Drug and Therapy for Osteoarthritis (OA)

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (15 August 2021) | Viewed by 43465

Special Issue Editor


E-Mail Website
Guest Editor
Department of Biological Sciences, Sungkyunkwan University, Suwon 16419, Republic of Korea
Interests: oteoarthritis; rheumatoid arthritis; autoimmune diseases; inflammation

Special Issue Information

Dear Colleagues,

Osteoarthritis (OA) is a whole-joint disease involving structural and functional alterations of all joint tissues such as cartilage destruction, subchondral bone remodeling, osteophyte formation, and synovial inflammation. Since various genes associated with osteoarthritis were discovered, pharmacological drugs, or therapies targeting the genes have not yet been developed. In addition, current management for osteoarthritis through non-pharmacological interventions and pharmacological treatment do exist, but they are limited to analgesic efficacy and side effects. New pharmacological therapies have been developed to overcome these issues. This Special Issue focuses on currently developing new drugs and treatments for knee osteoarthritis. This issue in particular focuses on proving OA therapeutic reagent with DMM (destabilization of medial meniscus) induced OA model, most suitable for human OA development, but not acute mouse models (collagenase or MIA induced model). We invite investigators to contribute original research articles and review articles on novel pharmacological medicines and therapies for knee osteoarthritis. This Special Issue will cover the below topics:

  • Gene targeting pharmaceutical drug for knee osteoarthritis, specific on the transcription factors
  • Novel analgesic therapies in knee osteoarthritis
  • Single or mixture natural compounds for knee osteoarthritis

Prof. Dr. Siyoung Yang
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Published Papers (12 papers)

Order results
Result details
Select all
Export citation of selected articles as:

Research

Jump to: Review

17 pages, 4608 KiB  
Article
Inhibitory Effects of IL-6-Mediated Matrix Metalloproteinase-3 and -13 by Achyranthes japonica Nakai Root in Osteoarthritis and Rheumatoid Arthritis Mice Models
by Xiangyu Zhao, Dahye Kim, Godagama Gamaarachchige Dinesh Suminda, Yunhui Min, Jiwon Yang, Mangeun Kim, Yaping Zhao, Mrinmoy Ghosh and Young-Ok Son
Pharmaceuticals 2021, 14(8), 776; https://doi.org/10.3390/ph14080776 - 7 Aug 2021
Cited by 9 | Viewed by 3274
Abstract
Achyranthes japonica Nakai root (AJNR) is used to treat osteoarthritis (OA) and rheumatoid arthritis (RA) owing to its anti-inflammatory and antioxidant effects. This study investigated the inhibitory effects of AJNR on arthritis. AJNR was extracted using supercritical carbon dioxide (CO2), and [...] Read more.
Achyranthes japonica Nakai root (AJNR) is used to treat osteoarthritis (OA) and rheumatoid arthritis (RA) owing to its anti-inflammatory and antioxidant effects. This study investigated the inhibitory effects of AJNR on arthritis. AJNR was extracted using supercritical carbon dioxide (CO2), and its main compounds, pimaric and kaurenoic acid, were identified. ANJR’s inhibitory effects against arthritis were evaluated using primary cultures of articular chondrocytes and two in vivo arthritis models: destabilization of the medial meniscus (DMM) as an OA model, and collagenase-induced arthritis (CIA) as an RA model. AJNR did not affect pro-inflammatory cytokine (IL-1β, TNF-α, IL-6)-mediated cytotoxicity, but attenuated pro-inflammatory cytokine-mediated increases in catabolic factors, and recovered pro-inflammatory cytokine-mediated decreases in related anabolic factors related to in vitro. The effect of AJNR is particularly specific to IL-6-mediated catabolic or anabolic alteration. In a DMM model, AJNR decreased cartilage erosion, subchondral plate thickness, osteophyte size, and osteophyte maturity. In a CIA model, AJNR effectively inhibited cartilage degeneration and synovium inflammation in either the ankle or knee and reduced pannus formation in both the knee and ankle. Immunohistochemistry analysis revealed that AJNR mainly acted via the inhibitory effects of IL-6-mediated matrix metalloproteinase-3 and -13 in both arthritis models. Therefore, AJNR is a potential therapeutic agent for relieving arthritis symptoms. Full article
(This article belongs to the Special Issue Drug and Therapy for Osteoarthritis (OA))
Show Figures

Graphical abstract

19 pages, 1393 KiB  
Article
Pharmacokinetic Study of Anti-osteoarthritic Compounds of a Standardized Fraction from Sphaeralcea Angustifolia
by Jade Serrano-Román, Pilar Nicasio-Torres, Elizabeth Hernández-Pérez and Enrique Jiménez-Ferrer
Pharmaceuticals 2021, 14(7), 610; https://doi.org/10.3390/ph14070610 - 25 Jun 2021
Cited by 4 | Viewed by 2261
Abstract
Sphaeralcea angustifolia has been widely used in inflammatory conditions such as blows, bruises, fractures, and wounds. The compounds identified as active in plants and suspension cell culture of S. angustifolia were tomentin, scopoletin, and sphaeralcic acid. To consolidate the integral use of knowledge [...] Read more.
Sphaeralcea angustifolia has been widely used in inflammatory conditions such as blows, bruises, fractures, and wounds. The compounds identified as active in plants and suspension cell culture of S. angustifolia were tomentin, scopoletin, and sphaeralcic acid. To consolidate the integral use of knowledge about the S. angunstifolia and strengthen its pharmacological use in patients with knee osteoarthritis, the pharmacokinetic behavior of the active compounds was characterized. The SaTSS (S. angustifoloia standardized in Tomentin, Scopoletin, and Sphaeralcic acid) anti-ostearthritic fraction was obtained from cell suspension. The analytical method of High-Performance Liquid Chromatography (HPLC) for tomentin, scopoletin, and sphaeralcic acid were validated determining the accuracy, precision linearity, sensibility, specificity, detection limits, and quantification time-range parameters, as well as extraction efficiency and stability of compounds. The pharmacokinetic assay was performed with ICR mice strain, in which the mice were administrated with a single oral or intravenous dose (400 mg/kg with 7.1 mg/kg of scopoletin and tomentin in mixture and 34.6 mg/kg of sphaeralcic acid) of the SaTSS standardized active fraction. The results of the validated analytical methods allowed establishing, in a validated manner, that a coumarin mixture and sphaeralcic acid present in the SaTES fraction were detected in plasma. According to the values of Akaike Information Criteria (AIC), Sum of Squares (SS), Schwarz Criteria (SC), and by the determination coefficient (R2), the compounds follow a two-compartment model. Full article
(This article belongs to the Special Issue Drug and Therapy for Osteoarthritis (OA))
Show Figures

Figure 1

15 pages, 15594 KiB  
Article
Autologous Adipose-Derived Mesenchymal Stem Cells Combined with Shockwave Therapy Synergistically Ameliorates the Osteoarthritic Pathological Factors in Knee Joint
by Jai-Hong Cheng, Ke-Tien Yen, Wen-Yi Chou, Shun-Wun Jhan, Shan-Ling Hsu, Jih-Yang Ko, Ching-Jen Wang, Chun-En Aurea Kuo, Szu-Ying Wu, Tsai-Chin Hsu and Chieh-Cheng Hsu
Pharmaceuticals 2021, 14(4), 318; https://doi.org/10.3390/ph14040318 - 1 Apr 2021
Cited by 3 | Viewed by 2361
Abstract
Adipose-derived mesenchymal stem cells (ADSCs) and shockwave (SW) therapy have been shown to exert a chondroprotective effect for osteoarthritis (OA). The results of this study demonstrated that autologous ADSCs had dose-dependent and synergistic effects with SW therapy (0.25 mJ/mm2 with 800 impulses) [...] Read more.
Adipose-derived mesenchymal stem cells (ADSCs) and shockwave (SW) therapy have been shown to exert a chondroprotective effect for osteoarthritis (OA). The results of this study demonstrated that autologous ADSCs had dose-dependent and synergistic effects with SW therapy (0.25 mJ/mm2 with 800 impulses) in OA rat knee joint. Autologous, high-dose 2 × 106 ADSCs (ADSC2 group) combined with SW therapy significantly increased the bone volume, trabecular thickness, and trabecular number among in the treatment groups. ADSC2 combined with SW therapy significantly reduced the synovitis score and OARSI score in comparison with other treatments. In the analysis of inflammation-induced extracellular matrix factors of the articular cartilage in OA, the results displayed that ADSC2 combined with SW therapy had a greater than other treatments in terms of reducing tumor necrosis factor-inducible gene (TSG)-6 and proteoglycan (PRG)-4, in addition to increasing tissue inhibitor matrix metalloproteinase (TIMP)-1 and type II collagen. Furthermore, ADSC2 combined with SW therapy significantly reduced the expression of inflammation-induced bone morphogenetic protein (BMP)-2 and BMP-6. Therefore, the results demonstrated that ADSC2 combined with SW therapy had a synergistic effect to ameliorate osteoarthritic pathological factors in OA joints. Full article
(This article belongs to the Special Issue Drug and Therapy for Osteoarthritis (OA))
Show Figures

Figure 1

14 pages, 3816 KiB  
Article
Safflower Seed Extract Attenuates the Development of Osteoarthritis by Blocking NF-κB Signaling
by Seong Jae Han, Min Ju Lim, Kwang Min Lee, Eunjeong Oh, Yu Su Shin, Seokho Kim, Joong Sun Kim, Seung Pil Yun and Li-Jung Kang
Pharmaceuticals 2021, 14(3), 258; https://doi.org/10.3390/ph14030258 - 12 Mar 2021
Cited by 10 | Viewed by 2850
Abstract
Although safflower seed extract exhibits pharmacological activity against various diseases, the effects of its individual compounds on osteoarthritis (OA) have not been elucidated. Here, we evaluated the effects of these extracts and their single compounds on OA. N-(p-Coumaroyl) serotonin and N-feruloyl serotonin, main [...] Read more.
Although safflower seed extract exhibits pharmacological activity against various diseases, the effects of its individual compounds on osteoarthritis (OA) have not been elucidated. Here, we evaluated the effects of these extracts and their single compounds on OA. N-(p-Coumaroyl) serotonin and N-feruloyl serotonin, main components of safflower seed extract, were isolated by high-performance liquid chromatography. Under in vitro OA mimic conditions, the expression of the matrix metalloproteinases (MMPs) MMP3/13 and a disintegrin and metalloproteinase with thrombospondin motifs (ADAMTS) ADAMTS5 were reduced in mouse chondrocytes treated with safflower seed extract. Furthermore, the oral administration of safflower seed extract attenuated cartilage destruction in a mouse OA model induced by destabilization of the medial meniscus. N-(p-Coumaroyl) serotonin and N-feruloyl serotonin, but not serotonin, reduced MMP3, MMP13, and ADAMTS5 expression in IL-1β-treated chondrocytes. Additionally, they significantly blocked the nuclear factor-κB (NF-κB) pathway by inhibiting IκB degradation and p65 phosphorylation. Our results suggest that safflower seed extract and its single compounds can attenuate cartilage destruction by suppressing MMP and ADMATS5 expression. The anti-arthritic effects are mediated by NF-κB signaling and involve the inhibition of IκB degradation and p65 phosphorylation. These results indicate that safflower seed extract may serve as a novel therapeutic agent against OA. Full article
(This article belongs to the Special Issue Drug and Therapy for Osteoarthritis (OA))
Show Figures

Graphical abstract

9 pages, 2965 KiB  
Article
Obtusifolin, an Anthraquinone Extracted from Senna obtusifolia (L.) H.S.Irwin & Barneby, Reduces Inflammation in a Mouse Osteoarthritis Model
by Jiho Nam, Dong-Won Seol, Choong-Gu Lee, Gabbine Wee, Siyoung Yang and Cheol-Ho Pan
Pharmaceuticals 2021, 14(3), 249; https://doi.org/10.3390/ph14030249 - 10 Mar 2021
Cited by 8 | Viewed by 2584
Abstract
Osteoarthritis (OA) is an age-related degenerative disease that causes cartilage dysfunction and inflammation. Obtusifolin, an anthraquinone extracted from Senna obtusifolia (L.) H.S.Irwin & Barneby seeds, has anti-inflammatory functions; it could be used as a drug component to relieve OA symptoms. In this study, [...] Read more.
Osteoarthritis (OA) is an age-related degenerative disease that causes cartilage dysfunction and inflammation. Obtusifolin, an anthraquinone extracted from Senna obtusifolia (L.) H.S.Irwin & Barneby seeds, has anti-inflammatory functions; it could be used as a drug component to relieve OA symptoms. In this study, we investigated the effects of obtusifolin on OA inflammation. In vitro, interleukin (IL)-1β (1 ng/mL)-treated mouse chondrocytes were co-treated with obtusifolin at different concentrations. The expression of matrix metalloproteinase (Mmp) 3, Mmp13, cyclooxygenase 2 (Cox2), and signaling proteins was measured by polymerase chain reaction and Western blotting; collagenase activity and the PGE2 level were also determined. In vivo, OA-induced C57BL/6 mice were administered obtusifolin, and their cartilage was stained with Safranin O to observe damage. Obtusifolin inhibited Mmp3, Mmp13, and Cox2 expression to levels similar to or more than those after treatment with celecoxib. Additionally, obtusifolin decreased collagenase activity and the PGE2 level. Furthermore, obtusifolin regulated OA via the NF-κB signaling pathway. In surgically induced OA mouse models, the cartilage destruction decreased when obtusifolin was administered orally. Taken together, our results show that obtusifolin effectively reduces cartilage damage via the regulation of MMPs and Cox2 expression. Hence, we suggest that obtusifolin could be a component of another OA symptom reliever. Full article
(This article belongs to the Special Issue Drug and Therapy for Osteoarthritis (OA))
Show Figures

Figure 1

14 pages, 1968 KiB  
Article
Schisandrol A Suppresses Catabolic Factor Expression by Blocking NF-κB Signaling in Osteoarthritis
by Seong Jae Han, Jimoon Jun, Seong-il Eyun, Choong-Gu Lee, Jimin Jeon and Cheol-Ho Pan
Pharmaceuticals 2021, 14(3), 241; https://doi.org/10.3390/ph14030241 - 8 Mar 2021
Cited by 3 | Viewed by 2336
Abstract
Schisandrol A possesses pharmacological properties and is used to treat various diseases; however, its effects on osteoarthritis (OA) progression remain unclear. Here, we investigated Schisandrol A as a potential therapeutic agent for OA. In vitro, Schisandrol A effects were confirmed based on the [...] Read more.
Schisandrol A possesses pharmacological properties and is used to treat various diseases; however, its effects on osteoarthritis (OA) progression remain unclear. Here, we investigated Schisandrol A as a potential therapeutic agent for OA. In vitro, Schisandrol A effects were confirmed based on the levels of expression of catabolic factors (MMPs, ADAMTS5, and Cox2) induced by IL-1β or Schisandrol A treatment in chondrocytes. In vivo, experimental OA in mice was induced using a destabilized medial meniscus (DMM) surgical model or oral gavage of Schisandrol A in a dose-dependent manner, and demonstrated using histological analysis. In vitro and in vivo analyses demonstrated that Schisandrol A inhibition attenuated osteoarthritic cartilage destruction via the regulation of Mmp3, Mmp13, Adamts5, and Cox2 expression. In the NF-κB signaling pathway, Schisandrol A suppressed the degradation of IκB and the phosphorylation of p65 induced by IL-1β. Overall, and Schisandrol A reduced the expression of catabolic factors by blocking NF-κB signaling and prevented cartilage destruction. Therefore, Schisandrol A attenuated OA progression, and can be used to develop novel OA drug therapies. Full article
(This article belongs to the Special Issue Drug and Therapy for Osteoarthritis (OA))
Show Figures

Figure 1

11 pages, 3958 KiB  
Article
Ameliorative Effects of Loganin on Arthritis in Chondrocytes and Destabilization of the Medial Meniscus-Induced Animal Model
by Eunkuk Park, Chang Gun Lee, Seung Hee Yun, Seokjin Hwang, Hyoju Jeon, Jeonghyun Kim, Subin Yeo, Hyesoo Jeong, Seong-Hoon Yun and Seon-Yong Jeong
Pharmaceuticals 2021, 14(2), 135; https://doi.org/10.3390/ph14020135 - 8 Feb 2021
Cited by 8 | Viewed by 2129
Abstract
Arthritis is a common inflammatory disease that causes pain, stiffness, and joint swelling. Here, we investigated the ameliorative effects of loganin on arthritis in vitro and in vivo. A single bioactive compound was fractionated and isolated from Cornus officinalis (CO) extract to screen [...] Read more.
Arthritis is a common inflammatory disease that causes pain, stiffness, and joint swelling. Here, we investigated the ameliorative effects of loganin on arthritis in vitro and in vivo. A single bioactive compound was fractionated and isolated from Cornus officinalis (CO) extract to screen for anti-arthritic effects. A single component, loganin, was identified as a candidate. The CO extract and loganin inhibited the expression of factors associated with cartilage degradation, such as cyclooxygenase-2 (COX-2), matrix metalloproteinase 3 (MMP-3), and matrix metalloproteinase 13 (MMP-13), in interukin-1 beta (IL-1β)-induced chondrocyte inflammation. In addition, prostaglandin and collagenase levels were reduced following treatment of IL-1β-induced chondrocytes with loganin. In the destabilization of the medial meniscus (DMM)-induced mouse model, loganin administration attenuated cartilage degeneration by inhibiting COX-2, MMP-3, and MMP-13. Transverse micro-CT images revealed that loganin reduced DMM-induced osteophyte formation. These results indicate that loganin has protective effects in DMM-induced mice. Full article
(This article belongs to the Special Issue Drug and Therapy for Osteoarthritis (OA))
Show Figures

Figure 1

12 pages, 3544 KiB  
Article
GSK5182, 4-Hydroxytamoxifen Analog, a New Potential Therapeutic Drug for Osteoarthritis
by Yunhui Min, Dahye Kim, Godagama Gamaarachchige Dinesh Suminda, Xiangyu Zhao, Mangeun Kim, Yaping Zhao and Young-Ok Son
Pharmaceuticals 2020, 13(12), 429; https://doi.org/10.3390/ph13120429 - 27 Nov 2020
Cited by 4 | Viewed by 2518
Abstract
Estrogen-related receptors (ERRs) are the first identified orphan nuclear receptors. The ERR family consists of ERRα, ERRβ, and ERRγ, regulating diverse isoform-specific functions. We have reported the importance of ERRγ in osteoarthritis (OA) pathogenesis. However, therapeutic approaches with ERRγ against OA associated with [...] Read more.
Estrogen-related receptors (ERRs) are the first identified orphan nuclear receptors. The ERR family consists of ERRα, ERRβ, and ERRγ, regulating diverse isoform-specific functions. We have reported the importance of ERRγ in osteoarthritis (OA) pathogenesis. However, therapeutic approaches with ERRγ against OA associated with inflammatory mechanisms remain limited. Herein, we examined the therapeutic potential of a small-molecule ERRγ inverse agonist, GSK5182 (4-hydroxytamoxifen analog), in OA, to assess the relationship between ERRγ expression and pro-inflammatory cytokines in mouse articular chondrocyte cultures. ERRγ expression increased following chondrocyte exposure to various pro-inflammatory cytokines, including interleukin (IL)-1β, IL-6, and tumor necrosis factor (TNF)-α. Pro-inflammatory cytokines dose-dependently increased ERRγ protein levels. In mouse articular chondrocytes, adenovirus-mediated ERRγ overexpression upregulated matrix metalloproteinase (MMP)-3 and MMP-13, which participate in cartilage destruction during OA. Adenovirus-mediated ERRγ overexpression in mouse knee joints or ERRγ transgenic mice resulted in OA. In mouse joint tissues, genetic ablation of Esrrg obscured experimental OA. These results indicate that ERRγ is involved in OA pathogenesis. In mouse articular chondrocytes, GSK5182 inhibited pro-inflammatory cytokine-induced catabolic factors. Consistent with the in vitro results, GSK5182 significantly reduced cartilage degeneration in ERRγ-overexpressing mice administered intra-articular Ad-Esrrg. Overall, the ERRγ inverse agonist GSK5182 represents a promising therapeutic small molecule for OA. Full article
(This article belongs to the Special Issue Drug and Therapy for Osteoarthritis (OA))
Show Figures

Graphical abstract

Review

Jump to: Research

15 pages, 3093 KiB  
Review
Orally Administered NSAIDs—General Characteristics and Usage in the Treatment of Temporomandibular Joint Osteoarthritis—A Narrative Review
by Marcin Derwich, Maria Mitus-Kenig and Elzbieta Pawlowska
Pharmaceuticals 2021, 14(3), 219; https://doi.org/10.3390/ph14030219 - 5 Mar 2021
Cited by 15 | Viewed by 4271
Abstract
Background: Temporomandibular joint osteoarthritis (TMJ OA) is a degenerative joint disease. The aim of this review was to present the general characteristics of orally administered nonsteroidal anti-inflammatory drugs (NSAIDs) and to present the efficacy of NSAIDs in the treatment of TMJ OA. [...] Read more.
Background: Temporomandibular joint osteoarthritis (TMJ OA) is a degenerative joint disease. The aim of this review was to present the general characteristics of orally administered nonsteroidal anti-inflammatory drugs (NSAIDs) and to present the efficacy of NSAIDs in the treatment of TMJ OA. Methods: PubMed database was analyzed with the keywords: “(temporomandibular joint) AND ((disorders) OR (osteoarthritis) AND (treatment)) AND (nonsteroidal anti-inflammatory drug)”. After screening of 180 results, 6 studies have been included in this narrative review. Results and Conclusions: Nonsteroidal anti-inflammatory drugs are one of the most commonly used drugs for alleviation of pain localized in the orofacial area. The majority of articles predominantly examined and described diclofenac sodium in the treatment of pain in the course of TMJ OA. Because of the limited number of randomized studies evaluating the efficacy of NSAIDs in the treatment of TMJ OA, as well as high heterogeneity of published researches, it seems impossible to draw up unequivocal recommendations for the usage of NSAIDs in the treatment of TMJ OA. However, it is highly recommended to use the lowest effective dose of NSAIDs for the shortest possible time. Moreover, in patients with increased risk of gastrointestinal complications, supplementary gastroprotective agents should be prescribed. Full article
(This article belongs to the Special Issue Drug and Therapy for Osteoarthritis (OA))
Show Figures

Figure 1

20 pages, 356 KiB  
Review
Comprehensive Review of Knee Osteoarthritis Pharmacological Treatment and the Latest Professional Societies’ Guidelines
by Dragan Primorac, Vilim Molnar, Vid Matišić, Damir Hudetz, Željko Jeleč, Eduard Rod, Fabijan Čukelj, Dinko Vidović, Trpimir Vrdoljak, Borut Dobričić, Darko Antičević, Martina Smolić, Mladen Miškulin, Damir Ćaćić and Igor Borić
Pharmaceuticals 2021, 14(3), 205; https://doi.org/10.3390/ph14030205 - 2 Mar 2021
Cited by 50 | Viewed by 9345
Abstract
Osteoarthritis is the most common musculoskeletal progressive disease, with the knee as the most commonly affected joint in the human body. While several new medications are still under research, many symptomatic therapy options, such as analgesics (opioid and non-opioid), nonsteroid anti-inflammatory drugs, symptomatic [...] Read more.
Osteoarthritis is the most common musculoskeletal progressive disease, with the knee as the most commonly affected joint in the human body. While several new medications are still under research, many symptomatic therapy options, such as analgesics (opioid and non-opioid), nonsteroid anti-inflammatory drugs, symptomatic slow-acting drugs in osteoarthritis, and preparations for topical administration, are being used, with a diverse clinical response and inconsistent conclusions across various professional societies guidelines. The concept of pharmacogenomic-guided therapy, which lies on principles of the right medication for the right patient in the right dose at the right time, can significantly increase the patient’s response to symptom relief therapy in knee osteoarthritis. Corticosteroid intra-articular injections and hyaluronic acid injections provoke numerous discussions and disagreements among different guidelines, even though they are currently used in daily clinical practice. Biological options, such as platelet-rich plasma and mesenchymal stem cell injections, have shown good results in the treatment of osteoarthritis symptoms, greatly increasing the patient’s quality of life, especially when combined with other therapeutic options. Non-inclusion of the latter therapies in the guidelines, and their inconsistent stance on numerous therapy options, requires larger and well-designed studies to examine the true effects of these therapies and update the existing guidelines. Full article
(This article belongs to the Special Issue Drug and Therapy for Osteoarthritis (OA))
14 pages, 824 KiB  
Review
Therapeutic Applications of Type 2 Diabetes Mellitus Drug Metformin in Patients with Osteoarthritis
by Parkyong Song, Ji Sun Hwang, Hyean Cheal Park, Keun Ki Kim, Hong-Joo Son, Yu-Jin Kim and Kwang Min Lee
Pharmaceuticals 2021, 14(2), 152; https://doi.org/10.3390/ph14020152 - 13 Feb 2021
Cited by 10 | Viewed by 3448
Abstract
Type 2 diabetes mellitus (T2DM) and osteoarthritis (OA) are common chronic diseases that frequently co-exist. The link between OA and T2DM is attributed to common risk factors, including age and obesity. Several reports suggest that hyperglycemia and accumulated advanced glycosylation end-products might regulate [...] Read more.
Type 2 diabetes mellitus (T2DM) and osteoarthritis (OA) are common chronic diseases that frequently co-exist. The link between OA and T2DM is attributed to common risk factors, including age and obesity. Several reports suggest that hyperglycemia and accumulated advanced glycosylation end-products might regulate cartilage homeostasis and contribute to the development and progression of OA. Metformin is used widely as the first-line treatment for T2DM. The drug acts by regulating glucose levels and improving insulin sensitivity. The anti-diabetic effects of metformin are mediated mainly via activation of adenosine monophosphate (AMP)-activated protein kinase (AMPK), which is an energy sensing enzyme activated directly by an increase in the AMP/ATP ratio under conditions of metabolic stress. Dysregulation of AMPK is strongly associated with development of T2DM and metabolic syndrome. In this review, we discuss common risk factors, the association between OA and T2DM, and the role of AMPK. We also address the adaptive use of metformin, a known AMPK activator, as a new drug for treatment of patients with OA and T2DM. Full article
(This article belongs to the Special Issue Drug and Therapy for Osteoarthritis (OA))
Show Figures

Figure 1

18 pages, 1834 KiB  
Review
Therapeutic Single Compounds for Osteoarthritis Treatment
by Hyemi Lee, Xiangyu Zhao, Young-Ok Son and Siyoung Yang
Pharmaceuticals 2021, 14(2), 131; https://doi.org/10.3390/ph14020131 - 6 Feb 2021
Cited by 13 | Viewed by 4659
Abstract
Osteoarthritis (OA) is an age-related degenerative disease for which an effective disease-modifying therapy is not available. Natural compounds derived from plants have been traditionally used in the clinic to treat OA. Over the years, many studies have explored the treatment of OA using [...] Read more.
Osteoarthritis (OA) is an age-related degenerative disease for which an effective disease-modifying therapy is not available. Natural compounds derived from plants have been traditionally used in the clinic to treat OA. Over the years, many studies have explored the treatment of OA using natural extracts. Although various active natural extracts with broad application prospects have been discovered, single compounds are more important for clinical trials than total natural extracts. Moreover, although natural extracts exhibit minimal safety issues, the cytotoxicity and function of all single compounds in a total extract remain unclear. Therefore, understanding single compounds with the ability to inhibit catabolic factor expression is essential for developing therapeutic agents for OA. This review describes effective single compounds recently obtained from natural extracts and the possibility of developing therapeutic agents against OA using these compounds. Full article
(This article belongs to the Special Issue Drug and Therapy for Osteoarthritis (OA))
Show Figures

Graphical abstract

Back to TopTop