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氟代硼苯丙氨酸用于优化 BNCT:增强硼对热中子的氢散射吸收。

Fluorinated borono-phenylalanine for optimizing BNCT: Enhancing boron absorption against hydrogen scattering for thermal neutrons.

机构信息

Dipartimento di Fisica and NAST Centre, Università degli Studi di Roma "Tor Vergata", Rome, Italy.

National Research Council, Institute for Complex Systems (ISC), Rome, Italy.

出版信息

Med Phys. 2024 Jan;51(1):439-446. doi: 10.1002/mp.16802. Epub 2023 Nov 13.

Abstract

BACKGROUND

Boron-containing compounds, such as 4-borono-phenylalanine (BPA) are used as drugs for cancer treatment in the framework of Boron Neutron Capture Therapy (BNCT). Neutron irradiation of boron-rich compounds delivered to cancer cells triggers nuclear reactions that destroy cancer cells.

PURPOSE

We provide a modeling of the thermal neutron cross section of BPA, a drug used in Boron Neutron Capture Therapy (BNCT), to quantify the competing contributions of boron absorption against hydrogen scattering, for optimizing BNCT by minimizing the latter.

METHODS

We perform the experimental determination of the total neutron scattering cross section of BPA at thermal and epithermal neutron energies using neutron transmission measurements. We isolate the contribution related to the incoherent scattering by hydrogen atoms as a function of the neutron energy by means of the Average Functional Group Approximation, and we calculate the probability for a neutron of being absorbed as a function of the neutron energy both for BPA and for its variants where either one or all four aromatic hydrogen atoms are substituted by F, and both for the samples with natural occurrence or enriched concentration of B.

RESULTS

While referring to the already available literature for in vivo use of fluorinated BPA, we show that fluorine-rich variants of BPA increase the probability of neutrons being captured by the molecule. As the higher absorption efficiency of fluorinated BPA does not depend on whether the molecule is used in vivo or not, our results are promising for the higher efficiency of the boron neutron capture treatment.

CONCLUSIONS

Our results suggest a new advantage using fluorinated compounds for BNCT, in their optimized interaction with neutrons, in addition to their already known capability to be used for monitoring and pharmacokinetics studies using F-Nuclear Magnetic Resonance or in F-Positron Emission Tomography.

摘要

背景

含硼化合物,如 4-硼苯丙氨酸(BPA),在硼中子俘获治疗(BNCT)框架中被用作癌症治疗药物。将富含硼的化合物输送到癌细胞中进行中子辐照会引发核反应,从而破坏癌细胞。

目的

我们对硼中子俘获治疗(BNCT)中使用的药物 4-硼苯丙氨酸(BPA)的热中子截面进行建模,以量化硼吸收对氢散射的竞争贡献,从而通过最小化后者来优化 BNCT。

方法

我们通过中子透射测量,在热中子和超热中子能区对 BPA 的总中子散射截面进行实验测定。我们通过平均官能团近似,将与氢原子的非相干散射相关的贡献与作为中子能量的函数分离出来,并计算出 BPA 及其变体中一个或所有四个芳族氢原子被 F 取代时作为中子能量函数的被吸收概率,以及天然丰度或 B 富集浓度的样品。

结果

在参考已有文献中氟代 BPA 的体内应用时,我们表明富氟 BPA 变体增加了分子吸收中子的概率。由于富氟 BPA 的更高吸收效率不取决于该分子是否在体内使用,因此我们的结果对于硼中子俘获治疗的更高效率具有很大的应用前景。

结论

除了已知的用于使用 F-磁共振或 F-正电子发射断层扫描进行监测和药代动力学研究的能力之外,我们的结果表明,在硼中子俘获治疗中使用氟代化合物具有新的优势,因为它们与中子的优化相互作用,除了它们已经已知的能力之外。

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