Kartogenin is an inducer of cartilage-like tissue formation (EC50: 100nM) [1]. Kartogenin activates chondrogenesis and promotes cartilage matrix synthesis by regulating signaling pathways such as filaminA/CBFβ/RUNX1, Ihh, and TGF-β/Smad [2-3]. Kartogenin is commonly used to treat osteoarthritis and tendon repair [4].
In rabbit bone marrow stromal cells (BMSCs), Kartogenin (1nM–5µM; 3d) enhances cell proliferation and induces chondrogenic differentiation of stem cells in a concentration-dependent manner [5]. In rat cartilage-derived chondrogenic stem/progenitor cells (CSPCs), Kartogenin (10µM; 7d) promotes the proliferation of cell [6].
In surgically induced osteoarthritis mouse model, Kartogenin (1μM, 100μM; intra-articular injection; 4 weeks) prevents cartilage degradation and alleviates osteoarthritis progression in mice via the miR-146a/NRF2 axis [7]. In monoiodoacetate-induced osteoarthritis mouse model, Kartogenin (100μM; intra-articular injection; 14d) inhibits pain behavior, chondrocyte inflammation, and attenuates osteoarthritis progression in mice through induction of IL-10 [8].
References:
[1]. Johnson K A. A stem cell-based approach to cartilage repair[J]. Osteoarthritis and Cartilage, 2013, 21: S4.
[2]. Cai J, Zhang L, Chen J, et al. Kartogenin and its application in regenerative medicine[J]. Current medical science, 2019, 39(1): 16-20.
[3]. Bhuyan S, Swain S, Misra R D K, et al. Nanomedicine-Driven Approaches for Kartogenin Delivery: Advancing Chondrogenic Differentiation and Cartilage Regeneration in Tissue Engineering[J]. International Journal of Nanomedicine, 2025: 7443-7468.
[4]. Im G I. Application of kartogenin for musculoskeletal regeneration[J]. Journal of Biomedical Materials Research Part A, 2018, 106(4): 1141-1148.
[5]. Zhang J, Wang J H C. Kartogenin induces cartilage-like tissue formation in tendon–bone junction[J]. Bone research, 2014, 2(1): 1-10.
[6]. Liu T, Li X, Wang T, et al. Kartogenin mediates cartilage regeneration by stimulating the IL-6/Stat3-dependent proliferation of cartilage stem/progenitor cells[J]. Biochemical and Biophysical Research Communications, 2020, 532(3): 385-392.
[7]. Hou M, Zhang Y, Zhou X, et al. Kartogenin prevents cartilage degradation and alleviates osteoarthritis progression in mice via the miR-146a/NRF2 axis[J]. Cell death & disease, 2021, 12(5): 483.
[8]. Kwon J Y, Lee S H, Na H S, et al. Kartogenin inhibits pain behavior, chondrocyte inflammation, and attenuates osteoarthritis progression in mice through induction of IL-10[J]. Scientific reports, 2018, 8(1): 13832.
Kartogenin是软骨样组织形成的诱导剂（EC50: 100 nM） [1]。Kartogenin通过调节细丝蛋白A/CBFβ/RUNX1、Ihh和TGF-β/Smad等信号通路来激活软骨形成并促进软骨基质合成 [2-3]。Kartogenin常用于治疗骨关节炎和肌腱修复 [4]。
在兔骨髓基质细胞（BMSCs）中，Kartogenin（1nM-5µM；3d）以浓度依赖性方式增强细胞增殖并诱导干细胞向软骨形成分化 [5]。在大鼠软骨来源的软骨形成干细胞/祖细胞（CSPCs）中，Kartogenin（10µM；7d）促进细胞增殖 [6]。
在手术诱发的骨关节炎小鼠模型中，Kartogenin（1μM，100μM；关节内注射；4周）通过miR-146a/NRF2轴防止小鼠软骨退化并减轻骨关节炎进展 [7]。在单碘乙酸诱发的骨关节炎小鼠模型中，Kartogenin（100μM；关节内注射；14d）通过诱导IL-10抑制小鼠疼痛行为、软骨细胞炎症并减缓骨关节炎进展 [8]。