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使用碳点作为纳米载体评价百里香酚的抗风湿性质对弗氏完全佐剂诱导的关节炎大鼠的影响。

Evaluation of the anti-rheumatic properties of thymol using carbon dots as nanocarriers on FCA induced arthritic rats.

机构信息

Department of Biotechnology, Anna University, BIT-Campus, Tiruchirappalli 620 024, Tamil Nadu, India.

Department of Chemistry, B. S. Abdur Rahman Crescent Institute of Science and Technology, Vandalur, Chennai - 600 048, Tamil Nadu, India.

出版信息

Food Funct. 2021 Jun 8;12(11):5038-5050. doi: 10.1039/d1fo00471a.

Abstract

Rheumatoid Arthritis (RA) is an autoimmune disease that commences as inflammation and progressively destroys the articular joint. In this study, we assess the anti-rheumatic potential of the monoterpenoid class of thymol conjugated with Carbon Dots (CDs). Waste biomass in the form of dried rose petals was chosen as a precursor for the synthesis of CDs via a one-step hydrothermal bottom-up methodology. The prepared CDs exhibited absorption in the near-visible region, and unique excitation-dependent emission behaviour was confirmed from UV-Visible and fluorescence measurements. The surface morphology of CDs was confirmed by SEM and HR-TEM analysis to be quasi-spherical particles with an average size of ∼5-6 nm. The presence of various functional moieties (hydroxyl, carbonyl, and amino) was confirmed via FT-IR measurement. The graphitization of CDs was confirmed by the D and G bands for sp2 and sp3 hybridization, respectively, through Raman analysis. Esterification methodology was adopted to prepare the CDs-thymol conjugate and confirmed via FT-IR analysis. CDs play the role of a nanocarrier for thymol, an anti-arthritic agent. The bioactive compound of thymol showed potent anti-arthritic activity against RA targets through in silico docking studies. Further, the in vivo studies revealed that CDs-thymol conjugates (10 mg per kg body weight) showed a significant reduction in rat paw volume along with reduced levels of RF and CRP (2.23 ± 0.42 IU ml-1 and 16.96 ± 0.22 mg ml-1) when compared to the disease control rats. X-ray radiography and ultrasonic imaging revealed less bone destruction, joint derangement, and swelling in arthritis-induced Wistar rats. They could also potentially improve the Hb (14.14 ± 0.19), RBC (6.01 ± 0.11), PCV (6.01 ± 0.11) levels and elevate the status of antioxidant enzymes (GPx, SOD, MDA), and the activity was comparable to the standard drug, ibuprofen (10 mg kg-1), suggesting that the CDs-thymol conjugate at 10 mg kg-1 could act as a strong anti-arthritic agent. This work is evidence for the utilization of waste biomass as a value-added product such as a nanocarrier for biomedical applications.

摘要

类风湿关节炎(RA)是一种自身免疫性疾病,最初表现为炎症,随后逐渐破坏关节。本研究评估了与碳点(CDs)结合的单萜类百里酚的抗风湿潜力。我们选择干玫瑰花瓣形式的废物生物质作为通过一步水热自上而下方法合成 CDs 的前体。制备的 CDs 在近可见区域表现出吸收,并且通过紫外可见和荧光测量证实了独特的激发依赖性发射行为。通过 SEM 和 HR-TEM 分析证实了 CDs 的表面形态为具有平均尺寸约为 5-6nm 的准球形颗粒。通过 FT-IR 测量证实了各种官能团(羟基、羰基和氨基)的存在。通过拉曼分析分别确认 D 和 G 带对于 sp2 和 sp3 杂化的 CDs 的石墨化。通过酯化方法制备了 CDs-百里酚缀合物,并通过 FT-IR 分析进行了确认。CDs 充当百里酚的纳米载体,百里酚是一种抗关节炎药物。通过计算机对接研究,百里酚的生物活性化合物显示出针对 RA 靶标的有效抗关节炎活性。此外,体内研究表明,与疾病对照组大鼠相比,CDs-百里酚缀合物(每公斤体重 10mg)在大鼠爪体积减少以及 RF 和 CRP 水平降低(2.23±0.42IUml-1和 16.96±0.22mgml-1)方面表现出显著的降低。X 射线射线照相术和超声成像显示,关节炎诱导的 Wistar 大鼠的骨破坏、关节紊乱和肿胀减少。它们还可能潜在地提高 Hb(14.14±0.19)、RBC(6.01±0.11)、PCV(6.01±0.11)水平,并提高抗氧化酶(GPx、SOD、MDA)的状态,其活性与标准药物布洛芬(10mgkg-1)相当,表明 10mgkg-1 的 CDs-百里酚缀合物可以作为一种强大的抗关节炎药物。这项工作证明了废物生物质作为生物医学应用的纳米载体等增值产品的利用。

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