photosensitizer

Photosensitizer-3, a photosensitizer that generates single-linear oxygen upon near-infrared light excitation in combination with FAP, exhibited potent and selective killing of transfected HEK cells and affibody-targeted A431 cancer cells.

Type-I/-II Photosensitizer-1 (compound 8b) is a photosensitizer with anticancer properties. It exhibits significant phototoxicity against A549 and 4T1 tumor cells. Under laser irradiation, Type-I/-II Photosensitizer-1 demonstrates strong oxygen-independent antitumor activity with an IC50 ranging from 1.50 to 1.76 μM.

Photosensitizer-8 (Compound 4) is a derivative of 2-anthrol and serves as a photosensitizer activated by alkaline phosphatase (ALP). In the presence of ALP, it undergoes a phosphate ester hydrolysis reaction, rapidly converting into the active photosensitizer 2-anthrol. Upon irradiation, Photosensitizer-8 exhibits cytotoxicity against cancer cells with ALP overexpression, such as HeLa, A549, and HCT116, with IC50 values of 14.3 μM, 21.6 μM, and 17.5 μM respectively, while showing no significant cytotoxicity towards normal lung fibroblasts (WI-38) with IC50 ≥ 30 μM. Photosensitizer-8 is applicable in researching photodynamic therapy for cancers associated with ALP overexpression.

Photosensitizer-2 (compound 1), an organic D-π-A sensitizer, exhibits antitumor properties and potent phototoxicity due to an acrylic acid moiety. It demonstrates significant activity against HeLa cells, with IC 50 values of 20.9 ± 4.5 μM (dark) and 0.046 ± 0.012 μM (irradiation) [1].

Hematoporphyrin dihydrochloride (Hematoporphyrin IX dihydrochloride) is a substrate for affinity chromatography of heme-binding proteins.

Photosensitizer-7 is a photosensitizer (PS) that targets the endoplasmic reticulum (ER) with absorption and emission wavelengths at λab= 610 nm and λem= 622 nm, respectively. Under illumination, it shows an IC50 of 4.006 μM in HeLa cells and 3.28 μM in MCF-7 cells. Photosensitizer-7 is taken up by cells in a dose-dependent manner and primarily colocalizes with the ER. Light exposure induces dose-dependent intracellular ROS generation, reduces mitochondrial membrane potential, and increases apoptosis. Furthermore, Photosensitizer-7 significantly inhibits tumor growth in MCF-7 tumor-bearing mice, making it a valuable candidate for photodynamic anti-cancer research applications.

Photosensitizer-6 (Compound 4) is a metal ion complex that inhibits TrxR. It induces apoptosis in 4T1 cells, targeting cancer cells and eliminating tumors through chemophototherapy and immunogenic cell death under illumination. Additionally, Photosensitizer-6 can be utilized for tumor imaging.

Antitumor photosensitizer-5 (Ru2) is an effective photosensitizing agent that targets tumor mitochondria, with an IC50 of 0.3 μM for phototoxicity against A549 cells. Upon exposure to 460 nm light, it induces reactive oxygen species production and NADH depletion, leading to mitochondrial damage, caspase-3 activation, apoptosis induction, and inhibition of cell migration. Antitumor photosensitizer-5 shows potential for preventing malignant tumor growth and may be applicable in photodynamic therapy.

Antitumor photosensitizer-9 is a near-infrared photosensitizer (PS) with a high singlet oxygen production rate (relative rate = 1.79). It demonstrates significant phototoxicity against various cancer cells by inducing ROS generation under light exposure. In vivo, it inhibits tumor growth effectively and exhibits excellent anticancer photodynamic therapy (PDT) effects at low drug and light doses. Antitumor photosensitizer-9 is suitable for photodynamic therapy research.

Antimicrobial Photosensitizer-1 demonstrates significant potential as an effective agent for treating infections caused by pathogenic microorganisms, with notable antimicrobial efficacy observed in S. aureus-infected mouse wound models [1].

Antitumor Photosensitizer-3 (Compound I), a chlorin derivative, effectively induces apoptosis and necrosis in tumor cells upon exposure to 650 nm laser irradiation. This compound demonstrates reduced skin phototoxicity compared to the positive reference m-THPC in vivo [1].

Photosensitizer-1 (Compound CLB-13) is a photosensitizer [1] .

Photosensitizer-1 (Compound CLB-13) hydrochloride is a photosensitizer [1].

Antitumor Photosensitizer-4 (compound 10b), a conjugate of dasatinib and imatinib, serves as a potent tyrosine kinase inhibitor (TKI) targeting ABCG2. This photosensitizer (PS) induces apoptosis and reactive oxygen species (ROS) production, while demonstrating significant phototoxicity against both HepG2 and B16-F10 cells [1].

Compound Ru2 (Antitumor photosensitizer-6) exhibits synergistic type I/II photosensitization and photocatalytic activities under illumination at 595 nm. It causes oxidative redox imbalance within cells, affecting biosynthesis and metabolic processes, leading to cell apoptosis (Apoptosis). Compound Ru2 is applicable in studies of photodynamic therapy (PDT).

Antitumor photosensitizer-7 (compound 15), a photosensitizer possessing anti-cancer properties, demonstrates substantial cytotoxic effects on the G361 melanoma cell line when exposed to 414 nm blue light irradiation.

Verteporfin (BPD-MA) is a YAP inhibitor that inhibits YAP-TEAD interactions. Verteporfin is also a photosensitizer used in photodynamic therapy. Verteporfin also induces apoptosis and inhibits autophagy.

Pyridinium bisretinoid A2E (A2E) is a fluorescent chromophore isolated from lipofuscin in retinal pigment epithelium, a lipophilic cation and weak photosensitizer with cytotoxicity. A2E promotes apoptosis under blue light exposure and induces autophagy under photoactivation, damaging membrane integrity in a concentration-dependent manner.

PPA-904, a specific phenothiazine photosensitizer, is used in photodynamic therapy (PDT).

PPA-904 FA is a cationic photosensitizer with broad-spectrum antimicrobial activity for use in photodynamic studies (PDT) studies, which can be used to study chronic leg ulcers and diabetic foot ulcers.

Octocrylene (Octocrilene) is used as an ingredient in sunscreens and cosmetics. This organic compound can penetrate into the skin where it acts as a photosensitizer. This results in an increased production of free radicals under illumination.

Bithionol (Actamer), formerly marketed as an active ingredient in various topical drug products, was shown to be a potent photosensitizer with the potential to cause serious skin disorders. Approvals of the NDA's for bithionol drug products were withdrawn on October 24, 1967.

Chlorin E6 (CE6) is a second-generation photosensitizer with antitumor activity when used in combination with irradiation. In a mouse model of implanted fibrosarcoma, Chlorin E6 (2.5-10 mg/kg, i.v., 50-200 J/cm2 irradiation) resulted in complete tumor disappearance after varying degrees of irradiation. Agents including Chlorin E6 were tested in a Phase I clinical study in patients with early superficial squamous cell carcinoma of bronchial origin with favorable results (40 mg/m2, IV, 100 J/cm2 laser irradiation). In a Phase II clinical trial in patients with early stage lung cancer, the same mode of administration resulted in a complete response in 82.9% of patients. Chlorin E6 has been investigated as a nanotechnology drug delivery tool.

Methylene Violet 3RAX is a cationic dye, a potential photosensitizer in photodynamic therapy, with antitumor activity that alters the molecular structure of DNA, disrupts the modules of DNA, and induces the production of reactive monoclinic oxygen species, which are used to stain the mitochondria of cells.Methylene Violet 3RAX inhibits the subcellular localization of cancer cells by severing the Methylene Violet 3RAX inhibits subcellular localization of cancer cells, leading to cell death by cutting DNA strands in tumor cells.