Stellavato Antonietta, Restaino Odile Francesca, Vassallo Valentina, Cassese Elisabetta, Finamore Rosario, Ruosi Carlo, Schiraldi Chiara
Department of Experimental Medicine, Section of Biotechnology and Molecular Biology, University of Campania Luigi Vanvitelli, 80138 Naples, Italy.
Department of Public Health, School of Medicine and Surgery "Federico II" of Naples, A.O.U. Federico II of Naples, 80131 Naples, Italy.
Pharmaceutics. 2021 May 17;13(5):737. doi: 10.3390/pharmaceutics13050737.
The biological activity of chondroitin sulfate (CS) and glucosamine (GlcN) food supplements (FS), sold in USA against osteoarthritis, might depend on the effective CS and GlcN contents and on the CS structural characteristics. In this paper three USA FS were compared to two pharmaceutical products (Ph). Analyses performed by HPAE-PAD, by HPCE and by SEC-TDA revealed that the CS and GlcN titers were up to -68.8% lower than the contents declared on the labels and that CS of mixed animal origin and variable molecular weights was present together with undesired keratan sulfate. Simulated gastric and intestinal digestions were performed in vitro to evaluate the real CS amount that may reach the gut as biopolymer. Chondrocytes and synoviocytes primary cells derived from human pathological joints were used to assess: cell viability, modulation of the NF-κB, quantification of cartilage oligomeric matrix protein (COMP-2), hyaluronate synthase enzyme (HAS-1), pentraxin (PTX-3) and the secreted IL-6 and IL-8 to assess inflammation. Of the three FS tested only one (US FS1) enhanced chondrocytes viability, while all of them supported synoviocytes growth. Although US FS1 proved to be less effective than Ph as it reduced NF-kB, it could not down-regulate COMP-2; HAS-1 was up-regulated but with a lower efficacy. Inflammatory cytokines were markedly reduced by Ph while a slight decrease was only found for US-FS1.
在美国销售的用于对抗骨关节炎的硫酸软骨素(CS)和氨基葡萄糖(GlcN)食品补充剂(FS)的生物活性,可能取决于有效的CS和GlcN含量以及CS的结构特征。本文将三种美国FS与两种药品(Ph)进行了比较。通过高效阴离子交换色谱-脉冲安培检测(HPAE-PAD)、毛细管电泳(HPCE)和尺寸排阻色谱-多角度光散射(SEC-TDA)进行的分析表明,CS和GlcN的效价分别比标签上宣称的含量低达68.8%,并且混合动物来源且分子量可变的CS与不需要的硫酸角质素同时存在。进行了体外模拟胃和肠道消化,以评估可能作为生物聚合物到达肠道的实际CS量。使用源自人类病理关节的软骨细胞和滑膜细胞原代细胞来评估:细胞活力、核因子κB(NF-κB)的调节、软骨寡聚基质蛋白(COMP-2)、透明质酸合酶(HAS-1)、五聚素(PTX-3)的定量以及分泌的白细胞介素-6(IL-6)和白细胞介素-8(IL-8)以评估炎症。在所测试的三种FS中,只有一种(美国FS1)提高了软骨细胞活力,而所有FS都支持滑膜细胞生长。尽管美国FS1被证明比药品效果差,因为它降低了NF-κB,但它不能下调COMP-2;HAS-1被上调但效果较低。药品显著降低了炎性细胞因子,而仅在美国FS1中发现略有下降。