containing different wax components, it can be found that the longer the wax molecular chain, the more easily the wax molecules aggregate. The influence of temperature on the aggregation process of wax molecules with different chain lengths is also studied. The lower the temperature, the greater the difference in wax molecular aggregation degree caused by the difference in molecular chain length. Nonequilibrium molecular dynamics is used to simulate the shear process of a multivariate system of crude oil, and the micromechanisms of the shear effect on the aggregation process of wax molecules are studied. Shearing can destroy the stable structure of crude oil, resulting in the orientation and conformational transformation of wax molecules, and obtaining the region of wax molecules sensitive to temperature and shear effects, the temperatures of which are below the wax precipitation point and the shear rate of which is lower than the maximum shear rate to prevent the molecular structure from being destroyed. At the same time, the sensitivity of wax components with different chain lengths to the shear effect is studied. The research results provide theoretical guidance for ensuring the safe and economic operation of waxy crude oil production. 相似文献
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M. Mansourpoor S. Osfouri A. A. Izadpanah 《Journal of Dispersion Science and Technology》2019,40(2):161-170
Wax deposition is a frequent problem in oil pipelines and down-stream industries. Correct prediction of wax formation conditions is required to prevent this phenomenon. In this study, wax appearance temperature (WAT) of 12 Iranian oil and condensate samples were measured using viscometry data and differential scanning Calorimetry (DSC) analysis. Also, a new empirical correlation and intelligent artificial neural network (ANN) model were developed to estimate wax disappearance temperature (WDT) of crude oils. Specific gravity, pressure, and molecular weight of oil sample were used as input variables for these models. The ANN model was trained using different hidden neurons and training algorithms. Experimental measurements studies were used for validation of the new correlation. Comparing the results indicated that the ANN model has 0.27% error while most thermodynamic models have an average error of 0.35% to 2.19%. Also, the proposed correlation can predict WDT with good accuracy and minimum input data. Results show that this correlation has a maximum error of 1.16% for 310 published experimental data and 1.19% for 9 Iranian samples. 相似文献
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M. Paczuski R. Pulawski F. Tomaszewska 《Journal of Thermal Analysis and Calorimetry》1995,43(1):143-147
The processes of oxidation of microcrystalline petroleum (residual) wax were investigated. DSC was applied to estimate the thermal conditions and the influence of selected catalysts on the process. Laboratory tests of oxidation fully confirmed the results of the DSC investigations. 相似文献
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褐煤蜡主要是由蜡质、树脂和地沥青三种组分所组成的混合物,其中树脂对产品质量影响较大,常需预先加以除去。作者利用树脂在较低温度下能溶于多种溶剂的特性,用冷却结晶法对粗褐煤蜡脱树脂进行了研究。考察了粗褐煤蜡脱树脂的主要影响因素——含蜡苯溶液的浓度、冷却速率和最终冷却结晶温度等。研究结果表明,这是一种很有实用价值的脱树脂方法。 相似文献