Docebenone (AA-861) is a potent, selective and orally active 5-LO (5-lipoxygenase) inhibitor. T. vaginalis-derived secretory products (TvSP)-induced IL-8 production was efficiently inhibited when trichomonads were pretreated with docebenone. Docebenone increased [Ca(2+)](i) in Madin Darby canine kidney cells by releasing Ca(2+) from multiple internal stores in a manner independent of the formation of inositol-1,4,5-trisphosphate, followed by Ca(2+) entry from external medium. In animal model, it was shown that docebenone may prove useful in the treatment of acute pancreatitis. Docebenone showed a dose-dependent inhibition of slow reacting substance of anaphylaxis (SRS-A) release, with no effect on histamine release from passively sensitized guinea pig, monkey (M. irus) and human lung fragments. It markedly suppresses biosynthesis of the leukotrienes. This drug inhibits the release of histamine as well as SRS-A from lung fragments of anaphylactic monkey (M. mulatta) and in the Ca ionophore-stimulated rat peritoneal cavity. AA-861 suppressed the anaphylactically-induced airway resistance in mepyramine- and cimetidine-treated guinea pigs. These results suggest that AA-861 may be clinically effective for treating allergy-related asthma by modulating the 5-lipoxygenase pathway and that an inhibitory mechanism of histamine release by AA-861 may be present in some species. Docebenone has shown anti-inflammatory effects in several animal models following local dosing: phorbol ester-induced oedema and neutrophil influx in mouse skin, arachidonate-induced plasma extravasation in rabbit skin, the pleural reversed passive Arthus reaction in rats.

4-(3-((4-(2-Methyl-1H-Imidaz-1-yl)Phenyl)Sulfanyl)Phenyl)Tetrahydro-2H-Pyran-4-Carboxamide, better known as CJ13610, is an orally active inhibitor of 5-lipoxygenase. Originally discovered by deCode Genetics, and later developed by Pfizer, CJ13610 has shown promise in preclinical models for pain. The compound was investigated in phase II clinical trials for asthma and chronic obstructive pulmonary disease; however, these efforts have been discontinued.

Β-boswellic acid (β-BA) is one of the active triterpenoid compounds from the extract of boswellia serrate, known in Indian Ayurvedic system of medicine as Salai guggal. Beta-boswellic acid has been indicated in apoptosis of cancer cells. β-boswellic acid belonds to class of boswellic acids exhibiting anti-inflammatory activities, which are in the phase II clinical trial for study of safety and tolerability in subjects with Relapsing Remitting Multiple Sclerosis.

Asarinin, an urofuran lignan, is the epimer of sesamin. Asarinin is listed in Chinese Pharmacopoeia and used as a quality control (QC) index of crude herbs by the State Food and Drug Administration of China. Asarinin exhibits several biological activities such as decreasing cholesterol levels, exhibiting antihypertensive and antiangiogenic properties and providing immunosuppressive and hepatoprotective activities. Asarinin can also inhibit myocardial injury in metabolic syndrome of rats and decrease the possibility of acute heart transplant rejection. Sesamin was first isolated from sesame seed oil, while asarinin was first isolated from prickly ash bark. Both sesamin and asarinin have been shown to act as insecticidal synergists with pyrethrins.

Wedelolactone, a compound originally extracted from Eclipta alba, has been shown to inhibit caspase-11, which is a key regulator of proinflammatory cytokine IL-1β maturation and pathological apoptosis. Mechanistic studies suggest that caspase-11 is inhibited by reduction of NF-κB-mediated transcription. Furthermore, this compound has been shown to inhibit IKKγ, a kinase that is crucial for activation of NF-κB, as well as IKK α and IKK β. Weldelolactone also displays potent trypsin inhibition capacities. Additional studies suggest that Wedelolactone contains antagonistic properties towards two PLA2 myotoxins that were isolated from Agkistrodon contortix laticinctus and Crotalus virdis virdis. This agent has also been noted to contain antihepatotoxic behavior consequentially protecting primary cultured liver cells from the toxicity of CC14, Phalloidin, and galactosamine, and inhibit 5-lipoxygenase (5-LO) activity in porcine leukocytes. Wedelolactone was shown to act as anti-cancer agent for breast and prostate carcinomas in vitro and in vivo targeting multiple cellular proteins including androgen receptors, 5-lipoxygenase and topoisomerase IIα. It is cytotoxic to breast, prostate, pituitary and myeloma cancer cell lines in vitro at uM concentrations.

1-Phenyl-3-pyrazolidinone (phenidone) is a dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX). Phenidone inhibits both the LO (lipoxygenase) and Cox (cyclooxygenase) pathways, the synthesis of Fos-related antigen protein, and is described as an anti-inflammatory and anti-oxidant compound. Phenidone is a potent hypotensive agent in the spontaneously hypertensive rat. Phenidone was also the best in suppressing LPS induced neurotoxicity, where the more potent neuroprotection by phenidone may be attributable to the synergistic effects of dual COX and LOX inhibition. Therefore, dual inhibitors of COX and LOX, such as phenidone, represent valuable candidates for the development of novel drugs for inflammation-related neurodegenerative disorders including PD.