Hypocrellin A

Hypocrellin A is a PKC inhibitor that exerts antidiabetic activity by reversing the effects of high glucose on endothelin (ET-1) expression. Hypocrellin A is also a photosensitizer for photodynamic therapy (PDT) with anticancer, antibacterial and antiviral activities, especially against human immunodeficiency virus (HIV). In addition, Hypocrellin-A also possesses anti-Leishmania activity (IC₅₀=0.27 μg/ml)^{[1][2][3][4][5][6][7][8][9]}. IC50 & Target:PKC^[1] In Vitro: Hypocrellin A (150 nM; 24 h) significantly reduces the release of VEGF and ET-1 from human umbilical vein endothelial cells (HUVECs) incubated in glucose (20 mM)^[1].
Hypocrellin A shows good activity against Candida albicans (IC₅₀=0.65 μg/ml) and moderates activity against Staphylococcus aureus, MRSA, Pseudomonas aeruginosa, and Mycobacterium intracellularis^[4].
Hypocrellin A (0.055-5.5 µM) loses the infectivity of both HIV-1 and VSV in a concentration-dependent manner when treats with 1 J/cm² white light^[5].
Hypocrellin A (5 µM; 6 h) increases the secretion of multiple anti-angiogenic factors in LN229 glioma, U937 macrophages and SVHCEC endothelial cells after photochemotherapy^[6].
Hypocrellin A (0.25-1 µM; 48 h) has a negative impact on cell viability, migration, invasion and apoptosis of three non-small cell lung cancer cells, H460, PC-9 and H1975^[8].
In Vivo: Hypocrellin A (2.5 and 5 mg/kg; i.p.; once every two days for fourteen days) inhibits tumor growth in a non-small cell lung cancer xenograft model mouse model^[8].