Ferroptosis-centered Drug Response Information

General Information of the Drug (ID: ferrodrug0124)
Name
Chrysin
Synonyms
chrysin; 480-40-0; 5,7-Dihydroxyflavone; 5,7-Dihydroxy-2-phenyl-4H-chromen-4-one; Chrysine; 5,7-dihydroxy-2-phenylchromen-4-one; Crysin; 4H-1-Benzopyran-4-one, 5,7-dihydroxy-2-phenyl-; NSC-407436; FLAVONE, 5,7-DIHYDROXY-; NSC 407436; Chrysinic acid; 5,7-Dihydroxy-2-phenyl-4H-1-benzopyran-4-one; EINECS 207-549-7; UNII-3CN01F5ZJ5; 5,7-Dihydroxy-2-phenyl-chromen-4-one; BRN 0233276; 3CN01F5ZJ5; DTXSID1022396; CHEBI:75095; MFCD00006834; NSC407436; 5,7-Dihydroxy-2-phenyl-4H-benzo(b)pyran-4-one; CHEMBL117; DTXCID902396; 5-18-04-00076 (Beilstein Handbook Reference); CAS-480-40-0; 5,7-dihydroxy-2-phenyl-4H-benzo[b]pyran-4-one; SMR000112318; 5,7-dihydroxy-flavone; SR-01000765660; 3ebo; 4des; 57D; Chrysin,(S); 5,7-diOH-Flavone; Flavone,7-dihydroxy-; Chrysin, 97%; Ois 3; Spectrum_000245; 5, 7-Dihydroxyflavone; CHRYSIN [INCI]; CHRYSIN [MI]; Prestwick0_000889; Prestwick1_000889; Prestwick2_000889; Prestwick3_000889; Spectrum2_000753; Spectrum3_001399; Spectrum4_000780; Spectrum5_001503; Chrysin, analytical standard; Oprea1_045160; SCHEMBL44474; BSPBio_000678; BSPBio_002514; BSPBio_003018; KBioGR_001200; KBioSS_000725; MLS000697728; MLS001074879; MLS006011841; BIDD:ER0484; DivK1c_000614; SPECTRUM1500709; SPECTRUM1505144; SPBio_000766; SPBio_002897; BDBM7461; BPBio1_000746; GTPL8789; MEGxp0_001416; ACon1_000087; cid_5281607; HMS501O16; KBio1_000614; KBio2_000725; KBio2_003293; KBio2_005861; KBio3_002238; NINDS_000614; HMS1570B20; HMS1921E20; HMS2097B20; HMS2268I23; HMS3468N08; HMS3655L20; BCP22863; Tox21_302335; BBL010449; CCG-40148; LMPK12110189; NSC818102; s2281; STK801609; AKOS000275936; BCP9000172; CS-7531; DB15581; GS-0927; NSC-818102; SDCCGMLS-0066586.P001; IDI1_000614; SMP1_000070; NCGC00016456-01; NCGC00016456-02; NCGC00016456-03; NCGC00016456-04; NCGC00016456-05; NCGC00016456-06; NCGC00016456-07; NCGC00016456-08; NCGC00016456-09; NCGC00016456-10; NCGC00016456-12; NCGC00094842-01; NCGC00094842-02; NCGC00094842-03; NCGC00094842-04; NCGC00094842-05; NCGC00168807-01; NCGC00168807-02; NCGC00168807-03; NCGC00168807-04; NCGC00255307-01; AC-10052; HY-14589; NCI60_003886; SY050125; AB00513947; C1652; FT-0619846; FT-0686390; SW197197-2; 5,7-Dihydroxy-2-phenyl-4H-chromen-4-one #; 4H-1-Benzopyran-4-one,7-dihydroxy-2-phenyl-; C-5980; EN300-303044; S00112; Chrysin 1000 microg/mL in Acetonitrile:Methanol; A827426; Q973741; SR-01000765660-3; SR-01000765660-4; 34B3B4AD-EEDD-4943-A1C6-8857D2FAA8E0; 5,7-Dihydroxy-2-phenyl-4H-1-benzopyran-4-one, 9CI; BRD-K22861715-001-07-5; BRD-K22861715-001-12-5; Z1824566175

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Status
Investigative
Drug Type
Small molecular drug
Structure
Formula
C15H10O4
IUPAC Name
5,7-dihydroxy-2-phenylchromen-4-one
Canonical SMILES
C1=CC=C(C=C1)C2=CC(=O)C3=C(C=C(C=C3O2)O)O
InChI
InChI=1S/C15H10O4/c16-10-6-11(17)15-12(18)8-13(19-14(15)7-10)9-4-2-1-3-5-9/h1-8,16-17H
InChIKey
RTIXKCRFFJGDFG-UHFFFAOYSA-N
PubChem CID
5281607
TTD Drug ID
D01UYI
Full List of Ferroptosis Target Related to This Drug
Ferritin heavy chain (FTH1)
 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/Suppressor
Responsed Disease Pancreatic cancer ICD-11: 2C10
 Disease Info 
Responsed Regulator Carbonyl reductase [NADPH] 1 (CBR1) Suppressor
 Regulator Info 
Pathway Response Fatty acid metabolism hsa01212
Ferroptosis hsa04216
Autophagy hsa04140
Cell Process Cell ferroptosis
Cell proliferation
Cell autophagy
In Vitro Model PANC-1 cells Pancreatic ductal adenocarcinoma Homo sapiens CVCL_0480
Capan-2 cells Pancreatic ductal adenocarcinoma Homo sapiens CVCL_0026
BxPC-3 cells Pancreatic ductal adenocarcinoma Homo sapiens CVCL_0186
AsPC-1 cells Pancreatic ductal adenocarcinoma Homo sapiens CVCL_0152
In Vivo Model
Male BALB/c nude mice (5 weeks old, weighing 18-20 g) were provided by Jiangsu Jicui Yaokang Biotechnology Co., Ltd. (Nanjing, China). The mice were subcutaneously transplanted with non-targeting shRNA (shcontrol) or CBR1-targeting shRNA (shCBR1)-transfected PANC-1 cells (200 uL, 1 x 107 cells). Tumor volumes and body weights were measured every 4 days (n = 4, each), tumor volume = 0.5 x (a x a x b) (a, smallest diameter; b, largest diameter). The mice were subcutaneously inoculated with PANC-1 cells (200 uL, 1 x 107 cells) in the combination treatment. When the tumor volume reached 80-100 mm3, the mice were treated with chrysin (30 mg/kg/i.P., daily), gemcitabine (20 mg/kg/i.p., once every other day), or in combination for four weeks.

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Response regulation Inhibition of CBR1 by chrysin increased cellular ROS levels and led to ROS-dependent autophagy, which resulted in the degradation of ferritin heavy polypeptide 1 (FTH1) and an increase in the intracellular free iron level that participates in ferroptosis in pancreatic cancer (PC) cells. Finally, chrysin enhanced PC sensitivity to gemcitabine by inducing ferroptotic death in vitro and in vivo.?
Transferrin receptor protein 1 (TFRC)
 Target Info 
In total 1 item(s) under this Target
Experiment 1 Reporting the Ferroptosis-centered Drug Act on This Target [2]
Target for Ferroptosis Driver
Responsed Disease Cerebral ischemia ICD-11: 8B10
 Disease Info 
Pathway Response Fatty acid metabolism hsa01212
Ferroptosis hsa04216
Cell Process Cell ferroptosis
In Vitro Model hBCs (Brain cells)
In Vivo Model
Male SD rats were randomly divided into a sham group, a model group, high-, medium-, and low-dose chrysin groups (200, 100, and 50 mg/kg), and a positive drug group (Ginaton, 21.6 mg/kg). The CIRI model was induced in rats by transient middle cerebral artery occlusion (tMCAO). The indexes were evaluated and the samples were taken 24 h after the operation.

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Response regulation The chrysin groups showed reduced content of total iron, lipid peroxide, and malondialdehyde in brain tissues and serum, increased mRNA and protein expression levels of SLC7A11 and GPX4, and decreased mRNA and protein expression levels of TFR1, PTGS2, and ACSL4. Chrysin may regulate iron metabolism via regulating the related targets of ferroptosis and inhibit neuronal ferroptosis induced by cerebral ischemia-reperfusion injury.
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 [2]
Target for Ferroptosis Marker
Responsed Disease Cerebral ischemia ICD-11: 8B10
 Disease Info 
Pathway Response Fatty acid metabolism hsa01212
Ferroptosis hsa04216
Cell Process Cell ferroptosis
In Vitro Model hBCs (Brain cells)
In Vivo Model
Male SD rats were randomly divided into a sham group, a model group, high-, medium-, and low-dose chrysin groups (200, 100, and 50 mg/kg), and a positive drug group (Ginaton, 21.6 mg/kg). The CIRI model was induced in rats by transient middle cerebral artery occlusion (tMCAO). The indexes were evaluated and the samples were taken 24 h after the operation.

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Response regulation The chrysin groups showed reduced content of total iron, lipid peroxide, and malondialdehyde in brain tissues and serum, increased mRNA and protein expression levels of SLC7A11 and GPX4, and decreased mRNA and protein expression levels of TFR1, PTGS2, and ACSL4. Chrysin may regulate iron metabolism via regulating the related targets of ferroptosis and inhibit neuronal ferroptosis induced by cerebral ischemia-reperfusion injury.
Phospholipid hydroperoxide glutathione peroxidase (GPX4)
 Target Info 
In total 1 item(s) under this Target
Experiment 1 Reporting the Ferroptosis-centered Drug Act on This Target [2]
Target for Ferroptosis Suppressor
Responsed Disease Cerebral ischemia ICD-11: 8B10
 Disease Info 
Pathway Response Fatty acid metabolism hsa01212
Ferroptosis hsa04216
Cell Process Cell ferroptosis
In Vitro Model hBCs (Brain cells)
In Vivo Model
Male SD rats were randomly divided into a sham group, a model group, high-, medium-, and low-dose chrysin groups (200, 100, and 50 mg/kg), and a positive drug group (Ginaton, 21.6 mg/kg). The CIRI model was induced in rats by transient middle cerebral artery occlusion (tMCAO). The indexes were evaluated and the samples were taken 24 h after the operation.

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Response regulation The chrysin groups showed reduced content of total iron, lipid peroxide, and malondialdehyde in brain tissues and serum, increased mRNA and protein expression levels of SLC7A11 and GPX4, and decreased mRNA and protein expression levels of TFR1, PTGS2, and ACSL4. Chrysin may regulate iron metabolism via regulating the related targets of ferroptosis and inhibit neuronal ferroptosis induced by cerebral ischemia-reperfusion injury.
Long-chain-fatty-acid--CoA ligase 4 (ACSL4)
 Target Info 
In total 1 item(s) under this Target
Experiment 1 Reporting the Ferroptosis-centered Drug Act on This Target [2]
Target for Ferroptosis Driver
Responsed Disease Cerebral ischemia ICD-11: 8B10
 Disease Info 
Pathway Response Fatty acid metabolism hsa01212
Ferroptosis hsa04216
Cell Process Cell ferroptosis
In Vitro Model hBCs (Brain cells)
In Vivo Model
Male SD rats were randomly divided into a sham group, a model group, high-, medium-, and low-dose chrysin groups (200, 100, and 50 mg/kg), and a positive drug group (Ginaton, 21.6 mg/kg). The CIRI model was induced in rats by transient middle cerebral artery occlusion (tMCAO). The indexes were evaluated and the samples were taken 24 h after the operation.

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Response regulation The chrysin groups showed reduced content of total iron, lipid peroxide, and malondialdehyde in brain tissues and serum, increased mRNA and protein expression levels of SLC7A11 and GPX4, and decreased mRNA and protein expression levels of TFR1, PTGS2, and ACSL4. Chrysin may regulate iron metabolism via regulating the related targets of ferroptosis and inhibit neuronal ferroptosis induced by cerebral ischemia-reperfusion injury.
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 [2]
Target for Ferroptosis Suppressor
Responsed Disease Cerebral ischemia ICD-11: 8B10
 Disease Info 
Pathway Response Fatty acid metabolism hsa01212
Ferroptosis hsa04216
Cell Process Cell ferroptosis
In Vitro Model hBCs (Brain cells)
In Vivo Model
Male SD rats were randomly divided into a sham group, a model group, high-, medium-, and low-dose chrysin groups (200, 100, and 50 mg/kg), and a positive drug group (Ginaton, 21.6 mg/kg). The CIRI model was induced in rats by transient middle cerebral artery occlusion (tMCAO). The indexes were evaluated and the samples were taken 24 h after the operation.

    Click to Show/Hide
Response regulation The chrysin groups showed reduced content of total iron, lipid peroxide, and malondialdehyde in brain tissues and serum, increased mRNA and protein expression levels of SLC7A11 and GPX4, and decreased mRNA and protein expression levels of TFR1, PTGS2, and ACSL4. Chrysin may regulate iron metabolism via regulating the related targets of ferroptosis and inhibit neuronal ferroptosis induced by cerebral ischemia-reperfusion injury.
References
Ref 1 Chrysin induces autophagy-dependent ferroptosis to increase chemosensitivity to gemcitabine by targeting CBR1 in pancreatic cancer cells. Biochem Pharmacol. 2021 Nov;193:114813. doi: 10.1016/j.bcp.2021.114813. Epub 2021 Oct 18.
Ref 2 [Chrysin alleviates cerebral ischemia-reperfusion injury by inhibiting ferroptosis in rats]. Zhongguo Zhong Yao Za Zhi. 2023 Mar;48(6):1597-1605. doi: 10.19540/j.cnki.cjcmm.20221201.705.