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Synedrella nodiflora (L.) Gaertn. (Asteraceae), is a weed with ethnomedicinal uses. To extend scientific information on this species, we evaluated the effects of different extraction procedures (maceration, Soxhlet, sonication and homogenizer-assisted extraction (HAE)) using methanol as solvent, on the chemical composition and biological potential. The chemical profiles of the extracts were identified using a chromatographic (UHPLC-HRMS) technique. The antioxidant and enzyme inhibitory activities of the studied extracts were determined. The extract obtained by Soxhlet technique showed a higher level of total phenolic (TPC) and flavonoid content (TFC) and was a superior source of antioxidant compounds. The macerated extract was the most potent inhibitor of cholinesterases and α-glucosidase, whereas the highest activity against tyrosinase was observed in the order of sonication > Soxhlet > HAE > maceration. A modest activity was observed against α-amylase for all the extracts. Multivariate analysis showed that the bioactive compounds recovery and the biological activities of S. nodiflora were mostly dependent on the nature of the extraction technique used. In conclusion, S. nodiflora extracts showed good biological potential and data massed from this study could serve as a scientific baseline for further investigation in order to exploit its potential for designing novel bio-products with therapeutic applications.

In the present study, extracts of four medicinal plants (Cajanus cajan, Carica papaya, Morinda morindoides, and Senna alexandrina) obtained at two different extraction temperatures (24 and 45 degrees C) were investigated for their polyphenolic contents, antioxidant, and enzyme inhibitory properties. For instance, extracts of the studied species yielded total phenolic and flavonoid contents in the range of 17.8-66.3 mg GAE/g and 4.18-26.8 mg RE/g, respectively. High performance liquid chromatography (HPLC) coupled with antioxidant assays (HPLC-FRAP and HPLC-DPPH) was employed for direct identification of antioxidant compounds. The extracts showed moderate to high antioxidant potentials in various assays performed (radical scavenging activity: 10.15-240.08 mg TE/g; reducing activity: 24.88-229.59 mg TE/g; metal chelating activity: 5.56-18.32 mg EDTAE/g and total antioxidant capacity: 1.40-2.18 mM TE/g). Additionally, the extracts were found to exert inhibitory properties against all the studied enzymes (anti-acetylcholinesterase: 1.80-2.29 mg GALAE/g; anti-butyrylcholinesterase: 0.19-3.13 mg GALAE/g; anti-amylase: 0.39-0.58 mmol ACAE/g; anti-glucosidase: 0.17-1.36 mmol ACAE/g and anti-tyrosinase: 60.97-73.71 mg KAE/g). Of all, C. cajan extracts were revealed to be the best antioxidants and inhibitors of most enzymes. Therefore, this study demonstrated the pharmacological potentials of the four medicinal plants, especially C. cajan as viable sources of phyto-ingredients that could be of interest in nutraceutical development. Novelty impact statement The methanol extracts from four medicinal plant with different extraction temperatures (24 and 45 degrees C) were investigated. HPLC-DPPH and HPLC-FRAP methodologies were used. Different levels of phenolics in the tested extracts were determined. Cajamus cajan extracts were found to be the best one in the antioxidant assays. Our findings could be opened valuable windows in the further pharmaceutical studies and applications

The genus Acacia (Family Leguminosae) is composed of several medicinal plants used for treating miscellaneous diseases. Amid the important members of this genus, A. nilotica and A. ataxacantha are widely employed for their tremendous healing properties. Hence, this present work aimed to determine the total phenolic and flavonoid contents and investigate the antioxidant, antiproliferative, anti-enzyme and antimicrobial potentials of methanolic and water extracts of leaves and stem bark of A. nilotica and A. ataxacantha obtained by maceration and ultrasonication. The total phenolic and flavonoid contents were obtained in the range of 33.35–116.60 mg GAE/g and 0.26–49.90 mg RE/g, respectively, with the methanolic leaf extracts of both species showing the highest contents. Moreover, the methanolic extracts were observed to display higher antioxidant potentials in almost all antioxidant assays performed compared to the water extracts (ABTS: 52.66–943.81 mg TE/g, DPPH: 8.51–493.90 mg TE/g, CUPRAC: 106.39–1193.75 mg TE/g; FRAP: 31.38–416.21 mg TE/g, and phosphomolybdenum: 0.90–4.17 mM TE/g). However, the water extracts were seen to be better metal chelators than the methanolic extracts (8.47–36.85 mg EDTAE/g). Additionally, all extracts were found to exhibit anti-tyrosinase (30.79–74.80 mg KAE/g) and anti-amylase (0.10–1.10 mM ACAE/g) properties. With the exception of a few extracts, glucosidase and acetylcholinesterase inhibitions (1.69–2.12 mg ACAE/g and 0.42–2.61 mg GALAE/g, respectively) were also demonstrated. While the methanolic extracts of both species showed antimicrobial potency against all the 18 tested microorganisms (gram positive, gram negative, and fungi), the water extracts were effective only against the gram positive bacteria. The extracts were also found to exhibit antiproliferative effects on SH-SY5Y human neuroblastoma cells, with the methanolic extracts showing higher cytotoxic potential than the water extracts. Therefore, this study showed these species to be good sources of antioxidants, enzyme inhibitors, antimicrobials and antiproliferative agents, which could be of great interest for their applications as natural bioactive ingredients in the development of pharmaceuticals and nutraceuticals.

© 2021 Elsevier LtdThe 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 (IC50: 1.05 mg/mL) and ABTS (IC50: 1.02 mg /mL). The best cholinesterase inhibitory abilities were observed with the methanol extract (IC50: 0.51 and 0.52 mg/mL for AChE and BChE, respectively), while DCM exhibited the strongest α-amylase (IC50: 1.21 mg/mL) and α-glucosidase (IC50: 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 IC50 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.

Spermacoce verticillata (L.) G. Mey. is commonly used in the folk medicine by various cultures to manage common diseases. Herein, the chemical and biological profiles of S. verticillata were studied in order to provide a comprehensive characterization of bioactive compounds and also to highlight the therapeutic properties. The in vitro antioxidant activity using free-radical scavenging, phosphomolybdenum, ferrous-ion chelating and reducing power assays, and the inhibitory activity against key enzymes such as acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), tyrosinase, α-amylase and α-glucosidase of S. verticillata extracts (dichloromethane, ethyl acetate, methanol and water) were investigated. The highest total phenolic and flavonoid content were observed in the methanolic and aqueous extracts. Exhaustive 2DNMR investigation has revealed the presence of rutin, ursolic and oleanoic acids. The methanolic extract, followed by aqueous extract have showed remarkable free radical quenching and reducing ability, while the dichloromethane extract was the best source of metal chelators. The tested extracts showed notable inhibitory activity against cholinesterases (AChE: 1.63-4.99 mg GALAE/g extract and BChE: 12.40-15.48 mg GALAE/g extract) and tyrosinase (60.85-159.64 mg KAE/g extract). No inhibitory activity was displayed by ethyl acetate and aqueous extracts against BChE and tyrosinase, respectively. All the tested extracts showed modest α-amylase inhibitory activity, while only the ethyl acetate and aqueous extracts were potent against α-glycosidase. This study further validates the use of S. verticillata in the traditional medicine, while advocating for further investigation for phytomedicine development.

Jatropha L. species, in particular, J. curcas and J. gossypiifolia, are well known medicinal plants used for treating various diseases. In the present study, leaf and stem bark extracts of J. curcas and J. gossypiifolia obtained by maceration or homogenizer assisted extraction, were investigated for their phytochemical contents and biological potential as antioxidants, enzyme inhibitors and neuromodulators. In this regard, the gene expression of tumor necrosis factor α (TNFα) and brain-derived neurotrophic factor (BDNF) was investigated in hypothalamic HypoE22 cells. Finally, a bioinformatics analysis was carried out with the aim to unravel the putative mechanisms consistent with both metabolomic fingerprints and pharmacological effects. The leaf extracts of J. curcas showed higher total phenolic content (TPC) and total flavonoid content (TFC) than the stem bark extracts (range: 5.79–48.95 mg GAE/g and 1.64–13.99 mg RE/g, respectively), while J. gossypiifolia possessed TPC and TFC in the range of 42.62–62.83 mg GAE/g and 6.97–17.63 mg RE/g, respectively. HPLC-MS/MS analysis revealed that the leaf extracts of both species obtained by homogenizer assisted extraction are richer in phytochemical compounds compared to the stem bark extracts obtained by the same extraction method. In vitro antioxidant potentials were also demonstrated in different assays (DPPH: 6.89–193.93 mg TE/g, ABTS: 20.20–255.39 mg TE/g, CUPRAC: 21.07–333.30 mg TE/g, FRAP: 14.02–168.93 mg TE/g, metal chelating activity: 3.21–17.51 mg EDTAE/g and phosphomolybdenum assay: 1.76–3.55 mmol TE/g). In particular, the leaf extract of J. curcas and the stem bark extract of J. gossypiifolia, both obtained by homogenizer assisted extraction, showed the most potent antioxidant capacity in terms of free radical scavenging and reducing activity, which could be related to their higher TPC and TFC. Furthermore, anti-neurodegenerative (acetylcholinesterase inhibition:1.12–2.36 mg GALAE/g, butyrylcholinetserase inhibition: 0.50–3.68 mg GALAE/g), anti-hyperpigmentation (tyrosinase inhibition: 38.14–57.59 mg KAE/g) and antidiabetic (amylase inhibition: 0.28–0.62 mmol ACAE/g, glucosidase inhibition: 0.65–0.81 mmol ACAE/g) properties were displayed differentially by the different extracts. Additionally, the extracts were effective in reducing the gene expression of both TNFα and BDNF, which could be partially mediated by phenolic compounds such as naringenin, apigenin and quercetin. Indeed, the scientific data obtained from the present study complement the several other reports highlighting the pharmacological potentials of these two species, thus supporting their uses as therapeutically active plants.

To avail the possible pharmacological actions of Brideliaferruginea Benth., the present investigation was designed to quantitatively analyze the total flavonoid and phenolic contents and assess the various antioxidant and enzyme inhibition properties of leaf and stem bark extracts (ethyl acetate, water and methanolic) of B. ferruginea. Anti-proliferative effect was also investigated against human colon cancer cells (HCT116) as well as the antimicrobial potential against multiple bacterial and fungal (yeasts and dermatophytes) strains. The methanolic and water extracts of the stem bark demonstrated the highest phenolic content (193.58 ± 0.98 and 187.84 ± 1.88 mg/g, respectively), while the leaf extracts showed comparatively higher flavonoid contents (24.37–42.31 mg/g). Overall, the methanolic extracts were found to possess the most significant antioxidant potency. Compared to the other extracts, methanolic extracts of the B. ferruginea were revealed to be most potent inhibitors of acetyl- and butyryl-cholinesterases, tyrosinase α-amylase, except α-glucosidase. Only the ethyl acetate extracts were found to inhibit glucosidase. Additionally, the stem bark methanolic extract also showed potent inhibitory activity against E. coli and gram-positive bacteria (MIC (minimum inhibitory concentration): 2.48–62.99 µg/mL), as well as all the tested fungi (MIC: 4.96–62.99 µg/mL). In conclusion, B. ferruginea can be regarded as a promising source of bioactive compounds displaying multifunctional pharmacological activities and thus is a potential candidate for further investigations in the endeavor to develop botanical formulations for pharmaceutical and cosmeceutical industries.

Alchornea cordifolia (Schumach. & Thonn.) Müll. Arg. is a well-known African medicinal plant traditionally used for various healing purposes. In the present study, methanolic, ethyl acetate and infusion extracts of A. cordifolia leaves were studied for their total phenolic and flavonoid contents and screened for their chemical composition. Moreover, the enzyme (acetyl- and butyryl-cholinesterases, α-amylase, α-glucosidase, and tyrosinase) inhibitory and cytotoxicity activities on HepG2: human hepatocellular carcinoma cells, B16 4A5: murine melanoma cells, and S17: murine bone marrow (normal) cells of extracts were evaluated. Finally, components-targets and docking analyzes were conducted with the aim to unravel the putative mechanisms underlying the observed bio-pharmacological effects. Interestingly, the infusion and methanolic extracts showed significantly higher total phenolic and flavonoid contents compared with the ethyl acetate extract (TPC: 120.38–213.12 mg GAE/g and TFC: 9.66–57.18 mg RE/g). Besides, the methanolic extracts followed by the infusion extracts were revealed to contain a higher number of compounds (84 and 74 compounds, respectively), while only 64 compounds were observed for the ethyl acetate extract. Gallic acid, ellagic acid, shikimic acid, rutin, quercetin, myricetin, vitexin, quercitrin, kaempferol, and naringenin were among the compounds that were commonly identified in all the studied extracts. Additionally, the methanolic and infusion extracts displayed higher antioxidant capacity than ethyl acetate extract in all assays performed. In ABTS and DPPH radical scavenging assays, the methanol extract (500.38 mg TE/g for DPPH and 900.64 mg TE/g for ABTS) exhibited the best ability, followed by the water and ethyl acetate extracts. Furthermore, the extracts exhibited differential enzyme inhibitory profiles. In particular, the methanolic and infusion extracts showed better cytotoxic selectivity activity against human hepatocellular carcinoma cells. Overall, this study demonstrated A cordifolia to be a species worthy of further investigations, given its richness in bioactive phytochemicals and wide potentialities for antioxidants and pharmacological agents. info:eu-repo/semantics/publishedVersion

Caesalpinia bonduc and C. decapeleta var. japonica have great importance in traditional medicine systems but scientific information's are still lacking for their potentials. To explore their bioactivity, we assessed the antioxidant, enzyme inhibitory abilities of the dichloromethane (DCM), ethyl acetate, methanol, and water extracts prepared from the leaves and bark. The cytotoxicity and anticancer properties of the extracts were also assessed in vitro. The water extract of C. decapeleta leaves possessed highest phenolic content (108.16 mg gallic acid equivalent (GAE)/g extract), while the highest flavonoid content was recorded for the C. bonduc leaf methanolic extract (27.89 mg rutin equivalent (RE)/g extract). In general, C. decapeleta extracts possessed higher radical scavenging potential compared to C. bonduc extracts. C. decapeleta DCM leaves extract (10.20 mg galantamine equivalent (GALAE)/g extract) showed highest inhibition against butyrylcholinesterase. The cytotoxicity of the most potent methanolic and aqueous extracts were assessed against four cell lines. The chemical profiles of both species appeared to be different. C. bonduc was abundant in organic and phenolic acids as well as their esters. Flavonoid glycosides, bonducellin and its derivatives and caesalminaxins were identified. Whereas, C. decalpetala possessed many galloylated compounds. The cytotoxicity of C. bonduc and C. decapetala extracts was tested using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) based assay on VERO (kidney of an adult African Green monkey cells), HeLa (human cervical adenocarcinoma cells), RKO (human colon carcinoma cells), FaDu (human hypopharyngeal squamous carcinoma cells) cell lines. C. bonduc bark water extract exhibited the highest cytotoxicity towards HeLa (50 % cytotoxic concentration (CC50): 28.5 μg/mL) cancer cell line, as compared to normal VERO cells (CC50:35.87 μg/mL). For C. decapetala, the highest cytotoxicity was found for bark methanol extract on the HeLa cells with CC50 of 46.08 μg/mL and selectivity index of 3.33. In the gene ontology analysis, prostate cancer, nuclear factor kappa B (NF-kappa B) signaling, proteoglycans in cancer pathways might support the results of the cytotoxic assays. These results showed that the tested Caesalpinia species, showing potent inhibitory action against butyrylcholinesterase, might represent novel phytotherapeutic avenues for the management of Alzheimer's disease.

Croton hirtus L’Hér methanol extract was studied by NMR and two different LC-DAD-MSn 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.

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.

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

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.

：Achyranthes aspera Linn. (Amaranthaceae), commonly known as the Prickly Chaff flower, is used as herbal medicine in the Ivorian&rsquo, 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&rsquo, s disease, (cholinesterases: AchE and BChE), type 2 diabetes (&alpha, glucosidase and &alpha, 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 &plusmn, 0.12 mg GAE/g), while the dichloromethane extract (38.48 &plusmn, 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 &plusmn, 5.05 mgKAE/g), as well. Modest to moderate inhibitory activity was observed against &alpha, amylase (all extracts) and &alpha, 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.

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.

WOS: 000506413200012, Crotalaria retusa L (Fabaceae) also known as 'rattlebox' has been used in traditional medicine for the management of various human ailments. The present study comparatively evaluated the alpha-amylase, alpha-glucosidase, acetylcholinesterase, butyrylcholinesterase, and tyrosinase inhibitory activity, antioxidant properties, as well as phytochemical profiles of extracts of C. retusa (bark, fruits, and flowers) obtained by homogenization, maceration, ultrasonication, and Soxhlet extractions. Little variation was noted between the phytochemical profiles obtained by liquid chromatography-mass spectrometry/mass spectrometry (LC-MS/MS) of C. retusa same plant parts extracted by different methods while the different plant parts showed specific phytochemical fingerprints. For instance, myricetin was identified in C. retusa fruits only. Fruit and bark extracts possessed the highest concentrations of quercetin and rutin, respectively. p-hydroxybenzoic acid, a phenolic derivative of benzoic acid, was identified in all C. retusa plant parts. Spectrophotometric determinations revealed that C. retusa bark extracts have highest concentrations of phenolic and flavonoids. Besides, C. retusa bark extracts showed highest antioxidant capacity. The extracts showed high inhibitory activity against alpha-glucosidase (21.22-4.81 mmol acarbose equivalent/g), acetylcholinesterase (8.71-8.26 mg galantamine equivalent/g), butyrylcholinesterase (4.16-2.36 mg galantamine equivalent/g), and tyrosinase (133.11-125.26 mg kojic acid equivalent/g). Multivariate component analysis showed that the plant part was the main factor responsible for the observed variability between the extracts. Data collected proved that C. retusa has the potential for the development of novel biopharmaceutical, nutraceutical, and cosmetical products. (C) 2019 SAAB. Published by Elsevier B.V. All rights reserved., European Regional Development Fund (ERDF)European Union (EU); University of Rijeka [uniri-biomed-18-133]; Croatian Government; European Union (European Regional Development Fund-the Competitiveness and Cohesion Operational Programme) [KK.01.1.1.01, KK.01.1.1.01.0002], We greatly appreciate the granted access to equipment owned by the University of Rijeka within the project "Research Infrastructure for Campus-based Laboratories at University of Rijeka," financed by the European Regional Development Fund (ERDF). We also acknowledge the University of Rijeka research support uniri-biomed-18-133. We would like to thank Croatian Government and the European Union (European Regional Development Fund-the Competitiveness and Cohesion Operational Programme - KK.01.1.1.01) for funding this research through project Bioprospecting of the Adriatic Sea (KK.01.1.1.01.0002) granted to The Scientific Centre of Excellence for Marine Bioprospecting-BioProCro.

In African traditional medicine Cochlospermum planchonii is used to manage various diseases such as malaria, diarrhoea, jaundice, infections and inflammation, hence presents the potential to be a good source of bioactive compounds. In this study, traditional and green extraction techniques have been used namely green extraction (homogenizer assisted extraction (HAE) and Sonication (SON)) and conventional extraction (Maceration (MAC), and Soxhlet (SOX)). Extracts prepared from aerial parts were studied for the total phenolic, flavonoids, total antioxidant and enzyme inhibitory properties also relating their biological properties and chemical content by multivariate analysis. The total phenolic contents obtained were in the order of HAE (221.78 mg gallic acid equivalent (GAE)/g) > SON (202.64 mg GAE/g) > SOX (190.28 mg GAE/g) > MAC (187.45 mg GAE/g). The highest flavonoid content (rutin equivalent (RE)) was obtained by SOX (65.67 ± 0.43 mg rutin equivalent (RE)/g). The highest antioxidant activity was recorded for HAE. C. planchonii extracts showed inhibitory activity against acetylcholinesterase (8.46–8.56 mg galantamine equivalent (GALAE)/g), tyrosinase (165.76–171.10 mg kojic acid equivalent (KAE)/g) and α-amylase (1.18–1.30 mmol acarbose equivalent (ACAE)/g) enzymes. It was found that the observed enzyme inhibitory properties was dependent on the type of extraction methods. Only SOX extract presented α-glucosidase inhibition (21.26 mmol ACAE/g) suggesting potential studies of this extract as antidiabetic. Liquid chromatography coupled to diode array detection and electrospray ionization tandem mass spectrometry (LC-DAD-ESI-MSn) was used for the qualitative analysis of the samples, allowing the quantification of gallic acid, prodelphynidins and flavonol derivatives. Based on multivariate analysis, green extraction techniques (HAE and SON) were different from conventional techniques (MAC and SOX). Results showed the usefulness of green extraction techniques for obtaining bioactive enriched fractions and tend to highlight the need for additional investigations to fully explore the potential usefulness of C. planchonii as source of antioxidant, antidiabetic and whitening agent as well as cholinesterase inhibitors.

In the present study, Passiflora foetida extracts characterized by different polarities were studied for their phytochemical profile, enzyme inhibitory, and antioxidant potentials. In silico, in vitro and ex vivo studies were also carried out on methanol and water extracts for predicting pharmacokinetics and pharmacodynamics. In this regard, neuronal HypoE22 cells, isolated mouse skin tissues, and pathogen dermatophytes strains were exposed to extracts. Emphasis was given to the preventing effects induced by the extracts on hydrogen peroxide-induced alterations of prostaglandin E2 (PGE2), l-dopa, and serotonin. Chemical analysis revealed the presence of similar compounds in infusion and methanolic extracts. The ex vivo studies also showed protective skin properties by P. foetida water and methanol extracts, as evidenced by the decrease of hydrogen peroxide-induced PGE2 level. Additionally, the blunting effects on hydrogen peroxide-induced l-dopa levels are consistent with the anti-tyrosinase effect exerted by both extracts. In silico studies demonstrated the affinity of extracts&rsquo, phytochemicals, namely apigenin, chrysoeriol, loliolide, luteolin, quercetin, and vitexin, towards cyclo-oxygenase-2 and tyrosinase. Finally, microbiological tests demonstrated the efficacy of P. foetida methanol and water extracts as anti-mycotic agents against Trichophyton and Arthroderma species, involved in skin inflammation. Hence, P. foetida L. extracts could represent potential sources of pharmaceuticals and nutraceuticals.

In the present investigation, extracts of Erigeron floribundus leaves obtained by four isolation procedures, including homogenizer-assisted extraction, maceration, sonication and Soxhlet extraction...

Khaya senegalensis A. Juss (Meliaceae) is a popular medicinal plant, widely used in the management of various ailments in the African traditional medicine. This study attempts to investigate into the different extraction methods (homogenizer-assisted extraction (HAE), maceration (MAC), infusion and Soxhlet (SE) extraction) on the pharmacological properties and chemical profiles of K. senegalensis. Antioxidant properties and inhibitory potential against key enzymes were assessed and bioinformatics analysis was conducted on selected limonoids to predict putative pharmacokinetics and protein targets underlying the pharmacological effects. Overall, the leaf extracts showed notable flavonoid (20.59–104.43 mg RE/g) content and the stem barks extracts displayed the highest total phenolic (87.69–46.28 mg GAE/g), phenolic acid (62.96–107.22 mg CE/g), flavanol (3.60–135.40 mg CAE/g) contents. All extracts showed remarkable antioxidant activities, with the MAC-Water leaf extract being most active in all the assays. Regarding stem bark, the MAC-MeOH extract exerted the highest free radical scavenging abilities, while HAE and MAC extracts were better sources of reducing agent and metal chelators. The HAE-MeOH, MAC-Water, and SE extracts showed noteworthy inhibitory activity against AChE, BChE (only stem barks), tyrosinase and α-glucosidase (only stem barks). All extracts displayed moderate inhibitory activities against α-amylase. The bioinformatics approach showed that khayanoside A and C interacted with multiple isoforms of metalloproteinase, while humilin B and khayanone interacted with opioid receptors. To sum up, the chemical profiles and biological activities of K. senegalensis were closely dependent on the extraction methods. Results amassed from this study showed that K. senegalensis is a potent source of bioactive compounds which could be explored as a functional food.

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 (IC50 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.

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.