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Chondroitin sulfate (CS) being a natural glycosaminoglycan is found in the cartilage and extracellular matrix. It shows clinical benefits in symptomatic osteoarthritis (OA) of the finger, knee, hip joints, low back, facial joints and other diseases due to its anti-inflammatory activity. It also helps in OA by providing resistance to compression, ma...
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... The presence of sulfate groups provides this polysaccharide with a permanent negative charge, regardless of the pH of the environment. CS is one of the major structural components of animal cartilage, extracellular matrix (ECM), synovial fluid, and other animal connective tissues [10]. Due to the content and location of sulfate groups, there are several structural varieties of CS, which differ in their biological functions [11]. ...
Oil-core nanocapsules (NCs, also known as nanoemulsions) are of great interest due to their application as efficient carriers of various lipophilic bioactives, such as drugs. Here, we reported for the first time the preparation and characterization of NCs consisting of chondroitin sulfate (CS)-based shells and liquid oil cores. For this purpose, two amphiphilic CS derivatives (AmCSs) were obtained by grafting the polysaccharide chain with octadecyl or oleyl groups. AmCS-based NCs were prepared by an ultrasound-assisted emulsification of an oil phase consisting of a mixture of triglyceride oil and vitamin E in a dispersion of AmCSs. Dynamic light scattering and cryo-transmission electron microscopy showed that the as-prepared core–shell NCs have typical diameters in the range of 30–250 nm and spherical morphology. Since CS is a strong polyanion, these particles have a very low surface potential, which promotes their stabilization. The cytotoxicity of the CS derivatives and CS-based NCs and their impact on cell proliferation were analyzed using human keratinocytes (HaCaTs) and primary human skin fibroblasts (HSFs). In vitro studies showed that AmCSs dispersed in an aqueous medium, exhibiting mild cytotoxicity against HaCaTs, while for HSFs, the harmful effect was observed only for the CS derivative with octadecyl side groups. However, the nanocapsules coated with AmCSs, especially those filled with vitamin E, show high biocompatibility with human skin cells. Due to their stability under physiological conditions, the high encapsulation efficiency of their hydrophobic compounds, and biocompatibility, AmCS-based NCs are promising carriers for the topical delivery of lipophilic bioactive compounds.
... Chondroitin sulfate (CS), a sulfated glycosaminoglycan, is primarily observed in the extracellular matrix of humans and other animal species, particularly within the connective tissue. 14,15 The crucial role of CS in the regulation of various diseases, encompassing osteoarthritis, 14,16 cardiovascular and cerebrovascular disorders, 17 central nervous system pathologies 18 and human cancers 19 has been previously reported. CS has been implicated in the modulation of immune responses and the inhibition of angiogenesis, thereby exerting potential anticancer effects. ...
Colorectal cancer (CRC) is a highly prevalent malignancy affecting the digestive system on a global scale. This study aimed to explore the previously unexplored role of CHPF in the progression of CRC. Our results revealed a significant upregulation of CHPF expression in CRC tumour tissues compared to normal tissues, with its levels correlating with tumour malignancy. In vitro experiments using CRC cell lines demonstrated that inhibiting CHPF expression suppressed cell proliferation, colony formation and cell migration, while promoting apoptosis. Conversely, overexpressing CHPF had the opposite effect. Additionally, our xenograft models in mice confirmed the inhibitory impact of CHPF knockdown on CRC progression using various cell models. Mechanistic investigations unveiled that CHPF may enhance VEGFB expression through E2F1‐mediated transcription. Functionally, suppressing VEGFB expression successfully mitigated the oncogenic effects induced by CHPF overexpression. Collectively, these findings suggest that CHPF may act as a tumour promoter in CRC, operating in a VEGFB‐dependent manner and could be a potential target for therapeutic interventions in CRC treatment.
... Osteoarthritis is a painful, disabling, and slowly developing degenerative disease that affects about 240 million people globally [1][2][3]. Chondroitin sulfate (CS) is a dominant family of sulfated linear polysaccharides that exist ubiquitously both on the cell surfaces and in the extracellular matrices of the human body [4][5][6]. Previous studies have indicated that CS is the most abundant structural component in the cartilage of the human joint tissues [4,7,8]. In this regard, following the recommendations of the European League Against Rheumatism (EULAR) and the European Society for Clinical and Economic Aspects of Osteoporosis, Osteoarthritis, and Musculoskeletal Diseases (ESCEO), CS has widely been used as a symptomatic slow-acting drug (SYSADOA) or a dietary supplement for the treatment and prevention of osteoarthritis [9,10]. ...
... Chondroitin sulfate (CS) is a dominant family of sulfated linear polysaccharides that exist ubiquitously both on the cell surfaces and in the extracellular matrices of the human body [4][5][6]. Previous studies have indicated that CS is the most abundant structural component in the cartilage of the human joint tissues [4,7,8]. In this regard, following the recommendations of the European League Against Rheumatism (EULAR) and the European Society for Clinical and Economic Aspects of Osteoporosis, Osteoarthritis, and Musculoskeletal Diseases (ESCEO), CS has widely been used as a symptomatic slow-acting drug (SYSADOA) or a dietary supplement for the treatment and prevention of osteoarthritis [9,10]. ...
Chondroitin sulfate (CS) has widely been used as a symptomatic slow-acting drug or a dietary supplement for the treatment and prevention of osteoarthritis. However, CS could not be absorbed after oral intake due to its polyanionic nature and large molecular weight. Gut microbiota has recently been proposed to play a pivotal role in the metabolism of drugs and nutrients. Nonetheless, how CS is degraded by the human gut microbiota has not been fully characterized. In the present study, we demonstrated that each human gut microbiota was characterized with a unique capability for CS degradation. Degradation and fermentation of CS by the human gut microbi-ota produced significant amounts of unsaturated CS oligosaccharides (CSOSs) and short-chain fatty acids. To uncover which microbes were responsible for CS degradation, we isolated a total of 586 bacterial strains with a potential CS-degrading capability from 23 human fecal samples. Bacteroides salyersiae was a potent species for CS degradation in the human gut microbiota and produced the highest amount of CSOSs as compared to other well-recognized CS-degraders, including Bacteroides finegoldii, Bacteroides thetaiotaomicron, Bacteroides xylanisolvens, and Bacteroides ovatus. Genomic analysis suggested that B. salyersiae was armed with multiple carbohydrate-active enzymes that could potentially degrade CS into CSOSs. By using a spent medium assay, we further demonstrated that the unsaturated tetrasaccharide (udp4) produced by the primary degrader B. salyersiae could serve as a "public goods" molecule for the growth of Bacteroides stercoris, a secondary CS-degrader that was proficient at fermenting CSOSs but not CS. Taken together, our study provides insights into the metabolism of CS by the human gut microbiota, which has promising implications for the development of medical and nutritional therapies for osteoarthritis.
... The marketed formulations were available in combination with the mentioned synergistic nutraceuticals. The products were marketed in India, United States, Europe and some other countries [61,62]. Chicory Cichorium intybus (Chicory) is a perennial herb. ...
The use of nutraceuticals and supplements are increasing day by day due to the drawbacks associated with synthetic drugs. Clinicians are aware of these therapies and prescribing the nutraceuticals in addition to the current choice of therapy. Many scientific studies, meta-analysis, randomised clinical trials have proved the effects of nutraceuticals in arthritis. Arthritis is the inflammatory disorder characterized by pain, swelling and stiffness of one or more joints. Two common types of arthritis are rheumatoid arthritis and osteoarthritis. The review covers all the possible nutraceuticals used in these two types of arthritis with their evidence and mechanism of action. Search engines like PubMed, Scopus, Google scholar, Researchgate and Science Direct are used to collect articles published from
... As one of the important components of cartilage, chondroitin sulfate attaches to proteins to form proteoglycans, endowing cartilage with strong compressive resistance and providing mechanical protection. 94 At the same time, it has also been reported to promote cell differentiation, 98 improve anti-inflammatory activity, 99 and aid cartilage recovery, 100 and has been manufactured as a dietary supplement, forming a method to improve and even treat osteoarthritis (OA). 6,99 Markel Lafuente-Merchan et al. added chondroitin sulfate to nanocellulose alginate saline gel to improve the rheological properties of bio-ink and improve the resolution and shape fidelity of scaffold printing: The viscosity of bio-inks increased somewhat with the addition of ChS. ...
Osteoarthritis caused by articular cartilage defects is a particularly common orthopedic disease that can involve the entire joint, causing great pain to its sufferers. A global patient population of approximately 250 million people has an increasing demand for new therapies with excellent results, and tissue engineering scaffolds have been proposed as a potential strategy for the repair and reconstruction of cartilage defects. The precise control and high flexibility of 3D printing provide a platform for subversive innovation. In this perspective, cartilage tissue engineering (CTE) scaffolds manufactured using different biomaterials are summarized from the perspective of 3D printing strategies, the bionic structure strategies and special functional designs are classified and discussed, and the advantages and limitations of these CTE scaffold preparation strategies are analyzed in detail. Finally, the application prospect and challenges of 3D printed CTE scaffolds are discussed, providing enlightening insights for their current research.
... Крім того, передбачається його вплив на субхондральну кістку за рахунок зниження резорбтивної активності в ній [34], а також ХС зменшує ядерну транслокацію NF-κB, що знижує утворення прозапальних цитокінів IL-1β і TNF-α і прозапальних ферментів, таких як ЦОГ-2 і NOS-2 [13]. Цей протизапальний засіб здатний стимулювати синтез протеогліканів і гіалуронової кислоти і одночасно інгібувати синтез протеолітичних ферментів і NF-κB, що сприяють пошкодженню хряща [1]. ...
Background. Osteoarthritis of the knee (OAK) causes severe pain and sometimes disability, which reduces the quality of life and work capacity of patients. Today, the prevalence of OAK is increases; therefore, the development of methods for its treatment and the use of means that slow down or stop the progression of OAK are relevant. Since OAK is a slowly progressive disease, the search for effective drugs with minimal toxicity and a long-lasting effect, which prevent the destruction of articular cartilage and improve the working conditions of the patient, is ongoing. Thus, the main goals of OAK treatment are to reduce symptoms and slow the progression of the disease, which can reduce the negative impact of OAK on the patient’s functional capacity, as well as improve quality of life. OAK is characterized by the progressive destruction of the articular cartilage, especially when it bears a load. In the joint, cartilage aggrecan is the main structural component that provides hydrophilicity and allows to withstand compression loads. Aggrecan is a complex of proteoglycans with hyaluronic acid and is characterized by a high content of chondroitin sulfate chains, while proteoglycan consists of protein and glycosaminoglycan chains (the precursor of the latter is glucosamine).
... Chondroitin sulphate is glycosaminoglycan that promotes the anabolism of chondrocytes, stimulates PG and hyaluronic acid synthesis and inhibits ECM degradation by enzymes, which contribute to relief of joint pain and improvement of joint function (137). ...
Knee osteoarthritis (KOA) is a common chronic articular disease worldwide. It is also the most common form of OA and is characterized by high morbidity and disability rates. With the gradual increase in life expectancy and ageing population, KOA not only affects the quality of life of patients, but also poses a burden on global public health. OA is a disease of unknown etiology and complex pathogenesis. It commonly affects joints subjected to greater loads and higher levels of activity. The knee joint, which is the most complex joint of the human body and bears the greatest load among all joints, is therefore most susceptible to development of OA. KOA lesions may involve articular cartilage, synovium, joint capsule and periarticular muscles, causing irreversible articular damage. Factors such as mechanical overload, inflammation, metabolism, hormonal changes and ageing serve key roles in the acceleration of KOA progression. The clinical diagnosis of KOA is primarily based on combined analysis of symptoms, signs, imaging and laboratory examination results. At present, there is no cure for KOA and the currently available therapies primarily focus on symptomatic treatment and delay of disease progression. Knee replacement surgery is typically performed in patients with advanced disease. The current study presents a review of epidemiological characteristics, risk factors, histopathological manifestations, pathogenesis, diagnosis, treatment modalities and progress in KOA research.
... CS is well known as a slow-acting drug for osteoarthritis and has been officially accepted by the World Health Organization/International League of Associations for Rheumatology Task Force in 1994. It is recommended at doses of approximately 1200-1600 mg/day for oral intake 55 . The dose of CS for the human body is in the range used in this study (approximately 0.9-90 mg/kg [0.01-1 mg/mL × approximately 90 mL/day] in rats vs. 17-22.8 ...
Although widespread pain, such as fibromyalgia, is considered to have a central cause, peripheral input is important. We used a rat repeated cold stress (RCS) model with many characteristics common to fibromyalgia and studied the possible involvement of decreased muscle pH in muscle mechanical hyperalgesia. After a 5-day RCS, the muscle pH and the muscular mechanical withdrawal threshold (MMWT) decreased significantly. Subcutaneously injected specific inhibitor of vacuolar ATPase (V-ATPase), bafilomycin A1, reversed both changes almost completely. It also reversed the increased mechanical response of muscle thin-fibre afferents after RCS. These results show that V-ATPase activation caused muscle pH drop, which led to mechanical hypersensitivity after RCS. Since extracellular matrix proteoglycan and acid sensitive ion channels (TRPV1 and ASIC3) have been considered as possible mechanisms for sensitizing/activating nociceptors by protons, we investigated their involvement. Manipulating the extracellular matrix proteoglycan with chondroitin sulfate and chondroitinase ABC reversed the MMWT decrease after RCS, supporting the involvement of the extracellular mechanism. Inhibiting ASIC3, but not TRPV1, reversed the decreased MMWT after RCS, and ASIC3 mRNA and protein in the dorsal root ganglia were upregulated, indicating ASIC3 involvement. These findings suggest that extracellular mechanism and ASIC3 play essential roles in proton-induced mechanical hyperalgesia after RCS.
... Крім того, хондроїтинсульфат позитивно впливає на субхондральну кістку за рахунок зниження її резорбтивної активності [36], зменшує ядерну транслокацію NF-κB, що знижує утворення прозапальних цитокінів IL-1β і TNF-аі ферментів (ЦОГ-2 та NOS-2) [10]. Цей препарат інгібує протеолітичні ферменти іNF-Κb, здатний стимулювати синтез протеогліканів та гіалуронової кислоти [4]. Отже, багатогранний механізм дії хондроїтинсульфату пояснює його сприятливий вплив на хрящ, синовіальну оболонку та субхондральну кістку. ...
... Тому комбінація НПЗЗ з хондропротекторами -найбільш ефективна терапія для цієї категорії пацієнтів. З аналізу сучасної літератури щодо лікування ОА видно, що лікарі часто застосовують глюкозамін сульфат і хондроїтинсульфат, але найбільш перспективним вважають перший [4]. Крім того, незважаючи на те, що тенденція вивчення хондроїтинсульфату була статичною протягом останнього десятиліття, особливо роль цього препарату у дослідженнях різко зросла за останні два роки через його величезну медичну цінність [38]. ...
Остеоартрит (ОА) є найбільш поширеним захворюванням суглобів та основною причиною порушення їх функції і інвалідності. Незважаючи на досягнення у вивченні патогенезу цього захворювання, лікування його досі залишається складним завданням. В наш час, як варіанти фармакологічного лікування ОА, для контролю болю та запалення застосовують нестероїдні протизапальні засоби (НПЗЗ), анальгетики, глюкокортикостероїди. Однак вони діють як симптоматичне лікування та мають високий ризик побічних ефектів Симптоматичні препарати повільної дії (SYSADOA) для лікування ОА не є швидкодіючими, такими як НПЗЗ і їхня клінічна ефективність щодо зменшення симптомів ОА може бути продемонстрована лише через кілька тижнів регулярного їх прийому. Проте при ОА вони не тільки зменшують біль у суглобах, а й уповільнюють прогресування захворювання. Одним із таких препаратів є хондроїтинсульфат – складний гетерогенний полісахарид, який має відмінний профіль безпеки. Саме хондроїтинсульфат і глюкозамін сульфатостаннім часом набули широкого використання як варіанти SYSADOA для лікування ОА. Вони діють як хондропротектори та/або як «ліки, що модифікують захворювання при ОА»,які полегшують біль та частково відновлюють функцію суглобів у пацієнтів з ОА, і таким чиномпроявляючи не лише симптоматичне лікування, а і вплив на патогенетичні ланки ОА. Хондроїтинсульфат знижує активність прозапальних цитокінів та фактору транскрипції, що беруть участь у запаленні. Глюкозамін сульфатпосилює специфічні компоненти матриксу хряща і запобігає дегенерації колагену в хондроцитах шляхом інгібування гідролітичних ферментів. Клінічні дослідження хондроїтинсульфату при лікуванні ОА показали, що він ефективний, безпечний та добре переноситься. Отже, використання препаратів SYSADOA знижує застосування кількості НПЗЗ при терапії ОА і, зменшує ризик розвитку побічної дії їх. Мета. Провести збір і аналіз літератури щодо терапевтичної ефективності симптоматичних препаратів повільної дії (SYSADOA) при лікуванні ОА. Методи. Пошук наукової інформації проведений в електронних базах PubMed, Google Scholar. Результати. Проведено огляд і аналіз літературищодотерапевтичної ефективності SYSADOA при лікуванні ОА. Висновки. Симптоматичні препарати повільної діїзменшують біль, скутість, функціональні обмеження при ОА та мають гарний профіль безпеки.
... CSA-SeNP can inhibit the degradation of aggrecan. Chondroitin sulfate is a kind of sulfated glycosaminoglycan with high biological activity which mainly exists in extracellular matrix (Bishnoi et al., 2016). Chondroitin sulfate has biological activities such as promoting cartilage regeneration, anti-oxidation, anti-fibrosis, and antiinflammation (Takeoka et al., 2021;Ustyuzhanina et al., 2018;Zhu et al., 2018). ...
Cartilage repair is a significant clinical issue due to its restricted ability to regenerate and self-heal after cartilage lesions or degenerative disease. Herein, a nano-elemental selenium particle (chondroitin sulfate A‑selenium nanoparticle, CSA-SeNP) is developed by the supramolecular self-assembly of Na2SeO3 and negatively charged chondroitin sulfate A (CSA) via electrostatic interactions or hydrogen bonds followed by in-situ reducing of l-ascorbic acid for cartilage lesions repair. The constructed micelle exhibits a hydrodynamic particle size of 171.50 ± 2.40 nm and an exceptionally high selenium loading capacity (9.05 ± 0.03 %) and can promote chondrocyte proliferation, increase cartilage thickness, and improve the ultrastructure of chondrocytes and organelles. It mainly enhances the sulfation modification of chondroitin sulfate by up-regulating the expression of chondroitin sulfate 4-O sulfotransferase-1, -2, -3, which in turn promotes the expression of aggrecan to repair articular and epiphyseal-plate cartilage lesions. The micelles combine the bio-activity of CSA with selenium nanoparticles (SeNPs), which are less toxic than Na2SeO3, and low doses of CSA-SeNP are even superior to inorganic selenium in repairing cartilage lesions in rats. Thus, the developed CSA-SeNP is anticipated to be a promising selenium supplementation preparation in clinical application to address the difficulty of healing cartilage lesions with outstanding repair effects.
