U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Status:
Investigational
Source:
NCT01234506: Phase 2 Interventional Completed Oxidative Stress
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Secoisolariciresinol diglucoside (SDG) isolated from flaxseed is a lipid-lowering and antioxidant agent. It suppresses the development of hypercholesterolemic atherosclerosis in rabbits. Secoisolariciresinol diglucoside has been shown to have antioxidant and cardioprotective properties. SDG interferes with the development of different types of diseases like cardiovascular, diabetic, lupus nephritis, bone, kidney, menopause, reproduction, mental stress, immunity, atherosclerosis, hemopoietic, liver necrosis and urinary disorders due to its various biological properties including anti-inflammatory, antioxidant, antimutagenic, antimicrobial, antiobesity, antihypolipidemic and neuroprotective effects. Moreover, SDG has a defending mediator against various cancers by modulating multiple cell signaling pathways. The animal and human studies have shown the prevention role of SDG against some cancers (breast, lung and colon) as a result of its strong anti-proliferative, antioxidant, anti-oestrogenic and/or anti-angiogenic activity. It is proposed that the anticancer activity of SDG is associated with the inhibition of enzymes involved in carcinogenesis. Human studies showed the SDG as potential cardiovascular protector by mediating the mechanisms of total cholesterol, LDL-cholesterol, HDL-cholesterol, triacylglycerides and glucose metabolism. It was observed that 20 hypercholesterolaemia and hypertriglyceridaemia subjects receiving 600 mg SDG per day for 8 weeks led to significant reductions in total cholesterol, LDL-cholesterol and glucose concentrations compared with the placebo group. The animal and human studies revealed that high fat diet containing 0 · 5 to 1 · 0 % SDG reduces liver triglycerides content, serum triglycerides, total cholesterol, and insulin and leptin concentrations that resulted in significantly reduced visceral fat gain as compared to group of mice receiving high fat diet without SDG. SDG reduces C-reactive protein concentrations which are associated with insulin resistance and diabetes mellitus in type 2 diabetics. Daily consumption of low-fat muffin enriched with SDG (500 mg/day) for 6 week can reduce CRP concentrations. SDG has long acting hypotensive effect mediated through the guanylate cyclase enzyme.
Status:
Investigational
Source:
INN:salacetamide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Salacetamide is a derivative of salicylic acid. It is analgesic, anti-inflammatory and antipyretic agent.
Pravadoline is the anti-nociceptive agent, which has analgesic efficacy against postoperative pain in humans. Pravadoline inhibits the enzyme cyclooxygenase, but in contrast to cyclooxygenase-inhibiting NSAIDs does not produce gastrointestinal irritation. Pravadoline inhibited the synthesis of prostaglandins in mouse brain both in vitro and ex vivo. Pravadoline demonstrated only weak anti-inflammatory activity relative to its anti-nociceptive potency. Single doses of pravadoline were safe and effective in humans, without serious adverse events. Single oral administration of pravadoline maleate induced acute tubular necrosis in male and female beagle dogs.
Status:
Investigational
Source:
INN:hydroxytoluic acid
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Hydroxytoluic acid is a long-acting derivative of salicylate with antilipidemic properties. It shows fibrinolytic activity in human plasma by activating the fibrinolytic system and has been shown to lower plasma free fatty acid, cholesterol levels, and to raise metabolic oxygen consumption.
Status:
Investigational
Source:
INN:nicotredole
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Nicotredole (Tryptamide), similarly to ibuprofen and piroxicam, shows anti-inflammatory and analgesic properties. Tryptamide reversed pyrogen-induced hyperthermia in rats, elicited analgesic effects in rats, but not in mice, prolonged the time of hexobarbital sleep in rats and inhibited locomotor activity in rats and mice. Tryptamide has not elicited side effects on the circulatory system of rats and cats.
Status:
Investigational
Source:
INN:lofemizole [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Lofemizole is a non-steroidal anti-inflammatory drug. Lofemizole has proved to possess an interesting antiphlogistic activity in both animals and humans, associated with a favorable gastric and systemic tolerability.
Disogluside (Trillin) is an active ingredient isolated from Dioscorea nipponica Makino. Trillin reduces liver chronic inflammation and fibrosis in carbon tetrachloride (CCl4) induced liver injury in mice. Trillin exhibited protective effect on LPS-induced ALI by the regulations of related inflammatory events via the activations of Nrf2, HO-1 and NF-κB pathway. Trillin has being shown to exert protective effects against hyperlipidemia and oxidative stress. Trillin induced multinucleation in HL-60, NB4 and K562 cells, indicating it could induce mitotic arrest in these leukemia cells.
Licofelone (ML 3000) is a pyrrolizine derivative originally discovered by Merckle GmbH and developed by EuroAllaince with a unique pharmacological profile, which comprises optimal gastrointestinal tolerability and high analgesic and anti-inflammatory activity. These effects are due to balanced and selective inhibition of both cyclo-oxygenase and 5-lipoxygenase. Inhibition of 5-lipoxygenase may reduce the gastrointestinal toxicity associated with other non steroidal anti-inflammatory drugs, which only inhibit cyclooxygenase. Licofelone also has antipyretic and antiaggregatory properties. Clinical and preclinical trials were also undertaken for osteoarthritis, rheumatoid arthritis, asthma, pain and inflammation. However, development for these indications appear to have been discontinued.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



Senkyunolide A is one of the major ingredients in a traditional Chinese medicinal (TCM) herb Rhizoma Chuanxiong. This herb is derived from the dried rhizome of Ligusticum chuanxiong Hort (Umbelliferae) and is one of the most commonly used TCM herbs for the treatment of cardio and cerebrovascular diseases in China. Senkyunolide A has a low oral bioavailability. It has anti-cancer potential. Senkyunolide A may be considered as potential drug candidate for treating inflammatory processes associated with cerebrovascular diseases and related disorders based on their inhibitory activity on TNF-alpha production and TNF-alpha bioactivity.
RS25344 is a potent and selective phosphodiesterase (PDE) 4 inhibitor. It preferentially inhibits phosphorylated PDE4D. The compound demonstrated efficacy in animal models of inflammation and anaphylaxis. RS25344 inhibited eosinophil chemotaxis, increased the progressive motility of bovine spermatozoa, inhibited leukotriene B4 biosynthesis by human polymorphonuclear leukocytes.