Ferroptosis-centered Drug Response Information

General Information of the Drug (ID: ferrodrug0136)
Name
Tanshinone IIA
Synonyms
Tanshinone IIA; 568-72-9; Tanshinone II; Dan Shen Ketone; Tanshinone B; Tanshinon II; 1,6,6-Trimethyl-6,7,8,9-tetrahydrophenanthro[1,2-b]furan-10,11-dione; UNII-4GPC9FQG6L; 4GPC9FQG6L; C19H18O3; 1,6,6-trimethyl-8,9-dihydro-7H-naphtho[1,2-g][1]benzofuran-10,11-dione; NSC 686518; SALVIOL IIA; HSDB 8104; Phenanthro[1,2-b]furan-10,11-dione, 6,7,8,9-tetrahydro-1,6,6-trimethyl-; NSC-686519; MLS001048863; DTXSID60205352; Phenanthro(1,2-b)furan-10,11-dione, 6,7,8,9-tetrahydro-1,6,6-trimethyl-; NSC686519; NSC-686518; SMR000387068; 1,6,6-trimethyl-8,9-dihydro-7H-naphtho[1,2-g]benzofuran-10,11-dione; TANSHINONE IIA (USP-RS); TANSHINONE IIA [USP-RS]; tanshinone II A; 1,6,6-TRIMETHYL-6,7,8,9-TETRAHYDROPHENANTHRO(1,2-B)FURAN-10,11-DIONE; 6,7,8,9-TETRAHYDRO-1,6,6-TRIMETHYLPHENANTHRO(1,2-B)FURAN-10,11-DIONE; SR-01000758926; tanshinone-IIA; 6,7,8,9-Tetrahydro-1,6,6-trimethylphenanthro[1,2-b]furan-10,11-dione; Tanshinone centoA; Tanshinone 2-A; MFCD00238692; TASHINONE IIA; Tanshinone Iia ,(S); BSPBio_001597; BSPBio_002426; KBioGR_000317; KBioSS_000317; MLS006011834; SPECTRUM1505824; CHEMBL187266; cid_164676; SCHEMBL2026738; Tanshinone IIA (Tanshinone B); TANSHINONE IIA [WHO-DD]; BDBM83922; KBio2_000317; KBio2_002885; KBio2_005453; KBio3_000633; KBio3_000634; DTXCID60127843; CHEBI:108595; Bio2_000317; Bio2_000797; HMS1361P19; HMS1791P19; HMS1989P19; HMS2089H08; HMS2270D15; HMS3402P19; HMS3656C11; NP474; BCP28199; HY-N0135; Tanshinone IIA, analytical standard; BBL028449; s2365; STK801917; Tanshinone IIA, >=97% (HPLC); AKOS004120032; AC-1440; CCG-207955; CCG-208275; IDI1_034067; NCGC00095709-01; NCGC00095709-02; NCGC00095709-03; NCGC00095709-04; NCGC00095709-05; NCGC00095709-06; NCGC00095709-08; AS-16136; NCI60_031209; FT-0652880; SW220025-1; T2987; A831217; Q-100654; SR-01000758926-2; SR-01000758926-4; SR-01000758926-5; BRD-K00141480-001-03-0; Q27187517; TANSHINONE IIA (CONSTITUENT OF CHINESE SALVIA); Phenanthro[1,11-dione, 6,7,8,9-tetrahydro-1,6,6-trimethyl-; TANSHINONE IIA (CONSTITUENT OF CHINESE SALVIA) [DSC]; Tanshinone IIA, European Pharmacopoeia (EP) Reference Standard; Tanshinone IIA, United States Pharmacopeia (USP) Reference Standard; 1,6,6-Trimethyl-6,7,8,9-tetrahydrophenanthro[1,2-b]furan-10,11-dione #; 1,6,6-trimethyl-8,9-dihydro-7H-naphtho[1,2-g]benzofuran-10,11-quinone; 1,6,6-trimethyl-8,9-dihydro-7H-naphtho[8,7-g]benzofuran-10,11-dione

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Status
Investigative
Drug Type
Small molecular drug
Structure
Formula
C19H18O3
IUPAC Name
1,6,6-trimethyl-8,9-dihydro-7H-naphtho[1,2-g][1]benzofuran-10,11-dione
Canonical SMILES
CC1=COC2=C1C(=O)C(=O)C3=C2C=CC4=C3CCCC4(C)C
InChI
InChI=1S/C19H18O3/c1-10-9-22-18-12-6-7-13-11(5-4-8-19(13,2)3)15(12)17(21)16(20)14(10)18/h6-7,9H,4-5,8H2,1-3H3
InChIKey
HYXITZLLTYIPOF-UHFFFAOYSA-N
PubChem CID
164676
Full List of Ferroptosis Target Related to This Drug
Cystine/glutamate transporter (SLC7A11)
 Target Info 
In total 1 item(s) under this Target
Experiment 1 Reporting the Ferroptosis-centered Drug Act on This Target [1]
Target for Ferroptosis Suppressor
Responsed Disease Gastric cancer ICD-11: 2B72
 Disease Info 
Responsed Regulator Cellular tumor antigen p53 (TP53) Driver
 Regulator Info 
Pathway Response Fatty acid metabolism hsa01212
Cell Process Cell ferroptosis
Cell proliferation
In Vitro Model BGC-823 cells Gastric carcinoma Homo sapiens CVCL_3360
NCI-N87 cells Gastric tubular adenocarcinoma Homo sapiens CVCL_1603
In Vivo Model
All mice were housed under a setting of 12-h light/dark cycle at 22 ± 1, 55% humidity and fed with water and food provided at regular time. During the entire maintenance period, all mice were permitted free cage activity without joint immobilization. The initial body weights of the mice were between 20 and 23 grams. After subcutaneous injection of 2 x 106 BGC-823 gastric cancer cells into the back of NOD-SCID mice, the mice were treated with or without Tan IIA (50 mg/kg) or Tan IIA in combination with Fer-1 (50 mg/kg). Tan IIA was diluted in DMSO:Methanol:Hydroxypropyl-b-cydodextrin (HP-b-CD) = 1:1:1. Fer-1 was also dissolved in DMSO:Methanol:HP-b-CD. Seven days after BGC-823 gastric cancer cells injection, intraperitoneal injection with Tan IIA was carried out every other day followed by killing at day 22 of tumor cell inoculation. All mice were killed by dislocation of the cervical vertebrae. Before killing, the tumor volume was measured every 3 days. All experiments were carried out using six mice each group in three independent experiments of a time-dependent manner with three time points.

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Response regulation Tanshinone IIA increased lipid peroxidation and up-regulated Ptgs2 and Chac1 expression, two markers of ferroptosis. In addition, Tan IIA also up-regulated p53 expression and down-regulated xCT (SLC7A11) expression. Therefore, Tan IIA could suppress the proliferation of gastric cancer via inducing p53 upregulation-mediated ferroptosis.
Prostaglandin G/H synthase 2 (PTGS2)
 Target Info 
In total 1 item(s) under this Target
Experiment 1 Reporting the Ferroptosis-centered Drug Act on This Target [1]
Target for Ferroptosis Marker
Responsed Disease Gastric cancer ICD-11: 2B72
 Disease Info 
Pathway Response Fatty acid metabolism hsa01212
Cell Process Cell ferroptosis
Cell proliferation
In Vitro Model BGC-823 cells Gastric carcinoma Homo sapiens CVCL_3360
NCI-N87 cells Gastric tubular adenocarcinoma Homo sapiens CVCL_1603
In Vivo Model
All mice were housed under a setting of 12-h light/dark cycle at 22 ± 1, 55% humidity and fed with water and food provided at regular time. During the entire maintenance period, all mice were permitted free cage activity without joint immobilization. The initial body weights of the mice were between 20 and 23 grams. After subcutaneous injection of 2 x 106 BGC-823 gastric cancer cells into the back of NOD-SCID mice, the mice were treated with or without Tan IIA (50 mg/kg) or Tan IIA in combination with Fer-1 (50 mg/kg). Tan IIA was diluted in DMSO:Methanol:Hydroxypropyl-b-cydodextrin (HP-b-CD) = 1:1:1. Fer-1 was also dissolved in DMSO:Methanol:HP-b-CD. Seven days after BGC-823 gastric cancer cells injection, intraperitoneal injection with Tan IIA was carried out every other day followed by killing at day 22 of tumor cell inoculation. All mice were killed by dislocation of the cervical vertebrae. Before killing, the tumor volume was measured every 3 days. All experiments were carried out using six mice each group in three independent experiments of a time-dependent manner with three time points.

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Response regulation Tanshinone IIA increased lipid peroxidation and up-regulated Ptgs2 and Chac1 expression, two markers of ferroptosis. In addition, Tan IIA also up-regulated p53 expression and down-regulated xCT expression. Therefore, Tan IIA could suppress the proliferation of gastric cancer via inducing p53 upregulation-mediated ferroptosis.
Glutathione-specific gamma-glutamylcyclotransferase 1 (CHAC1)
 Target Info 
In total 1 item(s) under this Target
Experiment 1 Reporting the Ferroptosis-centered Drug Act on This Target [1]
Target for Ferroptosis Marker/Driver
Responsed Disease Gastric cancer ICD-11: 2B72
 Disease Info 
Pathway Response Fatty acid metabolism hsa01212
Cell Process Cell ferroptosis
Cell proliferation
In Vitro Model BGC-823 cells Gastric carcinoma Homo sapiens CVCL_3360
NCI-N87 cells Gastric tubular adenocarcinoma Homo sapiens CVCL_1603
In Vivo Model
All mice were housed under a setting of 12-h light/dark cycle at 22 ± 1, 55% humidity and fed with water and food provided at regular time. During the entire maintenance period, all mice were permitted free cage activity without joint immobilization. The initial body weights of the mice were between 20 and 23 grams. After subcutaneous injection of 2 x 106 BGC-823 gastric cancer cells into the back of NOD-SCID mice, the mice were treated with or without Tan IIA (50 mg/kg) or Tan IIA in combination with Fer-1 (50 mg/kg). Tan IIA was diluted in DMSO:Methanol:Hydroxypropyl-b-cydodextrin (HP-b-CD) = 1:1:1. Fer-1 was also dissolved in DMSO:Methanol:HP-b-CD. Seven days after BGC-823 gastric cancer cells injection, intraperitoneal injection with Tan IIA was carried out every other day followed by killing at day 22 of tumor cell inoculation. All mice were killed by dislocation of the cervical vertebrae. Before killing, the tumor volume was measured every 3 days. All experiments were carried out using six mice each group in three independent experiments of a time-dependent manner with three time points.

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Response regulation Tanshinone IIA increased lipid peroxidation and up-regulated Ptgs2 and Chac1 expression, two markers of ferroptosis. In addition, Tan IIA also up-regulated p53 expression and down-regulated xCT expression. Therefore, Tan IIA could suppress the proliferation of gastric cancer via inducing p53 upregulation-mediated ferroptosis.
References
Ref 1 Tanshinone IIA induces ferroptosis in gastric cancer cells through p53-mediated SLC7A11 down-regulation. Biosci Rep. 2020 Aug 28;40(8):BSR20201807. doi: 10.1042/BSR20201807.