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新型非甾体抗炎类药物的合成:以没食子酰基-β-谷甾醇为模型药物,以木质素为载体,以银为内核的载药纳米粒子。

Synthesis of novel nonsteroidal anti-inflammatory galloyl β-sitosterol-loaded lignin-capped Ag-based drug.

机构信息

Department of Biochemistry, Bahauddin Zakariya University, Multan, 60800, Pakistan.

HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, 75270, Pakistan.

出版信息

Inflammopharmacology. 2024 Apr;32(2):1333-1351. doi: 10.1007/s10787-023-01390-y. Epub 2023 Nov 23.

DOI:10.1007/s10787-023-01390-y
PMID:37994993
Abstract

Biocompatible anti-inflammatory lignin-capped Ag (LCAg) nanoparticles (NPs) were synthesized for the delivery of galloyl β-sitosterol (Galloyl-BS). β-Sitosterol (BS) is effective against inflammatory responses, like cancer-induced inflammations. BS was modified via gallic acid esterification to enhance its anti-inflammatory potential. LCAg NPs were synthesized by a green method and loaded with galloyl-BS. For comparison, pure BS was also loaded onto LCAg NPs in a separate assembly. The antioxidant potential of Galloyl-BS was greater (IC 177 µM) than pure BS. Materials were characterized by FT-IR, SEM, XRD, and Zeta potential. Using UV-Vis spectroscopy, drug release experiments were performed by varying pH, time, concentration, and temperature. Maximum drug release was observed after 18 h at pH 6 and 40 °C. Galloyl-BS showed improved drug loading efficiency, release %age, and antioxidant activity compared to pure BS when loaded onto LCAg NPs. DLCAg exhibited excellent anti-inflammatory activity in rat models. These findings indicate that galloyl-BS (drug)-loaded LCAg (DLCAg) NPs have the potential as an anti-inflammatory agent without any prior release and scavenging in normal cells.

摘要

生物相容型抗炎木质素封端银(LCAg)纳米粒子(NPs)被合成用于递送没食子酰基 β-谷甾醇(Galloyl-BS)。β-谷甾醇(BS)对炎症反应有效,如癌症引起的炎症。BS 通过没食子酸酯化进行修饰,以增强其抗炎潜力。LCAg NPs 通过绿色方法合成,并负载 Galloyl-BS。为了比较,纯 BS 也被分别组装到 LCAg NPs 上。Galloyl-BS 的抗氧化潜力更大(IC 177 µM)比纯 BS。材料通过傅里叶变换红外光谱(FT-IR)、扫描电子显微镜(SEM)、X 射线衍射(XRD)和 Zeta 电位进行了表征。通过紫外可见光谱,通过改变 pH 值、时间、浓度和温度进行了药物释放实验。在 pH 6 和 40°C 下 18 小时后观察到最大药物释放。与纯 BS 相比,当负载到 LCAg NPs 上时,Galloyl-BS 显示出更高的载药效率、释放百分比和抗氧化活性。DLCAg 在大鼠模型中表现出优异的抗炎活性。这些发现表明,载药 LCAg(DLCAg) NPs 有望成为一种抗炎剂,而不会在正常细胞中预先释放和清除。

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