Permeation of Boswellia extract in the Caco-2 model and possible interactions of its constituents KBA and AKBA with OATP1B3 and MRP2

Krüger, Phillip; Kanzer, Johanna; Hummel, Jessica J.A.; Fricker, Gert; Schubert‐Zsilavecz, Manfred; Abdel‐Tawab, Mona

doi:10.1016/j.ejps.2008.10.005

Cited by 53 publications

(37 citation statements)

References 25 publications

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“…However, studies indicate that upon oral administration, Boswellia extracts exhibit poor intestinal absorption of AKBA and poor bioavailability which limits its anti-inflammatory efficacy 31,32. Aflapin is a novel synergistic composition, which contains B. serrata extract enriched to 20% AKBA and B. serrata non-volatile oil (PCT/IN2009/000505).…”

Section: Discussionmentioning

confidence: 99%

A Double Blind, Randomized, Placebo Controlled Clinical Study Evaluates the Early Efficacy of Aflapin^® in Subjects with Osteoarthritis of Knee

Vishal¹,

Mishra

Raychaudhuri³

2011

Int. J. Med. Sci.

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Aflapin® is a novel synergistic composition derived from Boswellia serrata gum resin (Indian Patent Application No. 2229/CHE/2008). Aflapin is more efficacious as an anti-inflammatory agent compared to the existing Boswellia products, 5-Loxin® and traditional 65% Boswellia extract. A 30-day, double-blind, randomized, placebo-controlled study was conducted to validate the efficacy of Aflapin® in the management of clinical symptoms of osteoarthritis (OA) of the knee (Clinical trial registration number: ISRCTN69643551). Sixty eligible OA subjects selected through screening were included in the study. The subjects received either 100 mg (n=30) of Aflapin® or placebo (n=30) daily for 30 days. Each subject 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 5, 15 and 30. A series of biochemical tests in serum, urine and hematological parameters established the safety of Aflapin. The observations suggest that Aflapin conferred clinically and statistically significant improvements in pain scores and physical function scores in OA subjects. Aflapin provided significant improvements in pain score and functional ability in as early as 5 days of treatment. In conclusion, our observations suggest that Aflapin is a safe, fast acting and effective alternative intervention in the management of OA.

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Section: Discussionmentioning

confidence: 99%

A Double Blind, Randomized, Placebo Controlled Clinical Study Evaluates the Early Efficacy of Aflapin^® in Subjects with Osteoarthritis of Knee

Vishal¹,

Mishra

Raychaudhuri³

2011

Int. J. Med. Sci.

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“…Similarly, AKBA and KBA failed to suppress PGE2 formation in human whole blood and in rats, despite significant inhibition of mPGES1 in the cellfree assay. The failure of KBA and AKBA to suppress LT and PGE2 formation in vivo could be related to the marginal permeability of AKBA and moderate absorption of KBA (Kruger et al, 2009), resulting in poor bioavailability (Kruger et al, 2008) with fairly low plasma concentrations (0.3 and <0.1 mM) (Buchele and Simmet, 2003;Tausch et al, 2009). The marked loss of activity of AKBA in whole blood might be related to its strong plasma protein binding .…”

Section: Discussionmentioning

confidence: 99%

Inhibition of microsomal prostaglandin E₂ synthase‐1 as a molecular basis for the anti‐inflammatory actions of boswellic acids from frankincense

Siemoneit

Koeberle

Rossi

et al. 2010

British J Pharmacology

113

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BACKGROUND AND PURPOSEFrankincense, the gum resin derived from Boswellia species, showed anti-inflammatory efficacy in animal models and in pilot clinical studies. Boswellic acids (BAs) are assumed to be responsible for these effects but their anti-inflammatory efficacy in vivo and their molecular modes of action are incompletely understood. EXPERIMENTAL APPROACHA protein fishing approach using immobilized BA and surface plasmon resonance (SPR) spectroscopy were used to reveal microsomal prostaglandin E2 synthase-1 (mPGES1) as a BA-interacting protein. Cell-free and cell-based assays were applied to confirm the functional interference of BAs with mPGES1. Carrageenan-induced mouse paw oedema and rat pleurisy models were utilized to demonstrate the efficacy of defined BAs in vivo. KEY RESULTSHuman mPGES1 from A549 cells or in vitro-translated human enzyme selectively bound to BA affinity matrices and SPR spectroscopy confirmed these interactions. BAs reversibly suppressed the transformation of prostaglandin (PG)H2 to PGE2 mediated by mPGES1 (IC50 = 3-10 mM). Also, in intact A549 cells, BAs selectively inhibited PGE2 generation and, in human whole blood, b-BA reduced lipopolysaccharide-induced PGE2 biosynthesis without affecting formation of the COX-derived metabolites 6-keto PGF1a and thromboxane B2. Intraperitoneal or oral administration of b-BA (1 mg·kg -1 ) suppressed rat pleurisy, accompanied by impaired levels of PGE2 and b-BA (1 mg·kg -1 , given i.p.) also reduced mouse paw oedema, both induced by carrageenan. CONCLUSIONS AND IMPLICATIONSSuppression of PGE2 formation by BAs via interference with mPGES1 contribute to the anti-inflammatory effectiveness of BAs and of frankincense, and may constitute a biochemical basis for their anti-inflammatory properties.

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“…The studies in retinal explants further demonstrate a direct effect of AKBA in the retina, confirming the results obtained in vivo. The antiangiogenic effects of AKBA at relatively low doses may be due to the fact that AKBA shows high lipid solubility (Park et al, 2011b;Krüger et al, 2009) and easily crosses the bloodretinal barrier, in particular when it is altered as in the OIR model , thus resulting in a good AKBA bioavailability to retinal tissues. As a result of this inhibitory effect on retinal angiogenesis, AKBA may be regarded as a possible therapeutic tool in retinal diseases characterized by neovascularization originating either from retinal or from choroidal vessels.…”

Section: Akba Is Well Tolerated By the Retina And Reduces Retinal Neomentioning

confidence: 98%

Acetyl-11-keto-β-boswellic acid reduces retinal angiogenesis in a mouse model of oxygen-induced retinopathy

Lulli

Cammalleri

Fornaciari

et al. 2015

Experimental Eye Research

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Permeation of Boswellia extract in the Caco-2 model and possible interactions of its constituents KBA and AKBA with OATP1B3 and MRP2

Cited by 53 publications

References 25 publications

A Double Blind, Randomized, Placebo Controlled Clinical Study Evaluates the Early Efficacy of Aflapin^® in Subjects with Osteoarthritis of Knee

A Double Blind, Randomized, Placebo Controlled Clinical Study Evaluates the Early Efficacy of Aflapin^® in Subjects with Osteoarthritis of Knee

Inhibition of microsomal prostaglandin E₂ synthase‐1 as a molecular basis for the anti‐inflammatory actions of boswellic acids from frankincense

Acetyl-11-keto-β-boswellic acid reduces retinal angiogenesis in a mouse model of oxygen-induced retinopathy

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Permeation of Boswellia extract in the Caco-2 model and possible interactions of its constituents KBA and AKBA with OATP1B3 and MRP2

Cited by 53 publications

References 25 publications

A Double Blind, Randomized, Placebo Controlled Clinical Study Evaluates the Early Efficacy of Aflapin® in Subjects with Osteoarthritis of Knee

A Double Blind, Randomized, Placebo Controlled Clinical Study Evaluates the Early Efficacy of Aflapin® in Subjects with Osteoarthritis of Knee

Inhibition of microsomal prostaglandin E2 synthase‐1 as a molecular basis for the anti‐inflammatory actions of boswellic acids from frankincense

Acetyl-11-keto-β-boswellic acid reduces retinal angiogenesis in a mouse model of oxygen-induced retinopathy

Contact Info

Product

Resources

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A Double Blind, Randomized, Placebo Controlled Clinical Study Evaluates the Early Efficacy of Aflapin^® in Subjects with Osteoarthritis of Knee

A Double Blind, Randomized, Placebo Controlled Clinical Study Evaluates the Early Efficacy of Aflapin^® in Subjects with Osteoarthritis of Knee

Inhibition of microsomal prostaglandin E₂ synthase‐1 as a molecular basis for the anti‐inflammatory actions of boswellic acids from frankincense