Groenlandicine
Based on 2 publication(s) in Google Scholar
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 .
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.72%
- CAS No.: 38691-95-1
- 화학식: C19H16NO4+
- 분자량:322.34
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보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Publications Citing Use of MedChemExpress (MCE) Groenlandicine
MoreAll Topoisomerase Isoforms
More
Biological Activity
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Topoisomerase I |
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.
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Cell Line:SJSA-1 and MG63 cells
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Concentration:0, 0.05 ,0.1 ,0.25 ,0.5 ,1, 2 μM
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Incubation Time:24 h
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Result:Showed IC50 values of 21.94 μM (EV1) and 111.3 μM (LV-TOP1) in SJSA-1 cells, 57.65 μM (EV1) and 181.3 μM (LV-TOP1) in MG63 cells, 37.93 μM (EV2) and 8.918 μM (sh-TOP1) in SJSA-1 cells, and 58.03 μM (EV2) and 11.47 μM (sh-TOP1) in MG63 cells.
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Cell Line:SJSA-1 and MG63 cells
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Concentration:5, 10 μM combined with Cisplatin (5 μM)
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Incubation Time:24 h
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Result:Decreased the level of TOP1 and Bcl-2.
Increased the level of BAX, cleaved-Caspase-3 and cleaved-Caspase-9.
Cannot reduce the expression of Bcl-2, nor can it activate BAX, cleaved-Caspase-3 and cleaved-Caspase-9 in the presence of SC79, but its down-regulating effect on TOP1 was not affected in the presence of SC79.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SJSA-1/R cells (5 × 106) were subcutaneously injected into 5-week-old BALB/c-nu nude mice[1]
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Dosage:1.5 mg/kg combined with Cisplatin (0.5 mg/kg)
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Administration:Intraperitoneal injection every 3 days for 18 days
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Result:Inhibited the growth of subcutaneous xenografts in nude mice.
Reduced tumor weight.
Down-regulated the level of TOP1 in tumors.
Showed low nephrotoxicity.
Chemical Information
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CAS No. 38691-95-1
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Appearance Solid
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분자량 322.34
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화학식 C19H16NO4+
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Color Orange to red
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SMILES
COC1=CC2=C(C=C1O)CC[N+]3=CC4=C(C=CC5=C4OCO5)C=C23
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Structure Classification
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Initial Source
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (2)
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Journal Impact Factor
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Most Recent
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Molecules
Discovery of Nine Dipeptidyl Peptidase-4 Inhibitors from Coptis chinensis Using Virtual Screening, Bioactivity Evaluation, and Binding Studies. [Abstract]2024 May 14;29(10):2304. PMID: 38792165 -
J Bone Oncol
Groenlandicine enhances cisplatin sensitivity in cisplatin-resistant osteosarcoma cells through the BAX/Bcl-2/Caspase-9/Caspase-3 pathway. [Abstract]2024 Aug 24:48:100631. PMID: 39263651
용액&용해도
DMSO : 1 mg/mL (3.10 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1023 mL | 15.5116 mL | 31.0231 mL | 77.5579 mL |
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