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Buddlejol, a new alpha-chymotrypsin inhibitor from Buddleja asiatica

Authors Khan, Farman Ali; Khan, Nasir Mehmood; Khan, Hidayat Ullah; Khan, Shahanz; Ali, Nayab; Ahmad, Shujaat; Maitland, Derek James

Journal MEDICINAL CHEMISTRY RESEARCH , MAR 2015,3:24

DOI 10.1007/s00044-014-1192-9

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.

Species covered 七里香 Buddleja asiatica