TITLE:
Fusarium lini Potential for the Biotransformation of Norandrostenedione and Evaluation of Urease and Chymotrypsin Properties of the Transformed Products
AUTHORS:
Simeon Pierre Chegaing Fodouop, Alex Doris Kengni Mboussaah, Didiane Yemele Mefokou, Alain Bertrand Fowa, Mahwish Siddiqui, Gabriel T. Kamsu, Donatien Gatsing, Muhammad Iqbal Choudhary
KEYWORDS:
Chymotrypsin Inhibition, Norandrostenedione, Fusarium lini, Urease Inhibition
JOURNAL NAME:
Advances in Biological Chemistry,
Vol.11 No.2,
April
22,
2021
ABSTRACT: Several androgenic steroids have been biotransformed
by fungi into metabolites with numerous biological properties. Incubation of
norandrostenedione (1) with Fusarium lini NRRL 2204 was carried out for the first time, yielding two new
metabolites, 3,7β-dihydroxy-19-norandrost-1,3,5-trien-17-one (3) and 6α,10β,17β-trihydroxy-19-nor-4-androsten-3-one (4), along with three known compounds, 3-hydroxy-19-norandrost-1,3,5-trien-17-one
(2), 10β, 17β-dihydroxy-19-nor-4-androsten-3-one (5) and 10β-hydroxy-19-nor-4- androsten-3,17-dione (6). Their structures were elucidated by extensive
spectroscopic analyses, including 1D-, 2D-NMR, and HR-MS experiments. Substrate 1 and its derivatives 2-6 were evaluated in vitro for their urease and chymotrypsin inhibitory properties.
Compounds 2 and 3 were found to have strong urease activity with
IC50 = 23.7 ± 0.17 and 10.2 ± 0.28 μm, respectively, as compared
to the standard drug thiourea (IC50 = 21.6 ± 0.12 μm). Compounds 4, 5 and 6 showed good chymotrypsin activity with IC50 values of
6.4 ± 0.19, 15.6 ± 0.46 and 18.4 ± 0.65 μm, respectively, as compared to standard chymostatin
with IC50 = 5.7 ± 0.14 μm. These transformed metabolites may form the basis for the future
development of new drugs against ulcer, inflammation, bacterial and viral
diseases.