| Description: |
The biological screening of cycleanine and the root bark alkaloidal extract revealed potent antibacterial, antifungal, antiplasmodial, and cytotoxic activities. Cycleanine, like its isomer – tetrandrine isolated from T. subcordata, could be a potential new anti-ovarian cancer agent acting through the apoptosis pathway. It also shows antiplasmodial activities against Plasmodium falciparum 3D7 with IC50 values of 0.08 µM.Cycleanine may have anti-inflammatory activity. Cycleanine markedly inhibited Na(+),K(+)-ATPase activity with an IC(50) value of 6.2 x 10(-4)M. It slightly inhibited Mg(2+)-ATPase, H(+)-ATPase, and Ca(2+)-ATPase, it might interact with the enzyme in Na.E(1)-P form and prevents the reaction step from Na.E(1)-P to E(2)-P.
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| In vitro: |
| Planta Medica, 2016, 81(S 01):S1-S381. | | Cytotoxicity effects and apoptosis induction by cycleanine and tetrandrine.[Reference: WebLink] | Ovarian cancer remains one of the main causes of death in all gynecologic malignancies [1]. Natural products continue to be important sources of clinically approved anti-cancer drugs [2, 3]. Triclisia subcordata Oliv (Menispermeaceae) is a medicinal plant traditionally used for the treatment of various diseases [4], including cancer, in West Africa. This study aims to evaluate the in vitro anti-ovarian cancer activities of the crude extracts and the isolated components in T. subcordata.
METHODS AND RESULTS:
The ethanol extract of T. subcordata and its fractions (crude alkaloids) were screened for in vitro anti-ovarian cancer activities on Ovcar-8, Ovcar-4, A2780, and Igrov-1 ovarian cancer cell lines using the Sulforhodamine B assay method to measure cell growth. Bioassay-guided fractionation using silica gel column chromatography and HPLC were used to isolate the bioactive compound, whose identity and structure was identified by NMR and LC-MS techniques. Caspase and PARP cleavage assays were used to detect apoptotic activities. The effect of isolated pure compounds on cell cycle and apoptosis was analyzed by flow cytometry. The crude alkaloids showed the strongest activity in cell growth assays on A2780 and Ovcar-8 cell lines (IC50 < 2.4 µg/mL). A bisbenzylisoquinoline alkaloid-cycleanine was isolated using HPLC and identified by MS and NMR analyses. The IC50values of cycleanine and tetrandrine ranged from 7 to 14µM on A2780, Ovcar-8, Ovcar-4 and Igrov-1 ovarian cancer cell lines. The IC50 of cycleanine on human normal ovarian surface epithelial cells was 35 ± 1µM hinting at modest selectivity towards cancer cells. Both cycleanine and tetrandrine caused apoptosis as shown by activation of caspases 3/7 and cleavage of poly (ADP) ribose polymerase (PARP) to form PARP-I. The percentage of Ovcar-8 cells in subG1 phase increased after exposure of cycleanine and tetrandrine to cells for 48h compared to control.
CONCLUSIONS:
In conclusion, cycleanine, like its isomer – tetrandrine isolated from T. subcordata, could be a potential new anti-ovarian cancer agent acting through the apoptosis pathway.
| | Nat Prod Commun. 2015 Sep;10(9):1541-2. | | Anti-malarial Activity of Isoquinoline Alkaloids from the Stem Bark of Actinodaphne macrophylla.[Pubmed: 26594753] |
METHODS AND RESULTS:
Seven isoquinoline alkaloids isolated from the bark of Actinodaphne macrophylla in this study demonstrated in vitro antiplasmodial activities against Plasmodium falciparum 3D7 with IC50 values of 0.08 µM, 0.05 µM, 1.18 µM, 3.11 µM, 0.65 µM, 0.26 µM, and 1.38 µM for cycleanine, 10-demethylxylopinine, reticuline, laurotetanine, bicuculine, α-hydrastine and anolobine, respectively, which are comparable with the reference standard, chloroquine.
CONCLUSIONS:
10-Demethylxylopinine was found to be the most active of these compounds. | | J Ethnopharmacol. 2004 Aug;93(2-3):331-5. | | Antibacterial, antifungal, antiplasmodial, and cytotoxic activities of Albertisia villos[Pubmed: 15234773 ] | Albertisia villosa (Menispermaceae) is a subtropical medicinal plant that is widely used in traditional African medicines against various diseases.
METHODS AND RESULTS:
Three known bisbenzylisoquinoline alkaloids; cycleanine, cocsoline, and N-desmethylcycleanine have been identified. Cycleanine, the most abundant (85%) of all identified bisbenzylisoquinoline alkaloids, accounts for all of the activity of the crude drug. The biological screening of cycleanine and the root bark alkaloidal extract revealed potent antibacterial, antifungal, antiplasmodial, and cytotoxic activities.
CONCLUSIONS:
These results may partly explain and support the use of Albertisia villosa root barks for the treatment of malaria and other infectious diseases in traditional Congolese medicine. |
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