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. 2019 Dec 24;10(1):32. doi: 10.3390/biom10010032

Table 5.

Effect of catalpol in experimental models of cancer.

Experimental Model Dose and Duration Key Findings of Catalpol References

  • Human gastric cancer cells (MKN-45)

  • Athymic nude mice

 Catalpol (in vitro): 2.5, 5, 10, 20, 40, 80, or 160 µM for 24 h
Catalpol (in vivo): 10, 20, or 40 mg/kg, for 3 weeks

  • Reduced proliferation and migration of cancer cells (as shown by suppression of MMP-2, α-SMA, RhoA, ROCK1, and N-cadherin)

  • Induced apoptosis in cancer cells (as shown by elevation of apoptosis-associated markers, cleaved Caspase-3 and PARP

  • Prevented tumor growth in xenograft nude mice

 [75]
Human solid tumor cell lines (A2780, HBL-100, HeLa, SW1573, T-47D and WiDr) Catalpol: 1, 2, 3, or 5 µm for 24 h

  • Showed antiproliferative activity

  • Cell cycle arrest at G1 phase

  • Reduced expression of Cyclin D1

 [76]
Human non–small-cell lung cancer (NSCLC) cells- A549 cells

  • Significantly inhibited the TGF-β1-induced cell migration and invasion of A549 cells.

  • Attenuated MMP-2 and MMP-9 expression.

  • Significant attenuation of Smad2/3 activation and NF-κB signaling pathways induced by TGF-β1 in A549 cells

[77]
Human colorectal cancer cells (HCT116) Catalpol: 0, 25, 50, or 100 µg/mL for 48 h

  • Inhibited HCT116 cancer cell proliferation via the downregulation of the PI3K-Akt signaling pathway

  • Induced apoptosis of HCT116 cancer cells via increased activities of caspase-3 and caspase-9, and upregulation of microRNA-200 expression

 [78]

  • Colon cancer cells (CT26)

  • C57BL6 mice and SD rats

 Catalpol: 2.5, 5, 10, 20, 40, or 80 µM for 24 and 48 h

  • Inhibited proliferation and growth of CT26 cancer cells in vitro and in vivo

  • Suppressed tumor cell-induced vascularization of endothelial cells and rat aortic ring angiogenesis

  • Reduced expression of angiogenic markers, VEGF, VEGFR2, bFGF and HIF-1α in colon cancer tissues

  • Halted the expression of pro-inflammatory factors, IL-1β, IL-6, IL-8, COX-2, and iNOS

 [79]
Randomized, placebo-controlled parallel clinical study in patients that had undergone surgical resection for locally advanced colon adenocarcinoma (n = 345) Catalpol: 10 mg/kg twice daily for 12 weeks
Positive control: 5 mg/kg bevacizumab twice weekly for 12 weeks
Placebo group: no treatment

  • Reduced serum levels of CA 19-9, CEA, MMP-2, and MMP-9 (colon cancer biomarkers) compared to the placebo group

  • Reduced tumor recurrences and improvement in overall survival compared to the placebo and positive control group

 [80]
Human breast cancer cells (MCF-7) Catalpol: 0, 25, 50, or 100 µg/mL for 24, 48 and 72 h

  • Reduced proliferation and induced apoptosis in MCF-7 cancer cells

  • Reduced expression of the tumor invasion enzyme, MMP-16

  • Upregulated expression of microRNA-146a (reducing metastatic potential)

 [81]
Human osteosarcoma cancer cells (MG63 and U2OS) Catalpol: 20, 40, or 80 µm for 48 h

  • Reduced progression, viability and migration of osteosarcoma cells

  • Decreased expression of RACK1 and MMP-2 indicating cancer cell migration inhibition

  • Induced apoptosis in cancer cells as shown by improved cleavage of Caspase-8, Caspase-3, Caspase-9 and PARP

 [82]