Cellular and molecular mechanisms of anti-inflammatory effect of Aflapin: a novel Boswellia serrata extract
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There is significant number of evidences suggesting the anti-inflammatory properties of gum resin extracts of Boswellia serrata containing 3-O-acetyl-11-keto-β-boswellic acid (AKBA) and their promising potential as therapeutic interventions against inflammatory diseases such as osteoarthritis (OA). Unfortunately, the poor bioavailability of AKBA following oral administration might limit the anti-inflammatory efficacy of standardized Boswellia extract(s). To address this issue, we describe a novel composition called Aflapin, which contains B. serrata extract enriched in AKBA and non-volatile oil portion of B. serrata gum resin. Our observations show that the availability of AKBA in systemic circulation of experimental animals is increased by 51.78% in Aflapin-supplemented animals, in comparison with that of 30% AKBA standardized extract or BE-30 (5-Loxin®). Consistently, Aflapin confers better anti-inflammatory efficacy in Freund’s Complete Adjuvant (FCA)-induced inflammation model of Sprague–Dawley rats. Interestingly, in comparison with BE-30, Aflapin® also provides significantly better protection from IL-1β-induced death of human primary chondrocytes and improves glycosaminoglycans production in human chondrocytes. In Tumor necrosis factor alpha (TNFα)-induced human synovial cells, the inhibitory potential of Aflapin (IC50 44.736 ng/ml) on matrix metalloproteinase-3 (MMP-3) production is 14.83% better than that of BE-30 (IC50 52.528 ng/ml). In summary, our observations collectively suggest that both the Boswellia products, BE-30 (5-Loxin®) and Aflapin, exhibit powerful anti-inflammatory efficacy and anti-arthritic potential. In particular, in comparison with BE-30, Aflapin provides more potential benefits in recovering articular cartilage damage or protection from proteolytic degradation due to inflammatory insult in arthritis such as osteoarthritis or rheumatoid arthritis.
Keywords3-O-acetyl-11-keto-β-boswellic acid Aflapin Boswellia serrata Chondrocytes Matrix metalloproteinase-3 Osteoarthritis
We sincerely thank Sri G Ganga Raju, Chairman; Mr. G Rama Raju, Director; and Mr. B. Kiran, CEO of Laila Group of Industries, India for their generous support and encouragements. We also thank Mr. K Gopal Rao for his help in analyzing serum samples for the bio-availability study. This study was supported by Laila Nutraceuticals, Vijayawada, India.
The authors declare there are no competing interests.
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