Salsalate is a dimer of salicylic acid. Upon administration, it is metabolically hydrolyzed to salicylic acid. Salsalate is is a nonsteroidal anti-inflammatory agent for oral administration for treatment of rheumatoid arthritis, osteoarthritis and related rheumatoid disorders. In addition, salsalate is investigated for treatment of type 2 diabetes.

Carprofen is an anti-inflammatory drug developed in Japan by Nippon Roche Research Center. Carprofen, as many NSAIDs, selectively inhibits COX-2 and was shown to suppress inflammation in vitro, using osteoarthritis models. The drug was approved by FDA for human use under the name Ridamyl, however, now it is sold only for veterinary purposes and prescribed for the treatment of postoperative pain and the relief of pain and inflammation associated with osteoarthritis in dogs.

Oxyphenbutazone is a non-steroidal anti-inflammatory drug, cyclooxygenase (prostaglandin synthetase) inhibitors which was marked under brand name tandearil for the treatment rheumatic disorders such as ankylosing spondylitis, osteoarthritis, and rheumatoid arthritis. But this drug was withdrawn from markets due to bone marrow suppression.

Rutin, also called rutoside, is the glycoside flavonoid found in a certain fruits and vegetables. Most rutine-rich foods are capers, olives, buckwheat (whole grain flour), asparagus, raspberry.In a clinical trial, rutin was found to aid control of intraocular pressure in patients with primary open angle glaucoma. As a component of dietary supplement Phlogenzym, rutin is used for treatment of osteoarthritis. Rutin is also used for treatment of post-surgical swelling of the arm after breast cancer surgery. Traditionally, rutin is used to prevent mucositis due to cancer treatment, to treat blood vessel disease such as varicose veins, bleeding, hemorrhoids.

Sesamin is the most prominent lignan compound found in sesame seeds, one of the two highest sources of lignans in the human diet (the other being flax). Sesamin is catered to be a nutritional supplement that confers antioxidant and antiinflammatory effects (if touting its health properties) or possibly being an estrogen receptor modulator and fat burner (if targeting atheltes or persons wishing to lose weight). Sesamin has a few mechanisms, and when looking at it holistically it can be summed up as a fatty acid metabolism modifier. It appears to inhibit an enzyme known as delta-5-desaturase (Δ5-desaturase) which is a rate-limiting enzyme in fatty acid metabolism; inhibiting this enzyme results in lower levels of both eicosapentaenoic acid (EPA, one of the two fish oil fatty acids) as well as arachidonic acid, and this mechanism appears to be relevant following oral ingestion. The other main mechanism is inhibiting a process known as Tocopherol-ω-hydroxylation, which is the rate limiting step in the metabolism of Vitamin E; by inhibiting this enzyme, sesamin causes a relative increase of vitamin E in the body but particularly those of the gamma subset (γ-tocopherol and γ-tocotrienol) and this mechanism has also been confirmed to be active following oral ingestion. Sesamin is a potent and specific inhibitor of delta 5 desaturase in polyunsaturated fatty acid biosynthesis. Sesamin inhibits a particular CYP3A enzymes that is involved in vitamin E metabolism, where the enzyme initially ω-hydroxylates vitamin E (required step) and then the rest of vitamin E is subject to fat oxidation. By inhibiting this step, sesamin causes an increase in circulating and organ concentrations of vitamin E. Sesamin is thought to have PPARα activating potential in the liver, but it is uncertain how much practical relevance this has in humans due to this being a mechanism that differs between species.

Wogonin is an O-methylated flavone compound isolated from Scutellaria baicalensis. Wogonin is an a positive allosteric modulator of benzodiazepine site of the GABAA ion channel, and displays anxiolytic properties in animal models. It possesses anti-tumor effect in models of osteosarcoma and lung cancer. Hepatoprotective action of wogonin was demonstrated in the mouse model of alcoholic liver disease and in a model of nonalcoholic fatty liver disease, where it was shown that wogonin upregulates PPAR-gamma and PPARalpha respectively. Wogonin possess chondroprotective action which was demonstrated in models of osteoarthritis.

Harpagoside is an anti-inflammatory small molecule natural product originally isolated from the Harpagophytum procumbens (Devil's Claw) root, but can be isolated from other plants such as Crophularia ningpoensis Hemsl (Figwort). Treatment of HepG2 cells with Harpagoside demonstrated suppression of NF-κB nuclear translocation and degradation of IκB-α, blocking NF-κB activation. Multiple anti-inflammatory cellular effects were correlated with this blockade, as Harpagoside was observed to inhibit the expression of inflammation-mediating enzymes cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS), and to reduce lipopolysaccharide-induced mRNA levels. The suppression of NF-κB activation is indicated as the mechanism beneath the anti-inflammatory effects of Harpagoside. Harpagoside is widely used as a folk remedy to treat rheumatic complaints.

Psoralen, the active ingredient of Fructus Psoraleae (FP) the dried ripe fruit of Psoralea corylifolia L., which is used in Chinese herbal medicine. Psoralen promotes chondrocyte proliferation by activating the Wnt/β-catenin signaling pathway and can play an important role in the treatment of osteoarthritis. Besides, this compound stimulates osteoblast proliferation through the activation of NF-κB and MAPK signaling and may be a viable therapeutic agent in the treatment of osteoporosis.

GALLIPRANT® (grapiprant tablets) is a prostaglandin E2 (PGE2) EP4 receptor antagonist; a non-cyclooxygenase (COX) inhibiting, non-steroidal antiinflammatory drug (NSAID) in the piprant class. Grapiprant is indicated for the control of pain and inflammation associated with osteoarthritis in dogs. It is approved for veterinary use, but it is in phase II development in Japan for the treatment of chronic inflammatory pain, including osteoarthritis and rheumatoid arthritis. Grapiprant shows similar in vitro binding affinity (Ki) for the rat and dog EP4 receptor, 20 and 24 nM, respectively.

Bornyl acetate is the main volatile constituent in numerous conifer oils and some Chinese traditional herbs, which has displayed an anti-inflammatory effect. In addition was shown, that this compound had therapeutic potentials for the osteoarthritis and may be developed as a preventive agent for lung inflammatory diseases. In combination with 5-fluorouracil, bornyl acetate possesses the anticancer activity by inducing apoptosis, DNA fragmentation as well as G2/M cell cycle arrest.