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. 2021 May 11;17(8):2034–2049. doi: 10.7150/ijbs.59918

Table 2.

Role of TRPV1 in Proliferation.

Drug Dose (μM) Duration (h) Tissue/Cell Type Mechanism Outcomes Ref.
Human colorectal cancer HCT116 cells Overexpression of TRPV1 suppressed EGFR phosphorylation at Y1068 Proliferation ↓ 70
Trpv1 knockout mice TRPV1 knockout increased constitutive EGFR Y1068 phosphorylation and PCNA, c-Fos and c-Myc expression levels Proliferation ↑ 70
Human colorectal cancer HCT116 cells TRPV1 activation activates calpain and PTP1B, which dephosphorylates EGFR Proliferation ↓ 70
Human melanoma A2058 and A375 cells Overexpression of TRPV1 activated p53 and, subsequently, upregulated its downstream target genes p21, PUMA, and mdm2 to induce apoptosis Proliferation ↓ 71
Human pancreatic cancer cell line, PANC-1 Overexpression of TRPV1 downregulates EGFR levels by inducing EGFR ubiquitination and degradation Proliferation ↓ 72
Human skin A431 cells Overexpression of TRPV1 promotes EGFR ubiquitylation and lysosomal degradation Proliferation ↓ 73
Capsaicin 100 24 Human urothelial cancer RT4 cells Induced cell cycle arrest in G0/G1 phase and apoptosis by activating p53 to upregulate Fas/CD95 in TRPV1-overexpressing cells Proliferation ↓ 74
Capsaicin 50-400 24-48 Human renal carcinoma 786-O cells Activated p38 and JNK MAPK pathways to induce apoptosis Proliferation ↓ 75
Capsaicin 0.1-20 48 Human prostate tumor androgen-responsive LNCaP cells Activated PI3K and p44/42 MAPK pathways to suppress ceramide production and increased androgen receptor expression Proliferation ↑ 76
Capsaicin 15 96-120 Human ESCC cell lines Eca109 Proliferation ↑ 77
Capsaicin 100 24 Human hepatocellular carcinoma PLC/PRF/5 cells Induced apoptosis by increasing the phosphorylation level of ERK and attenuating STAT3 phosphorylation Proliferation ↓ 81
Capsaicin 20 36 Human prostate tumor androgen-resistant PC-3 cells Induced apoptosis by producing ROS originating from the mitochondria and decreasing perturbations in the inner transmembrane potential (△Ψm) independently of TRPV1 Proliferation ↓ 82
Capsaicin 100 24-72 Human pancreatic neuroendocrine tumor BON and QGP-1 cells Disrupted mitochondrial membrane potential and suppressed ATP synthesis to induce apoptosis Proliferation ↓ 83
Capsaicin 75 24/48 Human nasopharyngeal carcinoma CNE2 and SUNE1 cells Inhibited MKK3-induced p38 activation Proliferation ↓ 84
Capsaicin 3 48/96 Human breast carcinoma cell line MCF-7 cells Proliferation ↑ 90
Cannabidiol 10 48 Human breast carcinoma cell line MBA-MD-231 cells Induced apoptosis via activation of CB2 and TRPV1 to elevate reactive oxygen species Proliferation ↓ 78
Cannabidiol 10 24 Human colon adenocarcinoma cell line Caco-2 cells Reduced the phosphorylation level of Akt, which was dependent on TRPV1 and CB1 Proliferation ↓ 79
Noradrenaline 100 24 Human prostate tumor androgen-resistant PC-3 cells Activated both alpha 1D-AR and TRPV1 and, subsequently, elicited the PLC/PKC/ERK pathways Proliferation ↑ 80
Cannabigerol 10 24 Human colon adenocarcinoma cell line Caco-2 cells Stimulated ROS generation, increased CHOP expression level, and promoted apoptosis Proliferation ↓ 85
AEA 10 24-72 The murine neuroblastoma cell line N1E-115 Seemed to occur via a lipid raft-dependent mechanism Proliferation ↓ 86