General Information of Drug (ID: DMOJQGT)

Drug Name
ICARIIN Drug Info
Synonyms
Icariin; 489-32-7; Ieariline; UNII-VNM47R2QSQ; CHEBI:78420; VNM47R2QSQ; Icariine; 3-((6-Deoxymannopyranosyl)oxy)-7-(glucopyranosyloxy)-5-hydroxy-2-(4-methoxyphenyl)-8-(3-methyl-2-butenyl)-4H-1-benzopyran-4-one; Icarin; 5-hydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-en-1-yl)-7-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)-3-(((2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-4H-chromen-4-one; 4H-1-Benzopyran-4-one, 3-((6-deoxy-alpha-L-mannopyranosyl)oxy)-7-(be
Cross-matching ID
PubChem CID
5318997
ChEBI ID
CHEBI:78420
CAS Number
CAS 489-32-7
TTD Drug ID
DMOJQGT

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tadalafil DMJZHT1 Benign prostatic hyperplasia GA90 Approved [9]
Udenafil DM1IQRP Erectile dysfunction HA01.1 Approved [10]
Vardenafil DMTBGW8 Cystic fibrosis CA25 Approved [11]
Dipyridamole DMXY30O Atrial fibrillation BC81.3 Approved [12]
Papaverine DMCA9QP Brain ischaemia 8B1Z Approved [13]
Avanafil DM75CXN Erectile dysfunction HA01.1 Approved [14]
Rhucin DM3ADGP Erectile dysfunction HA01.1 Approved [15]
EXISULIND DMBY56U Colorectal cancer 2B91.Z Phase 3 [16]
PF-489791 DM3C8GQ Chronic obstructive pulmonary disease CA22 Phase 2 [17]
UK-371800 DMI8795 Erectile dysfunction HA01.1 Phase 1 [18]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Nitric oxide synthase 3 (NOS3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [19]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [20]
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [21]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [22]
Methotrexate DM2TEOL Anterior urethra cancer Approved [23]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [24]
Quercetin DM3NC4M Obesity 5B81 Approved [25]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [26]
Fructose DM43AN2 Vomiting MD90 Approved [27]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [28]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [29]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [30]
Selenium DM25CGV N. A. N. A. Approved [31]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [32]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [33]
Deoxycholic acid DM3GYAL Subcutaneous fat disorder EF02 Approved [34]
Quercetin DM3NC4M Obesity 5B81 Approved [35]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [36]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [37]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [38]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Rhucin DM3ADGP Erectile dysfunction HA01.1 Approved [39]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [40]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [41]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [42]
Zoledronate DMIXC7G Adenocarcinoma 2D40 Approved [43]
Tadalafil DMJZHT1 Benign prostatic hyperplasia GA90 Approved [44]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [45]
Vardenafil DMTBGW8 Cystic fibrosis CA25 Approved [44]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [46]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [47]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [48]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [49]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [50]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [51]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [52]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [53]
Cidofovir DMA13GD Cytomegalovirus infection 1D82 Approved [52]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [54]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [55]
Ethanol DMDRQZU Chronic pain MG30 Approved [56]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Interleukin-1 beta (IL1B)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [29]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [57]
Gefitinib DM15F0X Colon adenocarcinoma Approved [58]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [59]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [60]
Lumiracoxib DM1S4AG Chronic renal failure GB61.Z Approved [59]
Imiquimod DM1TMA3 Alopecia areata ED70.2 Approved [61]
Selenium DM25CGV N. A. N. A. Approved [62]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [63]
Spironolactone DM2AQ5N Chronic heart failure BD1Z Approved [64]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Trefoil factor 1 (TFF1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [65]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [48]
Spironolactone DM2AQ5N Chronic heart failure BD1Z Approved [66]
Quercetin DM3NC4M Obesity 5B81 Approved [67]
Estrone DM5T6US Acne vulgaris ED80 Approved [68]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [69]
Reserpine DM6VM38 Hypertension BA00-BA04 Approved [66]
Testosterone DM7HUNW Hot flushes GA30 Approved [70]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [53]
Exemestane DM9HPW3 Hormonally-responsive breast cancer 2C60-2C65 Approved [71]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Progesterone receptor (PGR)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [72]
Drospirenone DM1A9W3 Acne vulgaris ED80 Approved [73]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [74]
Estrone DM5T6US Acne vulgaris ED80 Approved [75]
Tibolone DM78XFG Anabolic metabolism 5C50-5C8Z Approved [76]
Testosterone DM7HUNW Hot flushes GA30 Approved [77]
Exemestane DM9HPW3 Hormonally-responsive breast cancer 2C60-2C65 Approved [71]
Goserelin DMAT8CG Breast cancer 2C60-2C65 Approved [78]
Lindane DMB8CNL Infestations of lice and scabies 1G00.Z Approved [79]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [42]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [80]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [81]
Quercetin DM3NC4M Obesity 5B81 Approved [82]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [83]
Panobinostat DM58WKG Chronic graft versus host disease Approved [84]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [85]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [41]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [86]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [42]
Demecolcine DMCZQGK Solid tumour/cancer 2A00-2F9Z Approved [87]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Caspase-1 (CASP1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [29]
Gefitinib DM15F0X Colon adenocarcinoma Approved [58]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [88]
Imiquimod DM1TMA3 Alopecia areata ED70.2 Approved [61]
Salicyclic acid DM2F8XZ Acne vulgaris ED80 Approved [89]
Quercetin DM3NC4M Obesity 5B81 Approved [90]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [91]
Cyclophosphamide DM4O2Z7 Advanced cancer 2A00-2F9Z Approved [92]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [93]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [94]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [95]
Selenium DM25CGV N. A. N. A. Approved [31]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [96]
Quercetin DM3NC4M Obesity 5B81 Approved [97]
Isoniazid DM5JVS3 Latent tuberculosis infection Approved [98]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [99]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [100]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [101]
Testosterone DM7HUNW Hot flushes GA30 Approved [102]
Olaparib DM8QB1D Ovarian cancer 2C73 Approved [103]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [29]
Selenium DM25CGV N. A. N. A. Approved [62]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [104]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [105]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [94]
Testosterone DM7HUNW Hot flushes GA30 Approved [102]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [106]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [107]
Ethanol DMDRQZU Chronic pain MG30 Approved [108]
Atropine DMEN6X7 Organophosphate poisoning NE6Z Approved [109]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Warfarin DMJYCVW Atrial fibrillation BC81.3 Approved [110]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [111]
Hydroxyurea DMOQVU9 Chronic myelogenous leukaemia 2A20.0 Approved [112]
Trospium chloride DM32XZT Discovery agent N.A. Approved [113]
Deoxycholic acid DM3GYAL Subcutaneous fat disorder EF02 Approved [114]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [115]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [50]
Cholic Acid DM7OKQV Cholelithiasis DC11 Approved [114]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [85]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [107]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Phosphodiesterase 5A (PDE5A) TTJ0IQB PDE5A_HUMAN Inhibitor [1]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Bone morphogenetic protein 2 (BMP2) OT23T37S BMP2_HUMAN Gene/Protein Processing [2]
Caspase-1 (CASP1) OTZ3YQFU CASP1_HUMAN Protein Interaction/Cellular Processes [3]
cGMP-specific 3',5'-cyclic phosphodiesterase (PDE5A) OTT8Q1AP PDE5A_HUMAN Gene/Protein Processing [4]
Interleukin-1 beta (IL1B) OT0DWXXB IL1B_HUMAN Gene/Protein Processing [3]
NACHT, LRR and PYD domains-containing protein 3 (NLRP3) OTZM6MHU NLRP3_HUMAN Gene/Protein Processing [3]
NAD-dependent protein deacetylase sirtuin-1 (SIRT1) OTAYZMOY SIR1_HUMAN Gene/Protein Processing [5]
Nitric oxide synthase 3 (NOS3) OTLDT7NR NOS3_HUMAN Gene/Protein Processing [6]
Progesterone receptor (PGR) OT0FZ3QE PRGR_HUMAN Gene/Protein Processing [7]
Solute carrier organic anion transporter family member 1B3 (SLCO1B3) OTOM3BUH SO1B3_HUMAN Gene/Protein Processing [8]
Solute carrier organic anion transporter family member 2B1 (SLCO2B1) OTERJ4VQ SO2B1_HUMAN Gene/Protein Processing [8]

References

1 Potent inhibition of human phosphodiesterase-5 by icariin derivatives. J Nat Prod. 2008 Sep;71(9):1513-7.
2 [Effects of Epimedium pubescens icariine on proliferation and differentiation of human osteoblasts]. Zhongguo Zhong Yao Za Zhi. 2005 Feb;30(4):289-91.
3 Icariin inhibits gastric cancer cell growth by regulating the hsa_circ_0003159/miR-223-3p/NLRP3 signaling axis. Hum Exp Toxicol. 2022 Jan-Dec;41:9603271221097363. doi: 10.1177/09603271221097363.
4 Potent inhibition of human phosphodiesterase-5 by icariin derivatives. J Nat Prod. 2008 Sep;71(9):1513-7.
5 Icariin protects against intestinal ischemia-reperfusion injury. J Surg Res. 2015 Mar;194(1):127-38. doi: 10.1016/j.jss.2014.10.004. Epub 2014 Oct 8.
6 Icariin enhances endothelial nitric-oxide synthase expression on human endothelial cells in vitro. Vascul Pharmacol. 2007 Jul;47(1):18-24.
7 Proliferation-stimulating effects of icaritin and desmethylicaritin in MCF-7 cells. Eur J Pharmacol. 2004 Nov 19;504(3):147-53. doi: 10.1016/j.ejphar.2004.10.002.
8 Interaction of the bioactive flavonol, icariin, with the essential human solute carrier transporters. J Biochem Mol Toxicol. 2014 Feb;28(2):91-7. doi: 10.1002/jbt.21540. Epub 2013 Nov 21.
9 Pulmonary arterial hypertension: the most devastating vascular complication of systemic sclerosis. Rheumatology (Oxford). 2009 Jun;48 Suppl 3:iii25-31.
10 Increased expression of the nitric oxide synthase gene and protein in corpus cavernosum by repeated dosing of udenafil in a rat model of chemical d... Asian J Androl. 2009 Jul;11(4):435-42.
11 The effect of vardenafil, a potent and highly selective phosphodiesterase-5 inhibitor for the treatment of erectile dysfunction, on the cardiovascular response to exercise in patients with coronary artery disease. J Am Coll Cardiol. 2002 Dec 4;40(11):2006-12.
12 Anti-platelet therapy: phosphodiesterase inhibitors.Br J Clin Pharmacol.2011 Oct;72(4):634-46.
13 Effects of icariin on cGMP-specific PDE5 and cAMP-specific PDE4 activities. Asian J Androl. 2003 Mar;5(1):15-8.
14 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
15 cGMP-hydrolytic activity and its inhibition by sildenafil in normal and failing human and mouse myocardium. J Pharmacol Exp Ther. 2009 Sep;330(3):884-91.
16 Exisulind induction of apoptosis involves guanosine 3',5'-cyclic monophosphate phosphodiesterase inhibition, protein kinase G activation, and attenuated beta-catenin. Cancer Res. 2000 Jul 1;60(13):3338-42.
17 Highlights of the society for medicinesresearch symposium held december 10th 2009 at the national heart and lung institute, London, UK. Drugs of the Future 2010, 35(4): 349-358.
18 Highly potent and selective chiral inhibitors of PDE5: an illustration of Pfeiffer's rule. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6033-6.
19 Protective effects of S-carvedilol on doxorubicin-induced damages to human umbilical vein endothelial cells and rats. J Appl Toxicol. 2019 Aug;39(8):1233-1244. doi: 10.1002/jat.3809. Epub 2019 May 7.
20 Oxidative stress in kidney transplant patients with calcineurin inhibitor-induced hypertension: effect of ramipril. J Cardiovasc Pharmacol. 2002 Oct;40(4):625-31.
21 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
22 Hydrogen peroxide decreases endothelial nitric oxide synthase promoter activity through the inhibition of Sp1 activity. DNA Cell Biol. 2009 Mar;28(3):119-29.
23 Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
24 Simvastatin inhibits cigarette smoking-induced emphysema and pulmonary hypertension in rat lungs. Am J Respir Crit Care Med. 2005 Oct 15;172(8):987-93. doi: 10.1164/rccm.200501-041OC. Epub 2005 Jul 7.
25 A blend of polyphenolic compounds explains the stimulatory effect of red wine on human endothelial NO synthase. Nitric Oxide. 2005 Mar;12(2):97-104.
26 The thiazolidinedione drug troglitazone up-regulates nitric oxide synthase expression in vascular endothelial cells. J Diabetes Complications. 2006 Sep-Oct;20(5):336-42.
27 Fructose induces the inflammatory molecule ICAM-1 in endothelial cells. J Am Soc Nephrol. 2008 Sep;19(9):1712-20.
28 Upregulation of nitric oxide production in vascular endothelial cells by all-trans retinoic acid through the phosphoinositide 3-kinase/Akt pathway. Circulation. 2005 Aug 2;112(5):727-36. doi: 10.1161/CIRCULATIONAHA.104.500959. Epub 2005 Jul 25.
29 Cannabidiol Modulates the Immunophenotype and Inhibits the Activation of the Inflammasome in Human Gingival Mesenchymal Stem Cells. Front Physiol. 2016 Nov 24;7:559. doi: 10.3389/fphys.2016.00559. eCollection 2016.
30 -Carotene Induces Apoptosis in Human Esophageal Squamous Cell Carcinoma Cell Lines via the Cav-1/AKT/NF-B Signaling Pathway. J Biochem Mol Toxicol. 2016 Mar;30(3):148-57. doi: 10.1002/jbt.21773. Epub 2016 Jan 6.
31 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
32 Differential gene expression of sulindac-treated human breast epithelial cells. Int J Oncol. 2005 Dec;27(6):1727-36.
33 Suppression of RAGE as a basis of simvastatin-dependent plaque stabilization in type 2 diabetes. Arterioscler Thromb Vasc Biol. 2006 Dec;26(12):2716-23.
34 Prevention of deoxycholate-induced gastric apoptosis by aspirin: roles of NF-kappaB and PKC signaling. J Surg Res. 2008 Mar;145(1):66-73. doi: 10.1016/j.jss.2007.04.039. Epub 2007 Jul 20.
35 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
36 Peroxisome proliferator-activated receptor-gamma agonists inhibit respiratory syncytial virus-induced expression of intercellular adhesion molecule-1 in human lung epithelial cells. Immunology. 2007 May;121(1):71-81. doi: 10.1111/j.1365-2567.2006.02539.x.
37 Differential modulation of PI3-kinase/Akt pathway during all-trans retinoic acid- and Am80-induced HL-60 cell differentiation revealed by DNA microarray analysis. Biochem Pharmacol. 2004 Dec 1;68(11):2177-86.
38 Glucosamine regulation of LPS-mediated inflammation in human bronchial epithelial cells. Eur J Pharmacol. 2010 Jun 10;635(1-3):219-26. doi: 10.1016/j.ejphar.2010.02.044. Epub 2010 Mar 20.
39 Sildenafil ameliorates effects of inhaled nitric oxide withdrawal. Anesthesiology. 1999 Jul;91(1):307-10. doi: 10.1097/00000542-199907000-00041.
40 Development of a neural teratogenicity test based on human embryonic stem cells: response to retinoic acid exposure. Toxicol Sci. 2011 Dec;124(2):370-7.
41 Integrative "-Omics" analysis in primary human hepatocytes unravels persistent mechanisms of cyclosporine A-induced cholestasis. Chem Res Toxicol. 2016 Dec 19;29(12):2164-2174.
42 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
43 Interleukin-19 as a translational indicator of renal injury. Arch Toxicol. 2015 Jan;89(1):101-6.
44 Pharmacotherapy of erectile dysfunction: focus on cardiovascular safety. Expert Opin Drug Saf. 2005 May;4(3):531-40. doi: 10.1517/14740338.4.3.531.
45 Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
46 Multiple microRNAs function as self-protective modules in acetaminophen-induced hepatotoxicity in humans. Arch Toxicol. 2018 Feb;92(2):845-858.
47 Comparative effects of raloxifene, tamoxifen and estradiol on human osteoblasts in vitro: estrogen receptor dependent or independent pathways of raloxifene. J Steroid Biochem Mol Biol. 2009 Feb;113(3-5):281-9.
48 Global gene expression analysis reveals differences in cellular responses to hydroxyl- and superoxide anion radical-induced oxidative stress in caco-2 cells. Toxicol Sci. 2010 Apr;114(2):193-203. doi: 10.1093/toxsci/kfp309. Epub 2009 Dec 31.
49 Differential gene expression in human hepatocyte cell lines exposed to the antiretroviral agent zidovudine. Arch Toxicol. 2014 Mar;88(3):609-23. doi: 10.1007/s00204-013-1169-3. Epub 2013 Nov 30.
50 Rifampin Regulation of Drug Transporters Gene Expression and the Association of MicroRNAs in Human Hepatocytes. Front Pharmacol. 2016 Apr 26;7:111.
51 In vitro study of transporters involved in intestinal absorption of inorganic arsenic. Chem Res Toxicol. 2012 Feb 20;25(2):446-53. doi: 10.1021/tx200491f. Epub 2012 Jan 26.
52 Transcriptomics hit the target: monitoring of ligand-activated and stress response pathways for chemical testing. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):7-18.
53 Identification of vitamin D3 target genes in human breast cancer tissue. J Steroid Biochem Mol Biol. 2016 Nov;164:90-97.
54 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
55 Gene Expression Regulation and Pathway Analysis After Valproic Acid and Carbamazepine Exposure in a Human Embryonic Stem Cell-Based Neurodevelopmental Toxicity Assay. Toxicol Sci. 2015 Aug;146(2):311-20. doi: 10.1093/toxsci/kfv094. Epub 2015 May 15.
56 Prenatal ethanol exposure increases maternal bile acids through placental transport pathway. Toxicology. 2021 Jun 30;458:152848. doi: 10.1016/j.tox.2021.152848. Epub 2021 Jul 2.
57 ERE-independent ERalpha target genes differentially expressed in human breast tumors. Mol Cell Endocrinol. 2005 Dec 21;245(1-2):53-9. doi: 10.1016/j.mce.2005.10.003. Epub 2005 Nov 17.
58 Reactive metabolite of gefitinib activates inflammasomes: implications for gefitinib-induced idiosyncratic reaction. J Toxicol Sci. 2020;45(11):673-680. doi: 10.2131/jts.45.673.
59 An in vitro coculture system of human peripheral blood mononuclear cells with hepatocellular carcinoma-derived cells for predicting drug-induced liver injury. Arch Toxicol. 2021 Jan;95(1):149-168. doi: 10.1007/s00204-020-02882-4. Epub 2020 Aug 20.
60 Gypenosides protect retinal pigment epithelium cells from oxidative stress. Food Chem Toxicol. 2018 Feb;112:76-85.
61 (9)-Tetrahydrocannabinol Suppresses Monocyte-Mediated Astrocyte Production of Monocyte Chemoattractant Protein 1 and Interleukin-6 in a Toll-Like Receptor 7-Stimulated Human Coculture. J Pharmacol Exp Ther. 2019 Oct;371(1):191-201. doi: 10.1124/jpet.119.260661. Epub 2019 Aug 5.
62 Changes in gene expression profiles in response to selenium supplementation among individuals with arsenic-induced pre-malignant skin lesions. Toxicol Lett. 2007 Mar 8;169(2):162-76. doi: 10.1016/j.toxlet.2007.01.006. Epub 2007 Jan 19.
63 Profiling the immunotoxicity of chemicals based on in vitro evaluation by a combination of the Multi-ImmunoTox assay and the IL-8 Luc assay. Arch Toxicol. 2018 Jun;92(6):2043-2054. doi: 10.1007/s00204-018-2199-7. Epub 2018 Mar 29.
64 Spironolactone induces apoptosis in human mononuclear cells. Association between apoptosis and cytokine suppression. Apoptosis. 2006 Apr;11(4):573-9. doi: 10.1007/s10495-006-4919-3.
65 Resveratrol modulates the phosphoinositide 3-kinase pathway through an estrogen receptor alpha-dependent mechanism: relevance in cell proliferation. Int J Cancer. 2004 Mar 20;109(2):167-73. doi: 10.1002/ijc.11720.
66 Evaluation of an imaging-based in vitro screening platform for estrogenic activity with OECD reference chemicals. Toxicol In Vitro. 2022 Jun;81:105348. doi: 10.1016/j.tiv.2022.105348. Epub 2022 Mar 18.
67 Estrogenic activities of Ginkgo biloba extracts. Life Sci. 2004 Jan 30;74(11):1325-35. doi: 10.1016/j.lfs.2003.06.045.
68 Tartrazine and sunset yellow are xenoestrogens in a new screening assay to identify modulators of human oestrogen receptor transcriptional activity. Toxicology. 2012 Aug 16;298(1-3):40-51. doi: 10.1016/j.tox.2012.04.014. Epub 2012 May 3.
69 Arsenic induces functional re-expression of estrogen receptor by demethylation of DNA in estrogen receptor-negative human breast cancer. PLoS One. 2012;7(4):e35957. doi: 10.1371/journal.pone.0035957. Epub 2012 Apr 27.
70 Co-culture of primary human mammary fibroblasts and MCF-7 cells as an in vitro breast cancer model. Toxicol Sci. 2005 Feb;83(2):257-63.
71 Characterization of the weak estrogen receptor alpha agonistic activity of exemestane. Breast Cancer Res Treat. 2009 Aug;116(3):461-70. doi: 10.1007/s10549-008-0151-x. Epub 2008 Aug 3.
72 Effects of the environmental estrogens bisphenol A, o,p'-DDT, p-tert-octylphenol and coumestrol on apoptosis induction, cell proliferation and the expression of estrogen sensitive molecular parameters in the human breast cancer cell line MCF-7. J Steroid Biochem Mol Biol. 2002 Jan;80(1):61-70. doi: 10.1016/s0960-0760(01)00173-x.
73 Conception and pharmacodynamic profile of drospirenone. Steroids. 2003 Nov;68(10-13):891-905. doi: 10.1016/j.steroids.2003.08.008.
74 Biological activity of all-trans-retinoic acid with and without tamoxifen and alpha-interferon 2a in breast cancer patients. Int J Oncol. 2000 Nov;17(5):991-1000. doi: 10.3892/ijo.17.5.991.
75 Estrogen-induced loss of progesterone receptor expression in normal and malignant ovarian surface epithelial cells. Oncogene. 2005 Jun 23;24(27):4388-400. doi: 10.1038/sj.onc.1208623.
76 Tibolone and its metabolites enhance tissue factor and PAI-1 expression in human endometrial stromal cells: Evidence of progestogenic effects. Steroids. 2005 Nov;70(12):840-5. doi: 10.1016/j.steroids.2005.04.010.
77 Expression of estrogen-, progesterone-, and androgen-responsive genes in MCF-7 and MDA-MB-231 cells treated with o,p'-DDT, p,p'-DDT, or endosulfan. J Biochem Mol Toxicol. 2021 Jun;35(6):1-8. doi: 10.1002/jbt.22773. Epub 2021 Mar 16.
78 A comparative study of the effect of raloxifene and gosereline on uterine leiomyoma volume changes and estrogen receptor, progesterone receptor, bcl-2 and p53 expression immunohistochemically in premenopausal women. Eur J Obstet Gynecol Reprod Biol. 2007 Nov;135(1):94-103. doi: 10.1016/j.ejogrb.2006.07.042. Epub 2006 Sep 14.
79 Serum free BG-1 cell proliferation assay: a sensitive method for determining organochlorine pesticide estrogen receptor activation at the nanomolar range. Toxicol In Vitro. 2006 Apr;20(3):382-94. doi: 10.1016/j.tiv.2005.08.016. Epub 2005 Oct 19.
80 Peripheral blood expression profiles of bone morphogenetic proteins, tumor necrosis factor-superfamily molecules, and transcription factor Runx2 could be used as markers of the form of arthritis, disease activity, and therapeutic responsiveness. J Rheumatol. 2010 Feb;37(2):246-56. doi: 10.3899/jrheum.090167. Epub 2009 Dec 15.
81 Compactin and simvastatin, but not pravastatin, induce bone morphogenetic protein-2 in human osteosarcoma cells. Biochem Biophys Res Commun. 2000 May 19;271(3):688-92. doi: 10.1006/bbrc.2000.2697.
82 Quercetin, a flavonoid, inhibits proliferation and increases osteogenic differentiation in human adipose stromal cells. Biochem Pharmacol. 2006 Nov 15;72(10):1268-78. doi: 10.1016/j.bcp.2006.08.021. Epub 2006 Sep 22.
83 Human oligodendrocytes derived from embryonic stem cells: Effect of noggin on phenotypic differentiation in vitro and on myelination in vivo. Mol Cell Neurosci. 2007 Mar;34(3):310-23. doi: 10.1016/j.mcn.2006.11.008. Epub 2006 Dec 28.
84 A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors. Arch Toxicol. 2015 Sep;89(9):1599-618.
85 Large-scale in silico and microarray-based identification of direct 1,25-dihydroxyvitamin D3 target genes. Mol Endocrinol. 2005 Nov;19(11):2685-95.
86 Simvastatin and atorvastatin enhance gene expression of collagen type 1 and osteocalcin in primary human osteoblasts and MG-63 cultures. J Cell Biochem. 2007 Aug 15;101(6):1430-8. doi: 10.1002/jcb.21259.
87 Characterization of formaldehyde's genotoxic mode of action by gene expression analysis in TK6 cells. Arch Toxicol. 2013 Nov;87(11):1999-2012.
88 Cannabidiol Protects Human Skin Keratinocytes from Hydrogen-Peroxide-Induced Oxidative Stress via Modulation of the Caspase-1-IL-1 Axis. J Nat Prod. 2021 May 28;84(5):1563-1572. doi: 10.1021/acs.jnatprod.1c00083. Epub 2021 May 6.
89 Some non-sensitizers upregulate CD54 expression by activation of the NLRP3 inflammasome in THP-1 cells. J Toxicol Sci. 2019;44(3):213-224. doi: 10.2131/jts.44.213.
90 Integrated assessment by multiple gene expression analysis of quercetin bioactivity on anticancer-related mechanisms in colon cancer cells in vitro. Eur J Nutr. 2005 Mar;44(3):143-56. doi: 10.1007/s00394-004-0503-1. Epub 2004 Apr 30.
91 Systems analysis of transcriptome and proteome in retinoic acid/arsenic trioxide-induced cell differentiation/apoptosis of promyelocytic leukemia. Proc Natl Acad Sci U S A. 2005 May 24;102(21):7653-8.
92 Comparative gene expression analysis of a chronic myelogenous leukemia cell line resistant to cyclophosphamide using oligonucleotide arrays and response to tyrosine kinase inhibitors. Leuk Res. 2007 Nov;31(11):1511-20.
93 Improved apoptotic cell death in drug-resistant non-small-cell lung cancer cells by tumor necrosis factor-related apoptosis-inducing ligand-based treatment. J Pharmacol Exp Ther. 2014 Mar;348(3):360-71. doi: 10.1124/jpet.113.210054. Epub 2013 Dec 17.
94 Hydroquinone triggers pyroptosis and endoplasmic reticulum stress via AhR-regulated oxidative stress in human lymphocytes. Toxicol Lett. 2023 Mar 1;376:39-50. doi: 10.1016/j.toxlet.2023.01.005. Epub 2023 Jan 13.
95 SIRT3 Mediates the Antioxidant Effect of Hydrogen Sulfide in Endothelial Cells. Antioxid Redox Signal. 2016 Feb 20;24(6):329-43. doi: 10.1089/ars.2015.6331. Epub 2015 Nov 10.
96 Expression profile analysis of colon cancer cells in response to sulindac or aspirin. Biochem Biophys Res Commun. 2002 Mar 29;292(2):498-512.
97 The p53/miR-34a/SIRT1 Positive Feedback Loop in Quercetin-Induced Apoptosis. Cell Physiol Biochem. 2015;35(6):2192-202. doi: 10.1159/000374024. Epub 2015 Apr 7.
98 AMPK activator acadesine fails to alleviate isoniazid-caused mitochondrial instability in HepG2 cells. J Appl Toxicol. 2017 Oct;37(10):1219-1224. doi: 10.1002/jat.3483. Epub 2017 May 29.
99 Arsenic trioxide induces apoptosis in NB-4, an acute promyelocytic leukemia cell line, through up-regulation of p73 via suppression of nuclear factor kappa B-mediated inhibition of p73 transcription and prevention of NF-kappaB-mediated induction of XIAP, cIAP2, BCL-XL and survivin. Med Oncol. 2010 Sep;27(3):833-42. doi: 10.1007/s12032-009-9294-9. Epub 2009 Sep 10.
100 Dual targeting of the antagonistic pathways mediated by Sirt1 and TXNIP as a putative approach to enhance the efficacy of anti-aging interventions. Aging (Albany NY). 2009 Mar 31;1(4):412-24. doi: 10.18632/aging.100035.
101 Hydroquinone-induced malignant transformation of TK6 cells by facilitating SIRT1-mediated p53 degradation and up-regulating KRAS. Toxicol Lett. 2016 Sep 30;259:133-142. doi: 10.1016/j.toxlet.2016.08.006. Epub 2016 Aug 8.
102 The exosome-like vesicles derived from androgen exposed-prostate stromal cells promote epithelial cells proliferation and epithelial-mesenchymal transition. Toxicol Appl Pharmacol. 2021 Jan 15;411:115384. doi: 10.1016/j.taap.2020.115384. Epub 2020 Dec 25.
103 Iron overload inhibits cell proliferation and promotes autophagy via PARP1/SIRT1 signaling in endometriosis and adenomyosis. Toxicology. 2022 Jan 15;465:153050. doi: 10.1016/j.tox.2021.153050. Epub 2021 Nov 23.
104 Transcriptional and Metabolic Dissection of ATRA-Induced Granulocytic Differentiation in NB4 Acute Promyelocytic Leukemia Cells. Cells. 2020 Nov 5;9(11):2423. doi: 10.3390/cells9112423.
105 AS3MT facilitates NLRP3 inflammasome activation by m(6)A modification during arsenic-induced hepatic insulin resistance. Cell Biol Toxicol. 2023 Oct;39(5):2165-2181. doi: 10.1007/s10565-022-09703-7. Epub 2022 Feb 28.
106 Imatinib-induced hepatotoxicity via oxidative stress and activation of NLRP3 inflammasome: an in vitro and in vivo study. Arch Toxicol. 2022 Apr;96(4):1075-1087. doi: 10.1007/s00204-022-03245-x. Epub 2022 Feb 22.
107 Primary Human Hepatocyte Spheroids as Tools to Study the Hepatotoxic Potential of Non-Pharmaceutical Chemicals. Int J Mol Sci. 2021 Oct 12;22(20):11005. doi: 10.3390/ijms222011005.
108 Pterostilbene attenuates RIPK3-dependent hepatocyte necroptosis in alcoholic liver disease via SIRT2-mediated NFATc4 deacetylation. Toxicology. 2021 Sep;461:152923. doi: 10.1016/j.tox.2021.152923. Epub 2021 Aug 30.
109 Prediction of drug-induced liver injury using keratinocytes. J Appl Toxicol. 2017 Jul;37(7):863-872. doi: 10.1002/jat.3435. Epub 2017 Jan 31.
110 Identification of two novel genes SLC15A2 and SLCO1B3 associated with maintenance dose variability of warfarin in a Chinese population. Sci Rep. 2017 Dec 12;7(1):17379. doi: 10.1038/s41598-017-17731-1.
111 Involvement of multiple efflux transporters in hepatic disposition of fexofenadine. Mol Pharmacol. 2008 May;73(5):1474-83.
112 Transcellular movement of hydroxyurea is mediated by specific solute carrier transporters. Exp Hematol. 2011 Apr;39(4):446-56.
113 Expression of drug transporters and drug metabolizing enzymes in the bladder urothelium in man and affinity of the bladder spasmolytic trospium chloride to transporters likely involved in its pharmacokinetics. Mol Pharm. 2015 Jan 5;12(1):171-8.
114 Potency of individual bile acids to regulate bile acid synthesis and transport genes in primary human hepatocyte cultures. Toxicol Sci. 2014 Oct;141(2):538-46. doi: 10.1093/toxsci/kfu151. Epub 2014 Jul 23.
115 Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.