Drug Information

Drug (ID: DG00271) and It's Reported Resistant Information

• Name: Capsaicin
• Synonyms: Capsaicin (transdermal patch formulation, neuropathic pain)
• Indication:
  In total 1 Indication(s)
  General pain disorder [ICD-11: 8E43]; Approved; [1]
• Target: Transient receptor potential cation channel V1 (TRPV1); TRPV1_HUMAN; [1]
• Formula: C18H27NO3
• IsoSMILES: CC(C)/C=C/CCCCC(=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
• PubChem CID: 1548943
• ChEBI ID: CHEBI:3374
• TTD Drug ID: D0U5CE
• INTEDE ID: DR0268
• DrugBank ID: DB06774

Type(s) of Resistant Mechanism of This Drug

  IDUE: Irregularity in Drug Uptake and Drug Efflux

  MRAP: Metabolic Reprogramming via Altered Pathways

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-01: Infectious/parasitic diseases

Fungal infection [ICD-11: 1F29-1F2F]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Irregularity in Drug Uptake and Drug Efflux (IDUE)

Key Molecule: Pleiotropic ABC efflux transporter of multiple drugs (PDR5) [1]

• Sensitive Disease: Fungal infection [ICD-11: 1F29-1F2F]
• Molecule Alteration: Expression; Down-regulation
• Experimental Note: Discovered Using In-vivo Testing Model
• In Vitro Model: Saccharomyces cerevisiae S288C; 559292
• In Vitro Model: Yeast deletion strains; N.A.; Homo sapiens (Human); N.A.
• Experiment for Molecule Alteration: DNA sequencing assay
• Mechanism Description: Capsaicin does not affect the growth rate signicantly but increases the lag period, the addition of capsaicin increased the lag period, especially that of the YOR153W (PDR5, a multi-drug resistance transporter) deletion strain.

ICD-02: Benign/in-situ/malignant neoplasm

Tongue cancer [ICD-11: 2B62]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Metabolic Reprogramming via Altered Pathways (MRAP)

Key Molecule: AMP-activated kinase alpha-2 (PRKAA2) [2]

• Metabolic Type: Glucose metabolism
• Sensitive Disease: Tongue squamous cell carcinoma [ICD-11: 2B62.0]
• Molecule Alteration: Expression; Up-regulation
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: mTOR signaling pathway; Activation; hsa04150
• Cell Pathway Regulation: AMPK signaling pathway; Activation; hsa04152
• Cell Pathway Regulation: Insulin signaling pathway; Activation; hsa04910
• In Vivo Model: Tumor xenograft model; Mice
• Experiment for Drug Resistance: Tumor weight assay
• Mechanism Description: Overall, combined treatment with capsaicin and cisplatin reversed cisplatin resistance by inhibiting the Warburg effect and facilitating mitochondrial-dependent apoptosis via the AMPK/AKT/mTOR axis.

Key Molecule: AMP-activated kinase alpha-2 (PRKAA2) [2]

• Metabolic Type: Glucose metabolism
• Sensitive Disease: Tongue squamous cell carcinoma [ICD-11: 2B62.0]
• Molecule Alteration: Expression; Up-regulation
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: mTOR signaling pathway; Activation; hsa04150
• Cell Pathway Regulation: AMPK signaling pathway; Activation; hsa04152
• Cell Pathway Regulation: Insulin signaling pathway; Activation; hsa04910
• In Vitro Model: CAL27 cells; Oral; Homo sapiens (Human); CVCL_1107
• Experiment for Drug Resistance: Cell viability assay
• Mechanism Description: Overall, combined treatment with capsaicin and cisplatin reversed cisplatin resistance by inhibiting the Warburg effect and facilitating mitochondrial-dependent apoptosis via the AMPK/AKT/mTOR axis.

References

• Ref 1: Studies on the antimicrobial mechanisms of capsaicin using yeast DNA microarray. Biosci Biotechnol Biochem. 2002 Mar;66(3):532-6. doi: 10.1271/bbb.66.532.
• Ref 2: Capsaicin reverses cisplatin resistance in tongue squamous cell carcinoma by inhibiting the Warburg effect and facilitating mitochondrial-dependent apoptosis via the AMPK/AKT/mTOR axis. Cell Biol Int. 2024 Aug;48(8):1097-1110.