Inhibition of Candida rugosa Lipase by Secondary Metabolites Extracts of Three Algerian Plants and their Antioxydant Activities

Abstract

Lipase inhibitors have generated a great interest because they could help in the prevention or the therapy of lipase-related diseases. Therefore, the aim of this work was to evaluate the inhibitory effect of secondary metabolites extracts such as phenolic compounds and saponins of three Algerian medicinal plants: Achillea santolina, Inonotus hispidus and Zizyphus lotus, indeed their antiradicalaire activity using DPPH• (1, 1-diphenyl-2-picryl-hydrazyl). The phenolic extracts have shown a strong antiradicalaire activity than the saponin extracts with EC50 values ranged from 6 to 11 µg/ml and from 51 to 82 µg/ml, respectively. The enzymatic inhibition produced by these plant extracts is described here for the first time. The results have shown that the phenolic extracts are more potent than the saponin extracts with Ki values ranged from 0.011 mg/ml to 0.027 mg/ml for phenolic extracts, and ranged from 0.071 mg/ml to 0.69 mg/ml for saponin extracts. The nature, mechanism and possible physiological relevance of lipase inhibition by extract components are discussed.

Harmaline and hispidin from Peganum harmala and Inonotus hispidus with binding affinity to Candida rugosa lipase: In silico and in vitro studies

“…The powdered material of the two species (2 g) was extracted for 24 h with 100 ml of increased solvent polarity following this order: hexane, dichloromethane, ethyl acetate, acetone and methanol, this process was repeated until total exhaustion of metabolites. The second method applied for I. hispidus is the same used by Benarous et al [14]. Therefore, the third method of Ross and Rain (1977) in Harborne [23] was used for the alkaloid extraction for P. harmala.…”

“…It produces a considerable quantity of yellow-brown pigments, e.g. hispidin, bis-noryangonin and hypholomin B [13,14]. This fungus is used in folk medicine for treating gastric ulcer [15] and it is known by its antiviral activity [16].…”

“…Obesity increases the risk of suffering from a number diseases, including hypertension, type 2 diabetes, dyslipidemia, coronary artery disease, osteoarthritis and cancer of postmenopausal breast. The prevalence of obesity was significantly increased in the past 30 years, and about 32% of adults in the United States are currently obese [14,20].…”

“…mangiferin, hesperidin) [60][61][62]. Therefore, the investigation of new natural lipase inhibitors for the therapy of candidiasis and obesity [14] has generated a great interest.…”

“…Continuing our search for new natural lipase inhibitors [14], we have found that the phenolic and alkaloid extracts of I. hispidus and P. harmala exhibit substantial binding affinity for C. rugosa lipase. This study aimed first to identify the bioactive compounds of the phenolic and alkaloids extracts and evaluate their binding affinity to C. rugosa lipase and, second, to predict the binding orientation using docking experiments.…”