Abstract
Boswellia serrata resin is regarded as a potent anti-inflammatory agent in traditional and herbal medicine in the Indian subcontinent. The compound 3-O-acetyl-11-keto-β-boswellic acid (AKBA) is the most effective boswellic acid and mostly responsible for B. serrata's anti-inflammatory properties. Here, we reexamined the anti-inflammatory potential of a product selectively enriched with 30% AKBA (BE-30, also known as 5-Loxin®) and evaluated its underlying possible molecular mechanism of action. BE-30 was 42.96% more effective than regular Boswellia extract (BE-3) in inhibiting 5-lipoxygenase activity. In lipopolysaccharide (LPS)-induced THP-1 human monocytes, BE-30 showed a strong anti-TNFα activity (half maximal inhibitory concentration 4.61 ± 0.87 ̄g/mL), which provides 71.14% (P < 0.001) better efficacy than BE-3. Our investigations suggest that BE-30 inhibits the LPS-induced activation of serine/threonine kinases of mitogen-activated protein kinase family, which are the key players responsible for a variety of cellular responses, including inflammation. Additionally, we also show that BE-30 blocks the LPS-induced NFκB activation by inhibiting IκBα phosphorylation and p65 translocation to the nuclear compartment of THP-1 monocytes. Collectively, these findings provide molecular basis for the anti-inflammatory properties of BE-30. PRACTICAL APPLICATIONS This article describes the underlying molecular mechanisms for the anti-inflammatory activities of an enriched formulation containing up to 30% 3-O-acetyl-11-keto- β-boswellic acid (AKBA), the active principle that is mainly responsible for Boswellia serrata's anti-inflammatory properties. This AKBA-enriched formulation (BE-30), known as 5-Loxin, is commercially available in the United States and is being used as a key ingredient of several formulations for improvement of joint health. This work explains anti-TNFα properties of BE-30 in a cellular inflammation model in vitro and its inhibitory action on MAPK pathways in inflammation and, in addition, its anti-NFκB activities. The findings will provide a further comprehensive mechanism of anti-inflammatory action of 5-Loxin at the cellular and molecular level.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 325-344 |
| Number of pages | 20 |
| Journal | Journal of Food Lipids |
| Volume | 16 |
| Issue number | 3 |
| DOIs | |
| State | Published - Aug 2009 |
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ASJC Scopus subject areas
- Food Science
- Chemistry(all)
Cite this
Inhibition of TNFα production and blocking of mitogen-activated protein kinase/NFκB activation in lipopolysaccharide-induced thp-1 human monocytes by 3-o-acetyl-11-keto-β-boswellic acid. / Sengupta, Krishanu; Golakoti, Trimurtulu; Marasetti, Ajit K.; Tummala, Tejaswi; Ravada, Suryachandra R.; Krishnaraju, Alluri V.; Raychaudhuri, Siba P.
In: Journal of Food Lipids, Vol. 16, No. 3, 08.2009, p. 325-344.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Inhibition of TNFα production and blocking of mitogen-activated protein kinase/NFκB activation in lipopolysaccharide-induced thp-1 human monocytes by 3-o-acetyl-11-keto-β-boswellic acid
AU - Sengupta, Krishanu
AU - Golakoti, Trimurtulu
AU - Marasetti, Ajit K.
AU - Tummala, Tejaswi
AU - Ravada, Suryachandra R.
AU - Krishnaraju, Alluri V.
AU - Raychaudhuri, Siba P
PY - 2009/8
Y1 - 2009/8
N2 - Boswellia serrata resin is regarded as a potent anti-inflammatory agent in traditional and herbal medicine in the Indian subcontinent. The compound 3-O-acetyl-11-keto-β-boswellic acid (AKBA) is the most effective boswellic acid and mostly responsible for B. serrata's anti-inflammatory properties. Here, we reexamined the anti-inflammatory potential of a product selectively enriched with 30% AKBA (BE-30, also known as 5-Loxin®) and evaluated its underlying possible molecular mechanism of action. BE-30 was 42.96% more effective than regular Boswellia extract (BE-3) in inhibiting 5-lipoxygenase activity. In lipopolysaccharide (LPS)-induced THP-1 human monocytes, BE-30 showed a strong anti-TNFα activity (half maximal inhibitory concentration 4.61 ± 0.87 ̄g/mL), which provides 71.14% (P < 0.001) better efficacy than BE-3. Our investigations suggest that BE-30 inhibits the LPS-induced activation of serine/threonine kinases of mitogen-activated protein kinase family, which are the key players responsible for a variety of cellular responses, including inflammation. Additionally, we also show that BE-30 blocks the LPS-induced NFκB activation by inhibiting IκBα phosphorylation and p65 translocation to the nuclear compartment of THP-1 monocytes. Collectively, these findings provide molecular basis for the anti-inflammatory properties of BE-30. PRACTICAL APPLICATIONS This article describes the underlying molecular mechanisms for the anti-inflammatory activities of an enriched formulation containing up to 30% 3-O-acetyl-11-keto- β-boswellic acid (AKBA), the active principle that is mainly responsible for Boswellia serrata's anti-inflammatory properties. This AKBA-enriched formulation (BE-30), known as 5-Loxin, is commercially available in the United States and is being used as a key ingredient of several formulations for improvement of joint health. This work explains anti-TNFα properties of BE-30 in a cellular inflammation model in vitro and its inhibitory action on MAPK pathways in inflammation and, in addition, its anti-NFκB activities. The findings will provide a further comprehensive mechanism of anti-inflammatory action of 5-Loxin at the cellular and molecular level.
AB - Boswellia serrata resin is regarded as a potent anti-inflammatory agent in traditional and herbal medicine in the Indian subcontinent. The compound 3-O-acetyl-11-keto-β-boswellic acid (AKBA) is the most effective boswellic acid and mostly responsible for B. serrata's anti-inflammatory properties. Here, we reexamined the anti-inflammatory potential of a product selectively enriched with 30% AKBA (BE-30, also known as 5-Loxin®) and evaluated its underlying possible molecular mechanism of action. BE-30 was 42.96% more effective than regular Boswellia extract (BE-3) in inhibiting 5-lipoxygenase activity. In lipopolysaccharide (LPS)-induced THP-1 human monocytes, BE-30 showed a strong anti-TNFα activity (half maximal inhibitory concentration 4.61 ± 0.87 ̄g/mL), which provides 71.14% (P < 0.001) better efficacy than BE-3. Our investigations suggest that BE-30 inhibits the LPS-induced activation of serine/threonine kinases of mitogen-activated protein kinase family, which are the key players responsible for a variety of cellular responses, including inflammation. Additionally, we also show that BE-30 blocks the LPS-induced NFκB activation by inhibiting IκBα phosphorylation and p65 translocation to the nuclear compartment of THP-1 monocytes. Collectively, these findings provide molecular basis for the anti-inflammatory properties of BE-30. PRACTICAL APPLICATIONS This article describes the underlying molecular mechanisms for the anti-inflammatory activities of an enriched formulation containing up to 30% 3-O-acetyl-11-keto- β-boswellic acid (AKBA), the active principle that is mainly responsible for Boswellia serrata's anti-inflammatory properties. This AKBA-enriched formulation (BE-30), known as 5-Loxin, is commercially available in the United States and is being used as a key ingredient of several formulations for improvement of joint health. This work explains anti-TNFα properties of BE-30 in a cellular inflammation model in vitro and its inhibitory action on MAPK pathways in inflammation and, in addition, its anti-NFκB activities. The findings will provide a further comprehensive mechanism of anti-inflammatory action of 5-Loxin at the cellular and molecular level.
UR - http://www.scopus.com/inward/record.url?scp=68849118134&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=68849118134&partnerID=8YFLogxK
U2 - 10.1111/j.1745-4522.2009.01150.x
DO - 10.1111/j.1745-4522.2009.01150.x
M3 - Article
AN - SCOPUS:68849118134
VL - 16
SP - 325
EP - 344
JO - Journal of Food Lipids
JF - Journal of Food Lipids
SN - 1065-7258
IS - 3
ER -