10.3.1 Antihypercholesterolemic Compounds
from Endophytes
HMG–CoA reductase (HMGR) is the key enzyme in the cholesterol biosynthesis
pathway and it is the attractive target of several antihypercholesterolemic drugs.
Statins, the fungal secondary metabolites, are widely used as competitive inhibitors
of HMG–CoA reductase all over the world. Lovastatin, a highly potent inhibitor of
HMG–CoA reductase is commercially produced using a micro-fungus,Aspergillus
terreus(Patil et al.2011). Endophytic fungus,Aspergillus nigerwas isolated from
Taxus baccatawhich was able to produce lovastatin when cultivated in solid-state
fermentation (Raghunath et al.2012 ). In another study, rosuvastatin, a potent inhi-
bitor of HMG-CoA reductase, used for treating dyslipidemias, was produced from
Penicillium citrinumandP. brevicompactum(Scott et al.2004). Bhargavi et al.
(2014 ) studied lovastatin production using soil and endophytic fungi, demonstrated
that the soil isolate,Aspergillus terreusNCBI (KM017963) produced lovastatin
whereas none of the endophytic fungi tested showed lovastatin production when
cultured in solid-state fermentation. Endophytic fungi have been recognized as an
important source for these antihypercholesterolemic compound/metabolites and
structures of a few compounds obtained from them are shown in Fig.10.2.
Another metabolite, chartarlactams A-P, phenylspirodrimanes produced by
Sponge- associated endophytic fungusStachybotrys chartarumexhibited potent
antihyperlipidemic activity in HepG2 cells assessed by Oil Red O staining (Yong
et al. 2013 ). On the other hand, endophytic fungusMycosphaerellasp. PF13 was
Fig. 10.2 Antihypercholesterolemic compounds produced by endophytic fungi
220 S.I. Mohammed et al.