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改良富含姜黄素提取物脂质体CRE-SD通过经典核因子κB信号通路抑制破骨细胞生成。

Modified Curcuminoid-Rich Extract Liposomal CRE-SDInhibits Osteoclastogenesis via the Canonical NF-κB Signaling Pathway.

作者信息

Jantarawong Sompot, Swangphon Piyawut, Lauterbach Natda, Panichayupakaranant Pharkphoom, Pengjam Yutthana

机构信息

Division of Biological Science, Faculty of Science, Prince of Songkla University, Songkhla 90110, Thailand.

Faculty of Medical Technology, Prince of Songkla University, Songkhla 90110, Thailand.

出版信息

Pharmaceutics. 2023 Aug 30;15(9):2248. doi: 10.3390/pharmaceutics15092248.

DOI:10.3390/pharmaceutics15092248
PMID:37765217
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10537735/
Abstract

Curcuminoids, namely curcumin, demethoxycurcumin, and bisdemethoxycurcumin, are the major active compounds found in L. (turmeric). Although their suppressive effects on bone resorption have been demonstrated, their pharmacokinetic disadvantages remain a concern. Herein, we utilized solid dispersion of a curcuminoid-rich extract (CRE), comprising such curcuminoids, to prepare CRE-SD; subsequently, we performed liposome encapsulation of the CRE-SD to yield liposomal CRE-SD. In vitro release assessment revealed that a lower cumulative mass percentage of CRE-SD was released from liposomal CRE-SD than from CRE-SD samples. After culture of murine RANKL-stimulated RAW 264.7 macrophages, our in vitro examinations confirmed that liposomal CRE-SD may impede osteoclastogenesis by suppressing p65 and IκBα phosphorylation, together with nuclear translocation and transcriptional activity of phosphorylated p65. Blind docking simulations showed the high binding affinity between curcuminoids and the IκBα/p50/p65 protein complex, along with many intermolecular interactions, which corroborated our in vitro findings. Therefore, liposomal CRE-SD can inhibit osteoclastogenesis via the canonical NF-κB signaling pathway, suggesting its pharmacological potential for treating bone diseases with excessive osteoclastogenesis.

摘要

姜黄素类化合物，即姜黄素、去甲氧基姜黄素和双去甲氧基姜黄素，是姜黄中发现的主要活性化合物。尽管它们对骨吸收的抑制作用已得到证实，但其药代动力学方面的缺点仍然令人担忧。在此，我们利用富含姜黄素类化合物的提取物（CRE）的固体分散体来制备CRE-SD；随后，我们对CRE-SD进行脂质体包封，得到脂质体CRE-SD。体外释放评估显示，与CRE-SD样品相比，脂质体CRE-SD释放的CRE-SD累积质量百分比更低。在对小鼠RANKL刺激的RAW 264.7巨噬细胞进行培养后，我们的体外实验证实，脂质体CRE-SD可能通过抑制p65和IκBα磷酸化以及磷酸化p65的核转位和转录活性来阻碍破骨细胞生成。分子对接模拟显示姜黄素类化合物与IκBα/p50/p65蛋白复合物之间具有高结合亲和力，以及许多分子间相互作用，这证实了我们的体外研究结果。因此脂质体CRE-SD可通过经典的NF-κB信号通路抑制破骨细胞生成，表明其在治疗破骨细胞生成过多的骨疾病方面的药理学潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bac3/10537735/f62d8206cda8/pharmaceutics-15-02248-g010.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bac3/10537735/0ad2a4d651d7/pharmaceutics-15-02248-g008.jpg
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