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Cytotoxic indole alkaloids against human leukemia cell lines from the toxic plant Peganum harmala.

Wang C, Zhang Z, Wang Y, He X - Toxins (Basel) (2015)

Bottom Line: The cytotoxicity against human leukemia cells was assayed for the alkaloids and some of them showed potent activity.Harmalacidine (compound 8, HMC) exhibited the highest cytotoxicity against U-937 cells with IC50 value of 3.1 ± 0.2 μmol/L.The results strongly demonstrated that the alkaloids from Peganum harmala could be a promising candidate for the therapy of leukemia.

View Article: PubMed Central - PubMed

Affiliation: School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China. wangchunhua@whu.edu.cn.

ABSTRACT
Bioactivity-guided fractionation was used to determine the cytotoxic alkaloids from the toxic plant Peganum harmala. Two novel indole alkaloids, together with ten known ones, were isolated and identified. The novel alkaloids were elucidated to be 2-(indol-3-yl)ethyl-α-L-rhamnopyranosyl-(1 → 6)-β-D-glucopyranoside (2) and 3-hydroxy-3-(N-acetyl-2-aminoethyl)-6-methoxyindol-2-one (3). The cytotoxicity against human leukemia cells was assayed for the alkaloids and some of them showed potent activity. Harmalacidine (compound 8, HMC) exhibited the highest cytotoxicity against U-937 cells with IC50 value of 3.1 ± 0.2 μmol/L. The cytotoxic mechanism of HMC was targeting the mitochondrial and protein tyrosine kinase signaling pathways (PTKs-Ras/Raf/ERK). The results strongly demonstrated that the alkaloids from Peganum harmala could be a promising candidate for the therapy of leukemia.

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Alkaloids isolated from P. harmala.
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toxins-07-04507-f001: Alkaloids isolated from P. harmala.

Mentions: The chemical structures of compounds 1–12 are shown in Figure 1. They were classified as indole alkaloids.


Cytotoxic indole alkaloids against human leukemia cell lines from the toxic plant Peganum harmala.

Wang C, Zhang Z, Wang Y, He X - Toxins (Basel) (2015)

Alkaloids isolated from P. harmala.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4663518&req=5

toxins-07-04507-f001: Alkaloids isolated from P. harmala.
Mentions: The chemical structures of compounds 1–12 are shown in Figure 1. They were classified as indole alkaloids.

Bottom Line: The cytotoxicity against human leukemia cells was assayed for the alkaloids and some of them showed potent activity.Harmalacidine (compound 8, HMC) exhibited the highest cytotoxicity against U-937 cells with IC50 value of 3.1 ± 0.2 μmol/L.The results strongly demonstrated that the alkaloids from Peganum harmala could be a promising candidate for the therapy of leukemia.

View Article: PubMed Central - PubMed

Affiliation: School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China. wangchunhua@whu.edu.cn.

ABSTRACT
Bioactivity-guided fractionation was used to determine the cytotoxic alkaloids from the toxic plant Peganum harmala. Two novel indole alkaloids, together with ten known ones, were isolated and identified. The novel alkaloids were elucidated to be 2-(indol-3-yl)ethyl-α-L-rhamnopyranosyl-(1 → 6)-β-D-glucopyranoside (2) and 3-hydroxy-3-(N-acetyl-2-aminoethyl)-6-methoxyindol-2-one (3). The cytotoxicity against human leukemia cells was assayed for the alkaloids and some of them showed potent activity. Harmalacidine (compound 8, HMC) exhibited the highest cytotoxicity against U-937 cells with IC50 value of 3.1 ± 0.2 μmol/L. The cytotoxic mechanism of HMC was targeting the mitochondrial and protein tyrosine kinase signaling pathways (PTKs-Ras/Raf/ERK). The results strongly demonstrated that the alkaloids from Peganum harmala could be a promising candidate for the therapy of leukemia.

Show MeSH
Related in: MedlinePlus