Buddlejol, a new alpha-chymotrypsin inhibitor from Buddleja asiatica
Khan, F.A. Khan, N.M. Khan, H.U. Khan, S. Ali, N. Ahmad, S. Maitland, Derek J.
Khan, F.A.
Khan, N.M.
Khan, H.U.
Khan, S.
Ali, N.
Ahmad, S.
Maitland, Derek J.
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2015
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Abstract
Buddlejol (1), a new sterol, has been isolated from the ethyl acetate soluble fraction of the antispasmodic plant Buddleja asiatica along with stigmasterol (2), lignoceric acid (3), taraxerol (4) and alpha-amyrin (5), respectively. The structure of Buddlejol (1) was established as (24S)-stigmast-5,22-diene-7 beta-ethoxy-3 beta-ol by spectral analysis and comparison with closely related structures. Buddlejol revealed to be a competitive inhibitor of chymotrypsin with the Ki value of 10.60 A mu M as indicated by Lineweaver-Burk and Dixon plots and their re-plots against its chymotrypsin inhibition assay, while the other compounds showed less inhibitory potential. The bioassay-guided isolation was stimulated by the preliminary cytotoxic screening of various fractions of B. asiatica.
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Khan FA, Khan NM, Khan HU et al (2015) Buddlejol, a new alpha-chymotrypsin inhibitor from Buddleja asiatica. Medicinal Chemistry Research. 24(3): 980-986.
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