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Natural Product (NP) Details

General Information of the NP (ID: NP6740)
Name
Capsaicin
Synonyms
Capsaicin (transdermal patch formulation, neuropathic pain)
    Click to Show/Hide
Species Origin Capsicum annuum ...     Click to Show/Hide
Capsicum annuum
Kingdom: Viridiplantae
Phylum: Streptophyta
Class: Magnoliopsida
Order: Solanales
Family: Solanaceae
Genus: Capsicum
Species: Capsicum annuum
Disease Neuropathic pain [ICD-11: 8E43] Approved [1]
Structure
Click to Download Mol
2D MOL

3D MOL

    Click to Show/Hide the Molecular Information and External Link(s) of This Natural Product
Formula
C18H27NO3
PubChem CID
1548943
Canonical SMILES
CC(C)C=CCCCCC(=O)NCC1=CC(=C(C=C1)O)OC
InChI
1S/C18H27NO3/c1-14(2)8-6-4-5-7-9-18(21)19-13-15-10-11-16(20)17(12-15)22-3/h6,8,10-12,14,20H,4-5,7,9,13H2,1-3H3,(H,19,21)/b8-6+
InChIKey
YKPUWZUDDOIDPM-SOFGYWHQSA-N
CAS Number
CAS 404-86-4
Herb ID
HBIN019690
ETMC ID
3734
SymMap ID
SMIT00161
TCMSP ID
MOL002579
TTD Drug ID
D0U5CE
Combinatorial Therapeutic Effect(s) Validated Clinically or Experimentally
    α. A List of Drug(s) Whose Efficacy can be Enhanced by This NP
          3,3'-diindolylmethane      Breast cancer     Click to Show/Hide the Molecular Data of This Drug
                 Achieving Therapeutic Synergy     Click to Show/Hide
                    Representative Experiment Reporting the Effect of This Combination [2]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Molecule(s)
                    Regulation
Up-regulation Expression BAK  Molecule Info 
Pathway MAP
Up-regulation Expression BAX  Molecule Info 
Pathway MAP
Up-regulation Expression BBC3  Molecule Info 
Pathway MAP
Up-regulation Expression BID  Molecule Info 
Pathway MAP
Down-regulation Expression CDK4  Molecule Info 
Pathway MAP
Down-regulation Expression CDK6  Molecule Info 
Pathway MAP
Up-regulation Expression CDKN1A  Molecule Info 
Pathway MAP
Up-regulation Expression FAS  Molecule Info 
Pathway MAP
Up-regulation Expression IFI27  Molecule Info 
Pathway MAP
Up-regulation Expression p105  Molecule Info 
Pathway MAP
Up-regulation Expression TP53  Molecule Info 
Pathway MAP
                    In-vitro Model HCT 116 CVCL_0291 Colon carcinoma Homo sapiens
SW480 CVCL_0546 Colon adenocarcinoma Homo sapiens
LoVo CVCL_0399 Colon adenocarcinoma Homo sapiens
Caco-2 CVCL_0025 Colon adenocarcinoma Homo sapiens
HT-29 CVCL_0320 Colon adenocarcinoma Homo sapiens
                    Experimental
                    Result(s)
Capsaicin and DIM work synergistically to inhibit cell proliferation and induce apoptosis in colorectal cancer through modulating transcriptional activity of NF-kappaB, p53, and target genes associated with apoptosis.
          Erlotinib      Lung cancer     Click to Show/Hide the Molecular Data of This Drug
                 Augmenting Drug Sensitivity     Click to Show/Hide
                    Representative Experiment Reporting the Effect of This Combination [3]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Molecule(s)
                    Regulation
Down-regulation Phosphorylation AKT1  Molecule Info 
Pathway MAP
Down-regulation Expression ERCC1  Molecule Info 
Pathway MAP
                    In-vitro Model A-549 CVCL_0023 Lung adenocarcinoma Homo sapiens
NCI-H1975 CVCL_1511 Lung adenocarcinoma Homo sapiens
                    Experimental
                    Result(s)
Capsaicin enhances erlotinib-induced cytotoxicity via AKT inactivation and excision repair cross-complementary 1 (ERCC1) down-regulation in human lung cancer cells.
          TNF-related apoptosis inducing ligand      Lung cancer     Click to Show/Hide the Molecular Data of This Drug
                 Augmenting Drug Sensitivity     Click to Show/Hide
                    Representative Experiment Reporting the Effect of This Combination [4]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Molecule(s)
                    Regulation
Down-regulation Expression BIRC5  Molecule Info 
Pathway MAP
Down-regulation Expression CCNB1  Molecule Info 
Pathway MAP
Down-regulation Expression POLD1  Molecule Info 
Pathway MAP
Up-regulation Expression TRAIL-R2  Molecule Info 
Pathway MAP
                    In-vitro Model U-87MG ATCC CVCL_0022 Glioblastoma Homo sapiens
U-343MG CVCL_S471 Glioblastoma Homo sapiens
T98 CVCL_B368 Glioblastoma Homo sapiens
SNU-444 CVCL_5060 Glioblastoma Homo sapiens
U-251MG CVCL_0021 Astrocytoma Homo sapiens
                    Experimental
                    Result(s)
Capsaicin sensitizes malignant glioma cells to TRAIL-mediated apoptosis via DR5 upregulation and survivin downregulation.
          Sorafenib      Renal cell carcinoma     Click to Show/Hide the Molecular Data of This Drug
                 Achieving Therapeutic Synergy     Click to Show/Hide
                    Representative Experiment Reporting the Effect of This Combination [5]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Molecule(s)
                    Regulation
Up-regulation Expression BAX  Molecule Info 
Pathway MAP
Down-regulation Expression BCL-2  Molecule Info 
Pathway MAP
Up-regulation Expression CASP3  Molecule Info 
Pathway MAP
Down-regulation Expression EGFR  Molecule Info 
Pathway MAP
Up-regulation Expression PARP1  Molecule Info 
Pathway MAP
                    In-vitro Model LM3 CVCL_D269 Malignant neoplasms Mus musculus
Hep 3B2.1-7 CVCL_0326 Childhood hepatocellular carcinoma Homo sapiens
Huh-7 CVCL_0336 Adult hepatocellular carcinoma Homo sapiens
                    In-vivo Model Five-week-old BALB/C nude mice received a subcutaneous injection of 1*107 LM3 cells suspended in 100 uL sterile PBS into the right flank.
                    Experimental
                    Result(s)
Capsaicin and sorafenib combination treatment exerts synergistic anti-hepatocellular carcinoma activity by suppressing EGFR and PI3K/Akt/mTOR signaling.
          5-fluorouracil      Solid tumour/cancer     Click to Show/Hide the Molecular Data of This Drug
                 Achieving Therapeutic Synergy     Click to Show/Hide
                    Representative Experiment Reporting the Effect of This Combination [6]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Molecule(s)
                    Regulation
Up-regulation Phosphorylation AKT1  Molecule Info 
Pathway MAP
Down-regulation Expression ATG3  Molecule Info 
Pathway MAP
Down-regulation Expression BECN1  Molecule Info 
Pathway MAP
Up-regulation Expression MAP1LC3A  Molecule Info 
Pathway MAP
Up-regulation Phosphorylation S6K1  Molecule Info 
Pathway MAP
                    In-vitro Model QBC939 CVCL_6942 Cholangiocarcinoma Homo sapiens
SK-ChA-1 CVCL_6952 Cholangiocarcinoma Homo sapiens
Mz-ChA-1 CVCL_6932 Gallbladder carcinoma Homo sapiens
                    Experimental
                    Result(s)
Capsaicin enhances 5FU sensitivity of cholangiocarcinoma through the inhibition of 5FU-induced autophagy by activating the PI3K/AKT/mTOR pathway.
    β. A List of Drug(s) Whose Resistance can be Reversed by This NP
          Cisplatin      Bladder cancer     Click to Show/Hide the Molecular Data of This Drug
                 Reversing Drug Resistance     Click to Show/Hide
                    Representative Experiment Reporting the Effect of This Combination [7]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Molecule(s)
                    Regulation
Down-regulation Expression AURKA  Molecule Info 
Pathway MAP
Down-regulation Phosphorylation NFKBIA  Molecule Info 
Pathway MAP
                    Biological
                    Regulation
Induction Cell cycle arrest in G1/S phase
                    In-vitro Model SNU-1 CVCL_0099 Gastric adenocarcinoma Homo sapiens
SNU-5 CVCL_0078 Gastric adenocarcinoma Homo sapiens
SNU-16 CVCL_0076 Gastric adenocarcinoma Homo sapiens
SNU-601 CVCL_0101 Gastric adenocarcinoma Homo sapiens
SNU-638 CVCL_0102 Gastric adenocarcinoma Homo sapiens
SNU-668 CVCL_5081 Gastric adenocarcinoma Homo sapiens
                    Experimental
                    Result(s)
Capsaicin induces apoptosis of cisplatin-resistant stomach cancer cells by causing degradation of cisplatin-inducible Aurora-A protein.
Target and Pathway
Target(s) Transient receptor cation channel V1 (TRPV1)  Molecule Info  [8]
KEGG Pathway Neuroactive ligand-receptor interaction Click to Show/Hide
2 Inflammatory mediator regulation of TRP channels
NetPath Pathway IL2 Signaling Pathway Click to Show/Hide
Pathway Interaction Database Trk receptor signaling mediated by the MAPK pathway Click to Show/Hide
2 Trk receptor signaling mediated by PI3K and PLC-gamma
Reactome TRP channels Click to Show/Hide
References
Reference 1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2486).
Reference 2 Synergistic anticancer activity of capsaicin and 3,3'-diindolylmethane in human colorectal cancer. J Agric Food Chem. 2015 May 6;63(17):4297-304.
Reference 3 Capsaicin enhances erlotinib-induced cytotoxicity via AKT inactivation and excision repair cross-complementary 1 (ERCC1) down-regulation in human lung cancer cells. Toxicol Res (Camb). 2019 Mar 12;8(3):459-470.
Reference 4 Capsaicin sensitizes malignant glioma cells to TRAIL-mediated apoptosis via DR5 upregulation and survivin downregulation. Carcinogenesis. 2010 Mar;31(3):367-75.
Reference 5 Capsaicin and sorafenib combination treatment exerts synergistic anti?hepatocellular carcinoma activity by suppressing EGFR and PI3K/Akt/mTOR signaling. Oncol Rep. 2018 Dec;40(6):3235-3248.
Reference 6 Capsaicin Enhances the Drug Sensitivity of Cholangiocarcinoma through the Inhibition of Chemotherapeutic-Induced Autophagy. PLoS One. 2015 May 1;10(5):e0121538.
Reference 7 Capsaicin induces apoptosis of cisplatin-resistant stomach cancer cells by causing degradation of cisplatin-inducible Aurora-A protein. Nutr Cancer. 2011;63(7):1095-103.
Reference 8 Capsaicin receptor: TRPV1 a promiscuous TRP channel. Handb Exp Pharmacol. 2007;(179):155-71.
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Cite NPCDR
Visitor Map
Correspondence

X. N. Sun, Y. T. Zhang, Y. Zhou, X. C. Lian, L. L. Yan, T. Pan, T. Jin, H. Xie, Z. M. Liang, W. Q. Qiu, J. X. Wang, Z. R. Li, F. Zhu*, X. B. Sui*. NPCDR: natural product-based drug combination and its disease-specific molecular regulation. Nucleic Acids Research. 50(D1): 1324-1333 (2020). PMID: 34664659

Prof. Feng ZHU  (zhufeng@zju.edu.cn)

College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China


Prof. Xinbing SUI  (hzzju@hznu.edu.cn)

School of Pharmacy and Department of Medical Oncology, the Affiliated Hospital of Hangzhou Normal University, Hangzhou Normal University, Hangzhou, China