Antityrosinase activity and LC-MS/MS analysis of optimized ultrasound-assisted condition extracts and fractions from strawberry tree (Arbutus unedo L.).

Investigation of utilization possibilities of natural sources has been an important area for research. Tyrosinase inhibitory activity plays a key role in food and medicine industry. Strawberry tree (Arbutus unedo), a widely distributed plant among Mediterranean countries, possess fruits and leaves with rich bioactive phytochemicals, especially polyphenolic compounds. In this study, we aimed to investigate the antityrosinase activity of the fruit and leaf extracts of the plant, and to determine the phenolic compounds that contribute to the antityrosinase activity. In this regard, we evaluated the effect of solvent composition on the extraction of phenolic compounds from A. unedo and on its antityrosinase activity using a simplex centroid design approach, and used chromatographic and LC-MS/MS techniques. The leaf extracts prepared using EtOH:water (50:50) provided higher TPC (456.39 mg GAE/g extract) and acetone:EtOH:water (33:33:33) provided higher TFC (56.15 mg QE/g extract) values than of fruit extracts. LC-MS/MS analysis revealed 23 phenolic/flavonoid compounds in leaf extracts (L1-8), and major metabolites were detected as quercitrin, quinic acid, catechin, tannic acid, isoquercitrin, gallic acid, and ellagic acid. Among the leaf extracts, L3 (aceton:water, 50:50) exhibited 72.01% tyrosinase inhibition at 500 µg/mL. After fractionation studies guided by antityrosinase activity, its subfraction L3-Fr2 exhibited 40.06% inhibition at 50 µg/mL concentration (IC50: 146 ± 7.75 µg/mL), and catechin (113.19 mg/g), tannic acid (53.14 mg/g), ellagic acid (22.14 mg/g), gallic acid (10.27 mg/g), and epicatechin gallate (8.65 mg/g) were determined as major metabolites. Its subfraction L3-Fr2-sub7 exhibited better antityrosinase activity (IC50: 206.23 ± 9.87 µg/mL), and quantitative analysis results revealed the presence of tannic acid (127.40 mg/g), gallic acid (13.96 mg/g), ellagic acid (7.66 mg/g), quercetin-3-O-glucuronide (5.06 mg/g), and quinic acid (3.2 mg/g) as major metabolites, and correlation analysis showed that ellagic acid and quinic acid were positively correlated with antityrosinase activity.

Chemical Composition, Repellent, and Oviposition Deterrent Potential of Wild Plant Essential Oils against Three Mosquito Species.

In this study, the chemical composition, repellent, and oviposition deterrent effects of five plant essential oils (EOs) extracted from Lantana camara (Verbenaceae), Schinus terebinthifolia (Anacardiaceae), Callistemon viminalis (Myrtaceae), Helichrysum odoratissimum (Asteraceae), and Hyptis suaveolens (Lamiaceae) were evaluated against Aedes aegypti, Anopheles gambiae, and Culex quinquefasciatus. When tested at 33.3 µg/cm2, L. camara, S. terebinthifolia, C. viminalis, and H. odoratissimum were effective repellents against Ae. aegypti (89%, 91%, 90%, and 51% repellency, respectively), but they were less repellent against An. gambiae (66%, 86%, 59%, and 49% repellency, respectively). Interestingly, L. camara, S. terebinthifolia, C. viminalis, and H. odoratissimum exhibited 100% repellency against Cx. quinquefasciatus at 33.3 µg/cm2. In time-span bioassays performed at 333 µg/cm2, the EO of L. camara exhibited 100% repellence against Ae. aegypti and An. gambiae for up to 15 min and against Cx. quinquefasciatus for 75 min. The oviposition bioassays revealed that L. camara exhibited the highest activity, showing 85%, 59%, and 89% oviposition deterrence against Ae. aegypti, An. gambiae, and Cx. quinquefasciatus, respectively. The major compounds of L. camara, S. terebinthifolia, and C. viminalis were trans-ß-caryophyllene (16.7%), α-pinene (15.5%), and 1,8-cineole (38.1%), respectively. In conclusion, the L. camara and S. terebinthifolia EOs have the potential to be natural mosquito repellents.

Characterization of flours from the aroeira leaf (Schinus terebinthifolius Raddi), obtained by different drying methods.

The present work aimed at the development and characterization of aroeira leaf flour (Schinus terebinthifolius Raddi), obtained by lyophilization and drying in an air circulation oven. The technological, physical, physico-chemical, morphological, functional, and microbiological aspects were analyzed. Physico-chemical analysis identified the following properties with values provided respectively for fresh leaves (FOin) and flours (FES and FLIO): low water activity (0.984, 0.370, 0.387 g/100 g), moisture (64.52, 5.37, 7.97 g /100 g), ash (2.69, 6.51, and 6.89 g/100 g), pH (0.89, 4.45, 4.48 g/100 g), lipids (0.84, 1.67, 5.23 g/100 g), protein (3.29, 8.23, 14.12 g/100 g), carbohydrates (17.02, 53.12, 33.02 g/100 g), ascorbic acid (19.70, 34.20, 36.90 mg/100 g). Sources of fiber from plant leaves and flours (11.64, 25.1, 32.89 g/100 g) showed increased levels of luminosity. For NMR, the presence of aliphatic and aromatic compounds with olefinic hydrogens and a derivative of gallic acid were detected. The most abundant minerals detected were potassium and calcium. Micrographs identified the presence of irregular, non-uniform, and sponge-like particles. The main sugars detected were: fructose, glucose, and maltose. Malic, succinic, citric, lactic, and formic acids were found. Fifteen phenolic compounds were identified in the samples, highlighting: kaempferol, catechin, and caffeic acid. The values ​​found for phenolics were (447, 716.66, 493.31 mg EAG/100 g), flavonoids (267.60, 267.60, 286.26 EC/100 g). Antioxidant activity was higher using the ABTS method rather than FRAP for analysis of FOin, FES, and FLIO. Since the flours of the aroeira leaf have an abundant matrix of nutrients with bioactive properties and antioxidant activity, they have a potential for technological and functional use when added to food.

Botanical, nutritional, phytochemical characteristics, and potential health benefits of murici (Byrsonima crassifolia) and taperebá (Spondias mombin): insights from animal and cell culture models.

Brazil has great biodiversity, and the Amazon biome stands out for a variety of native fruits with high economic and nutritional potential. Murici (Byrsonima crassifolia) and taperebá (Spondias mombin) are sources of vitamins, minerals, and phytochemicals with potential health benefits. Because of the bioactive potential of these Brazilian fruits, this review aims to gather the most current existing knowledge about their botanical, nutritional, and phytochemical properties, because the presence of several bioactive compounds may bring promising strategies to the prevention and treatment of several diseases. The search was conducted of the LILACS, MEDLINE, PubMed, and Science Direct databases, considering articles published between 2010 and 2023. The compiled results showed that these fruits, their leaves, and seeds have great antioxidant activity and are a good source of phytochemicals, especially phenolic compounds. In vitro and in vivo studies indicate that these bioactive compounds have several health benefits related to the prevention or treatment of diseases, including antioxidant effects; anti-inflammatory effects; and antidiabetic, antidepressant, neuroprotective, antiproliferative, anticancer, hypolipemic, cardioprotective, gastroprotective, hepatoprotective, and nephroprotective effects, and they are particularly related to the reduction of damage from oxidative stress. This review highlights the potential of these fruits as functional foods and for therapeutic purposes. However, it is recommended to conduct more studies on the identification and quantification of phytochemicals present in these fruits and studies in humans to better understand the mechanisms of action related to their effects and to understand the interaction of these compounds with the human body, as well as to prove the safety and efficacy of these compounds on health.

Pharmacological, toxicological and phytochemical analysis of Spondias dulcis parkinson.

Spondias dulcis Parkinson have been used in traditional medicine in Asia, Oceania, and South America, for different diseases conditions and as a functional food. The scientific literature described as different potential pharmacology such as antioxidant, anti-inflammatory, antimicrobial, thrombolytic and enzymatic inhibitor. This study aimed to: (1) establish the pharmacological activity in intestinal motility in vivo and antioxidant activity in vitro; (2) perform the acute toxicology test in mouse; (3) characterize the phytochemical profile based on counter-current chromatography (CCC) and NMR analysis. The results revealed a laxative effect of S. dulcis extract and a high antioxidant activity (IC50 = 5.10 for DPPH assay and 14.14 for hydrogen peroxide scavenging test). No side effects were observed in the oral acute toxicity test for a dose up to 2000 mg/kg. The chemical profile was identified by CCC and NMR, and the comparison of the data obtained with previous literature revealed the presence of the flavonoid rutin (Quercetin-3-O-rutinoside) in the extract.

Flours from Spondias mombin and Spondias tuberosa seeds: Physicochemical characterization, technological properties, and antioxidant, antibacterial, and antidiabetic activities.

Yellow mombin (Spondias mombin) and Brazil plum (Spondias tuberosa) seeds are byproducts of exploiting their pulp and currently have no relevant food or industrial applications. Thus, the present study aimed to evaluate the physicochemical, technological, and functional characteristics of flours obtained from yellow mombin (YMF) and Brazil plum (BPF) residues. The flours presented a high percentage of insoluble fiber (68.8-70.2 g/100 g) and low carbohydrate (2.7-4.0 g/100 g) and caloric (91.9-95.3 kcal) values. The flours showed potential for technological application. In addition, the highest concentration of total phenolic content (31.1-50.2 mg GAE/g) was obtained with 70% acetone, which provided excellent results for antioxidant capacity evaluated by 2,2'-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (81.0%-89.7%) and 2,2-diphenyl-1-picrylhydrazyl (60.6%-69.1%) radical scavenging capacity assays. Flour extracts in 70% acetone also exhibited inhibition of α-amylase (63.3%-78.8%) and amyloglucosidase (63.5%-71.0%). The antibacterial study revealed that extracts inhibited the growth of Escherichia coli, Burkholderia cepacia, and Burkholderia multivorans. Therefore, this study suggests the use of yellow mombin and Brazil plum residues for different food or industrial applications. PRACTICAL APPLICATION: The knowledge gained from this study will open a new approach to add value to yellow mombin and Brazil plum fruit seeds as sources of fiber and bioactive compounds, with promising application in the formulation of functional and nutraceutical products, benefiting both a sustainable environment and a sustainable industry.

Schinus terebinthifolius Raddi (Brazilian pepper) leaves extract: in vitro and in vivo evidence of anti-inflammatory and antioxidant properties.

The aim of this work was to evaluate the anti-inflammatory and antioxidant effects of ethyl acetate extract obtained from the leaves of Brazilian peppertree Schinus terebinthifolius Raddi (EAELSt). Total phenols and flavonoids, chemical constituents, in vitro antioxidant activity (DPPH and lipoperoxidation assays), and cytotoxicity in L929 fibroblasts were determined. In vivo anti-inflammatory and antioxidant properties were evaluated using TPA-induced ear inflammation model in mice. Phenol and flavonoid contents were 19.2 ± 0.4 and 93.8 ± 5.2 of gallic acid or quercetin equivalents/g, respectively. LC-MS analysis identified 43 compounds, of which myricetin-O-pentoside and quercetin-O-rhamnoside were major peaks of chromatogram. Incubation with EAELSt decreased the amount of DPPH radical (EC50 of 54.5 ± 2.4 µg/mL) and lipoperoxidation at 200-500 µg/mL. The incubation with EAELSt did not change fibroblast viability up to 100 µg/mL. Topical treatment with EAELSt significantly reduced edema and myeloperoxidase activity at 0.3, 1, and 3 mg/ear when compared to the vehicle-treated group. In addition, EAELSt decreased IL-6 and TNF-α levels and increased IL-10 levels. Besides, it modulated markers of oxidative stress (reduced total hydroperoxides and increased sulfhydryl contents and ferrium reduction potential) and increased the activity of catalase and superoxide dismutase, without altering GPx activity.

Effect of extraction methods on phytochemical constituents and antioxidant activity of de-kernelled Sclerocarya birrea seeds.

BACKGROUND: Marula (Sclerocarya birrea) is an indigenous African fruit-bearing tree with many commercial uses; however, de-kernelled seeds generated from marula fruit-processing are wasted. The phytochemical constituents of de-kernelled marula seeds have not been investigated previously and its extract/tea may potentially serve as a promising source of antioxidants and phytochemicals. This study aimed to investigate the effect of different extraction methods (maceration and decoction) on the recovery of phenolic compounds, sugars, organic acids, and antioxidants from de-kernelled marula seeds. RESULTS: Extracts produced from decoction for 30 min contained the highest phenolic content (2253.93 ± 25.72 mg gallic acid equivalent kg-1 extract), flavonoid content (1020.99 ± 23.90 mg rutin equivalent kg-1 extract), as well as combined sugars and organic acids (1884.03 mg kg-1 extract). Fourier-transform infrared spectroscopy analysis confirmed the presence of functional groups typically present in phenolic compounds, sugars, and organic acids in the extracts obtained from decoction. CONCLUSION: The characterization revealed that decoction extraction increased solubility, variety, and yield of phytochemical and antioxidant compounds recovered from de-kernelled marula seeds. The highest concentrations of phytochemicals were obtained using the decoction method. This study may therefore pave the way for extract composition and future utilization of de-kernelled marula seeds in the food industry. © 2023 Society of Chemical Industry.

Avaliação do efeito anti-inflamatório do extrato de Spondias Mombin L. Em um modelo experimental de periodontite / Evaluation of the anti-inflammatory effect of Spondias Mombin L. extract in an experimental model of periodontitis

A doença periodontal (DP) é uma doença crônica de caráter inflamatório multifatorial, que acomete somente os tecidos de proteção (gengivite) ou os tecidos de proteção e sustentação dentárias (periodontite). O extrato hidroetanólico de Spondias mombin L. (EHSM) vem se destacando em função de sua eficácia antimicrobiana frente a patógenos bucais e de suas atividades anti-inflamatória e antioxidante. O objetivo deste trabalho foi avaliar o efeito antiinflamatório do EHSM em um modelo experimental de periodontite. Foi realizado um ensaio pré-clínico, controlado e in vivo, utilizando-se 61 ratos wistar machos, distribuídos aleatoriamente nos seguintes grupos: salina (n=7); DP (n=14); DP + SM 50mg/ml (n=12); DP + SM 100mg/kg (n=13) e DP + SM 200mg/kg (n=15). Foi realizada a gavagem diariamente desde o dia da indução da periodontite até o 11º dia experimental (eutanásia). Amostras sanguíneas, gengivais e maxilares foram obtidas e destinadas para as análises bioquímica, quantitativa de citocinas (IL-1ß e IL-6), histológica e microtomográfica computadorizada. Para análise estatística foram utilizados o teste paramétrico ANOVA, seguido pelo teste T de student e o teste não paramétrico de Kruskall-Wallis. A administração do EHSM não causou alterações sistêmicas nos animais, mostrando-se capaz de reduzir a concentração de IL-6, na dose de 50mg/kg (p<0,05), e de IL-1ß, na dose de 100mg/kg (p<0,01), assim como reduziu a reabsorção óssea e aumentou a integridade óssea em animais que receberam o EHSM nas concentrações de 100mg/kg (p<0,05) e 200mg/kg (p<0,001). Ademais, os animais submetidos à gavagem oral com o extrato na concentração de 200mg/kg (p<0,01) apresentou os melhores resultados histológicos, com infiltrado inflamatório escasso, restrito à gengiva marginal, e preservação do ligamento periodontal e do osso alveolar. Como conclusão, os achados deste estudo indicam que o EHSM, nas diferentes concentrações testadas, apresenta efeito anti-inflamatório local em um modelo experimental in vivo de periodontite, sem causar toxicidade sistêmica, apontando assim para o potencial uso do referido extrato no tratamento dessa doença (AU).

Periodontal disease (PD) is a chronic disease with a multifactorial inflammatory nature, which exclusively affects the protective tissues (gingivitis) or the tissues that protect and support the teeth (periodontitis). The hydroethanolic extract of Spondias mombin L. (HESM) has been highlighted due to its antimicrobial action against oral pathogens and its anti-inflammatory and antioxidant activities. The aim of this work was to evaluate the anti-inflammatory effect of HESM in an experimental model of periodontitis. A pre-clinical, controlled and in vivo test was carried out, using 61 male Wistar rats, randomly distributed in the following groups: saline (n=7); PD (n=14); PD + MS 50mg/ml (n=12); PD + MS 100mg/kg (n=13) and PD + MS 200mg/kg (n=15). Gavage was performed daily from the day of periodontitis induction to the 11th experimental day (euthanasia). Blood, gingival and jaw samples were transferred and sent for biochemical, quantitative cytokine (IL-1ß and IL-6), histological and computerized microtomographic analyses. For statistical analysis, the parametric ANOVA test was used, followed by Student's t test and the non-parametric Kruskall-Wallis test. The administration of HESM did not cause systemic diseases in the animals, being able to reduce the concentration of IL-6, at a dose of 50mg/kg (p<0.05), and of IL-1ß, at a dose of 100mg/kg (p<0.01), as well as bone resorption and increased bone integrity in animals that received HESM at concentrations of 100mg/kg (p<0.05) and 200mg/kg (p<0.001). In addition, the animals confirmed by oral gavage with the extract at a concentration of 200mg/kg (p<0.01) showed the best histological results, with limited infiltration, restricted to the marginal gingiva, and preservation of the periodontal ligament and alveolar bone. In conclusion, the findings of this study indicate that HESM, at different concentrations, presents local antiinflammatory activity in an experimental in vivo model of periodontitis, without causing systemic toxicity, thus pointing to the potential use of the aforementioned extract in the treatment of this disease (AU).

Isolation and characterization of natural inhibitors of post-proline specific peptidases from the leaves of Cotinus coggygria Scop.

ETHNOPHARMACOLOGICAL RELEVANCE: Cotinus coggygria has a number of applications in traditional medicine most of which are connected with its anti-inflammatory and anti-oxidant properties. Since inflammation and oxidative stress are recognized as triggering factors for cancer, anti-cancer activity has also been documented and the possible mechanisms of this activity are under investigation. Important components of C. coggygria extracts are shown to be hydrolysable gallotannins of which pentagalloyl-O-glucose has been studied in details. This compound inhibits various enzymes including prolyl oligopeptidase which is involved in tumorigenesis and tumour growth. According to our pilot studies, oligo-O-galloylglucoses with more than five galloyl residues are also presented in the herb of Bulgarian origin, but their activities have not been examined. AIM OF THE STUDY: To establish an extraction method by which it is possible to concentrate high molecular hydrolysable gallotannins from dried leaves of Cotinus coggygria and to determine their inhibitory properties towards prolyl oligopeptidase and fibroblast activation protein α. MATERIALS AND METHODS: Dried leaves of C. coggygria were extracted using different solvents in single-phase or biphasic systems under various extraction conditions. Main compounds of the extracts were identified by using high performance liquid chromatography and liquid chromatography - high resolution mass spectrometry. The extracts' inhibitory properties towards prolyl oligopeptidase and fibroblast activation protein α were studied on recombinant human enzymes by enzyme kinetic analyses using a fluorogenic substrate. RESULTS: Ethyl acetate/water (pH 3.0) extraction of dried plant leaves proved to be the most efficient method for isolation of high molecular hydrolysable gallotannins which can be further concentrated by precipitation of dicyclohexylammonium salts in ethyl acetate. The main components of those extracts were oligo-O-galloyl glucoses with more than five gallic acid residues. They were shown to inhibit both enzymes studied but were about 30 times more effective inhibitors of prolyl oligopeptidase. CONCLUSIONS: C. coggygria from Bulgarian origin is shown to possess a substantial quantity of oligo-O-galloyl glucoses with more than five gallic acid residues which has not been described thus far in the same herb from other sources. An extraction method useable for concentrating those compounds is established. They are found to inhibit prolyl oligopeptidase with a very good selectivity to fibroblast activation protein α. The previously described antitumor activity of this plant may be at least in part due to the inhibition of the above enzymes which has been shown to participate in the genesis and development of various types of tumors.

Use of yellow mombin (Spondias mombin L.) in marination: Effect on quality properties of Boston butt pork during refrigerated storage.

This research aimed to evaluate the effect of yellow mombin (Spondias mombin L.) juice as a marinade liquid on the quality properties of Boston butt pork during refrigerated storage. Yellow mombin juice was used as a marinade liquid at different concentrations: 0% (C0), 50% (C50), 75% (C75), and 100% (C100) in Boston butt pork samples which were analyzed for technological properties, proximate composition, and sensory characteristics on day 0 of storage. In addition, the pH, lipid oxidation, textural, and microbiological analyzes were carried out during refrigerated storage for 21 days. The results showed that the pH of the marinated samples was affected by yellow mombin juice (P < 0.05), with final values of 4.65 (C50), 4.56 (C75), and 4.39 (C100). Regarding the texture properties, C75 and C100 had the lowest values for hardness during storage. In addition, C100 had the lowest total aerobic mesophilic (5.69 log CFU g-1), total aerobic psychrophilic (7.10 log CFU g-1), and Enterobacteriaceae (5.30 log CFU g-1) counts at the end of storage. Regarding sensory properties, samples C50 and C75 were the best-rated marinated samples regarding overall acceptability and purchase intention. Therefore, the use of 75% yellow mombin juice (C75) as a marinade liquid could be a viable alternative for marinating Boston butt pork.

Chemical and cytotoxicity profiles of 11 pink pepper (Schinus spp.) samples via non-targeted hyphenated high-performance thin-layer chromatography.

INTRODUCTION: Pink pepper is a worldwide used spice that corresponds to the berries of two species, Schinus terebinthifolia Raddi or S. molle L. (Anacardiaceae). Toxic and allergic reactions by ingestion or contact with these plants were reported, and classical in vitro studies have highlighted the cytotoxic properties of apolar extracts from the fruits. OBJECTIVES: Perform a non-targeted screening of 11 pink pepper samples for the detection and identification of individual cytotoxic substances. METHODS: After reversed-phase high-performance thin-layer chromatography (RP-HPTLC) separation of the extracts and multi-imaging (UV/Vis/FLD), cytotoxic compounds were detected by bioluminescence reduction from luciferase reporter cells (HEK 293 T-CMV-ELuc) applied directly on the adsorbent surface, followed by elution of detected cytotoxic substance into atmospheric-pressure chemical ionization high-resolution mass spectrometry (APCI-HRMS). RESULTS: Separations for mid-polar and non-polar fruit extracts demonstrated the selectivity of the method to different substance classes. One cytotoxic substance zone was tentatively assigned as moronic acid, a pentacyclic triterpenoid acid. CONCLUSION: The developed non-targeted hyphenated RP-HPTLC-UV/Vis/FLD-bioluminescent cytotoxicity bioassay-FIA-APCI-HRMS method was successfully demonstrated for cytotoxicity screening (bioprofiling) and respective cytotoxin assignment.

Antiproliferative activity of compounds isolated from the root bark of Lannea acida in multiple myeloma cell lines.

Lannea acida A. Rich. is a native plant of West Africa used in traditional medicine against diarrhea, dysentery, rheumatism, and women infertility. Eleven compounds were isolated from the dichloromethane root bark extract using various chromatographic techniques. Among those, nine compounds have not been previously reported, i.e. one cardanol derivative, two alkenyl 5-hydroxycyclohex-2-en-1-ones, three alkenyl cyclohex-4-ene-1,3-diols, two alkenyl 7-oxabicyclo[4.1.0]hept-4-en-3-ols, and one alkenyl 4,5-dihydroxycyclohex-2-en-1-one, together with two known cardanols. The structure of the compounds was elucidated using NMR, HRESIMS, ECD, IR, and UV. Their antiproliferative activity was evaluated in three multiple myeloma cell lines: RPMI 8226, MM.1S, and MM.1R. Two compounds showed activity in all cell lines with IC50 values < 5 µM. Further investigations are needed to understand the mechanism of action.

Antileishmanial and Antiplasmodial Activities of Secondary Metabolites from the Root of Antrocaryon klaineanum Pierre (Anacardiaceae).

Antrocaryon klaineanum is traditionally used for the treatment of back pain, malaria, female sterility, chlamydiae infections, liver diseases, wounds, and hemorrhoid. This work aimed at investigating the bioactive compounds with antileishmanial and antiplasmodial activities from A. klaineanum. An unreported glucocerebroside antroklaicerebroside (1) together with five known compounds (2-6) were isolated from the root barks of Antrocaryon klaineanum using chromatographic techniques. The NMR, MS, and IR spectroscopic data in association with previous literature were used for the characterization of all the isolated compounds. Compounds 1-4 are reported for the first time from A. klaineanum. The methanol crude extract (AK-MeOH), the n-hexane fraction (AK-Hex), the dichloromethane fraction (AK-DCM), the ethyl acetate fraction (AK-EtOAc), and compounds 1-6 were all evaluated for their antiparasitic effects against Plasmodium falciparum strains susceptible to chloroquine (3D7), resistant to chloroquine (Dd2), and promastigotes of Leishmania donovani (MHOM/SD/62/1S). The AK-Hex, AK-EtOAc, AK-MeOH, and compound 2 were strongly active against Dd2 strain with IC50 ranging from 2.78 ± 0.06 to 9.30 ± 0.29 µg/mL. Particularly, AK-MeOH was the most active-more than the reference drugs used-with an IC50 of 2.78 ± 0.06 µg/mL. The AK-EtOAc as well as all the tested compounds showed strong antileishmanial activities with IC50 ranging from 4.80 ± 0.13 to 9.14 ± 0.96 µg/mL.

Cotinus coggygria Scop. Attenuates Acetic Acid-Induced Colitis in Rats by Regulation of Inflammatory Mediators.

In traditional medicine, many medicinal plants are used in the treatment of various diseases caused by inflammation. The objective of the present study is to elucidate for the first time the effects of Cotinus coggygria (CC) ethanol extract (CCE) on colonic structure and inflammation of acetic acid-induced ulcerative colitis in rats. Colonic damage was assessed using disease activity index score, enzyme-linked immunosorbent assay, and hematoxylin-eosin staining. Also, in vitro antioxidant activity of CCE was investigated by ABTS methods. Total phytochemical content of CCE was measured spectroscopically. Acetic acid caused colonic damage according to disease activity index and macroscopic scoring. CCE significantly reversed these damages. While the levels of proinflammatory cytokines TNF-alpha, IL-1beta, IL-6, and TGF-1beta increased in tissue with UC, IL-10 level decreased. CCE increased inflammatory cytokine levels to values close to the sham group. At the same time, while markers indicating disease severity such as VEGF, COX-2, PGE2, and 8-OHdG indicated the disease in the colitis group, these values returned to normal with CCE. Histological research results support biochemical analysis. CCE exhibited significant antioxidant against ABTS radical. Also, CCE was found to have a high content of total polyphenolic compounds. These findings provide evidence that CCE might be benefit as a promising novel therapy in the treatment of UC in humans due to high polyphenol content and justify the use of CC in folkloric medicine for treatment of inflamed diseases.

Screening of trypsin inhibitors in Cotinus coggygria Scop. extract using at-line nanofractionation coupled with semi-preparative reverse-phase liquid chromatography.

In this study, an at-line nanofractionation (ANF) platform was successfully fabricated in parallel with mass spectrometry and trypsin inhibitory bioactivity assessment for rapid screening of trypsin inhibitors (TIs) from natural products for the first time. After systematic optimization, the ANF platform was applied to screen and identify TIs in the extract of a traditional Chinese herb, i.e., Cotinus coggygria Scop. The semi-preparative reverse-phase liquid chromatography was used subsequently to further simplify and enrich the insufficiently separated components. After comprehensive evaluation and validation, the ANF platform successfully identified 12 compounds as potential TIs, including 8 flavonoids and 2 organic acids. Additionally, a comparison study was conducted using two other ligand fishing approaches, i.e., capillary monolithic and magnetic beads-based trypsin-immobilized enzyme microreactors, which successfully identified 8 identical flavonoids as TIs. Importantly, the molecular docking study showed the molecular interactions between enzymes and inhibitors, thus strongly supporting the experimental results. Overall, this work has fully demonstrated the feasibility of the established ANF platform for screening TIs from Cotinus coggygria Scop., and proved its great prospects for screening bioactive components from natural products.

The impacts of pink pepper (Schinus terebinthifolius Raddi) on fatty acids and cholesterol oxides formation in canned sardines during thermal processing.

The effect of adding pink pepper (Schinus terebinthifolius Raddi) fruits during sardines canning to minimize cholesterol oxidation were investigated. Canning resulted in an exchange of fatty acids, cholesterol and cholesterol oxides between fish muscle and liquid medium (soybean oil). It also induced lipid oxidation, which was demonstrated by the degradation of fatty acids and the formation of cholesterol oxides. Cholesterol oxides increased from 39.53 ± 2.14 µg/g (raw sardines) to 116.04 ± 0.78 µg/g (control sardines) after canning. However, lower levels were found in samples with pink pepper. Additionally, chromatographic analyses showed the migration of compounds (phenolic acids, flavonoids, tannins, terpenes) from pink pepper to sardines, indicating the constituents that could have contributed to its antioxidant properties. Thus, pink pepper may be highlighted as a suitable additive to reduce the intake of cholesterol oxides, minimizing the loss of nutritional quality in canned fish.

Extraction and characterization of pectic polysaccharides from Choerospondias axillaris peels: Comparison of hot water and ultrasound-assisted extraction methods.

Influences of conventional thermal and innovative non-thermal extraction methods on the physicochemical characteristics and properties of pectic polysaccharides from Choerospondias axillaris peels were investigated. Results showed that ultrasound-assisted extracted polysaccharides (UP) had a heterogeneous nature with lower molecular weight (127.7 kDa) and lower neutral sugar content (35.1%) but higher contents of protein (4.8%) and phenolic compounds (5.1%) than those of polysaccharides extracted by hot water (HP). Additionally, the monosaccharide composition results showed that glucose (77.8%) was the most abundant monosaccharide in HP, while arabinose (67.1%) was the most abundant monosaccharide in UP. The ultrasound significantly induced the degradation of polysaccharide chains but reduced the thermal degradation of phenolics. Finally, we found that UP had higher apparent viscosity, interfacial, emulsifying and antioxidant activity but lower α-glucosidase inhibition activity than those of HP. The results indicated that we could obtain polysaccharides with different functional and biological properties by using different extraction methods.

Geographical variation in the chemical composition, anti-inflammatory activity of the essential oil, micromorphology and histochemistry of Schinus terebinthifolia Raddi.

ETHNOPHARMACOLOGICAL RELEVANCE: Schinus terebinthifolia Raddi (Anacardiaceae) is rich in essential oil, distinguished by a predominance of monoterpenes and sesquiterpenes, it being widely used in traditional medicine for the treatment of inflammations. AIM OF STUDY: This study's objective was to investigate the chemical composition of the essential oil of S. terebinthifolia (EOST) collected in six states of Brazil, evaluate its anti-inflammatory effects in mice, and analyze the histochemistry and micromorphology of leaves and stems. MATERIALS AND METHODS: Aerial parts of S. terebinthifolia were collected in six states of Brazil, and the essential oil was extracted by hydrodistillation and analyzed by gas chromatography-mass spectrometry (GC-MS). The histochemistry and micromorphology of leaves and stems were performed using standard reagents, light and field emission scanning electron microscopy, beyond energy-dispersive X-ray spectroscopy. The EOST were evaluated for anti-inflammatory activity and hyperalgesia using the carrageenan-induced paw edema methodology. RESULTS: The EOST showed variation across the six states in its yield (0.40%-0.86%) and chemical composition: hydrocarbon monoterpenes (28.76%-47.73%), sesquiterpenes, (31.43%-41.76%), oxygenated monoterpenes (14.31%-19.57%), and oxygenated sesquiterpenes (4.87%-14.38%). Both α-pinene and limonene were predominant constituents of essential in five regions, except for one state where α-phellandrene and limonene were the dominant components. A comprehensive description of the leaf and stem micromorphology and histochemistry was performed. In the in vivo testing, all EOST samples exerted antiedematogenic and anti-hyperalgesic effects, when tested in a carrageenan-induced paw inflammation (mechanical and thermal hyperalgesia) model with oral doses of 30 mg/kg. CONCLUSION: Our results indicate that the EOST samples collected in six Brazilian states differed in their chemical composition but not their anti-inflammatory and antihyperalgesic effects, which was correlated with the synergistic effect of its components, collaborating the etnhopharmacologycal use of this plant due to its an anti-inflammatory effect. Also, micromorphology and histochemistry of leaves and stems presented in this study provide anatomical and microchemical information, which aids species identification.

Avaliação dos perfis fitoquímicos, antioxidante e citotóxicos do extrato alcoólico de folhas de cajá-manga (spondias dulcis) / Evaluation of phytochemical, antioxidant and cytotoxic profiles of the alcoholic extract of cajamanga leaves (spondias dulcis) / Evaluación de perfiles fitoquímicos, antioxidante y citotóxicos del extracto alcohólico de hojas de cajamanga (spondias dulcis)

Introdução: As espécies de plantas frutíferas, além da importância nutricional, podem ser usadas como fontes de compostos bioativos de interesse para o desenvolvimento de novos medicamentos. Entre as plantas com potencial terapêutico destacamos a Spondias dulcis (cajá-manga) indicada pela medicina tradicional para tratamento de condições médicas dos sistemas tegumentar, respiratório e genitourinário. Objetivos: Realizar a caraterização fitoquímica, antioxidante e citotóxica do extrato alcoólico bruto de folhas de Spondia dulcis. Material e Métodos: O extrato bruto foi obtido por percolação com o uso de 20 g das folhas secas e trituradas de Spondia dulcis e 100 ml de etanol a 70o por 24h. Na padronização do extrato foram utilizadas diferentes reações para análises de identificação de compostos do metabolismo secundário, bem como a determinação da atividade antioxidante pela captura do radical livre do DPPH. Após retirada do álcool por rotaevaporação, foram realizados testes de citotoxidade in vitro (hemólise) em solução glicosilada (5%) de hemácias (4%) nas diferentes concentrações do extrato (0,5%, 1% e 1,5%). Resultados: As análises fitoquímicas qualitativas identificaram a presença de compostos fenólicos, flavonoides, taninos genéricos e cumarinas. A avaliação dos compostos terpenoides mostrou presença de saponinas e ausência de sesquiterpenos e triterpenos. Os alcaloides foram detectados pelas reações de Bouchardat, Dragendorff, Mayer e Sheibler. A análise da atividade antioxidante do extrato indicou alta capacidade antioxidante (71%). No ensaio de hemólise a citotoxidade foi baixa nas concentrações de 0,5% e 1% e relativa na concentração de 1,5%. Conclusão: O extrato alcoólico bruto de Spondia dulciscontém compostos bioativos anti-inflamatórios, alta capacidade antioxidante e baixa citotoxicidade até a concentração de 1,5% com potencial de aplicação farmacológica (AU)

Introduction: Fruit plant species, in addition to their nutritional importance, can be used as sources of bioactive compounds of interest for the development of new drugs. Among the plants with therapeutic potential, we highlight Spondias dulcis (cajá-manga) indicated by traditional medicine for the treatment of medical conditions of the integumentary, respiratory and genitourinary systems. Objectives: To carry out the phytochemical, antioxidant and cytotoxic characterization of the leaves crude alcoholic extract of Spondia dulcis. Material and Methods: The crude extract was obtained by percolation using 20 g of dried and crushed leaves of Spondia dulcis and 100 ml of ethanol at 70° for 24 hours. In the standardization of the extract, different reactions were used to analyze the identification of compounds of secondary metabolism, as well as the determination of the antioxidant activity by capturing the free radical of DPPH. After removing the alcohol by rotary evaporation, in vitro cytotoxicity tests (hemolysis) were performed in a glycosylated solution (5%) of red blood cells (4%) at different concentrations of the extract (0.5%, 1% and 1.5%). Results: Qualitative phytochemical analyzes identified the presence of phenolic compounds, flavonoids, generic tannins and coumarins. The evaluation of terpenoid compounds showed the presence of saponins and the absence of sesquiterpenes and triterpenes. Alkaloids were detected by Bouchardat, Dragendorff, Mayer and Sheibler reactions. The analysis of the antioxidant activity of the extract indicated that the crude extract of Spondia dulcis has a high antioxidant capacity (71%). In the hemolysis assay, cytotoxicity was low at concentrations of 0.5% and 1% and relative at concentrations of 1.5%. Conclusion: The crude alcoholic extract of Spondia dulcis contains anti-inflammatory bioactive compounds, high antioxidant capacity and low cytotoxicity up to a concentration of 1.5% with potentialfor pharmacological application (AU)

Introducción: Las especies de plantas frutales, además de su importancia nutricional, pueden ser utilizadas como fuentes de compuestos bioactivos de interés para el desarrollo de nuevos fármacos. Entre las plantas con potencial terapéutico destacamos Spondias dulcis (cajamanga) indicada por la medicina tradicional para el tratamiento de afecciones médicas de los sistemas tegumentario, respiratorio y genitourinario. Objetivos: Realizar la caracterización fitoquímica, antioxidante y citotóxica del extracto alcohólico crudo de hojas de Spondia dulcis. Material y Métodos: El extracto crudo se obtuvo por percolación utilizando 20 g de hojas secas y trituradas de Spondia dulcis y 100 ml de etanol a 70° durante 24 horas. En la estandarización del extracto se utilizaron diferentes reacciones para analizar la identificación de compuestos de metabolismo secundario, así como la determinación de la actividad antioxidante mediante la captura del radical libre de DPPH. Después de eliminar el alcohol por evaporación rotatoria, se realizaron pruebas de citotoxicidad (hemólisis) in vitro en una solución glicosilada (5%) de glóbulos rojos (4%) a diferentes concentraciones del extracto (0,5%, 1% y 1,5%). Resultados: Los análisis fitoquímicos cualitativos identificaron la presencia de compuestos fenólicos, flavonoides, taninos genéricos y cumarinas. La evaluación de los compuestos terpenoides mostró la presencia de saponinas y la ausencia de sesquiterpenos y triterpenos. Los alcaloides fueron detectados por las reacciones de Bouchardat, Dragendorff, Mayer y Sheibler. Los estudios han demostrado que el extracto crudo de Spondiadulcis tiene una alta capacidad antioxidante (71%). En el ensayo de hemólisis, la citotoxicidad fue baja a concentraciones de 0,5% y 1% y relativa a concentraciones de 1,5%. Conclusión: El extracto alcohólico crudo de Spondia dulcis contiene compuestos bioactivos antiinflamatorios, alta capacidad antioxidante y baja citotoxicidad hasta una concentración de 1,5% conpotencial de aplicación farmacológica (AU)