Original article from Designs for Health

Arthritis is among the most common joint disorders and is characterized by cartilage degeneration. Osteoarthritis, in particular, is the primary cause of mobility problems in the elderly. An activated immune system and heightened inflammatory process is at the core of arthritis, leading to joint pain, swelling, and immobility.

Pharmaceuticals have been the traditional option for managing the pain associated with arthritis, but long-term non-steroidal anti-inflammatory drug (NSAID) use comes with its own bag of side effects. Therefore, interest in complementary and alternative methods for managing arthritic symptoms has been growing and a plethora of research has been conducted with these goals in view.

Among the various options for alternative therapeutic approaches for managing arthritis, flavonoids are among the most well-studied. They have been shown to target cartilage and work to reduce inflammation and an activated immune response by inhibiting regulatory enzymes involved in arachidonic acid metabolism – the pathway for proinflammatory cytokine production. Additionally, flavonoids have been shown in research to downregulate matrix metalloproteinases (MMP) enzymes that are involved in breaking down cartilage. Since pain is rooted in inflammation and immune activation, flavonoids indirectly help to manage pain by focusing on the root cause of joint pain.

The Flavonoid Baicalin

Baicalin is a flavonoid compound sourced from the roots of Scutellaria baicalensis. Animal studies suggest that it possesses powerful anti-inflammatory properties and may protect against arthritis. Significantly reduced pain thresholds and reduced clinical arthritic scores were the clinical outcomes of a randomized controlled animal study that sought to determine the effects of baicalin in a collagen-induced arthritis model. In this study, baicalin was shown to reduce proinflammatory cytokines (including TNF-α, IL-1β, and IL-6), inhibit matrix metalloproteinases (MMPs), attenuate inflammatory markers (such as iNOS and COX-2), and downregulate JAK1/STAT3 signaling, which causes apoptosis of inflammatory cells. By reducing the infiltration of activated inflammatory cells into the joint synovium, pain and arthritic symptoms improved.

In another randomized controlled animal study, baicalin was administered for 42 days in a collagen-induced arthritis model. As in the previous study, the flavonoid was able to suppress the production of several cytokines, including tumor necrosis factor α (TNF-α), IL-6,IL-17, and IL-1β, reducing the severity of the inflammation-driven symptoms of arthritis. Baicalin treatment also lowered the expressions of p-JAK2/JAK2 and p-STAT3/STAT3, which are cytokine signaling pathways, and suppressed Th17 cells, which are the major components of the adaptive immune response system.

In vivo studies on human osteoarthritis chondrocytes also show baicalin significantly inhibits the IL-1β-induced production of nitric oxide (NO) and prostaglandin E2, expression of COX-2, iNOS, MMP-3, and MMP-13, as well as the degradation of aggrecan (cartilage-specific proteoglycan core protein) and collagen-II. Furthermore, baicalin dramatically suppressed IL-1β-stimulated NF-κB activation. Collectively, these actions protect against osteoarthritis and its accompanying symptoms.

A More Potent Blend

The flavonoid of Scutellaria baicalensis holds may promises for those with arthritis, but when combined with the flavonoids of another botanical – Acacia catechu – the effects may be even more dramatic; particularly for those struggling with osteoarthritis, according to the research. The combined flavonoids of these botanical species act much like a traditional NSAID, functioning to help inhibit COX-2, proinflammatory cytokines (interleukins), and TNF-α. The clinical outcome of these actions is reduced pain and joint stiffness, leading to improved range of motion and mobility. In a double blind randomized controlled study of 252 otherwise healthy, overweight or obese men and women aged 40 to 90 years old with clinically diagnosed mild to moderate bilateral or unilateral osteoarthritis of the knee, subjects received either 440 mg of naproxen sodium per day or 500 mg of a supplement containing extracts of Scutellaria baicalensis and Acacia catechu. Subjects took the capsules for 1 week, after which pain, range of motion, and physical activity were reanalyzed and compared with a baseline measurement. Serum interleukins 1β and 6, tumor necrosis factor-α, C-reactive protein, and hyaluronic acid were also compared. The outcomes indicated that the group receiving the botanical blend experienced a significant reduction in perceived pain and a significant increase in mean range of motion. Both groups experienced a significant reduction in stiffness.

Individuals experiencing the pain, inflammation, and immobility associated with arthritis do not have to resign to traditional pharmaceuticals that are accompanied by a host of side effects, such as gastrointestinal distress. Flavonoids such as baicalin and catechin flavonoids extracted from Acacia catechu have proven to be useful in helping to manage the pain and inflammation associated with arthritis without accompanying side effects, offering a welcoming alternative therapy.