Brazilin cream from Caesalpinia sappan inhibit periodontal disease: in vivo study.

Background: Gingivitis is an inflammation of the gums that is the initial cause of the development of periodontal disease by the activity of Nuclear Factor-kappa B (NF-κB), Interleukin-1ß (IL-1ß), Interleukin-6 (IL-6), p38, and Tumor Necrosis Factor-α (TNF-α). Unaddressed chronic inflammation can lead to persistent disturbances in other parts of the body. Brazilin is a naturally occurring plant chemical that may have antibacterial and anti-inflammatory effects. Treatment based on the natural plant compound, brazilin, is developed in the form of a topical cream for easy application. Objective: The aim is to develop the natural compound brazilin in the form of a topical cream as an anti-inflammatory agent to reduce NF-κB expression through Imunohistochemistry (IHC) methods, and the expression of pro-inflammatory genes IL-1ß, IL-6, p38, and TNF-α. Methods: Male Sprague-Dawley rats were induced with gingivitis using P. gingivalis bacteria. The observed groups included rats treated with a single application of brazilin cream and rats treated with two applications of brazilin cream. The treatment was administered for 15 days. On days 3, 6, 9, 12, and 15, anatomical wound observations and wound histology using hematoxylin-eosin and Masson's Trichrome staining were performed. NF-κB protein expression was analyzed using the IHC method. Gingival inflammation gene expression of NF-κB, IL-1ß, IL-6, p38, and TNF-α was measured using q-RTPCR. Results: Single and double applications of brazilin cream increased angiogenesis and decreased NF-κB protein expression, in addition to the IL-1ß, IL-6, p38, and TNF-α gene expressions. Conclusion: In a rat gingivitis model, Brazilin cream may function as an anti-inflammatory agent in the gingival tissue.

Strawberries treated with biodegradable film containing plant extracts.

Strawberry (Fragaria x ananassa Duch.) is a highly perishable fruit whose characteristics make it susceptible to developing microorganisms. Plant extracts have been studied as an alternative to pesticides to control spoilage microorganisms, responding to the expectation of the population seeking a healthier way of life. The fungus Botrytis cinerea is a facultative pathogen of vegetables, which can affect all stages of the development of several fruits, such as the strawberry, where it causes gray rot. Trichilia catigua (catuaba), Paullinia cupana (guarana), Stryphnodendron barbatiman (barbatimão), and Caesalpinia peltophoroides (sibipiruna) are planted in the Brazilian flora and have demonstrated pharmacological properties in their extracts. This work aimed to treat strawberries with a biodegradable film containing extracts of these species to evaluate strawberry conservation. There were notable distinctions in mass loss between the extract-treated and control samples. The pH, total acidity (TA), and soluble solids parameters exhibited consistently significant means across both sets of samples. Luminosity increased over the course of days in the color parameters, with the exception of strawberries coated with guarana. The red color showed greater intensity, except for those coated with barbatimão extract. Considering the results, it is possible to conclude that the coatings used can become an alternative to enhance the conservation of strawberries.

Brazilin from Caesalpinia sappan inhibits viral infection against PRRSV via CD163ΔSRCR5 MARC-145 cells: an in silico and in vitro studies.

This research aimed to identify bioactive compounds from Caesalpinia sappan extract that function as novel porcine reproductive and respiratory syndrome virus (PRRSV) infection inhibitors by computational molecular screening. We obtained a set of small-molecule compounds predicted to target the scavenger receptor cysteine-rich domain 5 (SRCR5) of CD163. In addition, the functions of positive hits were assessed and verified utilizing an in vitro antiviral activity assay with PRRSV-infected MARC-145 cells. Combining molecular docking with the results of binding affinity and ligand conformation, it was found that brazilin had the highest binding energy with the SRCR5 receptor compared to catechin and epicatechin (- 5.8, - 5.5, and - 5.1 kcal/mol, respectively). In terms of molecular mechanics, the binding free energy between the SRCR5 receptor was - 15.71 kcal/mol based on the Poisson-Boltzmann surface area of brazilin. In addition, PRRSV infection in MARC-145 cells was significantly inhibited by brazilin compared to the control (virus titer, 4.10 vs. 9.25 TCID50/mL, respectively). Moreover, brazilin successfully limited the number of PRRSV RNA copies in MARC-145 cells as determined by RT-qPCR. By inhibiting the PRRSV-CD163 interaction with brazilin from Caesalpinia sappan, it may be possible to prevent PRRSV infection in pigs, as suggested by this research.

Molecular docking of brazilin and its analogs to barrier-to-autointegration factor 1 (BAF1).

The tetracyclic phenolic compound brazilin, derived from the wood of Caesalpinia sappan, has been shown to bind to the chromatin protein BAF1 (barrier-to-autointegration factor 1), a protein essential to maintain integrity of the nuclear envelope in cells. BAF1 plays a role in cancer development. Using molecular docking, we have located the binding site for brazilin on the surface of the BAF1 monomer and compared its binding to that of four analogs. The oxidized product brazilein (ΔE = -57.7 kcal/mol) exhibits a higher affinity for BAF1 compared to the reduced form brazilin (ΔE = -38.2 kcal/mol). Incorporation of a 4-hydroxyl substituent on the indenochromene unit affords hematoxylin and hematein. In silico analysis predicts that the oxidized form hematein (ΔE = -66.2 kcal/mol) displays a higher affinity for BAF1 than the reduced form hematoxylin (ΔE = -42.2 kcal/mol). In contrast, the atypical bis-lactone product brazilide A cannot form good complexes with BAF1. The analysis points to the formation of more stable BAF1 complexes with the oxidized molecules compared to the reduced ones, but the position of the binding site on the protein cavity is different for brazilin/hematoxylin compared to brazilein/hematein. Our study may be useful to guide the design of BAF1 ligands.

Phytochemical characterisation and in vivo antilithiatic activity of the stems of Caesalpinia bahamensis (Brasilete).

The aim of this work was to identify the main chemical constituents and to evaluate the antilithiatic activity of the aqueous and hydroalcoholic extracts of stems of Caesalpinia bahamensis Lam. Fractionation and isolation of constituents from the hydroalcoholic extract was carried out by flash chromatography and semi-preparative liquid chromatography. The antilithiatic activity of the aqueous and hydroalcoholic extracts was evaluated in Wistar rats, where kidney stones were induced by ethylene glycol and ammonium chloride. Creatinine, calcium, and oxalate levels were evaluated and histological analysis was carried out. The homoisoflavonoids protosappanin B, 10-methyl-protosappanin B and brazilin were isolated and the antilithiatic activity of the aqueous and hydroalcoholic extracts was demonstrated by the reduction of the concentration of calcium and oxalate in urine compared to the lithiasis group. It was corroborated by histological analysis. Brazilin and protosappanin B were proposed as chemical markers for this plant species.

Polysaccaride-rich extract of Caesalpina ferrea stem barks attenuates mice acute inflammation induced by zymosan: Oxidative stress modulation.

ETHNOPHARMACOLOGICAL RELEVANCE: Stem barks of Caesalpinia ferrea Mart. Ex Tul. (Caesalpiniaceae), also known as pau-ferro jucá or jucaína, are popularly used to treat contusions, diabetes, rheumatism and other inflammatory conditions in the form of tea, lick or decoction. OBJECTIVE: To evaluate the effect of the polysaccharide-rich extract obtained from C. ferrea stem barks (PE-Cf) in mice models of acute inflammation induced by zymosan and the involvement of oxidative stress biomarkers. MATERIALS AND METHODS: Mice were treated with PE-Cf (0.001, 0.01, 0.1, 1 mg/kg) by endovenous route (i.v.) or per oral (p.o.) 30 or 60 min before injection of the inflammatory stimuli zymosan (0.5 mg; intraperitoneal or subcutaneous intraplantar). The inflammatory parameters (edema, nociception, leukocyte migration) and oxidative stress markers (myeloperoxidase-MPO, malondialdehyde-MDA, nitrite, reduced glutathione-GSH, glutathione peroxidase-GPx) were evaluated in the models of paw edema (hidropletysmometry/expressed as ml or area under curve-AUC) and peritonitis (optical microscopy/expressed as n° of cells/mm3 of peritoneal fluid). Statistical analysis was performed by ANOVA, followed by Bonferroni test. RESULTS: PE-Cf (0.1, 0.01 and 1 mg/kg) dose-dependently inhibited paw edema, showing maximal effect (74%) at 1 mg/kg in the 5th (52 ± 9.6 µl vs. zymosan: 204 ± 3.6 µl). PE-Cf (1 mg/kg) also inhibited by 43% MPO activity in the paw tissues (17 ± 1 vs. zymosan: 30 ± 2.6 U/mg). Besides, 4 h after peritonitis induction, PE-Cf (1 mg/kg) reduced neutrophil migration by 84% (432 ± 45 vs. zymosan: 2651 ± 643 cells/mm3); visceral nociception by 76% (3 ± 0.6 vs. zymosan: 16 ± 4 writhes); nitric oxide by 73% (0.131 ± 0.033 vs. zymosan: 0.578 ± 0.185 NO2-/NO3-ml); MDA (98 ± 10 vs. zymosan:156 ± 21 U/ml), and increased GSH by 65% (736 ± 65 vs. zymosan: 259 ± 58 µmol/ml) and GPx by 72% (0.037 ± 0.007 vs. zymosan: 0.010 ± 0.005 U/mg protein). CONCLUSION: The polysaccharide-rich extract of Caesalpinia ferrea stem barks present anti-inflammatory and antioxidant effects in mice models of acute inflammation induced by zymosan.

Evaluation of chemotherapy and P2Et extract combination in ex-vivo derived tumor mammospheres from breast cancer patients.

The main cause of death by cancer is metastasis rather than local complications of primary tumors. Recent studies suggest that breast cancer stem cells (BCSCs), retains the ability to self-renew and differentiate to repopulate the entire tumor, also, they have been associated with resistance to chemotherapy and tumor recurrence, even after tumor resection. Chemotherapy has been implicated in the induction of resistant phenotypes with highly metastatic potential. Naturally occurring compounds, especially phytochemicals such as P2Et, can target different populations of cancer cells as well as BCSC, favoring the activation of immune response via immunogenic tumor death. Here, we evaluated the presence of BCSC as well as markers related to drug resistance in tumors obtained from 78 patients who had received (or not) chemotherapy before surgery. We evaluated the ex vivo response of patient tumor-derived organoids (or mammospheres) to chemotherapy alone or in combination with P2Et. A xenotransplant model engrafted with MDA-MB-468 was used to evaluate in vivo the activity of P2Et, in this model P2Et delay tumor growth. We show that patients with luminal and TNBC, and those who received neoadjuvant therapy before surgery have a higher frequency of BCSC. Further, the treatment with P2Et in mammospheres and human breast cancer cell lines improve the in vitro tumor death and decrease its viability and proliferation together with the release of immunogenic signals. P2Et could be a good co-adjuvant in antitumor therapy in patients, retarding the tumor growth by enabling the activation of the immune response.

The delay in cell death caused by the induction of autophagy by P2Et extract is essential for the generation of immunogenic signals in melanoma cells.

P2Et extract obtained from the Caesalpinia spinosa plant is abundant in phenolic compounds such as gallic acid and ethyl gallate and can generate signals to activate the immune response by inducing a mechanism known as immunogenic cell death in murine models of breast cancer and melanoma. Immunogenic cell death involves mechanisms such as autophagy, which can be modulated by various natural compounds, including phenolic compounds with a structure similar to those found in P2Et extract. Here, we determine the role of autophagy in apoptosis and the generation of immunogenic signals using murine wild-type B16-F10 melanoma cells and cells with beclin-1 gene knockout. We show that P2Et extract and ethyl gallate induced autophagy, partially protecting tumor cells from death and promoting calreticulin exposure and the release of ATP. Although ethyl gallate showed a mechanism similar to that of P2Et, the induction of apoptosis and immunogenic signals was significantly weaker. In contrast, gallic acid-induced autophagy acted by blocking autophagic flux, which was associated with increased cell death. However, this compound did not induce any of the immunogenic death signals evaluated. Therefore, the complex extract has greater antitumor potential than isolated compounds. Here, we show that inducing autophagic flux with P2Et protects cancer cells from cell death and that this delay in cell death is required for the generation of immunogenic signals.

Caesalpinia ferrea C. Mart. (Fabaceae) Phytochemistry, Ethnobotany, and Bioactivities: A Review.

Caesalpinia ferrea C. Mart., popularly known as "Jucá" or "Pau-ferro", belongs to the Fabaceae family, and is classified as a native and endemic species in Brazil. Numerous studies that portray its ethnobotany, chemical composition, and biological activities exist in the literature. The present study aimed to systematically review publications addressing the botanical aspects, uses in popular medicine, phytochemical composition, and bioactivities of C. ferrea. The searches focused on publications from 2015 to March 2020 using the Scopus, Periódicos Capes, PubMed, Google Scholar, and ScienceDirect databases. The leaves, fruits, seeds, and bark from C. ferrea are used in popular medicine to treat disorders affecting several systems, including the circulatory, immune, cardiovascular, digestive, respiratory, genitourinary, musculoskeletal, and conjunctive systems. The most commonly found chemical classes in phytochemical studies are flavonoids, polyphenols, terpenoids, tannins, saponins, steroids, and other phenolic compounds. The biological properties of the extracts and isolated compounds of C. ferrea most cited in the literature were antibacterial, antifungal, antioxidant, antiproliferative, anti-inflammatory, and healing potential. However, further studies are still needed to clarify a link between its traditional uses, the active compounds, and the reported pharmacological activities, as well as detailed research to determine the toxicological profile of C. ferrea.

Aqueous ethanol extract of Libidibia ferrea (Mart. Ex Tul) L.P. Queiroz (juca) exhibits antioxidant and migration-inhibiting activity in human gastric adenocarcinoma (ACP02) cells.

Libidibia ferrea (juca) is a plant belonging to the Fabaceae (Leguminosae) family, whose antioxidant activity has been widely described in the literature. We evaluated this parameter of Aqueous ethanol extract (AE), ethyl acetate (ACO), chloroform (CLO) and hexane (HEX) extracts of L. ferrea. We then tested the most active extract for its toxicity and ability to inhibit migratory activity in the ACP02 gastric adenocarcinoma cell line in vitro. The AE and ACO extracts both had antioxidant activity, the AE extract showing greater potential. This may reflect that both extracts contained phenolic compounds. Although AE extract showed no cytotoxic, mutagenic or genotoxic effect, it altered cell morphology and migration activity. Analysis of apoptosis/necrosis indicated that this parameter does not appear to account for the apparent ability of AE to inhibit cancer cell migration. We speculate that the morphological changes in AE-treated cells could be due to cytoskeleton alterations related to the presence of myo-inositol in AE extract. Together, our results demonstrate this extract of L. ferrea can act as an exogenous antioxidant and might prove useful in efforts to fight secondary tumors.

[Preparation of brazilein from Caesalpinia sappan by high performance countercurrent chromatography].

Brazilein is among the main chemical constituents of Caesalpinia sappan. It has diverse pharmacological activities. Modern pharmacological studies have shown that the compound has antitumor, anti-inflammatory, antibacterial, antioxidant, immunomodulatory, and other pharmacological activities. Brazilein is often used as a stain in various industries. The separation of brazilein by traditional column chromatography will not only result in contamination of the chromatographic column materials, but also lead to loss of the active ingredient. Countercurrent chromatography is an advanced liquid-liquid chromatographic separation technique. It has been widely used for natural product separation and isolation as it offers several advantages, such as low solvent consumption, a highly selective solvent system, and high recoveries. Typical countercurrent chromatography techniques include centrifugal partition chromatography (CPC), high-speed countercurrent chromatography (HSCCC), and high performance countercurrent chromatography (HPCCC). It is well known that choosing a suitable solvent system is vital in countercurrent separation. Therefore, two methods were introduced for choosing a suitable solvent system. One is the generally useful estimation of solvent systems (GUESS) method, which employs thin-layer chromatography (TLC) to identify a suitable solvent system with minimal labor for the rapid purification of target compounds, and another is the Shake-Flash method. The solvent system could be determined by observing the distribution of the sample in the upper and lower phases. Two kinds of solvent systems were screened using the TLC-GUESS and Shake-Flash methods, and tested through the analysis mode of the HPCCC instrument. The results showed that chloroform-methanol-water (4:3:2, v/v/v) was the optimal solvent system for HPCCC separation. A total of 15.2 mg of brazilein and 5.7 mg of caesappanin C were obtained from an ethyl acetate extract with high purities (95.6% and 89.0%, analyzed by HPLC) in one step using the preparation mode of HPCCC, the reversed-phase liquid chromatography mode with the apparatus rotated at 1600 r/min, a flow rate of 10 mL/min, separation temperature of 25℃, and detection wavelength of 285 nm. Their structures were determined by spectroscopic and spectrometric analyses. Brazilein stained the solid packing material in the column and was difficult to elute. The results showed that the use of HPCCC for the separation of brazilein can not only prevent the loss of target active ingredients in Caesalpinia sappan, but also shorten the separation and purification times and improve the operating efficiency. Therefore, HPCCC can be used for the separation and preparation of other pigment compounds in Caesalpinia sappan and other dye plants.

Galactomannan from the seeds of Caesalpinia pulcherrima prevents indomethacin-induced gastrointestinal damage via neutrophil migration.

Galactomannans are neutral polysaccharides isolated from the endosperm of some Leguminosae seeds. They consist of a (1 → 4) linked ß-mannopyranosyl backbone partially substituted at O-6 with α-d-galactopyranosyl side groups. C. pulcherrima have anti-inflammatory and muco-adhesive proprieties. Acute gastritis is an inflammatory disease triggered by use of non-steroidal anti-inflammatory drugs. We investigated the gastroprotective effect of galactomannan obtained from the seeds of Caesalpinia pulcherrima L. (GM-CP) in acute gastritis model induced by indomethacin. Gastritis was induced with indomethacin (30 mg/kg, P.·O.) in female Swiss mice. Animal groups (n = 7) were pretreated with saline-dissolved GM-CP (3 mg/kg, 10 mg/kg, 30 mg/kg, P.O.) or vehicle 1 h before gastritis induction. Mice were euthanized seven hours after the induction. The stomach and blood samples were collected for analysis. At 10 mg/kg, GP-CP reduced the extension of macroscopic lesion and the loss of superficial cells by alleviating inflammatory symptoms (neutrophil infiltration, migration and adhesion of mesenteric leukocytes, production of TNF-α and thiobarbituric acid reactive species (TBARS) and helping to maintain mucin labeling of the tissue. Thus, the findings of the study suggest that GM-CP exhibits gastroprotective effects.

Antibacterial activity of compounds isolated from Caesalpinia coriaria (Jacq) Willd against important bacteria in public health.

Antimicrobial resistance has been increasing in recent years and is most frequently found in pathogenic microorganisms resistant or multiresistant to drugs. The secondary metabolites of plants have been evaluated as alternatives for control and treatment of these microorganisms. The aim of this study was to isolate and identify the secondary metabolites with antibacterial activity from Caesalpinia coriaria (Jacq) Willd fruit. Hydroalcoholic extract (CCHA), was subjected to a bipartition with ethyl acetate giving two fractions an aqueous (Aq-F) and an organic (EtOAc-F). The isolation of bioactive fraction (EtOAc-F) allowed obtain two important compounds, methyl gallate (1) and gallic acid (2). These compounds were identified by high-performance liquid chromatography (HPLC) and nuclear magnetic resonance (NMR). The CCHA, both fractions and the isolated compounds were evaluated in vitro to determine their Minimal Inhibitory Concentration (MIC) and Minimal Bactericidal Concentration (MBC) against Escherichia coli, Pseudomonas aeruginosa, Salmonella typhi, Listeria monocytogenes and Staphylococcus aureus. Gallic acid (2) showed the lowest MIC on S. typhi, (0.156 mg/mL), L. monocytogenes and S. aureus (1.25 mg/mL), while methyl gallate (1) had the best inhibitory effect against E. coli and P. aeruginosa (1.25 mg/mL). On the other hand, methyl gallate (1) showed the best MBC on P. aeruginosa (2.50 mg/mL), and gallic acid (2) had the lowest MBC on P. aeruginosa and L. monocytogenes. In conclusion, methyl gallate (1) and gallic acid (2) are the compounds responsible for the antibacterial activity of Caesalpinia coriaria fruit.

Optimization of Caesalpinia sappan L. heartwood extraction procedure to obtain the highest content of brazilin and greatest antibacterial activity.

OBJECTIVE: The objective of the work was to optimize the extraction conditions of Caesalpinia sappan L. heartwood in order to maximize the brazilin content and antibacterial activity of the extract. METHODS: Two independent factors were studied: extraction temperature (45-95 °C) and extraction time (30-60 min). In addition, five dependent factors were monitored, including extraction yield, brazilin content, and clear zones against Staphylococcus aureus TISTR 1466, Staphylococcus epidermidis TISTR 518 and Propionibacterium acnes DMST 14961. The brazilin content was quantified by high-performance liquid chromatography and antibacterial activity was determined by disk diffusion assay. RESULTS: The high temperature provided high total extract yield as well as brazilin content, while extraction time had little effect on yield or brazilin content. Extraction time had a positive effect, while extraction temperature had little effect on clear zone against S. aureus. The largest clear zone against S. epidermidis was achieved at low extraction temperature and long extraction time. Conversely, short extraction time and high extraction temperature provided the largest clear zone against P. acnes. The optimal conditions providing the highest brazilin content was an extraction temperature and extraction time of 95 °C and 30 min, respectively. The same optimal conditions also provided the simultaneous greatest antibacterial activity against the three bacteria. Modeled optimal conditions were validated be conducting extraction using these values. Yield and antibacterial activity of the resulting extract demonstrated that the model had a low percentage error. CONCLUSION: The optimal condition will be used as a standard condition for extraction of C. sappan heartwood to maximize brazilin content and antibacterial activity.

Physicochemical, thermal and rheological properties of synthesized carboxymethyl tara gum (Caesalpinia spinosa).

Carboxymethyl tara gum (CMTG) was synthesized from the reaction between tara gum (TG) and monochloroacetic acid (MCA) in the presence of sodium hydroxide. The modification reaction was optimized in terms of the MCA/NaOH ratio, reaction time and temperature evaluated for degree of substitution (DS). The etherification was confirmed by FTIR and 13C NMR spectroscopy, and it was characterized by different analyses. After carboxymethylation, CMTG showed new bonds at 1592, 1413 and 1320 cm-1 by FTIR and a new peak at δ = 178 ppm by 13C NMR in response to the insertion of the carbonyl group. The microscopy showed higher degradation on the surface of the CMTG particles, and XRD indicated low crystallinity of the CMTG. Static light scattering demonstrated a reduction in the molar mass of tara gum after carboxymethylation. Thermal analysis (TGA and DSC) revealed a lower thermal stability of carboxymethylated gum compared to that of unmodified gum. Despite the insertion of negative charges demonstrated by the potential-zeta, CMTG and TG presented pseudoplastic behavior according to the rheological analyses, and CMTG presented lower viscosity at the concentrations that were studied.

Crude extract from Libidibia ferrea (Mart. ex. Tul.) L.P. Queiroz leaves decreased intra articular inflammation induced by zymosan in rats.

BACKGROUND: Libidibia ferrea (L. ferrea) has been used in folk medicine to treat several conditions and to prevent cancer. This study performed a chromatographic analysis of the crude aqueous extract of Libidibia ferrea (Mart. ex. Tul.) L.P. Queiroz (LfAE) leaves and evaluated its in vivo antioxidant and anti-inflammatory potential. METHODS: Polyphenols present in LfAE were characterized by high performance liquid chromatography (HPLC). Anti-inflammatory activity was studied in an experimental model of zymosan-induced intra-articular inflammation, conducted in Wistar rats treated with LfAE at the doses of 100, 200 and 300 mg/kg by gavage. Synovial fluid was collected for global leukocyte count, for spectrocopical UV/VIS analysis of myeloperoxidase (MPO) activity, total glutathione and malondialdehyde (MDA), and for quantification of inflammatory cytokines IL1-ß and TNF-α by enzyme-linked immunosorbent assay. Synovial membrane was collected for histological analysis. The level of statistical significance was p < 0.05. RESULTS: HPLC detected concentrations of 1.56 (0.77) %m/m for ellagic acid and 1.20 (1.38) %m/m for gallic acid in LfAE leaves. Treatment with LfAE at all doses significantly decreased the leukocyte influx into the synovial fluid (p < 0.001) and myeloperoxidase activity (p < 0.001), an important marker of neutrophils. LfAE at doses of 100 (p < 0.05), 200 and 300 mg/kg (p < 0.001) also reduced the levels of MDA. LfAE at doses of 200 and 300 mg/kg significantly decreased the levels of IL-1ß (p < 0.05) and TNF-α (p < 0.001). All doses of LfAE resulted in increased levels of total glutathione (p < 0.001). Histopathological findings confirmed a reduction of the inflammatory infiltrate in the rats treated with LfAE at a dose of 200 mg/kg (p < 0.05). CONCLUSION: LfAE has an important anti-oxidant and anti-inflammatory effect on intra-articular inflammation.

Effect of Caesalpinia coriaria Fruits and Soybean Oil on Finishing Lamb Performance and Meat Characteristics.

To evaluate phenolic compounds and whether the combination of a tanniferous fruit and soybean oil could improve the performance, meat characteristics, and fatty acid (FA) profile in lambs, an experiment was conducted over 40 days with twenty creole male lambs (23.71 ± 3.46 kg). The lambs were allotted in a completely randomised design, with factorial arrangement 2 × 2, with the following dietary treatments: (1) control diet, (2) 2% Caesalpinia coriaria ground fruit dry matter (DM), (3) 2% soybean oil DM, and (4) 2% Caesalpinia coriaria fruit plus 2% soybean oil. The concentration of condensed tannins (CT) in Caesalpinia coriacea was 21.71 g/kg DM. No interactions were detected (P > 0.05) among soybean oil and Caesalpinia coriaria, and there were no differences in daily gain, intake, and feed conversion. Soybean oil reduced (P < 0.05) DM digestibility (68.05 versus 59.56%). In fat from the longissimus thoracis et lumborum (LTL) muscle, only linoleic acid presented differences (P < 0.05) between treatments. The combination of Caesalpinia coriacea fruit and soybean oil did not improve lamb performance at the included levels.

Brazilin and Caesalpinia sappan L. extract protect epidermal keratinocytes from oxidative stress by inducing the expression of GPX7.

Caesalpinia sappan L., belonging to the family Leguminosae, is a medicinal plant that is distributed in Southeast Asia. The dried heartwood of this plant is used as a traditional ingredient of food, red dyes, and folk medicines in the treatment of diarrhea, dysentery, tuberculosis, skin infections, and inflammation. Brazilin is the major active compound, which has exhibited various pharmacological effects, including anti-platelet activity, anti-hepatotoxicity, induction of immunological tolerance, and anti-inflammatory and antioxidant activities. The present study aimed to evaluate the antioxidant activity and expression of antioxidant enzymes of C. sappan L. extract and its major compound, brazilin, in human epidermal keratinocytes exposed to UVA irradiation. Our results indicated that C. sappan L. extract reduced UVA-induced H2O2 production via GPX7 activation. Moreover, brazilin exhibited antioxidant effects that were similar to those of C. sappan L. via glutathione peroxidase 7 (GPX7), suggesting that C. sappan L. extract and its natural compound represent potential treatments for oxidative stress-induced photoaging of skin.

In Vitro Anthelmintic Activity of Methanolic Extract from Caesalpinia coriaria J. Willd Fruits against Haemonchus contortus Eggs and Infective Larvae.

The aim of this study was to evaluate the in vitro lethal effect of a methanolic extract (ME) from Caesalpinia coriaria fruits against Haemonchus contortus eggs and infective larvae. The anthelmintic activity was assessed using the egg hatching inhibition assay (EHI) and the mortality test. The ME was assessed using five concentrations as follows: 6.15, 3.12, 1.56, and 0.78 mg/mL to eggs and 150, 100, 75, and 50 mg/mL to larvae, respectively. Ivermectin (5 mg/mL) was used as positive control and 4% methanol and distilled water were used as negative controls. The data of ovicidal and larvicidal effect were analyzed with a completely randomized design through ANOVA analysis using the general linear model (GLM) and lethal concentrations (LC50 and LC90) were estimated through a Probit analysis using the SAS program. A clear ME increased concentration dependence effect was observed in the EHI and mortality tests. The highest activity of the methanolic extract was observed at the highest concentration (P < 0.05) to obtain a similar effect to the positive control (ivermectin), with LC50 = 78.38 and 0.00064 mg/mL and LC90 =235.63 and 0.024 mg/mL, respectively, for larvae and eggs. The results indicate that the C. coriaria fruit ME possesses in vitro ovicidal and larvicidal properties (gallotannins: methyl gallate) against H. contortus that needs to be investigated more in vivo for the control of gastroenteric nematodes in ruminants.

Uso de extratos de polissacarídicos da planta medicinal caesalpinea ferrea na estimulação do edema na pata de ratos / Use of polysaccharidic extracts from the Caesalpinia ferrea medicinal plant in edema stimulation in the rats paw

O sistema imune inato é capaz de promover respostas inflamatórias imediatas a lesões e atua como mecanismo inicial de defesa no corpo, estando seus defeitos associados a respostas exacerbadas, como na asma, ou a deficiências que levam a infecções graves,de aparecimento rápido. Assim, um melhor entendimento do processo inflamatório, bem como a utilização de moléculas modulatórias é de extrema importância. Polissacarídeos de plantas são reconhecidos por suas atividades antiviral, antitumoral, imunoestimulante, anti-inflamatória e anticoagulante. O extrato polissacarídico da casca de Caesalpinia ferrea(Caesalpinioideae), planta muito utilizada na medicina popular, possui efeito cicatrizante de feridas. O presente estudo avaliou a atividade inflamatória de extratos polissacarídicos obtidos da casca (EPC), vagens (EPV) e folhas (EPF) de Caesalpinia ferrea. A planta foi coletada em Custódio, município de Quixadá-CE, para extração dos polissacarídeos.Casca, vagens e folhas foram suspensas em metanol, ressuspensas em NaOH (0,1 M), neutralizadas com HCl (1 M) e avaliadas quanto aos teores de carboidrato e proteína. EPC, EPV e EPF foram testados em ratos Wistar fêmeas (150-250g) no modelo de edema de pata, induzido pela administração subcutânea (s.c.) intraplantar de dextrana (300 μg), carragenana (300 μg) ou dos extratos polissacarídicos (0,01, 0,1 e 1 mg/kg), e mensurado por plestismometria(0-8 horas). Os extratos polissacarídicos apresentaram elevado teor de carboidratos (EPC: 44%; EPV: 31%; EPF: 44%) e atividade edematogênica, com maior eficácia na dose de 1 mg/kg: EPC(0,75±0,05 mL vs. salina: 0,45±0,04 mL); EPV (0,46±0,06 mL; vs salina: 0,16±0,02 mL); EPF (0,3±0,01 mL; salina: 0,18±0,02 mL).

The innate system is able to promote immediate inflammatory response to injuries, acting as an initial defense mechanism, being its failing associated to exacerbated response as asthma or to deficiencies, that lead to rapid serious infection. Thus, the better understanding of this process as well as the use of modulatory molecules is extremely important. Plant polysaccharides are recognized for its antiviral, antitumor, immunostimulant, anti-inflammatory and anticoagulant effects. Polysaccharide extract obtained from Caesalpinia ferreabarks, a plant widely is used in folk medicine for wound healing, among others. This effect had been confirmed for the polysaccharide extract obtained from it barks. The present study evaluated the inflammatory activity of polyssaccharide extracts obtained from barks (PEB), pods (PEP) and leaves (PEL) of Caesalpinia ferrea. The plant was collected at Custódio, Quixadá-CE for obtention of the polyssaccharide extracts. Barks, pods and leaves were suspended in methanol, re-suspended in 0.1 M NaOH, neutralized with 1 M HCl and evaluated for carbohydrate and protein content. PEB, PEP and PEL were tested in female Wistar rats (150-250g) in the model of paw edema induced by subcutaneous (s.c.) intraplantar administration of dextran (300 μg), carrageenan (300 μg) or polyssaccharide extracts (0.01, 0.1 e 1 mg/kg) and measured by plesthysmometry (0 -8h). C. ferrea polyssaccharide extracts presented high content of carbohydrate (PEB: 44%; PEP: 31%; PEL: 44%) and edematogenic activity, with maximal efficacy at 1 mg/kg: PEB (0.75±0.05 mL vs. saline: 0.45±0.04 mL); PEP (0.46±0.06 mL; vs saline: 0.16±0.02 mL); PEL (0.3±0.01 mL; saline: 0.18±0.02 mL).