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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 (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.

A new dimeric withanolide, ashwagandhanolide (1), was isolated from the roots of an Ayurvedic medicinal herb, Withania somnifera. A detailed spectroscopic evaluation revealed its identity as a dimer with an unusual thioether linkage. Compound 1 displayed growth inhibition against human gastric (AGS), breast (MCF-7), central nervous system (SF-268), colon (HCT-116), and lung (NCI H460) cancer cell lines, with IC50 values in the range 0.43-1.48 microg/mL. In addition, it inhibited lipid peroxidation and the activity of the enzyme cyclooxygenase-2 in vitro.

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Investigation of the methanol extract of Aswagandha (Withania somnifera) roots for bioactive constituents yielded a novel withanolide sulfoxide compound (1) along with a known withanolide dimer ashwagandhanolide (2) with an S-linkage. The structure of compound 1 was established by extensive NMR and MS experiments. Compound 1 was highly selective in inhibiting cyclooxygenase-2 (COX-2) enzyme by 60% at 100 microm with no activity against COX-1 enzyme. The IC(50) values of compound 1 against human gastric (AGS), breast (MCF-7), central nervous system (SF-268) and colon (HCT-116) cancer cell lines were in the range 0.74-3.63 microm. Both S-containing dimeric withanolides, 1 and 2, completely suppressed TNF-induced NF-kappaB activation when tested at 100 microm. The isolation of a withanolide sulfoxide from W. somnifera roots and its ability to inhibit COX-2 enzyme and to suppress human tumor cell proliferation are reported here for the first time. In addition, this is the first report on the abrogation of TNF-induced NF-kappaB activation for compounds 1 and 2.

The present study demonstrates a novel herbal formulation LI85008F inhibiting adipocyte differentiation and potentiates lipolysis in 3T3-L1 mouse adipocytes. LI85008F is formulated by combining extracts of three Indian herbs Moringa oleifera, Murraya koenigii and Curcuma longa. Oil red O staining of 3T3-L1 adipocytes reveals that LI85008F is a synergistic formulation that inhibits adipocyte differentiation in a dose dependent manner and concurrently down regulates the key adipogenic transcription factors Peroxisome Proliferator-Activated Receptor gamma (PPAR) and CCAAT/enhancer binding protein α (C/EBP). LI85008F confers significant reductions in intracellular triglyceride content in a dose dependent manner. Evidence suggests that LI85008F antagonizes PPAR through Ser112 phosphorylation via MAPK/ERK activation. Immunoblot analyses reveal that LI85008F treatment also down regulates the protein expressions of key PPAR responsive gene products such as Adipocyte differentiation related protein (ADRP), CD36, Adipocyte specific binding protein 2 (aP2) and perilipin. In differentiated adipocytes culture, LI85008F treatment results in significantly (p = 0.0169) increased lipolysis as measured by the release of glycerol. LI85008F does not exhibit cytotoxic effect on adipocytes. Taken together, the results suggest that LI85008F inhibits lipogenesis in adipocytes and concurrently antagonizes PPAR? and other lipogenic factors and in addition, potentiates triglyceride mobilization from the fat cells or enhances lipolysis

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Problem statement: Free radical stress leads to tissue injury and progression of disease conditions such as arthritis, hemorrhagic shock, atherosclerosis, diabetes, hepatic injury, aging and ischemia, reperfusion injury of many tissues, gastritis, tumor promotion, neurodegenerative diseases and carcinogenesis. Safer antioxidants suitable for long term use are needed to prevent or stop the progression of free radical mediated disorders. Approach: Many plants possess antioxidant ingredients that provided efficacy by additive or synergistic activities. A. polystachya bark was a strong astringent, used for the treatment of liver and spleen diseases, rheumatism and tumors. Antioxidant activity of the crude extracts of bark of A. polystachya were assessed using NBT, DPPH, ABTS and FRAP assays. The potent fraction (AP-110/82C) was tested for in vivo efficacy Results: The methanol, aqueous methanol and water extracts exhibited potent antioxidant activity compared to known antioxidants. In vivo studies on potent fraction AP-110/82C demonstrated dose dependent reduction in hepatic malondialdehyde (320.6, 269.3 and 373.69 µM mg −1 protein) with simultaneous improvement in hepatic glutathione (6.9, 17.1 and 5.8 µg mg −1 protein) and catalase levels (668.9, 777.0 and 511.94 µg mg −1 protein) respectively for 50, 100 mg kg −1 doses and control) compared to control group. Conclusion: Due to its natural origin and potent free-radical scavenging ability A. polystachya could be used as a potential preventive intervention for free radical-mediated diseases.