alpha-Amyrin palmitate
alpha-Amyrin palmitate is antiarthritic in the adjuvant model of arthritis in rats. alpha-Amyrin palmitate is a potent non-competitive inhibitor of chymotrypsin (Ki=6 microM), it also shows weak cytotoxicity against the A2780 human ovarian cancer cell line.
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Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to
24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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Drugs Exp Clin Res. 1994;20(1):1-5.
Effect of alpha-amyrin palmitate on adjuvant arthritis.[Pubmed:
7924889]
METHODS AND RESULTS:
alpha-Amyrin palmitate was synthesized and tested on adult male Wistar rats made arthritic by subplantar injection of complete Freund's adjuvant. When administered orally at 66 mg/kg BW every 48 h for 5 days from days 32 to 40 post-adjuvant and assessed on day 50, alpha-Amyrin palmitate returned the increases in serum hyaluronate and blood granulocytes toward non-arthritic levels and corrected the moderate anaemia of adjuvant arthritis. Histological examinations of the second and third proximal foot interphalangeal joints showed reduced synovial proliferation and invasion of joints and reduced leucocyte infiltration of bone marrow in alpha-Amyrin palmitate-treated rats. In addition, the drug prevented or reduced bone (subchondral or cortical) and cartilage (articular) destruction in arthritic rats.
CONCLUSIONS:
The results suggest that alpha-Amyrin palmitate is antiarthritic in the adjuvant model of arthritis in rats.
Planta Med. 2000 Apr;66(3):206-10.
Inhibition of serine proteases by anti-inflammatory triterpenoids.[Pubmed:
10821043]
The lupane triterpenoid lupeol, the ursane triterpenoid alpha-amyrin and esters of these compounds are present in the bark of roots of Alstonia boonei (Apocynaceae) and have anti-inflammatory properties.
METHODS AND RESULTS:
alpha-Amyrin is a competitive inhibitor of bovine trypsin and chymotrypsin (Ki values 29 microM and 18 microM, respectively). Lupeol linoleate, lupeol palmitate and alpha-amyrin linoleate are non-competitive inhibitors of trypsin (Ki values 7 microM, 10 microM and 16 microM, respectively). alpha-Amyrin linoleate is also a non-competitive inhibitor of chymotrypsin (Ki value 28 microM). Lupeol is a competitive inhibitor of both trypsin and chymotrypsin (Ki values 22 and 8 microM, respectively). alpha-Amyrin palmitate is a potent non-competitive inhibitor of chymotrypsin (Ki 6 microM). Lupeol, alpha-amyrin and the palmitic and linoleic acid esters of these compounds are ineffective or very weak as inhibitors of porcine pancreatic elastase and of Lucilia cuprina and Helicoverpa punctigera leucine aminopeptidases.
CONCLUSIONS:
These hydrophobic triterpenoids represent further examples of anti-inflammatory triterpenoids that are PKA inhibitors as well as being selective protease inhibitors.obic triterpenoids represent further examples of anti-inflammatory triterpenoids that are PKA inhibitors as well as being selective protease inhibitors.
