Arak Branch of Razi Vaccine and Serum Research Institute, Agricultural Research, Education and Extension Organisation (AREEO), Arak, Iran.
Department of Genetics, Faculty of Biological Sciences, Tarbiat Modares University, P.O. Box: 14115-154, Tehran, Iran.
BMC Complement Med Ther. 2024 Oct 2;24(1):350. doi: 10.1186/s12906-024-04634-8.
Nano-drug delivery systems have become a promising approach to overcoming problems such as low solubility and cellular uptake of drugs. Along with various delivery devices, dendrimers are widely used through their unique features. PEG-citrate dendrimers are biocompatible and nontoxic, with the ability to improve drug solubility. Curcumin, a naturally occurring polyphenol, has multiple beneficial properties, such as antiviral activities. However, its optimum potential has been significantly hampered due to its poor water solubility, which leads to reduced bioavailability. So, the present study attempted to address this issue and investigate its antiviral effects against HIV-1.
The G2 PEG-citrate dendrimer was synthesized. Then, curcumin was conjugated to it directly. FTIR, HNMR, DLS, and LCMS characterized the structure of products. The conjugate displayed an intense yellow color. In addition, increased aqueous solubility and cell permeability of curcumin were achieved based on flow cytometry results. So, it could be a suitable vehicle for improving the therapeutic applications of curcumin. Moreover, cell toxicity was assessed using XTT method. Ultimately, the SCR HIV system provided an opportunity to evaluate the level of HIV-1 inhibition by the curcumin-dendrimer conjugate using a p24 HIV ELISA kit.
The results demonstrated a 50% up to 90% inhibition of HIV proliferation at 12 μm and 60 μm, respectively. Inhibition of HIV-1 at concentrations much lower than CC50 (300 µM) indicates a high potential of curcumin-dendrimer conjugate against this virus.
Thereby, curcumin-dendrimer conjugate proves to be a promising tool to use in HIV-1 therapy.
纳米药物传递系统已成为克服药物低溶解度和细胞摄取等问题的有前途的方法。除了各种传递装置外，树枝状大分子因其独特的特性而得到广泛应用。PEG-柠檬酸树枝状大分子具有生物相容性和低毒性，能够提高药物的溶解度。姜黄素是一种天然存在的多酚，具有多种有益特性，如抗病毒活性。然而，由于其较差的水溶性导致生物利用度降低，其最佳潜力受到了显著限制。因此，本研究试图解决这一问题，并研究其对 HIV-1 的抗病毒作用。
合成了 G2 PEG-柠檬酸树枝状大分子。然后，直接将姜黄素与之偶联。FTIR、HNMR、DLS 和 LCMS 对产物的结构进行了表征。该偶联物呈现出强烈的黄色。此外，基于流式细胞术结果，姜黄素的水溶解度和细胞通透性得到了提高。因此，它可以作为一种合适的载体，以提高姜黄素的治疗应用。此外，使用 XTT 法评估细胞毒性。最终，SCR HIV 系统提供了一个机会，使用 p24 HIV ELISA 试剂盒评估姜黄素-树枝状大分子偶联物对 HIV-1 的抑制水平。
结果表明，在 12μm 和 60μm 时，HIV 增殖的抑制率分别高达 50%至 90%。在 CC50（300µM）以下的浓度下抑制 HIV-1 表明姜黄素-树枝状大分子偶联物对该病毒具有很高的潜力。
因此，姜黄素-树枝状大分子偶联物被证明是一种有前途的 HIV-1 治疗工具。
