N-butanol Extract Research Articles

Activation of the Keap1-Nrf2 pathway by specioside and the n-butanol extract from the inner bark of Tabebuia rosea (Bertol) DC

Background: A large number of chemical compounds exert their antioxidant effects by activation of key transcriptional regulatory mechanisms, such as the transcription factor Nrf2. The aim of this study was to evaluate the activation of the Keap1-Nrf2 pathway by both the n-butanol extract obtained from the inner bark of Tabebuia rosea (Bertol) DC and specioside isolated from this extract. Methods: The antioxidant activity of the extract and specioside isolated from the inner bark of T. rosea were evaluated using the oxygen radical absorbance capacity (ORAC) and the 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity (DPPH) techniques, whereas their effects on the viability of HepG2 cells was determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. The effects of the compound and the extract on activating the Keap1-Nrf2 pathway were evaluated using a Nrf2 Transcription Factor Assay kit. Induction of the Nrf2-mediated antioxidant response genes HMOX-1 and NQO1 was evaluated by real-time PCR. The protective effects against H 2O 2-induced oxidative stress in HepG2 cells was determined as the percent protection using the MTT method. Results: Both the n-butanol extract and specioside exhibited activity at low concentrations without affecting cellular viability, since the cell viability was greater than 80% after 24 hours of exposure at each tested concentration. In addition, Nrf2 dissociated from Keap1 after treatment with the n-butanol extract at a concentration of 0.25 µg/mL after 4 hours of exposure. An increase in the Nrf2 level in the cytoplasm after 4 hours of exposure to 2 μM specioside was observed. Nrf2 levels stabilized in the nucleus 12 hours after stimulation with both specioside and the extract. After 6 hours of stimulation, both the extract and specioside induced the expression of HMOX-1 and NQO1. Conclusion: The n-butanol extract from the inner bark of T. rosea and specioside produced protective effects against H 2O 2-induced oxidative stress in HepG2 cells.

Antioxidant Activity of the Extracts from Tussilago farfara

Objective: The antioxidative properties of Chinese medicine Tussilago farfara were determined by spectrophotometry. Methods: The anti-oxidation activity of petroleum ether, ethyl acetate and n-butanol extracts from ethanol extract of Tussilago farfar were studied, using DPPH free radical scavenging, hydroxyl radical scavenging, and total reducing power determination. Results: Compared with the Vc activity of the positive control, the extracts of ethyl acetate part and the n-butanol part showed significant antioxidant activity, and the antioxidant activity in the ethyl acetate part was higher than Vc. Conclusion: Antioxidant activity of ethyl acetate extract is better than vitamin C, N-butanol extract also has obvious antioxidant activities.

Activation of the Keap1-Nrf2 pathway by specioside and the n-butanol extract from the inner bark of Tabebuia rosea (Bertol) DC.

Background: A large number of chemical compounds exert their antioxidant effects by activation of key transcriptional regulatory mechanisms, such as the transcription factor Nrf2. The aim of this study was to evaluate the activation of the Keap1-Nrf2 pathway by both the n-butanol extract obtained from the inner bark of Tabebuia rosea (Bertol) DC and specioside isolated from this extract. Methods: The antioxidant activity of the extract and specioside isolated from the inner bark of T. rosea were evaluated using the oxygen radical absorbance capacity (ORAC) and the 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity (DPPH) techniques, whereas their effects on the viability of HepG2 cells was determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. The effects of the compound and the extract on activating the Keap1-Nrf2 pathway were evaluated using a Nrf2 Transcription Factor Assay kit. Induction of the Nrf2-mediated antioxidant response genes HMOX-1 and NQO1 was evaluated by real-time PCR. The protective effects against H 2O 2-induced oxidative stress in HepG2 cells was determined as the percent protection using the MTT method. Results: Both the n-butanol extract and specioside exhibited activity at low concentrations without affecting cellular viability, since the cell viability was greater than 80% after 24 hours of exposure at each tested concentration. In addition, Nrf2 dissociated from Keap1 after treatment with the n-butanol extract at a concentration of 0.25 µg/mL after 4 hours of exposure. An increase in the Nrf2 level in the cytoplasm after 4 hours of exposure to 2 μM specioside was observed. Nrf2 levels stabilized in the nucleus 12 hours after stimulation with both specioside and the extract. After 6 hours of stimulation, both the extract and specioside induced the expression of HMOX-1 and NQO1. Conclusion: The n-butanol extract from the inner bark of T. rosea and specioside produced protective effects against H 2O 2-induced oxidative stress in HepG2 cells.

Antiglycaemic potentials and molecular docking studies of the extracts of Cassia alata L.

BackgroundThis study assessed the antiglycaemic properties of the methanolic extracts of the dried leaf of Cassia alata L. through in vitro and in silico approaches. The methanolic crude extract (MCE) of the dried leaf was prepared and partitioned into n-butanol (BPE) and aqueous (ARE) extracts. The antiglycaemic potential was assessed in vitro by studying the inhibitory actions of the extracts with α-amylase, α-glucosidase, and sucrase. The antiglycation capacity of the extracts was evaluated through the inhibition of albumin glycation, thiol oxidation, and β-fibril formation. Previously identified compounds (emodin, quercetin, chrysoeriol, and kaempferol) were docked with α-amylase (1HNY), α-glucosidase (5ZCB), and sucrase-isomaltase (3LPO) using the Pyrex Virtual Screening tool.ResultsThe results revealed that MCE had the highest inhibitory potential with the lowest IC50 values of 69.67 ± 0.88, 65.54 ± 0.34, and 48.35 ± 1.45 μg/mL for α-amylase, α-glucosidase, and sucrase inhibitions, respectively. The molecular docking studies showed that quercetin and kaempferol had the best docking scores with 1HNY while emodin and chrysoeriol had the best scores towards 5ZCB and 3LPO. MCE and BPE significantly (p < 0.05) inhibited glucose-induced albumin glycation and modification.ConclusionThis study suggested that the extract of the leaf of C. alata could contain a mix of different phytochemicals that could be beneficial in reducing the absorption of glucose and preventing diabetes-induced complications.

Ethnomedicinal documentation and anti-inflammatory effects of n-butanol extract and of four compounds isolated from the stems of Pituranthos scoparius: An in vitro and in vivo investigation

Ethnopharmacological relevancePituranthos scoparius is a medicinal plant belonging to the Apiaceae family. It thrives in North Africa, and is widely distributed in the high plateau of most parts of the Sahara in Algeria. This plant is widely used in the Algerian traditional medicine to treat numerous infectious diseases, dermatoses, nervous breakdowns, digestive disorders, and calm abdominal pain. Aim of the studyThe aim of the present work was to examine the ethnomedicinal uses of Pituranthos scoparius in Setif region, Algeria, isolate and identify the chemical constituents of the n-butanol stem extract of P. scoparius (BEPS), and to determine the toxicity and anti-inflammatory effects of these compounds in addition to the extract. Materials and methodsThe anti-inflammatory effects of BEPS and the four compounds isolated from the extract were evaluated using the in vitro protein denaturation assay, whereas the topical anti-inflammatory activity was assessed using the croton oil-induced ear edema in mice. Toxicity was determined based on assessment of in vitro cytotoxicity using hemolytic activity against human red blood cells (RBCs). ResultsFour compounds, identified as the rare isorhamnetin-3-O-β-apiofuranosyl (1 → 2)-β glucopyranoside (2), in addition to three known compounds, namely isorhamnetin-3-O-β-glucoside (1), D-mannitol (3), and isorhamnetin-3-O-β-glucopyranosyl-(1 → 6)-β-glucopyranoside (4) were isolated from BEPS. These compounds were characterized by means of NMR and high-resolution mass spectral (HRMS) data. These four compounds were isolated for the first time from this traditional Algerian medicinal plant. Screening of the extract indicated the presence of alkaloids, polyphenols, flavonoids, free quinones, coumarins and tannins. Topical anti-inflammatory effect showed that the four isolated compounds, as well as BEPS, exhibit a significant (p < 0.05) dose-dependent (0.5 and 1 mg/ear) anti-inflammatory effect. At a dose of 1 mg/ear, compounds 1, 2, and 4, exhibited remarkable anti-inflammatory effect with a percentage inhibition of 85.50 ± 2.78, 79.78 ± 4.68, and 75.78 ± 2.98%, respectively. Results from in vitro cytotoxicity showed that the % lysis of the extract, along with isolated compounds was found to be virtually nontoxic. ConclusionsThese results suggest that BEPS and isolated compounds are safe, nontoxic, and exert remarkable anti-inflammatory effects, and can be new sources of natural anti-inflammatory agents.

Protective effects of n-Butanol extract and iridoid glycosides of Veronica ciliata Fisch. Against ANIT-induced cholestatic liver injury in mice

Ethnopharmacological relevanceVeronica ciliata Fisch. is a traditional medical herb that present in more than 100 types of Tibetan medicine prescriptions, most of which are used for liver disease therapy. Iridoid glycosides have been identified as the major active components of V.ciliata with a variety of biological activities.Aims of the study: The aim of this study is to explore the protective effect and potential mechanism of n-Butanol extract (BE) and iridoid glycosides (IG) from V.ciliata against ɑ-naphthyl isothiocyanate (ANIT)-induced hepatotoxicity and cholestasis in mice. Materials and methodsMice were intragastrically (i.g.) given BE and IG at different dose or positive control ursodeoxycholic acid (UCDA) once a day for 14 consecutive days, and were treated with ANIT to cause liver injury on day 12th. Serum levels of hepatic injury markers and cholestasis indicators, liver index and liver histopathology were measured to evaluate the effect of BE and IG on liver injury caused by ANIT. The protein levels of tumor necrosis factor-α (TNF-α), nuclear factor kappa B(NF-κB), interleukin-6 (IL-6), Na+/taurocholate cotransporting polypeptide (NTCP), bile salt export pump (BSEP), multidrug resistance-associated protein 2 (MRP2), and the levels of oxidative stress indicators in liver tissue were investigated to reveal the underlying protective mechanisms of BE and IG against ANIT-induced hepatotoxicity and cholestasis. ResultsThe n-Butanol extract (BE) and iridoid glycosides (IG) isolated from V.ciliata significantly decreased serum level of cholestatic liver injury markers aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), γ-glutamyl transferase (GGT), total bile acid (TBA), total bilirubin (TBIL), and direct bilirubin (DBIL) in ANIT-treated mice. Histopathology of the liver tissue showed that pathological damages were relieved upon BE and IG treatment. Meanwhile, the results indicated BE and IG notably restored relative liver weights, inhibited oxidative stress induced by ANIT through increasing hepatic level of superoxide dismutase (SOD), reduced glutathione (GSH), catalase (CAT) and decreasing hepatic content of malondialdehyde (MDA). Western blot revealed that BE and IG inhibited the expression of pro-inflammatory factors TGF-α, IL-6 and NF-κB. Furthermore, the decreased protein expression of bile acid transporters NTCP, BSEP, MRP2 were upregulated by BE and IG in a dose-dependent manner. ConclusionThe results have demonstrated that BE and IG exhibited a dose-dependently protective effect against ANIT-induced liver injury with acute intrahepatic cholestasis in mice, which might be related to the regulation of oxidative stress, inflammatory response and bile acid transport. In addition, these findings pointed out that iridoid glycosides as main active components of V.ciliata play a critical role in hepatoprotective effect of V.ciliata.

Uji Aktivitas Antimikroba Ekstrak n-Butanol Madu Hutan (Apis nigrocincta) dari Kabupaten Selayar dengan Metode KLT-Bioautografi

Preliminary research has been conducted on the antimicrobial activity of n-Butanol extract of forest honey (Apis nigrocincta). This study aims to determine the antimicrobial activity of forest honey from Selayar Regency on the growth of test microbes, using the method of solid dilution with the test microbial Bacillus subtilis, Staphylococcus aureus, Streptococcus mutans, Pseudomonas aeruginosa, Salmonella typhi, Escherichia coli, Vibrio sp, Staphylococcus epidermidis, and Candida albicans against n-butanol extract from forest honey (Apis nigrocincta) at 1 mg/ml. The results obtained showed that n-butanol extract inhibited the growth of bacteria Bacillus subtilis, Escherichia coli, Staphylococcus aureus, Staphylococcus epidermidis, and Staphylococcus aureus. To estimate the compounds that provide antimicrobial activity, the TLC-Bioautography test is performed. Obtained the best results from the separation of compounds by TLC using Chlorophorom eluate: Acetone (3: 1). The TLC-Bioautographic test results showed that the spots with an Rf value of 0.29 gave activity to Bacillus subtilis, Escherichia coli, and Staphylococcus epidermidis, and gave positive results on the appearance of flavonoid compounds.

Investigation of Cytotoxic Constituents from Seed Pulp of Entada Phaseoloides and Metabolite Profiling Using UPLC-QTOF-MSE

Entada phaseoloides (Linn.) Merr. (Family: Fabaceae) is a well-known, traditional, medicinal plant that has been extensively used in the Ayurvedic system of medicine for centuries to combat a wide range of ailments. The goal of this work was to investigate the bioactive constituents from n-butanol extracts of Entada. phaseoloides and develop a method for the comprehensive characterization of saponins using liquid chromatography with an electrospray ionization quadrupole time-of-flight mass spectrometer (LC-ESI-QTOF-MS). A hyphenated technique, ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS/MS), has been proposed to integrate LC and MS together with NMR for structural elucidation. This method allowed comprehensive characterization of saponin glycosides from E. phaseoloides based on their MS/MS fragmentation study. The phytochemical study of E. phaseoloides resulted in the isolation and identification of three bio-active constituents. Further, the UPLC-QTOF-MS/MS method led the structure elucidation of saponin constituents directly from crude extracts via comparison of the exact molecular masses from their MS/MS spectra. Identified common fragments m/z 648, 630, 498, 366, and 204 were used for the screening of saponin components. The present study summarizes the isolation and identification of bio-compounds from n-butanol extract and the demonstration of UPLC-QTOF-MS/MS analysis for the characterization of compounds in complex crude extracts. To the best of our knowledge, this is the first systematic study in structural characterization on complex saponins and other metabolites from crude extract of E. phaseoloides using UPLC-ESI-QTOF-MSE. Rapid analysis and characterizations of three new saponins from E. phaseoloides using UPLC-ESI-QTOF-MSE were tentatively identified based on the mass fragmentation study.

N-butanol extract of Hedyotis diffusa protects transgenic Caenorhabditis elegans from Aβ-induced toxicity.

Hedyotis diffusa Willd (Rubiaceae) is a widely used and resourceful traditional Chinese medicine that exerts protection against aging and age-related diseases. However, the underlying mechanisms of the protective effects remain largely unclear. Alzheimer's disease (AD) is an age-related neurodegenerative disease, of which β-amyloid (Aβ)-induced toxicity has been suggested as a main cause. Herein, we use the transgenic Caenorhabditis elegans CL4176, CL2006, and CL2355 strains, which express human Aβ1-42 peptide, to investigate the effects and the possible mechanisms of n-butanol extract of H.diffusa (HDB)-mediated protection against Aβ toxicity in vivo. During the experiments, a method of quality control for HDB was established by HPLC. Additionally, we examined the effects of HBD on gene expression changes with qRT-PCR, aggregation of Aβ plagues with thioflavin-S staining, and protein detection with GFP labeling. HDB improved lifespan, locomotion, and stress resistance. Further study showed that HDB decreased paralysis, the accumulation of ROS, and AChE activity. Moreover, HDB suppressed neuronal Aβ-expression-induced defects in chemotaxis behavior and increased SOD activity. HDB also downregulated the Aβ mRNA level and decreased the number of Aβ deposits. Furthermore, HDB increased the expression levels of sod-3, daf-16, hsf-1, and hsp-16.2 gene and upregulated hsp-16.2::GFP and gst-4::GFP expression. Taken together, these results suggest that HDB may protect against Aβ-induced toxicity in C. elegans via the insulin/insulin-like growth factor-1 (IGF-1) signaling pathway.

Chemical Composition, Antioxidant, and Anti-inflammatory Activities of Whole Parts of Onobrychis crista-galli (L.) Lam

Objective: The aim of the present study is to examine the phytochemical components and the biological activities of the whole parts of Onobrychis crista-galli (L.) Lam. growing in Algeria. Methods: The structures of the isolated compounds 1-15 were elucidated using different spectroscopic methods and by comparison with literature data. The biological evaluation of the plant was determined by the in vitro antioxidant and anti-inflammatory activities. The antioxidant activity of various extracts (petroleum ether, ethyl acetate, and n-butanol) and some isolated flavonoids was assessed by using five different test systems, namely, 1,1-diphenyl-2-picryl-hydrazil (DPPH), 2,2’- azinobis (3-ethylbenzothiazoline-6-sulfonic acid (ABTS), cupric reducing antioxidant capacity (CUPRAC), superoxide alkaline DMSO, and β-carotene/linoleic acid tests. In addition, the total phenolic and flavonoid contents of the extracts were determined as gallic acid and quercetin equivalents, respectively. In vitro anti-inflammatory activity by protein denaturation was measured for all extracts. Results: Phytochemical investigation of the ethyl acetate and n-butanol extracts of Onobrychis crista- galli led to the isolation for the first time of fifteen known compounds. The present study reports for the first time the isolation and identification of fifteen known compounds from this species. The ethyl acetate extract had rich phenolic content indicating (31.09 ± 0.40 mg gallic acid equivalents/g of fresh weight), while n-butanol extract displayed a high content in flavonoid compounds (60.70±0.7 mg quercetin equivalents/ g of fresh weight). This investigation indicated that the ethyl acetate extract of O. crista-galli showed the highest antioxidant activity (IC50= 17.13±0.51 μg/mL, DPPH), (IC50= 82.99±2.50 μg/mL, ABTS), and (A0.50= 94.67±0.41 μg/mL, CUPRAC), (IC50= 97.09±2.20 μg/mL, DMSO), (IC50: 36.73±1.17 μg/mL, β-carotene/linoleic acid). Furthermore, the compound luteolin 5-methyl ether (14) exhibited a good antioxidant activity in DPPH (IC50= 06.05 ± 0.15 μg /mL) and CUPRAC (A0.5= 12.57 ± 0.34 μg /mL) assays. Moreover, the ethyl acetate and nbutanol extracts of O. crista-galli evidenced a good to moderate in vitro anti-inflammatory activity. Conclusion: The extracts of the whole plant of O. crista-galli (L.) Lam. showed potent antioxidant and anti-inflammatory activities.

Anti-inflammatory activity of ethyl acetate and n-butanol extracts from Ranunculus macrophyllus Desf. and their phenolic profile

Ethnopharmacological relevanceThe members of the genus Ranunculus have counter-irritating properties and thus, they are traditionally used for treating anti-inflammatory disorders and other skin conditions. Ranunculus macrophyllus Desf. is a wild medicinal plant growing in Algeria and traditionally used to treat some cutaneous skin disorders. AimThe aim of this study was to characterize the composition of the ethyl acetate and n-butanol extracts from Ranunculus macrophyllus Desf. as well as to elucidate and to compare their effect against acute skin inflammation. Moreover, both the antioxidant activity and the acute toxicity of the plant extracts were also studied. Materials and methodsSpectrophotometric and chromatographic methods were employed to identify and quantify phenolic compounds and triterpenoids from R. macrophyllus Desf. fractions. The antioxidant activity was estimated using the phosphomolebdenum, DPPH, reducing power and β-carotene bleaching assays. The ethyl acetate and n-butanol extracts were screened for their anti-inflammatory activities using ex-vivo membrane stabilizing assays and in-vivo acute skin inflammation model. ResultsEthyl acetate fraction showed the highest amounts of total phenolic compounds (413 ± 4 μg GAE/mg extract) and triterpenoids (70.4 ± 1.8 μg UAE/mg extract). Rutin, hesperidin, myricetin and kaempferol were the major compounds identified in the different fractions. Ethyl acetate fraction exhibited strong DPPH• radical scavenging ability (IC50 1.6 ± 0.2 μg/mL), high total antioxidant capacity (447 ± 7 μg AAE/mg extract) and reducing power (514 ± 8 μg AAE/mg extract). Ethyl acetate fraction inhibited (73.4 ± 0.3) % of linoleic acid peroxidation. Ethyl acetate and n-butanol fractions did not have any visible toxicity at 2000 mg/kg and presented excellent membrane stabilizing ability. The inhibition of xylene induced ear inflammation was (38 ± 4) % and (46 ± 1) % for RM-B and RM-EA, respectively. ConclusionsThe high content of both phenolic compounds and triterpenoids combined with the remarkable anti-inflammatory effect and antioxidant activity of ethyl acetate and n-butanol extracts from R. macrophyllus Desf. support the wide spread use of this traditional plant on some skin disorders (inflammatory skin disorders).

Phytochemical screening, antimicrobial, antioxidant and cytotoxic potential of different extracts of Psidium guajava leaves

Psidium guajava (Myrtaceae) is an important food crop and medicinal plant supporting its traditional uses. The aim of the present study was to evaluate phytochemical, antimicrobial, antioxidant and cytotoxic activity of various solvent extracts of leaves of P. guajava. Phytochemical analysis revealed the presence of terpenoids, tannins, steroids, flavonoids, saponins, alkaloids and highest amount of phytocompounds was reported with methanol, ethanol and acetone extract. Total phenolic and flavonoid content was found to be highest in acetone extract (256.32 ± 4.56 mg/g GAE) and n-butanol extract (198.64 ± 1.23 mg/g RE) respectively. The antimicrobial assay revealed that acetone extract (13.5 ± 2.12 mm) exhibit maximum zone of inhibition against P. aeruginosa; while acetone (14 ± 0.71 mm) and ethanol (14.5 ± 2.12 mm) showed maximum zone of inhibition against S. aureus. Chloroform extract (10.2 ± 1.13 mm) showed maximum inhibition to the growth of C. albicans. Guava leaves also possess antioxidant activity which was evaluated in terms of % DPPH (2, 2-diphenyl-1-picrylhydrazyl) free radical scavenging activity and was found highest in acetone extract (41%). Cytotoxic activity was evaluated in terms of stimulation index using bovine lymphocytes and highest stimulation index was found with methanol extract (1.432 ± 0.193). This study revealed that acetone extract of guava leaf comprises effective antimicrobial, antioxidant and cytotoxicity and can be used for therapeutic applications.

The inhibitory effects of metabolites from Bacillus pumilus on potato virus Y and the induction of early response genes in Nicotiana tabacum

To develop a new antiviral preparation from a microbial source, the halophilic bacterium Bacillus pumilus E303035 was isolated from a soil sample collected at Qarhan Salt Lake in Qinghai, China. The inhibitory activity of an ethyl acetate extract of its fermentation broth was higher than that of an n-butanol extract. After isolation and purification, 9 compounds were obtained: cyclo(L-Leu-L-Pro) (1), cyclo(L-Pro-L-Tyr) (2), Brevianamide F (3), 2-(3-Indolyl) ethanol (4), N-[2-(1H-indol-3-yl) ethyl] acetamide (5), 3, 3-di(1H-indol-3-yl)propane-1,2-diol (6), Lincomycin B (7), dibutylphthalate (8), and p-hydroxyphenethyl alcohol (9). Compounds 1, 5, and 9 showed inhibitory activities against potato virus Y (PVY). Compounds 1, 4, and 9 had significant inhibitory activity against genes HC-pro, P3, and Nib, compound 5 against gene P3, and compounds 1 and 4 against NIa. Compounds 1, 4, 5, and 9 had significant inhibitory activity against genes VPg and 6K1. Active compounds 1, 5, and 9 had various effects on the expression of viral genes related to pathogenesis. Expression of genes cullin and XTH was up-regulated and CP was down-regulated, compared to the positive control. In conclusion, compounds 1, 5, and 9 might be considered as potential antiviral agents for future development.

Phytochemical, Antibacterial and Antioxidant Activity Evaluation of Rhodiola crenulata.

The chemical components, as well as the antibacterial and antioxidant activities of the essential oil (EO) and crude extracts prepared from Rhodiola crenulata were investigated. The essential oil was separated by hydrodistillation, and gas chromatography-mass spectrometry (GC-MS) was used to identify its constituents. A total of twenty-seven compounds was identified from the EO, and its major components were 1-octanol (42.217%), geraniol (19.914%), and 6-methyl-5-hepten-2-ol (13.151%). Solvent extraction and fractionation were applied for preparing the ethanol extract (crude extract, CE), petroleum ether extract (PE), ethyl acetate extract (EE), n-butanol extract (BE), and water extract (WE). The CE, EE and BE were abundant in phenols and flavonoids, and EE had the highest total phenol and total flavonoid contents. Gallic acid, ethyl gallate, rosavin and herbacetin were identified in the EE. The antibacterial activity results showed that the EO exhibited moderate inhibitory activity to the typical clinic bacteria, and EE exhibited the strongest antibacterial activity among the five extracts. For the compounds, ethyl gallate showed the strongest inhibitory activity to the test bacteria, and its minimum inhibitory concentration (MIC) value and minimum bactericidal concentration (MBC) value for all the tested bacteria was 0.24 mg/mL and 0.48 mg/mL, respectively. The results of antioxidant activity showed that both CE and EE exhibited strong antioxidant activities in the DPPH radical scavenging and Fe2+ reducing power tests, however, EO showed relatively weaker antioxidant ability. Ethyl gallate and rosavin exhibited excellent activity in the DPPH radical scavenging assay, and their IC50 value was 5.3 µg/mL and 5.9 µg/mL, respectively. Rosavin showed better reduction power activity than the other three compounds. These results could provide more evidence for the traditional use of R. crenulata, and would be helpful for improving its application further.

Antidiabetic effect of partitioned methanol extract of Boswellia dalzielii (Frankincense tree) in rats

Medicinal plants have been the major source of bioactive phytochemicals employed for the treatment and management of disease since time immemorial. The present study was aimed at investigating the antidiabetic potentials of various partitioned portions of crude methanol extract of Boswellia dalzielii in alloxan-induced diabetic rats. Fresh leaf of Boswellia dalzielii was air-dried, pulverized and extracted using cold maceration method with 85% methanol and concentrated to dryness. The crude methanol extract was partitioned using n-hexane, chloroform, ethylacetate and n-butanol to afford portions encoded BMENH, BMECM, BMEEA, BMENB respectively, and were screened for phytochemicals. The portions were evaluated for their anti-diabetic effects on alloxan-induced rats. The phytochemical studies of the crude methanol leaf, stem and root bark extracts revealed the presence alkaloids, cardiac glycoside, flavonoids, saponins, tannins and terpenoids. The partitioned crude methanol leaf extract yielded 14.12 % ( w/w) n-hexane, 6.85 % (w/w) chloroform, 4.18% (w/w) ethyl acetate and 36.40 % (w/w) n-butanol extracts respectively. Antidiabetic activity of fractions BMEH, BMEC, BMEE at doses of 200 and 400 mg/kg bd wt. produced significant (p&lt;0.05) % inhibitions of glycaemia of 13.51, 18.91, 53.36 and 71.21 respectively, as the highest inhibitions at 400 mg/kg bwt. compared to 52.67 % of Glibenclamide 2.0 mg. (a standard drug). Thus, the leaf of Boswellia dalzielii possesses potent antidiabetic activity which increases as the extract is purified. The anti-diabetic effect of the plant in rats may likely be due to the presence of alkaloids, flavonoids, tannins and terpenoids.

Structural characterization, antioxidant, and antibiofilm activities of Coffea canephora green seeds.

In order to explore Coffea canephora green seeds as natural extract for application in the functional-food industry, we focused this study to the evaluation of the antioxidant and the antiadhesion effect of C. canephora green seeds extracts. The analysis of C. canephora green seeds extracts was carried out by RP-HPLC-PDA. These extracts were screened for antioxidant activities by ABTS and phenanthroline assays. The antibacterial activity was determined by microdilution method against three reference bacteria. The inhibition of bacterial adhesion at 1/8 MIC was carried out against three reference bacteria. The RP-HPLC-PDA revealed the presence of gallic acid, vanillin, quercetin, chlorogenic acid, and P-coumaric acid. The n-buatnol extract have the highest activity ABTS assays (3.96±0.08μg/mL). For this extract, the A0.5 was 1.90±0.05μg/mL for phenanthroline assay. The n-butanol extract and the methanolic extract have the higher antibacterial activity against Staphylococcus aureus ATCC 25923 (40µg/mL).At MIC/8, the extracts of C. canephora showed 70% higher antidhesive activity against S. aureus ATCC 25923. Our finding provides an effective and specific new approach to the search of antioxidant and antiadhesive compounds for different uses.

Endophytic fungi from Passiflora incarnata: an antioxidant compound source.

Endophytes are considered one of the most important microbial resources for obtaining biomolecules of therapeutic use. Passiflora incarnata, widely employed by the pharmaceutical industry, shows therapeutic effects on anxiety, nervousness, constipation, dyspepsia and insomnia based on their antioxidant compounds. In this study, from 315 endophytic fungi isolated from P. incarnata leaves, 60 were selected to determinate presence of chemical constituents related with antioxidant activity, based on their production of soluble pigments. The promising fungi were evaluated specifically on their potential to produce phenolic compounds, flavonoids and for antioxidant activity. Five isolates significantly produced flavonoids and phenolic compounds in the ethyl acetate and n-Butanol extracts, also saponins and high antioxidant activity against the DPPH (2.2-diphenyl-1-picrylhydrazyl) free radical. A strain of Aspergillus nidulans var. dentatus (former Emericella dentata) was able to produce tannins as well; its butanolic extract was very similar than the BHT (butylated hydroxytoluene) (94.3% × 94.32%) and Rutin (95.8%) reference substances in the DPPH radical scavenging. Similarly, a Chaetomium strain exhibited 93.6% and 94.7% of antioxidant activity in their ethyl acetate and butanolic fractions, respectively. The chromatographic analysis of the ethyl acetate fraction from the Aspergillus strain revealed the production of orcinol (3.19%). Four-methoxymethylphenol (4.79%), sorbicillin (33.59%) and ergosterol (23.08%) was produced by Trichoderma longibrachiatum and isopropenyl-1,4-dimethyl-1,2,3,3a,4,5,6,7-octahydroazulene were found in two Fusarium oxysporum strains. The phytochemical screening showed that all analyzed fungi were able to produce a kind of secondary metabolite (phenols, flavonoids, tannins and/or saponins). The study shows a great underexplored potential for industrial application of P. incarnata endophytes.

Multidirectional insights into the phytochemical, biological, and multivariate analysis of the famine food plant (Calligonum polygonoides L).: A novel source of bioactive phytocompounds

Calligonum polygonoides L. also known as famine food plant, is normally consumed in times of food scarcity in India and Pakistan and also used traditionally in the management of common diseases. The present design aims to provide an insight into the medicinal potential of four solvent extracts of C. polygonoides via an assessment of its phytochemical profile, antioxidant and enzyme inhibitory potential. Phytochemical composition was estimated by deducing total bioactive constituents, UHPLC-MS secondary metabolites profile, and HPLC phenolic quantification. Antioxidant potential was determined via six methods (radical scavenging (DPPH and ABTS), reducing power (FRAP and CUPRAC), phosphomolybdenum total antioxidant capacity and metal chelation activity). Enzyme inhibitory potential was assessed against clinical enzymes (acetylcholinesterase -AChE, butyrylcholinesterase -BChE, tyrosinase, and α-amylase). The highest amounts of phenolic contents were found in chloroform extract (76.59 mg GAE/g extract) which may be attributed to its higher radical scavenging, reducing power and tyrosinase inhibition potential. The n-butanol extract containing the maximum amount of flavonoids (55.84 mg RE/g extract) exhibited highest metal chelating capacity. Similarly, the n-hexane extract was found to be most active against AChE (4.65 mg GALAE/g extract), BChE (6.59 mg GALAE/g extract), and α-amylase (0.70 mmol ACAE/g extract) enzymes. Secondary metabolite assessment of the crude methanol extract as determined by UHPLC-MS analysis revealed the presence of 24 (negative ionization mode) and 15 (positive ionization mode) secondary metabolites, with most of them belonging to phenolic, flavonoids, terpene, and alkaloid groups. Moreover, gallic acid and naringenin were the main phenolics quantified by HPLC-PDA analysis in all the tested extracts (except n-butanol extract). PCA statistical analysis was also conducted to establish any possible relationship amongst bioactive contents and biological activities. Overall, the C. polygonoides extracts could be further considered to isolate bioactive enzyme inhibitory and antioxidant natural phytocompounds.

Isolation of Antidiabetic Withanolides from Withania coagulans Dunal and Their In Vitro and In Silico Validation.

Withania coagulans (W. coagulans) is well-known in herbal medicinal systems for its high biological potential. Different parts of the plant are used against insomnia, liver complications, asthma, and biliousness, as well as it is reported to be sedative, emetic, diuretic, antidiabetic antimicrobial, anti-inflammatory, antitumor, hepatoprotective, antihyperglycemic, cardiovascular, immuno-suppressive and central nervous system depressant. Withanolides present in W. coagulans have attracted an immense interest in the scientific field due to their diverse therapeutic applications. The current study deals with chemical and biological evaluation of chloroform, and n-butanol fractions of W. coagulans. The activity-guided fractionation of both extracts via multiple chromatographic steps and structure elucidation of pure isolates using spectroscopies (NMR, mass spectrometry, FTIR and UV-Vis) led to the identification of a new withanolide glycoside, withacogulanoside-B (1) from n-butanol extract and five known withanolides from chloroform extract [withanolid J (2), coagulin E (3), withaperuvin C (4), 27-hydroxywithanolide I (5), and ajugin E (6)]. Among the tested compounds, compound 5 was the most potent α-glucosidase inhibitor with IC50 = 66.7 ± 3.6 µM, followed by compound 4 (IC50: 407 ± 4.5 µM) and compound 2 (IC50: 683 ± 0.94 µM), while no antiglycation activity was observed with the six isolated compounds. Molecular docking was used to predict the binding potential and binding site interactions of these compounds as α-glucosidase inhibitors. Consequently, this study provides basis to discover specific antidiabetic compounds from W. coagulans.

Beneficial effects of Ajuga chamaepitys (L.) Schreber subsp. chia (Schreber) and its iridoids on the colitis model: Histopathological and biochemical evidence

In Turkish folk medicine, aerial parts of Ajuga chamaepitys (L.) Schreber subsp. chia (Schreber) are used for the treatment of diarrhea. The crude methanolic extract of aerial parts of A. chamaepitys subsp. chia was sequentially fractionated into five subextracts; n-hexane, dichloromethane, ethyl acetate, n-butanol and aqueous extracts. Effects of the methanol extract, subextracts and fractions were investigated in acetic acid–induced rat colitis model. The MeOH extract and n-BuOH subextract have regulated the caspase-3, myeloperoxidase, TNF-α, IL-6 levels and antioxidant parameters. After confirmation of the activity against ulcerative colitis, n-BuOH subextract was subjected to more chromatographic separation for the isolation of compounds ajugoside (1), asperulosidic acid (2) and deacetyl-asperulosidic acid (3). As a conclusion, A. chamaepitys subsp. chia can be used in cell, tissue, or individual-specific treatments that will be developed in the future treatment of IBD, or as a complementary therapeutic agent that contributes to these treatments.