Rubropunctatin, an orange azaphilone pigment, is isolated from the extracts of Monascus pilosus-fermented rice (red-mold rice). Rubropunctatin has anti-inflammatory, immunosuppressive and antioxidative effects, and also exhibits anti-tumor activity[1][2][3].
Rubropunctatin (1.5-30 μM; 24 h) shows selective tumoricidal effect on the human gastric carcinoma BGC-823 cells and no significant toxicity toward normal epithelial cell GES-1[1].
Rubropunctatin (5-30 μM; 6-24 h) induces apoptosis in a dose- and time-dependent manner in BGC-823 cells[1].
Rubropunctatin (0.75-8.0 µg/ml) exhibits DDPH radical scavenging activity, inhibition of super oxide radical generation and ferric reducing activity[2].
Cell Viability Assay[1]
| Cell Line: | BGC-823 and GES-1cells |
| Concentration: | 1.5, 3, 6, 12, 15, 18, 30 μM |
| Incubation Time: | 24 hours |
| Result: | Decreased the viability of BGC-823 cells with an IC50 of 12.57 μM for 24 h. Did not show obvious cytotoxic effects on the normal cells. |
Cell Cycle Analysis[1]
| Cell Line: | BGC-823 cells |
| Concentration: | 0, 5, 10, 30 μM |
| Incubation Time: | 0, 6, 12, 24 hours |
| Result: | Increased the percentage of cells in sub-G1 phase in a dose- and time-dependent manner. |
Rubropunctatin (8-32 mg/kg; i.v. for 5 times) has anti-tumor effect mice[1].
Rubropunctamine inhibits 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation in mice, with an ID50 of 0.11 mg/ear[3].
| Animal Model: | Male nude mice (5 weeks) are inoculated with BGC-823 cells[1] |
| Dosage: | 8, 32 mg/kg |
| Administration: | I.v. five times (day 1st, 4th, 7th, 10th, and 13th) |
| Result: | Diminished the tumor volume by 11.1% (8 mg/kg) and 24.2% (32 mg/kg). Reduced the tumor weight by 23.5% (8 mg/kg) and 37.7% (32 mg/kg). No significant difference was observed on the body weight. |
[1]. Zheng Y, et, al. Anti-cancer effect of rubropunctatin against human gastric carcinoma cells BGC-823. Appl Microbiol Biotechnol. 2010 Nov;88(5):1169-77.
[2]. Dhale MA, et, al. Protective and antioxidative effect of rubropunctatin against oxidative protein damage induced by metal catalyzed reaction. Int J Biol Macromol. 2018 Sep;116:409-416.
[3]. Akihisa T, et, al. Azaphilones, furanoisophthalides, and amino acids from the extracts of Monascus pilosus-fermented rice (red-mold rice) and their chemopreventive effects. J Agric Food Chem. 2005 Feb 9;53(3):562-5.