5-Aminolevulinic acid (hydrochloride)

5-Aminolevulinic acid (5-ALA; δ-Aminolevulinic acid; 5-Amino-4-oxopentanoic acid) hydrochloride is an orally active heme precursor. 5-Aminolevulinic acid hydrochloride promotes aerobic energy metabolism and increases ATP levels by enhancing the activity of cytochrome c oxidase. 5-Aminolevulinic acid hydrochloride enhances LPS-induced proinflammatory cytokine production and gene activation, and restores the phagocytic activity and ROS generation capacity of neutrophils. 5-Aminolevulinic acid hydrochloride selectively accumulates protoporphyrin IX in tumor cells; as a photosensitizer and radiosensitizer, it induces ROS burst upon light or X-ray irradiation to inhibit tumor growth. 5-Aminolevulinic acid hydrochloride can be applied to the research of septic shock, melanoma, and cancer radiotherapy^[1][2][3]. In Vitro:5-Aminolevulinic acid (hydrochloride) (100 μM; 24 h pre-treatment) significantly enhances LPS-induced expression of pro-inflammatory cytokine (Il1b, Il6, Tnfa) and mitochondrial (mt-Nd1, Pgc1a) genes in GM-CSF-differentiated bone marrow-derived cells from C57BL/6 mice^[2].
5-Aminolevulinic acid (hydrochloride) (0.1-100 μg/mL; 2-24 h) induces time- and concentration-dependent accumulation of porphyrins (predominantly PpIX) in B16-BL6 mouse melanoma cells in vitro^[3].
5-Aminolevulinic acid (hydrochloride) (1-100 μg/mL; 24 h prior to X-ray irradiation) enhances X-ray-induced intracellular reactive oxygen species generation in B16-BL6 mouse melanoma cells in vitro in a concentration-dependent manner, with significant increases observed at doses as low as 1 μg/mL under high X-ray exposure^[3]. In Vivo:Hydrochloride of 5-Aminolevulinic acid (10 mg/kg/day; p.o.; daily administration; for 15 consecutive weeks) increases liver mitochondrial COX activity by 1.5-fold, COX IV protein level by 1.6-fold, and liver ATP level by 1.6-fold in female C57BL/6N mice, without inducing toxicity^[1].
Hydrochloride of 5-Aminolevulinic acid (12 mg per mouse; p.o.; daily administration; for 2 consecutive weeks) fully restores the impaired neutrophil phagocytic activity and reactive oxygen species production in 5-ALA-deficient Alas1^± mice to wild-type levels^[2].
Hydrochloride of 5-Aminolevulinic acid (50 mg/kg; topical administration) significantly enhances the tumor inhibitory effect in the mouse B16-BL6 melanoma model, with no systemic toxicity observed^[3].