Modern and traditional extraction techniques affect chemical composition and bioactivity of Tanacetum parthenium (L.) Sch.Bip

Tanacetum parthenium (L.) Sch.Bip (TP), a flowering plant, is famous in traditional medicine to prevent migraine and headache. However, there is currently a dearth of studies to advocate the phytochemical profile and bio- logical propensities of extracts prepared from this plant. This study endeavors to highlight the biological po- tential of TP extracts prepared by modern (ultrasound-UAE, microwave-MAE and accelerated-ASE extractions) and traditional (maceration and Soxhlet) extraction techniques. The chemical profile of the extracts was es- tablished via ultra-high-pressure liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) technique. Sixty different polyphenolic compounds belonging to the classes of phenolic acids, flavonoid glycosides and flavonoid aglycones were recorded in the extracts. Additionally, the quantity of 17 components was measured using appropriate standards and it was found that the modern extraction gave extracts with the higher content of observed compounds than the traditional techniques. Evaluation of antioxidant activity was determined in vitro via five standard assays. The inhibitory potential of TP extracts against key enzymes implicated in the non- communicable diseases such as diabetes (α-amylase and α-glucosidase), neurodegenerative diseases (acetyl- and butyrylcholinesterase) and skin diseases (tyrosinase), was assessed. Potent antioxidant ability of all TP extract was revealed with a predominance for the extracts yielded using the ASE method. This potent antioxidant activity of the extracts corroborated with the high phenolic (65.05 ± 0.27 mg gallic acid equivalent (GAE)/g extract) and flavonoid contents (55.40 ± 0.52 mg rutin equivalent (RE)/g extract). Tanacetum parthenium ex- tracts also showed significant α-glucosidase inhibitory activity (1.63–1.67 mmol acarbose equivalent (ACAE)/g extract) and moderate inhibition activity against α-amylase (0.51-0.56 mmol ACAE/g extract). The extracts also showed potent activity against cholinesterases and tyrosinase. This study tend to validate the use of TP extracts obtained by novel extraction techniques such as ASE, as potent bioactive extracts to be further studied for therapeutic bio-product development

LC-ESI-QTOF-MS/MS Analysis, Cytotoxic, Antiviral, Antioxidant, and Enzyme Inhibitory Properties of Four Extracts of Geranium pyrenaicum Burm. f.: A Good Gift from the Natural Treasure

This study focused on the biological evaluation and chemical characterization of Geranium pyrenaicum Burm. f. Different solvent extracts (hexane, ethyl acetate, methanol, and water extracts) were prepared. The phytochemical profile, antioxidant, and enzyme inhibitory activity were investigated. Cytotoxicity was assessed using VERO, FaDu, HeLa and RKO cells. The antiviral activity was carried out against HSV-1 (Herpes simplex virus 1) propagated in VERO cell line. The aqueous extract, possessing high phenolic content (170.50 mg gallic acid equivalent/g extract), showed the highest reducing capacity (613.27 and 364.10 mg Trolox equivalent/g extract, for cupric reducing antioxidant capacity and ferric reducing antioxidant power, respectively), radical scavenging potential (469.82 mg Trolox equivalent/g extract, against 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)), metal chelating ability (52.39 mg ethylenediaminetetraacetic acid equivalent/g extract) and total antioxidant capacity (3.15 mmol Trolox equivalent/g extract). Liquid chromatography-electrospray ionization-quadrupole time-of-flight-mass spectrometry (LC-ESI-QTOF-MS/MS) alloved to tentatively identify a total of 56 compounds in the extracts, including ellagitannins, gallic acid and galloyl derivatives amongst others. The ethyl acetate extracts substantially depressed cholinesterase enzymes (4.49 and 12.26 mg galantamine equivalent/g extract against AChE and BChE, respectively) and α-amylase enzyme (1.04 mmol acarbose equivalent/g extract). On the other hand, the methanolic extract inhibited tyrosinase (121.42 mg kojic acid equivalent/g extract) and α-glucosidase (2.39 mmol acarbose equivalent/g extract) activities. The highest selectivity towards all cancer cell lines (SI 4.5–10.8) was observed with aqueous extract with the FaDu cells being the most sensitive (CC50 40.22 µg/mL). It can be concluded that the presence of certain bioactive antiviral molecules may be related to the high anti HSV-1 activity of the methanolic extract. This work has generated vital scientific data on this medicinal plant, which is a prospective candidate for the creation of innovative phyto-pharmaceuticals

Qualitative Fingerprint Analysis and Multidirectional Assessment of Different Crude Extracts and Essential Oil from Wild Artemisia santonicum L.

Artemisia species are used as folk medicines in several countries. This work was aimed to shed more light on the effect of methanol, water, ethyl acetate extracts, and essential oil (EO) of A. santonicum on selected enzymes (cholinesterase, tyrosinase α-amylase, and α-glucosidase) as well of their antioxidant and pharmacological effects. The chemical profile of the essential oil was determined using gas chromatography coupled to mass spectrometry (GC-MS) analysis, while the extracts were chemically characterized by high performance liquid chromatography coupled to mass spectrometry (HPLC-MS). Forty-nine constituents were identified and camphor (36.6%), 1,8-cineole (10.2%), α-thujone (10.1%), borneol (4.5%), and β-thujone (3.6%) were the major components. Overall, 45, 74, and 67 components were identified from the ethyl acetate, methanol, and water extracts, respectively. The EO and extracts showed significant antioxidant properties, in a cell-free model; particularly, methanol and water extracts revealed promising sources of antioxidant compounds. Additionally, we evaluated protective effects of EO and extracts in isolated rat colon tissue challenged with lipopolysaccharide (LPS), as an ex vivo model of colon inflammation, and human colon cancer HCT116 cell line. Particularly, we observed that, among all tested samples, A. santonicum ethyl acetate displayed the best pharmacological profile, being able to blunt LPS-induced levels of all tested biomarkers of inflammation and oxidative stress, including colon nitrites, lactate dehydrogenase, prostaglandin E2, and serotonin. Additionally, this extract was also able to reduce HCT116 cell viability, thus suggesting potential antiproliferative effects against colon cancer cells. Based on our results, A. santonicum has great potential for developing novel functional agents including pharmaceuticals, cosmeceuticals, and nutraceuticals

Phytochemical Analysis, Network Pharmacology and in Silico Investigations on Anacamptis pyramidalis Tuber Extracts

Anacamptis pyramidalis (L.) Rich. forms part of the Orchidaceae family that is highly valued for its horticultural as well as therapeutic benefits. The present study set out to investigate the inhibitory activity of A. pyramidalis tubers against key biological targets for the management of type 2 diabetes, Alzheimer disease, and skin hyperpigmentation. In addition, the antioxidant potential of the extracts was also assessed using multiple methods. The detailed phytochemical profiles of the extracts were determined using high-performance liquid chromatography. Based on qualitative phytochemical fingerprint, a network pharmacology analysis was conducted as well. Parishin was identified from the water extract only, whereas gastrodin and caffeic acid derivatives were present in the methanol extract. The methanol extract exhibited high inhibitory activity against tyrosinase (69.69 mg kojic acid equivalent/g extract), α-amylase (15.76 mg acarbose equivalent/g extract), and α-glucosidase (20.07 mg acarbose equivalent/g extract). Similarly, the methanol extract showed highest antioxidant potential (22.12, 44.23, 45.56, and 29.38 mg Trolox equivalent/g extract, for 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), CUPric Reducing Antioxidant Capacity (CUPRAC), and Ferric Reducing Antioxidant Power (FRAP) assays, respectively). Finally, the results of network pharmacology analysis, besides corroborating traditional uses of plant extracts in the management of cold and flu, confirmed a direct involvement of identified phytochemicals in the observed enzyme inhibitory effects, especially against tyrosinase, α-amylase, and α-glucosidase. Furthermore, based on the results of both colorimetric assays and network pharmacology analysis related to the activity of A. pyramidalis extracts and identified phytocompounds on enzymes involved in type 2 diabetes, a docking study was conducted in order to investigate the putative interactions of oxo-dihydroxy octadecenoic acid trihydroxy octadecenoic acid against aldose reductase, peroxisome proliferator-activated receptor (PPAR)-α, dipeptidyl peptidase (DPP)-IV, and α-glucosidase. Docking analysis suggested the inhibitory activity of these compounds against the aforementioned enzymes, with a better inhibitory profile shown by oxo-dihydroxy octadecenoic acid. Overall, the present findings supported the rationale for the use of A. pyramidalis as source of bioactive metabolites and highlight, today more than ever, for the strong necessity of linkage strategy between wild resource valorization and conservation policy

Chemical Characterization and Bioactive Properties of Different Extracts from Fibigia clypeata, an Unexplored Plant Food

Fibigia clypeata (L.) Medik. is a poorly studied plant species belonging to the Brassicaceae family, and usually used as cress in the salads. The current investigation aimed at assessing the antioxidant potential and inhibitory activity of ethyl acetate, methanol, and aqueous extracts of F. clypeata against key enzymes targeted in the management of type II diabetes (\u3b1-amylase and \u3b1- glucosidase), Alzheimer\u2019s disease (acetylcholinesterase and butyrylcholinesterase), and skin hyperpigmentation (tyrosinase). Cytotoxicity of the extracts was also determined using normal VERO and cancer FaDu and SCC-25 cell lines. Besides, LC-MS was employed to investigate the detailed phytochemical profiles of the extracts. The methanol extract showed potent enzyme inhibitory activity (4.87 mg galantamine equivalent/g, 3.52 mg galantamine equivalent/g, 126.80 mg kojic acid equivalent/g, and 24.68 mg acarbose equivalent/g, for acetylcholinesterase, butyrylcholinesterase, tyrosinase, and \u3b1-glucosidase, respectively) and antioxidant potential (96.52, 109.10, 154.02, and 104.85 mg trolox equivalent/g, for DPPH, ABTS, CUPRAC, and FRAP assays, respectively). Interestingly, caffeic acid-O-hexoside derivative, caffeyl alcohol O-glucopyranoside, and ferulic acid derivative were identified in all extracts. F. clypeata extracts showed no cytotoxicity towards VERO cell line and a weak cytotoxic potential against FaDu and SCC-25 cell lines. Interesting scientific evidence gathered from the present study support further investigation on F. clypeata in the view of designing and developing a novel therapeutic agent for the management of Alzheimer\u2019s disease, type II diabetes, skin hyperpigmentation problems, as well as cancer

Comprehensive Chemical Profiling and Multidirectional Biological Investigation of Two Wild Anthemis Species (Anthemis tinctoria var. Pallida and A. cretica subsp. tenuiloba): Focus on Neuroprotective Effects

Ethyl acetate (EA), methanol (MeOH), and aqueous extracts of aerial parts of Anthemis tinctoria var. pallida (ATP) and A. cretica subsp. tenuiloba (ACT) were investigated for their phenol and flavonoid content, antioxidant, and key enzyme inhibitory potentials. All extracts displayed antiradical effects, with MeOH and aqueous extracts being a superior source of antioxidants. On the other hand, EA and MeOH extracts were potent against AChE and BChE. Enzyme inhibitory effects against tyrosinase and α-glucosidase were observed, as well. We also studied Anthemis extracts in an ex vivo experimental neurotoxicity paradigm. We assayed extract influence on oxidative stress and neurotransmission biomarkers, including lactate dehydrogenase (LDH) and serotonin (5-HT), in isolated rat cortex challenged with K+ 60 mM Krebs-Ringer buffer (excitotoxicity stimulus). An untargeted proteomic analysis was finally performed in order to explore the putative mechanism in the brain. The pharmacological study highlighted the capability of ACT water extract to blunt K+ 60 mM increase in LDH level and 5-HT turnover, and restore physiological activity of specific proteins involved in neuron morphology and neurotransmission, including NEFMs, VAMP-2, and PKCγ, thus further supporting the neuroprotective role of ACT water extract