Groenlandicine 

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, K_i = 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]}.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

322.34

C₁₉H₁₆NO₄⁺

38691-95-1

Solid

Orange to red

COC1=CC2=C(C=C1O)CC[N+]3=CC4=C(C=CC5=C4OCO5)C=C23

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Zhao Z, et al. Groenlandicine enhances cisplatin sensitivity in cisplatin-resistant osteosarcoma cells through the BAX/Bcl-2/Caspase-9/Caspase-3 pathway. J Bone Oncol. 2024 Aug 24;48:100631.  [Content Brief]

  [2]. Jung HA, et al. Anti-Alzheimer and antioxidant activities of Coptidis Rhizoma alkaloids. Biol Pharm Bull. 2009 Aug;32(8):1433-8.  [Content Brief]

  [3]. Yokozawa T, et al. Protective role of Coptidis Rhizoma alkaloids against peroxynitrite-induced damage to renal tubular epithelial cells. J Pharm Pharmacol. 2005 Mar;57(3):367-74.  [Content Brief]

  [4]. Jung HA, et al. Inhibitory activities of the alkaloids from Coptidis Rhizoma against aldose reductase. Arch Pharm Res. 2008 Nov;31(11):1405-12.  [Content Brief]

  [5]. Kobayashi Y, et al. Inhibitors of DNA topoisomerase I and II isolated from the Coptis rhizomes. Planta Med. 1995 Oct;61(5):414-8.  [Content Brief]