Effect of Casearia sylvestris on the obliteration of dentinal tubules and the control of dental sensitivity / Efecto de Casearia sylvestris sobre la obliteración de los túbulos dentinarios y el control de la sensibilidad dental

The present study evaluated the efficacy of the mineralizing action of Casearia sylvestris ethanolic extract on bovine dentin blocks in its pure form and in dental paste, through scanning electron microscopy. The dentin blocks were immersed in artificial saliva and incubat ed at 37°C for 7 days. Subsequently, six groups were treated with different test substances and analysed qualitatively and quantitatively at 30 and 60 days. The tests used were Kruskal - Wallis and Dunn's. Shapiro - Wilk and ANOVA. The qualitative analysis at 30 days showed a difference between the groups treated with ethanolic extract and toothpaste. Quantitatively, at 30 days, treatment with ethanolic extract of Casearia showed a greater number of open dentinal tubules. At 60 days, the difference persisted on ly for the blocks treated with toothpaste. The results obtained indicated that there is a positive relationship between the use of Casearia sylvestris and obliteration of dentinal tubules

El presente estudio evaluó la eficacia de la acción mineralizante del extracto etanólico de Casearia sylvestris sobre bloques de dentina bovina en su forma pura y en pasta dental, mediante microscopía electrónica de barrido. Los bloques de dentina se sumergieron en saliva artificial y se incubaron a 37°C durante 7 días. Posteriormente, se trataron seis grupos con diferentes sustancias de ensayo y se analizaron cualitativa y cuantitativamente a los 30 y 60 días. Las p ruebas utilizadas fueron Kruskal - Wallis y Dunn's. Shapiro - Wilk y ANOVA. El análisis cualitativo a los 30 días mostró una diferencia entre los grupos tratados con extracto etanólico y pasta dentífrica. Cuantitativamente, a los 30 días, el tratamiento con ex tracto etanólico de Casearia mostró un mayor número de túbulos dentinarios abiertos. A los 60 días, la diferencia persistió sólo para los bloques tratados con pasta dentífrica. Los resultados obtenidos indicaron que existe una relación positiva entre el us o de Casearia sylvestris y la obliteración de los túbulos dentinarios

Bioactive constituents from Flacourtia vogelii Hook.f. (Flacourtiaceae).

The chemical investigation of the methanolic root extract of Flacourtia vogelii led to the isolation of a new arylbenzoate derivative, vogelinal (1), together with thirteen known compounds (2-14). The structures of the isolates were elucidated by extensive spectroscopic and spectrometric analyses (1D and 2D NMR, ESI-MS) and by comparison with previously reported data. All the compounds were tested for their antioxidant, antifungal and antibacterial activities. Compound 7 exhibited the highest antioxidant potential, with RSa50of 11.80 ± 2.13 µg/mL, RSa50of 42.60 ± 6.32 µg/mL and RC50 of 51.60 ± 7.71 µg/mL for the DPPH, ABTS and FRAP assay, respectively. Compound 13 displayed weak antifungal effect with MIC value of 125 µg/mL against Candida parapsilosis. Compound 8 showed weak antibacterial effect with MIC value of 125 µg/mL, against Shigella dysenteria. The present study, conclude that this species could be a promising source of antioxidant and antibacterial constituents.

A comprehensive study on physicochemical properties, bioactive compounds, and emulsified lipid digestion characteristics of Idesia polycarpa var. Vestita Diels fruits oil.

Idesia polycarpa var. vestita Diels fruits oil (IPO) has the potential to broaden the availability of healthy vegetable oil and relieve pressure on the edible oil supply. In this study, we compared the physicochemical, bioactivity, and digestive properties of IPO, olive oil (OO), and soybean oil (SO) to comprehensively evaluate the edible potential of IPO. The results revealed no significant differences in relative density or refractive index among the three oils. IPO was rich in ß-sitosterol (366.74 mg/100 g), ß-tocopherol (8.42 mg/100 g), and α-tocopherol (37.10 mg/100 g). The digestive properties of IPO emulsion were investigated for the first time using in vitro simulated digestion. The IPO emulsion stood out regarding its free fatty acid release (88.03 %). Finally, the IPO emulsion released mainly unsaturated fatty acids and had a higher monoacylglycerol content. This study provides new insights into IPO as a high-quality edible vegetable oil.

Extraction of Phenolic Compounds from Populus Salicaceae Bark.

Lignocellulosic residues have the potential for obtaining high value-added products that could be better valorized if biorefinery strategies are adopted. The debarking of short-rotation crops yields important amounts of residues that are currently underexploited as low-grade fuel and could be a renewable source of phenolic compounds and other important phytochemicals. The isolation of these compounds can be carried out by different methods, but for attaining an integral valorization of barks, a preliminary extraction step for phytochemicals should be included. Using optimized extraction methods based on Soxhlet extraction can be effective for the isolation of phenolic compounds with antioxidant properties. In this study, poplar bark (Populus Salicaceae) was used to obtain a series of extracts using five different solvents in a sequential extraction of 24 h each in a Soxhlet extractor. Selected solvents were put in contact with the bark sample raffinate following an increasing order of polarity: n-hexane, dichloromethane, ethyl acetate, methanol, and water. The oily residues of the extracts obtained after each extraction were further subjected to flash chromatography, and the fractions obtained were characterized by gas chromatography coupled with mass spectrometry (GC-MS). The total phenolic content (TPC) was determined using the Folin-Ciocalteu method, and the antioxidant activity (AOA) of the samples was evaluated in their reaction with the free radical 2,2-Diphenyl-picrylhydrazyl (DPPH method). Polar solvents allowed for higher individual extraction yields, with overall extraction yields at around 23% (dry, ash-free basis). Different compounds were identified, including hydrolyzable tannins, phenolic monomers such as catechol and vanillin, pentoses and hexoses, and other organic compounds such as long-chain alkanes, alcohols, and carboxylic acids, among others. An excellent correlation was found between TPC and antioxidant activity for the samples analyzed. The fractions obtained using methanol showed the highest phenolic content (608 µg of gallic acid equivalent (GAE)/mg) and the greatest antioxidant activity.

Anticancer, antioxidant, antiviral and antimicrobial activities of Kei Apple (Dovyalis caffra) fruit.

Secondary plant metabolites remain one of the key sources of therapeutic agents despite the development of new approaches for the discovery of medicinal drugs. In the current study, chemical analysis, and biological activities of Kei apple (Dovyalis caffra) methanolic extract were evaluated. Chemical analysis was performed using HPLC and GC-MS. Antiviral and anticancer effect were assessed using the crystal violet technique and activity against human liver cells (HepG2), respectively. Antibacterial activity was tested with the disc diffusion method. The obtained results showed that chlorogenic acid (2107.96 ± 0.07 µg/g), catechin (168 ± 0.58 µg/g), and gallic acid (15.66 ± 0.02 µg/g) were the main bioactive compounds identified by HPLC techniques. While, compounds containing furan moieties, as well as levoglucosenone, isochiapin B, dotriacontane, 7-nonynoic acid and tert-hexadecanethiol, with different biological activities were identified by GC-MS. Additionally, inhibition of 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH) scavenging was 79.25% at 2000 µg/mL, indicating its antioxidant activity with IC50 of 728.20 ± 1.04 µg/mL. The tested extract exhibited potential anticancer activity (58.90% toxicity) against HepG2 cells at 1000 µg/mL. Potential bacterial inhibition was observed mainly against Escherichia coli and Proteus vulgaris, followed by Staphylococcus aureus and Bacillus subtilis with a diameter of growth inhibition ranging from 13 to 24 mm. While weak activities were recorded for fungi Candida albicans (10 mm). The extract showed mild antiviral activity against human coronavirus 229E with a selective index (SI) of 10.4, but not against human H3N2 (SI of 0.67). The molecular docking study's energy ratings were in good promise with the experiment documents of antibacterial and antiviral activities. The findings suggest that D. caffra juice extract is a potential candidate for further experiments to assess its use as potential alternative therapeutic agent.

Perspectives on Populus spp. (Salicaceae) bud extracts as antioxidant and anti-inflammatory agents.

Hydroalcoholic extracts obtained from buds of P. nigra, P. deltoides and P. trichocarpa were characterized by HPLC-DAD-MS analysis and subsequently evaluated in vitro for their antioxidant and anti-inflammatory activities. ABTS and DPPH assays evidenced that P. nigra showed the best antioxidant activity in line with its highest total phenolic content. The analysis of the anti-inflammatory activity clearly demonstrated that all extracts suppressed the production of key pro-inflammatory cytokines (IL-6, Il-1ß and TNF-α) and HMGB1 inflammatory danger signal. These results show antioxidant and critical anti-inflammatory activities mediated by the extracts, emphasising their potentiality as therapeutic agents.

Homalium zeylanicum attenuates streptozotocin-induced hyperglycemia and cellular stress in experimental rats via attenuation of oxidative stress imparts inflammation.

ETHNOPHARMACOLOGICAL RELEVANCE: Homalium zeylanicum (Gardner) Benth (Salicaceae) leaves are being used as folklore medicine to treat diabetes by the local folk of Andhra Pradesh, India. The medicinal claim of this plant with hypoglycaemic effects was initially studied by the authors. Results demonstrated the important antioxidant activities of the hydroalcohol fraction of leaves of H. zeylanicum leaves (HAHZL) were positively correlated with phenols and flavonoids contents. AIM OF THE STUDY: Based on the previous findings, additional research is needed to examine the efficacy of using HAHZL to treat hyperglycemia. We therefore investigated in vitro and in vivo glycemic response of HAHZL, and evaluation of possible mechanism of bioactive molecules in mitigating streptozotocin-induced cellular stress in experimental rats via attenuation of oxidative stress imparts inflammation. METHODS: GC-MS/MS analysis of HAHZL was carried out to identify bioactive constituents. In vitro antidiabetic (α-glucosidase, α-amylase) and anti-inflammatory activities were investigated. HFD/low-STZ-prompted diabetic Wistar rats were administered with HAHZL (300 and 400 mg/kg; oral) for 28 days. Blood serum, oxidative stress, inflammation, DNA damage, and antidiabetic markers of pancreas and liver were determined. Histopathological studies of liver and pancreas were performed to assess the protective role of HAHZL. RESULTS: GC-MS/MS study revealed 7 bioactive compounds e.g., Phenol, 4-ethenyl-, acetate (28.68%), hydroquinone (9.10%), n-hexadecanoic acid (0.55%), phytol (0.57%), arbutin (17.65%), Vitamin E (1.04%), ß-Sitosterol (1.54%) which possess antioxidant, anti-inflammatory and anti-diabetic activities. HAHZL showed significant in vitro glycemic response as evidenced by the inhibition of α-amylase, and α-glucosidase activities. Lineweaver-Burk plot revealed that HAHZL exhibited competitive and mixed competitive inhibition towards α-amylase and α-glucosidase, respectively. HAHZL at 400 mg/kg modulated the pathophysiology associated with HFD/STZ-induced type2 diabetes mellitus and significantly (p < 0.001) improved antihyperglycemic (SG, SI, HOMA-IR, and HbA1C), antidyslipidemic (TC, HDL-C, LDL-C, and TG), antioxidative (MDA, SOD, CAT, GSH, and 8-OHdG) and anti-inflammatory (TNF-α, and CRP) markers in serum, pancreas and liver. In vitro and in vivo test results were corroborated by the improvement of pancreatic and hepatic tissue architecture in diabetic rats. CONCLUSION: HAHZL bearing bioactive components phenol, 4-ethenyl-,acetate, hydroquinone, n-hexadecanoic acid, arbutin, phytol, vitamin E and ß-sitosterol balanced glycemic level by normalising the levels of glycaemic indices, lipid profile, pancreas and liver functional markers in STZ-induced T2DM rats.

Phenolic glycosides from the stems of Homalium stenophyllum.

The phytochemical investigation of the stems of Homalium stenophyllum afforded seven new phenolic glycosides (1-5 and 8-9) and two known compounds (6 and 7). Their structures were elucidated by comprehensive analyses of NMR spectroscopic, mass spectrometric data and chemical hydrolysis. Additionally, their anti-inflammatory activities against the NO production in LPS-induced macrophages were evaluated.

Macroscopic, biochemical and hystological evaluation of topical anti-inflammatory activity of Casearia sylvestris (Flacourtiaceae) in mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Inflammatory skin diseases presents high prevalence and lack of alternatives that can be used for self-care by the population. Casearia sylvestris is a plant used topically in different communities in Brazil, to treat wounds or promote cutaneous healing. To evaluate the topical anti-inflammatory activity for the crude hydroalcoholic extract of Casearia sylvestris (HCE-CS) in the models of single or multiple administration of chroton oil to induce ear edema in mice. MATERIALS AND METHODS: Experimental study using male Swiss mice (25-35g) kept under constant conditions in the Laboratory of Experimental Neuroscience (LaNEx)-UNISUL. Edema was induced in both models, respectively, by the single or multiple application of croton oil (CO, 2.5%, in 20 µl) on the external surface of the ear. The different groups of animals (n = 8) received different treatments: vehicle, dexamethasone (DEXA) or different doses of HCE-CS. Edema was evaluated macroscopically for 6 h (early edema) or 8 days (late edema) after the first application of the CO and immediately after the animals were submitted to euthanasia for the collection of the samples (treated ears). For early edema, the tissue was biochemically evaluated for myeloperoxidase activity (MPO) and levels of nitrite/nitrate. In the late edema model, the ears were histologically evaluated for general morphometry, degranulated and non-degranulated mast cells, as well as acanthosis. RESULTS: Topic treatment with HCE-CS significantly reduced the early and late edema, as well as MPO activity and tissue levels of nitrite/nitrate. Finally, in the late edema model there was a lower density of degranulated mast cells in relation to the vehicle treated group and decreased thickness of the epidermis (acanthosis). CONCLUSION: These results suggest a possible benefit of topical treatment with HCE-CS in inflammatory conditions of the skin.

Amelioration by Idesia polycarpa Maxim. var. vestita Diels. of Oleic Acid-Induced Nonalcoholic Fatty Liver in HepG2 Cells through Antioxidant and Modulation of Lipid Metabolism.

Idesia polycarpa Maxim. var. vestita Diels (I. polycarpa) is well known as an edible oil plant which contains abundant linoleic acid and polyphenols. The objective of this study was to maximize the by-product of defatted fruit of I. polycarpa. We found that the fraction D of ethyl acetate extract (EF-D) contained more polyphenols, which contribute to its strong antioxidant activity by antioxidant assays (DPPH, ABTS, and FRAP). Meanwhile, EF-D showed a significant lipid-lowering effect on oleic acid- (OA-) induced hepatic steatosis in HepG2 cells through enhancing antioxidant activity, reducing liver damage, and regulating lipid metabolism, antioxidant, and inflammation-related gene expression. The SOD and T-AOC levels significantly increased, but the levels of MDA, AST, and ALT decreased obviously when treated with EF-D. In general, EF-D improved the antioxidant enzyme activities and decreased the hepatic injury activities. Besides, treatment with EF-D for NAFLD influenced lipid metabolism and inflammation by activating PPARα which was associated with the increased expression of CPT1 and decreased expression of SCD, NF-κB, and IL-1. Moreover, EF-D improved the oxidative stress system through activation of the Nrf2 antioxidant signal pathways and upregulated its target genes of HO-1, NQO1, and GSTA2. The results highlighted the EF-D from the defatted fruit of I. polycarpa regarding lipid-lowering, proving it to be a potential drug resource of natural products for treating the nonalcoholic fatty liver disease (NAFLD).

The modulatory role of prime identified compounds in the bioactive fraction of Homalium zeylanicum in high-fat diet fed-streptozotocin-induced type 2 diabetic rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Homalium zeylanicum (Gardner) Benth. is a medicinal plant traditionally used in controlling diabetes which thus far has been assessed by the authors only to a very limited extent. PURPOSE: To fill the research gap in the literature review, we investigated the antihyperglycemic effects of hydro alcohol fraction of bark of H. zeylanicum (HAHZB) by modulating oxidative stress and inflammation in high-fat diet fed-streptozotocin (HFD/STZ)-induced type-2 diabetic rats. MATERIALS AND METHODS: To understand the antioxidant capacity of HAHZB, oxygen radical absorbance capacity (ORAC) and cell-based antioxidant protection in erythrocytes (CAP-e) were performed. GC-MS/MS analysis was performed to assess the bioactive components in HAHZB. HFD/STZ-induced diabetic rats were treated orally with HAHZB (300 and 400 mg/kg) for 28 days. After the end of the experiment, marker profiling and histopathological observation of blood and pancreas were examined. The study also highlights interaction between diabetes, oxidative stress and inflammation by examining the increased pro-inflammatory cytokines e.g. TNF-α and C-reactive protein (CRP) promotes DNA damage e.g. oxidation of 8-hydroxy-2-deoxyguanosine (8-OHdG) in chronic hyperglycaemia. RESULTS: In ex vivo cellular antioxidant capacity of -CAP-e and ORAC assays, HAHZB showed remarkable free radical scavenging ability in a dose dependent manner. GC-MS/MS analysis identified 28 no. of compounds and out of which, oleic acid (1.03%), ethyl tridecanoate (11.77%), phytol (1.29), 9,12-octadecadienoic acid, methyl ester, (E,E)-(5.97%), stigmasterol (1.30%) and ß-sitosterol (2.86%) have antioxidant, anti-inflammatory and anti-diabetic activities. HAHZB 400 mg/kg significantly (p < 0.001) improved the lipid profile (TC: 74.66 ± 0.59, HDL-C: 22.08 ± 0.46, LDL-C: 38.06 ± 0.69, and TG: 171.92 ± 1.01 mg/dL) as well as restoring antidiabetic markers (SG: 209.62 ± 1.05 mg/dL, SI: 15.07 ± 0.11 µIU/mL, HOMA-IR: 7.79 ± 0.04 %, and HbA1C: 8.93 ± 0.03 %) and renal functional markers (Tg: 291.26 ± 0.57 pg/mL, BUN: 23.79 ± 0.14 mg/dL, and Cr: 1.34 ± 0.04 mg/dL) in diabetic rats. Oxidative stress markers of pancreas (MDA: 3.65 ± 0.17 nM TBARS /mg protein, SOD: 3.14 ± 0.28 U/mg protein, CAT: 7.88 ± 0.23 U/mg protein, GSH: 12.63 ± 0.28 µM/g of tissue) were restored to normal as evidenced by histological architecture of pancreatic islet cells. The increased level of pro-inflammatory cytokines and oxidative DNA damage were significantly restored (TNF-α: 54.48 ± 3.19 pg/mL, CRP: 440.22 ± 7.86 ng/mL, and 8-OHdG: 63.65 ± 1.84 ng/mL) by HAHZB in diabetic rats. CONCLUSION: The present findings confirm that the presence of bioactive compounds in HAHZB exert therapeutic protective effect by decreasing oxidative, inflammation and pancreatic ß-cell damage in oxidative stress induced diabetic rats.

Chemical Constituents and Pharmacological Activities of Family Flacourtiaceae: A Class of Important Phytomedicine.

Flacourtiaceae plants are widely used as folk medicines in traditional medicine systems for its chemical diversity and pharmacological activities. In many different areas, Flacourtiaceae plants are used as traditional medicines for the treatment of ulcers, malaria, rheumatism. The Flacourtiaceae plants contain a very plentiful chemical composition, and phytochemical studies show that the Flacourtiaceae plants contained terpenoids, aromatic glycosides, flavnoids, phenylpropanoids, alkaloids, fatty hydrocarbon, and other compounds. In pharmacological studies, various extract and isolated individual compounds exhibited antitumor, anti-oxidation, and anti-inflammatory activities. In this review, the literature data on the chemical constituents and pharmacological investigations of the Flacourtiaceae plants are summarized, to provide information about a more comprehensive chemical composition and detailed pharmacological activities of Flacourtiaceae plants, with a view of further development of clinical medication. However, research on quantitative analysis, toxicity, and drug safety in vitro and in vivo is still insufficient, and further research is required.

Computational and experimental validation of free radical scavenging properties of high-performance thin-layer chromatography quantified phenyl myristate in Homalium nepalense.

Phenyl myristate was isolated from Homalium nepalense, which is known for its therapeutic virtues in traditional medicine. However, the study of radical scavenging-capacity of phenyl myristate is limited by its relatively low abundance in medicinal plants. We have studied the isolation, structure-elucidation, and bioactivities of high-performance thin-layer chromatography validated phenyl myristate from hydroalcohol-extract of bark of H. nepalense. The chemical structure of phenyl myristate was elucidated by spectroscopic methods. The chromatography was performed on high-performance thin-layer chromatography aluminum plates coated with silica-gel 60 F254 . Determination and quantitation of phenyl myristate were performed by densitometric-scanning at 254 nm (chloroform-methanol, 9:1, v/v; Rf 0.49). The method was validated according to International Council for Harmonisation guidelines in terms of linearity, specificity, sensitivity, accuracy, precision, robustness, and stability. Linearity-range of phenyl myristate was 100-500 ng/5 µL with correlation-coefficient r2  = 0.9997. Limits of detection and quantitation were 3.35 and 10.17 ng, respectively. Phenyl myristate showed significant free-radical-scavenging activities in 2,2-diphenyl-1-picrylhydrazyl, oxygen-radical-absorbance-capacity, and ex vivo cell-based-antioxidant-protection-in-erythrocytes assays. Molecular-docking approach of phenyl myristate showed effective binding at active sites of human serum albumin (HSA) with the lowest binding energy (-8.4 kcal/mol) that was comparable with ascorbic acid (-5.0 kcal/mol). These studies provide mechanistic insight into the potential free radical scavenging activities of phenyl myristate.

Isolation and purification of four phenolic glycoside isomers from the leaves of Idesia polycarpa Maxim. by high-speed counter-current chromatography and preparative high-performance liquid chromatography.

We established an efficient method using high-speed counter-current chromatography (HSCCC) combined with preparative high-performance liquid chromatography (prep-HPLC) for isolating and purifying phenolic glycoside isomers. The method involves a rapid and sensitive ultra-performance liquid chromatography-under voltage(UPLC-UV) technique using a sub-2 µm core-shell particle column for qualitative and quantitative analysis of four phenolic glycoside isomers from Idesia polycarpa Maxim. leaves. The partially purified samples from ethyl acetate extraction of ethanol extracts of I. polycarpa Maxim. leaves were obtained by HSCCC with a two-phase solvent system composed of n-hexane-ethyl acetate-methanol-water solution (3:5:3:5, v/v/v/v) to obtain fractions I and II, which contain two phenolic glycoside isomers. The two fractions were further isolated by prep-HPLC to yield compounds 1, 2, 3, and 4 with purities of 98.29%, 98.71%, 98.49% and 98.52%, and total recoveries of 93.5%, 72.2%, 75.5% and 88.3%, respectively. Compound 1 was first isolated from I. polycarpa Maxim., while compound 2 was reported to be a new phenolic glycoside, which is 1-[(6'-O-(Z)-p-coumaroyl)-ß-D-glucopyranosyl]-oxy-2-phenol. The chemical structures of the four phenolic glycoside isomers were analyzed and confirmed by UPLC, UV, electrospray ionization mass spectrometry (ESI-MS), fourier transform infra-red (FT-IR), 1H-nuclear magnetic resonance (1H NMR), 13C-nuclear magnetic resonance (13C NMR) and 2D nuclear magnetic resonance (2D NMR) spectra. This study opens prospects for broad industrial applications of HSCCC/prep-HPLC for the isolation and purification of isomers.

Ethnobotanical uses, biological activities and chemical properties of Kei-apple [Dovyalis caffra (Hook.f. & Harv.) Sim]: An indigenous fruit tree of southern Africa.

ETHNOPHARMACOLOGICAL RELEVANCE: Dovyalis caffra (Hook.f. & Harv.) Sim (commonly called Kei-apple) is an indigenous fruit tree that has medicinal values for various ethnic groups in southern Africa. AIM OF THE REVIEW: This review aims to provide a critical appraisal of the existing knowledge on the ethnobotanical value, biological activities and phytochemicals of Dovyalis caffra. In addition, the potential of producing a functional health product from Kei-apple due to its therapeutic effects and rich pool of phytochemicals was explored. METHODS: A detailed literature search was conducted using various online search engines, such as Scopus, Google Scholar, Mendeley and Web of Science. Additional information was sourced from ethnobotanical literature focusing on southern African flora. RESULTS: Dovyalis caffra has diverse uses in local and popular medicine, specifically for relieving pain and rheumatism in humans. Ethno-veterinary potential of Kei-apple has also been documented in East Africa. Non-medicinal uses of the tree include its role in biological hedging and as a traditional herb for African magical purpose. Regarding its biological activities, polar extracts from the seeds exhibited noteworthy antibacterial (minimum inhibitory concentration of 1 µg/ml against Staphylococcus aureus) activity. Quantitative analysis (e.g. GC-MS, HPLC) indicated the presence of a rich (>80) pool of chemicals, including sterols, phenolic acids and fatty acids from different parts of the plant while 11 compounds have been isolated from its leaves and twigs. CONCLUSIONS: Dovyalis caffra has been tested for various biological activities and the extracts (seeds in particular) demonstrated promising antibacterial potential. A lack of alignment between the ethno-medicinal uses and existing biological screenings was observed, indicting the need for anti-inflammatory and anti-rheumatism potential of Dovyalis caffra to be explored. In vivo validation of antibacterial and anti-parasitic activities against clinical bacterial strains and parasites, respectively is required. Other areas that need investigation are safety evaluations and development of integrated cultivation approach in order to fully explore the plant's potential.

A new phenolic glycoside from the Idesia polycarpa Maxim. leaves.

Phytochemical investigation on the ethyl acetate extract of Idesia polycarpa Maxim. Leaves led to the isolation of four phenolic glycoside isomers (1-4). Compound 2 appeared to be new reported phenolic glycoside, while compound 1 was the first time isolated from the titled species. Their structures were established by IR, UV, HRESI-MS and 1D and 2D NMR spectroscopies analysis and comparison of spectral data with previously reported data. The compounds 3 and 4 showed stronger activity of scavenging the DPPH free radical than the other two compounds, while the compounds 1 and 2 showed a significant activity of scavenging the ABTS free radical. Compounds 2 and 4 exhibited stronger cytotoxicity against HepG2 cell lines compared to compounds 1 and 3. Moreover, compound 3 presented the highest cytotoxicity against MCF cell lines with IC50 value of 37.17 ± 0.26 µg/mL than compounds 1, 2 and 4.

Effects of TNT contaminated soil on vegetation at an explosive range by probing UPLC-qTOF MS profiling method.

Three tree species (Wild olive, Stinkwood and Cape Holy) and a shrub (Dovyalis caffra) were each potted in 20 L pots in order to evaluate the effect of 1,3,5-trinitrotoluene (TNT)-contaminated soil on vegetation. TNT contamination was established by dissolving flake TNT in acetone at 300 and 600 mg per kilogram soil concentrations. One pot for every species was left uncontaminated as control elements. A set of 16 samples, four contaminated, four uncontaminated aerial parts and their corresponding soils, were gathered. These were processed and subjected to a solid phase extraction method to isolate analytes of interest. A laboratory analytical method was applied using ultra-performance liquid chromatography coupled to quadrupole time-of-flight mass spectrometry (UPLC-qTOF MS). For the UPLC-qTOF MS a gradient for the mobile phase was found which allowed the profiling and separation of metabolites in the aerial parts of the vegetation. This method allowed identification and quantification of major changes caused by TNT contaminated soil on vegetation. The Synapt High Definition Mass Spectrometer SYNAPT HDMS G1 was operated using the electrospray ionisation (ESI) technique in both positive and negative mode. A clear comparison of profiles was achieved and this has been demonstrated by the distinct newly-formed metabolites in the TNT contaminated vegetation understudy. The results have also shown that the chlorophyll region in the contaminated profile was also affected by the uptake of TNT degradation products. This has been observed in the contaminated profiles of Wild olive, Stinkwood and Cape Holly extracts indicating enhanced nutrient availability.

The ameliorative effect of Homalium nepalense on carbon tetrachloride-induced hepatocellular injury in rats.

The purpose of this study was to evaluate ameliorative effects of Homalium nepalense Benth. (Flacourtiaceae) on CCl4-induced hepatocellular injury in rats. Oxygen-radical absorbance-capacity (ORAC) and cell-based-antioxidant-protection-in-erythrocytes (CAP-e) were performed and found that the ethyl acetate fractions of bark (HNEB) and leaf (HNEL) showed a remarkable degree of antioxidant activities in a dose dependent manner. Antioxidant potential HNEB was higher than HNEL and was comparable with trolox. HNEB and HNEL at 300 and 400 mg/kg showed significant hepatoprotective activities against CCl4-induced hepatotoxicity as evidenced by restoration of SGOT, SGPT, ALP, TB and TP level. The level of TBARS, SOD, CAT and GSH were significantly improved and restored towards normal value. Both fractions at 400 mg/kg showed remarkable improvements in marker levels as comparable to silymarin. Histopathological observations of liver tissues revealed the reduction of necrosis with appearance of sinusoidal space, central vein, and bile duct both in case of HNEB and HNEL. GC-MS and LC-MS confirmed occurrence of a total 53 no. of phytocompounds in HNEB and HNEL. Based on their retention times-(RT) and mass-to-charge-ratios-(m/z), some of the major bioactive compounds were catechol (5.89%), 5-hydroxymethylfurfural (5.87%), salicylic acid (4.89%), eugenol (1.60%), doconexent (0.31%), ß-sitosterol (1.59%), 2,3-dihydro-3,5-dihydroxy-6-methyl-4H-pyran-4-one (1.15%), coniferyl alcohol (2.99%), hexadecanoic acid methyl ester (1.05%), and betulin (1.20%). H. nepalense possesses significant hepatoprotection effect because of its antioxidant constituents.

A phenolic glycoside from Flacourtia indica induces heme mediated oxidative stress in Plasmodium falciparum and attenuates malaria pathogenesis in mice.

BACKGROUND: Flacourtia indica is especially popular among the various communities of many African countries where it is being used traditionally for the treatment of malaria. In our previous report, we have identified some phenolic glycosides from the aerial parts of F. indica as promising antiplasmodial agents under in vitro conditions. PURPOSE: Antimalarial bioprospection of F. indica derived phenolic glycoside in Swiss mice (in vivo) with special emphasis on its mode of action. METHODS: Chloroquine sensitive strain of Plasmodium falciparum was routinely cultured and used for the in vitro studies. The in vivo antimalarial potential of phenolic glycoside was evaluated against P. berghei in Swiss mice through an array of parameters viz., hematological, biochemical, chemo-suppression and mean survival time. RESULTS: 2-(6-benzoyl-ß-d-glucopyranosyloxy)-7-(1α, 2α, 6α-trihydroxy-3-oxocyclohex-4-enoyl)-5-hydroxybenzyl alcohol (CPG), a phenolic glycoside isolated from the aerial parts of F. indica was found to exhibit promising antiplasmodial activity by arresting the P. falciparum growth at the trophozoite stage. Spectroscopic investigations reveal that CPG possesses a strong binding affinity with free heme moieties. In addition, these interactions lead to the inhibition of heme polymerization in malaria parasite, augmenting oxidative stress, and delaying the rapid growth of parasite. Under in-vivo condition, CPG exhibited significant antimalarial activity against P. berghei at 50 and 75mg/kg body weight through chemo-suppression of parasitemia and ameliorating the parasite induced inflammatory and oxidative (hepatic) imbalance in the experimental mice. CONCLUSION: CPG was found to be a potential antimalarial constituent of F. indica with an explored mechanism of action, which also offers the editing choices for developing CPG based antimalarial chemotypes.

Bioprofiling of Salicaceae bud extracts through high-performance thin-layer chromatography hyphenated to biochemical, microbiological and chemical detections.

The buds of poplars (Populus L.) and willows (Salix L.), both from the same family (Salicaceae Mirbel), are increasingly used in gemmotherapy and importantly contribute to the production of the physiologically active propolis by European bee Apis mellifera L. In order to study their phenolic profiles, polar extracts of buds from P. nigra L. were compared to those of P. alba L. and S. alba L. through high-performance thin-layer chromatography (HPTLC). Five chemotypical patterns were distinguished after derivatisation with the Natural Product reagent and confirmed by principal component analysis. The HPTLC analysis was directly hyphenated to various microbiological and biochemical assays as well as spectrometric techniques, directly linking to active molecules in the chromatograms. At a glance, polyvalent compounds were evident when all derivatisation and activity assays, to which HPTLC was hyphenated at ease, were combined together. In Populus buds, at least three antimicrobial compound zones were detected using Aliivibrio fischeri and Bacillus subtilis bioassays, and one phyto-œstrogen with the planar yeast œstrogen screen. In all samples, several inhibitors of acetyl- and butyrylcholinesterase and rabbit liver esterase were detected. Hyphenation to high resolution mass spectrometry supported the assignment of bioactive compounds, as shown for chrysin as selective cholinesterase inhibitor as well as caffeic acid and galangin as antimicrobials in P. nigra and P. alba. This fast and cost-efficient method can be appropriately extended and applied to the botanical origin determination and quality control of bud extracts and propolis samples.