Studies: Clinicals & Literature on Univestin™, and the anti-inflammatory and analgesic effects of Scutellaria baicalensis & Acacia catechu

A number of studies have been undertaken focussing on the effective properties of Univestin™ — Cararthron^®'s active ingredient — and the anti-inflammatory and analgesic effects of Scutellaria baicalensis & Acacia catechu, concerning their use in the treatment of osteoarthritis and rheumatoid arthritis.

A selection of these clinical scientific articles, and their abstracts are listed below:

Safety Information

• B.P. Burnett, Q. Jia, Y. Zhao, and R.M. Levy, (2007) A Medicinal Extract of Scutellaria baicalensis and Acacia catechu Acts as a Dual Inhibitor of Cyclooxygenase and 5-Lipoxygenase to Reduce Inflammation. Journal of Medicinal Food.
  Abstract
  
  A mixed extract containing two naturally occurring flavonoids, baicalin from Scutellaria baicalensis and catechin from Acacia catechu, was tested for cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) inhibition via enzyme, cellular, and in vivo models. The 50% inhibitory concentration for inhibition of both ovine COX-1 and COX-2 peroxidase enzyme activities was 15 μg/mL, while the mixed extract showed a value for potato 5-LOX enzyme activity of 25 μg/mL. Prostaglandin E2 generation was inhibited by the mixed extract in human osteosarcoma cells expressing COX-2, while leukotriene production was inhibited in both human cell lines, immortalized THP-1 monocyte and HT-29 colorectal adenocarcinoma. In an arachidonic acid-induced mouse ear swelling model, the extract decreased edema in a dose-dependent manner. When arachidonic acid was injected directly into the intra-articular space of mouse ankle joints, the mixed extract abated the swelling and restored function in a rotary drum walking model. These results suggest that this natural, flavonoid mixture acts via “dual inhibition” of COX and LOX enzymes to reduce production of pro-inflammatory eicosanoids and attenuate edema in an in vivo model of inflammation.
• B.P. Burnett, S. Silva, M.H. Mesches, S. Wilson, Q. Jia, Safety Evaluation of a Combination, Defined Extract of Scutellaria baicalensis and Acacia catechu
  Abstract
  
  A combined extract containing primarily baicalin from Scutellaria baicalensis and (+)- catechin from Acacia catechu used in both joint supplements and a prescription medical food was tested for safety. Cytotoxicity testing in THP-1 monocytes showed limited cell death compared to NSAIDs. Acute and subchronic toxicity testing demonstrated no abnormalities in any toxicological endpoints examined including animal body weights, gross organ pathology and tissue histology, and blood chemistries or serology. The extract, when dosed in Fischer 344 rats, a model for gastric toxicity of NSAIDs, showed no evidence of ulceration. No mutagenicity or drug interactions were seen by AMES and CYP450 enzyme inhibition, respectively. When the extract was compared with placebo after administration to a healthy human population, no changes in blood chemistry or serology were observed. Based on these findings, the combined extract with baicalin and catechin appears to possess a safety profile that justifies further testing in humans.

Anti-Inflammatory Action

• B.P. Burnett, Y. Zhao, Q. Jia, M.H. Mesches, A Combination of Free-B-Ring Flavonoid and Flavan, Anti-Inflammatory Plant Extract Maintains Memory and Speed of Processing in Animal and Human Clinical Models
  Abstract
  
  Over 1200 plant extracts were screened for novel cyclooxygenase (COX) and lipoxygenase (LOX) inhibitors. Two polyphenol extracts derived from the roots of Scutellaria baicalensis and heartwoods of Acacia catechu containing Free-B-Ring flavonoids and flavans, respectively, were combined into a proprietary blend called UP326. UP326 also induced a down-regulation of cox-2, interleukin-1β (il-1β), tumor necrosis factor-α (tnfα), and interleukin-6 (il-6) gene expression concomitant with a decrease in nuclear factor kappa B (nfκb) mRNA levels in cells exposed to lipopolysaccharide (LPS). UP326 had a high ORAC value of 5,517 μmole TE/g indicating a strong antioxidant capacity. We used a radial arm water maze (RAWM) and contextual fear conditioning (CFC) to assess the effect of UP326 fed to aged Fischer (F344) male rats for changes in memory and learning. In a separate human clinical trial, test subjects administered 300 mg of UP326 per day for 30 days showed marked improvement in speed and accuracy of processing complex information and reduced their standard deviation of performance compared to baseline and the placebo group. This data suggests that UP326 might maintain memory, help sustain speed of processing, and reduce the number or memory errors as we age.

Clinical Data

• R.M. Levya, R. Saikovskyb, E. Shmidtc, A. Khokhlovd, B.P. Burnett, (2009) Flavocoxid is as effective as naproxen for managing the signs and symptoms of osteoarthritis of the knee in humans: a short-term randomized, double-blind pilot study, Nutrition Research Journal
  Abstract
  
  Flavocoxid (Limbrel), a proprietary mixture of flavonoid molecules (baicalin and catechin), was tested against a traditional nonsteroidal anti-inflammatory drug, naproxen, for the management of the signs and symptoms of moderate osteoarthritis (OA) in humans. Discomfort and global disease activity were used as the primary end points, and safety assessments were also taken for both treatments as a secondary endpoint. In this double-blind study, 103 subjects were randomly assigned to receive either flavocoxid [500 mg twice daily (BID)] or naproxen (500 mg BID) in a 1-month onset of action trial. Outcome measures included the short Western Ontario and McMaster University Osteoarthritis Index, subject Visual Analogue Scale for discomfort and global response, and investigator Visual Analogue Scale for global response and fecal occult blood. Both flavocoxid and naproxen showed significant reduction in the signs and symptoms of knee OA (P ≤ .001). There were no statistically detectable differences between the flavocoxid and naproxen groups with respect to any of the outcome variables. Similarly, there were no statistically detectable differences between the groups with respect to any adverse event, although there was a trend toward a higher incidence of edema and nonspecific musculoskeletal discomfort in the naproxen group. In this short-term pilot study, flavocoxid was as effective as naproxen in controlling the signs and symptoms of OA of the knee and would present a safe and effective option for those individuals on traditional nonsteroidal anti-inflammatory drugs or cyclooxygenase-2 inhibitors. A low incidence of adverse events was reported for both groups.

Compiled Abstracts

• Compiled Abstracts of Clinical & Scientific Articlesfor the safety and efficacy of Scutellaria baicalensis & Acacia catechu.
  Abstract
  
  • Flavocoxid/Ingredients
  • Ingredients Class (flavonoids)
  • Mode of Action
  • Other Abstracts of Interest