Phytochemical profiling,in vitro biological activities,and in-silico molecular docking studies of Typha domingensis

A comparative study between methanolic extract and n-hexane fraction of Typha domingensis (Typhaceae) was conducted for the evaluation of phytochemical potential, in vitro biological activities, and in-silico molecular docking studies. The phytochemical composition was estimated by total phenolic and total flavonoid contents, and by GC–MS analysis. Several biological activities were performed such as antioxidant assays (ABTS, FRAP, DPPH, & CUPRAC), enzyme inhibition activity (Tyrosinase, Acetylcholinesterase & Butyrylcholinesterase), thrombolytic activity, and antimicrobial activity (antibacterial & antiviral) to evaluate the medicinal importance of Typha domingensis. The results of the comparative study showed that methanolic extract has more total phenolic and total flavonoid contents (95.72 ± 5.76 mg GAE/g, 131.66 ± 7.92 mg QE/g, respectively) as compared to n-hexane fraction which confirms its maximum antioxidant potential (ABTS 114.31 ± 8.17, FRAP 116.84 ± 3.01, DPPH 283.54 ± 7.3 & CUPRAC 284.16 ± 6.5 mg TE/g). In the case of in vitro enzyme inhibition study and thrombolytic activity, better results were observed for methanolic extract. Almost similar antimicrobial patterns were observed for both methanolic extract and n-hexane fraction of Typha domingensis. The major bioactive phytochemicals identified by GC–MS were further analyzed for in-silico molecular docking studies to determine the binding affinity between ligands and the enzymes. The docking study indicated that most of the bioactive compounds showed a better binding affinity with enzymes as compared to the standard compounds (kojic acid & galantamine). The results of this study recommended that Typha domingensis has promising pharmaceutical importance and it should be further analyzed for the isolation of bioactive phytochemicals which may be useful for the treatment of several diseases.     

Polyphenolic characterization and evaluation of multimode antioxidant,cytotoxic, biocompatibility and antimicrobial potential of selected ethno-medicinal plant extracts

IntroductionScientific evidence about biological profile of natural products can support their traditional uses. The current work was aimed to assess phytochemical and biological profile of nine medicinal plants collected from Herbalists.MethodsExtracts prepared in different solvents were subjected to phytochemical, antioxidant, enzyme inhibitory, cytotoxic, and antimicrobial activities. Reverse phase-high performance liquid chromatography (RP-HPLC) analysis was performed for the quantification of polyphenols.ResultsResults showed methanol extract (M) being potent as compared to others. Gentian lutea M showed maximum extract recovery (15.00 ± 0.11 % w/w) and TFC (30.82 ± 0.21 μg QE/mg extract). Nigella sativa M displayed highest TPC (44.99 ± 0.43 μg GAE/mg extract) and TAC (334.72 ± 0.35 μg AAE/ mg extract). Results showed noteworthy quantities of vanillic acid, rutin, kaempferol, emodin in ethyl acetate (EA) and methanol (M) extracts of plants assessed by RP-HPLC. Gentisic acid was highest (11.75 µg/mg extract) in T. arjuna M extract. Similarly, maximum %FRSA (82.28 ± 0.03 %) and TRP (160.40 ± 0.38 μg AAE/ mg extract) were depicted by Terminalia chebula and Chamomilla recutita, respectively. Moreover, Mentha longifolia and G. lutea M demonstrated noteworthy (p < 0.05) antibacterial activity against Staphylococcus aureus (14 ± 0.7 mm) and Klebsiella pneumoniae (12 ± 0.3 mm), respectively. Curcuma amada, C. recutita, Murraya koenigii and G. lutea M had significant α-glucosidase activity. Another good solvent for extraction was ethyl acetate (EA), whose extracts were secondary to methanol in producing significant biological profile. For example, EA of N. sativa (TPC: 1.46 ± 0.45 µg GAE/ mg extract), G. lutea (TRP: 160.33 ± 0.52 μg AAE/mg extract: ZOI of 12 ± 0.5 mm in K. pneumoniae) and Mormodica charantia (α-amylase inhibition: 39.5 ± 0.10 %) showed significant bioactivities. All extracts displayed mild antifungal protein kinase inhibition activities and were significantly (greater than80 %: p < 0.05) cytotoxic to brine shrimps with negligible hemolytic activity.ConclusionBriefly, variable polarity solvent extracts of studied plants will be processed for isolation of antioxidant, cytotoxic, carbohydrate enzyme inhibitory and antibacterial compounds.     

Novel silver-platinum bimetallic nanoalloy synthesized from Vernonia mespilifolia extract: Antioxidant,antimicrobial, and cytotoxic activities

In this study, bimetallic nanoparticles comprising silver and platinum with promising therapeutic activities were synthesized using ethanolic Vernonia mespilifolia plant extract for the first time. The bimetallic silver-platinum nanoparticles (AgPtNPs) were characterized using solid-state techniques including UV–vis spectroscopy, Fourier transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), and energy-dispersive X-ray spectroscopy (EDX) techniques. The internal morphological structure showed that the AgPtNPs were spherical with a diameter of approximately 35.5 ± 0.8 nm, while FTIR confirmed the effective capping and formation of the nanoparticles by phytoconstituents. The polyphenolic contents of the green synthesized nanoparticles from the ethanolic extract of V. mespilifolia (AgNPs and AgPtNPs) was found to be (28.0 ± 0.8 and 13.6 ± 0.1 mg GAE/g) total phenol, while the flavonoids content was (366.2 ± 17.0 and 126.6 ± 0.2 mg QE/g), and proanthocyanins content was (161.8 ± 0.6 and 70.2 ± 0.6 mg CE/g). The AgPtNPs displayed a greater ability to scavenge free radicals, especially DPPH and ABTS (IC₅₀ 19.5 and 21.6 µg/mL) respectively when compared with AgNPs and ascorbic acid. Besides, the AgPtNPs had a higher ferric reducing antioxidant power (FRAP) (44.1 mg GAE/g) when compared to AgNPs (18.5 mg GAE/g). Moreover, the AgPtNPs showed a two-fold antimicrobial activity towards pathogenic microbes compared to AgNPs and a selective cytotoxic potency towards MCF-7 breast cancer cell line compared to HEK 293 normal cell line. In summary, these fascinating bioactivities displayed by the AgPtNPs highlighted their potential in therapeutic biomedical applications.     

Phytochemical,antioxidant, enzyme inhibitory,thrombolytic, antibacterial,antiviral and in silico studies of Acacia jacquemontii leaves

The main objective of this work was to gain insight into biological propensities, and bioactive phytochemicals of Acacia jacquemontii Benth, a wild plant providing medicinal components, as well as to establish a link between its phytochemical profile and biological activities. Phytochemical profiling revealed the presence of a higher amount of total phenolic (271.44 ± 4.41 mg GAE/g) and flavonoid contents (216.47 ± 5.82 mg QE/g) in methanolic extract (MEAJ), and as compared to n-hexane fraction (HEAJ) and stronger biological activities of MEAJ were possibly linked to the higher bioactive contents. The freshly collected plant leaves showed a strong antioxidant potential (total antioxidant capacity 1.03 ± 0.19 mmol TE/g), which was found even stronger in dried methanolic extract (TAC; 4.36 ± 1.12 mmol TE/g), moreover, MEAJ also showed strong antioxidant potential when investigated by different antioxidant assays (DPPH; 154.04 ± 2.47, ABTS; 122.36 ± 0.80, FRAP; 453.18 ± 5.9, CUPRAC; 1389.97 ± 5.32 mg TE/g). The MEAJ showed good tyrosinase inhibition activity (71.69 %), compared with 83 % inhibition by kojic acid. Ten major compounds identified by GC–MS were docked and eight legends showed lower binding energies (-6 to ?7.8 kcal/mol) compared with kojic acid (-5.9 kcal/mol), which shows the possible role of these compounds in the anti-tyrosinase activity of the extract, and the ADMET analysis predicted the drug-likeness and safety profile of the studied compounds. The thrombolytic effect of MEAJ was 56.41 ± 0.75 to 57.15 ± 1.41 % which was comparable with streptokinase (82.44 ± 1.15 to 84.14 ± 0.95 %). Antibacterial activity of MEAJ was also good (MEAJ; 0.5–2.0 mg/mL, and co-amoxiclav; 5.0–12.5 µg/mL), and the highest activity was observed against Bacillus subtilis (MEAJ; 0.5 mg/mL, co-amoxiclav; 5.0 µg/mL). The antiviral activity of MEAJ was highly strong (HA titer; 00 to 08) against all the tested strains. It can be concluded that A. jacquemontii is a prospective source of phytochemicals with strong biological activities, and their usage in formulations of natural products and pharmaceuticals is recommended, however, further research may address the discovery and development of novel drugs for the pharmaceutical industry.     

Total phenolic and flavonoid contents,antioxidant, antidiabetic and antiplasmodial activities of Garcinia forbesii King: A correlation study

Garcinia forbesii King belongs to Clusiaceae is a source of secondary metabolites especially xanthones with various biological activities. G. forbesii King is also known for its empirical use for malaria and diabetes. This study investigated the total phenolic and flavonoid contents, in vitro antioxidant, antidiabetic and antiplasmodial activities of four extracts attained from the stem bark of G. forbesii King. The total phenolic and flavonoid contents were determined by spectrophotometric methods and antioxidant activity was evaluated by DPPH, ABTS, FRAP assays. In vitro antidiabetic activity was assessed by α-glucosidase and α-amylase assays and antiplasmodial activity was studied against chloroquine sensitive Plasmodium falciparum strain 3D7. The highest value of total phenolic (187.37 ± 0.06 mg GAE/g) and flavonoid (35.97 ± 0.02 mg QE/g) contents were recorded in n-hexane and methanolic extracts. n-Hexane extract showed the highest DPPH activity with IC₅₀ of 8.12 ± 0.02 μg/mL. Ethyl acetate extract exhibited better scavenging ability for ABTS with IC₅₀ of 3.88 ± 0.04 μg/mL. The FRAP assay showed better activity in methanol extract with an inhibition value of 73.68 ± 3.66 µM Fe²⁺/g. The strong inhibition against α-glucosidase and α-amylase were displayed by dichloromethane extract with IC₅₀ of 35.13 ± 2.01 μg/mL and 4.83 ± 0.20 μg/mL. n-Hexane and methanol extracts showed significant antiplasmodial activity with IC₅₀ of 0.23 ± 0.01 μg/mL and 0.73 ± 0.01 μg/mL, respectively. The correlation analysis indicated a positive relationship of total phenolic and flavonoid contents with antiplasmodial activity. The results revealed that n-hexane and methanol extracts could be used as a potential natural antiplasmodial, while dichloromethane extract is a promising natural antidiabetic.     

Chemical profiling of Aristolochia tagala Cham. leaf extracts by GC-MS analysis and evaluation of its antibacterial activity

Aristolochia tagala Cham. (Aristolochiaceae) is an underexplored medicinal plant traditionally used to treat snakebites, stomachaches, and poisonous bites. In this study, chemical profiling of the petroleum ether, chloroform, ethyl acetate, methanol, and hydro-alcoholic extracts of the plant was investigated by gas chromatography-mass spectrometry. The antibacterial activity of the plant was tested against ten bacterial strains using the agar disc diffusion and microdilution method. In total, forty two compounds were identified from the extracts with neophytadiene, palmitic acid, phytol, trans-δ9-octadecenoic acid, phytyl palmitate, phytyl tetradecanoate, ergost-5-en-3-ol, (3beta,24r)-,z,z-8,10-hexadecadien-1-ol, stigmasterol, and tetrapentacontane as major phytoconstituents. The hydro-alcoholic extract possessed maximum total phenolics (52.58 ± 06 mg GAE/g), total flavonoids (48.66 ± 91 QRE/g), total flavanols (67.20 ± 64 QRE/g) and vitamin E content (31.26 ± 0.05 mg ATE/g). For antibacterial activity, hydro-alcoholic extract of Aristolochia tagala effectively controlled the growth of bacterial strains such as Proteus valgaris (26.3 mm) and Pseudomonas aeruginosa (19.33 mm) and the same extract showed notable minimum inhibitory concentration (MIC) against the growth of bacteria like Escherichia coli (10.93 μg/ml) and Enterobacter aerogenes (43.7 μg/ml). It was determined that, hydro-alcoholic and methanolic extracts Aristolochia tagala leaf found to have a number of bioactive compounds with significant antibacterial activity against the pathogenic bacteria. Further investigations are necessary to isolate and characterize bioactives and to evaluate its therapeutic potential.     

α-glucosidase inhibitory,antioxidant activity,and GC/MS analysis of Descurainia sophia methanolic extract: In vitro,in vivo,and in silico studies

Due to the presence of various phenolic compounds in D.sophia, this plant may have an inhibitory effect on α-Glc and ultimately diabetes control. Therefore, this work aims to scrutinize total phenolic, flavonoid contents, antioxidant capacity, and α-Glc inhibitory activity in aerial parts of methanolic D.sophia extract. The methanolic flower extracts were selected from among aerial parts for the experimental study of anti-diabetic effects by α-Glc inhibitory assays. The flower extracts were also studied by GC/MS to detect the compounds. The total phenolic and flavonoid contents were 21.38 ± 0.93 GAE/g and 96.2 ± 0.20 QE/g, respectively. The IC₅₀ value of flower extract for α-Glc inhibition with mixed (Competitive/non-competitive) mode was found to be 20.34 ± 0.11 mg/ml. Furthermore, in-vivo studies showed that the blood glucose level reduced after consumption of flower extract compared to the control group. Twenty-one compounds were identified by GC/MS technique. These compounds were assessed for high docking scores against α-Glc in silico. Docking score calculations exhibited that the DES-α-Glc complex had a significantly higher binding energy (-6.13 Kcal/mol) than other compounds. The DES-α-Glc complex which displayed a higher docking energy value than the ACR was subjected to MDs studies. The findings of this study suggest that the flower extract of D.sophia can be used as a suitable additive in syrups or foods with anti-diabetic capacity.     

Assessment on in vitro medicinal properties and chemical composition analysis of Solanum virginianum dried fruits

The study was aimed to screen the presence of phytoconstituents and determine distinct in vitro medicinal traits of aqueous and ethanolic extracts of Solanum virginianum dried fruits. Aqueous and ethanolic extract showed total phenolic content of 207.5 ± 0.16 and 268.4 ± 0.42 GAE/mg, respectively. Likewise, total flavonoid content of 50.12 ± 0.39 and 192.88 ± 0.27 QE/mg was estimated for the aqueous and ethanolic extract, respectively. In vitro antibacterial, antioxidant, α-amylase inhibition, anti-inflammatory, and anticancer attributes of extracts were assessed using standard protocols. The antibacterial traits of both the extracts were assessed against certain pathogenic bacteria which exhibited maximum zone of inhibition of 22.3 ± 0.6 mm against Staphylococcus aureus. Antioxidant tests showed not only significant scavenging of DPPH, superoxide, hydroxyl, and ABTS^●+ radicals but also estimated ferric reducing power and phosphomolybdenum reduction activities of extracts in a concentration dependent manner. The aqueous extract (54.12 ± 0.44–86.80 ± 0.27%) depicted higher rate of α-amylase inhibition than ethanolic extract (23.07 ± 0.47–81.61 ± 0.43%) at distinct concentrations. Similarly, the aqueous extract protected the haemolysis (46.19 ± 0.14–66.21 ± 0.17%) effectively as compared to the ethanolic extract (12.67 ± 0.19–38.03 ± 0.41%). The aqueous and ethanolic extract showed cytotoxicity against HepG2 cell lines in the range of 32.23 ± 0.34–54.82 ± 0.26% and 49.25 ± 0.38–73.2 ± 0.3%, respectively. Additionally, the GC–MS analysis confirmed the availability of total 15 predominant bioactive constituents in both extracts. Findings of this context indicated pronounced applications of S. virginianum fruits as future therapeutic.     

New mechanistic insights on Justicia vahlii Roth: UPLC-Q-TOF-MS and GC–MS based metabolomics,in-vivo,in-silico toxicological,antioxidant based anti-inflammatory and enzyme inhibition evaluation

Justicia vahlii Roth. (acanthaceae) is an important medicinal food plant used in pain relief and topical inflammation. The present study aimed to evaluate phytochemical composition, toxicity, anti-inflammatory, antioxidant and enzyme inhibition potential of n-butanol extract of J. vahlii (BEJv). The extract prepared through maceration was found rich in total phenolic contents (TPC) 196.08 ± 6.01 mg of Gallic acid equivalent (mg GAE/g DE) and total flavonoid contents (TFC) 59.08 ± 1.32 mg of Rutin equivalent (mg RE/g DE). The UPLC-Q-TOF-MS analysis of BEJv showed tentative identification of 87 compounds and 19 compounds were detected in GC–MS analysis. The HPLC-PDA quantification showed the presence of 14 polyphenols amongst which kaempferol (3.45 ± 0.21 µg/ mL DE) and ferulic acid (2.31 ± 1.30 µg/ mL DE) were found in highest quantity. The acute oral toxicity study revealed the safety and biocompatibility of the extract up to 3000 mg/kg in mice. There was no effect of BEJv on human normal liver cells (HL 7702) and very low cytotoxic effect on liver cancer cells (HepG2) and breast cancer cells (MCF-7). In anti-inflammatory evaluation, the BEJv treated groups showed significant inhibition (p < 0.001) of late phase carrageenan induced paw edema at 400 mg/kg and increased the levels of oxidative stress markers; catalase, superoxide dismutase (SOD) and glutathione (GSH) while decreased the inflammatory markers; interleukin-1beta (IL-β) and tumor necrosis factor alpha (TNF-α) in paw tissue of mice. BEJv displayed highest results in Ferric reducing antioxidant power (FRAP) assay 97. 21 ± 2.34 mg TE (trolox equivalent)/g DE, and highest activity 3.32 ± 0.31 mmol ACAE (acarbose equivalent)/g D.E against α-glucosidase. Docking study showed good docking score by the tested compounds against the various clinically significant enzymes. Conclusively the current study unveiled J. vahlii as novel non-toxic source with good antioxidant-mediated anti-inflammatory potential which strongly back the traditional use of the species in pain and inflammation.     

Anti sickling potential and chemical profiling of traditionally used Woodfordia fruticosa (L.) Kurz leaves

Woodfordia fruticosa (L.) Kurz is a widely used plant in traditional medicine systems. The tribal communities of Amarkantak, Madhya Pradesh (India) are using this plant for the treatment of general weakness, blood related complications like blood deficiency, blood purification and for the treatment of symptoms related to sickle cell disease (SCD). SCD is a genetic disease with life threatening complications. In the absence of any drugs without any side effects, the alternative plant based therapies that may either reduce/ reverse the sickling of the red blood cells can be safe and effective therapeutic agents. We evaluated W. fruticosa extracts for phytoconstituents, anti-oxidant and anti-inflammatory properties. Anti-sickling properties of the extracts were evaluated by estimation of reverse sickling, polymerization inhibition and osmotic fragility assays. Chemical profiling of the methanol extract was done using LC-MS analysis. Phytochemicals such as alkaloids, steroids, tannin, and saponins were present in all the extracts. Methanol extract displayed maximum reversal (66 ± 1%) of sickled Red blood Cells (RBC) and significantly inhibited Hb polymerization. The hexane and methanol extracts led to minimum hemolysis of sickled RBC in the osmotic fragility assays. Total tannin (365 ± 2.4 TAE) content was highest in acetone extract, while the total flavonoid and phenolic content (156.9 ± 2.0 QE) and (113.7 ± 0.7 GAE) were highest in methanol extract. The methanol extract displayed minimum IC₅₀ (8.1 ± 1.5) in 2, 2-diphenylpicrylhydrazyl (DPPH) while the acetone extract had minimum IC₅₀ (215.8 ± 5.7) in 2,2′-azino-bis 3-ethylbenzothiazoline-6-sulfonic acid (ABTS) assay. The hexane extract displayed maximum Ferric reducing anti-oxidant power (FRAP) value (1.5 ± 0.5 mM Fe(II)/mg dry weight) that were higher than methanol and aqueous extracts (1.45 ± 0.1, 1.45 ± 0.05 mM Fe(II)/mg dry weight). The methanol extract provided maximum RBC protection from hemolysis (73.8 ± 0.8%). Maximum Lipoxygenase (LOX) inhibition was observed by the acetone and methanol extracts at 400 μg/mL while the hexane extract displayed maximum Xanthine oxidase (XO) inhibition (57.0 ± 0.5%). LC-MS profiling of the methanol extract identified several secondary metabolites that might be responsible for the observed activities. The results validate the traditional use of W. fruticosa and present us with potential compounds for further development of novel anti sickling agents.     

Phenolic composition,antioxidant and enzyme inhibitory activities of Parkia biglobosa (Jacq.) Benth., Tithonia diversifolia (Hemsl) A. Gray,and Crossopteryx febrifuga (Afzel.) Benth

Medicinal plants from Chad grow under special climatic conditions in between the equatorial forest of Central Africa and the desert of North Africa and are understudied. Three medicinal plants from Chad (T. diversifolia, P. Biglobosa and C. Febrifuga) were evaluated for their phenolic composition, antioxidant and enzyme inhibition activities. The total phenolic composition varied from 203.19 ± 0.58 mg GAE/g DW in the ethyl acetate extract of P. biglobosa, to 56.41 ± 0.89 mg GAE/g DW in the methanol extract of C. febrifuga while the total flavonoid content varied from 51.85 ± 0.91 mg QE/g DW in the methanol extract of P. biglobosa to 08.56 ± 0.25 mg QE/g DW in the methanol extract of C. febrifuga. HPLC-DAD revealed that rutin, gallic acid and protocatechuic acid were the most abundant phenolics in T. diversifolia, P. Biglobosa and C. Febrifuga respectively. The antioxidant activity assayed by five different methods revealed very good activity especially in the DPPH^?, ABTS^?+ and CUPRAC assays where the extracts were more active than the standard compounds used. Good inhibition was exhibited against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with methanol (IC₅₀: 15.63 ± 0.72 µg/mL), ethyl acetate (IC₅₀: 16.20 ± 0.67 µg/mL) extracts of P. biglobosa, and methanol (IC₅₀: 21.53 ± 0.65 µg/mL) and ethyl acetate (IC₅₀: 30.81 ± 0.48 µg/mL) extracts of T. diversifolia showing higher inhibition than galantamine (IC₅₀: 42.20 ± 0.44 µg/mL) against BChE. Equally, good inhibition was shown on α-amylase and α-glucosidase. On the α-glucosidase, the ethyl acetate (IC₅₀ = 12.47 ± 0.61 µg/mL) and methanol extracts (IC₅₀ = 16.51 ± 0.18 µg/mL) of P. biglobosa showed higher activity compared to the standard acarbose (IC₅₀ = 17.35 ± 0.71 µg/mL) and on α-amylase, the ethyl acetate (IC₅₀ = 13.50 ± 0.90 µg/mL) and methanol (IC₅₀ = 18.12 ± 0.33 µg/mL) extracts of P. biglobosa showed higher activity compared to acarbose (IC₅₀ = 23.84 ± 0.25 µg/mL). The results indicate that these plants are good sources of antioxidant phenolics and can be used to manage oxidative stress linked illnesses such as Alzheimer’s disease and diabetes.     

In vitro wound healing properties,antioxidant activities,HPLC–ESI–MS/MS profile and phytoconstituents of the stem aqueous methanolic extract of Dracaena reflexa Lam

Column chromatography of the stem aqueous methanolic extract of Dracaena reflexa Lam. (DRSE) led to the isolation of five flavonoids, one phenolic glycoside, one triterpenoid and two steroidal saponins. Furthermore, 44 compounds were tentatively identified in the phytoconstituent profile of DRSE using HPLC–ESI–MS/MS. The antioxidant activity of DRSE was evaluated. In a DPPH radical scavenging assay, DRSE exhibited an IC₅₀ value of 311.6 ± 10.10 μg/ml compared with the IC₅₀ value of the standard Trolox (24.42 ± 0.87 μg/ml). The antioxidant activities of DRSE using ABTS assay and ferric reducing antioxidant power assay were 326.63 μm Trolox equivalents/mg extract and 208.67 μm Trolox equivalents/mg extract, respectively. The wound-healing activity of DRSE was studied by the scratch assay using Human Skin Fibroblast cells. After 24 h DRSE (at 10 and 20 μg/ml) decreased the wound width to 0.55 ± 0.37 and 0.47 ± 0.55 mm, respectively, compared with the wound width in the control cells (0.77 ± 0.17 mm). This result suggested that DRSE improved the wound-healing process by inducing the migration of fibroblasts. Moreover, a docking study was performed to evaluate the binding affinity of the identified phytoconstituents toward GSK-3β relative to the co-crystalized inhibitor and curcumin with the possible involvement of this pathway in the wound-healing activity of the extract.     

Phytochemical,Antimicrobial, Antidiabetic,Thrombolytic, anticancer Activities,and in silico studies of Ficus palmata Forssk

Ficus palmata Forssk. (Moraceae family) is medicinally valuable plant that is mostly used as folk medicine for the treatment of different diseases. Phytochemical composition was evaluated by preliminary phytochemical investigation, GCMS analysis, and total bioactive contents (TPC and TFC). The antioxidant, enzyme inhibition, antimicrobial, thrombolytic and anticancer activities were performed for biological evaluation. The extract exhibited the maximum total phenolic (49.24 ± 1.21 mg GAE/g) and total flavonoid contents (29.9 ± 1.13 mg QE/g) which may be correlated to higher antioxidant potential of extract. The GCMS investigation identified the presence of 27 phytocompounds of different classes related to aldehydes, esters of fatty acids, triterpenes, steroids, triterpenoid. The extract possessed the strong α-glucosidase (73.4 ± 4.65 %) and moderate α-amylase inhibition activity (47.1 ± 3.29 %). Significant results were observed in case of antiviral, antifungal, and antibacterial activities. F. palmata extract inhibited the growth of HepG2 cancer cells in a dose-dependent manner. The extract also exhibited moderate in vitro thrombolytic activity. In addition, the phytocompounds identified by GCMS were subjected to in silico molecular docking studies to analyze the binding affinity between phytocompounds and enzymes (α-glucosidase and α-amylase). Moreover, the best docked compounds were selected for ADMET studies which provide information about pharmacokinetics, physicochemical properties, drug-likeness, and toxicity of identified phytocompounds. The outcome of our research revealed that ethanolic extract of F. palmata possessed good antidiabetic, antimicrobial, thrombolytic and anticancer potential. This plant should be further explored to isolate the bioactive compounds for new drug development.     

Bioprospecting Dodonaea viscosa Jacq.; a traditional medicinal plant for antioxidant,cytotoxic, antidiabetic and antimicrobial potential

Purpose of studyDodonaea viscosa Jacq. is an ethnomedicinal plant that has been extensively used for the treatment of gout, rheumatism and pain. Current study was undertaken to mine its antioxidant, antimicrobial, cytotoxic and antidiabetic potential. Chromogenic assays were employed to establish plant’s multimode antioxidant profile whereas HPLC fingerprinting was performed to quantify polyphenols. Standard brine shrimp lethality, MTT and SRB assays proved its cytotoxicity potential.ResultsAmong all the extracts (flower, leaf, stem and root), maximum extract recovery (22% w/w), gallic acid equivalent total phenolic content (20.11 ± 0.11 ug GAE/mg DW), ascorbic acid equivalent total antioxidant capacity (22.5 ± 0.07 µg/mg DW) and total reducing power (31.1 ± 1.13 µg/mg DW) were recorded in the distilled water + acetone extract of leaf. The acetone extract of leaf showed maximum quercetin equivalent total flavonoid content (4.78 ± 0.13 µg/mg DW). HPLC-DAD analysis revealed significant amount of rutin, vanillic acid, coumaric acid, ferulic acid, gallic acid, syringic acid, cinnamic acid, gentisic acid, catechin, caffeic acid, apigenin and myricetin in the different plant parts. Maximum scavenging potential was exhibited by methanol + ethyl acetate stem extract (IC₅₀ = 23.8 µg/ml). The highest antibacterial potential was found in flower (85.7%) and root (71.4%) extracts. The ethanol + ethyl acetate (1:1) leaf extract showed noteworthy toxicity against brine shrimps (LC₅₀ = 95.46 µg/ml) while a notable antiproliferative activity against THP-1 (IC₅₀ = 3.4 µg/ml) and Hep G2 (IC₅₀ = 20 µg/ml) cell lines was shown by ethanol + ethyl acetate extracts (1:1) of stem and root, respectively. A moderate inhibition of α-amylase enzyme was observed in all parts of the plant.ConclusionThe results of the present study suggest D. viscosa as a potential source of antioxidant, anticancer and α-amylase inhibitory phytochemicals.     

Integration of in silico and in vitro approaches to evaluate antioxidant and anticancer properties of Tribulus terrestris extracts

Plants have been found useful in treating many human diseases caused by bacteria and viruses. The ability to synthesize compounds by plant secondary metabolism makes them an invaluable source of pharmaceutical and therapeutic products. The present study was designed to evaluate the phytochemical constituents, antioxidant, and anticancer activities of Tribulus terrestris seed extracts on HepG2 cell lines. TPC and TFC contents were 51 ± 0.7 mg GAE/g and 66.5 ± 0.4 mg QE/g, respectively. The antioxidant profile of the T. terrestris revealed that all the extracts have antioxidant potential and display the highest antiradical behavior in the pattern of methanolic > acetonic > chloroform > n-hexane, through DPPH, FRAP, OH radical scavenging, and NO radical scavenging assays. The antioxidant activity explored at the cellular level against H₂O₂-induced DNA damage showed a dose-dependent antioxidant effect of T. terrestris. Moreover, the methanolic extracts of all plant extracts showed notable thrombolytic potentials, the percentage of clot lysis accounted for T. terrestris was 33%, 27%, 17%, and 6% which indicated the significant clot lysis of methanolic and acetonic extracts in contrast to positive and negative standards. The genotoxicity was assessed through comet assay which exposed that T. terrestris at a low dose (0.5 mg/mL) is considered to be safe for effective treatment. MTT assay using HepG2 cell lines revealed that the highest tested concentration i.e., 100 μg/mL of the methanolic extract resulted in 86% cell viability compared to the control group. In silico study, from 14 selected compounds, three compounds, Heptacosane, Apiol, and Palmitic acid showed an affinity with target protein 51X0. The present findings may serve as a guideline for the standardization and validation of natural drugs containing the T. terrestris as an ingredient.     

Bioactive principles,anti-diabetic,and anti-ulcer activities of Ducrosia anethifolia Boiss leaves from the Hail region,Saudi Arabia

This work aimed to identify the bioactive constituents of Ducrosia anethifolia Boiss eaves through cold methanolic extract. The GC–MS study of cold methanolic extract showed the presence of various pharmaceutically important bioactive compounds with unique peaks at specified retention time. The significant compounds are α-linoleic acid, α-sitosterol, n-hexadecanoic acid, palmitic acid β-monoglyceride, 2-methoxy-4-vinylphenol and benzoic acid, methyl ester. The FT-IR study showed them fingerprint region at 3326.80, 2943.53, 2831.74, 1450, 1110.67 and 1020.80 cm^?1. The FT-IR study suggested the presence of glycosides, flavonoids, tannins, steroids, saponins, fatty acids and squalene. Oral administration of Ducrosia anethifolia Boiss leaves powder (DLP) (100 mg/kg body weight) was successfully reduced the blood sugar level after 14 d treatment in STZ (50 mg/kg bodyweight) induced diabetic rats significantly from 327.93 ± 24.5 to 171 0.03 ± 3.78 mg/dL. Furthermore, DLP (400 mg/kg body weight) was showed 74 ± 1.9 % inhibition of ulcer. The results of this study showed that DLP has both anti-diabetic and anti-ulcer characteristics when tested in vivo.     

Molecular docking of phenolic compounds and screening of antioxidant and antidiabetic potential of Olea europaea L. Ethanolic leaves extract

Oxidative stress has a crucial role in diabetic pathophysiology, therefore consuming naturally derived antioxidants as a remedial target. This study examines the naturally occurring antioxidant and antidiabetic of Olea europaea L. ethanolic leaves extract. Olea europaea L. leaves were macerated (OLE) by using absolute ethanol. Phytochemical and physiochemical analysis of OLE was screened using standard methods. The antioxidant effects were examined by DPPH (1, 1-diphenyl-2-picrylhydrazil) radical scavenging assay. In vitro antidiabetic was assayed by α-amylase enzyme inhibition study. Ethanolic extraction of OLE by maceration technique, 10% yield. Loss on drying, foreign organic matters and total ash value of OLE showed 2%, 0.2% and 16.5%, respectively. Phytochemical test on OLE confirmed saponin, flavonoid, glycoside, tannin, phenol and carbohydrate presences. The total phenolic and flavonoid contents of OLE is 490 mg GAE/g and 855 mg RUE/g of extract, respectively. OLE (IC₅₀ 38.37 ± 0.26 µg/ml) showed functional DPPH scavenging assay comparable to ascorbic acid (IC₅₀ 30.37 ± 0.17 µg/ml). In the alpha-amylase inhibitory activity, Acarbose showed an IC₅₀ value of 20.06 ± 0.19 µg/ml, while OLE portrayed an IC₅₀ value of 37.99 ± 0.15 µg/ml. The kinetic studies revealed that all samples at high concentrations reacted within a very short time, and a steady state was reached almost immediately. The lowest concentration showed slow kinetic behaviour implied longer periods before the constant state was reached. Molecular docking studies evidenced that most of the phenolic compounds of OLE interact with the active site of Human pancreatic α-amylase through the hydrogen bonding and hydrophobic interaction confirming the alpha-amylase inhibitory effect. The results suggest that Olea europaea L. has been a conceivable natural bioactive source as an antioxidant and an antidiabetic agent.     

Metabolic variations in seaweed,Sargassum polycystum samples subjected to different drying methods via 1H NMR-based metabolomics and their bioactivity in diverse solvent extracts

Seaweeds are known as excellent sources of unique bioactive metabolites. In the present study, proton nuclear magnetic resonance (¹H NMR) combined with principal component analysis (PCA) was used to distinguish the metabolic variations in Brown seaweed, Sargassum polycystum treated under different drying processes. The study also evaluated the phytochemistry, antioxidant, and antimicrobial effects of S. polycystum extracted in different solvents. Mutually under the different drying processes investigated, a total of 12 metabolites were identified from ¹H NMR analysis. Freeze drying emerged as the most efficient process that preserved most of the potentially beneficial metabolites in the samples. The results of the qualitative phytochemical screening of differentially dried S. polycystum extracts revealed the presence of various secondary metabolites. The 70% ethanol extract exhibited the highest total phenolic (627 ± 50.81 mg GAE/100 g dried samples) and also displayed the highest DPPH scavenging activity (61.4 ± 0.171%) at the highest concentration (3 mg ml⁻¹) tested. Methanol extract on the other hand contained the highest total antioxidant capacity (121.00 ± 0.003 mmol/g) followed by 70% ethanol extract (120.00 ± 0.001 mmol/g) at concentration of 1.25 mg/mL. The 70% ethanol extract also showed inhibition zone towards all bacteria samples tested compared to others solvent extracts. Based on these results, the identification of metabolites variations using PCA is considered as very useful procedure as a basis to recommend the most efficient processing (drying) method. The potential utilization of the tested Brown seaweed S. polycystum species as a source of antioxidants and antibacterial agents were also highlighted. The commercial cultivation of the species therefore, needs to be encouraged and promoted.     

Chitosan-polyvinyl alcohol membranes with improved antibacterial properties contained Calotropis procera extract as a robust wound healing agent

Due to excessive use of antibiotics, resistance against microorganisms is developed. An alternative use of antibiotics, natural remedies from plants have been used against infectious diseases. In the current study, bioactive compounds from Calotropis procera (C. procera) root were extracted and chitosan and polyvinyl alcohol (CS-PVA) were used asa carriers and for the delivery to treat induced infection. Different concentration of C. procera extracts (25–75 mg/mL) were loaded on CS-PVA membrane and applied on the induced wounds in rabbits. Wound reduction was recorded for 12 days. On 6th day, small tissue from healing area were collected and subject to histopathology for tissue regeneration. The antioxidant activity (DPPH, TPC and TFC) was also investigated of CS-PVA loaded C. procera root extract. The DPPH free radical inhibition for 75 mg/mL were recorded up to 66.37%. The TPC and TFC contents were recorded to be 36.52 ± 5.12 GAE mg/g of DW (dry weight) and 24.49 ± 6.27 CE mg/g of DW (dry weight), respectively. The antibacterial activity was evaluated against Escherichia coli and Staphylococcus aureus in comparison to control (Rifampicin). The zones of inhibition were recorded to be 18.50 ± 2.30 and 20.40 ± 4.20, respectively for CS-PVA membrane loaded with 75 mg extracts along with Rifampicin 28.50 ± 2.5 and 30.50 ± 1.38. The CS-PVA membranes were also studied for swelling and biodegradability. The biodegradability was increased, while swelling was decreased of CS-PVA membranes loaded with extract. The bioactive compounds from the CS-PVA loaded with extract released in controlled and sustainable way. Result revealed that CS-PVA loaded C. procera root extract has promising antimicrobial and antioxidant activity and could possibly be employed for the treatment of infectious diseases.     

Green and highly extraction of phenolic compounds and antioxidant capacity from kinkeliba (Combretum micranthum G. Don) by natural deep eutectic solvents (NADESs) using maceration,ultrasound-assisted extraction and homogenate-assisted extraction

Kinkeliba (C. micranthum) is a tropical plant widely used for its tremendous phytochemicals and biological activities. In the present study, three green carboxylic acid-based natural deep eutectic solvents (NADESs) were used to assess the extraction of phenolic compounds in terms of total phenolic content (TPC), total flavonoid content (TFC), individual phenolic compounds and antioxidant capacity (DPPH and FRAP assays) from dried C. micranthum leaves. For the synthesis of NADESs choline chloride was used as hydrogen bond acceptors (HBA) in combination with lactic acid (ChLa), acetic acid (ChAa) and tartaric acid (ChTa) as hydrogen bond donors (HBDs). The conventional solvents including distilled water, pure methanol and pure ethanol were used for comparison. Three extraction methods including maceration extraction (ME), homogenate-assisted extraction (HAE) and ultrasound-assisted extraction (UAE) were tested to determine the best extraction conditions. The solvents combined with the extraction methods were successfully applied for the recovery of phenolic compounds from C. micranthum leaves. ChLa exhibited the highest performance giving the TPC (21.12 ± 0.13–23.62 ± 0.58 mg GAE/g, followed by ChAc (15.49 ± 0.13–18.85 ± 0.39 mg GAE/g), water (17.08 ± 0.32–18.13 ± 0.13 mg GAE/g), ChTa (14.49 ± 0.26–17.44 ± 0.19 mg GAE/g), methanol (7.46 ± 0.45–11.64 ± 0.32 mg GAE/g) and ethanol (2.88 ± 0.39–4.60 ± 0.39 mg GAE/g), respectively. For TFC, ChLa (4.38 ± 0.09–5.01 ± 0.09 mg ECE/g) was the most prominent solvent, followed by ChAc (2.84 ± 0.04–5.01 ± 0.36 mg ECE/g), methanol (1.93 ± 053–4.85 ± 0.04 mg ECE/g), ethanol (1.49 ± 0.36–4.16 ± 0.04 mg ECE/g), ChTa (1.09 ± 0.04–3.22 ± 0.13 mg ECE/g) and water (1.15 ± 0.04–1.37 ± 0.44 mg ECE/g), respectively. The acidic NADESs especially ChLa and ChAa exhibited the best efficiencies compared to the conventional solvents. Furthermore, UAE and HAE provided good extraction efficiency in a short extraction time (30 min) in terms of the TPC, TFC, individual phenolic compounds and the antioxidant capacity compared to ME which gave a similar yield with 12 h of extraction time. Principal component analysis (PCA) showed that C. micranthum extracts could clearly be discriminated in terms of phytochemical compounds and antioxidant capacity and UAE, HAE or ME combined with ChLa ChAc or ChTa were the best choices to higher extraction efficiency.