Inhibition of HIV-1 infection with curcumin conjugated PEG-citrate dendrimer; a new nano formulation.

IF 3.3 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE BMC Complementary Medicine and Therapies Pub Date : 2024-10-02 DOI:10.1186/s12906-024-04634-8
Saeideh Ebrahimi, Majid Sadeghizadeh, Mohammad Reza Aghasadeghi, Mehdi Shafiee Ardestani, Shaghayegh Adib Amini, Roohollah Vahabpour
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Abstract

Background: 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.

Method: 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.

Results: 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.

Conclusion: Thereby, curcumin-dendrimer conjugate proves to be a promising tool to use in HIV-1 therapy.

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姜黄素共轭 PEG 柠檬酸树枝状聚合物抑制 HIV-1 感染;一种新型纳米配方。
背景:纳米给药系统已成为克服药物低溶解度和细胞吸收等问题的一种前景广阔的方法。树枝状聚合物以其独特的特性与各种给药装置一起被广泛应用。PEG 柠檬酸盐树枝状聚合物具有生物相容性和无毒性,能够提高药物的溶解度。姜黄素是一种天然多酚,具有多种有益特性,如抗病毒活性。然而,由于其水溶性较差,导致生物利用率降低,其最佳潜力受到严重阻碍。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:方法:合成 G2 PEG 柠檬酸盐树枝状聚合物。方法:合成 G2 PEG 柠檬酸盐树枝状聚合物,然后将姜黄素直接与之共轭。傅立叶变换红外光谱(FTIR)、核磁共振成像(HNMR)、荧光定量层析(DLS)和液相色谱(LCMS)对产物结构进行了表征。共轭物呈现浓黄色。此外,根据流式细胞术的结果,姜黄素的水溶性和细胞渗透性也得到了提高。因此,它可以作为一种合适的载体,改善姜黄素的治疗应用。此外,还使用 XTT 法评估了细胞毒性。最后,SCR HIV 系统为使用 p24 HIV 酶联免疫吸附试剂盒评估姜黄素-二聚体共轭物对 HIV-1 的抑制水平提供了机会:结果表明,在 12 μm 和 60 μm 浓度下,对 HIV 增殖的抑制率分别为 50%至 90%。在远低于 CC50(300 µM)的浓度下对 HIV-1 的抑制作用表明姜黄素-树枝状化合物共轭物对这种病毒具有很高的潜力:因此,姜黄素-树枝状聚合物共轭物被证明是一种很有希望用于治疗 HIV-1 的工具。
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来源期刊
BMC Complementary Medicine and Therapies
BMC Complementary Medicine and Therapies INTEGRATIVE & COMPLEMENTARY MEDICINE-
CiteScore
6.10
自引率
2.60%
发文量
300
审稿时长
19 weeks
期刊介绍:
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