Pheophorbide a is a chlorophyll-related compound studied for it’s anti-tumor & anti-cancer activity.
Pheophorbide-a has been used as a photosensitizer:
- for the photodynamic therapy (PDT) in oral cancer cell lines
- to test its effect on inducing oxidative stress and death in L. amazonensis
- to test its effect on the viability of HeLa cells
ChEBI: Pheophorbide a is a pheophorbide. It is a conjugate acid of a pheophorbide a(2-).
Pheophorbide-a, due to its photosensitizing effect, may serve as a promising bioactive compound to treat leishmaniasis. It is a metabolite of chlorophyll and possesses immunostimulation functionality. Pheophorbide-a is a photosensitizer for the photodynamic therapy. It is an ATP Binding Cassette Subfamily G Member 2 (ABCG2) transporter specific substrate. Overexpression of ATP-binding cassette (ABC) transporters in cancer cells is associated with the multidrug resistance phenotype.
Pheophorbide A-mediated photodynamic therapy (Pa-PDT) (10 mg/kg (i.v.) or 30 mg/kg (i.p.)) significantly inhibits tumor growth in C3H mouse model with subcutaneous injection of AT-84 cells[3].
| Animal Model: | Male immunocompetent C3H mouse (six-week-old, inoculated subcutaneously with AT-84 cells)[3] |
| Dosage: | 10 mg/kg intravenous (i.v.) or a 30 mg/kg intraperitoneal (i.p.) injection |
| Administration: | IV or IP; after 24 h, PDT was performed |
| Result: | Pa-PDT, especially i.v. Pa-PDT, significantly inhibited tumor growth up to 70%, while the i.p. Pa-PDT-induced inhibition was up to 43.4% relative to the control group at the end of period. |
This chlorophyll a degradation intermediate (MW = 579.68 g/mol; CAS 15664-29-6), which is identical to chlorophyll a, except for the absence of the latter’s magnesium ion and ester at the 17-position, is obtained by acid hydrolysis of chlorophyll a. Pheophorbide a inhibits acyl-CoA:cholesterol acyltransferase and magnesium protoporphyrin IX methyltransferase, acts as an endothelin receptor antagonist, and also induces apoptosis. Pheophorbide a is also as an anti-tumor promoter.
