Drug Information

Drug (ID: DG00026) and It's Reported Resistant Information

• Name: Silibinin
• Synonyms: Silibinin; Silybin; 22888-70-6; Flavobin; Silymarin I; Silybin A; Silybine; Silibinine; Silliver; Silibinin A; Silibininum; Silibinina; Flavobin Spofa; Silymarine I; Silibinin [INN]; Silymarine; Silibininum [INN-Latin]; Silibinine [INN-French]; Silibinina [INN-Spanish]; 7C3MT; UNII-33X338MNE4; EINECS 245-302-5; NSC 651520; Silimarin; Silibin; CHEBI:9144; 33X338MNE4; Silibinin (INN); NSC651520; C25H22O10; NCGC00091057-01; DSSTox_CID_6018; DSSTox_RID_77985; DSSTox_GSID_26018; (2R,3R)-3,5,7-trihydroxy-2-((2R,3R)-3-(4-hydroxy-
• Indication:
  In total 1 Indication(s)
  Liver disease [ICD-11: DB90-DB9Z]; Phase 2/3; [1]
• Formula: C25H22O10
• IsoSMILES: COC1=C(C=CC(=C1)[C@@H]2[C@H](OC3=C(O2)C=C(C=C3)[C@@H]4[C@H](C(=O)C5=C(C=C(C=C5O4)O)O)O)CO)O
• InChI: 1S/C25H22O10/c1-32-17-6-11(2-4-14(17)28)24-20(10-26)33-16-5-3-12(7-18(16)34-24)25-23(31)22(30)21-15(29)8-13(27)9-19(21)35-25/h2-9,20,23-29,31H,10H2,1H3/t20-,23+,24-,25-/m1/s1
• InChIKey: SEBFKMXJBCUCAI-HKTJVKLFSA-N
• PubChem CID: 31553
• ChEBI ID: CHEBI:9144
• TTD Drug ID: D02ADM
• VARIDT ID: DR00388
• DrugBank ID: DB09298

Type(s) of Resistant Mechanism of This Drug

  EADR: Epigenetic Alteration of DNA, RNA or Protein

  RTDM: Regulation by the Disease Microenvironment

Drug Resistance Data Categorized by Their Corresponding Diseases

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

Osteosarcoma [ICD-11: 2B51]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Epigenetic Alteration of DNA, RNA or Protein (EADR)

Key Molecule: hsa-mir-494 [1]

• Molecule Alteration: Expression; Up-regulation
• Sensitive Disease: Osteosarcoma [ICD-11: 2B51.0]
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: Cell apoptosis; Activation; hsa04210
• Cell Pathway Regulation: Cell proliferation; Inhibition; hsa05200
• In Vitro Model: MG63 cells; Bone marrow; Homo sapiens (Human); CVCL_0426
• Experiment for Molecule Alteration: qPCR
• Experiment for Drug Resistance: TUNEL cell apoptosis assay; XTT cell proliferation assay; MTT cell proliferation assay; Colony formation assay
• Mechanism Description: MMP-9 was targeted and negatively regulated by hsa-miR494 which inhibited cell proliferation and induced cell apoptosis. Silybin inhibited OS cell viability by altering the protein levels of beta-catenin and RUNX2, thus upregulating the level of hsa-miR494.

Regulation by the Disease Microenvironment (RTDM)

Key Molecule: Matrix metalloproteinase-9 (MMP9) [1]

• Molecule Alteration: Expression; Down-regulation
• Sensitive Disease: Osteosarcoma [ICD-11: 2B51.0]
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: Cell apoptosis; Activation; hsa04210
• Cell Pathway Regulation: Cell proliferation; Inhibition; hsa05200
• In Vitro Model: MG63 cells; Bone marrow; Homo sapiens (Human); CVCL_0426
• Experiment for Molecule Alteration: qPCR; Western blot analysis
• Experiment for Drug Resistance: TUNEL cell apoptosis assay; XTT cell proliferation assay; MTT cell proliferation assay; Colony formation assay
• Mechanism Description: MMP-9 was targeted and negatively regulated by hsa-miR494 which inhibited cell proliferation and induced cell apoptosis. Silybin inhibited OS cell viability by altering the protein levels of beta-catenin and RUNX2, thus upregulating the level of hsa-miR494.

References

• Ref 1: Matrix metallopeptidase 9 targeted by hsa-miR-494 promotes silybin-inhibited osteosarcoma. Mol Carcinog. 2018 Feb;57(2):262-271. doi: 10.1002/mc.22753. Epub 2017 Nov 2.