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Pleiocarpa pycnantha leaves and its triterpenes induce apoptotic cell death in Caco-2 cells in vitro.

Omoyeni OA, Hussein A, Meyer M, Green I, Iwuoha E - BMC Complement Altern Med (2015)

Bottom Line: The exposure of an ethanolic extract from the leaves of P. pycnantha (0.1-1000 μg/ml) and the isolated compounds C2 and C3 (6,25-100 μg/ml) to human colorectal cancer cells reduced the cell viability with an IC50 > 100, 40.9, 36.3 μg/ml for P, C2 and C3 respectively, after 24 h of incubation.Caspase 3 was also activated which is a hallmark of apoptosis.A further study with other cell lines is also recommended.

View Article: PubMed Central - PubMed

Affiliation: Department of Chemistry, University of the Western Cape, Bellville, South Africa. nikxyglo@yahoo.com.

ABSTRACT

Background: Recently, we reported that the crude fractions and pure triterpenes; ursolic acid (C1), 27-E and 27-Z p-coumaric esters of ursolic acid (C2, C3), together with a new triterpene 2,3-seco-taraxer-14-en-2,3-lactone [pycanocarpine (C4)] and its hydrolysed derivative - (2,3-seco-taraxen-4-hydroxy-14-en-2-oic acid) [pycanocarpene (C5)] from Pleiocarpa pycnantha leaves inhibit cell proliferation. However, there has not been any specific report on the use of Pleiocarpa pycnantha leaves and its constituents to kill colorectal adenocarcinoma cancer CaCo-2 cells. We performed in vitro study to evaluate the cytotoxic properties of the ethanolic extract of P. pycnantha P, compounds C2 and C3. A preliminary study of the potential mechanisms were also undertaken.

Methods: Cell viability was measured by WST-1 assay. The Apoptosis level was evaluated by staining with APOPercentage(™) dye and the induction of caspases 3/7 and 9 using Caspase-Glo(®) assays.

Results: The exposure of an ethanolic extract from the leaves of P. pycnantha (0.1-1000 μg/ml) and the isolated compounds C2 and C3 (6,25-100 μg/ml) to human colorectal cancer cells reduced the cell viability with an IC50 > 100, 40.9, 36.3 μg/ml for P, C2 and C3 respectively, after 24 h of incubation. The APOPercentage(TM) assay also showed a considerable increase in the percentage of apoptotic cells after 24 h; (25-38% for P, 5-23% for C2 and 6-47 % for C3). Caspase 3 was also activated which is a hallmark of apoptosis.

Conclusion: These findings suggest that the P. pycnantha and the isolated compounds induce cell apoptosis in human colorectal adenocarcinoma cells. A further study with other cell lines is also recommended.

No MeSH data available.


Related in: MedlinePlus

Chemical structure of compounds C2 and C3 [12]
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Fig1: Chemical structure of compounds C2 and C3 [12]

Mentions: Fraction P12 (5.2 g) was further chromatographed on silica gel column using EtOAc/hexane (50:50–100:0) to afford sub-fraction A-H. The sub-fraction P12E (140 mg) was further purified on sephadex LH-20 column using DCM/MeOH(95:5) and HPLC (MeOH/H2O, 80:20) to afford compound C2 (5.5 mg) and C3 (7.3 mg); their chemical structures are illustrated in Fig. 1.Fig. 1


Pleiocarpa pycnantha leaves and its triterpenes induce apoptotic cell death in Caco-2 cells in vitro.

Omoyeni OA, Hussein A, Meyer M, Green I, Iwuoha E - BMC Complement Altern Med (2015)

Chemical structure of compounds C2 and C3 [12]
© Copyright Policy - open-access
Related In: Results  -  Collection

License 1 - License 2
Show All Figures
getmorefigures.php?uid=PMC4499947&req=5

Fig1: Chemical structure of compounds C2 and C3 [12]
Mentions: Fraction P12 (5.2 g) was further chromatographed on silica gel column using EtOAc/hexane (50:50–100:0) to afford sub-fraction A-H. The sub-fraction P12E (140 mg) was further purified on sephadex LH-20 column using DCM/MeOH(95:5) and HPLC (MeOH/H2O, 80:20) to afford compound C2 (5.5 mg) and C3 (7.3 mg); their chemical structures are illustrated in Fig. 1.Fig. 1

Bottom Line: The exposure of an ethanolic extract from the leaves of P. pycnantha (0.1-1000 μg/ml) and the isolated compounds C2 and C3 (6,25-100 μg/ml) to human colorectal cancer cells reduced the cell viability with an IC50 > 100, 40.9, 36.3 μg/ml for P, C2 and C3 respectively, after 24 h of incubation.Caspase 3 was also activated which is a hallmark of apoptosis.A further study with other cell lines is also recommended.

View Article: PubMed Central - PubMed

Affiliation: Department of Chemistry, University of the Western Cape, Bellville, South Africa. nikxyglo@yahoo.com.

ABSTRACT

Background: Recently, we reported that the crude fractions and pure triterpenes; ursolic acid (C1), 27-E and 27-Z p-coumaric esters of ursolic acid (C2, C3), together with a new triterpene 2,3-seco-taraxer-14-en-2,3-lactone [pycanocarpine (C4)] and its hydrolysed derivative - (2,3-seco-taraxen-4-hydroxy-14-en-2-oic acid) [pycanocarpene (C5)] from Pleiocarpa pycnantha leaves inhibit cell proliferation. However, there has not been any specific report on the use of Pleiocarpa pycnantha leaves and its constituents to kill colorectal adenocarcinoma cancer CaCo-2 cells. We performed in vitro study to evaluate the cytotoxic properties of the ethanolic extract of P. pycnantha P, compounds C2 and C3. A preliminary study of the potential mechanisms were also undertaken.

Methods: Cell viability was measured by WST-1 assay. The Apoptosis level was evaluated by staining with APOPercentage(™) dye and the induction of caspases 3/7 and 9 using Caspase-Glo(®) assays.

Results: The exposure of an ethanolic extract from the leaves of P. pycnantha (0.1-1000 μg/ml) and the isolated compounds C2 and C3 (6,25-100 μg/ml) to human colorectal cancer cells reduced the cell viability with an IC50 > 100, 40.9, 36.3 μg/ml for P, C2 and C3 respectively, after 24 h of incubation. The APOPercentage(TM) assay also showed a considerable increase in the percentage of apoptotic cells after 24 h; (25-38% for P, 5-23% for C2 and 6-47 % for C3). Caspase 3 was also activated which is a hallmark of apoptosis.

Conclusion: These findings suggest that the P. pycnantha and the isolated compounds induce cell apoptosis in human colorectal adenocarcinoma cells. A further study with other cell lines is also recommended.

No MeSH data available.


Related in: MedlinePlus