Porphyrin/Chlorin Derivatives as Promising Molecules for Therapy of Colorectal Cancer

Abstract

Colorectal cancer (CRC) is a leading cause of cancer-related death. The demand for new therapeutic approaches has increased attention paid toward therapies with high targeting efficiency, improved selectivity and few side effects. Porphyrins are powerful molecules with exceptional properties and multifunctional uses, and their special affinity to cancer cells makes them the ligands par excellence for anticancer drugs. Porphyrin derivatives are used as the most important photosensitizers (PSs) for photodynamic therapy (PDT), which is a promising approach for anticancer treatment. Nevertheless, the lack of solubility and selectivity of the large majority of these macrocycles led to the development of different photosensitizer complexes. In addition, targeting agents or nanoparticles were used to increase the efficiency of these macrocycles for PDT applications. On the other hand, gold tetrapyrrolic macrocycles alone showed very interesting chemotherapeutic activity without PDT. In this review, we discuss the most important porphyrin derivatives, alone or associated with other drugs, which have been found effective against CRC, as we describe their modifications and developments through substitutions and delivery systems.

Recent Photosensitizer Developments, Delivery Strategies and Combination‐based Approaches for Photodynamic Therapy†

“…The family of porphyrin derivatives includes PS such as TMPyP (36), chlorins (37), protoporphyrin IX (38) and phthalocyanines (39). Several recent reports on the literature have emphasized the necessity to increase their solubility to improve their PDT performance.…”

Real-Time Monitoring of Colorectal Cancer Location and Lymph Node Metastasis and Photodynamic Therapy Using Fucoidan-Based Therapeutic Nanogel and Near-Infrared Fluorescence Diagnostic–Therapy System

“…Using this system, diagnosis and treatment were simultaneously performed in the same optical path using 5-ALA [ 20 ], Ce6 [ 21 , 22 ], and CFN-gel [ 23 ]. Colorectal cancer cells [ 24 , 25 , 26 ] were selected to confirm the performance of the proposed system and CFN-gel developed in previous studies with a longer blood circulation time than conventional PSs. This is because it takes a lot of time from the indication of colorectal cancer to surgery, so diagnosis/treatment is possible only when the fluorescence accumulated during that time remains [ 27 , 28 ].…”

Cellular Localization of Selected Porphyrins and Their Effect on the In Vitro Motility of Human Colon Tumors and Normal Cells

“…This estimation indicates that the number of cases of colorectal cancer might even double by 2040 [ 14 ]. Despite the fact that colorectal cancer is located inside the human body, which makes it difficult for the delivery of light, there have been trials with porphyrin-based substances, which have given promising results, as photosensitizers in PDT [ 15 , 16 , 17 ]. Although the most efficient porphyrin-based photosensitizers lack coordinated metal ions, several metalloporphyrins (including, Zn, Pd, Sn, Ru, Gd and Al) have, however, been developed for clinical purposes.…”