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      Pharmacological and mechanistic aspects of quercetin in osteoporosis

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          Abstract

          Osteoporosis (OP) is a bone disease associated with increasing age. Currently, the most common medications used to treat OP are anabolic agents, anti-resorptive agents, and medications with other mechanisms of action. However, many of these medications have unfavorable adverse effects or are not intended for long-term use, potentially exerting a severe negative impact on a patient’s life and career and placing a heavy burden on families and society. There is an urgent need to find new drugs that can replace these and have fewer adverse effects. Quercetin (Que) is a common flavonol in nature. Numerous studies have examined the therapeutic applications of Que. However, a comprehensive review of the anti-osteoporotic effects of Que has not yet been conducted. This review aimed to describe the recent studies on the anti-osteoporotic effects of Que, including its biological, pharmacological, pharmacokinetic, and toxicological properties. The outcomes demonstrated that Que could enhance OP by increasing osteoblast differentiation and activity and reducing osteoclast differentiation and activity via the pathways of Wnt/β-catenin, BMP/SMAD/RUNX2, OPG/RANKL/RANK, ERK/JNK, oxidative stress, apoptosis, and transcription factors. Thus, Que is a promising novel drug for the treatment of OP.

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          New substructure filters for removal of pan assay interference compounds (PAINS) from screening libraries and for their exclusion in bioassays.

          This report describes a number of substructural features which can help to identify compounds that appear as frequent hitters (promiscuous compounds) in many biochemical high throughput screens. The compounds identified by such substructural features are not recognized by filters commonly used to identify reactive compounds. Even though these substructural features were identified using only one assay detection technology, such compounds have been reported to be active from many different assays. In fact, these compounds are increasingly prevalent in the literature as potential starting points for further exploration, whereas they may not be.
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            European guidance for the diagnosis and management of osteoporosis in postmenopausal women

            Summary Guidance is provided in a European setting on the assessment and treatment of postmenopausal women at risk from fractures due to osteoporosis. Introduction The International Osteoporosis Foundation and European Society for Clinical and Economic Aspects of Osteoporosis and Osteoarthritis published guidance for the diagnosis and management of osteoporosis in 2013. This manuscript updates these in a European setting. Methods Systematic reviews were updated. Results The following areas are reviewed: the role of bone mineral density measurement for the diagnosis of osteoporosis and assessment of fracture risk; general and pharmacological management of osteoporosis; monitoring of treatment; assessment of fracture risk; case-finding strategies; investigation of patients; health economics of treatment. The update includes new information on the evaluation of bone microstructure evaluation in facture risk assessment, the role of FRAX® and Fracture Liaison Services in secondary fracture prevention, long-term effects on fracture risk of dietary intakes, and increased fracture risk on stopping drug treatment. Conclusions A platform is provided on which specific guidelines can be developed for national use.
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              The re-emergence of natural products for drug discovery in the genomics era.

              Natural products have been a rich source of compounds for drug discovery. However, their use has diminished in the past two decades, in part because of technical barriers to screening natural products in high-throughput assays against molecular targets. Here, we review strategies for natural product screening that harness the recent technical advances that have reduced these barriers. We also assess the use of genomic and metabolomic approaches to augment traditional methods of studying natural products, and highlight recent examples of natural products in antimicrobial drug discovery and as inhibitors of protein-protein interactions. The growing appreciation of functional assays and phenotypic screens may further contribute to a revival of interest in natural products for drug discovery.
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                Author and article information

                Contributors
                Journal
                Front Pharmacol
                Front Pharmacol
                Front. Pharmacol.
                Frontiers in Pharmacology
                Frontiers Media S.A.
                1663-9812
                25 January 2024
                2024
                : 15
                : 1338951
                Affiliations
                [1] 1 College of Traditional Chinese Medicine , Shandong University of Traditional Chinese Medicine , Jinan, China
                [2] 2 Shandong Institute of Endocrine and Metabolic Diseases , Jinan, China
                [3] 3 Endocrine and Metabolic Diseases Hospital of Shandong First Medical University , Shandong First Medical University and Shandong Academy of Medical Sciences , Jinan, China
                [4] 4 Bone Biomechanics Engineering Laboratory of Shandong Province , Shandong Medicinal Biotechnology Center , School of Biomedical Sciences , Neck-Shoulder and Lumbocrural Pain Hospital of Shandong First Medical University , Shandong First Medical University and Shandong Academy of Medical Sciences , Jinan, China
                [5] 5 NHC Key Laboratory of Biotechnology Drugs (Shandong Academy of Medical Sciences) , Biomedical Sciences College , Shandong First Medical University , Jinan, China
                [6] 6 Affiliated Hospital of Shandong University of Traditional Chinese Medicine , Jinan, China
                Author notes

                Edited by: Bee Ling Tan, Management and Science University, Malaysia

                Reviewed by: Chiara Ciaccio, Università di Roma Tor Vergata, Italy

                Brunella Grigolo, Rizzoli Orthopedic Institute (IRCCS), Italy

                Rogério Leone Buchaim, University of São Paulo, Brazil

                *Correspondence: Fan-Jie Liu, liufj198211@ 123456126.com ; Ying Yin, 563298098@ 123456qq.com ; Mei-Na Yang, meina861010@ 123456163.com
                Article
                1338951
                10.3389/fphar.2024.1338951
                10851760
                38333006
                9d7dde01-b948-4328-8f41-02ce071e853c
                Copyright © 2024 Deng, Ding, Lu, Zhang, Du, Wang, Yang, Yin and Liu.

                This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

                History
                : 15 November 2023
                : 10 January 2024
                Funding
                The author(s) declare financial support was received for the research, authorship, and/or publication of this article. This study was financially supported by the Natural Science Foundation of China (No. 82004212), the Shandong Province Medical Health Science and Technology Development Plan Project (No. 202204070951) and the TCM Science and Technology Project of Shandong Province (No. 2021M175).
                Categories
                Pharmacology
                Review
                Custom metadata
                Ethnopharmacology

                Pharmacology & Pharmaceutical medicine
                quercetin,antiosteoporosis,pharmacokinetics,toxicology,osteoblast,osteoclast

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