Cephaeline
Cephaeline was highly active against protected primary CLL cells (relative IC50's 35 nM ) and acted by repressing HIF-1α and disturbing intracellular redox homeostasis.
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Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to
24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
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Leukemia. 2019 Jul 12.
Oxidative stress as candidate therapeutic target to overcome microenvironmental protection of CLL.[Pubmed:
31300746]
Chronic lymphocytic leukemia (CLL) cells depend on microenvironmental non-malignant cells for survival.
METHODS AND RESULTS:
We compared the transcriptomes of primary CLL cells cocultured or not with protective bone marrow stromal cells (BMSCs) and found that oxidative phosphorylation, mitochondrial function, and hypoxic signaling undergo most significant dysregulation in non-protected CLL cells, with the changes peaking at 6-8 h, directly before induction of apoptosis. A subset of CLL patients displayed a gene expression signature resembling that of cocultured CLL cells and had significantly worse progression-free and overall survival. To identify drugs blocking BMSC-mediated support, we compared the relevant transcriptomic changes to the Connectivity Map database. Correlation was found with the transcriptomic signatures of the cardiac glycoside ouabain and of the ipecac alkaloids emetine and Cephaeline. These compounds were highly active against protected primary CLL cells (relative IC50's 287, 190, and 35 nM, respectively) and acted by repressing HIF-1α and disturbing intracellular redox homeostasis. We tested emetine in a murine model of CLL and observed decreased CLL cells in peripheral blood, spleen, and bone marrow, recovery of hematological parameters and doubling of median survival (31.5 vs. 15 days, P = 0.0001).
CONCLUSIONS:
Pathways regulating redox homeostasis are thus therapeutically targetable mediators of microenvironmental support in CLL cells.
J Nat Prod. 2000 May;63(5):723-5.
Two Alangium alkaloids from Alangium lamarckii.[Pubmed:
10843602 ]
METHODS AND RESULTS:
Two new Alangium alkaloids, 1',2'-dehydrotubulosine (1) and alangine (2), were isolated from the dried fruits of Alangium lamarckii along with tubulosine (3), isotubulosine (4), deoxytubulosine, Cephaeline, isoCephaeline, psychotrine, neoCephaeline, 10-O-demethylCephaeline, 2'-N-(1"-deoxy-1" -beta-D-fructopyranosyl)Cephaeline, protoemetine, protoemetinol, salsoline, and alangiside.
CONCLUSIONS:
The structures of the new alkaloids (1 and 2) were determined by spectroscopic and chemical means.
