Table 2.

12-Lipoxygenase Inhibitors and Targets

Inhibitor	Origin	Target(s)
CDC		12-LOX in human platelets; 5-LO in rats [91-93], 5-LO in human polymorphonuclear leukocytes and monocytes [93, 94]
Baicalein	Scutellariae roots	human reticulocyte 15-LOX and 12-LOX in platelets [27, 95, 96] , prolyl-4 hydroxylases (PHDs) in human hepatoma cells and mouse fibroblasts 3T3-L1 [97]; Raf-1 mediated phosphorylation of MEK-1 in rat glioma cells [98]; phosphatidylinositol 3-kinase (PI3K) inhibitor in human cancer cell lines e.g. colorectal, lung, gastric, ovarian, renal, melanoma, breast, glioma, prostate [99]
(NDGA)	Creosote bush	5-LOX, 12-LOX prostaglandin [100], inhibits HER2 and IGF-1 receptor tyrosine kinases in human breast cancer cells, [101, 102]; neutrophil phospholipase A2 [103]
BW755C	Phenidone analogue	dual inhibitor 12-LOX and COX-1 in platelets [104]; 5-LOX in leukocytes [105]
AA-861		5-LO in human and guinea pig peritoneal leukocytes [106]; 12-LO in mouse epidermis [107, 108]; tyrosine phosphatase of the receptor tyrosine kinase signaling pathway in mouse embryonic fibroblasts [109]
Timegadine		COX and LO in rabbit, rat, bovine, horse platelets [110-112] [110]
ETYA		12-LOX [113]; COX-1 [114-116], cytochrome P-450 ensymes in rat thyroid FRTLA-5 cells [117]; neutrophil phospholipase A2 [103]; Δ-6 desaturase in mouse hepatic cells [118]
Esculetin		12-LOX in human platelets [61, 119]; 5-LO [120],
BHPP	Hydroxamic acids	12/15-LO in rats and mice [121]
Panaxynol	a polyacetylene compound from Ginseng radix, Fang-Feng and Panx ginseng	COX, leukocyte 12-LO and platelet 12-LO in humans and porcine. 15-LO in rabbit [122]; cholesterol acyltransferase in rat liver [123]; 15-hydroxyprostaglandin dehydro- genase (PGDH) in rabbit gastric mucosa [124]
Falcarindiol	Panaxynol analog	leukocyte 12-LO and platelet 12-LO in human, and 15-LO [122]in rabbit reticulocyte; GABA degradative enzymes GABA transaminase (GABA-T) [125]
BW A4C	acetohydroaxmic acid	12- and 15-LO in bovine leukocyte, and 15-LO human leukocyte [126, 127]; secretory type II phospholipase A2 (sPLA2-II) in guinea-pig alveolar macrophages [128]
Hinokitiol	Derived from tropolone, a constituent of the wood Chymacyparis taiwanesis	12-LOX in human platelet [129, 130]; HIF-specific prolyl-4-hydroxylases (PHDs) [131] in human HepG2 hepatoma and HeLa cervical epithelial cells; metalloprotease in injects [132]
KY11449	Derived from Streptoverticillium hadanonense	Bovine 12-LO, rat basophilic leukemia cells (RBL-1) 12-LO [133]
Gossypol	Polyphenolic derived compound from cotton plant	5-LO and 12-LO [134] in human neutrophils and platelets, and rat basophilic leukemia cells (RBL-1) [135]; 11β-hydroxysteroid dehydrogenase (11β-HSD) activity in human and rat kidney [136]; Bcl-2 in human ovarian cancer cell lines OV433 and TOV112D [137]
Catechins	Green tea leaves	soybean lipoxygenases and 12-LO in rabbit and human [130]; tumor-associated NOX (tNOX) in human mammary adenocarcinoma cells (BT-20) and HeLa [138]
Quercetin		LOs in rat mast cells, 12-LOX, and 5-LO in RBL-1[139]; neutrophil phospholipase A2 [103]; P-glycoprotein-mediated efflux transport and CYP3A4 enzyme [140], human glycolate oxidase [141], sPLA2 in human platelets [142]
MK 866		12-LOX in human platelets [127] , 5-LO in rats [143, 144]
12-LOX small molecule inhibitors	Small molecule screen	selectively targets 12-LOX in human platelets [145]