Activity Of Methanolic Extract Research Articles

LC-MS/MS profiling of Tipuana tipu flower, HPLC-DAD quantification of its bioactive components, and interrelationships with antioxidant, and anti-inflammatory activity: in vitro and in silico approaches

BackgroundFabaceae plays a crucial role in African traditional medicine as a source of large number of important folk medication, agriculture and food plants. In a search of potential antioxidant and anti-inflammatory candidates derived from locally cultivated plants, the flowers of Tipuana tipu (Benth.) Lillo growing in Egypt were subjected to extensive biological and phytochemical studies. The impact of the extraction technique on the estimated biological activities was investigated.MethodsThe flowers were extracted using different solvents (aqueous, methanol, water/methanol (1:1), methanol/methylene chloride (1:1), and methylene chloride). The different extracts were subjected to antioxidant (DPPH, ABTS, and FRAP) and anti-inflammatory (COX-2 and 5-LOX) assays. The methanol extract was assessed for its inhibitory activity against iNOS, NO production, and pro-inflammatory cytokines (NF-KB, TNF-R2, TNF-α, IL-1β, and IL-6) in LPS-activated RAW 264.7 macrophages. The composition-activity relationship of the active methanol extract was further investigated using a comprehensive LC–QTOF-MS/MS analysis. The major identified phenolic compounds were further quantified using HPLC-DAD technique. The affinity of representative compounds to iNOS, COX-2, and 5-LOX target active sites was investigated using molecular docking and molecular dynamics simulations.ResultsThe methanol extract exhibited the highest radical scavenging capacity and enzyme inhibitory activities against COX-2 and 5-LOX enzymes with IC50 values of 10.6 ± 0.4 and 14.4 ± 1.0 µg/mL, respectively. It also inhibited iNOS enzyme activity, suppressed NO production, and decreased the secretion of pro-inflammatory cytokines. In total, 62 compounds were identified in the extract including flavonoids, coumarins, organic, phenolic, and fatty acids. Among them 18 phenolic compounds were quantified by HPLC-DAD. The highest docking scores were achieved by kaempferol-3-glucoside and orientin. Additionally, molecular dynamics simulations supported the docking findings.ConclusionThe flower could be considered a potentially valuable component in herbal medicines owing to its unique composition and promising bioactivities. These findings encourage increased propagation of T. tipu or even tissue culturing of its flowers for bioprospecting of novel anti-inflammatory drugs. Such applications could be adopted as future approaches that benefit the biomedical field.

Phytochemical profile by LC-MS/MS analysis and evaluation of antioxidant, antidiabetic, anti-Alzheimer, and anticancer activity of Onobrychis argyrea leaf extracts

IntroductionStudies on different species of Onobrychis, a member of the Fabaceae family, have revealed a number of biological activities with potential applications in alternative medicine. The phytochemical content of the plant Onobrychis argyrea subsp. argyrea and some of the important biological activities linked to its metabolism are quite limited. Therefore, this study was the first to determine the content of secondary metabolites in this species and to elucidate important biological activities related to metabolism. MethodsLC-MS/MS was used for the quantitative analysis of bioactive compounds in the aerial part of O. argyrea extracts. The antioxidant properties of the extracts were assessed based on their ability to scavenge DPPH radicals and reduce iron ions. The anti-diabetic effect of the extracts was tested by the inhibition of α-amylase and α-glycosidase enzymes, and the anti-Alzheimer's ability was tested by the inhibition of the enzymes AChE and BChE. The cytotoxic effects of the extracts were tested on four different cancer lines, namely A-549, HT-29, MCF-7 and MDA-MB 453 using the XTT assay. The mechanism of the anti-cancer effect was determined by means of flow cytometry analysis on HT-29 cells. ResultsTwenty-nine phytochemicals were identified via the LC-MS/MS analysis in the plant extracts. The most abundant phytochemicals in the extracts were quinic acid, isoquercitrin, epicatechin, and routine, respectively. Antioxidant analysis showed that among all extracts, methanol extract (ME) was most effective in scavenging DPPH (IC50: 23.93 ± 0.96 µg/mL) and in reducing iron ions (53.24 ± 2.14 mgTEAC/g). Enzyme activity studies demonstrated that ME is a potent inhibitor of α-glycosidase (IC50: 15.06±0.64 µg/mL), AChE (IC50: 24.75±0.76 µg/mL), and BChE (IC50: 3.36±0.14 µg/mL). XTT assay results disclosed the strongest anti-proliferative activity of ME against the human colorectal adenocarcinoma HT-29 cell line with an IC50 value of 33.35±0.92 µg/mL. Flow cytometry analysis revealed that ME caused mitochondrial membrane damage in HT-29 cells (**p<0.01) and subsequently induced apoptosis (**p<0.01) by activating the caspase pathway (**p<0.001). ConclusionO. argyrea, rich in bioactive compounds, showed remarkable antioxidant, antidiabetic, Alzheimer's, and anticancer properties in vitro, demonstrating that this plant contains secondary metabolites that may be potential drug candidates for the treatment of metabolic diseases.

Litsea glaucescens Kuth possesses bactericidal activity against Listeria monocytogenes.

Litsea glaucencens Kuth is an aromatic plant used for food seasoning food and in Mexican traditional medicine. Among, L. glaucencens leaves properties, it has proven antibacterial activity which can be used against opportunistic pathogens like Listeria monocytogenes, a foodborne bacteria that is the causal agent of listeriosis, a disease that can be fatal in susceptible individuals. The aim of this work was to investigate the antibacterial activity of L. glaucescens Kuth leaf extracts against L. monocytogenes and to identify its bioactive components. L. glaucences leaves were macerated with four solvents of different polarity (n-hexane, dichloromethane, ethyl acetate, and methanol). To determine the capacity to inhibit bacterial proliferation in vitro, agar diffusion and microdilution methods were used. Next, we determined the minimal bactericidal concentration (MBC). Finally, we determined the ratio of MBC/MIC. Metabolites present in the active methanolic extract from L. glaucescens Kuth (LgMeOH) were purified by normal-phase open column chromatography. The structure of the antibacterial metabolite was determined using nuclear magnetic resonance (1H, 13C, COSY, HSQC) and by comparison with known compounds. The LgMeOH extract was used to purify the compound responsible for the observed antimicrobial activity. This compound was identified as 5,7-dihydroxyflavanone (pinocembrin) by analysis of its spectroscopic data and comparison with those described. The MIC and MBC values obtained for pinocembrin were 0.68 mg/mL, and the ratio MBC/MIC for both LgMeOH and pinocembrin was one, which indicates bactericidal activity. L. glaucences Kuth leaves and its metabolite pinocembrin can be used to treat listeriosis due the bactericidal activity against L. monocytogenes.

Phytochemical Composition, Antioxidant, Antimicrobial, Antibiofilm, and Antiquorum Sensing Potential of Methanol Extract and Essential Oil from Acanthus polystachyus Delile (Acanthaceae).

The evolution of microbes in response to conventional antimicrobials leads to antimicrobial resistance (AMR) and multidrug resistance (MDR), and it is a global threat to public health. Natural products are possible solutions to this massive challenge. In this study, the potential of Acanthus polystachyus extracts was investigated for phytochemical composition and biological properties as antimicrobials. Gas chromatography-mass spectra (GC-MS) analysis of methanol extract (ME) and essential oil (EO) detected 79 and 20 compounds, respectively. The major compounds identified in ME and their abundance were β-sitosterol acetate (16.06%), cholest-5-en-3-yl (9Z)-9-octadecenoate (9.54%), 1-dodecanol (7.57%), (S)-(E)-(-)-4-acetoxy-1-phenyl-2-dodecen-1-one (6.03%), neophytadiene (5.7%), (E)-2-nonadecene (3.9%), hexanol-4-D2 (2.92%), and decane (2.4%). Most compounds have known bioactive functions. In EO, the major compounds were stearyl alcohol (25.38%); cis-9-tetradecenoic acid, isobutyl ester (22.95%); butyl 9-tetradecenoate (10.62%); 11,13-dimethyl-12-tetradecen-1-ol acetate (10.14%); ginsenol (3.48%); and diisooctyl phthalate (2.54%). All compounds are known to be bioactive. The antioxidant activity of ME and EO ranged from 48.3 to 84.2% radical scavenging activity (RSA) and 45.6 to 82% RSA, respectively, with dose dependency. The disc diffusion assay for the antimicrobial activity of ME revealed high inhibition against Acenetobacter baumannii (130.2%), Pseudomonas aeruginosa (100.3%), and Staphylococcus aureus (87.7%). The MIC, MBC/MFC, and MBIC values for ME were 0.5-1.0, 2-4, and 0.5-1.0 mg/mL and for EO were 0.31-0.62, 1.25-2.5, and 0.31-0.62 μL/mL, respectively, indicating inhibition potential as well as inhibition of biofilm formation. The tolerance test values indicated bactericidal activity against most strains and bacteriostatic/fungistatic activity against A. baumannii, E. faecalis, and C. albicans. The antiquorum sensing activity of ME achieved by pyocyanin inhibition assay on P. aeruginosa showed a 51.6% inhibition at 500 μg/mL. These results suggest that ME and EO derived from A. polystachyus leaves are potent, valuable, cost-effective antioxidants and antimicrobials. Both extracts may effectively combat pathogenic and resistant microbes.

LC-MS/MS Analysis and Biological Activities of Methanol Extract from Sagina apetala Ard.

This is the first study on the investigation of phenolic compounds of methanol extract (ME) of Sagina apetala and examination of its cell-based antioxidant and antibacterial activity against Staphylococcus aureus and Pseudomonas aeruginosa. The determination of phenolic compounds of ME was performed by LC-MS/MS and 25 main compounds were identified. For the cell-based antioxidant activity of ME, Vero cell line (Cercopithecus aethiops kidney epithelial, Monolayer) was used as the model cell line and ME was showed 61.22% cell viability. ME, also showed insignificant antibacterial activity against both gram-positive and gram-negative bacteria. In conclusion, this study in the species provides the basic data for future studies for the species.

Metabolomics analysis of Citrus medica var. sarcodactylis (Siebold ex Hoola van Nooten) Swingle and Limonia acidissima Linn. fruits and leaves in perspective to their antimicrobial potential.

Antimicrobial potential of Citrus medica var. sarcodactylis (Siebold ex Hoola van Nooten) Swingle and Limonia acidissima L. fruits and leaves extracts CMF, CML, LAF and LAL, respectively were evaluated. Gas chromatography-mass spectrometry (GC-MS) analysis for lipoidal matters revealed a high percentage of non-oxygenated compounds. Phytol was the major in LAL. Palmitic and linoleic acid were the major in CML and LAL, respectively. Rutin and P-hydroxy benzoic acid were the main compounds identified by High-performance liquid chromatography (HPLC) analysis. The antibacterial and antifungal activities of the plants extract were determined by the well diffusion method. Antimicrobial investigation for different successive fractions of active methanol extracts of CML, LAL, LAF and CMF showed the highest activity (CML), whereas the petroleum ether (CML PE) and MeOH (CML) fractions exhibit a significant antifungal activity against Candida albicans minimum inhibitory concentration (MIC) 12 and 15 µg/mL, respectively. The antifungal activity prevailed by C. medica leaves may be attributed to its polyphenolics (rutin, chlorogenic and rosmarinic acid) in addition to phenylated hydrocarbon.

A moderately active crude methanol extract from the whole plant of Kalanchoe crenata (Andrews) Haw. (Crassulaceae) strongly potentiated the effect of antibiotics against multidrug-resistant Gram-negative bacteria

Background: Resistant bacteria develop a high level of resistance to multiple drugs, limiting treatment options and increasing morbidity and mortality. This work was planned to evaluate the antibacterial potential of the methanol extract from the whole plant of Kalanchoe crenata (KCW) against multidrug-resistant (MDR) Gram-negative bacteria. Methods: The minimal inhibitory concentrations (MIC) and the minimal bactericidal concentrations (MBC) of KCW alone, in the presence of an efflux pump inhibitor (EPI) phenylalanine-arginine β-naphthylamide (PAβN), or in the presence of antibiotics were assessed using the broth microdilution method combined with the rapid para-iodonitrotetrazolium chloride (INT) colorimetric technique. Results: KCW displayed weak antibacterial activities with MIC values ranging from 128 to 1024 μg/mL against 10 of the 15 tested bacterial strains. Moderate antibacterial activities with MIC values ranging from 128-625 μg/mL were recorded against some strains belonging to Klebsiella pneumoniae, Escherichia coli, and Providencia stuartii. PAβN does not significantly enhance the activity KCW. At MIC/2, KCW potentiated the activity of doxycycline (DOX), levofloxacin (LEV), imipenem (IMI), ciprofloxacin (CIP), ceftriaxone (CRO), and tetracycline (TET) against at least 80% of the MDR bacterial strains tested. Conclusion: The present study demonstrated that KCW is a moderately active antibacterial agent, but a good efflux pump inhibitor that could potentiate the activity of antibiotics against MDR bacteria over-expressing active efflux pumps. Keywords: Antibacterial; antibiotic-potentiation; Crassulaceae; efflux pumps; Kalanchoe crenata; multidrug resistance.

Insecticidal effect of selected medicinal plants on Sitophilus zeamais Mostschulsky in stored maize

The aim of this study was to determine the insecticidal effect and phytochemical analysis of ten medicinal plant extracts against the maize weevil, Sitophilus zeamais (Order: Coleoptera Family: Curculionidae) on stored maize by using contact and repellency bioassays together with the evaluation of the Minimum Concentration of Lethality (MCL) of highly active Annona muricata. Out of the ten medicinal plant species tested, methanol extract of Annona muricata showed the highest mortality (100%) within 7 days. Repellency bioassay was done by using a Y-shaped glass tube. Ocimum selloi showed maximum (57.80 ± 21.2) repellency for the Sitophilus zeamais, while Ailanthus altissima and Eugenia caryophylata showed significant repulsion (46.67 ± 17.6) for this insect. The highly active methanol extract of A. muricata at the concentrations of 1000, 800, 600, 400, 200, and 100 ppm was tested against Sitophilus zeamais on stored maize and a 100% mortality was observed at a minimum concentration of 600 ppm. Preliminary results suggest that medicinal plants could be exploited for the isolation of insecticidal compounds. Phytochemical analysis was performed to ensure the presence of alkaloids, flavonoids, tannins, and saponins.

LC-MS/MS analysis and diverse biological activities of Hypericum scabrum L.: In vitro and in silico research

This study was designed to determine the phytochemical composition of Hypericum scabrum extracts and investigate their biologically prominent activities. LC-MS/MS analysis revealed the presence of 29 phytochemicals in the plant extracts. The methanol extract (ME) exhibited the strongest DPPH radical scavenging (IC 50 : 18.57 µg/mL) and ferric ion reducing capacity (74.20 mg TEAC/g). Besides, ME displayed the most promising α-glycosidase (IC 50 : 1.88 µg/mL) and acetylcholinesterase AChE (IC 50 : 8.41 µg/mL) inhibitory effect. The XTT assay results displayed the strong anti-proliferative activity of ME against MCF-7 (IC 50 : 56.45 µg/mL) and MDA-MB-453 (IC 50 : 67.79 µg/mL) cell lines. Flow cytometry studies confirmed the mitochondrial-dependent apoptotic effect of ME in MCF-7 cells. Finally, molecular docking studies revealed the best binding affinity of the compounds 1, 9, and 41 with AChE and α-Gly, while 41 exhibited the best affinity against caspase-3, caspase-9 and DNA. To conclude, this study provides essential data for further in vivo studies. • Phytochemical content and biological activities of Hypericum scabrum extracts were enlightened. • Methanol extract (ME) exhibited promising biological activities regarding metabolism and cancer. • •Flow cytometry results revealed the apoptotic effect of ME via mitochondria-dependent pathway. • The major phenolics showed best binding of with AChE, α-Gly, caspase-3, caspase-9 and DNA.

Bioactivity-Guided Fractionation and Identification of Antidiabetic Compound of Syzygium polyanthum (Wight.)'s Leaf Extract in Streptozotocin-Induced Diabetic Rat Model.

(1) Background: An earlier study on the hypoglycemic activity of S. polyanthum (Wight.) leaf methanol extract identified squalene as the major chemical compound. The present study was conducted to assess the hypoglycemic effect of fractions and subfractions of the methanol extract of S. polyanthum compared to the squalene using a bioassay-guided in vivo study. (2) Methods: The methanol extract was fractionated using the liquid–liquid fractionation method. Streptozotocin-induced type 1 diabetic rat was used to study the hypoglycemic effect. (3) Results: The findings showed that chloroform fraction significantly (p < 0.05) lowered blood glucose levels of diabetic rats as compared to the control. Further fractionation of chloroform fraction yielded subfraction-1 and -2, whereby subfraction-1 exhibited a higher blood-glucose-lowering effect. The lipid profile test showed that the total cholesterol level of subfraction-1 and squalene-treated groups decreased significantly (p < 0.05). An immunohistochemistry study revealed that none of the treatments regenerated pancreatic β-cells. Gas chromatography–mass spectrophotometer analysis identified the presence of squalene in the active methanol extract, chloroform fraction, and subfraction-1. In silico analysis revealed a higher affinity of squalene against protein receptors that control lipid metabolism than metformin. (4) Conclusions: Data obtained from the present work suggested the crude methanol extract exerted the highest hypoglycemic effect compared to fraction, subfraction, and squalene, confirming synergistic effect may be responsible for the hypoglycemic activity of S. polyanthum.

Phytochemical Analysis and Biological Evaluation of Hypericum linarioides Bosse: in Vitro and in Silico Studies

AbstractThe aim of this study is to determine the phenolic composition of Hypericum linarioides Bosse, to assess its various biological properties, and finally to confirm the experimental data of enzyme inhibitions via docking studies. LC‐MS/MS analysis performed over methanol extract (ME) revealed the presence of 27 phytochemicals. Antioxidant activity results indicated that ME had the strongest DPPH radical scavenging and ferric ion reducing capacity than water and hexane extracts. XTT assays revealed the strongest anti‐proliferative activity of ME against MCF‐7 and HT‐29 cancer cells. Flow cytometry results also confirmed the notable apoptotic effect of ME on MCF‐7 cells through mitochondria‐dependent pathway. Enzyme activity results exhibited the most promising acetylcholinesterase and α‐glycosidase inhibitory activities of the ME. Molecular docking calculations of α‐glycosidase with the major compounds (1, 15, 17 and 19) indicated that 17 (isoquercitrin) had the best docking binding energy (−10.92 kcal/mol) with appropriate binding interactions.

Green Synthesis of Antibacterial Silver Nanoparticles against Drug Resistant Bacteria

Background: Nanotechnology brings a massive revolution in the domain of medical biotechnology. Plants possess thousands of antimicrobial compounds; these compounds can be extracted and utilized in the production of medicines. Objective: The aim of this research is to design an economical method for the formation of nanoparticles from plants and explore their antibacterial activity. Methods: In the present study, we used the plants Aloe barbadensis, Azadirachta indica, Carica papaya, Mentha arvensis and Catharanthus roseus. Ethanolic, methanolic and aqueous extracts of the above mentioned plants were used to prepare silver nanoparticles. Antimicrobial activities of the nanoparticles of extracts were determined against pathogenic strains of bacteria. Results: Results showed that silver nanoparticles are formed from the ethanolic and methanolic extracts of Azadirachta indica, Carica papaya, Mentha arvensis and Catharanthus roseus and from the aqueous extracts of Aloe barbadensis and Mentha arvensis. It was observed that nanonoparticles of ethanolic extracts of Azadirachta indica, Carica papaya, Mentha arvensis and Catharanthus roseus exhibited the highest antibacterial activity against Pseudomonas specie, E.coli, Pseudomonas specie and S.typhi, respectively. On the other hand, the nanoparticles of methanolic extracts of Carica papaya, Mentha arvensis and Catharanthus roseus showed the highest inhibition against E.coli, whereas, maximum zone of inhibition of Pseudomonas was observed by the action of methanolic extract of Azadirachta indica. It is also found that nanoparticles of the aqueous extracts of Aloe barbadensis and Mentha arvensis inhibited the pathogenic strains and showed maximum activity against Pseudomonas and E.coli, respectively. Conclusion: The above results indicate that the nanoparticles formed from the extracts of the tested plants have high antimicrobial potential and could be utilized in the preparation of medicines to treat various disorders.

The modulation of PI3K/Akt pathway by 3β hydroxylup-12-en-28-oic acid isolated from Thymus linearis induces cell death in HCT-116 cells.

The presence of intricate carbon skeletons in natural compounds enhances their bioactivity spectrum with unique modes of action at several targets in various dreadful diseases like cancer. The present study was designed to purify the molecules from Thymus linearis and elucidate their antiproliferative activity. The compounds were isolated from the active methanolic extract of Thymus linearis through column chromatography and characterized by various spectroscopic techniques. Antiproliferative activity of isolated compounds was evaluated using MTT assay on cancer and normal cell lines. Mechanism of cell death was elucidated using flow cytometric, microscopic, and Western blot analysis. Four compounds, Sitosterol, Chrysin, 3β-hydroxylup-12-en-28-oic acid (3BH), and β-Sitosterol glycoside, were isolated. Among these, 3BH was most potent antiproliferative agent across all cell lines under study, HCT-116 being the most affected one. 3BH was demonstrated to downregulate PI3Ksubunits (p110α and p85α), downstream pAktSer473 and prompted G1 phase cell cycle arrest. The cell cycle CDK inhibitor p27 and p21 were upregulated with simultaneous downregulation of cyclin D1 and cyclin E in HCT-116 cells. This was accompanied by apoptosis, as depicted by decrease in Bcl-2/Bax ratio, with increase in active caspases-3 and caspase-9, cleavage of PARP-1, the generation of reactive oxygen species (ROS), and the loss of mitochondrial membrane potential. The findings established that 3BH induced cell death in HCT-116 cells by modulating PI3K/Akt signaling axis, impeding cell cycle, and instigating apoptosis.

CHROMATOGRAPHIC, INFRARED SPECTRAL AND ANTI-INFLAMMATORY STUDIES OF ETTHYL ACETATE AND METHANOL EXTRACT OF THE SEED OF D. EDULIS

The seed powder of Dacryodes edulis were extracted using n-hexane, ethyl acetate and methanol by the cold maceration method. The crude Methanol and ethyl acetate extracts were then biologically assayed for acute toxicity (LD50) using the method of Lorke (1983). Anti-inflammatory activities of the crude were also assayed using male albino rats. The most biologically active (methanol extract) was separated using series of column chromatography (CC) and thin layer chromatography (TLC). The extractives coded DEF, DEH, DEJ and DEK, respectively were then characterized using infra-red (IR) spectroscopy and gas chromatography-mass spectrometry (GC-MS). All the results obtained were statistically analyzed using analysis of variance. The acute toxicity studies showed that even at higher concentration of 5000mg/kg, the extracts were not lethal to all the animals used. The anti-inflammatory analysis showed that the methanol extract had the highest anti-inflammatory activities. The IR for the methanol extractives showed the following λ max: (3500-3200) for the O-H stretch of alcohols and phenols, 3391.9 and 3354.6 for the N-H stretch of amines and amides, 3261.4 for the O-H stretch of carboxylic acids, 2948.3 and 2847.7 for the C-H stretch of alkanes, 1431.3 and 1386.6 for the C-H bend of alkanes and 1364.2 for C-H rocking of alkanes. Also 2836.5 for the C-H stretch of aldehydes, 2210.3 for the C=N stretch of nitriles,1736.9 1699.7 and 1013.8 for the C=O stretch of aldehydes, ketones and carboxylic acids. Equally 1643.2 and1636.9 for the C=C stretch of alkenes and 1576.7 for the C=C stretch of aromatic ring. These functional groups correspond to some of the compounds listed in the GC-MS library suggestions such as tetra- decanoic acid, hexa-decanoic acid, octadecanoic acid, vaccenic acid, catechol, 2, 4-di-tert- butylphenol and others. Presence of N-H group of amines and amides the GC-MS suggested presence of tri-(2-aminoethylamine,3,3,3-trifluoro-N-(2-fluoro-phenyl-2-(trifluoro methyl)methyl propionamide etc. The C=C of alkenes agreed with the suggested presence of cetene and bi-cyclo (10,10) tridec-1-ene and others. The non- toxic nature of the seed and its ability to reduce inflammations gives credence to its use in traditional medicine practice.

Phenolics from Mangifera Indica (Tommy Atkins) peels and assessment of its Anticancer Activity

The aim of this study is to investigate the chemical and biological activity of Mangifera indica L. cv. peels extract, resulted that the methanolic extract of Mangifera indica L. cv. peels contains a complicated mixture of phenolics, which includes mainly gallotannins as previously detected by 2D paper chromatographic screening. and characterized by high-performance liquid chromatography (HPLC)to prove the presence of 13 compounds, five major compounds namely, Gallic acid (24621.70 µg/g), Naringenin(2624.57µg/g), vanillin (1322.85µg/g), Catechin(12681.37µg/g), Chlorogenic acid(638.08µg/g). potentially biologically active methanolic extract becomes much more efficient after identification of all compounds in that mixture. The invitro Cytotoxic activities by using SRB assay, of methanolic extract from mango (Mangifera indica L. cv. “Tommy Atkins”) peels Moderately effective against Cervical (HELA) cell line with IC50 25μg/ml. and weakly effective against Breast (MCF7) cell line with IC50 44 μg/ml. All identified phenolic compounds are therapeutically active compounds with anticancer potency which was reported for the first time.

GC-MS Analysis, Phytochemical Screening and Biological Activity of Bauhinia tomentosa (Linn.)

Present study aimed to evaluate the chemical composition and biological activity for methanolic extract of Bauhinia tomentosa (Linn.) leaves grown in Western Ghats region of South India. The preliminary phytochemical screening tests revealed the presence of steroids, alkaloids, terpenoids, flavonoids, glycosides and phenolic compounds in the leaf extract. A total of 19 compounds were identified through gas chromatography-mass spectroscopy (GC-MS) analysis of methanolic extract of B. tomentosa. The major compounds identified were phytol (23.96%), n-hexadecanoic acid (11.62%), squalene (8.85%) and the minor compounds are trans-bis(2-methylpropyl)-4,6-dioxane(0.13%), dihydro-cis-α-copaene-8-ol (0.14%), tetradecanoic acid (0.81%), respectively. Antibacterial activity of the extract showed the zone of inhibition 18 mm at 200 μg/mL against S. aureus, followed by 15 and 16 mm against S. anginosus, K. pneumoniae at 200 μg/mL, respectively. Antioxidant activity of methanolic extract of B. tomentosa leaves showed the maximum IC50 value with 75.07 % of scavenging activity at the concentration of 5 μg/mL.

Anti-inflammatory and analgesic activities of Neolamarckia cadamba and its bioactive monoterpenoid indole alkaloids

Ethnopharmacological relevanceNeolamarckia cadamba has been used traditionally to treat inflammation, fever, and pruritus in the Dai ethnopharmacy in Yunnan province, P.R. China. However, according to literature survey, the action basis of anti-inflammatory and analgesic activities of this plant were rarely reported, which accounts for the original intentions of this investigation. Aim of the studyThe study aimed to investigate the anti-inflammatory and analgesic action of methanolic extract (ME), ethyl acetate (EA), and aqueous (AQS) fractions of N. cadamba and further explore the accurate compounds responsible for the activities of EA fraction. Materials and methodsThe in vivo anti-inflammatory and analgesic activities of ME, EA, and AQS fractions at the doses of 200 and 400 mg/kg and two major constituents (compounds 5 and 7) at 50 and 100 mg/kg via intragastrically administrated, respectively, were evaluated by carrageenan-induced paw edema and acetic acid-stimulated writhing animal models. Aspirin (ASP) was used as the positive control at the dose of 200 mg/kg. The monoterpenoid indole alkaloids (MIAs) in EA fraction were phytochemically studied utilizing chromatographic techniques, and their structures and absolute configurations were established on the basis of multiple spectroscopic analyses and quantum computational chemistry method. Moreover, the in vitro anti-inflammatory activities of all the isolates were assessed by suppressing releases of LPS-activated inflammatory mediators (TNF-α, IL-1β, and COX-2) in RAW 264.7 macrophage cells at a concentration of 10 μg/mL. Dexamethasone (DXM) was used as the positive control. ResultsThree fractions (ME, EA, and AQS) significantly ameliorated the paw edema caused by carrageenan and reduced the number of writhing induced by acetic acid in comparison to the control group at the doses of 200 and/or 400 mg/kg (in vivo). Subsequent phytochemical investigation of EA fraction led to the structural characterization of four new monoterpenoid indole alkaloids, neocadambines A–D (1–4), as well as eight known analogues (5–12). Neocadambine A possesses a novel 14-nor-MIA skeleton that could be derived from the corynantheine-type MIAs via oxidative cleavage of C3–C14 bond and subsequently degradation of C14. Moreover, the structure of a bioactive known MIA, cadambine acid (6), was reassigned by analysis of its NMR spectroscopic data. Further biological assays revealed that the major constituent 3β-dihydrocadambine (7) significantly relieved the paw edema and decreased the number of writhing at 100 mg/kg in vivo. In addition, most of the isolates displayed remarkable in vitro anti-inflammatory effects by inhibiting the secretion of aforementioned inflammatory mediators (COX-2, IL-1β, and TNF-α) at a concentration of 10 μg/mL, and compounds 4, 7, and 9 showed better anti-inflammatory effects than that of positive control, dexamethasone. ConclusionsThis study further validated the anti-inflammatory and analgesic activities of N. cadamba, and revealed that monoterpenoid indole alkaloids could partly contribute to the efficacy of this ethnodrug. The major constituent 3β-dihydrocadambine (7) showed significant anti-inflammatory activities both in vitro and in vivo, which suggested that it could be a promising anti-inflammatory lead compound. Our findings provided scientific justification to support the traditional application of N. cadamba for treating inflammatory and nociceptive disorders.

ANTIOXIDATIVE AND FREE RADICAL SCAVENGING POTENTIALS OF HABENARIA PECTINATA

Objective: This study was designed to evaluate the antioxidative potential of tubers of Habenaria pectinata.&#x0D; Methods: The tubers of H. pectinata were extracted using hexane, ethyl acetate, methanol, and water as solvents. The anti-oxidant potential of extracts was evaluated using free radical scavenging and reducing power assays. The most active methanolic extract was then fractionated into four fractions using the above-mentioned solvents.&#x0D; Results: The phenol and flavonoid content was found to be maximum in the methanol extracts. All the extracts and fractions showed significant levels of antioxidant activity except hexane extract.&#x0D; Conclusion: The tubers of H. pectinata were found to possess a significant antioxidant potential and can be explored further for isolation and preclinical investigation for the ailment of various diseased states and disorders.

Larvicidal efficacy of Andrographis paniculata and Tinospora cordifolia against aedes aegypti: A dengue vector

Background: Aedes aegypti, dengue fever mosquito, is predominantly accompanying the transmission of dengue in tropical and subtropical countries of the world, causing millions of deaths every year. Materials and Methods: The current research was carried out to evaluate the larvicidal efficiency of Andrographis paniculata and Tinospora cordifolia against third instar larvae of A. aegypti using in silico and experimental study. Results: The methanolic extract of A. paniculata and ethanolic extract of T. cordifolia showed the highest larvicidal activity with LC50 and LC90 value of 15.75 ppm; 349.60 and 100.64 ppm; 386.37 ppm, respectively after 48 h exposure, which was statistically significant (P = 0.05). However, the combined action of methanolic extract of A. paniculata + ethanolic (50:50) extract of T. cordifolia and the bioactive fraction of methanolic extract of A. paniculata showed the effective larvicidal activity with LC50 value of 113.20 ppm and 236.08 ppm respectively after 24 h treatment which was statistically significant (P = 0.05). The m/z values in liquid chromatography-mass spectrometry graph of bioactive fraction of methanolic extract of A. paniculata predicted the possible amount of bioactive compound class like flavone, phenols, phenylpropanoids, flavonoids, phenolic acid, alkaloids, isopalmitic acid, diterpenoids and quinic acid. The best energy binding affinity score against sterol carrying protein-2 of A. aegypti, panicolin (-9.86 kcal/mol), berberine (-10.13 kcal/mol) and their combination (50:50) showed effective larvicidal movement with LC50 value of 25.41 ppm, 23.15 ppm and 17.56 ppm after 24 h treatment. Conclusion: The crude extracts, bioactive fractions and synthetic bioactive compounds and their combination study of A. paniculata and T. cordifolia can be utilized as bio-control agents against A. aegypti mosquito.

Velvet antler methanol extracts (MEs) protects against oxidative stress in Caenorhabditis elegans by SKN-1

Velvet antler is one of the most important animal medicines or functional foods widely used in East Asia for many centuries, which has several biological activities including anti-ageing and health promotion. To date, the mechanism underlying these effects of velvet antler is widely studied by its protein or polypeptide components. Few studies have been reported for the function of the other components in velvet antler. Herein, C. elegans is used as the model animal to dissect how none protein components of velvet antler affect in vivo oxidative stress. Methanol extracts (MEs) from velvet antler which has few protein components extends the maximum lifespan of C. elegans compared to the control under oxidative stress, while water extracts (WEs) which is protein-rich component has no apparent function. The activity of MEs is mediated by clk-1 signaling pathway, but not via daf-2, eat-2 or glp-1 pathway. Further investigations show MEs decrease endogenous ROS by promoting SKN-1 nuclei translocation, subsequently up-regulating the expression of its target genes gst-4, gst-7 and gst-10 in C. elegans. In all, MEs, the none protein components of velvet antler, protects against oxidative stress in C. elegans, which indicates it might be a product with potential of being a curative medicine.