Dietary Plant Polyphenols as the Potential Drugs in Neurodegenerative Diseases: Current Evidence, Advances, and Opportunities.

Neurodegenerative diseases, including Alzheimer's disease (AD), Parkinson's disease (PD), and Huntington's disease (HD), are characterized by the progressive degeneration of neurons. Although the etiology and pathogenesis of neurodegenerative diseases have been studied intensively, the mechanism is still in its infancy. In general, most neurodegenerative diseases share common molecular mechanisms, and multiple risks interact and promote the pathologic process of neurogenerative diseases. At present, most of the approved drugs only alleviate the clinical symptoms but fail to cure neurodegenerative diseases. Numerous studies indicate that dietary plant polyphenols are safe and exhibit potent neuroprotective effects in various neurodegenerative diseases. However, low bioavailability is the biggest obstacle for polyphenol that largely limits its adoption from evidence into clinical practice. In this review, we summarized the widely recognized mechanisms associated with neurodegenerative diseases, such as misfolded proteins, mitochondrial dysfunction, oxidative damage, and neuroinflammatory responses. In addition, we summarized the research advances about the neuroprotective effect of the most widely reported dietary plant polyphenols. Moreover, we discussed the current clinical study and application of polyphenols and the factors that result in low bioavailability, such as poor stability and low permeability across the blood-brain barrier (BBB). In the future, the improvement of absorption and stability, modification of structure and formulation, and the combination therapy will provide more opportunities from the laboratory into the clinic for polyphenols. Lastly, we hope that the present review will encourage further researches on natural dietary polyphenols in the treatment of neurodegenerative diseases.

Composition, Antioxidant and Anti-inflammatory activities of Hexane and Methanol extracts of Acmella uliginosa from Terai region of Uttarakhand

Abstract Acmella uliginosa, an edible herb belonging to Asteraceae family, was collected from the Terai region of Uttarakhand, India. Methanol and hexane extracts of the whole plant were prepared using soxhlet apparatus. The GC-MS analysis of plant extracts identifies 22 and 35 major compounds of methanol and hexane extracts which comprises of 74.21% and 73.20% of the total composition of extracts, respectively. The major compound in hexane was 2, 4-heptadienal (7.99%) whereas trans, trans-9, 12-octadecadienoic acid propyl ester (16.96%) was major compound in methanol extract. The extracts were evaluated for antioxidant and anti-inflammatory properties. Methanol extract showed higher free radical scavenging and reducing power activities with IC50 value 153.82±1.69 µg/mL and RP50 value of 152.28±0.41 µg/mL, respectively. The metal chelating activity was higher in hexane extract as compared to methanol extract i.e., 62.08±0.25 µg/mL. The anti-inflammatory activity assessed by its ability to inhibit denaturation was higher in methanol having IB50 value 87.33±0.15 µg/mL. The total phenolic content (TPC), total flavonoid content (TFC) and ortho-dihydric phenol content (ODP) of methanol and hexane extracts were also evaluated. TPC, TFC and ODP was higher in methanol extract having value of 122.23±0.22, 35.01±0.29 and 8±0.86 mg/mL, respectively. Acmella uliginosa, might be considered as a natural source for antioxidant and anti-inflammatory properties

Efficacy of an herbal compound in decreasing steatosis and transaminase activities in non-alcoholic fatty liver disease: A randomized clinical trial

Abstract Hepatoprotective effects of many herbal agents have been reported in animal studies and clinical trials. In this study, five hepatoprotective plants with potent antioxidant, anti-inflammatory, and hypolipidemic effects were chosen to prepare a polyherbal compound for managing NAFLD. Sixty patients with NAFLD were randomly divided into treatment and control groups (2:1 ratio). Both group were advised to take healthy diet and exercise. The treatment group also received herbal capsules containing 400 mg of the mixture of Anethum graveolens, Citrus aurantium, Cynara scolymus, Portulaca oleracea, and Silybum marianum (2 capsules, thrice daily, for two months). The liver ultrasound and biochemical markers including the serum lipids, liver enzymes, and glucose were evaluated before starting the study and at the end of the treatment. Thirty patients in the treatment group and sixteen patients in the control group completed the study. The herbal compound significantly decreased the serum level of alanine transaminase (ALT), aspartate transaminase (AST), and total cholesterol. Treatment with the herbal compound significantly improved the grade of the fatty liver, but no significant change was found in the control group. In conclusion, the formulated herbal compound appeared to be effective in biochemical improvement and decreasing the grade of the fatty liver in the patients with NAFLD.

Phytochemical Profile and Antioxidant Activity of Nigella sativa L Growing in Morocco.

BACKGROUND: Nigella sativa L (NS) is a powerful antioxidant and medicinal plant with many therapeutic applications particularly in traditional medicine for respiratory, gastrointestinal, rheumatic, and inflammatory disorders, as well as cancer. OBJECTIVE: The aim of this study is to extract the active ingredients from the Moroccan Nigella sativa L and determine its antioxidant properties. We hypothesize that the separation of the compounds from Nigella sativa L has either a positive or negative effect on antioxidants. To study this, we explored different methods to simultaneously extract and separate compounds from Nigella sativa L and performed antioxidant tests (ß-carotene and DPPH) for all collected fractions. METHODS: Nigella sativa L was hot-extracted by Soxhlet and mother extracts and was separated using silica column chromatography with adequate eluents. Qualitative phytochemical tests to determine the chemical families in Nigella sativa L seeds were performed on the fractions. They were also identified and characterized by GC-MS and HPLC-DAD. Then, antioxidant activity was examined by ß-carotene bleaching and DPPH radical scavenger tests. Results and Conclusion. The mother extract hexane FH generated eight different fractions (SH1-8) and the acetone extract FA generated 11 fractions (SA1-11). The FH fractions had a high percentage of fatty acids, and the FA fractions had some interesting polyphenols derivative compounds. Phytochemical screening revealed secondary metabolites such as polyphenols flavonoids, alkaloids, steroids, terpenes coumarins, tannins, and saponins. We found that only two solvents (hexane, acetone) of different polarities could easily extract and simultaneously separate the components of Nigella sativa L. The antioxidant fractions that we collected had close activity to reference compounds but were more active than the corresponding mother extracts. Moreover, several IC50 values of fractions from acetone extract were better than those from hexane. Therefore, the antioxidant activity of Nigella sativa L is more attributed to flavonoids and polyphenols than fatty acids. In summary, the separation of hexane extract presents a more pronounced positive effect for antioxidant tests than acetone extract.

Evaluation of Antioxidant and Enzyme Inhibition Properties of Croton hirtus L'Hér. Extracts Obtained with Different Solvents.

Croton hirtus L'Hér methanol extract was studied by NMR and two different LC-DAD-MSn using electrospray (ESI) and atmospheric pressure chemical ionization (APCI) sources to obtain a quali-quantitative fingerprint. Forty different phytochemicals were identified, and twenty of them were quantified, whereas the main constituents were dihydro α ionol-O-[arabinosil(1-6) glucoside] (133 mg/g), dihydro ß ionol-O-[arabinosil(1-6) glucoside] (80 mg/g), ß-sitosterol (49 mg/g), and isorhamnetin-3-O-rutinoside (26 mg/g). C. hirtus was extracted with different solvents-namely, water, methanol, dichloromethane, and ethyl acetate-and the extracts were assayed using different in vitro tests. The methanolic extracts presented the highest 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid (ABTS), and ferric reducing antioxidant power (FRAP) values. All the tested extracts exhibited inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with a higher activity observed for dichloromethane (AChE: 5.03 and BChE: 16.41 mgGALAE/g), while the methanolic extract showed highest impact against tyrosinase (49.83 mgKAE/g). Taken together, these findings suggest C. hirtus as a novel source of bioactive phytochemicals with potential for commercial development.

Comparison of Bioactive Phenolic Compounds and Antioxidant Activities of Different Parts of Taraxacum mongolicum.

Herbs derived from Taraxacum genus have been used as traditional medicines and food supplements in China for hundreds of years. Taraxacum mongolicum is a famous traditional Chinese medicine derived from Taraxacum genus for the treatment of inflammatory disorders and viral infectious diseases. In the present study, the bioactive phenolic chemical profiles and antioxidant activities of flowers, leaves, and roots of Taraxacum mongolicum were investigated. Firstly, a high performance liquid chromatography method combined with segmental monitoring strategy was employed to simultaneously determine six bioactive phenolic compounds in Taraxacum mongolicum samples. Moreover, multivariate statistical analysis, including hierarchical clustering analysis, principal component analysis, and partial least squares discriminant analysis were performed to compare and discriminate different parts of Taraxacum mongolicum based on the quantitative data. The results showed that three phenolic compounds, caftaric acid, caffeic acid, and luteolin, could be regarded as chemical markers for the differences of flowers, leaves, and roots of Taraxacum mongolicum. In parallel, total phenolic contents, total flavonoid contents and antioxidant activities of different parts of Taraxacum mongolicum were also evaluated and compared. It is clear that Taraxacum mongolicum had antioxidant properties, and the antioxidant capacities of different parts of Taraxacum mongolicum in three antioxidant assays showed a similar tendency: Flowers ≈ leaves > roots, which revealed a positive relationship with their total phenolic and flavonoid contents. Furthermore, to find the potential antioxidant components of Taraxacum mongolicum, the latent relationships of the six bioactive phenolic compounds and antioxidant activities of Taraxacum mongolicum were investigated by Pearson correlation analysis. The results indicated caftaric acid and caffeic acid could be the potential antioxidant ingredients of Taraxacum mongolicum. The present work may facilitate better understanding of differences of bioactive phenolic constituents and antioxidant activities of different parts of Taraxacum mongolicum and provide useful information for utilization of this herbal medicine.

Phenolic Compounds, Antioxidant Activities, and Inhibitory Effects on Digestive Enzymes of Different Cultivars of Okra (Abelmoschus esculentus).

In this study, the phenolic profiles and bioactivities of five representative cultivars of okra collected in China were investigated. Noticeable variations of phenolic compounds and their bioactivities were observed among these different cultivars of okra. The contents of total flavonoids (TFC) in "Shuiguo", "Kalong 8", "Kalong 3", "Wufu", and "Royal red" ranged from 1.75 to 3.39 mg RE/g DW, of which "Shuiguo" showed the highest TFC. Moreover, five individual phenolic compounds were found in okra by high performance liquid chromatography analysis, including isoquercitrin, protocatechuic acid, quercetin-3-O-gentiobioside, quercetin, and rutin, while isoquercitrin and quercetin-3-O-gentiobioside were detected as the main phenolic compounds in okra. Moreover, all tested okra exhibited significant antioxidant activities (2,2-diphenyl-1-picrylhydrazyl radical scavenging capacity, 2,2'-azino-bis (3-ethylenzthiazoline-6-sulphonic acid) radical scavenging capacity, and ferric reducing antioxidant power) and inhibitory effects on digestive enzymes (lipase, α-glucosidase, and α-amylase). Indeed, "Shuiguo" exhibited much better antioxidant activities and inhibitory activities on digestive enzymes, which might be attributed to its high TFC. Results suggested that okra, especially "Shuiguo", could be developed as natural antioxidants and inhibitors against hyperlipidemia and hyperglycemia in the fields of functional foods and pharmaceuticals, which could meet the increasing demand for high-quality okra with health-promoting properties in China.

New Chemical Constituents from the Bark of Dendropanax morbifera Leveille and their Evaluation of Antioxidant Activities.

Four new constituents, as cis-6-oxogeran-4-enyl-10-oxy-O-ß-arabinopyranosyl-4'-O-ß-arabinopyranosyl-2''-octadec-9''',12''',15'''-trienoate (1), geran-3(10)-enyl-1-oxy-O-ß-arabinopyranosyl-4'-O-ß-arabinopyranosyl-2''-octadec-9''',12''',15'''-trienoate (2), geranilan-8-oxy-O-α-d-xylopyranosyl-2'-n-octadec-9'',12'',15''-trienoate (3), 1-cyclohex-2', 5'-dienyl 1-cyclohexylethanol-O-ß-d-xylopyranoside (4), along with six known constituents, guaiacol-O-ß-d-arabinopyaranoside (5), n-tetradecanyl oleate (6), oleyl-O-ß-d-xyloside (7), n-octadec-9,12-dienoyl-O-ß-d-arabinopyranoside (8), linolenyl-O-ß-d-arabinofuranoside (9) andglyceryl-1,3-dipalmito-2-olein (10), were isolated and identified from the Dendropanax morbifera bark. The new structures were established by one-and two-dimensional NMR (and in combination with IR, FAB-MSand HR-ESI-FTMS. The comparative evaluation of antioxidant potential by phosphomolybdenum, DPPH, FRAP and the NO assay of four different compounds (1-4), we have found that the compounds 1 and 2 have power as a natural antioxidant, whereas the compound 3 and 4 exhibited mild activity in comparison to compounds 1 and 2.

Comparison of two different antioxidants in a nano lecithin-based extender for bull sperm cryopreservation.

The objective of the present study was to assess the effect of two different antioxidants, enzymatic compared with non-enzymatic, in a nano lecithin-based extender on post-thaw bull sperm quality. Semen samples (n = 36) were collected from six bulls. In the first experiment, 11 different extenders were prepared by adding five quantities of vitamin E (α-tocopherol) as a non-enzymatic antioxidant (VE: 0.1, 0.2, 0.4, 0.6 and 1.0 mM), or four quantities of glutathione peroxidase (GPx) as an enzymatic antioxidant (GPx: 0.5, 1, 2 and 3 mM) to the extender. Other extenders were a Control 1 (C1: Extender with ethanol) and Control 2 (C2: Extender without ethanol). Sperm motility (CASA), plasma membrane functionality test (HOST) and lipid peroxidation (MDA) were assessed to determine the optimal treatment in the first experiment. In the second experiment, the optimally supplemented group from the first experiment (GPx-1) was compared to C2 group. Apoptotic-like changes (Annexin staining), mitochondrial activity (Rhodamine-123 staining), acrosome integrity (PSA staining), DNA fragmentation (SCSA test) and in vitro embryo production capacity were evaluated. In the first experiment, there were the greatest percentages of plasma membrane functionality and least MDA (P ≤ 0.05) in sperm diluted GPx-1 group. In the second experiment, percentage of live sperm, blastocyst formation and hatching rate were greater (P ≤ 0.05) in the GPx-1 group compared with C2 group. In conclusion, data indicate adding 1.0 mM GPx as an enzymatic antioxidant to the nano lecithin-based extender can improve post-thaw quality and in vitro fertility of bull sperm.

Solidago graminifolia L. Salisb. (Asteraceae) as a Valuable Source of Bioactive Polyphenols: HPLC Profile, In Vitro Antioxidant and Antimicrobial Potential.

Solidago species are often used in traditional medicine as anti-inflammatory, diuretic, wound-healing and antimicrobial agents. Still, the bioactive compounds and biological activities of some species have not been studied. The present work aimed to investigate the polyphenolic profile and the biological properties of Solidago graminifolia L. Salisb., a poorly explored medicinal plant. The hydroalcoholic extracts from aerial parts were evaluated for total phenolic content (TPC), total flavonoid content (TFC) and the polyphenolic compounds were investigated by HPLC-MS. The antioxidant potential in vitro was determined using DPPH and FRAP assays. Antibacterial and antifungal effects were evaluated by dilution assays and MIC, MBC and MFC were calculated. The results showed that Solidago graminifolia aerial parts contain an important amount of total phenolics (192.69 mg GAE/g) and flavonoids (151.41 mg RE/g), with chlorogenic acid and quercitrin as major constituents. The hydroalcoholic extracts showed promising antioxidant and antimicrobial potential, with potent antibacterial activity against Staphylococcus aureus and important antifungal effect against Candida albicans and C. parapsilosis. The obtained results indicated that the aerial parts of Solidago graminifolia could be used as novel resource of phytochemicals in herbal preparations with antioxidant and antimicrobial activities.

Mesilato de desferroxamina como candidato a adjuvante farmacêutico e cosmético / Desferroxamine mesylate as a candidate for pharmaceutical and cosmetic adjuvant

Este trabalho propôs o uso do fármaco quelante mesilato de desferroxamina (DFO) como agente adjuvante para estabilização química e microbiológica de formulações. Soluções de ácido ascórbico (AA) 5,0% (p/v) foram preparadas com sistemas antioxidantes constituídos por diferentes combinações de DFO, ácido etilenodiamino tetra-acético (EDTA) e metabissulfito de sódio, cada adjuvante na concentração máxima de 0,1% (p/v). Os sistemas foram testados previamente quanto à atividade antioxidante, mediante adição de um complexo de ferro (III) redox-ativo e ensaio baseado em fluorescência. Os sistemas também foram associados ao metilparabeno e avaliados quanto à atividade antimicrobiana pelo método turbidimétrico, utilizando-se a técnica de microdiluição em meios líquidos e cepas padrão de bactérias e fungos, incluindo S. aureus (ATCC 6538), E. coli (ATCC 8739), P. aeruginosa (ATCC 9027), C. albicans (ATCC 10231) e A. brasiliensis (ATCC 16404). As soluções de AA foram expostas a condições de teste de estabilidade acelerada e avaliadas quanto à estabilidade química, empregando-se método volumétrico validado para quantificar AA. Verificou-se que o EDTA foi o agente quelante que melhor contribuiu na estabilidade química da solução de AA, entretanto, o DFO apresentou desempenho muito superior ao EDTA para bloquear a atividade pró-oxidante do ferro. Além disso, o DFO foi fator relevante na inibição do crescimento microbiano e demonstrou sinergia com o metilparabeno. A otimização estatística dos resultados indicou que o uso do DFO nos sistemas antioxidante e conservante pode reduzir consideravelmente a concentração dos adjuvantes convencionais, EDTA, metabissulfito e metilparabeno, os quais são muitas vezes associados a reações de hipersensibilidade ou a danos ao meio ambiente

In this work it was proposed the use of the chelating drug desferroxamine mesylate (DFO) as adjuvant for chemical and microbiological stabilization of formulations. Ascorbic acid (AA) solutions 5.0% (w/v) were prepared with antioxidant systems containing different combinations of DFO, ethylenediaminetetraacetic acid (EDTA) and sodium metabisulphite, using a maximum concentration of 0.1% (w/v) for each adjuvant. Previously, the systems were spiked with a redox-active iron (III) complex and tested for antioxidant activity by fluorescence-based assay. The systems also were associated with methylparaben and evaluated for antimicrobial activity by turbidimetric method, using the microdilution technique and standard strains of bacteria and fungi, including S. aureus (ATCC 6538), E. coli (ATCC 8739), P. aeruginosa (ATCC 9027), C. albicans (ATCC 10231) and A. brasiliensis (ATCC 16404). The AA solutions were exposed to accelerated stability test conditions and evaluated for chemical stability, using a volumetric method that was validated to quantify AA. It was found that EDTA was the chelating agent that most contributed to the chemical stability of AA solution, however, DFO demonstrated a much higher performance to EDTA to block the pro-oxidant activity of iron. In addition, DFO was a relevant factor in the inhibition of microbial growth and showed synergy with methylparaben. The statistical optimization of the results indicated that the use of DFO in the antioxidant and preservative systems might considerably reduce the concentration of the conventional adjuvants, EDTA, metabisulphite and methylparaben, which are often associated with hypersensitivity reactions or environmental damage

Phytochemical Composition and Antioxidant Capacity of Seven Saskatoon Berry (Amelanchier alnifolia Nutt.) Genotypes Grown in Poland.

The basic chemical composition, bioactive compounds, and antioxidant capacity of fruits of three new Polish breeding clones (No. 5/6, type S, and type N) and four Canadian cultivars (cvs.) ("Martin", "Smoky", "Pembina", and "Honeywood") grown in Poland in 2016 were investigated. Fruits were analyzed for their contents of triterpenoids, carotenoids, chlorophylls, and polyphenolics with the ultra-performance liquid chromatography photodiode detector-quadrupole/time-of-flight mass spectrometry (UPLC-PDA-Q/TOF-MS) method, sugar with the high-performance liquid chromatography-evaporative light scattering detector (HPLC-ELSD) method, and antioxidant capacity with the ability to reduce free radical (ABTS) and ferric reducing ability of plasma (FRAP) method. Thirty-eight bioactive compounds, including twenty-eight polyphenolic compounds (four anthocyanins, nine phenolic acids, nine flavonols, and seven flavan-3-ols), four carotenoids, two chlorophylls, and three triterpenoids were identified in the fruits. The fruits of the tested Saskatoon berry genotypes were found to be rich in phenolic compounds (3773.94-6390.36 mg/100 g·dm), triterpenoids (66.55-91.31 mg/kg·dm), and carotenoids (478.62-561.57 mg/kg·dm), with high ABTS and FRAP capacity (10.38-34.49 and 9.66-25.34 mmol·Trolox/100 g·dm, respectively). Additionally, the berries of these genotypes seemed to be a good source of sugar (9.02-19.69 g/100 g), pectins (0.67%-1.33%), and ash (0.59%-0.67%). Some genotypes of Saskatoon berry, especially the clones type S, type N, and cvs. "Honeywood" and "Smoky", may be selected for their potential applications in commercial cultivation to produce fruits with valuable health-promoting nutritional effects on human health. Additionally, three new genotypes that may offer new functional materials can be recommended for fruit growers.

Physical chemistry evaluation of stability, spreadability, in vitro antioxidant, and photo-protective capacities of topical formulations containing Calendula officinalis L. leaf extract

Calendula is used widely in cosmetic formulations that present phenolic compounds in their chemical constitution. The objective of our research was to develop and evaluate the stability of topical formulations containing 5% hydro-ethanolic extract of calendula leaves, including spreadability, and in vitro photo-protective, and antioxidant capacity. To evaluate the stability, we used organoleptic characteristics, pH, and viscosity parameters. Antioxidant capacity was measured by the DPPH (2,2-diphenyl-1-picrylhydrazyl) method, and the photo-protective capacity by SPF spectrophotometric measure. All formulations were stable. The calendula extract formulations in gel and cream showed no significant variations in pH, and the cream formulations presented lower viscosity variations than gel formulations. The spreadability of the gel formulations was superior to those in cream. The formulations also presented good antioxidant capacities and an FPS of around 1.75. In accordance with the results, the formulations can be used as antioxidants, but considering the low SPF obtained, calendula cannot be considered as a stand-alone sunscreen, yet may well be tested in future studies towards verifying enhancement of synthetic sunscreens.

A calêndula é amplamente utilizada em formulações cosméticas, apresentando compostos fenólicos em sua constituição química. Desta forma, o objetivo desta pesquisa foi desenvolver e avaliar a estabilidade de formulações tópicas contendo 5% de extrato hidroetanólico das folhas de calêndula, bem como a espalhabilidade, capacidade antioxidante e fotoprotetora in vitro nas mesmas. Para a avaliação da estabilidade, foram usados parâmetros como a verificação das características organolépticas, pH e viscosidade. A capacidade antioxidante foi verificada pelo método do DPPH (2,2-difenil,1- picril-hidrazila) e a capacidade fotoprotetora pela medida espectrofotométrica do FPS. Para as formulações testadas, observou-se que apresentaram uma boa estabilidade. As formulações de creme e gel com extrato de calêndula não apresentaram variações significativas nos valores de pH e o creme apresentou as menores variações de viscosidade em relação ao gel. A espalhabilidade das formulações de gel foi superior à do creme. As formulações também apresentaram uma boa capacidade antioxidante e um FPS em torno de 1.75. De acordo com os resultados, a formulação pode ser utilizada com ação antioxidante, porém com o FPS obtido, a calêndula não pode ser considerada um filtro solar isolado, mas poderá ser testada em estudos futuros para verificar a potencialização de filtros solares sintéticos.

Atividade antiulcerogênica do extrato aquoso de Salvia officinalis L. (Lamiaceae) / Antiulcerogenic activity of aqueous extract of Salvia officinalis L. (Lamiaceae)

RESUMO As úlceras pépticas são decorrentes de um desequilíbrio entre os agentes agressores endógenos, exógenos e agentes protetores. Neste estudo avaliou-se a atividade antiulcerogênica in vivo para o extrato aquoso de Salviaofficinalis (EAS). Após os tratamentos (n = 6; v.o) com o controle (C) água; pantoprazol (30 mg/kg) e EAS (100, 250 e 400 mg/kg, respectivamente) os ratos receberam uma solução de HCl 0,3 M em etanol 60% (v.o) e realizaram-se avaliações morfológicas dos estômagos por meio de uma tabela de escores de lesão (ANOVA; one way e Tukey). EAS (400 mg/kg) apresentou atividade antiulcerogênica (31,47%) semelhante ao pantoprazol (33,83%) em comparação (p<0,0001) com o grupo C. A análise fitoquímica por cromatografia líquida de alta eficiência revelou uma elevada concentração de ácido rosmarínico (3,53%) para EAS. Os flavonoides (0,25%) e os fenóis totais (309,0 EAG) foram quantificados por espectrofotometria de UV/Vis. EAS e ácido rosmarínico apresentaram elevadas atividades antioxidantes por DPPH (Concentração Efetiva 50%-CE50 9,2 e 0,7 mg/mL, respectivamente) justificando pelo menos em parte, o efeito antiulcerogênico do extrato.

ABSTRACT Peptic ulcers are caused by an unbalance among endogenous, exogenous damaging agents and protective agents. In this study we evaluated the in vivo antiulcerogenic activity for the aqueous extract of Salvia officinalis (EAS). After treatments (n = 6; v.o) with control (C) water; pantoprazole (30 mg/kg) and EAS (100, 250 and 400 mg/kg, respectively) the rats received a 0.3 M HCl solution in ethanol 60% (v.o) and it were performed morphological evaluations of the stomachs through the use of a table of injury scores (ANOVA, one way and Tukey). The EAS (400 mg/kg) showed an antiulcerogenic activity (32.53%). Similar to the pantoprazole (29.91%), in comparison with (p<0.0001) the group C. The phytochemical analysis through high performance liquid chromatography revealed high acid rosmarinic (3.53%) for the EAS. The flavonoids (0.25%) and the total phenolics (GAE 309.0) were quantified by spectrophotometry UV/Vis. The EAS and the rosmarinic acid exhibited elevated antioxidant activities by DPPH (Effective Concentration 50% -EC50 9.2 and 0.7 mg/mL, respectively,) at least partially explaining the antiulcerogenic effect of the extract.

Botanicals in Ribes nigrum bud-preparations: an analytical fingerprinting to evaluate the bioactive contribution to total phytocomplex.

UNLABELLED: CONTEXT. Ribes nigrum L. (Grossulariaceae) is among the most commonly used herbal medicines and it is popularized for its alleged tonic effect and curative and restorative properties. The current practice of identifying herbal extracts is by measuring the concentration of the main botanicals. Their concentrations are used to characterize the herbal preparations and fingerprinting is recommended by the main Pharmacopeias as a potential and reliable strategy for the quality control of complex mixtures. OBJECTIVE: The aim of this research was to perform an analytical study of R. nigrum bud-preparations, in order to identify and quantify the main bioactive compounds, obtaining a specific chemical fingerprint to evaluate the single class contribution to herbal preparation phytocomplex. MATERIALS AND METHODS: The same analyses were performed using a high-performance liquid chromatograph-diode array detector both on University lab preparations and on commercial preparations from different Italian locations. Different chromatographic methods were used to analyse the macerated samples, two for polyphenols and one for terpenic compounds. RESULTS. Ribes nigrum was identified as a rich source of anti-inflammatory and antioxidant compounds. The observed analytical firgerprint demonstrated that these bud-preparations represent a rich source of terpenic and polyphenolic compounds, especially catechins and phenolic acids. DISCUSSION AND CONCLUSION: Analytical fingerprinting could be an important tool to study the assessment of chemical composition and bioactivities of plant-derived products, helping to find new sources of natural health-promoting compounds: this study allowed the development of an effective tool for quality control through botanical fingerprinting of bud preparations.

Evaluation of the mutagenicity and genotoxicity of Arrabidaea chica Verlot (Bignoneaceae), an Amazon plant with medicinal properties.

Arrabidaea chica Verlot (Bignoniaceae) is an important folk medicine plant native to the Amazon region and used to treat anemia, hemorrhage, inflammation, intestinal colic, hepatitis, and skin affections. Although studies showed its therapeutic properties, little knowledge regarding genotoxic properties of this plant is available. The aim of this study was to determine the potential mutagenic and genotoxic/antigenotoxic effects of an A. chica chloroformic fraction (Ac-CF) obtained from leaves containing bioactive metabolites. The mutagenic effects were evaluated using the Salmonella mutagenicity assay, with TA98, TA97a, TA100, TA102, and TA1535 strains, with and without metabolic activation. In vivo mutagenic and genotoxic/antigenotoxic effects were investigated using the micronucleus (MN) test in bone marrow and alkaline comet assay in blood and liver after administration of 100, 500, or 1000 mg/kg Ac-CF in CF-1 mice by gavage (once a day for 3 d). In vitro antioxidant potential was evaluated using DPPH and xanthine/hypoxanthine assays. Ac-CF was not mutagenic in any of the Salmonella typhimurium strains tested and showed negative responses for mutagenicity and genotoxicity in mice. Further, Ac-CF displayed antigenotoxic effects by decreasing the oxidative DNA damage induced by hydrogen peroxide by greater than 50% in blood and liver. The antioxidant action detected in the in vitro assays demonstrated IC50 of 0.838 mg/ml in the xanthine/hypoxanthine assay and IC50 of 28.17 µg/ml in the DPPH assay. In conclusion, Ac-CF did not induce mutagenic and genotoxic effects and was able to protect DNA against oxidative damage in vivo, suggesting that this fraction may not pose genetic risks, although further toxicology assays are necessary.

[The content of phenolic compounds in medicinal plants of a botanical garden (Kaliningrad Oblast)].

The total content of phenolic compounds and antioxidants has been determined in medicinal plants (66 species from 31 families). Promising plant species with high antioxidant activity and maximum content of phenols have been found. Based on these data, the plants can be used as a basis for making innovative functional food products with an increased antioxidant effect.

Phenolic compounds and antioxidant, antimicrobial and antimycobacterial activities of Serjania erecta Radlk. (Sapindaceae)

Serjania erecta Radlk.(Sapindaceae) is a medicinal plant traditionally used in Brazil. We assayed the ethanolic extract of leaves and roots against seven microorganisms. The REMA (Resazurin Microtiter Assay) assay was used to measure the biological activity in vitro against Mycobacterium tuberculosis and our results showed moderate activity of the ethanolic extract. On the other hand S. aureus, P. aeruginosa, S. setubal, C. albicans, S. cerevisiae and E. coli revealed that the leaves and roots of S. erecta inhibited the growth of all microorganisms. The ethanolic extracts of leaves and roots showed low values of antioxidant activities. The ethanolic extracts of leaves and roots were analyzed by chromatographic and spectrometric methods. (-)-Epicatechin, kaempferol aglycone and five glycoside derivates were isolated: kaempferol-3-O-α-L-rhamnopyranoside, kaempferol-3-O-α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranoside from the roots and kaempferol, kaempferol 3,7-di-O-α-L-rhamnopyranoside, vitexin, isovitexin and (-)-epicatechin in the leaves. This is the first chemical study reported in the literature about this specie.

Serjania erecta Radlk. (Sapindaceae) é uma planta medicinal utilizada no Brasil. Analisamos o extrato etanólico de folhas e raízes para sete microorganismos. O REMA (Ensaio de Microtitulação Resazurina) foi utilizado para medir a atividade biológica in vitro contra o Mycobacterium tuberculosis e nossos resultados mostraram atividade moderada do extrato etanólico. Por outro lado, ensaios com S. aureus, P. aeruginosa, S. setubal, C. albicans, S. cerevisiae e E. coli revelaram que as folhas e raízes de S. erecta inibiram crescimento em todos os microorganismos. Os extratos etanólicos de folhas e raízes apresentaram valores baixos de atividade antioxidante. Os extratos etanólicos de folhas e raízes foram analisados por métodos cromatográficos e espectroscópicos. (-)-Epicatequina, canferol aglicona e cinco derivados glicosídicos foram isolados: canferol -3-O-α-L-ramnopiranosídeo, canferol-3-O-α-L-ramnopiranosil-(1→6)-β-D-glucopiranosídeo a partir das raízes e canferol, canferol 3,7-di-O-α-L-ramnopiranosídeo, vitexina, isovitexina e (-) epicatequina nas folhas. Este é o primeiro estudo químico na literatura sobre esta espécie.

Comparative study of Puerariae lobatae and Puerariae thomsonii by HPLC-diode array detection-flow injection-chemiluminescence coupled with HPLC-electrospray ionization-MS.

An on-line HPLC-diode array detection-flow injection chemiluminescence (HPLC-DAD-FICL) method was applied to estimate the difference of Puerariae lobatae and Puerariae thomsonii. Their chemical and active profiles could be obtained by HPLC-DAD-FICL in one run. Seventeen compounds in two species were tentatively identified by HPLC-electrospray ionization-MS (HPLC-ESI-MS) method. The main antioxidants were rapidly screened by active fingerprints coupled with MS data. Similarity and Hierarchical clustering analysis (HCA) were used to distinguish different samples. The results suggested that the chemical fingerprints of 16 batches of samples were similar by similarity evaluation, while HCA could discriminate the two species. The active fingerprints of Puerariae lobatae and Puerariae thomsonii were significantly different. More antioxidants were found in Puerariae lobatae than in Puerariae thomsonii. Main antioxidants, including 3'-hydroxypuerarin, genistein 8-C-glycoside-xyloside, puerarin, 6″-O-xylosylpuerarin, mirificin and daidzein in two species, may be reasonable markers for the discrimination of the two species. The integrated fingerprint based on the chemical and active characteristics may provide an objective quality evaluation for Puerariae lobatae and Puerariae thomsonii.

Establishment of a methodology for investigating protectants against ethanol-induced hepatotoxicity.

Ethanol-induced liver injury has been extensively reported in clinic, but still lacks an efficient in vitro platform for investigating its hepatotoxicity and protectants. This study aimed to establish a methodology on the culture conditions regarding the sealability against evaporation of ethanol, culture medium and 2D/3D culture of hepatocytes. Based on the experimental findings, it was indicated that the ethanol evaporation from culture plates was a severe problem reducing its toxicity in hepatocyte. According to the detected ethanol toxic response marked by reduced cell viability, 3D cultured hepatocytes in gel entrapment were suggested to be better than 2D hepatocyte in monolayer, but the cultures in either William's Medium E or DMEM exhibited comparable sensitivity to ethanol toxicity. Subsequently, 3D cultured hepatocytes with Parafilm sealing were systematically illustrated to well reflect the ethanol-induced lipid accumulation, reactive oxygen species/malondialdehyde generation, glutathione depletion and cytochrome 2E1 induction. Finally, such hepatocyte models were proposed as a platform for screening of herbal component against ethanol hepatotoxicity. Nano-silibinin, for the first time, found to perform significant protection against ethanol-induced hepatotoxicity while silibinin in normal particles could not inhibit such toxicity. This protection of nano-silibinin might relate to its improved bioavailability compared to normal insoluble silibinin and could act as an anti-oxidative and anti-steatosis agent against ethanol-induced hepatotoxicity.