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The aim of the present study was to quantify selected phenolic compounds, determine antioxidant activity and enzyme inhibitory effects of the aerial parts of Alkanna trichophylla Hub.-Mor. (A. trichophylla) and Convolvulus galaticus Rost.ex Choisy (C. galaticus) extracts prepared by homogenizer-assisted extraction (HAE), maceration (MAC) and infusion techniques. This is the first time such study has been designed to validate the phytochemical composition and bioactivity of these plants. Multivariate analysis was conducted on collected data. Rutin and caffeoylquinic acid derivatives were the most significant compounds in A. trichophylla and C. galaticus, respectively. The highest antioxidant activity of A. trichophylla was mostly exhibited by HAE/methanolic extracts as determined by DPPH, ABTS, FRAP (51.39, 112.70 and 145.73 mg TE/g, respectively) and phosphomolybdenum (2.05 mmol TE/g) assays. However, significant antioxidant activities varied within the extracts of C. galaticus. HAE/methanolic extract of A. trichophylla significantly depressed AChE (2.70 mg GALAE/g), BChE (5.53 mg GALAE/g) and tyrosinase (26.34 mg KAE/g) activities and that of C. galaticus inhibited AChE (2.04 mg GALAE/g), tyrosinase (31.25 mg KAE/g) and α-amylase (0.53 mmol ACAE/g) activities significantly. We concluded that HAE was the most efficient extraction technique as high yield of compounds and promising bioactivities were recorded from extracts prepared. Multivariate analysis showed that types of solvents influenced recovery of compounds and biological activities. This research study can be used as one methodological starting point for further investigation on these plants as all results are clearly promising and open the door to further research challenges such as cytotoxicity evaluation, molecular docking analysis, and more screening of pharmacological actions.

The recent emergence of Zika virus (ZIKV) in Brazil and the increasing resistance developed by pathogenic bacteria to nearly all existing antibiotics should be taken as a wakeup call for the international authority as this represents a risk for global public health. The lack of antiviral drugs and effective antibiotics on the market triggers the need to search for safe therapeutics from medicinal plants to fight viral and microbial infections. In the present study, we investigated whether a mangrove plant, Bruguiera gymnorhiza (L.) Lam. (B. gymnorhiza) collected in Mauritius, possesses antimicrobial and antibiotic potentiating abilities and exerts anti-ZIKV activity at non-cytotoxic doses. Microorganisms Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Klebsiella pneumoniae ATCC 70603, methicillin-resistant Staphylococcus aureus ATCC 43300 (MRSA), Salmonella enteritidis ATCC 13076, Sarcina lutea ATCC 9341, Proteus mirabilis ATCC 25933, Bacillus cereus ATCC 11778 and Candida albicans ATCC 26555 were used to evaluate the antimicrobial properties. Ciprofloxacin, chloramphenicol and streptomycin antibiotics were used for assessing antibiotic potentiating activity. ZIKVMC-MR766NIID (ZIKVGFP) was used for assessing anti-ZIKV activity. In silico docking (Autodock 4) and ADME (SwissADME) analyses were performed on collected data. Antimicrobial results revealed that Bruguiera twig ethyl acetate (BTE) was the most potent extract inhibiting the growth of all nine microbes tested, with minimum inhibitory concentrations ranging from 0.19–0.39 mg/mL. BTE showed partial synergy effects against MRSA and Pseudomonas aeruginosa when applied in combination with streptomycin and ciprofloxacin, respectively. By using a recombinant ZIKV-expressing reporter GFP protein, we identified both Bruguiera root aqueous and Bruguiera fruit aqueous extracts as potent inhibitors of ZIKV infection in human epithelial A549 cells. The mechanisms by which such extracts prevented ZIKV infection are linked to the inability of the virus to bind to the host cell surface. In silico docking showed that ZIKV E protein, which is involved in cell receptor binding, could be a target for cryptochlorogenic acid, a chemical compound identified in B. gymnorhiza. From ADME results, cryptochlorogenic acid is predicted to be not orally bioavailable because it is too polar. Scientific data collected in this present work can open a new avenue for the development of potential inhibitors from B. gymnorhiza to fight ZIKV and microbial infections in the future.

Syringodium isoetifolium (Asch.) Dandy (Family: Cymodoceaceae) is a seagrass growing in the oceans across the globe except in cold waters. This study investigated into the polyphenolic content, antioxidant [2,2-diphenyl-1-picrylhydrazyl(DPPH), 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS), cupric reducing antioxidant capacity (CUPRAC), ferric reducing antioxidant power (FRAP), metal chelating, phosphomolybdenum)]and enzymatic properties [α-amylase, α-glucosidase, tyrosinase, acetylcholinesterase (AChE), butylcholinesterase (BChE)] of S. isoetifolium. Detailed phytochemical profiling was also conducted using Ultra Performance High-Pressure Liquid Chromatography (UHPLC) technique. The methanolic extract was found to possess greater amount of phenolic than flavonoid compounds. Antioxidant results showed that the extract was a better ABTS radical scavenger (9.56 ± 0.40 mg TE/g) compared to DPPH (5.39 ± 0.09 mg TE/g and exhibited good reducing potential with CUPRAC assay (18.66 ± 0.46 mg TE/g). In terms of enzymatic inhibition, strong activities were noted against tyrosinase (25.92 ± 0.11 mg KAE/g) in contrast to α-amylase, α-glucosidase and cholinesterase. Phytochemical data revealed the presence of 14 compounds with chicoric acid and caftaric acid among them. Docking the identified compounds, namely, caftaric acid, loliolide and Iso-loliolide at the active site of the tyrosinase enzyme has elucidated the binding affinity of these inhibitors and their interactions with the active site. Based on our findings, S. isoetifolium may be considered as a good natural antioxidant and clinical enzyme inhibitors that can be exploited in pharmaceutical/or cosmeceutical industries.

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.

Members from the Verbascum genus are well appraised for their traditional uses against a variety of ailments including anti-inflammatory related disorders. This study thus attempts at validating the biological properties of two underexplored Verbascum members namely Verbascum euphraticum Benth. (V. euphraticum) and Verbascum oocarpum Murb. (V. oocarpum) in terms of their antioxidant and enzymatic inhibitory activities. Concentration of specific bioactive compounds was also established and molecular dynamic analysis were conducted on amassed data. Results showed that total phenolic and total flavonoid contents were higher for the methanolic extract of V. oocarpum compared to the methanolic extract of V. euphraticum. Phytochemical quantification revealed that the extraction solvents influenced the phytochemical composition of the extracts. Derivatives of phenolic acids such as 3-caffeoylquinic acid and 3,5-dicaffeoylquinic acid together with some phenolic acids i.e., gallic, vanillic, caffeic, syringic, p-coumaric and ferulic acid, have been detected in the extracts of both Verbascum species. Methanolic extracts of V. euphraticum and V. oocarpum yielded the highest total content of monitored compounds resulting in 162.758 and 3716.861 μg/g of dried weight extract, respectively. The methanolic extracts of both plants showed highest antioxidant potential while the ethyl acetate and hexane extracts were potent inhibitors of cholinesterase, α-amylase and α-glucosidase. Molecular dynamic results indicated that vanillic acid is able to make strong interactions with copper ions of tyrosinase, resulting into an effective anti-tyrosinase activity. In light of the above, both Verbascum species could be considered for future phytopharmaceutical development.

Cajanus cajan. (L.) Millsp. (C. cajan) (Family: Fabaceae) also known as pigeon pea, is a famous food and cover/forage crop bearing a high amount of key amino acids (methionine, lysine and tryptophan). This study investigated into the total phenolic (TPC), flavonoid content (TFC), antioxidant ]2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2 -azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP), cupric reducing antioxidant capacity, total antioxidant capacity (TAC) (phosphomolybdenum) and metal chelating] activities and enzyme [alpha-amylase, alpha-glucosidase, tyrosinase, acetyl-(AChE), butyry1-(BChE) cholinesterase] inhibitory effects of four extracts (methanol, hexane, ethyl acetate, aqueous) prepared from C. cajan stem bark. Direct identification of antioxidants was also conducted using the high performance liquid chromatography-ferric reducing antioxidant power (HPLC-FRAP) system. The highest TPC and TFC were recorded with the methanolic (23.22 +/- 0.17 mg GAE/g) and ethyl acetate extracts (19.43 +/- 0.24 mg RE/g), respectively. The methanolic extract exhibited important antioxidant activity with DPPH (38.41 +/- 0.05 mg Trolox equivalent (TE)/g), ABTS (70.49 +/- 3.62 mg TE/g), CUPRAC (81.86 +/- 2.40 mg TE/g), FRAP (42.96 +/- 0.59 mg TE/g) and metal chelating (17.00 +/- 1.26 mg ethylenediaminetetraacetic acid equivalent/g). p-coumaric and caffeic acid were the predominant antioxidants in the samples. Results from enzymatic assays showed the potential abilities of hexane extract in inhibiting the AChE, BChE, alpha-amylase and alpha-glucosidase enzymes. From the results obtained in this study, it can be concluded that C. cajan can be considered as a promising source of antioxidants and key enzyme inhibitors that can be exploited for future bioproduct development.

Olive and olive oil (OO) are a fundamental component of the Mediterranean culture and cuisine. Diverse traditional medicines include olive and its oil as a vital ingredient for the formulation of concoctions useful against urinary tract infection, diabetes, high blood pressure, hair loss, diarrhea, gout, rheumatism, mouth, and as a skin cleanser in various parts of the world. The use of OO as a healthy culinary ingredient has remained in vogue compared to other cooking oils given its promising benefits on the cardiovascular system among other health benefits. Indeed, results derived from in vitro, in vivo, and clinical studies have validated the potential benefits of olive and OO for the cardiovascular system. In vitro, both the methanolic and the ethanolic leaf extract downregulate hydroxynonenal-induced p-MAPKAPK-2 and p-c-Jun. Olive and OO are rich in bioactive metabolites such as oleuropein (OLE), hydroxytyrosol, and polyphenols. Notably, OLE inhibits the excess production of reactive oxygen species and stabilized mitochondrial membrane potential following simulated ischemia-/reperfusion-induced cardiomyocyte injury. In vivo, OLE reduced the plasma lipid peroxidation products and protein carbonyl levels in rabbits alongside providing strong antioxidant protection. Interestingly, it can also reduce doxorubicin-related cardiotoxicity. Both hydroxytyrosol and OLE significantly reversed chronic inflammation and oxidative stress consequently reducing cardiovascular, hepatic, and metabolic symptoms. Polyphenols also reduce chronic inflammation and oxidative stress. In furtherance, extra-virgin oil has demonstrated both cholesterol and blood pressure lowering properties while clinically decreasing cardiovascular disease risk by at least 35%. Virgin OO provides benefits among patients with stable coronary heart disease and can be employed as a supplement in patients with this disease.

In the present study, the methanolic, hydro-methanolic, dichloromethane, hexane and aqueous extracts of

Breynia retusa (Dennst.) Alston (also known as Cup Saucer plant) is a food plant with wide applications in traditional medicine, particularly in Ayurveda. Extracts obtained with four solvents (dichloromethane, methanol, ethyl acetate and water), from three plant parts, (fruit, leaf and bark) were obtained. Extracts were tested for total phenolic, flavonoid content and antioxidant activities using a battery of assays including 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP), cupric reducing antioxidant capacity (CUPRAC), total antioxidant capacity (TAC) (phosphomolybdenum) and metal chelating. Enzyme inhibitory effects were investigated using acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, α-amylase and α-glucosidase as target enzymes. Results showed that the methanolic bark extract exhibited significant radical scavenging activity (DPPH: 202.09 ± 0.15; ABTS: 490.12 ± 0.18 mg Trolox equivalent (TE)/g), reducing potential (FRAP: 325.86 ± 4.36: CUPRAC: 661.82 ± 0.40 mg TE/g) and possessed the highest TAC (3.33 ± 0.13 mmol TE/g). The methanolic extracts were subjected to LC-DAD-MSn and NMR analysis. A two-column LC method was developed to separate constituents, allowing to identify and quantify forty-four and fifteen constituents in bark and fruits, respectively. Main compound in bark was epicatechin-3-O-sulphate and isolation of compound was performed to confirm its identity. Bark extract contained catechins, procyanidins, gallic acid derivatives and the sulfur containing spiroketal named breynins. Aerial parts mostly contained flavonoid glycosides. Considering the bioassays, the methanolic bark extract resulted a potent tyrosinase (152.79 ± 0.27 mg kojic acid equivalent/g), α-amylase (0.99 ± 0.01 mmol acarbose equivalent ACAE/g) and α-glucosidase (2.16 ± 0.01 mmol ACAE/g) inhibitor. In conclusion, methanol is able to extract the efficiently the phytoconstituents of B. retusa and the bark is the most valuable source of compounds.

Mitracarpus hirtus (L.) DC. (Family: Rubiaceae) is a tropical annual herb commonly found in America and Mexico. In the present study, the methanol, ethyl acetate, dichloromethane and aqueous extracts of the plant were tested for total phenolic (TPC) and flavonoid content (TFC) and antioxidant activities were evaluated using a battery of assays including 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP), cupric reducing antioxidant capacity, total antioxidant capacity (TAC) (phosphomolybdenum) and metal chelating. Enzyme inhibitory effects were investigated using acetylcholinesterase (AChE), tyrosinase, α-amylase and α-glucosidase as target enzymes. The phytochemical profile was obtained using liquid chromatography-diode array detection-electrospray ionization-mass spectrometry (LC-DAD-ESI-MSn), liquid chromatography-atmospheric pressure chemical ionization-mass spectrometry (LC-APCI-MSn) and nuclear magnetic resonance (NMR) experiments. Results showed that the dichloromethane and ethyl acetate extracts yielded the highest TPC (29.10 ± 0.07 mg gallic acid equivalent/g) and TFC (38.14 ± 0.91 mg rutin equivalent/g), respectively. Aqueous extract showed weak activity against tested enzymes but demonstrated the strongest ABTS scavenging activity (59.39 ± 1.19 mg trolox equivalent/g) and is the strongest Fe3+ reducer (59.42 ± 0.59 mg trolox equivalent/g). Phytochemical analysis revealed the presence of phenolics, pyrrolizidine alkaloids and triterpene acid. This is the first report gathering scientific data on antioxidant, enzyme inhibitory activities and phytochemical composition of M. hirtus and the obtained results can be used as starting point for further investigation on this traditional medicinal herb.

This research study presents information for the first time on the nutritionally relevant lipophilic compounds obtained from Ecklonia radiata, a poorly studied brown kelp. The major lipophilic compounds were analyzed utilizing liquid chromatography (LC)-tandem mass spectrometry (MS/MS) and gas chromatography (GC)-mass spectrometry (MS). The LC-MS/MS results revealed the presence of eight major lipophilic compounds, including sterols, carotenoids, vitamin E, and phylloquinone (vitamin K1). Quantitative analysis showed that fucosterol was the most predominant phytosterol in the fronds and stipes of E. radiata. The carotenoids (all-E)-fucoxanthin and (all-E)-β-carotene were present in higher yield. In terms of vitamin E, α-tocopherol was identified as the main tocol. The coenzyme, phylloquinone, important for protein synthesis, was also identified in E. radiata. GC-MS identified 13 fatty acids with palmitic (C16:0) and oleic acid (C18:1n9c) present in the highest quantities. To our knowledge, this is the first report on E. radiata, and the valuable data presented herein can be used as a baseline for developing novel nutraceuticals.

Members of the genus Euphorbia have attracted much interest as potential sources of bioactive compounds. In this study, the ethyl acetate, methanolic and aqueous extracts of aerial parts of three Euphorbia species namely Euphorbia hirta L., Euphorbia heterophylla L. and Euphorbia convolvuloides Hochst. ex Benth. were screened for their antioxidant [2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP), cupric antioxidant reducing capacity (CUPRAC), metal chelating, total antioxidant capacity (phosphomolybdenum)], and enzymatic properties [α-amylase, α-glucosidase, tyrosinase, acetyl- (AChE), butyryl-cholinesterase (BChE)]. Total phenolic (TPC), total flavonoid content (TFC) and phytochemical profile were established via LC-DAD-MS

Bruguiera gymnorhiza (L.) Lam. is claimed to effectively manage a number of ailments including diabetes and associated complications. Nonetheless, no attempt has been made to delineate its pharmacological propensities and phytochemical profile. This study was designed to appraise the antioxidant and enzymatic inhibitory properties relevant to the management of diabetes mellitus, obesity, and neurodegenerative and skin disorders. A combination of colorimetric assays and ultra-high-performance liquid chromatography/electrospray ionization tandem mass spectrometry (UHPLC-ESI-MS/MS) were applied for the phytochemical screening of leaf, root, twig, and fruit extracts (methanol and ethyl acetate). In vitro antioxidant evaluations were via radical scavenging abilities (DPPH, ABTS), reducing potential (FRAP, CUPRAC), chelating power, and total antioxidant capacity (phosphomolybdenum). Seven key metabolic enzymes (&alpha, amylase, &alpha, glucosidase, tyrosinase, elastase, lipase, AChE, and BChE) were targeted to determine the inhibitory effects. Multivariate and in silico docking analysis were performed on collected data. Methanolic fruit extract yielded the highest total phenolic, tannin, and triterpenoid contents (174.18 &plusmn, 4.27 mg GAE/g, 176.24 &plusmn, 3.10 mg CE/g, 63.11 &plusmn, 3.27 mg OAE/g, respectively), significantly depressed tyrosinase, elastase, and &alpha, amylase activities (155.35 &plusmn, 0.29 mg KAE/g, 4.56 &plusmn, 0.10 mg CAE/g, 1.00 &plusmn, 0.05 mmol ACAE/g, accordingly), and harboured the most potent antioxidant capacities with DPPH, CUPRAC, FRAP (492.62 &plusmn, 5.31, 961.46 &plusmn, 11.18, 552.49 &plusmn, 8.71 mg TE/g, respectively), and phosphomolybdenum (4.17 &plusmn, 0.31 mmol TE/g) assays. Multivariate analysis suggested that the type of solvents used influenced the biological activities more compared to plant parts. Docking analysis showed that azelaic acid binds with tyrosinase by Van der Waals and conventional hydrogen bonds. We anticipate that the present study may establish baseline data on this halophyte that could open new avenues for the development of biomedicine.

Mangrove forests exemplify a multifaceted ecosystem since they do not only play a crucial ecological role but also possess medicinal properties. Methanolic, ethyl acetate and aqueous leaf and bark extracts were prepared using homogenizer-assisted extraction (HAE), infusion and maceration (with and without stirring). The different extracts were screened for phytochemical profiling and antioxidant capacities in terms of radical scavenging (DPPH, ABTS), reducing potential (CUPRAC, FRAP), total antioxidant capacity and chelating power. Additionally, R. racemosa was evaluated for its anti-diabetic (&alpha, amylase, &alpha, glucosidase), anti-tyrosinase and anti-cholinesterase (AChE, BChE) activities. Additionally, antimycotic and antibacterial effects were investigated against Eescherichia coli, Pseudomonas aeruginosa, Salmonella typhimurium, Listeria monocytogenes, Enterobacter cloacae, Bacillus cereus, Micrococcus luteus, Staphylococcus aureus, Aspergillus fumigatus, Aspergillus niger, Trichoderma viride, Penicillium funiculosum, Penicillium ludwigii and Penicillium verrucosum. Finally, based on phytochemical fingerprint, in silico studies, including bioinformatics, network pharmacology and docking approaches were conducted to predict the putative targets, namely tyrosinase, lanosterol-14-&alpha, demethylase and E. coli DNA gyrase, underlying the observed bio-pharmacological and microbiological effects. The methanolic leave and bark extracts (prepared by both HAE and maceration) abounded with phenolics, flavonoids, phenolic acids and flavonols. Results displayed that both methanolic leaf and bark extracts (prepared by HAE) exhibited the highest radical scavenging, reducing potential and total antioxidant capacity. Furthermore, our findings showed that the highest enzymatic inhibitory activity recorded was with the tyrosinase enzyme. In this context, bioinformatics analysis predicted putative interactions between tyrosinase and multiple secondary metabolites including apigenin, luteolin, vitexin, isovitexin, procyanidin B, quercetin and methoxy-trihydroxyflavone. The same compounds were also docked against lanosterol-14&alpha, demethylase and E. Coli DNA gyrase, yielding affinities in the submicromolar&ndash, micromolar range that further support the observed anti-microbial effects exerted by the extracts. In conclusion, extracts of R. racemosa may be considered as novel sources of phytoanti-oxidants and enzyme inhibitors that can be exploited as future first-line pharmacophores.

Vitellaria paradoxa C. F. Gaertn. (Family: Sapotaceae), is a well-known medicinal plant but with no consolidated published literature to substantiate its traditional uses. This research aimed to investigate the pharmaceutical potential of V. paradoxa extracts and attempts to compare the biological profiles and phytochemical analysis prepared by different extraction protocols. For preparation of the V. paradoxa leaves and stem bark extracts, four extraction techniques and two different solvent types were employed. First analysis included identification of bioactive compounds by use of high-resolution Quadrupole Time-Of-Flight instrument. Antioxidant capacities were evaluated as radical scavenging potential, reducing potential, total antioxidant capacity (phosphomolybdenum) and metal chelating power. The last evaluation step included analysis of the inhibitory properties of V. paradoxa extracts against key enzymes related to main health problems. Our findings revealed key details on phytochemical profiling of the V. paradoxa plant, whereas 17 phytochemicals were identified in leaves and 14 in stem bark. Antioxidant assays showed that extracts obtained by maceration extraction process exhibit potent antioxidant capacities. Extracts prepared by HAE generally showed the highest enzymatic activities. The presented findings confirmed the need for further studies geared towards discovery and development of novel bioactive components from V. paradoxa leaves and stem bark.

The genus Scorzonera contains important plants as traditional drugs and foods. In this sense, the aim of the present study was to determine the chemical composition, antioxidant activity and enzyme inhibitory effects of the root and aerial part of Scorzonera hispanica L. (S. hispanica) extracts. The antioxidant activities were evaluated using ferric reducing antioxidant power (FRAP), cupric reducing antioxidant capacity (CUPRAC), 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS), metal chelating and phosphomolybdenum assays and the enzyme inhibitory properties were assessed against acetyl- (AChE) and butyryl-cholinesterase (BChE), tyrosinase, α-amylase and α-glucosidase. The results showed that the methanolic and ethyl acetate extracts possessed the highest phenol and flavonoid contents. The methanolic aerial part extract represented the highest antioxidant properties (FRAP: 58.41±1.55; CUPRAC: 126.18±0.94; DPPH: 47.92±0.07; ABTS: 71.69±0.03 mg Trolox equivalent (TE)/g) compared to the root extracts. The root extract significantly depressed AChE (2.64±0.02 mg galantamine equivalent (GALAE)/g), BChE (5.36±0.45 mg galantamine equivalent (GALAE)/g), tyrosinase (60.36±0.23 mg kojic acid equivalent (KAE)/g), α-amylase (0.61±0.01 mmol acarbose equivalent (ACAE)/g) and α-glucosidase (0.82±0.01 mmol acarbose equivalent (ACAE)/g) enzymes. Liquid chromatography hyphenated with photodiode-array detection and tandem electrospray ionization mass spectrometry (LC-DAD-MSn) analysis revealed phytochemical fingerprint of the two part of the plant and the most abundant constituents were rutin and orientin for aerial parts, 3,5 and 4,5-dicaffeoyl quinic acids for roots respectively. This is the first report gathering scientific data on antioxidant, enzyme inhibitory activities and phytochemical composition of S. hispanica. Thus, this research can be used as one methodological starting point for further investigation on this plant.

Breynia retusa (Dennst.) Alston (also known as Cup Saucer plant) is a food plant with wide applications in traditional medicine, particularly in Ayurveda. Extracts obtained with four solvents (dichloromethane, methanol, ethyl acetate and water), from three plant parts, (fruit, leaf and bark) were obtained. Extracts were tested for total phenolic, flavonoid content and antioxidant activities using a battery of assays including 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP), cupric reducing antioxidant capacity (CUPRAC), total antioxidant capacity (TAC) (phosphomolybdenum) and metal chelating. Enzyme inhibitory effects were investigated using acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, &alpha, amylase and &alpha, glucosidase as target enzymes. Results showed that the methanolic bark extract exhibited significant radical scavenging activity (DPPH: 202.09 &plusmn, 0.15, ABTS: 490.12 &plusmn, 0.18 mg Trolox equivalent (TE)/g), reducing potential (FRAP: 325.86 &plusmn, 4.36: CUPRAC: 661.82 &plusmn, 0.40 mg TE/g) and possessed the highest TAC (3.33 &plusmn, 0.13 mmol TE/g). The methanolic extracts were subjected to LC-DAD-MSn and NMR analysis. A two-column LC method was developed to separate constituents, allowing to identify and quantify forty-four and fifteen constituents in bark and fruits, respectively. Main compound in bark was epicatechin-3-O-sulphate and isolation of compound was performed to confirm its identity. Bark extract contained catechins, procyanidins, gallic acid derivatives and the sulfur containing spiroketal named breynins. Aerial parts mostly contained flavonoid glycosides. Considering the bioassays, the methanolic bark extract resulted a potent tyrosinase (152.79 &plusmn, 0.27 mg kojic acid equivalent/g), &alpha, amylase (0.99 &plusmn, 0.01 mmol acarbose equivalent ACAE/g) and &alpha, glucosidase (2.16 &plusmn, 0.01 mmol ACAE/g) inhibitor. In conclusion, methanol is able to extract the efficiently the phytoconstituents of B. retusa and the bark is the most valuable source of compounds.

Currently, there is a renewed interest towards the development of plant-based pharmacophores. In this work, 16 extracts prepared from the leaves, twigs, roots and fruits of a hydro-halophyte, Rhizophora mucronata Lam. (Family: Rhizophoraceae), were studied for possible antioxidant activity and the phenolic profiles established. Thereafter, enzymatic inhibitory activities (&alpha, amylase, &alpha, glucosidase, tyrosinase, acetyl- (AChE), butyrylcholinesterase (BChE), lipase, and elastase) were assessed. The total phenolic, flavonoid, phenolic acid, tannin, flavanol and triterpenoid content were estimated using standard assays. An untargeted metabolomics-based approach, based on ultra-high-pressure liquid chromatography coupled to quadrupole-time-of-flight mass spectrometry (UHPLC-QTOF-MS) followed by multivariate statistics, was then used to comprehensively profile and describe the phenolics present. UHPLC-QTOF-MS allowed for putatively annotating 104 phenolic acids, 103 flavonols, 94 flavones, 71 anthocyanins, 66 tyrosols, 29 lignans, 15 alkylphenols and 10 stilbenes in the extracts. Nine strains (Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Methicillin-resistant Staphylococcus aureus (MRSA), Salmonella enteritidis, Sarcina lutea, Proteus mirabilis, Bacillus cereus and Candida albicans) were then used to investigate the antimicrobial properties. The methanolic twig extract exhibited significant reducing potential towards Cu (II)/Cu (I) and Fe (III)/Fe (II) (1336.88 &plusmn, 15.70 and 710.18 &plusmn, 21.04 mg TE/g, respectively) and was the most potent DPPH radical scavenger (807.07 &plusmn, 6.83 mg TE/g). Additionally, the methanolic twig extract showed significant inhibition against most targeted enzymes. Anti-microbial results showed that all extracts were active against MRSA. Multivariate analysis demonstrated that the phenolic profile of ethyl acetate extracts and leaves were the two most discriminative parameters in terms of solvents and organs, respectively. The present findings indicated that R. mucronata may be further explored for the management/prevention of oxidative stress, neurodegenerative complications and hyperpigmentation.

Africa is famous for its floral biodiversity, exploited by local people for therapeutic purposes. However, such plants need to be scrutinised scientifically for the presence of bioactive compounds and possible biological properties. This study attempts for the first time to highlight the pharmacological and phytochemical profile of extracts prepared from leaves and stem barks of three African plants (Macaranga hurifolia Beille, Sterculia tragacantha Lindl. and Zanthoxylum gilletii (De Wild.) P. G. Waterman. The extracts were tested for antioxidant and enzyme inhibitory effects. Free radical scavenging, metal chelator, reducing power and phosphomolybdenum assays were performed to evaluate antioxidant effects. To identify enzyme inhibitory effects, cholinesterases (acetylcholinesterase (AChE) and butrylcholinesterase (BChE)), tyrosinase, α-amylase and α-glucosidase were selected as target enzymes. High performance liquid chromatography-Electrospray tandem mass spectrometry (HPLC-ESI-MS) technique was also used for chemical profiling. ABTS (2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) and DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging assays showed that the stem barks of all three African plants were better scavenger than leaf extracts. Sterculia tragacantha was found to be a better metal chelator (64.10 ± 4.66 mg EDTAE/g) among the studied plants. All extracts exhibited good clinical enzyme inhibitory activities. The stem bark of S. tragacantha exhibited the best acetylcholinesterase activity compared to the other plants. HPLC-ESI-MS characterization showed that the most abundant compounds in stem bark were flavonoids in M. hurifolia (4.2 ± 0.2 mg/g DE), proanthocyanidins in S. tragacantha (42 ± 1 mg/g DE) and similar concentrations of phenolic acids and flavonoids in Z. gilletii (2.8–3.1 mg/g DE). Based on the biological activity, the most abundant and relevant bioactive compounds in the extracts were studied using molecular modelling approach against tyrosinase. The studied African plants showed good antioxidant and enzymatic propensities and thus can be considered as potential bioresources for future development of nutraceuticals and/or for pharmaceutical applications.

Members of the genus Euphorbia have attracted much interest as potential sources of bioactive compounds. In this study, the ethyl acetate, methanolic and aqueous extracts of aerial parts of three Euphorbia species namely Euphorbia hirta L., Euphorbia heterophylla L. and Euphorbia convolvuloides Hochst. ex Benth. were screened for their antioxidant [2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP), cupric antioxidant reducing capacity (CUPRAC), metal chelating, total antioxidant capacity (phosphomolybdenum)], and enzymatic properties [α-amylase, α-glucosidase, tyrosinase, acetyl- (AChE), butyryl-cholinesterase (BChE)]. Total phenolic (TPC), total flavonoid content (TFC) and phytochemical profile were established via LC-DAD-MSn. Results showed that the methanolic and aqueous extracts of the three plants yielded the highest TPC with values ranging from 35.84-141.90 mg gallic acid equivalent/g. E. hirta was the most potent DPPH scavenger and chelator reporting the highest equivalent [DPPH: 195.22 mg Trolox equivalent (TE)/g, chelator: 30.73 mg ethylenediaminetetraacetic acid equivalent (EDTAE)/g], while E. heterophylla demonstrated the most significant Fe3+ and Cu2+ reducing potential (FRAP: 194.28 mg TE/g; CUPRAC: 631.25 mg TE/g) and possessed the highest total antioxidant capacity (3.76 mmol TE/g). The AChE, BChE, α-amylase and α-glucosidase enzyme inhibitory effects of the three species were relatively the same. However, E. hirta exhibited the highest anti-tyrosinase activity (109.71 mg kojic acid equivalent /g). Euphorbia convolvuloides showed low antioxidant activities and enzymatic inhibitory effects compared to other. LC-DAD-MSn fingerprint of the phenolics of the three species showed the presence of different derivatives. Quantitative data revealed tannins and flavonoids (25 and 20 mg/g respectively) for E. hirta, high amount of tannins 63 and 21 mg/g of flavonoids for E. heterophylla, while high flavonoid contents for E. convolvuloides, 56 mg/g. Euphorbia hirta proved to the most promising among the three tested species and thus can be explored further by isolating and characterizing active bioactive agents that could be used to manage oxidative stress-related diseases and hyperpigmentation problems.

WOS: 000499762200015, The genus Rhanmus has a great attention as source of bioactive compounds. So, this work aimed to investigate phytochemical profile and biological activity of water and methanolic extracts of different parts of Rhamnus petiolaris Boiss. & Balansa, namely twigs, leaves, mature and unmature fruits. The in vitro antioxidant activity, enzyme inhibitory properties, along with their polyphenol and anthraquinone profiles were determined by untargeted metabolomics. Results showed that methanolic and aqueous unmature fruit extracts were the most effective 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) scavenger (470.96 mg trolox equivalent (TE)/g and 394.96 mg TE/g, respectively). The aqueous unmature fruit extract displayed the most potent cupric and ferric reducing power and showed the highest total phenolic contents (TPC) (137.17 mg gallic acid equivalent (GAE)/g). The methanolic twig extract showed the highest enzymatic inhibitory property against of alpha-glucosidase, tyrosinase, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). On the basis of the correlation coefficients calculated separately for all experimental parameter pairs, flavonols and anthocyanins highly correlated with DPPH, whereas tyrosols correlated with BChE activity. Multivariate statistics following untargeted metabolomics allowed to describe the differences in polyphenols and anthraquinones, as affected by the extraction solvent used. Mature and unmature fruits were substantially comparable and were affected in a similar way by the extraction conditions, while different profiles were recorded for Rhamnus leaves and twigs. These findings indicate that the recovery efficiencies of specific subclasses of compounds (above all when considering flavonoids, phenolic acids and anthraquinones) as a function of the matrix and extraction chosen, significantly affect the phytochemical profile and biological activity of Rhamnus.