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- Patent Pending |
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| Full Spectrum Anti-Inflammatory Bio-actives
from
Boswellia serrata |
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| Traditional Uses of Boswellia |
- Long history of use in religious ceremonies and for perfume production and its medicinal properties have been appreciated for millennia.
- In India, the gum resin exudates of Boswellia serrata, known in the vernacular as "Salai guggal", has been used in the Ayurvedic system of medicine in the management of several inflammatory disorders.
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| Boswellia Gum Composition |
| Typically the Gum Oleoresin of Boswellia is reported to consists of: |
- Sesquiterpenoid essential oils (8-12%),
- Polysaccharides (45-60%),
- Higher terpenoids, including Boswellic acids (25–35%).
Boswellin® PS is obtained from the gum exudate of Boswellia serrata trees commonly known as Frankincense.
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| Boswellin® PS |
| Boswellin® PS is standardized to contain: |
- AKBBA 10% (MIN)
- Total Identified Boswellic Acids 20% (MIN)
- Total Organic Acids 35% (MIN)
In addition to the active Boswellic acids, Boswellin® PS also contains Polysal which contributes to its immediate anti-inflammatory action.
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| Salient Features of Boswellin® PS |
- 100% Natural
- No Excipients
- No Preservatives
- Enhanced solubility in Water
- Enhanced AKBBA content than regular Boswellin®
- Contains Full-Spectrum Anti-Inflammatory Bio-actives from Boswellia Gum
- Standardized and contains both the hydrophilic and lipophilic fractions of Boswellia Gum
- Enhanced Safety
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| Proposed Mechanism of Action |
- Boswellin® PS contains the Boswellic acids and Polysal, both of which provide anti-inflammatory action.
- The water-soluble Polysal initiates and supports the anti-inflammatory activity, while the lipid-soluble Boswellic acids help to provide a sustained action.
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| Boswellin® - Chemistry |
The FOUR major identified pentacyclic triterpenoids in
Boswellin® are…
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- β -Boswellic acid
- Acetyl- β -Boswellic acid
- 11-keto- β -Boswellic acid
- Acetyl -11 –keto –β -Boswellic acid
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| Chemistry of Boswellic Acids |

β-Boswellic Acid |

Acetyl-β-Boswellic Acid |

11-Keto-β-Boswellic Acid |

Acetyl 11-Keto-β-Boswellic Acid |
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| Polysal - Chemistry |
- Polysal has been reported to contain mainly neutral sugars as Polysaccharides.
- The polysaccharide is reported to primarily consist of galactose, arabinose and D-glucuronic acid.
- 4-o-methyl-glucuronoarabino-galactan has been identified as one of the polysaccharides.
- The polysaccharide has a molecular weight of 5.1 – 5.6 X 105 against dextran standards.
- The polysaccharide has an Optical Rotation [α]D – 10.50 and contains 64% to 69% neutral sugars.
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| Mechanism of Action |
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| Arachidonic Acid Pathway and Action of Boswellic Acids |
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| A. Inhibition of Leukotrienes Formation |
- Leukotrienes are fatty acids which are formed from arachidonic acid by an enzyme called Lipoxygenase.
- Function of Leukotrienes is to sustain the inflammatory reactions in the body by acting as chemo attractants for leucocytes that are the reservoirs of pro-inflammatory cytokines like TNFα.
- Boswellic acids are reported to be non competitive inhibitors of 5-Lipoxygenase enzyme.
- AKBBA has been shown to be the most potent inhibitor of 5-Lipoxygenase enzyme.
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| Boswellic Acids in Inhibiting the Enzyme 5-lipoxygenase |
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| B. Inhibition of Human Leukocyte Elastase (HLE) |
- HLE is a serine protease and play an important role in several inflammatory diseases like
- Cystic fibrosis
- Pulmonary emphysema
- Rheumatic arthritis
- Chronic bronchitis
- Boswellic acids block the HLE activity
Dual inhibition of HLE and 5- Lipoxygenase enzyme is unique to the Boswellic acids
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| Anti-inflammatory Potential of Boswellia Extract and Polysal |
- Polysal showed a dose dependent anti-inflammatory potential, similar to the Boswellic acids.
- The Polysal and Boswellic acids when combined exhibited an enhanced effect with regard to its anti-inflammatory potential.
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| Pre-Clinical Experimental Study |
| Studies were carried out in 3 phases |
- In vitro - TNFα estimation in murine neutrophils
- In vivo - TNFα, IL-1β and inducible Nitric oxide (NO) estimation in male Swiss Albino mice
- In vivo study in Wistar Albino arthritis induced rats
- Developing arthritis (Prophylactic effect)
- Established arthritis (Therapeutic effect)
- Endpoints
- Paw oedema
- Tissue cytokines
- LTB4
- TNFα
- PGE2
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| In vitro - TNFα estimation in murine neutrophils |
| Anti-inflammatory Potential of Boswellin® and Boswellin® PS (in vitro) |
- LPS (Lipopolysaccharide) (E. Coli, Sigma Aldrich, India) endotoxin is an important triggering factor for systemic inflammatory response.
- TNF-α cytokine is a major pro-inflammatory cytokine and plays a very important role in the pathogenesis of septic shock induced by LPS.
- Anti-inflammatory potential of Boswellin® and Boswellin® PS was evaluated by Flow Cytometer studies in murine neutrophils.
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Intracellular in vitro TNF-α estimation in Murine Neutrophils
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| In vivo - TNFα, IL-1β & inducible Nitric oxide (NO) estimation in male Swiss Albino mice |
| Importance of the Inflammatory Markers-1 |
- TNF – α (tumor necrosis factor-alpha) is a cytokine involved in systemic inflammation and stimulates the acute phase reaction.
- Dysregulation of TNF production has been implicated in a variety of human diseases including cancer.
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Extracellular in vivo TNF-α Estimation in Serum |
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Importance of the Inflammatory Markers-2 |
- IL-1β (interleukin-1 beta) is one of the most potent pro‐inflammatory cytokines involved both in physiological immune responses and in the development of various immunopathological disorders.
- Checking IL-1β levels is useful in monitoring and diagnosis of various diseases including inflammatory, immunological and bone diseases.
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Extracellular in vivo IL-1 β Estimation in Serum |
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| Importance of the Inflammatory Markers-3 |
- Appropriate levels of Nitric Oxide production are important in protecting an organ such as the liver from ischemic damage.
- However sustained levels of NO production result in direct tissue toxicity and contribute to the vascular collapse.
- Chronic expression of NO is associated with various carcinomas and inflammatory conditions including juvenile diabetes, multiple sclerosis, arthritis and ulcerative colitis.
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| Extracellular in vivo IL-1 β Estimation in Serum |
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In vivo study in Wistar Albino
arthritis induced rats
Developing arthritis (Prophylactic effect)
Established arthritis (Therapeutic effect) |
| Boswellic Acids compared with Polysal |
- Polysal and Boswellic acids were compared and evaluated for their anti-arthritic potential in male wistar rats.
- Inhibition of oedema was studied on adjuvant induced developing and developed arthritic groups of animals.
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| Boswellic Acids compared with
Polysal Anti-Arthritic Potential |
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| Anti-arthritic activity (Prophylactic) of test samples in Mycobacterium tuberculosis induced inflammatory arthritis in rats (injected paw) |
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p value * < 0.01; **< 0.001; (ASA: Acetylsalicylic acid (standard)-100mg/kg; BA: Boswellia Regular
POLY: Polysal; BOS.PS: Boswellin® PS (Polysal + Boswellic acid + AKBBA-10%)
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Anti-arthritic activity (Therapeutic) of test samples (effective dose) in Mycobacterium tuberculosis induced established inflammatory arthritis in rats (injected paw)
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p value * < 0.01; **< 0.001; ASA: Acetylsalicylic acid (standard)-100mg/kg; BA: Boswellia Regular
POLY: Polysal; BOS.PS: Boswellin® PS (Polysal + Boswellic acid + AKBBA-10%)
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Expression of LTB4 in supernatant from arthritic paw tissue homogenate in Mycobacterium tuberculosis induced inflammatory arthritis in rats treated with different test samples at graded dose levels
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p value * < 0.01; **< 0.001; ASA: Acetylsalicylic acid (standard)-100mg/kg; BA: Boswellia Regular
POLY: Polysal; BOS.PS: Boswellin® PS (Polysal + Boswellic acid + AKBBA-10%) |
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Expression of TNF-alpha in supernatant from arthritic paw tissue homogenate in Mycobacterium tuberculosis induced inflammatory arthritis in rats treated with different test samples at graded dose levels
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p value * < 0.01; **< 0.001; (ASA: Acetylsalicylic acid (standard)-100mg/kg; BA: Boswellia Regular
POLY: Polysal; BOS.PS: Boswellin® PS (Polysal + Boswellic acid + AKBBA-10%) |
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Expression of PGE2 in supernatant from arthritic paw tissue homogenate in Mycobacterium tuberculosis induced inflammatory arthritis in rats treated with different test samples at graded dose levels
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p value * < 0.01; **< 0.001; ASA: Acetylsalicylic acid (standard)-100mg/kg; BA: Boswellia Regular
POLY: Polysal; BOS.PS: Boswellin® PS (Polysal + Boswellic acid + AKBBA-10%) |
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| Conclusion |
- The significant dose related inhibition of TNF-α in both in vitro and in vivo pre-clinical test models was observed in the isolated murine neutrophils.
- Boswellin® PS was shown to have most significant dose related anti-arthritic activity in Mycobacterium tuberculosis induced developing adjuvant arthritis test in rats which was comparatively more than the other test materials.
- Boswellin® PS showed the significant inhibition of absolute oedema by different test materials in Mycobacterium tuberculosis induced established adjuvant arthritis.
- Boswellin® PS may be
- partially immunosuppressive in nature and
- partially it may be due to the inhibition of pro-inflammatory cytokines and mediators.
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| Solubility |
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| Toxicity
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- Both Boswellic acids and Polysal were found to have good safety profile.
- Acute Oral Toxicity (LD0) [OECD Guideline] for Boswellic Acids was found to be 2000mg/kg b.w.
- Acute Oral Toxicity (LD0) [OECD Guideline] for Polysal was found to be 2000mg/kg b.w.
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| Dosage
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- Boswellin® PS can be suggested at a dosage of up to 200mg, 2 times a day.
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| Applications |
- Boswellin® PS can find potential use in management of various inflammatory disorders.
- Rheumatoid arthritis
- Osteoarthritis
- Chronic colitis
- Ulcerative colitis
- Crohn's disease
- Bronchial asthma
- Peritumoral brain edemas
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