PMID- 21479939 OWN - NLM STAT- MEDLINE DCOM- 20111021 LR - 20240109 IS - 1573-4919 (Electronic) IS - 0300-8177 (Linking) VI - 354 IP - 1-2 DP - 2011 Aug TI - Cellular and molecular mechanisms of anti-inflammatory effect of Aflapin: a novel Boswellia serrata extract. PG - 189-97 LID - 10.1007/s11010-011-0818-1 [doi] AB - There is significant number of evidences suggesting the anti-inflammatory properties of gum resin extracts of Boswellia serrata containing 3-O-acetyl-11-keto-beta-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((R))). 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((R)) also provides significantly better protection from IL-1beta-induced death of human primary chondrocytes and improves glycosaminoglycans production in human chondrocytes. In Tumor necrosis factor alpha (TNFalpha)-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((R))) 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. FAU - Sengupta, Krishanu AU - Sengupta K AD - Cellular and Molecular Biology Division, Laila Impex R&D Center, Jawahar Autonagar, Vijayawada 520 007, India. FAU - Kolla, Jayaprakash N AU - Kolla JN FAU - Krishnaraju, Alluri V AU - Krishnaraju AV FAU - Yalamanchili, Nandini AU - Yalamanchili N FAU - Rao, Chirravuri V AU - Rao CV FAU - Golakoti, Trimurtulu AU - Golakoti T FAU - Raychaudhuri, Smriti AU - Raychaudhuri S FAU - Raychaudhuri, Siba P AU - Raychaudhuri SP LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't DEP - 20110411 PL - Netherlands TA - Mol Cell Biochem JT - Molecular and cellular biochemistry JID - 0364456 RN - 0 (Aflapin) RN - 0 (Anti-Inflammatory Agents, Non-Steroidal) RN - 0 (Glycosaminoglycans) RN - 0 (Interleukin-1beta) RN - 0 (Lipoxygenase Inhibitors) RN - 0 (Plant Extracts) RN - 0 (Triterpenes) RN - 0 (Tumor Necrosis Factor-alpha) RN - 0 (acetyl-11-ketoboswellic acid) RN - 9007-81-2 (Freund's Adjuvant) RN - EC 1.13.11.34 (Arachidonate 5-Lipoxygenase) RN - EC 3.4.24.17 (MMP3 protein, human) RN - EC 3.4.24.17 (Matrix Metalloproteinase 3) SB - IM MH - Animals MH - Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics/*pharmacology/therapeutic use MH - Arachidonate 5-Lipoxygenase/metabolism MH - Biological Availability MH - *Boswellia MH - Cell Culture Techniques MH - Cell Death MH - Cell Line, Tumor MH - Cell Proliferation MH - Cells, Cultured MH - Female MH - Foot/pathology MH - Freund's Adjuvant MH - Glycosaminoglycans/metabolism MH - Hindlimb/pathology MH - Humans MH - Inflammation/chemically induced/drug therapy MH - Interleukin-1beta MH - Lipoxygenase Inhibitors/pharmacokinetics/*pharmacology/therapeutic use MH - Male MH - Matrix Metalloproteinase 3/metabolism MH - Osteoarthritis/*drug therapy MH - *Phytotherapy MH - Plant Extracts/pharmacokinetics/*pharmacology/therapeutic use MH - Rats MH - Rats, Sprague-Dawley MH - Rats, Wistar MH - Triterpenes/pharmacokinetics/*pharmacology/therapeutic use MH - Tumor Necrosis Factor-alpha/metabolism EDAT- 2011/04/12 06:00 MHDA- 2011/10/22 06:00 CRDT- 2011/04/12 06:00 PHST- 2010/11/15 00:00 [received] PHST- 2011/04/05 00:00 [accepted] PHST- 2011/04/12 06:00 [entrez] PHST- 2011/04/12 06:00 [pubmed] PHST- 2011/10/22 06:00 [medline] AID - 10.1007/s11010-011-0818-1 [doi] PST - ppublish SO - Mol Cell Biochem. 2011 Aug;354(1-2):189-97. doi: 10.1007/s11010-011-0818-1. Epub 2011 Apr 11.