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Characterization of lactoferrin receptor in brain endothelial capillary cells and mouse brain

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Journal of Biomedical Science

Summary

We present, herein, the evidence for lactoferrin (Lf) binding sites in brain endothelial capillary cells (BCECs) and mouse brain. The results from confocal microscopy showed the presence of Lf receptors on the surface of BCECs and the receptor-mediated endocytosis for Lf to enter the cells. Saturation binding analyses revealed that Lf receptors exhibited two classes of binding sites in BCECs (high affinity: dissociation constant (K d) = 6.77 nM, binding site density (B max) = 10.3 fmol bound/μg protein; low affinity: K d = 4815 nM, B max = 1190 fmol bound/μg protein) and membrane preparations of mouse brain (high affinity: K d = 10.61 nM, B max = 410 fmol bound/μg protein; low affinity: K d = 2228 nM, B max =  51641 fmol bound/μg protein). The distribution study indicated the effective uptake of 125I-Lf in brain after intravenous administration. The present study provides experimental evidence for the application of Lf as a novel ligand for brain targeting.

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Acknowledgment

This research was supported by the grant from National Natural Science Foundation of China (30400570).

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Authors and Affiliations

  1. Department of Pharmaceutics, School of Pharmacy, Fudan University, P.O. Box 130, 200032, Shanghai, China

    Rong-qin Huang, Wei-lun Ke, Ying-hua Qu, Jian-hua Zhu, Yuan-ying Pei & Chen Jiang

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  1. Rong-qin Huang
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  2. Wei-lun Ke
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  3. Ying-hua Qu
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  4. Jian-hua Zhu
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  5. Yuan-ying Pei
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  6. Chen Jiang
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Correspondence to Chen Jiang.

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Huang, Rq., Ke, Wl., Qu, Yh. et al. Characterization of lactoferrin receptor in brain endothelial capillary cells and mouse brain. J Biomed Sci 14, 121–128 (2007). https://doi.org/10.1007/s11373-006-9121-7

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  • DOI: https://doi.org/10.1007/s11373-006-9121-7

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