SenguptaK,KrishnarajuAV, VishalAA,MishraA,TrimurtuluG,SarmaKV,RaychaudhuriSK, RaychaudhuriSP. Comparative efficacy andtolerability of 5-Loxin and Aflapin against osteoarthritis of the knee: adouble blind, randomized, placebo controlled clinical study. Int J Med Sci. 2010 Nov1;7(6):366-77.
Aflapin(®) is a novel synergistic composition derived from Boswellia serrata gum resin (Indian Patent Application No. 2229/CHE/2008). Aflapin is significantly better as an anti-inflammatory agent compared to the Boswellia extracts presently available in the market. A 90-day, double-blind,randomized, placebo-controlled study was conducted to evaluate the comparative efficacy and tolerability of 5-Loxin(®)and Aflapin(®) in the treatment ofosteoarthritis (OA) of the knee (Clinical trial registration number: ISRCTN80793440). Sixty OA subjects were included in the study. The subjects received either 100 mg (n=20) of 5-Loxin(®) or 100 mg (n=20) of Aflapin(®) or a placebo (n=20)daily for 90 days. Each patient was evaluated for pain and physical functions by using the standard tools (visual analog scale, Lequesne's Functional Index,and Western Ontario and McMaster Universities Osteoarthritis Index) at the baseline (day 0), and at days 7, 30, 60 and 90. A battery of biochemical parameters in serum, urine and hematological parameters in citrated whole blood were performed to assess the safety of 5-Loxin(®) and Aflapin(®) in OAsubjects. Fifty seven subjects completed the study. At the end of the study,both 5-Loxin(®) and Aflapin conferred clinically and statistically significantimprovements in pain scores and physical function scores in OA subjects. Interestingly, significant improvements in pain score and functional abilitywere recorded as early as 7 days after initiation of the study in the treatment group supplemented with 100 mg Aflapin. Corroborating the improvements in pain scores in treatment groups, our in vitro studies provide evidences that Aflapin(®) is capable of inhibiting cartilage degrading enzyme MMP-3 and hasthe potential to regulate the inflammatory response by inhibiting ICAM-1.Aflapin(®) and 5-Loxin(®) reduce pain and improve physical functions significantly in OA subjects. Aflapin exhibited better efficacy compared to5-Loxin(®). In comparison with placebo, the safety parameters were almost unchangedin the treatment groups. Hence both 5-Loxin(®) and Aflapin(®) are safe forhuman consumption.
*Aflapin(®) is the same as AprèsFLEX™
Highlights of study:
• Significant improvement of VAS (visual analog scale) andLFI (Lequesne Algo Functional Index Score) pain scores compared to 5-LOXIN® inas early as 7 days.
• Highly significant reduction in WOMAC-pain andWOMAC-function scores (Western Ontario and McMaster Universities), compared to5-LOXIN®.
• 45% better reduction of overall pain scores compared to5-LOXIN®.
• Significant reduction in serum MMP-3 (matrixmetalloprotein 3) levels compared to baseline values.
SenguptaK, KollaJN, KrishnarajuAV, YalamanchiliN, RaoCV, GolakotiT, RaychaudhuriS, RaychaudhuriSP. Cellular and molecular mechanisms of anti-inflammatory effect of Aflapin: a novel Boswellia serrata extract.
Mol Cell Biochem. 2011Aug;354(1-2):189-97. Epub 2011 Apr 11.
There is significant number of evidences suggesting the anti-inflammatorypropertiesof gum resin extracts of Boswellia serrata containing 3-O-acetyl-11-keto-β-boswellicacid (AKBA) and their promising potential as therapeutic interventions againstinflammatory 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. serratagum resin. Our observations show that the availability of AKBA in systemic circulation of experimental animals is increased by 51.78% in Aflapin-supplemented animals, incomparison with that of 30% AKBA standardized extract or BE-30 (5-Loxin(®)).Consistently, Aflapin confers better anti-inflammatoryefficacy 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 andimproves glycosaminoglycans production in human chondrocytes. In Tumor necrosis factor alpha (TNFα)-induced human synovial cells, the inhibitory potential of Aflapin(IC(50) 44.736 ng/ml) on matrix metalloproteinase-3 (MMP-3) production is14.83% better than that of BE-30 (IC(50) 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 asosteoarthritis or rheumatoid arthritis.