Butanol Fraction Research Articles

Evaluation of the Anti-Malarial Activity of the Crude Root Extract and Solvent Fraction of Sesamum indicum (Fabaceae).

A major cumbersome factor in malaria control measure is the new coming antimalarial drug resistance strains. The increase of resistance to the available marketed antimalarial agents dictates the scientific community to search new alternative antimalarial agent from traditional plants. Therefore, our study assesses the antimalarial activity of the crude root extract and solvent fraction of Sesamum indicum in mice. The roots of Sesamum indicum were extracted by 80% methanol and fractionated using three solvents with different polarities. The in vivo antimalarial activity was assessed at 200 mg/kg, 400 mg/kg, and 600 mg/kg of the root crude extract and solvent fraction using the 4-day suppressive test. Similarly, the n- butanol fraction extract, which showed better suppression potential in 4-day suppressive test from other fractions was also evaluated in the curative model to assess its curative potential. The % parasitemia suppression, mean survival time, body weight change, rectal temperature change, and packed cell volume change were also evaluated in both models. Our finding revealed that the crude extract and solvent fraction treated groups had a statistical significant parasitemia suppression and mean survival time improvement as compared to the negative control (p<0.001) in both models in a dose-dependent fashion. The higher dose n-butanol fraction treated group (600mg/kg) showed the highest suppression effect and mean survival time prolongation in both tests from the other two fractions. However, the lowest suppressive effect was observed in 200 mg/kg aqueous fraction extract-treated groups in the 4-day suppressive test. The crude root extract and solvent fractions of Sesamum indicum possessed a dose dependent antimalarial activity and a significant change in other parameters in both models that strengthen the traditional claim.

In vitro immunomodulatory activity study of Garcinia cowa Roxb. fraction.

The objective of this study is to determine the activity of Garcinia cowa Roxb. n-hexane, ethyl acetate, and butanol fractions as an immunomodulator invitro and obtain the fraction that has the potential as an immunomodulator. Raw 264.7 macrophages were used to asses G.cowa Roxb. immunomodulatory activity. The MTT assay was chosen to measure cell viability to evaluate the cytotoxic effect on cells. ELISA method was used to measure the concentration of Interleukin-6 (IL-6) and Tumor Necrosis Factor Alpha (TNF-α) secreted by cells after being treated with G.cowa Roxb. fraction. The neutral red uptake assay determined the effect of Garcinia cowa Roxb. on the phagocytic activity. After Raw 264.7 macrophages were given the Hexan fraction (Hex) at concentrations of 12.5 and 25μg/mL, there was a decrease in the concentration of IL-6, TNF-α, and the phagocytosis index of cells. Administration of the Ethyl Acetate fraction (EtOAc) at concentrations of 12.5 and 25μg/mL on cells caused a decrease in IL-6 and TNF-α levels but did not affect the phagocytosis index. There was an increase in the level of TNF-α and the phagocytosis index after being given the Butanol fraction (BuOH) with concentrations of 12.5 and 25μg/mL but there was a slight decrease in the level of IL-6. Both Hex and EtOAc fractions could suppress immune responses through decreasing IL-6, TNF-α, and slightly decreased phagocytic activity. BuOH fraction could stimulate immunomodulatory activities through enhanced TNF-α levels and phagocytic index, but less potent in enhancing IL-6 production. The BuOH fraction could be developed as an immunostimulant.

Apple (Malus domestica Borkh) leaves attenuate indomethacin-induced gastric ulcer in rats

Malus domestica Borkh, the apple tree, exhibited numerous pharmacological properties including antioxidant, neuroprotective, anti-inflammatory, anticancer and antimicrobial activities. The present work aimed to annotate the secondary metabolites from a butanol fraction of apple leaves (BLE), evaluate the gastro-protective and healing effects of this fraction against indomethacin-induced gastric ulcers in rats and to identify its mechanism of action. BLE (100, and 200 mg/kg) was orally administered in rats as an acute treatment against indomethacin-induced gastric ulcer in comparison with famotidine as reference anti-ulcer drug. The stomachs of rats were collected to determine the ulcer index, the preventive ratio, measure the activity of glutathione peroxidase (GPx), and estimate the expression of cyclooxygenase-2 (COX-2), and heat shock protein 70 (HSP70). Furthermore, we evaluated both inflammatory and oxidative stress markers in the gastric tissues. We also performed histopathological study of gastric mucosa using H&E stain and periodic Schiff base stain to evaluate both gastric injury scores and gastric mucus content respectively. Pretreatment with BLE markedly lowered the severity of gastric injury induced by indomethacin, decreased oxidative stress, inflammatory cytokines, and COX-2 expression in the examined gastric tissues. The gastric healing effect of BLE was associated with increased mucoglycoproteins, and HSP70 expression. Additionally, gastric healing effect of high dose of BLE was superior to that of famotidine in decreasing gastric injury scores, COX-2, inflammatory cytokines, lipid peroxidation and in increasing gastric mucin content, HSP70, and reduced glutathione. These findings indicate that BLE is effective in accelerating ulcer healing by boosting HSP70 expression, and decreasing COX-2 expression, oxidative stress, and gastric inflammation which might be related to the presence of 21 phytoconstituents.

GC/MS and LC-MS/MS phytochemical evaluation of the essential oil and selected secondary metabolites of Ajuga orientalis from Jordan and its antioxidant activity

The current investigation aimed to shed light in the volatile and non-volatile secondary metabolites of Ajuga orientalis L. from Jordan. GC/MS and GC/FID analysis of the hydrodistilled essential oil obtained from aerial parts of the plant revealed tiglic acid (18.90 %) as main constituent. Each of the methanol and butanol fractions of A. orientalis were screened for their total phenol content (TPC), total flavonoid content (TFC), and antioxidant activity determined by DDPH and ABTS methods. The extracts were then analyzed by LC-ESI-MS/MS to unveil their chemical constituents, especially phenols and flavonoids. Results showed that the AO-B extract had the highest TPC (217.63 ± 2.65 mg gallic acid/g dry extract), TFC (944.41 ± 4.77 mg quercetin /g dry extract), highest DPPH and ABTS antioxidant activity ((4.00 ± 0.20) × 10-2; (3.00 ± 0.20) × 10-2 mg/mL, respectively) as compared to the AO-M extract. LC-ESI-MS/MS analysis of both extracts revealed the presence of several phenolics, flavonoids and nonphenolic acids.

Attenuation of Lipopolysaccharide-Induced Inflammatory Responses through Inhibition of the NF-κB Pathway and the Increased NRF2 Level by a Flavonol-Enriched n-Butanol Fraction from Uvaria alba.

Pathologic hyperreactive inflammatory responses occur when there is excessive activation of a proinflammatory NF-κB pathway and a reduced cytoprotective NRF2 cascade. The noncytotoxic, highly selective COX-2 inhibitory flavonol-enriched butanol fraction (UaB) from Uvaria alba (U. alba) was investigated for its inflammatory modulating potential by targeting NF-κB activation and NRF2 activity. Enzyme-linked immunosorbent assay was initially performed to measure levels of proinflammatory mediators [nitric oxide (NO), prostaglandin E2, and reactive oxygen species (ROS)] and cytokines [tumor necrosis factor-alpha (TNF-α), IL-1β, and IL-6], followed by reverse transcription-polymerase chain reaction and western blotting to determine mRNA and protein expression, respectively. Using immunofluorescence staining combined with western blot analysis, the activation of NF-κB was further investigated. NRF2 activity was also measured using a luciferase reporter assay. UaB abrogated protein and mRNA expressions of inducible nitric oxide synthase (iNOS), COX-2, TNF-α, IL-1β, and IL-6 in RAW 264.7 macrophages, thereby suppressing the production of proinflammatory mediators and cytokines. This was further validated when a concentration-dependent decrease in NO and ROS production was observed in zebrafish (Danio rerio) larvae. UaB also increased NRF2 activity in HaCaT/ARE cell line and attenuated NF-κB activation by inhibiting the nuclear translocation of transcription factor p65 in RAW 264.7 macrophages. Nontargeted LC-MS analysis of UaB revealed the presence of the flavonols quercitrin (1), quercetin (2), rutin (3), kaempferol (4), and kaempferol 3-O-rutinoside (5). Molecular docking indicates that major flavonol aglycones have high affinity toward COX-2 NSAID-binding sites, TNF-α, and TNF-α converting enzyme, while the glycosylated flavonoids showed strong binding toward iNOS and IKK-all possessing dynamic stability when performing molecular dynamics simulations at 140 ns. This is the first report to have elucidated the mechanistic anti-inflammatory potential of the Philippine endemic plant U. alba.

Antidiabetes study of Spondias mombin (Linn) stem bark fractions in high-sucrose diet-induced diabetes in Drosophilamelanogaster

ObjectiveThe onset of insulin resistant diabetes has been associated with a high-sucrose diet in vertebrates and invertebrates. However, various parts of Spondias mombin reportedly possess antidiabetic potential. However, the antidiabetic efficacy of S. mombin stem bark in high-sucrose diet-induced Drosophila melanogaster model has not been explored. In this study, the antidiabetic and antioxidant effects of the solvent fractions of S. mombin stem bark were evaluated using in vitro, in vivo, and in silico methods. MethodsSuccessive fractionation of S. mombin stem bark ethanol extract was performed; the resulting fractions were subjected to in vitro antioxidant and antidiabetic assays using standard protocols. The active compounds identified from the high-performance liquid chromatography (HPLC) study of the n-butanol fraction were docked against the active site of Drosophila α-amylase using AutoDoc Vina. The n-butanol and ethyl acetate fractions of the plant were incorporated into the diet of diabetic and nondiabetic flies to study the in vivo antidiabetic and antioxidant properties. ResultsThe results obtained revealed that n-butanol and ethyl acetate fractions had the highest in vitro anti-oxidant capacity by inhibiting 2,2-diphenyl-1-picrylhydrazyl (DPPH), ferric reducing antioxidant power, and hydroxyl radical followed by significant inhibition of α-amylase. HPLC analysis revealed the identification of eight compounds with quercetin having the highest peak followed by rutin, rhamnetin, chlorogenic acid, zeinoxanthin, lutin, isoquercetin, and rutinose showing the lowest peak. The fractions restored the glucose and antioxidant imbalance in diabetic flies, which is comparable with the standard drug (metformin). The fractions were also able to upregulate the mRNA expression of insulin-like peptide 2, insulin receptor, and ecdysone-inducible gene 2 in diabetic flies. The in silico studies revealed the inhibitory potential of active compounds against α-amylase with isoquercetin, rhamnetin, rutin, quercetin, and chlorogenic acid having higher binding affinity than the standard drug (acarbose). ConclusionOverall, the butanol and ethyl acetate fractions of S. mombin stem bark ameliorate type 2 diabetes in Drosophila. However, further studies are needed in other animal models to confirm the antidiabetes effect of the plant.

Ameliorative Effects of Thunbergia erecta L. Leaves Against the Initiation of Hepatocarcinogenesis Induced by Diethylnitrosamine in the Rat Model

Thunbergia erecta L. contains cytotoxic and liver-protective compounds. Thunbergia erecta L. leaves were macerated in 70% aqueous ethanol, then fractionated with ethyl acetate (9.3 g) and butanol (12.7 g), and attenuated Den-induced liver cancer in a Wistar rat experimental model. Ethyl acetate and butanol fractions were chromatographed using column chromatography and solid-phase extraction (SPE); Vicenin-II (1), kaempferol (2), biochanin A, sissotrin 7-O-β-glucopyranoside (3), gentianose (4), acacetin 7-O-β-glucopyranoside (5), apigenin 7-O-β-glucopyranoside (6), and rosmarinic acid (7) were extracted, and their structures were determined using NMR spectroscopy and ESI-mass spectrometry. Sixty rats were divided into six groups (ten each): control group, Den group, doxorubicin/Den-treated group, butanol fraction/Den-treated group, and isolated acacetin 7-O-β-glucopyranoside/Den-treated group. The liver enzymes and proinflammatory biomarkers were used to estimate the liver function. In addition, liver tissues were collected for analysis of oxidative stress markers, gene expression, and histopathology. There is a significant increase in the levels of liver enzymes, AFP, and TNF-ἁ. This was conveyed by a significant increase of IL-1 and caspase-3, elevation of MDA and reduction of GSH, and suppression of Bcl2 and elevation of Bax expression. All parameters in butanol, ethyl acetate fractions, and isolated acacetin 7-O-β-glucopyranoside (major constituents) of T. erecta L. were significantly improved to values close to those of the control group.

Nephroprotective effect of Physalis peruviana L. calyx extract and its butanolic fraction against cadmium chloride toxicity in rats and molecular docking of isolated compounds

BackgroundCadmium is an environmentally toxic metal that has deleterious effects on both animals and humans due to its accumulation in different body tissues. Physalis peruviana L. fruit and calyx contain many active constituents which are used traditionally for their different biological activities. Based on the traditional uses of P. peruviana L. calyx, we aimed to evaluate the nephroprotective effect of their 80% aqueous methanol extract (AME) and n-butanol fraction (Bu.F.) against cadmium chloride-induced nephrotoxicity in rats and to correlate this activity with phytoconstituents isolated using molecular docking studies.MethodsThe n-butanol fraction of P. peruviana L. calyx was fractionated using various chromatographic techniques and the isolated compounds were identified based on their chemical and spectroscopic data. The nephroprotective activity was assessed using cadmium chloride-induced nephrotoxicity in the rat model, by measuring some important parameters such as body weight, kidney weight, serum urea, and creatinine levels, oxidative stress markers, inflammatory markers, and histopathological examinations of kidney tissue. Molecular docking studies of the isolated compounds were performed.ResultsThree withanolides named 4 β-hydroxywithanolide E (1), Physalin B (2) and 3α, 14β-dihydroxywithaphysalin N (3) were isolated and identified from the n-butanol fraction of P. peruviana L calyx extract. The extract and its butanol fraction significantly improved the serum kidney function markers and tissue oxidative status including malondialdehyde (MDA), reduced glutathione (GSH) and catalase (CAT). Additionally, the extracts significantly decreased the levels of tumor necrosis factor-alpha (TNF-α) and nuclear factor kappaB (NF-κβ). Moreover, the histological changes were ameliorated by the extracts. The molecular docking study showed that the isolated compounds displayed a remarkable inhibitory activity against IκB kinase.ConclusionThe AME and its butanol fraction of P. peruviana L calyx showed potential nephroprotective activity against cadmium chloride-induced nephrotoxicity which is correlated at least in part to its considerable withanolides content.

Isolation and Characterization of Prophylactic Antimalarial Agents from Ochna kibbiensis Leaves

Ochna kibbiensis (Family: Ochnaceae) has been employed in ethnomedicine for the treatment of malaria and inflammation, among others. The aim of this study was to isolate and characterize prophylactic antimalarial agents from the leaves of O. kibbiensis against Plasmodium berghei, in vivo and in silico. The median lethal dose (LD50) of the methanol extract and its fractions (hexane, dichloromethane, ethylacetate and butanol) was determined according to Lorke’s method while the antimalarial effect of the extract and its fractions was investigated according to the method described by Peters prophylactic test using Chloroquine-sensitive Plasmodium berghei (NK65). All the extract/fractions exhibited LD50 values ≥ 5000 mg/kg with the exception of the n-butanol fraction (1702.94 mg/kg), which indicate that the plant is non-toxic. Dichloromethane fraction exhibited a significant (p &lt; 0.05) and dose-dependent prophylactic effect with 47.62, 85.12, and 100.0% prophylaxis (at 500, 250, and 125 mg/kg), while the least effect was observed by the butanol fraction with a percentage prophylaxis of 64.29 and 76.19, respectively; the standard drug, pyrimethamine, had 95.24% prophylaxis. Based on the results obtained, dichloromethane fraction of O. kibbiensis was subjected to chromatographic purification, which led to the isolation of a mixture of two compounds identified as stigmasterol and β-sitosterol by analysis of the NMR spectral data and comparison with existing literature; the compounds exhibited good binding affinities (−5.129 and −4.889 kcal/mol) against pfLDH and a favorable ADMET profile. In conclusion, the leaves of O. kibbiensis have demonstrated a significant prophylactic antimalarial activity and the two known steroids (stigmasterol and β-sitosterol) were isolated from the dichloromethane fraction for the first time.

Phytochemical Approach Including Total Phenolic and Flavonoid Contents and Evaluation of in vitro ABTS Antioxidant Capacity and Lipoxygenase Inhibition of Anisosciadium lanatum

Anisosciadium lanatum Boiss is commonly known in Bedouins as besbas. Traditional, it is palatable plant and used in medicine of livestock to treat skin conditions . The main objective of current approach was to screen the presence of different kind of metabolites applying standard procedures followed by assessment of total phenolic (TPC) and flavonoids (TFC) contents. In addition, the in vitro ABTS antioxidant and lipoxygenase activities were evaluated. Different organs (leaves, stems and flowers) of Anisosciadium lanatum were extracted using 70% methanol to yield total methanol extracts of leaves (TML), stems (TMS) and flowers (TMF). Results demonstrated that TML, TMS and TMF are characterized by the content of different constituents such as flavonoids, phenolics/tannins, steroids, saponins, and carbohydrates at different levels. Ethyl acetate (EA) and butanol (BT) fractions of TML and TMS demonstrated the highest percentage of TPC and TFC. The results demonstrated the competence of EA and BT as free radical scavenger fractions compared to other fractions and its opportunity to contain bioactive antioxidant metabolites . TML, TMS and TMF exhibited Lipoxygenase inhibitory activity with IC50 values of 4.88, 5.40 and 6.05 μg/mL, respectively when compared to that of the positive control baicalein (IC50: 0.27 μg /mL). In conclusion, present investigation highlighted the potential of Anisosciadium lanatum to be promising candidate with activity against wide range of inflammatory-related diseases.

Profound Assessment of Phytochemical, Botanical and Antioxidant Characteristics Including Determination of Total Phenolic and Flavonoid Contents of Stem Bark of Cordia obliqua L.

Cordia obliqua is known as Bumber. Its fruits and leaves are popularly used because of antioxidant and anti-diabetic activities. The purpose of this study is to evaluate the phytochemicals and antioxidant activity as well as botanical features of stem bark of Cordia obliqua. Chemical components were preliminary screened in various fractions based on the polarities including; n-hexane, chloroform, ethyl acetate, butanol and aqueous fractions of using standard procedures. Total phenolic (TPC) and flavonoid (TFC) contents were assessed by Folin-Ciocalteau and aluminium chloride methods respectively. The antioxidant activity was evaluated by ABTS antioxidant procedure, using ascorbic acid as standard. Results confirmed that stem bark of Cordia obliqua chemically is characterized by the presences of flavonoids, alkaloids, steroids, saponins, tannins and carbohydrates at different levels in various fractions and the absence of cardiac glycosides and anthraquinones. Microscopically, the plant is characterized by presence of big Ca oxalate clusters, various types of xylem vessels and big amount of cork cells. TPC was ranged from 13.6±1.4 and 220.5±3.4 mg GAE/g dry plant extract and TFC was ranged from 0.029±0.12and 15.46±0.33 mg QE/g dry plant extract. Due to the high phenolic and flavonoid content in butanol and ethyl acetate fractions; results of antioxidant using ABTS assay showed high antioxidant activity with IC50 valued 11.84±1.2 μg/ ml for butanol fraction and 14.81±1.1 μg/ml for ethyl acetate fraction. Taken together, the research work demonstrated the potential natural antioxidant value of the waste product stem bark of Cordia obliqua. The study endorses forthcoming work to isolate and identify the chemical constituents in stem bark of Cordia obliqua.

In vitro antimalarial activity of Syzygium cumini fruit fraction.

Malaria is still one of the most severe public health problems worldwide. The development of treatment, prevention, and control of malaria is one of the substantial problems in the world. To investigate the in vitro antimalarial activity of Syzygium cumini methanol fruit fraction. Syzygium cumini L fruit powder was macerated with methanol (PA) and the extract obtained was fractionated using the liquid-liquid partition method with n-hexane, ethyl acetate, butanol, chloroform, methanol, and water solvents. In vitro antimalarial assay was conducted using the culture of Plasmodium falciparum 3D7 strain culture that had reached >5% growth and was examined for IC50 values using a 24-well microplate in duplicate. Each treatment and control well contained 1,080 μl of complete media. Well, number 1 was added with 120 μl fraction, and then the solution was diluted until it reached 0.01, 0.1, 1, 10, and 100 μg/ml the final concentration in the microtiter well. The control only contained complete media and infected erythrocytes without the addition of anti-malarial drugs. The microplate was incubated for 48 hours. After 48 hours, a thin blood smear was made fixed with methanol and stained with 20% Giemsa for 20 minutes to determine the IC50 value by plotting sample concentrations and percentage of parasitemia in Excel. The IC50 values of ethyl acetate fraction, n.hexane fraction, butanol fraction, and water fraction were 1.189, 76.996, 1,769, and 15.058 μg/ml, respectively. Whereases the IC50 values of C1 fraction (mix fraction from chloroform: methanol 100:0 and 90:10) and C4 fraction (mix fraction from chloroform: methanol 20:80, 10:90, and 0:100) were 100.126 and 1.015 μg/ml, respectively. The results showed that the IC50 value of ethyl acetate, butanol, and C4 fraction were lower than 10μg/ml and were considered as good activity (strong antimalarial activity). The ethyl acetate, butanol and C4 subfraction from S. cumini fruit have the potential to be developed as an antimalarial agent.

Increase in Effect of Citrus natsudaidai on Brain-Derived Neurotrophic Factor.

The increase in brain-derived neurotrophic factor (BDNF) in the brain is beneficial for the treatment of depression, Alzheimer's disease (AD), and Parkinson's disease (PD); BDNF can cross the blood-brain barrier. Therefore, foods that elevate BDNF concentration in peripheral tissues may increase BDNF in the brain and thereby induce preventive and therapeutic effects against depression, AD, and PD. In this study, we aimed to determine whether Citrus natsudaidai extracts can increase BDNF concentration using the human kidney adenocarcinoma cell line ACHN, which has BDNF-producing and -secreting abilities. As test samples, methanol extracts of C. natsudaidai peel and pulp, and their n-hexane, ethyl acetate, n-butanol, and water fractions were prepared. The BDNF concentrations in culture medium of ACHN cells were assayed after 24 h cultivation in the presence of test samples. Compared with that of control (non-treated) cells, the BDNF concentration increased in the culture medium of ACHN cells treated with the methanol extract of C. natsudaidai peel and its hexane, butanol, and water fractions, as well as the butanol and water fractions of the pulp extract. Quantitative reverse transcription-polymerase chain reaction analysis revealed that ACHN cells treated with the butanol fractions of the peel and pulp extracts showed elevated levels of BDNF mRNA compared with those of non-treated cells. C. natsudaidai may increase BDNF concentration by acting on peripheral tissues and could be a medication for the prevention and treatment of depression, AD, and PD.

Study of Anti-Ulcerogenic Effect of Methanol Extract and Fractions of the Leaves of Ocimum Gratissimum (Lamiaceae), on Ethanol-Induced Ulcer in Rats

Peptic ulcer has been a ravaging gastrointestinal disorder in clinical practice. The symptomatic effect is the perforation of the stomach lining. The study was aimed at evaluating the anti-ulcer activity and phytochemical constituents of the leaves of Ocimum gratissimum. The powdered leaves were macerated in 95%v/v of methanol for 72 h, and the dried extract obtained was washed with n-hexane (Hex), ethyl acetate (EtOAc) and butanol (Buta) successively using the solvent partition method to fractionate. Phytochemical constituents were evaluated using validated methods. Acute toxicity was performed using a modified Lorke’s method. Antiulcer studies were conducted using an ethanol-induced ulcer in rat model. The rats received 200, 400 and 20 mg per kg body weight of O.gratissimum extract, its fractions and omeprazole respectively once daily for 14 days. The extraction yielded 3.3 % methanol extract, 16.8 % n-hexane 24.4 % ethyl acetate and 5.2 % butanol fractions. The phytochemical constituents of the extracts are alkaloids, flavonoids, tannins, terpenoids, carbohydrates, steroids and saponin. There was no mortality even at an oral dose of 5000 mg of extract/kg of mouse in the acute toxicity evaluation. The extract and its fractions (200 and 400 mg/kg doses) exhibited dose-dependent ulcer curative. The Hex fraction (400 mg/kg) demonstrated the best anti-ulcer effect with 78.5 % and ulcer index (UI) of 0.60±0.24 when compared to the standard with 50% and 1.40±0.24 respectively. A significant reduction (p&lt; 0.05) in the UI was observed in rats treated with the O. gratissimumextract and its fractions.

Holothuria scabra extracts confer neuroprotective effect in C.elegans model of Alzheimer's disease by attenuating amyloid-β aggregation and toxicity.

Alzheimer's disease (AD) is the most common aged-related neurodegenerative disorder that is associated with the toxic amyloid-β (Aβ) aggregation in the brain. While the efficacies of available drugs against AD are still limited, natural products have been shown to possess neuroprotective potential for prevention and therapy of AD. This study aimed to investigate the neuroprotective effects of H.scabra extracts against Aβ aggregation and proteotoxicity in C.elegans model of Alzheimer's diseases. Whole bodies (WB) and body wall (BW) of H.scabra were extracted and fractionated into ethyl acetate (WBEA, BWEA), butanol (WBBU, BWBU), and ethanol (BWET). Then C.elegans AD models were treated with these fractions and investigated for Aβ aggregation and polymerization, biochemical and behavioral changes, and level of oxidative stress, as well as lifespan extension. C.elegans AD model treated with H.scabra extracts, especially triterpene glycoside-rich ethyl acetate and butanol fractions, exhibited significant reduction of Aβ deposition. These H.scabra extracts also attenuated the paralysis behavior and improved the neurological defects in chemotaxis caused by Aβ aggregation. Immunoblot analysis revealed decreased level of Aβ oligomeric forms and the increased level of Aβ monomers after treatments with H.scabra extracts. In addition, H.scabra extracts reduced reactive oxygen species and increased the mean lifespan of the treated AD worms. In conclusion, this study demonstrated strong evidence of anti-Alzheimer effects by H.scabra extracts, implying that these extracts can potentially be applied as natural preventive and therapeutic agents for AD. Alzheimer's disease, Neurodegenerative disorder, Traditional medicine, Experimental model systems, Molecular biology.

BIOLOGICAL ACTIVITIES OF EXTRACTS AND SECONDARY METABOLITE OF Macaranga mappa BARK AS AN ANTIDIABETIC BY α-GLUCOSIDASE INHIBITOR, ANTIOXIDANT, AND CYTOTOXICITY

The biological activities of extracts and isolated compounds of Macaranga mappa stem bark for antidiabetic herbal medicine, antioxidant, and cytotoxicity activities have been determined. The antidiabetic, antioxidant, and cytotoxicity activities of the sample were carried out by inhibition value of α-glucosidase, DPPH method, and brine shrimp larvae method, respectively. The initial methanol extract and its fractions have good activities against antidiabetics and antioxidants, except for the hexane fraction. The fractions with the highest activity for the antidiabetic and antioxidant tests were the water fraction IC50 6.654 ppm and the butanol fraction IC50 32.34 ppm, respectively. The toxicity test results with the BSLT method showed that all fractions were non-toxic LC50&gt;1000 ppm. The isolated compound from the ethyl acetate fraction was a coumarin derivative, namely scopoletin, with antidiabetic and antioxidant activities.

Evaluation of anti-inflammatory potential of extract, fractions and major compounds of Ponciri Fructus in LPS-induced RAW 264.7 cells

Dried immature fruit of Poncirus trifoliata (L.) Raf., known as Ponciri Fructus, is a well-known traditional Korean medicine for treatment of allergy and gastrointestinal disorders. In previous study, we reported the anti-obesity effects of the extracts, fractions and major compounds of Ponciri Fructus on 3 T3-L1 preadipocytes. In continuation, in this research, we evaluated their anti-inflammatory potential using lipopolysaccharide (LPS) induced RAW 264.7 cells. Results showed that the ethanol extract of fruits and hexane and ethyl acetate soluble fractions of the extract inhibited nitrous oxide (NO) production in LPS stimulated macrophage in all doses. Whereas, butanol fraction of extract showed significant inhibition in production of NO only at higher dose of 80 µg/mL. Some of the isolated compounds such as poncirin, naringin, imperatorin and phellopterin, significantly inhibited NO production in LPS-stimulated macrophages. Poncirin and imperatorin showed anti-inflammatory potential by inhibiting cyclooxygenase (COX)-2 protein as evidenced by downregulation of that protein in western blot assay. Imperatorin also inhibited inducible nitric oxide synthase (iNOS) responsible for production of NO in macrophages. In conclusion, Ponciri Fructus has strong anti-inflammatory potential and possesses many active flavonoids and coumarins contributing to this activity.

Evaluation of the Anti-Inflammatory Activity of the Leaf Extract and Fractions of Ipomoea Quamoclit in Albino Wistar Rats

Background: Medicinal plants have been shown to contain intrinsic active ingredients that can be used for curative purpose for some diseases. Ipomoea quamoclit is one of such ethnomedicinal plants of reported health benefits. Aim of Study: This study was aimed at evaluating the anti-inflammatory activity of ethanol extract and fractions of the leaves of Ipomoea quamoclit Mill. Materials and Methods: Ipomoea quamoclit leaves were harvested and extracted with 80% ethanol by cold maceration for 48 hours and the crude extract was fractionated to obtain n-hexane, n-butanol and ethyl acetate fraction, respectively. The crude extract and its fractions were screened to unveil the resident phytochemical constituents. The ethanol extract was tested for acute toxicity (LD50). The systemic acute inflammation of the crude extract and fractions of Ipomoea quamoclit was studied using the water (fluid) displacement method after inducing inflammation with egg albumin, using rats. The effect of the crude extract and fractions of Ipomoea quamoclit on arthritis was studied using the formaldehyde-induced arthritis model in rats. Results: The results of the qualitative phytochemical evaluation of the plant confirmed the presence of these phytoconstituents such as alkaloids, flavonoids, saponins, tannins, steroids, terpenoids, glycosides, carbohydrates, proteins, and coumarins. There were no deaths recorded for acute toxicity study for both phases of the test. In the acute anti-inflammation assay, significant (P&lt;0.05) anti-inflammatory activities were observed from the 5th hour for the ethyl acetate fraction (150 and 400 mg/kg) and the butanol fraction (400 mg/kg). The anti-arthritic activity of the crude extract (150 mg/kg), ethyl acetate fraction (150 and 400 mg/kg), n-hexane fraction (150 mg/kg) and butanol fraction (150 and 400 mg/kg) was obvious from the second day after administration. By the 10th day the crude extract (50, 150, and 400 mg/kg) and ethyl acetate fraction (150 and 400 mg/kg) brought about a significant reduction of chronic inflammation (arthritis) in the test animals to normal basal levels. Conclusions: This study thus provides scientific information and validates the ethnobotanical use of Ipomoea quamoclit leaves in management of diseases and inflammation inclusive. The findings of this study also reveal that potentially Ipomoea quamoclit could be a source of pharmacologically active compounds of pharmaceutical importance.

Musanga cecropioides Attenuates Chemical and Diabetes Induced Oxidative Stress in Experimental Animal Models

Oxidative stress plays an important role in both induction of diabetes and development of diabetes complications. This study evaluated the effect of leaf extract and fractions of M. cecropioides on both chemical and disease induced oxidative stress. The leaves were extracted with methanol and partitioned into various fractions. Phytochemical analysis and total phenolic content (TPC) were done for the extract and fractions. The DPPH (2,2-diphenyl-1-picrylhydrazyl) and Ferric reducing antioxidant power assay were used to evaluate their in vitro antioxidant potentials of the extracts and fractions at 52.5, 125, 250, 500 and 1000 µg/ml concentrations with ascorbic acid as reference standard. Carbon tetrachloride and streptozotocin-Nicotinamide (STZ-NAD) were used to induce chemical and diabetes induced oxidative stress respectively. Treatments were done with 200 and 400 mg/kg of the extract and fractions using Silymarin as reference standard. Liver function tests and lipid peroxidation (LPO) were used to monitor CCL4 induced oxidative stress while serum antioxidant enzymes (catalase and superoxide dismutase), LPO and total plasma antioxidant assays were used to monitor diabetes induced oxidative stress. The ethyl acetate fraction (EAF) showed the highest TPC of 386.06 mgGAE/g. The EAF and butanol fraction (BF) showed better DPPH activity compared to the extract with IC50s of 49.78, 71.57, 98.92 µg/ml respectively. The EAF both at 200 and 400 mg/kg maintained non-significant (p &gt; 0.05) difference between pre-induction and post-induction ALT and AST concentrations. Also, only EAF at 400 mg/kg protected against significant rise in CCL4 induced LPO from baseline values which was not achieved with 100 mg/kg silymarin (reference standard treatment). The EAF at 400 mg/kg was the only treatment that produced significant (P&lt;0.05) reduction in blood glucose 24 h post-treatment compared to vehicle control group. The EAF and BF at 400 mg/kg just like 200 mg/kg metformin were able to restore serum catalase almost to their pre-induction values with no significant (P&gt;0.05) difference. M. cecropioides proved effective in both chemical and disease induced oxidative stress.

Phytochemical and Biological Investigation of the Leaves of Tridax procumbens

Aims: Because of various traditional uses of Tridax procumbens leaves, the authors choose the plant for investigating the numerous biological activities. The main objective for this study is to search antioxidant activity, hypoglycemic activity and antibacterial activities with initial phytochemical investigations of the leaves of Tridax procumbens.&#x0D; Methodology: The phytochemical purposes were achieved by using two different chromatographic techniques thin layer chromatography (TLC), vacuum liquid chromatography (VLC). DPPH test, glucose uptake activity of yeast cells and agar plate diffusion technique were performed to evaluate the antioxidant capacity, hypoglycemic activity and anti-bacterial properties respectively of different fraction obtained from VLC by using different solvent systems such as dichloromethane, butanol, ethyl acetate and methanol. 31.25 µg/ml, 62.5 µg/ml, 125 µg/ml, 250 µg/ml and 500 µg/ml sample were used from each fraction to investigate antioxidant and hypoglycemic activity where vitamin C tablet and metformin were used as standard respectively. Antibacterial capacity was measured by measuring zone of inhibition resulted by the fractions where ciprofloxacin was taken as reference drug. &#x0D; Results: Some visible spots were identified in the TLC plate which confirms the presence of different compounds in the fractions obtained from the methanolic extract of the leaves of Tridax procumbens. Butanol and ethyl acetate fractions showed the highest antidiabetic activity. In addition to, ethyl acetate, butanol and methanol fractions exerted more than 80% antioxidant capacity in DPPH assay. Furthermore, butanol fraction gives maximum zone of inhibition up to 21 mm against Staphylocuccos aureas which ensure anti-bacterial properties of the leaves of Tridax procumbens especially against Staphylocuccos aureas and its strains.&#x0D; Conclusion: Notwithstanding the all the research, the leaves had anti-inflammatory properties, which may have been generated by their antioxidant activity. As a result, if more therapeutic research is done, the separated compounds in those fractions may be employed as future therapeutic strategies.