Research Highlights
1998 - 1999
 
  
on Boswellin from 1998 to 1999
 

Redefining Our Standards, Boswellin® The Only Natural Leukotriene and HLE Inhibitor®
Majeed, M. Prakash, L, Badmaev, V., Nujoma, Y., Natarajan, S., Norton, T., Sysler, M., Gopinathan, S., and Alegesan, K. Sabinsa Corporation, 1999.

Acetyl-11-keto-b-Boswellic acid induces apoptosis in HL-60 and CCRF-CEM cells and inhibits topoisomerase I
Hoernlein, R.F., Orlikowsky, TH., Zehrer, C., Niethammer, D., Sailer, E.R., Simmet, TH., Dannecker, G.E., and Ammon, H.P.T.
J. Pharm. Exp. Therap. 1999, 288(2), 613-619

The present study focused on the antiproliferative action of Acetyl-11-keto-beta-boswellic acid (AKBA). It is a pentacyclic triterpene that inhibits 5-lipoxygenase in a selective, enzyme directed, nonredox, noncompetitive manner. They investigated a possible effect of AKBA on leukemic cell growth, proliferation of HL-60 and CCRF-CEM cells in the presence of AKBA and amyrin. The results suggest that induction of apoptosis in HL-60 by AKBA may be due to inhibition of topoisomerase I in these cells.

Boswellic acid acetate induces differentiation and apoptosis in leukemia cell lines
Jing Y, Nakajo S, Xia L, Nakaya K, Fang Q, Waxman S, Han R
Leuk Res. 1999 Jan; 23(1); 43-50

The study focused on the role of Boswellic acid acetate (BC-4), a compound isolated from the herb Boswellia carterii Birdw. can induce differentiation and apoptosis of leukemia cells. The growth inhibition effect was dose and time dependent and proved that BC-4 can induce cell apoptosis. The dual apoptotic and differentiation effects of BC-4 suggest it may be used in treatment of leukemia.

Weisman B, (1999). Natural composition for treating bone or joint inflammation, US Patent 5,888,514

Boswellic acids and malignant glioma: induction of apoptosis but no modulation of drug sensitivity
Glaser T, Winter S, Groscurth P, Safayhi H, Sailer ER, Ammon HP, Schabet M, Weller M
Br J Cancer 1999 May; 80(5-6); 756-765

The authors explored the role of Boswellic acids for phytotherapeutic anti-inflammatory use in the treatment of cerebral oedema. Here, they report that boswellic acids are cytotoxic to malignant glioma cells at low micromolar concentrations. In contrast to steroids, BA subtoxic concentrations do not interfere with cancer drug toxicity. Further studies are required to determine whether boswellic acids may be a useful for management of human malignant glioma.

Effects of Boswellia serrata gum resin in patients with bronchial asthma: results of a double-blind, placebo-controlled, 6-week clinical study
Gupta I, Gupta V, Parihar A, Gupta S, Lüdtke R, Safayhi H, Ammon HP
Eur J Med Res. 1998 Nov 17; 3(11); 511-514

This clinical study focused on the use of boswellic acids in a double-blind, placebo-controlled study of forty patients, 23 males and 17 females in the age range of 18 - 75 years having mean duration of illness, bronchial asthma of 9.58 +/- 6.07 years were treated with a preparation of gum resin of 300 mg thrice daily for a period of 6 weeks. 70% of patients showed improvement in conditions such as dysponoea, rhonchi, ESR. This data show a definite role for Boswellia serrata in the treatment of bronchial asthma.

Characterization of acetyl-11-keto-beta-boswellic acid and arachidonate-binding regulatory site of 5-lipoxygenase using photoaffinity labeling
Sailer ER, Schweizer S, Boden SE, Ammon HP, Safayhi H
Eur J Biochem 1998 Sep 1; 256(2); 364-368
Authors in this study used AKBA (acetyl-11-keto-beta-boswellic acid), a natural pentacyclic triterpene. It is the only leukotriene-synthesis inhibitor identified that inhibits 5 lipoxygenase activity. To characterize AKBA's effector site they prepared azido 125-IKBA (4-azido-5-125 iodo-salicyloyl-beta-alanyl-11-keto-beta-boswellic acid) as a photoaffinity analogue. The results conclude that AKBA-binding site is identical with a regulatory second arachidonate binding site of the enzyme.

Nonredox 5-lipoxygenase inhibitors require glutathione peroxidase for efficient inhibition of 5-lipoxygenase activity
Werz O, Szellas D, Henseler M, Steinhilber D
Mol Pharmacol 1998 Aug; 54(2); 445-451

Present study focused on the Nonredox type 5-lipoxygenase (5-LO) inhibitors, such as ZM 230487, its methyl analogue ZD 2138, Merck compound L-739,010, which suppress cellular leukotriene synthesis. In cell homogenates up to 150-fold higher concentrations are required for 5-LO activity. The data suggest that low hydroperoxide concentrations are important for efficient 5-LO inhibition by ZM 230487. This data suggest that physiological conditions associated with oxidative stress and increased peroxide levels lead to impaired efficacy of nonredox type 5-LO inhibitors like ZM 230487 or L-739010.

Effects of boswellic acids extracted from a herbal medicine on biosynthesis of leukotrienes and course of experimental autoimmune encephalomyelitis
Wildfeuer A, Neu IS, Safayhi H, Metzger G, Wehrmann M, Vogel U, Ammon HP
Arzneimittelforschung 1998 Jun; 48(6); 668-674

In this study authors explored on mixed acetylboswellic acids, pentacyclic triterpenes extracted from Boswellia serrata Roxb., significantly inhibited release of leukotrienes from human polymorphonuclear neutrophil leukocytes with IC50 values of 8.48 micrograms/ml and 8.43 micrograms/ml, respectively. Purified acetyl-11-keto-beta-boswellic acid was about three times more potent inhibitor. The boswellic acids have thus been characterized as selective, non redox and potent inhibitors of the biosynthesis of leukotrienes.

Inhibitory activity of boswellic acids from Boswellia serrata against human leukemia HL-60 cells in culture
Shao Y, Ho CT, Chin CK, Badmaev V, Ma W, Huang MT
Planta Med. 1998 May; 64(4); 328-331

The study looked at the four major triterpene acids including beta-boswellic acid (1), 3-O-acetyl-beta-boswellic acid (2), 11-keto-beta-boswellic acid (3), and 3-O-acetyl-11-keto-beta-boswellic acid (4), isolated from Boswellia serrata and examined their antitumor activity. Among them, compound 4 induced the most pronounced inhibitory effects on DNA, RNA and protein synthesis with IC50 values of 0.6, 0.5, and 4.1 microM, respectively. Compound 4 significantly inhibited the cellular growth of HL-60 cells, but did not affect cell viability.

Simmet, T. and Ammon, H.P.T. (1998), Use of boswellic acid for treating brain tumours. Patent WO 96/19212

 
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