Pancreatic lipase inhibition activity of trilactone terpenes of Ginkgo biloba

Abstract

The prevalence of obesity is increasing at an alarming rate, but, unfortunately, only a few drugs are currently available on the market. In the present study, the methanolic extract of Ginkgo biloba L. (Ginkgoaceae) was investigated as an inhibitor of pancreatic lipase (PL) in an attempt to explain its hypolipidaemic activity. In vitro assay of G. biloba leaves extract revealed a substantial PL inhibition activity (IC(50) = 16.5 µg/mL). Further investigation was performed by employing theoretical docking simulations and experimental testing to uncover the active constituents responsible for G. biloba anti-lipase activity. Virtually, terpene trilactones, including ginkgolides and bilobalide, were found to fit within the binding pocket of PL via several attractive interactions with key amino acids. Experimentally, ginkgolides A, B, and bilobalide were found to inhibit PL significantly (IC(50) = 22.9, 90.0, and 60.1 µg/mL, respectively). Our findings demonstrated that the hypolipidaemic effects of G. biloba extract can be attributed to the inhibition of PL by, at least in part, terpene trilactones. In conclusion, this work can be considered a new step towards the discovery of new natural safe hypolipidaemic PL inhibitors.

Anti-obesity potentials of aqueous and methanol extracts of <i>Vernonia amygdalina</i> Del. Leaves in high-fat diet fed rats

“…The observed hypolipidemic effect is suggestive of a possible effect on enzymes involved in lipid homeostasis, chief among which is the pancreatic lipase. This is noteworthy, especially given that the control drug is known to inhibit the said enzyme and some plant extracts are known to act in this manner (Bustanji et al, 2011). Though the differences in serum blood glucose concentrations were not statistically significant, it is worth noting that the extracts, especially AEVA, reduced the serum blood glucose concentrations to the level observed in the normal rats.…”

“…A few examples illustrate this assertion. Terpene trilactones from Ginkgo biloba L. possess hypolipidaemic and antiobesity activities as they are able to inhibit pancreatic lipase (Bustanji et al, 2011). The coumarin, esculetin, from Fraxinus rhynchophylla is reported to be active in inhibiting early stage adipogenic differentiation thereby being useful in obesity management (Shin et al, 2010) and in preventing HFD-induced hepatic steatosis (Um et al, 2013).…”

Antiobesity and antihyperglycaemic effects of Adiantum capillus-veneris extracts: in vitro and in vivo evaluations

“…According to Bustanji et al (2011), in vitro enzymatic PL activity was assayed. Subsequent determinations were undertaken for the tested extracts/phytoconstituents in comparison to the control evaluations to calculate the concentration value required for PL 50% inhibition (IC 50 ).…”

Antilipolytic and hypotriglyceridemic effects of dietary <i>Salvia triloba</i> Lf (Lamiaceae) in experimental rats

“…Enzyme assay was conducted by the spectrophotometric method as per the protocol from Al-Hallaq et al [8][9] and Bustanji et al [15]. Subsequent determinations were undertaken for the tested extracts and orlistat (n = 3) to calculate the concentration required for the PL 50 % inhibition (IC 50 ).…”