Periplocin (PP) is a cardiotonic steroid isolated from Periploca forrestii (PF). Periplocin is the highest level of cardiotonic steroid included in PF. Periplocin has the potential to facilitate wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase. Periplocin (5 - 20 μM; 48 hours; L929 cells) treatment shows increased proliferation up to 131% at 20 μM. It increases phosphorylation of Src, ERK, PI3K and Akt at active sites in a dosedependent and time-dependent manner. Periplocin (5 - 20 μM; 48 hours) significantly promotes migration of fibroblast cell and increases collagen production in L929 fibroblast. Periplocin induces Na/KATPase mediates the activation of Src/ERK and PI3K/Akt pathways[1]. In addition, intraperitoneal injection (IP) of periplocin repressed the growth of hepatocellular carcinoma (HCC) in xenograft tumor model in mice[2]. Periplocin inhibits the proliferation of gastric cancer cells and induces apoptosis in vitro and in vivo, indicating its potential to be used as an antitumor drug[3]. Periplocin led to growth inhibition and apoptosis induction by changing the expression of death receptors and inducing DNA double strand breaks in SW-872 cells[4].
Periplocin/杠柳毒苷 细胞实验
Cell Line
Concentration
Treated Time
Description
References
NCM460
44.95 ± 3.59 μM
24 h
NCM460 cells showed higher tolerance to periplocin
Autophagy. 2023 Dec;19(12):3132-3150.
RKO
0.12 μM to 0.82 μM
24 h
Periplocin significantly inhibited CRC cell growth and induced apoptosis
Autophagy. 2023 Dec;19(12):3132-3150.
LOVO
0.12 μM to 0.82 μM
24 h
Periplocin significantly inhibited CRC cell growth and induced apoptosis
Autophagy. 2023 Dec;19(12):3132-3150.
HT29
0.12 μM to 0.82 μM
24 h
Periplocin significantly inhibited CRC cell growth and induced apoptosis
Autophagy. 2023 Dec;19(12):3132-3150.
SW620
0.12 μM to 0.82 μM
24 h
Periplocin significantly inhibited CRC cell growth and induced apoptosis
Autophagy. 2023 Dec;19(12):3132-3150.
HCT116
0.12 μM to 0.82 μM
24 h
Periplocin significantly inhibited CRC cell growth and induced apoptosis
Autophagy. 2023 Dec;19(12):3132-3150.
SW480
0.12 μM to 0.82 μM
24 h
Periplocin significantly inhibited CRC cell growth and induced apoptosis
Autophagy. 2023 Dec;19(12):3132-3150.
DLD-1
0.12 μM to 0.82 μM
24 h
Periplocin significantly inhibited CRC cell growth and induced apoptosis
Autophagy. 2023 Dec;19(12):3132-3150.
KYSE-150
50, 100, 200 ng/ml
24 h and 48 h
CPP alone or in combination with TRAIL could inhibit the proliferation of ESCC cells and induce apoptosis.
J Exp Clin Cancer Res. 2019 Dec 21;38(1):501.
YES-2
50, 100, 200 ng/ml
24 h and 48 h
CPP alone or in combination with TRAIL could inhibit the proliferation of ESCC cells and induce apoptosis.
J Exp Clin Cancer Res. 2019 Dec 21;38(1):501.
Eca-109
50, 100, 200 ng/ml
24 h and 48 h
CPP alone or in combination with TRAIL could inhibit the proliferation of ESCC cells and induce apoptosis.
J Exp Clin Cancer Res. 2019 Dec 21;38(1):501.
Peripheral blood lymphocytes (PBLs)
50, 100, 200, 400 ng/mL
72 h
Periplocin had no effect on the proliferation of PBLs
Drug Des Devel Ther. 2021 Mar 26;15:1333-1344.
Jurkat cells
50, 100, 200, 400 ng/mL
24, 48, 72 h
Periplocin significantly inhibited the proliferation of Jurkat cells in a dose- and time-dependent manner
Drug Des Devel Ther. 2021 Mar 26;15:1333-1344.
HuT 78 cells
50, 100, 200, 400 ng/mL
24, 48, 72 h
Periplocin significantly inhibited the proliferation of HuT 78 cells in a dose- and time-dependent manner
Drug Des Devel Ther. 2021 Mar 26;15:1333-1344.
MDCK-MDR1 cells
75 µM and 100 µM
120 min
Evaluate the permeability of Periplocin in MDCK-MDR1 cells, showing that P-gp is involved in the transport of Periplocin.
Drug Des Devel Ther. 2014 May 9;8:475-83.
MDCK cells
75 µM and 100 µM
120 min
Evaluate the permeability of Periplocin in MDCK cells, showing that Periplocin has weak permeability.
Drug Des Devel Ther. 2014 May 9;8:475-83.
Periplocin/杠柳毒苷 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
SW480 xenograft model
Intraperitoneal injection
15 mg/kg
Once daily for two weeks
Periplocin significantly inhibited the growth of CRC xenografts with minimal toxicity
Autophagy. 2023 Dec;19(12):3132-3150.
BALB/c nude mice
ESCC xenografted tumor
Intraperitoneal injection
0.09 mg and 0.36 mg
Every two days for 14 days
CPP alone or in combination with TRAIL showed significant anti-tumor activity in vivo.
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