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. 2022 Feb 14;11(4):514.
doi: 10.3390/plants11040514.

Phytochemical Screening of Rosmarinus officinalis L. as a Potential Anticholinesterase and Antioxidant-Medicinal Plant for Cognitive Decline Disorders

Majid Rasool Kamli  1   2 , Abeer Abdullah M Sharaf  3 , Jamal S M Sabir  1   2 , Irfan A Rather  1   2
Affiliations

Phytochemical Screening of Rosmarinus officinalis L. as a Potential Anticholinesterase and Antioxidant-Medicinal Plant for Cognitive Decline Disorders

Majid Rasool Kamli et al. Plants (Basel). .

Abstract

The inhibition of acetylcholinesterase (AChE) by cholinergic agents has been promoted as a potent strategy for treating and managing cognitive decline disorders. A wide range of natural products has long been used as potential sources or formulations of cholinergic inhibitors. Therefore, this study aimed to evaluate different Rosmarinus officinalis L. (R. officinalis) extracts for their AChE inhibitory activity using galanthamine as a standard AChE inhibitor. In this study, the ethyl-acetate extract (at a concentration of 250 µg/mL) exhibited the greatest inhibitory effect against AChE with significant inhibition of 75%, comparable to the inhibitor galanthamine with an inhibition of 88%. Kinetic analysis revealed that the extracts could induce a mixed type of inhibition, as observed in the case of galanthamine, with the highest increased Km and decreased Vmax values in the ethyl acetate extract. The antioxidant potential of the three extracts tested was found to be in the order of ethyl-acetate > ethanol > aqueous, with IC50 values of 272 µg/mL, 387 µg/mL, and 534 µg/mL, respectively. Ethyl-acetate was found to have the highest total phenolic content in all extracts. Further, in silico study showed structural binding characterization of rosmarinic acid and carnosic acid with human AChE enzyme. Rosmarinic acid showed strong binding and formed two hydrogen-bonding interactions with Ser-293 and Arg-296. In light of this, the ethyl-acetate extract of the plant may provide some novel potential pharmacological leads for treating and managing cognitive disorders such as Alzheimer's.

Keywords: Alzheimer’s disease; Rosmarinus officinalis; acetylcholinesterase; carnosic acid; molecular docking; rosemary; rosmarinic acid.

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Conflict of interest statement

The authors declare no conflict of interest. This research did not involve any animal and/or human participant.

Figures

Figure 1
Figure 1
FTIR spectra of R. officinalis extract.
Figure 2
Figure 2
Major chemical constituents present in the R. officinalis extract.
Figure 3
Figure 3
Total phenolic content of different extracts of R. officinalis. Data represent the mean of the results obtained from three independent measurements with their standard deviations as error bars. Data were analyzed using t-test and one-way ANOVA. * Indicates significance at p < 0.05 when compared to the aqueous (p value = 0.0149), ns indicates not significant (p value = 0.0606).
Figure 4
Figure 4
DPPH radical scavenging activity of the extracts of R. officinalis. Catechin was used as a positive control. The presented data represent the mean of three independent measurements with an average 5–7% error. Data were analyzed using one-way ANOVA *** and **** indicate significance at p < 0.05 when compared to aqueous with p values 0.006 and 0.001, respectively.
Figure 5
Figure 5
Acetylcholinesterase inhibition potential of extracts of R. officinalis. Results presented are the mean of three independent measurements.
Figure 6
Figure 6
Kinetics of acetylcholinesterase inhibition by R. officinalis. Lineweaver–Burk plot of inhibition of acetylcholinesterase by different extracts of R. officinalis. Representative data are the average of 3 independent measurements.
Figure 7
Figure 7
Docking complex of cholinesterase with (a) rosmarinic acid and (b) carnosic acid.
Figure 8
Figure 8
Surface structure of cholinesterase with (a) rosmarinic acid and (b) carnosic acid.
Figure 9
Figure 9
Interaction of amino acid residues of acetylcholinesterase with (a) rosmarinic acid and (b) carnosic acid.
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