Simultaneous optimization of extraction and antioxidant activity from Blumea laciniata and the protective effect on Hela cells against oxidative damage

Blumea was the resource for medicine such as l-borneol showing a great economic value. Interestingly, Blumea laciniata was widely used as a folk medicine in south of China and Asia. But the chemical compounds and specific pharmacological activity were rarely reported. Therefore, in this present work, the chemical components from B. laciniata were determined and the antioxidant ability on scavenging radicals and the protection on Hela cells against H₂O₂ were evaluated. The results showed the antioxidant ability was associated with the presence of polyphenols via response surface method. Additionally, chlorogenic acid, isoorientin, rutin, luteolin-4′-O-glucoside and cinnamic acid were firstly identified in B. laciniata. Moreover, the extract from B. laciniata (EBL) showed a strong antioxidant on clearing DPPH and ABTS free radicals with a lower EC₅₀. Besides, EBL showed no toxicity on Hela cells and even could protect cells from H₂O₂ induced damage by sharply reducing the excessive reactive oxygen species, improving the mitochondrial membrane potential and then decreasing the generation of cell apoptosis. These outcomes could provide a promising understanding on the potential antioxidant.     

Rhamnus pallasii subsp. sintenisii fruit,leaf, bark and root: Phytochemical profiles and biological activities

The genus Rhamnus has received a lot of interest as a source of phenolic chemicals. There have been no reports on the phytochemicals and biological activities of R. pallasii subsp. sintenisii various morphological components (fruit, leaf, bark, and root) in Iran to yet. Two crude ether petroleum (EP) and hydro-methanolic (HM) extracts were obtained from the separate parts. The antioxidant and antibacterial capabilities of the extracts, as well as their phytochemical screening (total phenolic, flavonoid, phenolic acid, and anthocyanin concentrations), were measured. Furthermore, the phytochemical profiles of EP and HM extracts were determined using GC–MS and LC-ESI–MS, respectively. LC-ESI-MS detected 59 chemicals in HM extracts, including flavonoids (62.71 %), phenolic acids (10.16 %), and anthraquinones (16.94 %). Furthermore, the predominant group components in EP extracts examined by GC–MS were fatty acids (58.82%), phenolic compounds (49.28%), and hydrocarbons (35.15 to 59.45 %). In terms of biological testing (DPPH radical scavenging and anti-bacterial activity), all examined extracts, particularly the fruit, had the highest activities in both assays (IC₅₀: 7.52 to 22.39 µg/ml and MIC: 0.39 to 3.12 mg/ml), owing to their high phenolic content. As a result, individual morphological elements of the species might be thought of as natural antioxidant and antibacterial agents.     

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.     

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.     

UPLC-ESI-QTOF-MS phenolic compounds identification and quantification from ethanolic extract of Myrtus communis ‘Variegatha’: In vitro antioxidant and antidiabetic potentials

Global public health is seriously threatened by diabetes and its complications. Although several synthetic drugs are currently employed for managing diabetes, however, the adverse effects associated with their use cannot be underestimated. Thus, the quest for a safe and cost-effective alternative is highly imperative. In the present study, the phenolic contents, antioxidant, antidiabetic, and cytotoxic potentials of 70% ethanolic crude extract of Myrtus communis ‘Variegatha’ were investigated using in vitro biochemical protocols. The total polyphenols content was 116.44 mg GAE/g, flavonols (6.74 mg QE/g), flavanols (2.46 mg CE/g) and the ferric reducing antioxidant power (FRAP) value was 1267.28 µmol AAE/g, 2,2-diphenyl-1-picrylhydrazyl (DPPH) (1165.37 µmol TE/g), and Trolox equivalent antioxidant capacity (TEAC) (775.52 µmol TE/g). High-resolution ultra-performance liquid chromatography coupled with electrospray ionisation/quadrupole-time-of-flight-mass spectrometry (UPLC-ESI-QTOF-MS) was explored to identify the phenolic compounds, most of which were flavonoids. The extract demonstrated a strong α-glucosidase inhibition potential in a concentration-dependent manner with IC₅₀ (3.159 µg/mL), which was higher than epigallocatechin gallate (EGCG) (6.208 µg/mL), a positive control antidiabetic drug. A slight increase in glucose utilization was observed after 24 h of treatment in C3A hepatocytes at 25 μg/mL whereas an increase in glucose uptake was recorded at 25 and 50 μg/mL. The extract exhibited a cytotoxic effect (IC₅₀ 76.85 µg/mL) against C3A hepatocytes at 100 µg/mL, which correlates to the glucose utilization and uptake recorded. The findings from the study show the prospect of M. communis ‘Variegatha’ as a promising source of bioactive compounds that could be used in the development of new anti-diabetic agents, thus, further research into the plant is recommended.     

N-Hydroxypyridone alkaloids,chromone derivatives,and tetrahydroxanthones from the scale-insect pathogenic fungus Orbiocrella sp. BCC 33248

Six new compounds, an N-hydroxypyridone glucoside, orbiocrellin A (1), its aglycone orbiocrellin B (2), chromone glucosides 3 and 4, a dihydrochromone 5a/5b, and a chromone 6, were isolated from the scale-insect pathogenic fungus Orbiocrella sp. BCC 33248. Orbiocrellin A (1) exhibited antimalarial activity against Plasmodium falciparum K1 (IC₅₀ 3.1 μg/mL) while it was non-cytotoxic. In contrast, orbiocrellin B (2) showed both antimalarial (IC₅₀ 2.1 μg/mL) and cytotoxic (NCI-H187 cells, IC₅₀ 0.70 μg/mL) activities.     

Phytochemical and Biological Characterization of Tephrosia nubica Boiss. Growing in Saudi Arabia

The chloroform (TNC), ethyl acetate (TNE) and n-butanol (TNB) fractions of Tephrosia nubica Bioss. growing in Saudi Arabia were investigated for the first time using UPLC-ESI-MS/MS in two ionization modes. The analysis revealed the tentative identification of 107 compounds. Moreover, the therapeutic potential of T. nubica fractions was determined by in vitro evaluation of their cytotoxic, antioxidant, and anti-obesity activities using MTT assay, DPPH radical scavenging activity and pancreatic lipase inhibitory assay, respectively. The results showed that TNE, TNB, TNC fractions revealed weak antioxidant activity with SC₅₀ 139.9 ± 0.8, 144.9 ± 1.5, 148.9 ± 1.3 µg/mL, respectively compared to ascorbic acid 14.2 ± 0.5 µg/ml. Moreover TNE, TNC fractions showed more significant cytotoxic activity against HepG-2 with IC₅₀ 82.1 ± 3.1, 101 ± 2.8 µg/mL and MCF-7 with IC₅₀ 114 ± 3.2, 124 ± 3.9 µg/mL respectively. The TNB fraction showed weak cytotoxic activity against both cell lines compared to the other fractions. Ultimately, TNE fraction showed a remarkable anti-obesity activity with IC₅₀ 62.4 ± 1.5 µg/mL compared to chloroform fraction with IC₅₀ 535.6 ± 2.1 µg/mL and n-butanol fraction which did not show any activity. In conclusion, these findings represent the first insights into the phytochemical constituents and pharmacological properties of T. nubica. The ethyl acetate fraction of T. nubica might be a promising source of functional constituents with antioxidant, cytotoxic and anti-obesity potentials. It might be a natural alternative therapy and nutritional strategy, for obesity treatment without dangerous side effects. Isolation of the bioactive compounds from the ethyl acetate fraction of T. nubica and evaluating their biological activities are recommended.     

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.     

Chemical constituents,antioxidant and hepatoprotective properties of ethanol extract from Artemisia japonica Thumb. Leaves

The tender leaves of Artemisia japonica Thumb. are often used as vegetables and tea in China. They also used as a traditional Chinese medicine for the treatment of liver disease. However, the identity of components responsible for health benefits remains unclear. The present study aimed to investigate the antioxidant and hepatic protective effects of a 60 % ethanol extract of Artemisia japonica Thumb. leaves (AJLEE). Total phenol content of AJLEE was determined using Folin Ciocalteau Method and it was calculated to be 123.142 ± 8.441 mg GAE/g. AJLEE shows remarkable antioxidant activity in vitro; pretreatment at 150 µg/mL can almost completely eliminate H₂O₂-induced ALM12 cell death. Moreover, AJLEE at a dosage of 400 mg/kg exhibits a strong hepatic protective effect against α-naphthylisothiocyanate (ANIT)-induced liver injury though the upregulation of genes for the antioxidant enzymes Sod1, Cat, Gpx4 and Ho-1, while decreasing the level of MDA. These properties of AJLEE may be attributed to the existence of abundant phenolic acids, flavonoids and coumarins, identified by UPLC/QTOF-MS as chlorogenic acid, isochlorogenic acid A, 7-methoxycoumarin and quercetin, apigenin and luteolin glycoside derivatives. Our data support the use of Artemisia japonica leaves as functional tea and food additives to improve human health.     

One-pot multicomponent synthesis of novel 3, 4-dihydro-3-methyl-2(1H)-quinazolinone derivatives and their biological evaluation as potential antioxidants,enzyme inhibitors,antimicrobials, cytotoxic and anti-inflammatory agents

A series of novel 3, 4-dihydro-3-methyl-2(1H)-quinazolinone derivatives with substituted amine moieties (1–13) and substituted aldehyde (S) were designed and synthesized by a reflux condensation reaction in the presence of an acid catalyst to get N-Mannich bases. Mannich bases were evaluated pharmacologically for their antioxidant, α-amylase enzyme inhibition, antimicrobial, cell cytotoxicity and anti-inflammatory activities. Most of the compounds exhibited potent activities against these bioassays. Among them, SH1 and SH13 showed potent antioxidant activity against DPPH free radical at IC₅₀ of 9.94 ± 0.16 µg/mL and 11.68 ± 0.32 µg/mL, respectively. SH7, SH10 and SH13 showed significant results in TAC and TRP antioxidant assays, comparable to that of ascorbic acid. SH2 and SH3 showed potent activity in inhibiting α-amylase enzyme at IC₅₀ of 10.17 ± 0.23 µg/mL and 9.48 ± 0.17 µg/mL, respectively, when compared with acarbose (13.52 ± 0.19 µg/mL). SH7 was the most active against gram-positive and gram-negative bacterial strains, SH13 being the most potent against P. aeruginosa by inhibiting its growth up to 80% (MIC = 11.11 µg/mL). SH4, SH5 and SH6 exhibited significant activity against some fungal strains. Among the thirteen synthesized compounds (SH1-SH13), four were screened out based on the results of brine shrimp lethality assay (LD₅₀) and cell cytotoxicity assay (IC₅₀), to determine their anti-cancer potential against Hep-G2 cells. The study was conducted for 24, 48, and 72 h. SH12 showed potent results at IC₅₀ of 6.48 µM at 72 h when compared with cisplatin (2.56 µM). An in vitro nitric oxide (NO) assay was performed to shortlist compounds for in vivo anti-inflammatory assay. Among shortlisted compounds, SH13 exhibited potent anti-inflammatory activity by decreasing the paw thickness to the maximum compared to the standard, acetylsalicylic acid (ASA).     

Comparative Study of the Chemical Compositions and Antioxidant Activities of Fresh Juices from Romanian Cucurbitaceae Varieties

Cucurbitaceae is a family of health-promoting plants due to their compounds with beneficial effects. The aim of this study was to analyze, for the first time, the chemical composition, the antioxidant activity and the metal chelating properties of fruit juices obtained from four different species of the Cucurbitaceae family cultivated in Romania, namely Momordica charantia, Cucumis metuliferus, Benincasa hispida and Trichosanthes cucumerina. The samples of juice were analyzed by high-performance liquid chromatography (HPLC) and all the four species displayed high levels of the two triterpenes, oleanolic and ursolic acids, and also in phenolic compounds, including catechin, (−)-epicatechin and gallic acid. The juices demonstrated significant antioxidant activity against the free radical 2,2-diphenyl-1-picrylhydrazyl (ranging from 20 to 95%,), a good iron binding ability (ranging from 7.45 ± 0.28% to 86.95 ± 0.97%) and also promising antioxidant potential against the ABTS radical (ranging from 4.97 to 32.60 μETx/mL juice). Our findings raise interesting questions for further research on Cucurbitaceae fruit juices and, consequently, their very good antioxidant potential suggests these fruits should be further explored for their protective effect against oxidative damage. This is the first time the chemical composition and antioxidant activities of fruit juices from these four Romanian Cucurbitaceae varieties have been investigated.     

Comparative analysis of phytochemical profile,antioxidant and anti-inflammatory activity from Hibiscus manihot L. flower

Hibiscus manihot L. is a kind of healthy plant with edible value and health benefits, which possesses multiple pharmacological activities that are closely related to antioxidant and anti-inflammatory activities. The dynamic changes of main active components and biological activities in Hibiscus manihot L. flower (HMLF) during its flowering period were systematically studied to determine the appropriate harvest time. Chemopreventive efficacies of the investigated HMLF extracts, by means of their anti-inflammatory and antioxidant activities, were assessed. The sample harvested on early August had the supreme total flavonoid content, total phenolic content and the strongest antioxidant activity (DPPH radical scavenging activity (IC₅₀ 0.160 mg/mL), ABTS radical scavenging activity (1.570 mmol/g Trolox), reducing power (IC₅₀ 0.101 mg/mL) and FRAP (3.644 mmol FeSO₄/g)). The results of principal component analysis indicated that the primary active components included hyperin, isoquercetin, hibifolin and quercetin-3′-O-glucoside, which were strongly associated with the antioxidant activity in the early August sample, while neochlorogenic acid, chlorogenic acid and caffeic acid were associated with the anti-inflammatory activity. The extracts significantly inhibited lipopolysaccharide-induced nitric oxide production in RAW264.7 cells, especially the samples harvested around August, which was only 3.569 μΜ with the inhibition ratio of>50%. This study indicated that HMLF harvested on the early August possessed the highest antioxidant and anti-inflammatory potential and could be used as high bioactive resources for healthy production.     

Chemical variability and antioxidant activity of Cedrus atlantica Manetti essential oils isolated from wood tar and sawdust

The present research was devoted to evaluating the effect of provenance and wood pyrolysis process on the phytochemical and antioxidant activity of essential oils extracted from sawdust and tar of Cedrus atlantica Manetti of Morocco. The essential oils were obtained by hydro-distillation from Cedar wood growing in two geographical locations of the Middle Atlas of Morocco (Senoual and Itzer forests) using a Clevenger-type apparatus and analyzed by Gas Chromatography-Mass spectrometry (GC/MS). Seventy compounds were approximately identified for each essential oil, accounting for 94% of the total oil’s composition, with the predominance of sesquiterpene hydrocarbons, where, α-himachalene (13.75%, 1.15%, 12.2%, and 16.69%) and β-himachalene (24.05%, 24.25%, 27.67%, and 44.23%) represented the major constituents in the four essential oils obtained. Multivariate analysis was used to discriminate the essential oils using principal component analysis (PCA) and Hierarchical Clustering Analysis (HCA). In addition, heatmap for dendrogram was used to investigate any correlation between the chemical profiles of each essential oil. Moreover, the antioxidant properties of the essential oils were studied using DPPH scavenging and Ferric Ion Reducing Power (FRAP). The results indicate that the essential oils from wood tar of Cedrus atlantica possess a strong antioxidant activity (IC₅₀ = 0.126 mg/mL and 0.143 mg/mL) in comparison with those from sawdust (IC₅₀ = 15.6 mg/mL and 16.3 mg/mL).     

Fractionation and purification of antioxidant peptides from Chinese sturgeon (Acipenser sinensis) protein hydrolysates prepared using papain and alcalase 2.4L

Protein hydrolysates have the potential to be natural and safer sources of bioactive peptides. In this study, two proteases were used to hydrolyze Chinese sturgeon (Acipenser sinensis) protein, and the hydrolysates were then purified to yield antioxidant peptides. The degree of hydrolysis of 23.56 % and 18.14 % was obtained using papain and alcalase 2.4L, respectivly, and hydrolysates had 96.80 % and 87.24 % total amino acid content, respectivly. The papain hydrolysate (PH) and alcalase 2.4L hydrolysate (AH) showed good antioxidant activity against DPPH^? (IC₅₀ of 3.64 and 3.15 mg/mL) and ABTS^?+ (IC₅₀ of 1.92 and 1.58 mg/mL), respectively. The low-molecular-weight (<1000 Da) fraction of both hydrolysates demonstrated the highest antiradical activity (IC₅₀ of 2.59 and 2.31 mg/mL, DPPH) and (IC₅₀ of 1.54 and 1.36 mg/mL, ABTS), respectively. Nine peptides were separated from both hydrolysates using reverse phase high performance liquid chromatography (RP-HPLC). The IC₅₀ for ABTS^?+ scavenging activity of peptide P5 with valine, glycine and asparagine (MW of 282.13 Da) from PH, and peptide P3 with histidine, glycine and alanine (MW of 302.74 Da) from AH was 0.89 and 0.72 mg/mL, respectively. The fractions and purified peptides obtained from Chinese sturgeon hydrolysates could be utilized as natural antioxidant substitutes in pharmaceuticals and food products.     

Bioactive compounds,anti-inflammatory,anti-nociceptive and antioxidant potentials of ethanolic leaf fraction of Sida linifolia L. (Malvaceae)

This study investigated the bioactive compounds, anti-inflammatory, anti-nociceptive, and antioxidant properties of the ethanolic leaf fraction of Sida linifolia (ELFSL). The in vitro anti-inflammatory study employed membrane stabilization, phospholipase A2, platelet aggregation, albumin denaturation, and protease inhibition assays. Intraperitoneal injection of freshly prepared carrageenan solution (0.1 mL of 0.01 g/mL), undiluted egg albumin (0.1 mL), acetic acid (0.6 % (v/v) (10 mL/kg bw), and formalin solution (0.02 mL of 1 % v/v) into mice hind paw, were used to evaluate the anti-inflammatory and anti-nociceptive mechanisms, respectively. In vitro antioxidant potentials were determined using 1,1-Diphenyl-2-picryl-hydrazyl (DPPH), nitric oxide (NO), ferric reducing power (FRAP), and total antioxidant capacity (TAC) assays. Varying quantities of flavonoids, phenols, tannins, saponins, terpenoids, steroids, and alkaloids, were detected in the fraction. GC-FID phytochemical profiling of ELFSL revealed a high level of epicatechin, moderate levels of catechin, kaempferol, flavone, naringenin, rutin flavanones, tannins, sapogenins, proanthocyanidin, and steroids, and small amounts of sparteine, resveratrol, and lunamarine. The ELFSL exerted excellent dose-dependent in vitro anti-inflammatory activities comparable with standard drugs (aspirin/prednisolone). The LD₅₀ test showed safety up to 5000 mg/kg body weight (per oral) ELFSL. Interestingly, mice pre-administered various doses (200, 400, 600 mg/kg bw, po) of ELFSL showed significant (P < 0.05) reduction in edema, writhing, and time spent licking paw in all phases compared with control and were at par with 100 mg/kg bw (po) aspirin. The result also registered good concentration-dependent antioxidant potentials for ELFSL and was comparable to standards (gallic acid, butylated hydroxytoluene, and ascorbic acid). These imply that ELFSL possesses excellent antioxidant, anti-inflammatory, and anti-nociceptive potentials mediated by peripheral and central mechanisms.     

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.     

Antioxidant and α-Glucosidase Inhibitory Compounds of Centella Asiatica

Centella asiatica, as known as Pegagan was previously reported to have anti-hyperglycemic effects in animal diabetic model rats. However, its α-glucosidase activity in vitro assay not yet reported. Our goal in this study is to isolate and identify active compounds as α-glucosidase inhibitor and antioxidant from aqueous ethanol 70% (v/v) extract of C. asiatica. The extract was partitioned by n-hexane, EtOAc, and n-butanol sequentially. Among the fractions tested, EtOAc fraction was showed the highest antioxidant and α-glucosidase inhibitory activities with an IC₅₀ values of 45.42 and 73.17 μg/mL, respectively. The antioxidant activity was conducted by determination of DPPH radical scavenging activity, whereas α-glucosidase inhibitory activity was determined against yeast α-glucosidase. Furthermore, isolation of the ethyl acetate extract yielded two active compounds, which were identified as kaempferol (1) and quercetin (2). Both of the compounds showed good yeast α-glucosidase inhibitory activity with IC₅₀ values of 16.50 and 21.61 μg/mL, respectively. In addition those compounds also could scavenge DPPH radical activity with IC₅₀ values of 9.64 and 11.97 μg/mL, respectively. Due to its ability in reducing α-glucosidase activity and scavenging free radical activity, the C. asiatica appears to be a potential as a good resource for future development of antioxidant and antidiabetic drug.     

LC-MS characterization of bioactive metabolites from two Yemeni Aloe spp. with antioxidant and antidiabetic properties

Two Yemeni Aloe(s) have been investigated; the resin from A. perry Baker (APR, Socotran Aloe), and the gel from A. vera (AVG, Saber Yamaniis). LC-MS for APR identified aloin B, aloinoside B/A, homonataloin B and microdontin B/A as the major components, constituting 67.7% w/w of the extract. AVG showed the same pattern of anthrones (19.5% w/w), in addition to the chromones aloesin, aloeresin A, aloeresin D and aloeresin E. Dihydro-isocoumarin glucoside was identified in both Aloe species. Aloe extracts showed high antioxidant activity: DPPH (0.09 & 0.05 mM/g TE), ABTS (0.06 & 0.03 mM/g TE), and FRAP (20.5 & 15.5 mM Fe⁺²E), for APR & AVG, respectively. The antidiabetic properties was evaluated through inhibition of α-glucosidase enzyme. APR showed inhibitory activity with IC₅₀ 0.76 μg/mL higher than AVG (IC₅₀ 0.76 mg/mL). Aloin A showed the highest inhibitory activity with IC₅₀ 0.34 mg/mL that was higher than acarbose (0.54 mg/mL) the positive control, indicating that the activity of Aloe extract is linked to the aloin and other anthrone compounds. These findings highlight the phytochemical profile, antioxidant and potential antidiabetic activity of the Yemeni Aloe species and draw attention to their potential application in food, medicine and cosmetic products.     

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.     

The potential antioxidant ability of hydroxytyrosol on Caenorhabditis elegans against oxidative damage via the insulin signaling pathway

Hydroxytyrosol (HY) deriving from olive leaves is a phenolic component which has been proven to possess a strong antioxidant ability. However, the underling mechanism is still unclear. To evaluate the antioxidant ability of HY comprehensively, assays in vitro and in vivo (Caenorhabditis elegans (C. elegans) was used as a model organism) were conducted. The results showed HY could scavenge 2,2-Diphenyl-1-picryl-hydrazyl (DPPH) radicals with a strong total reducing power. Pretreated with HY for 48 h, the cell viability of Chinese hamster ovary (CHO) cells was enhanced under oxidative stress by reducing the level of reactive oxygen species (ROS) and malondialdehyde (MDA). A suitable concentration of HY showed no side effects on the development, fertility, and movement of C. elegans. With the treatment of HY, the survival was enhanced by 15.79% under thermal stress. The ROS and MDA contents were also reduced, which might be associated with the increasing abilities of antioxidant enzymes such as superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) and the heat shock protein HSP-16.2. Nuclear localization of DAF-16 was greatly increased after treated with HY. More outcomes demonstrated HY exhibited an excellent antioxidant capacity via the insulin signaling pathway by upregulating daf-16 and sod-3 and downregulating the genes of age-1 and daf-2.