Biochemical and molecular anticancer approaches for Boerhaavia diffusa root extracts in oral cancer.

Background: Boerhaavia diffusa is a medicinal herb with anti-inflammatory, antiproliferative, anticancer, and immunomodulatory properties, found across India. Aim and Objectives: The present study is designed to investigate the therapeutic potential for B. diffusa root extracts in oral cancer cell line. Materials and Methods: The aqueous and methanolic extracts of B. diffusa were prepared using Soxhlet apparatus. In order to determine the phytochemical constituents of B. diffusa, the extracts were subjected to gas chromatography-mass spectrometry analysis. The antioxidant potential of B. diffusa extracts was assessed by 2,2-Diphenyl-picrylhydrazyl, ferric ion-reducing antioxidant power, catalase and peroxidase assays. The effective concentration of B. diffusa root on cell viability was analyzed by [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay. The ability of B. diffusa root extracts to modify the cell-cycle phases was performed by FACS analysis. The apoptotic inducing potential of B. diffusa in oral cancer cells was confirmed by acridine orange-ethidium bromide and 4',6-diamidino-2-phenylindole staining. The protein profile of apoptotic processes was validated by the Western blot analysis; docking studies were also performed. Results: We observed that antioxidant activity was higher in B. diffusa methanolic extract compared with aqueous extract. The results showed that the methanolic and aqueous extracts of B. diffusa exhibited significant cytotoxic effect with IC50 value of 36 µg/ml and 30 µg/ml, respectively. The apoptotic DNA fragmentation and the apoptotic inducing potential in KB oral cancer cell line were higher for the methanolic extract compared with the aqueous extract. These results were also confirmed by in-silico analysis. Conclusion: The results indicate that extracts obtained from the roots of B. diffusa inhibit the progression of oral cancer. These compounds of pharmacological importance can be either used alone or in combination with other drugs to treat oral cancer.

Composition, Color Stability and Antioxidant Properties of Betalain-Based Extracts from Bracts of Bougainvillea.

Betalains in bracts of Bougainvillea are of great application potential as natural food colorants and antioxidants. This study explored the color, spectra, composition, storage stability, and antioxidant properties of betalain-based Bougainvillea bracts extracts (BBEs) to verify their application value. The results showed that Bougainvillea bract color variance is due to varied contents and proportions of betacyanins (Bc) and betaxanthins (Bx). Bc or Bx alone determined hues of purple or yellow, respectively; the co-existence of Bc and Bx would produce varied hues of red. BBEs showed bright color and good antioxidant properties under a wide pH range. The pH range of 5−6 was optimal for the highest color stability, and pHs 3−8 were optimal for stronger antioxidants. Bc mainly underwent color fading during storage, while Bx easily produced dark precipitates or melanism under strong acidic (pH < 4) or alkaline conditions (pH > 8). However, Bougainvillea Bx showed 3−4 times higher antioxidant ability than Bc. Different considerations for Bc and Bx are needed for varied application purposes. The purple bracts containing only Bc would be more suitable as colorant sources, while additional Bx can bring enhancement of antioxidant ability and richness of Bougainvillea extract color.

Evaluation of Nutritional Substances and Investigation of Antioxidant and Antimicrobial Potentials of Boerhavia diffusa with in Silico Molecular Docking.

Boerhavia diffusa L. Nyctanginaceae (B. diffusa) is a medicinal herb commonly considered as a weed. The exploration of phytochemicals in different parts of B. diffusa with different solvents will create awareness, along with the suitable solvent and method for extraction of pharmaceutical compounds. Hence, the present study focuses on phytochemical analysis of B. diffusa leaves, stems, and roots in various solvents with hot and cold extraction. The decoctions performed well in most of the qualitative and quantitative tests, along with the DPPH assay. The aqueous extract showed a good result in the FRAP assay and ABTS assay. In the antimicrobial test, the B. diffusa root ethanol extract inhibited the growth of Pseudomonas aeruginosa and Staphylococcus aureus with zones of inhibition of about 8 mm and 20 mm at 200 µg concentration, respectively. Using a molecular docking approach, the top four ranked molecules from the crude extract of B. diffusa profiled from GC-MS spectroscopy in terms of growth inhibition of the pathogenic bacterium P. aeruginosa were selected; among them, 2-(1,2 dihydroxyethyl)-5-[[2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-3,4-dihydrochromen-6-yl]oxy]oxolane-3,4-diol exhibited the minimum binding score, revealing high affinity in complex. B. diffusa is highly nutritious, and the maceration and decoction extracts were similar except for the chloroform extract that was found to be weak.

Computational study to evaluate the potency of phytochemicals in Boerhavia diffusa and the impact of point mutation on cyclin-dependent kinase 2-associated protein 1.

A protein's function is closely related to its structural properties. Mutations can affect the functionality of a protein. Different cancer tissues have found disordered expression of the cyclin-dependent kinase 2-associated Protein 1 (CDK2AP1) gene. A protein molecule's conformational flexibility affects its interaction with phytochemicals and their biological partners at various levels. Boerhavia diffusa has been investigated most extensively for its medicinal activities like anticancer properties. It contains many bioactive compounds like Boeravinone A, Boeravinone B, Boeravinone C, Boeravinone D, Boeravinone E, Boeravinone F, Boeravinone G, Boeravinone H, Boeravinone I and Boeravinone J. We have studied to analyse the binding efficacy properties as well as essential dynamic behaviour, free energy landscape of both the native and mutant protein CDK2AP1 with bioactive compounds from Boerhavia diffusa plant extracts through computational approaches by homology modelling, docking and molecular dynamics simulation. From the molecular docking study, we found that. Boeravinone J have best binding affinity (-7.9 kcal/mol) towards the native protein of CDKAP1 compared to others phytochemicals. However, we found the binding energy for H23R and C105R (mutation point) -7.8 and -7.6 kcal/mol, respectively. A single minima energy point (from 100 ns molecular dynamics simulation study) was found in the H23R mutant with Boeravinone J complex suggested that minimum structural changes with less conformational mobility compared C105A mutant model.Communicated by Ramaswamy H. Sarma.

Anxiolytic, antidepressant and inhibitory effect on MAO isoenzymes by Bougainvillea glabra flower extract in rats.

Main aim of current study was to determine the anxiolytic and antidepressant potential of Bougainvillea glabra Extract (BVE). The effects were investigated by using Open-Field-Test (OFT), Light-and-Dark Model (LD), Hole-Board (HB) and Forced-Swimming-Test (FST). Different doses for BVE were given to Wistar-Rats and compared with Control and Diazepam. Data has been collected by simple observations of animal behaviors in mentioned models. Collected data was analyzed by SPSS-22 version. In OFT (number of squares travelled), significant differences noted between Control and BV100mg/kg (p=0.001), Diazepam and BV100mg/kg (p=0.0001), Diazepam and BV200mg/kg (p=0.015), Diazepam and BV300 mg/kg (p=0.002). In LD-Test, significant differences were noted between Control and BV100mg/kg, BV200mg/kg and BV300mg/kg (p=0.0001), Diazepam and BV100mg/kg, 200mg/kg (p=0.0001), Diazepam and BV300mg/kg (p=0.028). In HB-Test by head dips, significant differences noted between control group and BV100mg/kg and 200mg/kg (p=0.0001), Control group and BV300mg/kg (p=0.005). For number of head dips, significant differences noted between Diazepam and BV100mg/kg, 200mg/kg and 300mg/kg (p=0.0001). In FST, significant differences were observed between Control group and BV100mg/kg, BV200mg/kg and BV300mg/kg (p=0.0001), Fluoxetine and BV100mg/kg, BV200mg/kg and BV300mg/kg (p=0.0001). It is observed that MAO-A and MAO-B are inhibited by BVE. Study demonstrates that BV flowers have anxiolytic and antidepressant activities.

Boerhaavia diffusa Extract Acts as a Specific Antituberculosis Agent in Vitro Against Mycobacterium tuberculosis H37Rv Infection.

The present study investigated Boerhaavia diffusa extract against Mycobacterium tuberculosis H37Rv (M.tb) infection in vitro and explored the underlying mechanism. The study demonstrated that Boerhaavia diffusa extract significantly (p < 0.05) reduced RAW 264.7 and A549 cell viability in concentration dependent manner. In BEAS-2B, NuLi-1 cells and splenocytes no significant (p > 0.05) reduction in viability was observed on treatment with 2.5 to 20 mg/L concentrations of Boerhaavia diffusa. The M. tb­induced increase in TNF­α expression was significantly (p < 0.05) reversed by Boerhaavia diffusa treatment in RAW 264.7 and BEAS-2B cells. Moreover, Boerhaavia diffusa treatment significantly (p < 0.05) inhibited M.tb­induced increase in IL-6 and IL­1ß expression in RAW 264.7 and BEAS-2B cells. Boerhaavia diffusa treatment of RAW 264.7 and BEAS-2B cells significantly (p < 0.05) reversed M.tb­induced increase in iNOS and COX­2 expression. Additionally, in Boerhaavia diffusa treated cells M.tb­induced increase in NO release was significantly (p < 0.05) reduced compared to untreated cells. In summary, Boerhaavia diffusa treatment inhibits pro-inflammatory cytokine production, NO release and regulate immunomodulatory mediators in M.tb­infected RAW 264.7 and BEAS-2B cells. Therefore, Boerhaavia diffusa may be developed as a therapeutic agent for treatment of M.tb­infection.

A Review on Rotenoids: Purification, Characterization and its Biological Applications.

Phytochemicals play a vital role as drugs for the treatment of various autoimmune, viral, and cancerous diseases. Rotenoids, a type of isoflavone compounds present in plants genus Boerhaavia sp., Mirabilis sp. and Abronia sp. which belong to the Nyctaginaceae family, are traditionally used as pesticides and insecticides. Boeravinones are groups of rotenoid compounds widely used as drugs or drug adjuvants for the treatment of various diseases. Extraction of rotenoids in various solvents, purification of rotenoids in various chromatographic technique studies, and the characterization of functional groups of rotenoids in various spectroscopic techniques have been reported. Biological applications of rotenoids such as anti-cancerous, antioxidant, anti-inflammatory, antimicrobial, and cytotoxic activities have been discussed. This review summarizes the extraction, isolation, purification, and characterization of rotenoid compounds and their effect on the treatment of cancer, inflammatory, spasmolytic, autoimmune, and microbial diseases.

Bougainvinones NP, three new flavonoids from Bougainvillea spectabilis.

In an effort to identify natural bioactive compounds, three new flavonoids (1-3) and six known compounds (4-9) were isolated from the stem bark of Bougainvillea spectabilis. The structures of these compounds were accomplished using comprehensive spectroscopic methods, including 1D and 2D NMR spectra with references to the literatures, as well as high-resolution mass spectrometric analysis. Their cytotoxicity against KB and HeLa S-3 cell lines was also evaluated.

Bougainvillea glabra (choisy): A comprehensive review on botany, traditional uses, phytochemistry, pharmacology and toxicity.

ETHNOPHARMACOLOGICAL RELEVANCE: Bougainvillea glabra (Choisy). (Family: Nyctinaginacea) is a valuable ornamental plant with culinary uses and also utilized in traditional medicine for treating common ailments. It is traditionally employed against several diseases such as diarrhoea, hypotension, intestinal disorders, stomachache, nausea, inflammation-related ailments, and in pain management. Though widely validated via in vitro and in vivo models, to date no endeavour has been made to compile in a single review the traditional, phytochemistry and pharmacological properties of B. glabra. AIMS: To provide an up-to-date, authoritative review with respect to the traditional uses, chemical composition, in vitro and in vivo pharmacological properties, and toxicological estimations accomplished either utilizing the crude extracts or, wherever applicable, the bioactive compounds isolated from B. glabra. Besides, a critical evaluation of the published literature has been undertaken with regards to the current biochemical and toxicological data. MATERIALS AND METHODS: Key databases per se, Ovid, Pubmed, Science Direct, Scopus, and Google scholar amongst others were probed for a systematic search using keywords to retrieve relevant publications on this plant. A total of 52 articles were included for the review depending on Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) guidelines. RESULTS: The studies conducted on either crude extracts, solvent fractions or isolated pure compounds from B. glabra had reported a varied range of biological effects comprising antibacterial, antifungal, antidiabetic, cytotoxic, analgesic, antipyretic, anti-inflammatory, and antioxidant activities. Phytochemical analysis of different parts of B. glabra unveiled 105 phytochemicals, belonging to phenolic, flavonoid, betacyanin, terpenoid, glycoside and essential oils classes of secondary metabolites. CONCLUSION: Most of the pharmacological activities of crude extracts from this plant have been reported. A very few studies have reported the isolation of compounds responsible for observed biological potential of this plant. Moreover, the toxicity studies of this plant still need to be explored comprehensively to ensure its safety parameters. Additional investigations are recommended to transmute the ethnopharmacological claims of this plant species in folklore medicines into scientific rationale-based information.

The leaves of Bougainvillea spectabilis suppressed inflammation and nociception in vivo through the modulation of glutamatergic, cGMP, and ATP-sensitive K+ channel pathways.

ETHNOPHARMACOLOGICAL RELEVANCE: Bougainvillea spectabilis is an ornamental shrub from Nyctaginaceae family, widely used in the traditional medicine in the treatment of pain, inflammation, and ulcer. Some research investigated the analgesic potential of this plant, however, the in-depth analysis of its antinociceptive properties and molecular mechanism(s) are yet to be revealed. PURPOSE OF THE STUDY: This study, therefore, investigated the antinociceptive potential of methanol extract of the leaves of B. spectabilis (MEBS) with possible molecular mechanism(s) of action using several pre-clinical models of acute and chronic pain in mice. MATERIALS AND METHODS: The dry leaf powder of B. spectabilis was macerated with 100% methanol, and then dried crude extract was used for in vivo experiments. Following the acute toxicity test with 500, 1000, and 2000 mg/kg b.w. doses of MEBS, the central antinociceptive activities of the extract (50, 100, and 200 mg/kg b.w.) were evaluated using hot plate and tail immersion tests, whereas the peripheral activities were investigated using acetic acid-induced writhing, formalin-induced licking and oedema, and glutamate-induced licking tests. Moreover, the possible involvements of cGMP and ATP-sensitive K+ channel pathways in the observed antinociceptive activities were also investigated using methylene blue (20 mg/kg b.w.) and glibenclamide (10 mg/kg b.w.), respectively. We also performed GC/MS-MS analysis of MEBS to identify the phyto-constituents and in silico modelling of the major compounds for potential molecular targets. RESULTS: Our results demonstrated that MEBS at 50, 100, and 200 mg/kg b.w. doses were not effective enough to suppress centrally mediated pain in the hot plate and tail immersion models. However, the extract was potent (at 100 and 200 mg/kg b.w. doses) in reducing peripheral nociception in the acetic acid-induced writhing and inflammatory phase of the formalin tests. Further analyses revealed that MEBS could interfere with glutamatergic system, cGMP and ATP-sensitive K+ channel pathways to show its antinociceptive properties. GC/MS-MS analysis revealed 35 different phytochemicals with potent anti-inflammatory and antinociceptive properties including phytol, neophytadiene, 2,4-Di-tert-butylphenol, fucoxanthin, and Vit-E. Prediction analysis showed high intestinal absorptivity and low toxicity profiles of these compounds with capability to interact with glutamatergic system, inhibit JAK/STAT pathway, scavenge nitric oxide and oxygen radicals, and inhibit expression of COX3, tumor necrosis factor, and histamine. CONCLUSION: Taken together, these results suggested the antinociceptive potentials of MEBS which were mediated through the modulation of glutamatergic, cGMP, and ATP-sensitive K+ channel pathways. These also suggested that MEBS could be beneficial in the treatment of complications associated with nociceptive pain.

Phytochemical profiling, antioxidant, enzyme inhibition and cytotoxic potential of Bougainvillea glabra flowers.

In this study, phytochemical composition, antioxidant, enzyme inhibition and cytotoxic activities of methanol and dichloromethane (DCM) extracts of Bougainvillea glabra (B. glabra) flowers were investigated. Methanol extract was found to have higher total bioactive contents and UHPLC-MS analysis of methanol extract revealed the presence of well-known phenolic and flavonoid compounds. Antioxidant activities were performed by radical scavenging (DPPH and ABTS), reducing power (FRAP and CUPRAC), phosphomolybdenum (TAC) and metal chelating assays. From our result, we observed that methanol extract had many antioxidant compounds. The DCM extract exhibited higher cholinesterases and α-glucosidase enzyme inhibition, while methanol extract showed significant urease inhibition. Both extracts exhibited strong to moderate cytotoxicity against MCF-7, MDA-MB-231, CaSki, DU-145 and SW-480 cancer cells with IC50 values ranging from 88.49 to 304.7 µg/mL. The findings showed the B. glabra to possess considerable antioxidant, enzyme inhibition and cytotoxic potentials and therefore has potential to discover novel bioactive molecules.

Prophylactic efficacy of Boerhavia diffusa L. aqueous extract in toluene induced reproductive and developmental toxicity in Drosophila melanogaster.

BACKGROUND: Environmental exposure to toxicants poses high risk to develop reproductive and developmental chronic toxicity in man. Toluene is one of the commonest industrial agents whose exposure is attributed with potential to induce reproductive and developmental toxicity. Since they contaminate the immediate environment of air and water to which humans are exposed, its containment is of great public health importance. Conventional treatment modalities fail owing to the difficulty to detect these highly volatile agents in environment and human body. The peril of such hazardous exposures is evident only when irreversible structural and functional damages have incurred. In such instances, prevention gains an upper hand when compared to therapeutic interventions. Several natural compounds derived from medicinal herbs possess potential to curb toxicities induced by such xenobiotic agents. Among them Boerhavia diffusa Linn. is a widely distributed and common herb attributed with antitoxic potential and capability for antioxidant defence. A study was performed on the prophylactic efficacy of aqueous extract of B. diffusa in curbing toluene induced developmental toxicity in Drosophila melanogaster. METHODS: The study consisted of a preliminary phytochemical screening and HPTLC profiling of B. diffusa aqueous extract (BDAE). LC50 of toluene was assessed and a sublethal dose of 200ppm was fixed for the study. Four doses of BDAE; 25, 50, 100 and 200mg/ml designated as Low dose, medium dose 1, medium dose 2 and high dose was used for the study. The parameters used for the study included the determination of larval period, pupal period, percentage of egg hatching, morphometric analysis of egg, larvae, pupae and adults, fertility, fecundity, lifespan and levels of antioxidant enzymes such as catalase, glutathione-S-transferase and superoxide dismutase. RESULTS: The phytochemical and HPTLC characters were as per the pharmacopoeial standards. LC50 of toluene was found to be 430ppm in this study. BDAE at medium dose 2 and high dose significantly prevented the deterioration of reproductive and developmental toxicity parameters of larval period, pupal period, percentage of egg hatching, morphometric characters of larva, pupa and adult, fertility, fecundity and lifespan in drosophila. Also the drug significantly elevated the levels of antioxidant enzymes. CONCLUSION: Toluene exposure during lifetime is inevitable. B. diffusa, equipped with its rich active ingredients prevented toluene induced developmental and reproductive toxicity in Drosophila. This medicinal herb provides a ray of hope in preventing environmental toxin induced reproductive and developmental toxicity.

Hepatoprotective effects of ethanolic extract of Boerhaavia diffusa against oxaliplatin induced hepatotoxicity in albino rats.

The hepatoprotective effects of Boerhaavia diffusa was studied against the hepatotoxicity induced by oxaliplatin. Male Wistar rats were divided in three groups.Group N* control group (0.9% normal saline), Group NP0 oxaliplatin treated group and Group NP2 were prophylactically treated with Boerhaavia diffusa and then with oxaliplatin in order to assess the protective effects of Boerhaavia diffusa against the toxicity of oxaliplatin. The levels of liver enzymes ALT, AST and γ-GT were significantly reduced in the group prophylactically treated with Boerhaavia diffusa (NP2) compared with the group treated with oxaliplatin (NP0). Boerhaavia diffusa was effective in reducing risk of hypercholestremia associated with oxaliplatin. Histopathological examination of rat liver revealed that prophylactically treated group with Boerhaavia diffusa was effective in reducing oxidative stress induced steatohepatitis by oxaliplatin.

Bougainvillea flower extract mediated zinc oxide's nanomaterials for antimicrobial and anticancer activity.

The zinc oxide nanomaterials (ZnO-NMs), owing to their broad biomedical applications have lately attracted the incredible interest in the development of therapeutic agents against microbial infections. In this contribution, we have biosynthesized ZnO-NMs with a size of ˜ 40 nm from the Bougainvillea flower extracts. The FTIR and SEM-EDX mapping analysis confirmed the size, shape and biogenic origin of ZnO-NPs. Furthermore, the purified ZnO-NMs were applied for antibacterial studies against susceptible and resistant bacterial strains and to elucidate the possible mechanism of their activity. The XTT assay and confocal imaging confirmed the ZnO-NMs materials anti-biofilm activities against medically important pathogens, i.e., S. aureus and E. coli. Moreover, the absence of cytotoxicity against healthy kidney cells (HEK-293) and erythrocytes confirmed their biocompatible nature. Furthermore, the biosynthesized ZnO-NMs showed potent anticancer activity against the breast cancer cell line (MCF-7). These biosynthesized ZnO-NMs are having excellent antimicrobial and anticancer activities and are highly biocompatible due to biogenic nature. During antimicrobial study, Zno-NMs showed excellent minimum inhibitory concentration 16 µg concentration againt E. coli, P. aeruginosa and S. aureus. While in anticancer activity, of ZnO-NMs with 15 µg/ml dose showed good response against MCF-7 cell line. Further, this killing was mechanically confirmed by ROS generation by the ZnO-NMs, which cause cell lysis by the peroxidation of membrane lipid. So, this biogenic ZnO-NMs can be used in the future for nanomaterial-based drug development.

Extract from Bougainvillea xbuttiana (Variety Orange) Inhibits Production of LPS-Induced Inflammatory Mediators in Macrophages and Exerts a Protective Effect In Vivo.

BACKGROUND: Different pharmacological properties, such as antioxidant, antiproliferative, and anti-inflammatory properties, have been described among natural products. We previously described that the Bougainvillea xbuttiana (Variety Orange) ethanolic extract (BxbO) has an anti-inflammatory effect; however, this action is not fully understood. In this study, the action of the BxbO extract on the secretion of inflammatory mediators in two experimental models, in vitro and in vivo, after LPS challenge was evaluated. METHODS: Peritoneal macrophages were obtained from female BALB/c mice and LPS-challenged with or without the BxbO extract. For the evaluation of mediators, the supernatants at 0, 12, 24, 36, and 48 hours were collected. For in vivo estimation, groups of female BALB/c mice were first intraperitoneously injected with different amounts of LPS and later administered the oral BxbO extract (v.o.) for 144 hours. To understand the mechanism of action, sera obtained from mice were collected at 0, 2, 4, 8, 12, and 24 hours after LPS challenge (with or without BxbO) for the detection of mediators. RESULTS: The results showed that, in both peritoneal macrophages and sera of mice treated with the BxbO extract 1 hour before or together with LPS challenge, proinflammatory cytokines and nitric oxide release were unquestionably repressed. In contrast, in both systems studied here, the IL-10 levels were elevated to 5 to 9 times. At lethal doses of LPS, the BxbO extract treatment was found to protect animals from death. CONCLUSIONS: The results revealed that the inhibitory, protective, and benign effects of the BxbO extract were due to its capacity to balance the secretion of mediators.

Multidirectional insights into the biochemical and toxicological properties of Bougainvillea glabra (Choisy.) aerial parts: A functional approach for bioactive compounds.

The current research work was conducted in order to probe into the biochemical and toxicological characterisation of methanol and dichloromethane (DCM) extracts of Bougainvillea glabra (Choisy.) aerial parts. Biological fingerprints were assessed for in vitro antioxidant, key enzyme inhibitory and cytotoxicity potential. Total bioactive contents were determined spectrophotometrically and the secondary metabolite components of methanol extract was assessed by UHPLC mass spectrometric analysis. The antioxidant capabilities were evaluated via six different in vitro antioxidant assays namely DPPH, ABTS (free radical scavenging), FRAP, CUPRAC (reducing antioxidant power), phosphomolybdenum (total antioxidant capacity) and ferrous chelating activity. Inhibition potential against key enzymes urease, α-glucosidase and cholinesterases were also determined. Methanol extract exhibited higher phenolic (24.01 mg GAE/g extract) as well as flavonoid (41.51 mg QE/g extract) contents. Phytochemical profiling of methanol extract identified a total of twenty secondary metabolites and the major compounds belonged to flavonoids, phenolics and alkaloid derivatives. The findings of antioxidant assays revealed the methanol extract to exhibit stronger antioxidant (except phosphomolybdenum) activities. Similarly, the methanol extract showed highest butyrylcholinesterase and urease inhibition. The DCM extract was most active for phosphomolybdenum and α-glucosidase inhibition assays. Moreover, both extracts exhibited significant cytotoxic potential against five (MCF-7, MDA-MB-231, CaSki, DU-145, and SW-480) human carcinoma cell lines with half maximal inhibitory concentration values of 22.09 to 257.2 µg/mL. Results from the present study highlighted the potential of B. glabra aerial extracts to be further explored in an endeavour to discover novel phytotherapeutics as well as functional ingredients.

ß-Secretase inhibition by C-methylisoflavones from Abronia nana.

The methanol extract of Abronia nana suspension cultures were subjected to column chromatography to identify potential inhibitors of ß-secretase, which is a major factor in Alzheimer's disease development. Two new C-methylisoflavones boeravinone T (1) and U (4) were isolated with three knowns boeravinone B (2), J (3) and X (5). The half-maximal inhibitory concentration (IC50) values of compounds 1-5 were 18.29, 8.57, 7.87, 12.02 and 5.30 µM, respectively. The most potent 5, non-competitively inhibited ß-secretase [inhibition constant (Ki) = 3.79 µM]. Compounds 1-5 did not inhibit other proteases such as chymotrypsin, trypsin and elastase at concentrations up to 1 mM, indicating that they were relatively specific inhibitors of ß-secretase. A free hydroxyl group at C-3 position of the C-methylisoflavone skeleton appeared to be responsible for the stronger inhibitory activity against ß-secretase.

Chemical composition, anti-nociceptive and anti-inflammatory activities of essential oil of Bougainvillea glabra.

ETHNOPHARMACOLOGICAL RELEVANCE: Bougainvillea glabra is widely used in Nigeria for the treatment of inflammatory-related conditions, and as remedy for pain ailments. AIM OF THE STUDY: Considering the lack of scientific studies focused on chemical constituents and pharmacological activity of B. glabra essential oil, this work was designed to characterize the volatile compounds and evaluate the anti-inflammatory and anti-nociceptive properties ascribed to this plant species. MATERIALS AND METHODS: The essential oil was extracted from the leaf of B. glabra by hydrodistillation in an all glass Clevenger-type apparatus and characterized by gas chromatography (GC-FID) and gas chromatography-mass spectrometry (GC-MS) on HP-5 column. The anti-inflammatory property of the essential was established by measurement of carrageenan induced rat paw edema while the anti-nociceptive activity was determined by hot plate test, according to established procedures. RESULTS: The essential oil was obtained in a yield of 0.08% (v/w) calculated on dry weight basis. A total of 11 compounds representing 96.2% of the oil contents were identified by GC/MS. The main constituents of the essential oil were (E)-nerolidol (31.4%), (E)-ß-ionone (10.3%) and linalool (10.1%). The anti-nociceptive property of the essential oil was statistically significant p < 0.001 at all doses of when compared to the control while exhibiting an activity in tandem with the standard drug. For the 1st and 2nd h, at doses of 100 and 200 mg/kg, the anti-inflammatory activity was statistically very significant (p < 0.001), while at 3rd h the activity declined (p < 0.01) at a dose of 200 mg. The activity was non-significant at the 4th h experimental duration. CONCLUSIONS: This is first report on the chemical constituents and biological activity of essential oil of B. glabra from Nigeria. Overall, the results herein presented sustain and strengthen the anti-nociceptive and anti-inflammatory properties traditionally ascribed to B. glabra.

Apoptosis in angiotensin II-stimulated hypertrophic cardiac cells -modulation by phenolics rich extract of Boerhavia diffusa L.

Herein, we investigated the effects of B. diffusa (BDE), a well-known cardiotonic edible medicinal plant against apoptosis in Angiotensin II (Ang II)-stimulated hypertrophic cardiac cells (H9c2). The cells were analyzed for viability, markers of hypertrophy, apoptosis, and the expression of various proteins related to apoptosis. Ang II (100 nM for 48 h)-exposed H9c2 cells treated with BDE (75 µg/ml) showed a significant reduction in apoptosis (58.60%↓) compared to Ang II-alone treated cells. BDE treatment significantly reduced the up-regulation of Bax and cytosolic cytochrome-C caused by Ang II as well as reduced the degree of Ang II- induced down-regulation of Bcl-2. A reduction in caspase-3 activity (33.77%↓) and down-regulation of TNF-α was also observed in BDE treated cells stimulated with Ang II. Furthermore, the up-regulation of phospho-p38 MAPK was attenuated by BDE treatment. Bioactive components in the extract were identified as boeravinone B, quercetin, kaempferol, and caffeic acid as evident from high-performance liquid chromatography (HPLC). Overall, our study shows that B. diffusa is effective in attenuating apoptosis in cardiac cells, which is a major contributor to sudden cardiac death in addition to its nutraceutical properties.

Boerhaavia diffusa inhibits key enzymes linked to type 2 diabetes in vitro and in silico; and modulates abdominal glucose absorption and muscle glucose uptake ex vivo.

The present study investigated the in vitro and ex vivo antioxidant, anti-diabetic and anti-obesogenic potentials of different solvent (ethyl acetate, ethanol and water) extracts from the aerial parts of Boerhaavia diffusa. The ferric reducing antioxidant power (FRAP), DPPH scavenging activity and the ameliorative effects of the extracts on Fe2+-induced oxidative injury was investigated both in vitro and ex vivo. Alpha glucosidase and pancreatic lipase inhibitory potentials of the extracts were examined in vitro, while the effects of the ethanol extract on abdominal glucose intake and muscle glucose uptake were determined in freshly harvested tissues ex vivo. The extracts were subjected to Gas Chromatography-Mass Spectrometry (GC-MS) analysis to identify their possible bioactive components. The ethanol extract showed the most potent FRAP and DPPH radical scavenging activities compared to other extracts. All extracts increased catalase and SOD activities, and GSH levels in oxidative pancreatic injury. Both ethanol and aqueous extracts exhibited remarkable enzyme inhibitory activities, which was significantly higher than ethyl acetate extract and acarbose but was not comparable to orlistat. The ethanol extract portrayed a dose-dependent inhibitory effect on jejunal glucose uptake and enhancement of muscle glucose uptake. 9-(4 methoxyphenyl) xanthene, xanthone and stigmasterol showed strong binding affinities for α-glucosidase and lipase enzymes tested. Data from this study suggest that aerial parts of B. diffusa (particularly the ethanol extract) may not only exhibit antioxidant potentials but may also mediate anti-lipidemic and anti-hyperglycemic effects via inhibiting fat and carbohydrate digestion as well as abdominal glucose intake and enhancing muscle glucose uptake.