Molecular osteoarthritis targeting of select nutraceuticals. Research findings support the concept that nutraceuticals can be used in a complementary manner to “shoot” multiple osteoarthritis molecular targets.
Nutraceuticals: Potential for Chondroprotection and Molecular Targeting of Osteoarthritis
Daniel J. Leong, Marwa Choudhury , David M. Hirsh, John A. Hardin, Neil J. Cobelli and Hui B. Sun
Int. J. Mol. Sci. 2013, 14(11), 23063-23085
Abstract
Osteoarthritis (OA) is a degenerative joint disease and a leading cause of adult disability. There is no cure for OA, and no effective treatments which arrest or slow its progression. Current pharmacologic treatments such as analgesics may improve pain relief but do not alter OA disease progression. Prolonged consumption of these drugs can result in severe adverse effects. Given the nature of OA, life-long treatment will likely be required to arrest or slow its progression. Consequently, there is an urgent need for OA disease-modifying therapies which also improve symptoms and are safe for clinical use over long periods of time. Nutraceuticals—food or food products that provide medical or health benefits, including the prevention and/or treatment of a disease—offer not only favorable safety profiles, but may exert disease- and symptom-modification effects in OA. Forty-seven percent of OA patients use alternative medications, including nutraceuticals. This review will overview the efficacy and mechanism of action of commonly used nutraceuticals, discuss recent experimental and clinical data on the effects of select nutraceuticals, such as phytoflavonoids, polyphenols, and bioflavonoids on OA, and highlight their known molecular actions and limitations of their current use. We will conclude with a proposed novel nutraceutical-based molecular targeting strategy for chondroprotection and OA treatment.
Conclusions
Nutraceuticals have been demonstrated to effectively suppress over activated inflammation and catabolic activity, and oxidative stress-induced deleterious responses. The suppression of inflammation and catabolic activity, in particular, are important properties of drugs targeting OA.
Current pre-clinical and clinical trial data are promising, and show that individual nutraceutical compounds exert beneficial effects on OA, such as relieving pain and improving function. Their effects on disease modification have not yet been clearly demonstrated, or are still under investigation. Based on the effectiveness and actions of these nutraceutical compounds, efficacy of using an individual compound to treat a complex and chronic disease with multiple risk factors such as OA, may be limited. Future nutraceutical-based approaches may require a combination of compounds, and the selected compounds should: exert active effects on OA targets such as inflammation and catabolism, suppress oxidative stress and relieve chronic pain, as well as exerting complementary, additive, and/or synergistic anti-arthritic effects with other compounds within the formulation. These novel nutraceutical-based compound formulations which “shoot” many of the OA molecular targets (Figure) may serve as a therapeutic strategy for a new generation of nutraceuticals in OA prevention and treatment.
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