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Buddlejol, a new α-chymotrypsin inhibitor from Buddleja asiatica

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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 α-amyrin (5), respectively. The structure of Buddlejol (1) was established as (24S)-stigmast-5,22-diene-7β-ethoxy-3β-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 µM 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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Authors and Affiliations

  1. Department of Chemistry, Shaheed Benazir Bhutto University, Sheringal, Dir (Upper), KP, 18000, Pakistan

    Farman Ali Khan

  2. Department of Biotechnology, Shaheed Benazir Bhutto University, Sheringal, Dir (Upper), KP, 18000, Pakistan

    Nasir Mehmood Khan

  3. Department of Biotechnology, University of Science and Technology, Bannu, KP, 28100, Pakistan

    Hidayat Ullah Khan

  4. Department of Chemistry, University of Science and Technology, Bannu, KP, 28100, Pakistan

    Shahanz Khan & Nayab Ali

  5. Department of Pharmacy, Shaheed Benazir Bhutto University, Sheringal, Dir (Upper), KP, 18000, Pakistan

    Shujaat Ahmad

  6. Chemical and Forensic Sconces, University of Bradford, Bradford, BD7 1DP, UK

    Derek James Maitland

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  1. Farman Ali Khan
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  2. Nasir Mehmood Khan
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  3. Hidayat Ullah Khan
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  4. Shahanz Khan
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  5. Nayab Ali
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  6. Shujaat Ahmad
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  7. Derek James Maitland
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Correspondence to Farman Ali Khan.

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Khan, F.A., Khan, N.M., Khan, H.U. et al. Buddlejol, a new α-chymotrypsin inhibitor from Buddleja asiatica . Med Chem Res 24, 980–986 (2015). https://doi.org/10.1007/s00044-014-1192-9

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  • DOI: https://doi.org/10.1007/s00044-014-1192-9

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