Title : Anti-tyrosinase, anti-cholinesterase and cytotoxic activities of extracts and phytochemicals from the Tunisian Citharexylum spinosum L.: Molecular docking and SAR analysis - Saidi_2020_Bioorg.Chem_102_104093 |
Author(s) : Saidi I , Nimbarte VD , Schwalbe H , Waffo-Teguo P , Harrath AH , Mansour L , Alwasel S , Ben Jannet H |
Ref : Bioorg Chem , 102 :104093 , 2020 |
Abstract :
Previously phytochemical investigations carried out on the flowers and trunk bark extracts of Citharexylum spinosum L. tree, allowed the isolation of twenty molecules belonging to several families of natural substances [triterpene acids, iridoid glycosides, phenylethanoid glycosides, 8,3'-neolignan glycosides, together with other phenolic compounds]. In the present work, a biological evaluation (anti-tyrosinase, anticholinesterase and cytotoxic activities) was performed on the prepared extracts and the isolated secondary metabolites. The results showed that the EtOAc extract of the trunk bark displayed the highest anti-tyrosinase effect with a percent inhibition of 55.0 +/- 1.8% at a concentration of 100 mug/mL. The highest anticholinesterase activity was presented by the same extract with an IC(50) value of 99.97 +/- 3.01 mug/mL. The EtOAc extract of flowers and that of the trunk bark displayed the best cytotoxic property with IC(50) values of 96.00 +/- 2.85 and 88.75 +/- 2.00 mug/mL, respectively, against the human cervical cancer cell line (HeLa), and IC(50) values of 188.23 +/- 3.88 and 197.00 +/- 4.25 mug/mL, respectively, against the human lung cancer (A549) cell lines. Biological investigation of the pure compounds showed that the two 8,3'-neolignan glycosides, plucheosides D(1)-D(2), generate the highest anti-tyrosinase potency with a percent inhibition of 61.4 +/- 2.0 and 79.5 +/- 2.3%, respectively, at a concentration of 100 muM. The iridoid glycosides exhibited a significant anticholinesterase activity with IC(50) values ranging from 17.19 +/- 1.02 to 52.24 +/- 2.50 muM. Triterpene pentacyclic acids and iridoid glycosides exerted encouraging cytotoxic effects against HeLa with IC(50) values ranging from 9.00 +/- 1.10 to 25.00 +/- 1.00 muM. The study of the structure-activity relationship (SAR) has been sufficiently and widely discussed. The natural compounds that exhibited the significant bioactivities were docked. |
PubMedSearch : Saidi_2020_Bioorg.Chem_102_104093 |
PubMedID: 32717693 |
Saidi I, Nimbarte VD, Schwalbe H, Waffo-Teguo P, Harrath AH, Mansour L, Alwasel S, Ben Jannet H (2020)
Anti-tyrosinase, anti-cholinesterase and cytotoxic activities of extracts and phytochemicals from the Tunisian Citharexylum spinosum L.: Molecular docking and SAR analysis
Bioorg Chem
102 :104093
Saidi I, Nimbarte VD, Schwalbe H, Waffo-Teguo P, Harrath AH, Mansour L, Alwasel S, Ben Jannet H (2020)
Bioorg Chem
102 :104093