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Manzamine A hydrochloride

MCE China：Manzamine A hydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-117025A

CAS：104264-80-4

Synonyms：Keramamine A hydrochloride

Purity：99.66%

Storage：4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Manzamine A hydrochloride, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A hydrochloride targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A hydrochloride has antimalarial and anticancer activities. Manzamine A hydrochloride also shows potent activity against HSV-1.

In Vitro：Manzamine A (5-50 µM, 18 h) hydrochloride decreases tau phosphorylation, measured with ELISA[1]. Manzamine A (10 µM) hydrochloride inhibits yeast S. cerevisiae growth by 30%[2]. Manzamine A hydrochloride displays a few enlarged vacuoles in yeast[2]. Manzamine A (2.5-10 µM, 24 h) hydrochloride increases acidity in pancreatic cancer cells and non-malignant Vero cells[2]. Manzamine A (1 µM, 24 h) hydrochloride inhibits HSV-1 infection in SIRC cells[4]. Manzamine A hydrochloride shows antimalarial activity with an IC50 of 8.0 nM (D6 clone) and 11 nM (W2 clone)[5].

In Vivo：Manzamine A (50 and 100 mol/kg, p.o. or i.p.) hydrochloride inhibits the growth of the rodent malaria parasite Plasmodium berghei in infected mice[6]. Manzamine A (8 mg/kg, i.p., daily for 8 consecutive days) hydrochloride prolongs the survival of SW mice to 20 days[7].

IC50 & Target：GSK-3β 10.2 μM (IC50) Plasmodium CDK5 1.5 μM (IC50) vacuolar ATPases Malaria HSV-1

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References：

[1]. Hamann M, et al. Glycogen synthase kinase-3 (GSK-3) inhibitory activity and structure-activity relationship (SAR) studies of the manzamine alkaloids. Potential for Alzheimer's disease. J Nat Prod. 2007;70(9):1397-1405.  [Content Brief]

[2]. Kallifatidis G, et al. The marine natural product manzamine A targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells [published correction appears in Mar Drugs. 2014;12(4):2305-7]. Mar Drugs. 2013;11(9):3500-3516. Published 2013 Sep 17.  [Content Brief]

[3]. Winkler JD, et al. Antimalarial activity of a new family of analogues of manzamine A. Org Lett. 2006;8(12):2591-2594.  [Content Brief]

[4]. Palem JR, et al. Manzamine A as a novel inhibitor of herpes simplex virus type-1 replication in cultured corneal cells. Planta Med. 2011;77(1):46-51.  [Content Brief]

[5]. Wahba AE, et al. Structure-activity relationship studies of manzamine A: amidation of positions 6 and 8 of the beta-carboline moiety. Bioorg Med Chem. 2009 Nov 15;17(22):7775-82.  [Content Brief]

[6]. Donia M, et al. Marine natural products and their potential applications as anti-infective agents. Lancet Infect Dis. 2003 Jun;3(6):338-48.  [Content Brief]

[7]. El Sayed KA, et al. New manzamine alkaloids with potent activity against infectious diseases. J Am Chem Soc. 2001 Mar 7;123(9):1804-8.  [Content Brief]