Inhibitory effect of acetyl-11-keto-beta-boswellic acid on androgen receptor by interference of Sp1 binding activity in prostate cancer cells.
Yuan HQ, Kong F, Wang XL, Young CY, Hu XY, Lou HX
Biochem Pharmacol 2008 Jun 1; 75(11); 2112-2121
In this study, researchers investigated the use of Acetyl-11-keto-beta-boswellic acid (AKBA), a compound isolated from the gum-resin of Boswellia carterii to target Androgen Receptor [AR] signalling so as to inhibit growth of prostate cancer cells. AKBA caused G1-phase cell cycle arrest with an induction of p21. AKBA-mediated inhibition of cellular proliferation was associated with a decreased AR expression at mRNA and protein levels. The results of this study suggest that anti-AR properties ascribed to AKBA could be used as a novel therapeutic chemical.

Metabolism of boswellic acids in vitro and in vivo
Krüger P, Daneshfar R, Eckert GP, Klein J, Volmer DA, Bahr U, Müller WE, Karas M, Schubert-Zsilavecz M, Abdel-Tawab M
Drug Metab Dispos 2008 Jun; 36(6); 1135-1142
Investigators in this study have used Boswellia serrata resin dry extract for the treatment of peritumoral brain edema. Pharmacokinetic studies revealed poor bioavailability, especially of 11-keto-beta-boswellic acid (KBA) and 3-acetyl-11-keto-beta-boswellic acid (AKBA), the most potent BAs. To address the question they determined the metabolic stability of KBA and AKBA in vitro and in vivo. In vitro, KBA yielded metabolic profiles similar to those obtained in-vivo, where as no metabolites of AKBA was identified in vivo and AKBA is not deacetylated to KBA. This study indicates that efficacy of B. serrata extract may be enhanced by increasing the bioavailability of AKBA.

The gastric ulcer protective effect of boswellic acids, a leukotriene inhibitor from Boswellia serrata, in rats
Singh S, Khajuria A, Taneja SC, Khajuria RK, Singh J, Johri RK, Qazi GN
Phytomedicine 2008 Jun; 15(6-7); 408-415
The present study was conducted to evaluate the anti-ulcer efficacy of boswellic acids (BA). The activity was evaluated by following universally accepted animal models viz., pyloric ligation, ethanol-HCl, acetylsalicylic acid, indomethacin and cold restrained stress-induced ulceration in rats. Results revealed that BA possess a dose dependent antiulcer effect against different experimental models. Ulcer score was 39%, 38%, 51%, 31%, 37% and 42% respectively at 250mg/kg. From the data, authors concluded that BA inhibited ulcer production non-specifically in all experimental models.

Boswellic acids: A leukotriene inhibitor also effective through topical application in inflammatory disorders
Singh S, Khajuria A, Taneja SC, Johri RK, Singh J, Qazi GN
Phytomedicine 2008 Jun; 15(6-7); 400-407
In this study authors have used Boswellic acids (BA), a natural mixture isolated from oleo gum resin of Boswellia serrata comprised of four major pentacyclic triterpene acids: beta-boswellic acid, 3-acteyl-beta-boswellic acid, 11-keto-beta-boswellic acid and 3-acetyl-11-keto-beta-boswellic acid to test its efficacy as anti-inflammatory and in Chron's disease. They report that anti-inflammatory activity of BA through topical applications using different acute and chronic models of inflammation. Results of the study revealed that BA when used through topical application is as effective.

Comparison of the irritation potentials of Boswellia serrata gum resin and of acetyl-11-keto-beta-boswellic acid by in vitro cytotoxicity tests on human skin-derived cell lines
Burlando B, Parodi A, Volante A, Bassi AM
Toxicol Lett. 2008 Mar 15; 177(2); 144-149
The investigators in this study have used Indian frankincense a gum resin from Boswellia serrata for testing the antinflammatory properties of boswellic acids, particularly 3-O-acetyl-11-keto-beta-boswellic acid (AKBA). They evaluated in vitro cytotoxicities of B. serrata extract and AKBA on differentiated and un differentiated keratinocytes. In vitro model compared the sensitivities of different human skin cells to B. serrata indicated that the gum resin and AKBA exert moderate to low toxicity on skin.

Acetyl-keto-beta-boswellic acid induces apoptosis through a death receptor 5-mediated pathway in prostate cancer cells
Lu M, Xia L, Hua H, Jing Y
Cancer Res. 2008 Feb 15; 68(4); 1180-1186
In this report authors explored on Acetyl-keto-beta-boswellic acid (AKBA), a triterpenoid isolated from Boswellia carterri and Boswellia serrata, which has been found to inhibit tumor cell growth and induce apoptosis. The apoptotic effects and the mechanisms of action of AKBA were studied in LNCaP and PC-3 human prostate cancer cells. AKBA induced apoptosis in both cell lines at concentrations above 10ug/mL. Results suggest that AKBA induces apoptosis in prostate cancer cells through DR5-mediated pathway.

Anti-inflammatory and anti-atherogenic effects of the NF-kappaB inhibitor acetyl-11-keto-beta-boswellic acid in LPS-challenged ApoE-/- mice
Cuaz-Pérolin C, Billiet L, Baugé E, Copin C, Scott-Algara D, Genze F, Büchele B,
Syrovets T, Simmet T, Rouis M
Arterioscler Thromb Vasc Biol. 2008 Feb; 28(2); 272-277
In this article, the authors studied the effect of acetyl-11-keto-beta-boswellic acid (AKbetaBA), a natural inhibitor of proinflammatory transcription factor NF-kappaB on the development of atherosclerotic lesions in apolipoprotein E-deficient (apoE-/-) mice. Atherosclerotic lesions were induced by weekly LPS injection in apoE-/- mice. LPS alone increased atherosclerotic lesion size by approximately 100%, and treatment with AKbetaBA significantly reduced it by approximately 50%. They conclude that inhibition of NF-kappaB activity might present a new treatment strategy for atherosclerosis.

Identification and functional analysis of cyclooxygenase-1 as a molecular target of boswellic acids
Siemoneit U, Hofmann B, Kather N, Lamkemeyer T, Madlung J, Franke L, Schneider G, Jauch J, Poeckel D, Werz O
Biochem Pharmacol. 2008 Jan 15; 75(2); 503-513
Authors in the present study analysed Boswellic acids (BAs) for its anti-inflammatory principles. Initially, it was found that BAs inhibit leukotriene biosynthesis and 5-lipoxygenase. They demonstrated that BAs also interfere with platelet-type 12-lipoxygenase. Here, they show that Bas, preferably 3-O-acetyl-11-keto-beta-BA (AKBA), inhibit COX-1 product formation in intact human platelets (IC(50)=6 microM) and the activity of isolated COX-1 enzyme (IC(50) =32 microM). In conclusion, AKBA directly interfere with COX-1 and may mediate their anti-inflammatory action.

Cytotoxic and apoptotic activities of novel amino analogues of boswellic acids
Shah BA, Kumar A, Gupta P, Sharma M, Sethi VK, Saxena AK, Singh J, Qazi GN, Taneja SC
Bioorg Med Chem Lett. 2007 Dec 1; 17(23); 6411-6416
In this study authors have checked if the 4-Amino analogues prepared from beta-boswellic acid and 11-keto-beta-boswellic acid, wherein the carboxyl group in ursane nucleus was replaced by an amino function via Curtius reaction. The results displayed improved cytotoxicity than the parent molecules and also exhibited apoptotic activity.

Incensole acetate, a novel anti-inflammatory compound isolated from Boswellia resin, inhibits nuclear factor-kappa B activation
Moussaieff A, Shohami E, Kashman Y, Fride E, Schmitz ML, Renner F, Fiebich BL, Munoz E, Ben-Neriah Y, Mechoulam R
Mol Pharmacol 2007 Dec; 72(6); 1657-1664
The authors analysed Boswellia resin for its anti-inflammatory activity using inhibitor of nuclear factor-kappaB alpha (IkappaB alpha) degradation in tumor necrosis factor (TNF) alpha-stimulated HeLa cells. They isolated two novel nuclear factor-kappaB (NF-kappaB) inhibitors from the resin, their structures elucidated as incensole acetate (IA) and its nonacetylated form, incensole. Cembrenoid diterpenoids specifically IA may thus constitute a potential novel group of NF-kappaB inhibitors

Screening of plant extracts for antimicrobial activity against bacteria and yeasts with dermatological relevance
Weckesser S, Engel K, Simon-Haarhaus B, Wittmer A, Pelz K, Schempp CM
Phytomedicine 2007 Aug; 14(7-8); 508-516
The authors have screened six plant extracts and isolated compounds for anti microbial effects on bacteria and yeasts with dermatological relevance. The following plant extracts have been tested: Gentiana lutea, Harpagophytum procumbens, Boswellia serrata, Usnea barbata, Rosmarinus officinalis and Salvia officinalis. Additionally, the following compounds were tested: usnic acid, carnosol, carnosic acid, ursolic acid, oleanolic acid, harpagoside, boswellic acid and gentiopicroside. The extracted compounds were tested against 29 aerobic and anaerobic bacteria. It is concluded that anti microbial effects of plant extracts may be used for treatment of acne vulgaris and seborrhoic eczema.

Boswellic acids and glucosamine show synergistic effect in preclinical anti-inflammatory study in rats
Singh S, Khajuria A, Taneja SC, Khajuria RK, Singh J, Qazi GN
Bioorg Med Chem Lett. 2007 Jul 1; 17(13); 3706-3711
Authors in the present study revealed the synergistic effect of boswellic acid mixture (BA) and glucosamine for anti-inflammatory and anti-arthritic activities in rats. Five groups of animals were included in each of the study: the vehicle control, positive control, boswellic acids (250 mg/kg), glucosamine (250 mg/kg) and a combination of boswellic acids (125 mg/kg) and glucosamine (125 mg/kg). The combination of boswellic acids and glucosamine did result in significant anti-arthritic activity. In conclusion, a synergistic effect was observed in chronic inflammatory conditions when two chemical entities were administered in combination in this preclinical study.

Natural products as a gold mine for arthritis treatment
Khanna D, Sethi G, Ahn KS, Pandey MK, Kunnumakkara AB, Sung B, Aggarwal A, Aggarwal BB
Curr Opin Pharmacol 2007 Jun; 7(3); 344-3451
In this study investigators reviewed the role of natural products. Arthritis, an nflammation of joints, is usually a chronic disease that results from dysregulation of pro-inflammatory cytokines and pro-inflammatory enzymes. Numerous plant derivatives can suppress cell signaling intermediates, including curcumin (from turmeric), resveratrol (red grapes, cranberries and peanuts), tea polyphenols, genistein (soy), quercetin (onions), silymarin (artichoke), guggulsterone (guggul), boswellic acid (salai guggul) and withanolides (ashwagandha). Preclinical and clinical studies suggest that these agents have potential for arthritis treatment.

Effect of acetyl 11-keto beta-boswellic acid on metastatic growth factor responsible for angiogenesis
Singh SK, Bhusari S, Singh R, Saxena A, Mondhe D, Qazi GN
Vascul Pharmacol. 2007 May; 46(5); 333-337
Present study revealed the role of Basic fibroblast growth factor (bFGF), a metastatic growth factor is known to be one of the promoting factors in the tumor induced angiogenesis. Authors screened the antiangiogenic activity of acetyl 11-keto beta-boswellic acid against bFGF-induced angiogenesis. Acetyl 11-keto beta-boswellic acids (10 mg/kg/d) inhibited the Matrigel+bFGF-induced angiogenesis significantly.

Co-administration of acetyl-11-keto-beta-boswellic acid, a specific 5-lipoxy genase inhibitor, potentiates the protective effect of COX-2 inhibitors in kainic acid-induced neurotoxicity in mice
Bishnoi M, Patil CS, Kumar A, Kulkarni SK
Pharmacology 2007; 79(1); 34-41
Authors looked at the role of Kainic acid, a glutamate receptor agonist responsible for neuronal excitotoxicity and oxidative damage via different mechanisms is capable of stimulating both COX-2 and 5-LOX in the brain. Study was designed to study the effects of COX inhibitors and a 5-LOX inhibitor (acetyl-11-keto-beta-boswellic acid; AKBA) and the combination of these inhibitors on kainic acid induced excitotoxicity and oxidative and nitrosative damage in mice. The results indicated that AKBA, indomethacin, and nimesulide per se did not produce any change in the behavioural parameters.