chondrocytes

BNTA is a potent extracellular matrix (ECM) modulator. In a rat model of arthritis, BNTA modulates arthritis by promoting the synthesis of cartilage structural molecules on chondrocytes through the induction of superoxide dismutase 3 (SOD3) and regulating chondrogenesis through superoxide anion elimination.

Amygdalin (Laetrile) has antifibrotic, antitumor, anti-inflammatory and analgesic effects, amygdalin joint HSYA could inhibit the degeneration of the endplate chondrocytes derived from intervertebral discs of rats induced by IL-1beta and better than the single use of Amygdalin or HSYA. Amygdalin induces apoptotic cell death in human DU145 and LNCaP prostate cancer cells by caspase-3 activation through down-regulation of Bcl-2 and up-regulation of Bax.

1. Monotropein (Monotropeine) has antinociceptive action. 2. Monotropein has anti-apoptosis and anti-catabolic activity in chondrocytes. 3. Monotropein has anti-inflammatory action by inhibition of the expressions of inflammatory mediators via NF-κB inactivation, and support its possible therapeutic role in colitis. 4. Monotrope ininhibit the expressions of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), tumor necrosis factor-α (TNF-α), and interleukin-1β (IL-1β) mRNA in LPS-induced RAW 264.7 macrophages.

RAD16-I hydrochloride is a self-assembling peptide with nanofibrous morphology that provides an optimal microenvironment for the proliferation and differentiation of human mesenchymal stem cells (hMSC) into chondrocytes. This peptide, known as RAD16-I, has been extensively studied and serves as a model to assess the amyloid-like staining properties of self-assembling peptide nanofibers (SAPNFs).

Vosoritide acetate (BMN 111) is an agonist of the natriuretic peptide receptor 2 (NPR2) that promotes bone growth by influencing chondrocyte proliferation and differentiation [1].

AB05831, also known as 2-Acetamido-1,2-dideoxynojirimycin, is a highly potent and specific inhibitor of beta-hexosaminidase. N-Acetyl-3-hexosaminidase (HEX) is a member of lysosomal hydrolases, which catalyzes hydrolysis of terminal, non-reducing N-acetyl-|3-D-glucosamine (GlcNAc) andN-acetyl-(3-D-galactosamine (GalNAc) residues in glycoproteins, gan-gliosides, and glycosaminoglycans (GAGs). HEX, released by chondrocytes into the extracellular compartment, promotes cartilage matrix degradation. Osteoarthritis patients have increased HEX activity in synovial fluid.

Tricetin is a flavonoid isolated from pomegranate.Tricetin is a potent competitive inhibitor of Keap1-Nrf2 protein-protein interaction (PPI) and protects Parkinson's disease patients from 6-OHDA-induced neurotoxicity by activating the Nrf2 HO-1 signaling pathway and blocking mitochondria-dependent apoptotic pathways.Tricetin Inhibits migration and expression of the indicator protease progerin-1 (PS-1) in nasopharyngeal carcinoma through the Akt GSK-1β pathway.Tricetin inhibits endothelial inflammation induced by oxidized LDL mediated by Egr-1, and protects rat chondrocytes from IL-1β-induced inflammation and apoptosis.Tricetin is an inhibitor of endothelial inflammation induced by oxidized LDL mediated by Egr-1 and protects against IL-1β-induced inflammation and apoptosis.

Caspase-3 7 inhibitor I is a potent and reversible inhibitor of caspase-3 and caspase-7, with Ki values of 60 and 170 nM, respectively. It effectively inhibits apoptosis in Jurkat cells and chondrocytes treated with Camptothecin.

BMP-4, a heparin-binding peptide, exhibits anti-inflammatory and anti-chondrogenic properties. In murine chondrocytes and macrophages, it effectively mitigates inflammation and alleviates symptoms of various arthritides by dose-dependently suppressing the expression of inflammatory proteins such as iNOS, COX2, IFN, and IL6 through modulation of the iNOS-IFN-IL6 signaling pathway.

Polygalacic acid (Virgaureagenin G) is a triterpenoid isolated from the root of Polygala tenuifolia Willd that inhibits MMP expression. Polygalacic acid (Virgaureagenin G) can significantly improve the responsiveness of the cholinergic system, such as decreased acetylcholinesterase (AChE) activity, increased choline acetyltransferase (ChAT) activity, and increased acetylcholine (ACh) levels in the hippocampus and frontal cortex. Polygalacic acid (Virgaureagenin G) can also inhibit IL-1β-induced Wnt β-catenin activation and mitogen-activated protein kinase (MAPK) signaling pathways in chondrocytes, and is used in osteoarthritis (OA) related research.

TIP39, a neuropeptide and an agonist for the parathyroid hormone receptor type 2 (PTH2R), effectively increases cAMP levels in COS-7 cells featuring recombinant PTH2R from humans or rats (EC50s = 0.5 and 0.8 nM, respectively), as well as in F-11 cells that naturally express PTH2R (EC50 = 1.15 nM). Furthermore, TIP39 at 1 nM halts the cell cycle at the G0/G1 phase and reduces Sox9 expression, a crucial regulator of cartilage differentiation, in CFK2 rat chondrocytes. Additionally, administering 100 pmol/animal of TIP39 reduces the immobility period in the forced swim test in mice, indicating a potential antidepressant effect.

SAP15 (Synthetic anti-inflammatory peptide 15) is a synthetic peptide composed of 15 amino acids, derived from human beta-defensin 3, with the ability to penetrate cells and mitigate intracellular inflammation. It achieves its anti-inflammatory effects by blocking the phosphorylation of HDAC5, which in turn reduces NF-κB p65 phosphorylation. In macrophages stimulated with LPS, SAP15 suppresses the phosphorylation of both HDAC5 and NF-κB p65, demonstrating potent anti-inflammatory actions. Furthermore, treatment with SAP15 in LPS-induced chondrocytes elevates aggrecan and type II collagen levels while reducing osteocalcin expression. This peptide is valuable for exploring inflammation regulation and the development of anti-inflammatory therapies in biomaterials.

Derazantinib Racemate (ARQ-087 Racemate) is the racemate of Derazantinib, an orally bioavailable, ATP-competitive tyrosine kinase inhibitor with potent activity against FGFR1 FGFR2 FGFR3 chondrocytes (IC50s: 4.5 nM 1.8 nM 4.5 nM).

Kartogenin (KGN) is an activator of the smad4 smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.

Indirubin-3′-oxime is an effective inhibitor of cyclin-dependent protein kinases, and may play an obligate role in neuronal apoptosis in Alzheimer's disease.