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Cellular and molecular mechanisms of anti-inflammatory effect of Aflapin: a novel Boswellia serrata extract

http://link.springer.com/article/10.1007/s11010-011-0818-1
First Online: 11 April 2011

Krishanu SenguptaJayaprakash N. KollaAlluri V. KrishnarajuNandini YalamanchiliChirravuri V. RaoTrimurtulu GolakotiSmriti RaychaudhuriSiba P. Raychaudhuri

Abstract
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.[color:#33FF33] 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®). [/color]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.

Comparative Efficacy and Tolerability of 5-Loxin® and Aflapin® Against Osteoarthritis of the Knee: A Double Blind, Randomized, Placebo Controlled Clinical Study

http://www.medsci.org/v07p0366.htm
Int J Med Sci 2010; 7(6):366-377. doi:10.7150/ijms.7.366

Krishanu Sengupta1, Alluri V. Krishnaraju1, Amar A. Vishal2, Artatrana Mishra3, Golakoti Trimurtulu1, Kadainti VS Sarma4, Smriti K Raychaudhuri5, Siba P Raychaudhuri5

Conclusion

In summary, the present study provides the evidence in support of the potential efficacy and tolerability of 5-Loxin® and Aflapin® in subjects with OA; 5-Loxin® and Aflapin significantly improved joint function. Aflapin exhibited better therapeutic efficacy over 5-Loxin® at 100 mg/day; it reduces pain rapidly, as early as after 1 week of treatment. Furthermore, in vitro studies also provide evidences that compared to 5-Loxin, Aflapin is capable of inhibiting cartilage degrading enzyme MMP-3 and has the potential to regulate the inflammatory component in by inhibiting ICAM-1. Most importantly, we have observed that 5-Loxin® and Aflapin® are safe for human consumption, even for long term supplementation. 5-Loxin® and Aflapin® are promising alternative therapeutic options, that may be used as nutritional supplements for management of OA.