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Updated: Jul 10, 2026
In Vitro and In Vivo Evaluation of Photocontrolled Biologically Active Compounds - Potential Drug Candidates for Cancer Photopharmacology
Published on: September 29, 2023
Imaging Transmembrane Kinetics: An Asymmetric Phthalocyanine Enables Fast Cellular Entry and Golgi Targeting for
Bingyang Liu1,2, Yuanyuan Han3, Kuizhi Chen1
1Key Laboratory of Optoelectronic Science and Technology for Medicine of Ministry of Education, Fujian Provincial Key Laboratory of Advanced Materials Oriented Chemical Engineering, Fujian Normal University, Fuzhou, China.
Abstract:
Photodynamic therapy (PDT) is fundamentally limited by the difficulty of concurrently achieving efficient cellular uptake and precise organelle-specific localization of photosensitizers (PSs). To address this challenge, we designed an asymmetric silicon phthalocyanine, Chol-SiPc-PIP, through axial conjugation with cholesterol and piperazine groups, aiming to optimize its cellular pharmacokinetics. Combining advanced optical microscopy techniques, we investigated the cellular behavior of Chol-SiPc-PIP at high spatiotemporal resolution. Two-photon CLSM showed rapid uptake and Golgi accumulation in MCF-7 cells, while FCS revealed that the piperazine moiety accelerates membrane translocation, driving fast cellular entry. Benefiting from enhanced cellular uptake kinetics, precise Golgi targeting, and favorable photophysical properties, Chol-SiPc-PIP demonstrates superior in vitro photodynamic performance, showing an IC50 value as low as 98 nM with excellent biocompatibility. This study highlights how asymmetric molecules can be strategically engineered to control subcellular pharmacokinetics and organelle-level photodynamic activity, offering a cell-focused design paradigm for developing advanced PSs with translational potential.
