Groenlandicine
CAS No. : 38691-95-1
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| Cat. No. : | HY-N6865 |
| M.Wt: | 322.34 |
| Formula: | C19H16NO4+ |
| Purity: | >98 % |
| Solubility: | DMSO : 1 mg/mL (ultrasonic;warming;heat to 60°C) |
Groenlandicine, a protoberberine alkaloid, is a cholinesterase inhibitor (AChE (IC50 = 0.54 μM), BChE (IC50 = 3.32 μM)). Groenlandicine non-competitively inhibits BACE1 (IC50 = 19.68 μM, Ki = 21.2) and inhibits RLAR (IC50 = 140.1 μM), HRAR (IC50 = 154.2 μM), and total ROS generation (IC50 = 51.78 μM) in vitro. Groenlandicine suppresses osteosarcoma cell proliferation while promoting apoptosis. Groenlandicine inhibits the tumor growth when combined with Cisplatin (HY-17394). Groenlandicine can be used for the study on osteosarcoma, Alzheimer's disease and diabetes mellitus [1][2][3][4][5].
IC50 & Target:IC50: 154.2 μM (HRAR)[1]
In Vitro:Groenlandicine (24 h) can reduce the expression level of TOP1 in osteosarcoma cells (OS cells) (SJSA-1 and MG63 cells) and promote cell apoptosis[1].
Groenlandicine (0-2 μM, 24 h) shows less sensitive to OS cells (SJSA-1 and MG63 cells) with up-regulated TOP1 and more sensitive to OS cells with down-regulated TOP1[1].
Groenlandicine (10 μM, 24 h) can inhibit the migration and proliferation of Cisplatin (HY-17394)-resistant osteosarcoma (SJSA-1/R and MG63/R) cells, promote their apoptosis, and the effect is more significant when combined with Cisplatin[1].
Groenlandicine (5-10 μM, 24 h) combined with cisplatin notably reduces Bcl-2 levels and activates BAX, cleaved-Caspase-3, and cleaved-Caspase-9 in cisplatin-resistant OS cells (SJSA-1/R and MG63/R), an effect inhibitable by SC79 (HY-18749)[1].
Groenlandicine (10-25 μg/mL, 24 h) significantly reduces peroxynitrite (ONOO-) formation, decreases DNA fragmentation, increases viability and causes G2/M phase arrest in SIN-1-treated LLC-PK1 cells[3].
Groenlandicine (40 μM) inhibits authentic ONOO- and total ROS generation, with IC50 values of 0.84 μM and 51.78 μM, respectively[3].
Groenlandicine (2.5-250 μM) induces topoisomerase I-mediated DNA cleavage in calf thymus topoisomerase I and pUL402 DNA reaction system in vitro[5].
In Vivo:Groenlandicine (1.5 mg/kg, i.p., every 3 days for 18 days) combined with Cisplatin can demonstrates excellent anti-tumor efficacy in SJSA-1/R xenograft model[1].
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