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Toddalia asiatica (L.) Lam. is extensively used in traditional medicinal systems by various cultures. Despite its frequent use in traditional medicine, there is still a paucity of scientific information on T. asiatica growing on the tropical island of Mauritius. Therefore, the present study was designed to appraise the pharmacological and phytochemical profile of extracts (methanol, ethyl acetate and water) and essential oil obtained from aerial parts of T. asiatica. Biological investigation involved the evaluation of in vitro antioxidant and enzyme inhibitory potentials. The chemical profile of the EO was determined using gas chromatography coupled to mass spectrometry (GC/MS) analysis, while for the extracts, the total phenolic (TPC) and flavonoid content were quantified as well as their individual phenolic compounds by LC/MS/MS. Quinic acid, fumaric acid, chlorogenic acid, quercitrin and isoquercitrin were the main compounds in the extracts. Highest total phenolic (82.5±0.94 mg gallic acid equivalent (GAE/g)) and flavonoid (43.8±0.31 mg rutin equivalent (RE/g)) content were observed for the methanol extract. The GC/MS analysis has shown the presence of 26 compounds with linalool (30.9 %), linalyl acetate (20.9 %) and β-phellandrene (7.9 %) being most abundant components in the EO. The extracts and EO showed notable antioxidant properties, with the methanol extract proved to be superior source of antioxidant compounds. Noteworthy anti-acetylcholinesterase (AChE) and anti-butyrylcholinesterase (BChE) effects were recorded for the tested samples, while only the methanol and ethyl acetate extracts were active against tyrosinase. With respect to antidiabetic effects, the extracts and EO were potent inhibitors of α-glucosidase, while modest activity was recorded against α-amylase. Docking results showed that linalyl acetate has the highest affinity to interact with the active site of BChE with docking score of -6.25 kcal/mol. The findings amassed herein act as a stimulus for further investigations of this plant as a potential source of bioactive compounds which can be exploited as phyto-therapeutics., (© 2021 Wiley-VHCA AG, Zurich, Switzerland.)

Croton hirtus L'Hér methanol extract was studied by NMR and two different LC-DAD-MS n using electrospray (ESI) and atmospheric pressure chemical ionization (APCI) sources to obtain a quali-quantitative fingerprint. Forty different phytochemicals were identified, and twenty of them were quantified, whereas the main constituents were dihydro α ionol- O -[arabinosil(1-6) glucoside] (133 mg/g), dihydro β ionol- O -[arabinosil(1-6) glucoside] (80 mg/g), β-sitosterol (49 mg/g), and isorhamnetin-3- O -rutinoside (26 mg/g). C. hirtus was extracted with different solvents-namely, water, methanol, dichloromethane, and ethyl acetate-and the extracts were assayed using different in vitro tests. The methanolic extracts presented the highest 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid (ABTS), and ferric reducing antioxidant power (FRAP) values. All the tested extracts exhibited inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with a higher activity observed for dichloromethane (AChE: 5.03 and BChE: 16.41 mgGALAE/g), while the methanolic extract showed highest impact against tyrosinase (49.83 mgKAE/g). Taken together, these findings suggest C. hirtus as a novel source of bioactive phytochemicals with potential for commercial development.

The present study outlines the phenolic composition and pharmacological properties of different extracts of Digitalis cariensis Boiss. ex Jaub. & Spach root and aerial parts. The metabolic profiles of the studied extracts were characterized by UHPLC-MS. The in vitro antioxidant and enzyme (acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, α-amylase, and α-glucosidase) inhibitory potential of the extracts were determined. Bioinformatics and docking investigations were also conducted to support the enzyme inhibition test and predict putative targets for potential pharmacological applications. Overall, the methanolic extract followed by the water extract of the D. cariensis root were found to be superior source of antioxidant compounds except for metal chelating ability, in which the water extract of the root (26.34 ± 1.54 mg EDTAE/g) and aerial parts (16.47 ± 0.88 mg EDTAE/g) have showed the highest activity. The tested extracts were potent against AChE (9.11 ± 0.27-9.79 ± 0.28 mg GEs/g extract), α-amylase (0.12 ± 0.01- 0.50 ± 0.01 mmol ACEs/g extract) and α-glucosidase (0.28 ± 0.01-17.29 ± 0.24 mmol ACEs/ g extract). Notable activity against tyrosinase was displayed by the methanolic extracts (Root-MeOH: 123.71 ± 2.70 and aerial parts - MeOH: 137.96 ± 1.07 mg KAE/g extract), while none of the extracts were potent against BChE. According to docking investigations, the observed anti-tyrosinase effect could be related, at least partially, to the presence of luteolin, rosmarinic acid and kaempferol in the extracts. Results amassed herein is the first report on the biological attributes of D. cariensis, which validate the pharmacological uses of this plant., Competing Interests: Declaration of Competing Interest The authors report no declarations of interest., (Copyright © 2020 Elsevier B.V. All rights reserved.)

In this study, we attempted for the first time to determine the phytochemical compositions and biopharmaceutical properties of the methanolic and aqueous extracts of Morinda morindoides fruits and seeds. Antioxidant propensities of the extracts were determined via free radical-scavenging, phosphomolybdenum, metal chelating, and reducing power assays. Inhibitory activities against cholinesterases (acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)), tyrosinase, α-amylase, and α-glucosidase were assessed. Moreover, the total phenolic and flavonoid contents were determined. High Performance Liquid Chromatography coupled to Electrospray Ionization Quadrupole Time-of-Flight Mass Spectrometry (HPLC-ESI-Q-TOF-MS) analysis was performed to establish the chemical profile of the investigated extracts. The tested extracts showed remarkable antioxidant abilities with aqueous fruit extract being most potent in all assays, except for ferrous ion chelating assay. Overall, the methanolic extracts were potent inhibitors of the tested enzymes. In conclusion, M. morindoides may be endorsed as promising sources of bioactive compounds and used for designing functional foods. PRACTICAL APPLICATIONS: In recent years, new compounds from plant sources have attracted great interest to design functional foods. Thus, we aimed to detect biological and chemical properties of Morinda morindoides fruits and seeds, a widely used as food with medicinal properties in Africa. Based on our findings, fruits extracts exhibited stronger activity when compared to seed extracts. Also, chemical identification was performed for each extracts. The presented findings could provide valuable information into the pool of scientific knowledge and may be basis for the design of novel functional applications from M. morindoides., (© 2020 Wiley Periodicals, Inc.)

α-lipoic acid (ALA, thioctic acid) is an organosulfur component produced from plants, animals, and humans. It has various properties, among them great antioxidant potential and is widely used as a racemic drug for diabetic polyneuropathy-associated pain and paresthesia. Naturally, ALA is located in mitochondria, where it is used as a cofactor for pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase complexes. Despite its various potentials, ALA therapeutic efficacy is relatively low due to its pharmacokinetic profile. Data suggests that ALA has a short half-life and bioavailability (about 30%) triggered by its hepatic degradation, reduced solubility as well as instability in the stomach. However, the use of various innovative formulations has greatly improved ALA bioavailability. The R enantiomer of ALA shows better pharmacokinetic parameters, including increased bioavailability as compared to its S enantiomer. Indeed, the use of amphiphilic matrices has capability to improve ALA bioavailability and intestinal absorption. Also, ALA's liquid formulations are associated with greater plasma concentration and bioavailability as compared to its solidified dosage form. Thus, improved formulations can increase both ALA absorption and bioavailability, leading to a raise in therapeutic efficacy. Interestingly, ALA bioavailability will be dependent on age, while no difference has been found for gender. The present review aims to provide an updated on studies from preclinical to clinical trials assessing ALA's usages in diabetic patients with neuropathy, obesity, central nervous system-related diseases and abnormalities in pregnancy.

Solanum erianthum D. Don. and S. torvum Swartz of the family Solanaceae have been extensively used for both food and pharmaceutical purposes. In this study, a metabolomic approach was used to compare the phytochemical composition and biological activity of the different plant parts of both species. The inhibitory activity against important enzymes (i.e., cholinesterases, tyrosinase, α-amylase and α-glucosidase), antimicrobial and antifungal potentials, in vitro antioxidant activity, as well as the phenolic and alkaloid profiles of the fruit, leaf and stem bark extracts of both species were studied. The results showed that the stem barks were characterized by the highest amounts of total phenolics (on average: 12.6 mg/g), whilst the S. erianthum leaves were the best source of total alkaloids (2.1 mg/g). Overall, the stem bark extracts of both species were found to be a good source of antioxidant compounds. All the extracts were effective against acetylcholinesterase and tyrosinase, while only the leaf extracts of both plants were a good source of butyrylcholinesterase inhibitors. The extracts have significant anti-microbial and anti-fungal potentials. A modest anti-diabetic effect was measured for α-amylase and α-glucosidase. Strong correlations (p <0.01) were found between the bioactives and the biological activities. Therefore, this study showed the potential of untargeted metabolomics to investigate the bioactive profile of plant extracts, thus providing discrimination between S. erianthum and S. torvum. [Display omitted] • Solanum erianthum and S. torvum are sources of antioxidants. • The stem barks of both species showed the highest phenolic contents. • S. erianthum leaves were rich in glycoalkaloids. • All the extracts inhibited AChE and tyrosinase enzymes. • Phytochemicals strongly correlated with biological properties. [ABSTRACT FROM AUTHOR]

Achyranthes aspera Linn. (Amaranthaceae), commonly known as the Prickly Chaff flower, is used as herbal medicine in the Ivorian's culture, Africa. Nonetheless, there is currently a paucity of scientific information on A. aspera from the Ivory Coast. Herein, the antioxidant activity of A. aspera extracts (methanol, dichloromethane, ethyl acetate and infusion) as well as the enzymatic inhibitory potentials towards key enzymes in human diseases, namely Alzheimer's disease, (cholinesterases: AchE and BChE), type 2 diabetes (α-glucosidase and α-amylase) and hyperpigmentation (tyrosinase) were assessed. The total phenolic (TPC) and flavonoid (TFC) content was determined using colorimetric methods and the individual compounds were characterized using ultra-high performance liquid chromatography coupled with hybrid quadrupole-Orbitrap high resolution mass spectrometry (UHPLC-HRMS). Furthermore, a network pharmacology analysis was conducted to predict putative targets of identified phenolic compounds. The highest TPC was observed in the infused extract (28.86 ± 0.12 mg GAE/g), while the dichloromethane extract (38.48 ± 1.48 mg RE/g) showed the highest level of TFC. UHPLC-HRMS analysis has revealed an abundance of fatty acids, flavonoids, phenols and acylquinic acids. Among tested extracts, the infused extract displayed the highest free radical quenching, reducing and metal-chelating ability. The extracts (except infusion) were effective as enzyme inhibitors against AChE, while only methanolic and infused extracts showed noteworthy anti-BChE effects. The methanolic extract showed a remarkable antityrosinase effect (56.24 ± 5.05 mg KAE/g), as well. Modest to moderate inhibitory activity was observed against α-amylase (all extracts) and α-glucosidase (only dichloromethane extract). Finally, the network pharmacology analysis suggested the carbonic anhydrase II enzyme as a putative target for explaining, at least in part, the traditional use of A. aspera preparations as diuretic and blood clotting agent. Data amassed herein tend to validate the use of A. aspera in traditional medicine, as well as act as a stepping stone for further studies in the quest for novel phytopharmaceuticals. In this context, it is desirable that this study will contribute to the validation of the traditional uses of this plant in the African herbal medicine, and to the valorization of the whole chain production of A. aspera, as a local and sustainable botanical resource. [ABSTRACT FROM AUTHOR]

Like other members of the Colchicum genus, C. szovitsii subsp. szovitsii is also of medicinal importance in Turkish traditional medicine. However, its biological properties have not been fully investigated. Herein, we focused on the evaluation of the in vitro antioxidant and enzyme inhibitory effects of flower, root and leaf extracts, obtained using different extraction methods. In addition, a comprehensive (poly)-phenolic and alkaloid profiling of the different extracts was undertaken. In this regard, ultra-high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC-QTOF-MS) allowed us to putatively annotate 195 polyphenols and 87 alkaloids. The most abundant polyphenols were flavonoids (83 compounds), whilst colchicine and 2-demethylcolchicine were some of the most widespread alkaloids in each extract analyzed. However, our findings showed that C. szovitsii leaf extracts were a superior source of both total polyphenols and total alkaloids (being, on average 24.00 and 2.50 mg/g, respectively). Overall, methanolic leaf extracts showed the highest (p < 0.05) ferric reducing antioxidant power (FRAP) reducing power (on average 109.52 mgTE/g) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging (on average 90.98 mgTE/g). Interestingly, each C. szovitsii methanolic extract was more active than the water extracts when considering enzymatic inhibition such as against tyrosinase, glucosidase, and acetylcholinesterase (AChE). Strong correlations (p < 0.01) were also observed between polyphenols/alkaloids and the biological activities determined. Multivariate statistics based on supervised orthogonal projections to latent structures discriminant analysis (OPLS-DA) allowed for the detection of those compounds most affected by the different extraction methods. Therefore, this is the first detailed evidence showing that C. szovitsii subsp. szovitsii might provide beneficial effects against oxidative stress and the associated chronic diseases. Nevertheless, the detailed mechanisms of action need to be further investigated. [ABSTRACT FROM AUTHOR]

[Display omitted] • Several biological activities and chemical constituents of Sida acuta were investigated. • Chemical profiles were detected by UHPLC-HRMS analysis. • Phenolic acids and flavonoid were main groups in the chemical profiles. • Methanol extract exhibited the best antioxidant properties and cytotoxic effects. • S. acuta might be novel sources of biologically-active compounds in the pharmaceutical and food industries. The chemical components, in vitro antioxidant capacities and enzyme inhibitory effects of dichloromethane (DCM), ethyl acetate (EA), methanol (MeOH) and water extracts of the medicinal plant, Sida acuta Burm. f. were evaluated. The individual phenolic components were assessed via ultra-high-performance liquid chromatography-high-resolution mass spectrometry (UHPLC-HRMS). In terms of chemical composition, phenolics (hydroxybenzoic and hydroxycinnamic acids) and flavonoids were identified as main groups. The antioxidant capacities were evaluated using a panoply of cell-free bioassays and the enzymatic inhibitory potentials against key enzymes involved in human diseases were also determined. The water extract exhibited the strongest scavenging abilities on DPPH (IC 50 : 1.05 mg/mL) and ABTS (IC 50: 1.02 mg /mL). The best cholinesterase inhibitory abilities were observed with the methanol extract (IC 50 : 0.51 and 0.52 mg/mL for AChE and BChE, respectively), while DCM exhibited the strongest α-amylase (IC 50 : 1.21 mg/mL) and α-glucosidase (IC 50 : 0.62 mg/mL) inhibitory effects. The anti-cancer effects of methanol and water extracts were tested on human breast cancer cells, MDA-MB-231, and the methanol extract showed the best anti-cancer effect with an IC 50 value of 102.4 μg/mL. In conclusion, the experimental data have demonstrated promising pharmacological activities of S. acuta extracts obtained using different solvents, thereby providing a scientific basis for the validation of the traditional medicinal uses of this plant. [ABSTRACT FROM AUTHOR]

Natural products are gaining much momentum worldwide because they have a broad spectrum of biological effects and present excellent opportunities for bioproducts development. With this fact, this study has been designed to investigate for the first time the effects of the ethyl acetate (EA), methanolic (MeOH), and water (W) extracts of Lotus aegaeus (La) and Iberis sempervirens (Is) on key enzymes as well as to quantify antioxidant capacities. The total phenolic and flavonoid content were determined using colorimetric methods and the individual phenolic compounds were assessed by LC–MS/MS analysis. Quercetin hexoside was the dominant compound in L. aegaeus , particularly in methanol extract, while the ethyl acetate and methanol extracts of I. sempervirens were characterized by the presence scopoletin and hinic acid. The antioxidant abilities of the investigated extracts were tested using different assays including free radical scavenging, reducing power, phosphomolybdenum, and metal chelating. All the extracts showed strong antioxidant abilities. For both species, the ethyl acetate extracts were more potent against cholinesterases and α-amylase, while the methanol extracts were most active against α-glucosidase. Only the water extract, followed by methanol of I. sempervirens exhibited notable inhibitory activity against tyrosinase. In addition, the dominant compounds were docked against tyrosinase and α-glucosidase to investigate their predicted binding affinity and interactions with the active site. In conclusion, L. aegaeus and I. sempervirens showed potent biological attributes, which advocates for further studies to explore their potential use as phytopharmaceuticals. [ABSTRACT FROM AUTHOR]

• Different methods and solvent extracts from Lophira lanceolata were investigated. • Antioxidant, cytotoxic and enzyme inhibitory effects were evaluated. • Lanceolatins and lophirones were identified in the extracts. • Stem bark extracts exhibited stronger biological propensities than leaf extracts. • The results might be valuable for designing novel bioproducts. Lophira lanceolata Tiegh. ex Keay, a native tropical plant to west and central Africa, is a multifunctional plant used as timber and also exploited in traditional medicine in Africa. The present study present the pharmacological properties of Lophira lanceolata leaf and stem bark extracts prepared from different extraction procedures (infusion, homogenizer‐assisted extraction, maceration, soxhlet). The detailed phytochemical composition, in vitro antioxidant and antiproliferative assays, as well as the key enzyme (cholinesterases, tyrosinase, α‐amylase and α‐glucosidase) inhibitory potentials of the extracts were evaluated. Chemical profiling confirmed the presence of lanceolatins and lophirones in all analyzed plant parts. Higher levels of total phenolics (156.42 mg gallic acid equivalent (GAE)/g for maceration-water), phenolic acids (165.84 mg caffeic acid equivalent (CE)/g for maceration-water) and flavanols (101.51 mg catechin equivalent (CAE)/g for soxhlet-methanol (MeOH)) were observed in the stem bark extracts. Antioxidant assays showed remarkable free radical scavenging and reducing power activities for all extracts, among which stem bark showed the highest potential. Stem bark extracts (IC 50 values: 57.55–93.10 μg/ml for colorectal adenocarcinoma (HT29) and 78.18–89.58 μg/ml for metastatic breast cancer cell line (MCF7)) also showed better antiproliferative effect than leaf (424.14–790.27 μg/ml for HT29 and 374.46–943.09 μg/ml for MCF7) on carcinoma cells while they induced proliferation in normal human cell lines (normal skin fibroblasts (HFF)). In the enzyme inhibitory assays, the methanol extracts of both plant parts were confirmed as effective against AChE, BChE (only stem barks extracts) and α-glucosidase enzymes. Regarding anti-tyrosinase effects, the methanol leaf extracts (122.21–131.17 mg kojic acid equivalent (KAE)/g) and all stem bark extracts (94.58–153.21 mg KAE/g) exhibited inhibitory effects. Findings amassed herein tend to validate the traditional uses of L. lanceolata and advocate for the development of phyto-medicaments based on its extracts. [ABSTRACT FROM AUTHOR]

• Biological activities and phytochemical profiles of six Consolida species were inspected. • Consolida regalis and C. stenocarpa exhibited the highest antiradical abilities. • Consolida hellospontica and C. glandulosa displayed the strongest cholinesterases inhibitory. • Flavonoids, phenolic acids, and alkaloids were the main groups of phytochemicals. • This study provided a scientific basis for industrial exploitation from the members of the genus Consolida. The genus Consolida is one of the most important within the Ranunculaceae family and several members of this genus contain important biologically active compounds, such as phenolics and alkaloids. The present study attempts for the first time to assess the biological properties and phytochemical constituents of six Consolida species (C. glandulosa (Boiss. & A. Huet) Bornm, C. hellospontica (Boiss.) Chater, C. raveyi (Boiss.) Schrödinger, C. regalis (Boiss.) Schrödinger, C. staminosa P.H. Davis & Sorger and C. stenocarpa (P.H. Davis & M. Hossain) P.H. Davis) growing in Turkey. A comprehensive phytochemical profiling of the different species was achieved by using an ultra-high-performance liquid chromatography-quadrupole time-of-flight (UHPLC-QTOF) mass spectrometry, targeting polyphenols and diterpene alkaloids. Also, the in vitro antioxidant assays (2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS), ferric reducing antioxidant power (FRAP), cupric reducing antioxidant capacity (CUPRAC), metal chelating and phosphomolybdenum) and enzyme inhibition (cholinesterases, tyrosinase, α-amylase, and α-glucosidase) potentials of the different Consolida methanolic extracts were evaluated. The UHPLC-QTOF profiling revealed 492 compounds, being 236 flavonoids, 93 phenolic acids, 78 tyrosol derivatives, 49 diterpene alkaloids, 29 lignans, and 7 stilbenes. The cumulative phenolic content ranged from 17.65 mg Eq./g for C. staminosa up to 43.04 mg Eq./g for C. glandulosa , whilst the total diterpene alkaloids content was exclusively found in C. glandulosa extracts (3.53 mg Eq./g). Consolida regalis (58. 61 mg trolox equivalent (TE)/g for DPPH and 65.38 mg TE/g for ABTS) and C. stenocarpa (46.81 mg TE/g for DPPH and 78.12 mg TE/g for ABTS) exhibited the highest anti-radical abilities, while the best reducing power values were recorded for C. glandulosa (129.46 mg TE/g for CUPRAC and 77.01 mg TE/g for FRAP) and C. raveyi (124.56 mg TE/g for CUPRAC and 78.36 mg TE/g for FRAP). Also, following the cholinesterases inhibition assays, C. hellospontica and C. glandulosa exhibited the highest inhibitory effects. Regarding tyrosinase inhibitory effects, C. raveyi showed the highest value, being 126.60 mg kojic acid equivalent (KAE)/g, followed by C. glandulosa (125.82 mg KAE/g) and C. stenocarpa (123.09 mg KAE/g). Besides, Consolida staminosa showed potential inhibition against α-amylase, but low glucosidase inhibitory properties. Therefore, the present findings could provide a starting point for further investigations to promote the industrial exploitation of these species with the aim of designing novel phyto-pharmaceuticals. [ABSTRACT FROM AUTHOR]