| Description | Cassiaside B2 is an inhibitor of protein tyrosine phosphatase 1B (PTP1B) and human monoamine oxidase A (hMAO-A).Cassiaside B2 is an agonist of the 5-HT2C receptor with anti-allergic activity.Cassiaside B2 is one of the active ingredients in the naphthylpyrone reference extract (NRE). |
| In vitro | Rubrofusarin showed potent inhibition against the PTP1B enzyme (IC50; 16.95 ± 0.49 μM), and its glycosides reduced activity (IC50; 87.36 ± 1.08 μM for 1 and >100 μM for 2-4) than did the reference drug, ursolic acid (IC50; 2.29 ± 0.04 μM). Similarly, in hMAO-A inhibition, rubrofusarin displayed the most potent activity with an IC50 value of 5.90 ± 0.99 μM, which was twice better than the reference drug, deprenyl HCl (IC50; 10.23 ± 0.82 μM). An enzyme kinetic and molecular docking study revealed rubrofusarin to be a mixed-competitive inhibitor of both these enzymes. In a western blot analysis, rubrofusarin increased glucose uptake significantly and decreased the PTP1B expression in a dose-dependent manner in insulin-resistant HepG2 cells, increased the expression of phosphorylated protein kinase B (p-Akt) and phosphorylated insulin receptor substrate-1 (p-IRS1) (Tyr 895), and decreased the expression of glucose-6-phosphatase (G6Pase) and phosphoenol pyruvate carboxykinase (PEPCK), key enzymes of gluconeogenesis. |
| Target activity | MAO-A:40.57 µM |
| Synonyms | 决明子苷B2 |
| molecular weight | 920.82 |
| Molecular formula | C39H52O25 |
| CAS | 218155-40-9 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50mg/mL(54.30 mM), Sonication is recommended. |
| References | 1. Paudel P, et al. Rubrofusarin as a Dual Protein Tyrosine Phosphate 1B and Human Monoamine Oxidase-A Inhibitor: An in Vitro and in Silico Study.ACS Omega. 2019 Jul 3;4(7):11621-11630. 2. Kitanaka S, et al. Antiallergic agent from natural sources. Structures and inhibitory effect of histamine release of naphthopyrone glycosides from seeds of Cassia obtusifolia L. Chem Pharm Bull (Tokyo). 1998;46(10):1650-165 3. Yuen H, et al. Mechanisms of Action of Cassiae Semen for Weight Management: A Computational Molecular Docking Study of Serotonin Receptor 5-HT2C. Int J Mol Sci. 2020;21(4):1326. |