1. Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR MAPK/ERK Pathway JAK/STAT Signaling Stem Cell/Wnt Apoptosis Autophagy
  2. Src PI3K JNK STAT EGFR Apoptosis Autophagy
  3. Peruvoside

Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib.

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Peruvoside Chemical Structure

Peruvoside Chemical Structure

CAS No. : 1182-87-2

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Description

Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib[1][2][3][4].

In Vitro

Peruvoside (50-1000 nM, 24 h) inhibits the viability and proliferation in PC9, PC9/gef, H3255, and H1975 cell lines[1].
Peruvoside (0.005-0.5 μM, 72 h) sensitizes A549, PC9/gef and H1975 to Gefitinib when in combination with Gefitinib (0.01~0.5 μM)[1].
Peruvoside (0-100 μM, 24 h) induces cell cycle arrest and apoptosis in MCF-7, HpG2, and A549 cells[2.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: PC9, PC9/gef, H3255, and H1975 cell lines
Concentration: 0, 0.01, 0.05, 0.1, 0.5, 1 μM
Incubation Time: 24, 48, 72, 96 h.
Result: Inhibited the viabilities of TKI-sensitive and TKI-resistant cell lines at all tested time points.
Inhibited the EGFR-mutant lung cancer cell viability and proliferation with 24 h IC50s of 48 nM, 74 nM, 67 nM, 143 nM, 277 nM and 428 nM for A549, PC9, PC9/gef, H3255, H1975 and BEAS-2B cells, respectively.
Significantly inhibited the proliferation of A549 (48, 72, and 96 h) and H3255 (24, 48, 72, and 96 h) lungcancer cells.

Cell Viability Assay[1]

Cell Line: A549, PC9/gef and H1975 cell lines
Concentration: 0.005, 0.0075, 0.01, 0.025, 0.05, 0.5 μM (in combination with 0.01, 0.05, 0.1, 0.25, 0.5 μM Gefitinib)
Incubation Time: 72 h.
Result: Had synergistic effects on A549 cells at the combination of 0.005, 0.075, or 0.01 μM and a low dose of gefitinib (0.01 or 0.05 μM).
Increased the sensitivity of PC9/gef and H1975 cells to Gefitinib at 0.025 or 0.05 μM.

Apoptosis Analysis[2]

Cell Line: MCF-7, A549 and HepG2 cell lines
Concentration: 0-100 μM
Incubation Time: 24 h
Result: Induced cell cycle arrest and apoptosis with lethal concentrations of IC50 for (MCF-7 - 100 nM), (A549 – 100 nM) and (HepG2 - 100 nM), respec-tively.
Arrested cell cycle at G0/G1 in MCF-7, A549 and HepG2 cells.
Significantly decreased the transcription of Chk1, Chk2, CDK6 and Cyclin D1 cell cycle genes in MCF-7, A549, and HepG2 cells.
In Vivo

Peruvoside (0.1 mg/kg for i.p; once daily for 28 days) suppresses the tumour growth in lung cancer mice model[1].
Peruvoside (0.59 mg/kg for i.p; once daily for 7 days) reduces mortality in EV-A71-infected mice model[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Lung cancer mouse model[1]
Dosage: 0.1 mg/kg
Administration: Intraperitoneal injection (i.p.); Once daily for 28 days
Result: Reduced the tumour size to 129.9 mm3, which was significantly smaller than the control group (348 mm3).
Significantly decreased levels of phosphorylated Src Y419 in tumour tissues compared with control tissues.
Animal Model: EV-A71-infected mice model[4]
Dosage: 0.59 mg/kg
Administration: Intraperitoneal injection (i.p.); Once daily for 7 days
Result: Substantially reduced clinical scores based on physical symptoms of body weight, activity,breathing, movement, and dehydration.
Showed about 6 log reduction in viral titre with 99.9% efficacy in inhibiting virus.
Molecular Weight

548.66

Formula

C30H44O9

CAS No.
SMILES

O=C[C@@]([C@](C1)([H])CC2)(CC[C@@H]1O[C@H](O[C@H]3C)[C@H]([C@@H]([C@H]3O)OC)O)[C@](CC[C@@]45C)([H])[C@]2([H])[C@]4(CC[C@@H]5C(CO6)=CC6=O)O

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Peruvoside
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HY-108016
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