title: Cellular and molecular mechanisms of anti-inflammatory effect of Aflapin: a novel Boswellia serrata extract.
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. 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 (IC(50) 44.736 ng/ml) on matrix metalloproteinase-3 (MMP-3) production is 14.83% 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 as osteoarthritis or rheumatoid arthritis.
authors.affiliation: Cellular and Molecular Biology Division, Laila Impex R&D Center, Jawahar Autonagar, Vijayawada 520 007, India.
authors.forename: Krishanu
authors.initials: K
authors.lastname: Sengupta
authors.forename: Jayaprakash N
authors.initials: JN
authors.lastname: Kolla
authors.forename: Alluri V
authors.initials: AV
authors.lastname: Krishnaraju
authors.forename: Nandini
authors.initials: N
authors.lastname: Yalamanchili
authors.forename: Chirravuri V
authors.initials: CV
authors.lastname: Rao
authors.forename: Trimurtulu
authors.initials: T
authors.lastname: Golakoti
authors.forename: Smriti
authors.initials: S
authors.lastname: Raychaudhuri
authors.forename: Siba P
authors.initials: SP
authors.lastname: Raychaudhuri
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D001094:Arachidonate 5-Lipoxygenase / Q000378:metabolism; D001682:Biological Availability; D029743:Boswellia; D018929:Cell Culture Techniques; D016923:Cell Death; D045744:Cell Line, Tumor; D049109:Cell Proliferation; D002478:Cells, Cultured; D005260:Female; D005528:Foot / Q000473:pathology; D005620:Freund's Adjuvant; D006025:Glycosaminoglycans / Q000378:metabolism; D006614:Hindlimb / Q000473:pathology; D006801:Humans; D007249:Inflammation / Q000139:chemically induced / Q000188:drug therapy; D053583:Interleukin-1beta; D016859:Lipoxygenase Inhibitors / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D008297:Male; D019278:Matrix Metalloproteinase 3 / Q000378:metabolism; D010003:Osteoarthritis / Q000188:drug therapy*; D008517:Phytotherapy; D010936:Plant Extracts / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D051381:Rats; D017207:Rats, Sprague-Dawley; D017208:Rats, Wistar; D014315:Triterpenes / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism
chemical_list: C555466:Aflapin; D000894:Anti-Inflammatory Agents, Non-Steroidal; D006025:Glycosaminoglycans; D053583:Interleukin-1beta; D016859:Lipoxygenase Inhibitors; D010936:Plant Extracts; D014315:Triterpenes; D014409:Tumor Necrosis Factor-alpha; C094432:acetyl-11-ketoboswellic acid; D005620:Freund's Adjuvant; D001094:Arachidonate 5-Lipoxygenase; C511768:MMP3 protein, human; D019278:Matrix Metalloproteinase 3