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Mona Abdel-tawab - One of the best experts on this subject based on the ideXlab platform.
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Enhanced absorption of boswellic acids by a micellar solubilized delivery form of Boswellia extract
NFS Journal, 2018Co-Authors: Juergen Meins, Dariush Behnam, Mona Abdel-tawabAbstract:Background: Boswellic acids (BAs) the pharmacologically active ingredients of the gum resin extract of Boswellia serrata are known for their anti-inflammatory effects. However they suffer from poor bioavailability because of their hydrophobicity and poor water solubility. Purpose: The present study aimed at investigating the effect of AQUANOVA micellation technology on the bioavailability of Boswellia extract in rats compared to its native form. Study design. Female albino wistar rats (n = 6) weighing around 250 g were orally administered solubilized (Sol-BE) and native (Nat-BE) Boswellia extract at an equimolar dosage of 128 mg/kg. Plasma samples collected at defined time points (0, 0.5, 1, 2, 3, 4, 6 and 8 h) were analyzed for the content of the six major boswellic acids (KBA, AKBA, αBA, βBA, AαBA and AβBA - 11-keto-β-boswellic acid (KBA), acetyl-11-keto-β-boswellic acid (AKBA), α-boswellic acid (αBA), β-boswellic acid (βBA), acetyl-α-boswellic acid (AαBA) and acetyl-β-boswellic acid (AβBA)) using a sensitive LC-MS/MS method. Results: The oral administration of Sol-BE led to a remarkable increase in the AUC and Cmaxof all BAs in plasma compared to Nat-BE. Whereas no KBA could be detected after the administration of Nat-BE, KBA could be detected at a maximal plasma concentration of 439.21 ng/mL and an AUClastof 1185.37 ng/mL*h following the administration of Sol-BE. The highest increase was observed in the case of AKBA where a 56-fold increase in the AUClastand a 25-fold increase in the Cmaxwas determined compared to Nat-BE. Conclusions: Micellar solubilisation represents a promising approach for enhancing the bioavailability of poorly soluble substances.
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Enhanced absorption of boswellic acids by a micellar solubilized delivery form of Boswellia extract
Elsevier, 2018Co-Authors: Juergen Meins, Dariush Behnam, Mona Abdel-tawabAbstract:Background: Boswellic acids (BAs) the pharmacologically active ingredients of the gum resin extract of Boswellia serrata are known for their anti-inflammatory effects. However they suffer from poor bioavailability because of their hydrophobicity and poor water solubility. Purpose: The present study aimed at investigating the effect of AQUANOVA micellation technology on the bioavailability of Boswellia extract in rats compared to its native form.Study design.Female albino wistar rats (n = 6) weighing around 250 g were orally administered solubilized (Sol-BE) and native (Nat-BE) Boswellia extract at an equimolar dosage of 128 mg/kg. Plasma samples collected at defined time points (0, 0.5, 1, 2, 3, 4, 6 and 8 h) were analyzed for the content of the six major boswellic acids (KBA, AKBA, αBA, βBA, AαBA and AβBA - 11-keto-β-boswellic acid (KBA), acetyl-11-keto-β-boswellic acid (AKBA), α-boswellic acid (αBA), β-boswellic acid (βBA), acetyl-α-boswellic acid (AαBA) and acetyl-β-boswellic acid (AβBA)) using a sensitive LC-MS/MS method. Results: The oral administration of Sol-BE led to a remarkable increase in the AUC and Cmax of all BAs in plasma compared to Nat-BE. Whereas no KBA could be detected after the administration of Nat-BE, KBA could be detected at a maximal plasma concentration of 439.21 ng/mL and an AUClast of 1185.37 ng/mL*h following the administration of Sol-BE. The highest increase was observed in the case of AKBA where a 56-fold increase in the AUClast and a 25-fold increase in the Cmax was determined compared to Nat-BE. Conclusions: Micellar solubilisation represents a promising approach for enhancing the bioavailability of poorly soluble substances. Keywords: Boswellia serrata extract, Boswellic acids, Micellar solubilisation, Bioavailability, Absorption, Pharmacokinetic
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Survey on the Quality of the Top-Selling European and American Botanical Dietary Supplements Containing Boswellic Acids
Planta Medica, 2016Co-Authors: Juergen Meins, Christian Artaria, Antonella Riva, Manfred Schubert-zsilavecz, Paolo Morazzoni, Mona Abdel-tawabAbstract:In consideration of the increasing popularity of frankincense and the widely published quality problems associated with botanical dietary supplements, a survey was conducted for the first time on the quality of frankincense containing botanical dietary supplements. Six US products representing 78 % of the units sold and 70 % of the market value, and 11 European products representing 30 % of the units sold and 40 % of the market value were tested for their boswellic acid composition profile, label compliance, and claimed health benefits. Special focus was also set on the statements made with regard to the frankincense applied.Only five products out of seventeen disclosed all relevant information for the Boswellia extract, mentioning the species, the part of plant used, and the boswellic acid content. Whereas all products but one claimed to use Boswellia serrata, three products did not mention the resin as the part applied and 10 products did not declare the boswellic acid content. Apart from the different boswellic acid composition determined with a sensitive LC/MS method, 41 % of the products did not comply with the label declaration. Hence, one product from Italy did not contain any of the six characteristic boswellic acids (KBA, AKBA, αBA, βBA, AαBA, AβBA) at all and another US product contained only traces, suggesting the absence of frankincense or the use of Boswellia frereana instead of B. serrata. In another product, the ratios of the individual boswellic acids were different from B. serrata gum resin, indicating the use of another species such as Boswellia sacra or Boswellia carterii. Furthermore, two products revealed different boswellic acid contents from those declared on the label. Further, two products did not declare the use of manipulated Boswellia gum resin extract being enriched in acetyl-11-keto-boswellic acid content reaching up to 66 %. In addition, consumers could be misled by outdated literature or references to in vitro studies performed at dosages that can never be achieved in humans following oral administration.In summary, this survey reveals that in spite of increased regulations on botanical dietary supplements, the problem of mislabeling still exists and needs to be addressed by the manufacturers, so that consumers get greater confidence in the botanical dietary supplements they use.
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Enhanced absorption of boswellic acids by a lecithin delivery form (Phytosome(®)) of Boswellia extract.
Fitoterapia, 2013Co-Authors: Jan Hüsch, Christian Artaria, Manfred Schubert-zsilavecz, Janine Bohnet, Gert Fricker, Carsten Skarke, Giovanni Appendino, Mona Abdel-tawabAbstract:The anti-inflammatory potential of Boswellia serrata gum resin extracts has been demonstrated in vitro and in animal studies as well as in pilot clinical trials. However, pharmacokinetic studies have evidenced low systemic absorption of boswellic acids (BAs), especially of KBA and AKBA, in rodents and humans. This observation has provided a rationale to improve the formulation of Boswellia extract. We present here the results of a murine comparative bioavailability study of Casperome™, a soy lecithin formulation of standardized B. serrata gum resin extract (BE), and its corresponding non-formulated extract. The concentration of the six major BAs [11-keto-β-boswellic acid (KBA), acetyl-11-keto-β-boswellic acid (AKBA), β-boswellic acid (βBA), acetyl-β-boswellic acid (AβBA), α-boswellic acid (αBA), and acetyl-α-boswellic acid (AαBA)] was evaluated in the plasma and in a series of tissues (brain, muscle, eye, liver and kidney), providing the first data on tissue distribution of BAs. Weight equivalent and equimolar oral administration of Casperome™ provided significantly higher plasma levels (up to 7-fold for KBA, and 3-fold for βBA quantified as area under the plasma concentration time curve, AUC(last)) compared to the non-formulated extract. This was accompanied by remarkably higher tissue levels. Of particular relevance was the marked increase in brain concentration of KBA and AKBA (35-fold) as well as βBA (3-fold) following Casperome™ administration. Notably, up to 17 times higher BA levels were observed in poorly vascularized organs such as the eye. The increased systemic availability of BAs and the improved tissue distribution, qualify Casperome™ for further clinical development to fully exploit the clinical potential of BE.
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In vitro metabolism, permeation, and brain availability of six major boswellic acids from Boswellia serrata gum resins
Fitoterapia, 2013Co-Authors: Kathleen Gerbeth, Oliver Werz, Manfred Schubert-zsilavecz, Jan Hüsch, Gert Fricker, Mona Abdel-tawabAbstract:Boswellia serrata gum resin extracts (BSE) revealed potent anti-inflammatory actions in preclinical and clinical studies. In 2002 BSE was assigned an orphan drug status by the European Medicines Agency (EMA) for the treatment of peritumoral edema. In the past pharmacological effects of BSE were mainly attributed to 11-keto-β-boswellic acid (KBA) and 3-acetyl-11-keto-β-boswellic acid (AKBA). Therefore pharmacokinetic and pharmacodynamic studies focused mainly on these two boswellic acids (BAs). However, other BAs, like β-boswellic acid (βBA), might also contribute to the anti-inflammatory actions of BSE. Here, we determined the metabolic stability, permeability and brain availability of six major BAs, that is, KBA, AKBA, βBA, 3-acetyl-β-boswellic acid (AβBA), α-boswellic acid (αBA), and 3-acetyl-α-boswellic acid (AαBA). For permeability studies, the Caco-2 model was adapted to physiological conditions by the addition of bovine serum albumin (BSA) to the basolateral side and the use of modified fasted state simulated intestinal fluid (FaSSIF) on the apical side. Under these conditions the four BAs lacking the 11-keto moiety revealed moderate permeability. Furthermore the permeability of AKBA and KBA was improved compared to earlier studies. In contrast to Aα- and AβBA, βBA and αBA were intensively metabolized after incubation with human and rat liver microsomes. Finally, the availability of all six major BAs could be confirmed in rat brain 8h after oral administration of 240mg/kg BSE to rats showing mean concentrations of 11.6ng/g for KBA, 37.5ng/g for AKBA, 485.1ng/g for αBA, 1066.6ng/g for βBA, 43.0ng/g for AαBA and 163.7ng/g for AβBA.
Manfred Schubert-zsilavecz - One of the best experts on this subject based on the ideXlab platform.
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Survey on the Quality of the Top-Selling European and American Botanical Dietary Supplements Containing Boswellic Acids
Planta Medica, 2016Co-Authors: Juergen Meins, Christian Artaria, Antonella Riva, Manfred Schubert-zsilavecz, Paolo Morazzoni, Mona Abdel-tawabAbstract:In consideration of the increasing popularity of frankincense and the widely published quality problems associated with botanical dietary supplements, a survey was conducted for the first time on the quality of frankincense containing botanical dietary supplements. Six US products representing 78 % of the units sold and 70 % of the market value, and 11 European products representing 30 % of the units sold and 40 % of the market value were tested for their boswellic acid composition profile, label compliance, and claimed health benefits. Special focus was also set on the statements made with regard to the frankincense applied.Only five products out of seventeen disclosed all relevant information for the Boswellia extract, mentioning the species, the part of plant used, and the boswellic acid content. Whereas all products but one claimed to use Boswellia serrata, three products did not mention the resin as the part applied and 10 products did not declare the boswellic acid content. Apart from the different boswellic acid composition determined with a sensitive LC/MS method, 41 % of the products did not comply with the label declaration. Hence, one product from Italy did not contain any of the six characteristic boswellic acids (KBA, AKBA, αBA, βBA, AαBA, AβBA) at all and another US product contained only traces, suggesting the absence of frankincense or the use of Boswellia frereana instead of B. serrata. In another product, the ratios of the individual boswellic acids were different from B. serrata gum resin, indicating the use of another species such as Boswellia sacra or Boswellia carterii. Furthermore, two products revealed different boswellic acid contents from those declared on the label. Further, two products did not declare the use of manipulated Boswellia gum resin extract being enriched in acetyl-11-keto-boswellic acid content reaching up to 66 %. In addition, consumers could be misled by outdated literature or references to in vitro studies performed at dosages that can never be achieved in humans following oral administration.In summary, this survey reveals that in spite of increased regulations on botanical dietary supplements, the problem of mislabeling still exists and needs to be addressed by the manufacturers, so that consumers get greater confidence in the botanical dietary supplements they use.
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Enhanced absorption of boswellic acids by a lecithin delivery form (Phytosome(®)) of Boswellia extract.
Fitoterapia, 2013Co-Authors: Jan Hüsch, Christian Artaria, Manfred Schubert-zsilavecz, Janine Bohnet, Gert Fricker, Carsten Skarke, Giovanni Appendino, Mona Abdel-tawabAbstract:The anti-inflammatory potential of Boswellia serrata gum resin extracts has been demonstrated in vitro and in animal studies as well as in pilot clinical trials. However, pharmacokinetic studies have evidenced low systemic absorption of boswellic acids (BAs), especially of KBA and AKBA, in rodents and humans. This observation has provided a rationale to improve the formulation of Boswellia extract. We present here the results of a murine comparative bioavailability study of Casperome™, a soy lecithin formulation of standardized B. serrata gum resin extract (BE), and its corresponding non-formulated extract. The concentration of the six major BAs [11-keto-β-boswellic acid (KBA), acetyl-11-keto-β-boswellic acid (AKBA), β-boswellic acid (βBA), acetyl-β-boswellic acid (AβBA), α-boswellic acid (αBA), and acetyl-α-boswellic acid (AαBA)] was evaluated in the plasma and in a series of tissues (brain, muscle, eye, liver and kidney), providing the first data on tissue distribution of BAs. Weight equivalent and equimolar oral administration of Casperome™ provided significantly higher plasma levels (up to 7-fold for KBA, and 3-fold for βBA quantified as area under the plasma concentration time curve, AUC(last)) compared to the non-formulated extract. This was accompanied by remarkably higher tissue levels. Of particular relevance was the marked increase in brain concentration of KBA and AKBA (35-fold) as well as βBA (3-fold) following Casperome™ administration. Notably, up to 17 times higher BA levels were observed in poorly vascularized organs such as the eye. The increased systemic availability of BAs and the improved tissue distribution, qualify Casperome™ for further clinical development to fully exploit the clinical potential of BE.
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In vitro metabolism, permeation, and brain availability of six major boswellic acids from Boswellia serrata gum resins
Fitoterapia, 2013Co-Authors: Kathleen Gerbeth, Oliver Werz, Manfred Schubert-zsilavecz, Jan Hüsch, Gert Fricker, Mona Abdel-tawabAbstract:Boswellia serrata gum resin extracts (BSE) revealed potent anti-inflammatory actions in preclinical and clinical studies. In 2002 BSE was assigned an orphan drug status by the European Medicines Agency (EMA) for the treatment of peritumoral edema. In the past pharmacological effects of BSE were mainly attributed to 11-keto-β-boswellic acid (KBA) and 3-acetyl-11-keto-β-boswellic acid (AKBA). Therefore pharmacokinetic and pharmacodynamic studies focused mainly on these two boswellic acids (BAs). However, other BAs, like β-boswellic acid (βBA), might also contribute to the anti-inflammatory actions of BSE. Here, we determined the metabolic stability, permeability and brain availability of six major BAs, that is, KBA, AKBA, βBA, 3-acetyl-β-boswellic acid (AβBA), α-boswellic acid (αBA), and 3-acetyl-α-boswellic acid (AαBA). For permeability studies, the Caco-2 model was adapted to physiological conditions by the addition of bovine serum albumin (BSA) to the basolateral side and the use of modified fasted state simulated intestinal fluid (FaSSIF) on the apical side. Under these conditions the four BAs lacking the 11-keto moiety revealed moderate permeability. Furthermore the permeability of AKBA and KBA was improved compared to earlier studies. In contrast to Aα- and AβBA, βBA and αBA were intensively metabolized after incubation with human and rat liver microsomes. Finally, the availability of all six major BAs could be confirmed in rat brain 8h after oral administration of 240mg/kg BSE to rats showing mean concentrations of 11.6ng/g for KBA, 37.5ng/g for AKBA, 485.1ng/g for αBA, 1066.6ng/g for βBA, 43.0ng/g for AαBA and 163.7ng/g for AβBA.
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Boswellia serrata
Clinical Pharmacokinetics, 2011Co-Authors: Mona Abdel-tawab, Oliver Werz, Manfred Schubert-zsilaveczAbstract:Non-steroidal anti-inflammatory drug (NSAID) intake is associated with high prevalence of gastro-intestinal or cardiovascular adverse effects. All efforts to develop NSAIDs that spare the gastrointestinal tract and the cardiovasculature are still far from achieving a breakthrough. In the last two decades, preparations of the gum resin of Boswellia serrata (a traditional ayurvedic medicine) and of other Boswellia species have experienced increasing popularity in Western countries. Animal studies and pilot clinical trials support the potential of B. serrata gum resin extract (BSE) for the treatment of a variety of inflammatory diseases like inflammatory bowel disease, rheumatoid arthritis, osteoarthritis and asthma. Moreover, in 2002 the European Medicines Agency classified BSE as an 'orphan drug' for the treatment of peritumoral brain oedema. Compared to NSAIDs, it is expected that the administration of BSE is associated with better tolerability, which needs to be confirmed in further clinical trials. Until recently, the pharmacological effects of BSE were mainly attributed to suppression of leukotriene formation via inhibition of 5-lipoxygenase (5-LO) by two boswellic acids, 11-keto-β-boswellic acid (KBA) and acetyl-11-keto-β-boswellic acid (AKBA). These two boswellic acids have also been chosen in the monograph of Indian frankincense in European Pharmacopoiea 6.0 as markers to ensure the quality of the air-dried gum resin exudate of B. serrata. Furthermore, several dietary supplements advertise the enriched content of KBA and AKBA. However, boswellic acids failed to inhibit leukotriene formation in human whole blood, and pharmacokinetic data revealed very low concentrations of AKBA and KBA in plasma, being far below the effective concentrations for bioactivity in vitro. Moreover, permeability studies suggest poor absorption of AKBA following oral administration. In view of these results, the previously assumed mode of action -- that is, 5-LO inhibition is questionable. On the other hand, 100-fold higher plasma concentrations have been determined for β-boswellic acid, which inhibits microsomal prostaglandin E synthase-1 and the serine protease cathepsin G. Thus, these two enzymes might be reasonable molecular targets related to the anti-inflammatory properties of BSE. In view of the results of clinical trials and the experimental data from in vitro studies of BSE, and the available pharmacokinetic and metabolic data on boswellic acids, this review presents different perspectives and gives a differentiated insight into the possible mechanisms of action of BSE in humans. It underlines BSE as a promising alternative to NSAIDs, which warrants investigation in further pharmacological studies and clinical trials. [ABSTRACT FROM AUTHOR]
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Metabolism of Boswellic Acids in Vitro and in Vivo
Drug Metabolism and Disposition, 2008Co-Authors: Phillip Kruger, Manfred Schubert-zsilavecz, Walter E. Müller, Gunter P. Eckert, Rambod Daneshfar, Jochen Klein, Dietrich A. Volmer, Ute Bahr, Michael Karas, Mona Abdel-tawabAbstract:Boswellia serrata resin dry extract is among the few herbal remedies designated with an orphan drug status for the treatment of peritumoral brain edema. In addition, boswellic acids (BAs), the main active ingredients of B. serrata extracts, have potent anti-inflammatory properties, and may represent promising agents for the treatment of inflammatory diseases. Pharmacokinetic studies, however, revealed poor bioavailability, especially of 11-keto-β-boswellic acid (KBA) and 3-acetyl-11-keto-β-boswellic acid (AKBA), the most potent BAs. To address the question of whether BAs are extensively metabolized, we determined the metabolic stability of KBA and AKBA in vitro, investigated the in vitro metabolism of BAs, and compared the metabolic profiles of KBA and AKBA with those obtained in rats in vivo. In rat liver microsomes and hepatocytes as well as in human liver microsomes, we found that KBA but not AKBA undergoes extensive phase I metabolism. Oxidation to hydroxylated metabolites is the principal metabolic route. In vitro, KBA yielded metabolic profiles similar to those obtained in vivo in rat plasma and liver, whereas no metabolites of AKBA could be identified in vivo. Furthermore, AKBA is not deacetylated to KBA. This study indicates that the efficacy of B. serrata extract may be enhanced by increasing the bioavailability of AKBA.
Juergen Meins - One of the best experts on this subject based on the ideXlab platform.
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Enhanced absorption of boswellic acids by a micellar solubilized delivery form of Boswellia extract
Elsevier, 2018Co-Authors: Juergen Meins, Dariush Behnam, Mona Abdel-tawabAbstract:Background: Boswellic acids (BAs) the pharmacologically active ingredients of the gum resin extract of Boswellia serrata are known for their anti-inflammatory effects. However they suffer from poor bioavailability because of their hydrophobicity and poor water solubility. Purpose: The present study aimed at investigating the effect of AQUANOVA micellation technology on the bioavailability of Boswellia extract in rats compared to its native form.Study design.Female albino wistar rats (n = 6) weighing around 250 g were orally administered solubilized (Sol-BE) and native (Nat-BE) Boswellia extract at an equimolar dosage of 128 mg/kg. Plasma samples collected at defined time points (0, 0.5, 1, 2, 3, 4, 6 and 8 h) were analyzed for the content of the six major boswellic acids (KBA, AKBA, αBA, βBA, AαBA and AβBA - 11-keto-β-boswellic acid (KBA), acetyl-11-keto-β-boswellic acid (AKBA), α-boswellic acid (αBA), β-boswellic acid (βBA), acetyl-α-boswellic acid (AαBA) and acetyl-β-boswellic acid (AβBA)) using a sensitive LC-MS/MS method. Results: The oral administration of Sol-BE led to a remarkable increase in the AUC and Cmax of all BAs in plasma compared to Nat-BE. Whereas no KBA could be detected after the administration of Nat-BE, KBA could be detected at a maximal plasma concentration of 439.21 ng/mL and an AUClast of 1185.37 ng/mL*h following the administration of Sol-BE. The highest increase was observed in the case of AKBA where a 56-fold increase in the AUClast and a 25-fold increase in the Cmax was determined compared to Nat-BE. Conclusions: Micellar solubilisation represents a promising approach for enhancing the bioavailability of poorly soluble substances. Keywords: Boswellia serrata extract, Boswellic acids, Micellar solubilisation, Bioavailability, Absorption, Pharmacokinetic
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Enhanced absorption of boswellic acids by a micellar solubilized delivery form of Boswellia extract
NFS Journal, 2018Co-Authors: Juergen Meins, Dariush Behnam, Mona Abdel-tawabAbstract:Background: Boswellic acids (BAs) the pharmacologically active ingredients of the gum resin extract of Boswellia serrata are known for their anti-inflammatory effects. However they suffer from poor bioavailability because of their hydrophobicity and poor water solubility. Purpose: The present study aimed at investigating the effect of AQUANOVA micellation technology on the bioavailability of Boswellia extract in rats compared to its native form. Study design. Female albino wistar rats (n = 6) weighing around 250 g were orally administered solubilized (Sol-BE) and native (Nat-BE) Boswellia extract at an equimolar dosage of 128 mg/kg. Plasma samples collected at defined time points (0, 0.5, 1, 2, 3, 4, 6 and 8 h) were analyzed for the content of the six major boswellic acids (KBA, AKBA, αBA, βBA, AαBA and AβBA - 11-keto-β-boswellic acid (KBA), acetyl-11-keto-β-boswellic acid (AKBA), α-boswellic acid (αBA), β-boswellic acid (βBA), acetyl-α-boswellic acid (AαBA) and acetyl-β-boswellic acid (AβBA)) using a sensitive LC-MS/MS method. Results: The oral administration of Sol-BE led to a remarkable increase in the AUC and Cmaxof all BAs in plasma compared to Nat-BE. Whereas no KBA could be detected after the administration of Nat-BE, KBA could be detected at a maximal plasma concentration of 439.21 ng/mL and an AUClastof 1185.37 ng/mL*h following the administration of Sol-BE. The highest increase was observed in the case of AKBA where a 56-fold increase in the AUClastand a 25-fold increase in the Cmaxwas determined compared to Nat-BE. Conclusions: Micellar solubilisation represents a promising approach for enhancing the bioavailability of poorly soluble substances.
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Survey on the Quality of the Top-Selling European and American Botanical Dietary Supplements Containing Boswellic Acids
Planta Medica, 2016Co-Authors: Juergen Meins, Christian Artaria, Antonella Riva, Manfred Schubert-zsilavecz, Paolo Morazzoni, Mona Abdel-tawabAbstract:In consideration of the increasing popularity of frankincense and the widely published quality problems associated with botanical dietary supplements, a survey was conducted for the first time on the quality of frankincense containing botanical dietary supplements. Six US products representing 78 % of the units sold and 70 % of the market value, and 11 European products representing 30 % of the units sold and 40 % of the market value were tested for their boswellic acid composition profile, label compliance, and claimed health benefits. Special focus was also set on the statements made with regard to the frankincense applied.Only five products out of seventeen disclosed all relevant information for the Boswellia extract, mentioning the species, the part of plant used, and the boswellic acid content. Whereas all products but one claimed to use Boswellia serrata, three products did not mention the resin as the part applied and 10 products did not declare the boswellic acid content. Apart from the different boswellic acid composition determined with a sensitive LC/MS method, 41 % of the products did not comply with the label declaration. Hence, one product from Italy did not contain any of the six characteristic boswellic acids (KBA, AKBA, αBA, βBA, AαBA, AβBA) at all and another US product contained only traces, suggesting the absence of frankincense or the use of Boswellia frereana instead of B. serrata. In another product, the ratios of the individual boswellic acids were different from B. serrata gum resin, indicating the use of another species such as Boswellia sacra or Boswellia carterii. Furthermore, two products revealed different boswellic acid contents from those declared on the label. Further, two products did not declare the use of manipulated Boswellia gum resin extract being enriched in acetyl-11-keto-boswellic acid content reaching up to 66 %. In addition, consumers could be misled by outdated literature or references to in vitro studies performed at dosages that can never be achieved in humans following oral administration.In summary, this survey reveals that in spite of increased regulations on botanical dietary supplements, the problem of mislabeling still exists and needs to be addressed by the manufacturers, so that consumers get greater confidence in the botanical dietary supplements they use.
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Determination of boswellic acids in brain and plasma by high-performance liquid chromatography/tandem mass spectrometry.
Analytical Chemistry, 2005Co-Authors: Karen Reising, Juergen Meins, Manfred Schubert-zsilavecz, Baerbel Bastian, Gunter P. Eckert, Walter E. Mueller, Mona Abdel-tawabAbstract:Peritumoral edema, one of the major causes for neurological disorders in brain tumor patients, is mainly treated with steroids, which unfortunately have significant side effects and interfere with the efficacy of chemotherapy. Boswellic acids, the main active ingredients of Boswellia serrata, are antiinflammatory agents, inhibiting 5-lipoxygenase, the key enzyme of leukotriene biosynthesis and one of the pathophysiological mechanisms of peritumoral edema. Based on positive results in clinical trials and animal studies, B. serrata resin dry extract was designated an orphan drug by the European Commission for the treatment of peritumoral edema resulting from brain tumors. Thus boswellic acids may be alternative drugs to corticosteroids. However, the question of the availability of boswellic acids in brain has not been addressed until now. Accordingly, a highly sensitive LC/MS method has been developed for the simultaneous determination of KBA and AKBA, the most potent boswellic acids, in plasma and brain. T...
G N Qazi - One of the best experts on this subject based on the ideXlab platform.
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Boswellic acids: A leukotriene inhibitor also effective through topical application in inflammatory disorders.
Phytomedicine, 2008Co-Authors: S Singh, Subhash C. Taneja, A Khajuria, R K Johri, J Singh, G N QaziAbstract:Abstract Boswellic acids (BA), a natural mixture isolated from oleo gum resin of Boswellia serrata comprised of four major pentacyclic triterpene acids: β-boswellic acid (the most abundant), 3-acteyl-β-boswellic acid, 11-keto-β-boswellic acid, and 3-acetyl-11-keto-β-boswellic acid, is reported to be effective as anti-inflammatory, immunomodulatory, anti-tumor, anti-asthmatic and in Chron's disease. It inhibits pro-inflammatory mediators in the body, specifically leukotrienes via inhibition of 5-lipoxygenase, the key enzyme of leukotriene synthesis, is the scientifically proved mechanism for its anti-inflammatory/anti-arthritic activity. All previous work on BA for its biological activity has been done through the systemic application but no pre-clinical data reported for its anti-inflammatory activity by topical application. We here by report anti-inflammatory activity of BA through this route by applying different acute and chronic models of inflammation i.e., arachidonic acid and croton oil-induced mouse ear edema, carrageenan-induced rats paw edema and adjuvant-induced developing arthritis in rats. The results of the study revealed that the effect observed through this route is in accordance to the study conducted with the systemic route, thus establishing that BA when used through topical application is as effective as through the systemic route.
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Boswellic acids: A leukotriene inhibitor also effective through topical application in inflammatory disorders.
Phytomedicine, 2008Co-Authors: S Singh, A Khajuria, S C Taneja, R K Johri, J Singh, G N QaziAbstract:Boswellic acids (BA), a natural mixture isolated from oleo gum resin of Boswellia serrata comprised of four major pentacyclic triterpene acids: beta-boswellic acid (the most abundant), 3-acteyl-beta-boswellic acid, 11-keto-beta-boswellic acid, and 3-acetyl-11-keto-beta-boswellic acid, is reported to be effective as anti-inflammatory, immunomodulatory, anti-tumor, anti-asthmatic and in Chron's disease. It inhibits pro-inflammatory mediators in the body, specifically leukotrienes via inhibition of 5-lipoxygenase, the key enzyme of leukotriene synthesis, is the scientifically proved mechanism for its anti-inflammatory/anti-arthritic activity. All previous work on BA for its biological activity has been done through the systemic application but no pre-clinical data reported for its anti-inflammatory activity by topical application. We here by report anti-inflammatory activity of BA through this route by applying different acute and chronic models of inflammation i.e., arachidonic acid and croton oil-induced mouse ear edema, carrageenan-induced rats paw edema and adjuvant-induced developing arthritis in rats. The results of the study revealed that the effect observed through this route is in accordance to the study conducted with the systemic route, thus establishing that BA when used through topical application is as effective as through the systemic route.
Hermann P. T. Ammon - One of the best experts on this subject based on the ideXlab platform.
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Effects of gum resin of Boswellia serrata in patients with chronic colitis
Planta Medica, 2001Co-Authors: I. Gupta, P. Malhotra, Hasan Safayhi, Abhinav Parihar, Rainer Ludtke, S. Gupta, Hermann P. T. AmmonAbstract:Patients studied here suffered from chronic colitis characterized by vague lower abdominal pain, bleeding per rectum with diarrhoea and palpable tender descending and sigmoid colon. The inflammatory process in colitis is associated with increased formation of leukotrienes causing chemotaxis, chemokinesis, synthesis of superoxide radicals and release of lysosomal enzymes by phagocytes. The key enzyme for leukotriene biosynthesis is 5-lipoxygenase. Boswellic acids were found to be non-redox, non-competitive specific inhibitors of the enzyme 5-lipoxygenase. We studied the gum resin of Boswellia serrata for the treatment of this disease. Thirty patients, 17 males and 13 females in the age range of 18 to 48 years with chronic colitis were included in this study. Twenty patients were given a preparation of the gum resin of Boswellia serrata (900 mg daily divided in three doses for 6 weeks) and ten patients were given sulfasalazine (3 gm daily divided in three doses for 6 weeks) and served as controls. Out of 20 patients treated with Boswellia gum resin 18 patients showed an improvement in one or more of the parameters: including stool properties, histopathology as well as scanning electron microscopy, besides haemoglobin, serum iron, calcium, phosphorus, proteins, total leukocytes and eosinophils. In the control group 6 out of 10 patients showed similar results with the same parameters. Out of 20 patients treated with Boswellia gum resin 14 went into remission while in case of sulfasalazine remission rate was 4 out of 10. In conclusion, this study shows that a gum resin preparation from Boswellia serrata could be effective in the treatment of chronic colitis with minimal side effects.
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3-Acetoxy group of genuine AKBA (acetyl-11-keto-β-boswellic acid) is α-configurated
Planta Medica, 2000Co-Authors: Susanne Schweizer, Karin Eichele, Hermann P. T. Ammon, Hasan SafayhiAbstract:The pentacyclic triterpenoid 3-acetyl-11-keto-beta-boswellic acid (AKBA) from the resin of Boswellia spec. is a potent inhibitor of 5-lipoxygenase (5-LO). We noticed discrepancies in the nomenclature and stereochemistry of the 3-acetoxy group of boswellic acids. Isolation of AKBA under mild conditions and the data from the first X-ray crystallography study evidence the 3 alpha-orientation of AKBA's acetoxy function.
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Workup-dependent formation of 5-lipoxygenase inhibitory boswellic acid analogues.
Journal of Natural Products, 2000Co-Authors: S. Schweizer, Hermann P. T. Ammon, A. F. W. Von Brocke, S. E. Boden, Ernst Bayer, Hasan SafayhiAbstract:Pentacyclic triterpenes from the 11-keto-boswellic acid series were identified as the active principal ingredients of Boswellia resin, inhibiting the key enzyme of leukotriene biosynthesis, 5-lipoxygenase (5-LO). Of the genuine boswellic acids hitherto characterized, 3-O-acetyl-11-keto-β-boswellic acid, AKBA (1), proved to be the most potent inhibitor of 5-LO. In the course of purification of further boswellic acid derivatives from Boswellia resin, we observed the degradation of the natural compound 3-O-acetyl-11-hydroxy-β-boswellic acid (2) to the thermodynamically more stable product 3-O-acetyl-9,11-dehydro-β-boswellic acid (4). The metastable intermediate of this conversion, under moderate conditions of workup in methanolic solutions, was identified as 3-O-acetyl-11-methoxy-β-boswellic acid (3). The novel artifactual boswellic acid derivatives inhibited 5-LO product formation in intact cells with different characteristics: 4 almost totally abolished 5-LO activity, with an IC50 of 0.75 μM, whereas 3 an...
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Effects of Boswellia serrata gum resin in patients with ulcerative colitis.
European journal of medical research, 1997Co-Authors: I. Gupta, P. Malhotra, Hasan Safayhi, Abhinav Parihar, Rainer Ludtke, G.b. Singh, Hermann P. T. AmmonAbstract:Ulcerative colitis is a chronic inflammatory disease of the colon where leukotrienes are suggested to play an important role for keeping inflammation active. Boswellic acids, the biologically active ingredients of the gum resin of Boswellia serrata (Sallai guggal), have been shown to be specific, nonredox and noncompetitive inhibitors of 5-lipoxygenase, the key enzyme of leukotriene biosynthesis. In patients suffering from ulcerative colitis grade II and III the effect of Boswellia serrata gum resin preparation (350 mg thrice daily for 6 weeks) on stool properties, histolopathology and scan microscopy of rectal biopsies, blood parameters including Hb, serum iron, calcium, phosphorus, proteins, total leukocytes and eosinophils was studied. Patients receiving sulfasalazine (1 g thrice daily) served as controls. All parameters tested improved after treatment with Boswellia serrata gum resin, the results being similar compared to controls: 82% out of treated patients went into remission; in case of sulfasalazine remission rate was 75%.
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Mechanism of antiinflammatory actions of curcumine and boswellic acids
Journal of Ethnopharmacology, 1993Co-Authors: Hermann P. T. Ammon, Hasan Safayhi, Till Mack, J. SabierajAbstract:Curcumine from Curcuma longa and the gum resin of Boswellia serrata, which were demonstrated to act as antiinflammatories in in vivo animal models, were studied in a set of in vitro experiments in order to elucidate the mechanism of their beneficial effects. Curcumine inhibited the 5-lipoxygenase activity in rat peritoneal neutrophils as well as the 12-lipoxygenase and the cyclooxygenase activities in human platelets. In a cell free peroxidation system curcumine exerted strong antioxidative activity. Thus, its effects on the dioxygenases are probably due to its reducing capacity. Boswellic acids were isolated from the gum resin of Boswellia serrata and identified as the active principles. Boswellic acids inhibited the leukotriene synthesis via 5-lipoxygenase, but did not affect the 12-lipoxygenase and the cyclooxygenase activities. Additionally, boswellic acids did not impair the peroxidation of arachidonic acid by iron and ascorbate. The data suggest that boswellic acids are specific, non-redox inhibitors of leukotriene synthesis either interacting directly with 5-lipoxygenase or blocking its translocation. © 1993.