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Marine organisms represent a potential source of secondary metabolites with various therapeutic properties. However, the pharmaceutical industry still needs to explore the algological resource. The species Caulerpa lamouroux Forssk presents confirmed biological activities associated with its major compound caulerpin, such as antinociceptive, spasmolytic, antiviral, antimicrobial, insecticidal, and cytotoxic. Considering that caulerpin is still limited, such as low solubility or chemical instability, it was subjected to a structural modifications test to establish which molecular regions could accept structural modification and to elucidate the cytotoxic bioactive structure in Vero cells (African green monkey kidney cells, Cercopithecus aethiops ; ATCC, Manassas, VA, USA) and antiviral to Herpes simplex virus type 1. Substitution reactions in the N -indolic position with mono- and di-substituted alkyl, benzyl, allyl, propargyl, and ethyl acetate groups were performed, in addition to conversion to their acidic derivatives. The obtained analogs were submitted to cytotoxicity and antiviral activity screening against Herpes simplex virus type 1 by the tetrazolium microculture method. From the semi-synthesis, 14 analogs were obtained, and 12 are new. The cytotoxicity assay showed that caulerpin acid and N -ethyl-substituted acid presented cytotoxic concentrations referring to 50% of the maximum effect of 1035.0 µM and 1004.0 µM, respectively, values significantly higher than caulerpin. The antiviral screening of the analogs revealed that the N -substituted acids with methyl and ethyl groups inhibited Herpes simplex virus type 1-induced cytotoxicity by levels similar to the positive control acyclovir.

In 2019, the emergence of the seventh known coronavirus to cause severe illness in humans triggered a global effort towards the development of new drugs and vaccines for the SARS-CoV-2 virus. These efforts are still ongoing in 2024, including the present work where we conducted a ligand-based virtual screening of terpenes with potential anti-SARS-CoV-2 activity. We constructed a Quantitative Structure-Activity Relationship (QSAR) model from compounds with known activity against SARS-CoV-2 with a model accuracy of 0.71. We utilized this model to predict the activity of a series of 217 terpenes isolated from the Fabaceae family. Four compounds, predominantly triterpenoids from the lupane series, were subjected to an in vitro phenotypic screening in Vero CCL-81 cells to assess their inhibitory activity against SARS-CoV-2. The compounds which showed high rates of SARS-CoV-2 inhibition along with substantial cell viability underwent molecular docking at the SARS-CoV-2 main protease, papain-like protease, spike protein and RNA-dependent RNA polymerase. Overall, virtual screening through our QSAR model successfully identified compounds with the highest probability of activity, as validated using the in vitro study. This confirms the potential of the identified triterpenoids as promising candidates for anti-SARS-CoV-2 therapeutics.

This study evaluated the effects of acerola and guava fruit processing co-products fermented with probiotic Lactobacillus acidophilus LA-05 and Lacticaseibacillus paracasei L-10 on the abundance of different intestinal bacterial groups and microbial metabolic activity during 48 h of in vitro fecal fermentation. Digested fermented fruit co-products increased the relative abundance of beneficial bacterial groups while overall decreasing or maintaining the relative abundance of non-beneficial bacterial groups, suggesting selective stimulatory effects on beneficial bacterial intestinal populations. The fermented co-products stimulated microbial metabolic activity due to decreased pH, sugar consumption, short-chain fatty acid production, phenolic compound and metabolic profile alteration, and high antioxidant capacity during fecal fermentation. Acerola and guava co-products have high nutritional value and bioactive compounds whose fermentation with probiotics improves their potential functionalities. The results show that fermented fruit co-products could induce beneficial changes in the relative abundance of several bacterial groups as well as in the metabolic activity of the human intestinal microbiota. These results highlight their potential as novel and circular candidates for use as synbiotic ingredients.

The aim of this research was to evaluate the effect of cactus flour on the anxious-like behavior and cerebral lipid peroxidation in elderly rats (18 months of life). The rats were divided into four groups (n=10). control (CG) - received the AIN-93M ration. P5%. P10% and P15%. treated with the AIN-93M ration with the addition of 5, 10 and 15% of cactus flour respectively. In the elevated plus maze (EPM) groups P5%, P10% and P15% remained longer in the open arms. P15% remained longer in this region and less time in the closed arms. No significant differences were observed between the groups regarding the time the rats remained in the center of the apparatus. P5%. P10% and P15% performed a greater number of head dips. Regarding the open field animals P5%. P10% and P15% performed a greater number of rearing and stayed for a longer time in the center of the apparatus with P15% being the group that remained for the longest time when compared to the other groups. There was no difference in locomotion and grooming. As for the light-dark box. P15% spent more time in the light part. less time in the dark part and performed a smaller number of transitions. P5%. P10% and P15% had the lowest concentrations of brain lipid peroxidation. Our data demonstrated that consumption of cactus flour by rats promoted anxiolytic effects and minimized brain lipid peroxidation in aging. Given the above, it can be deduced that cactus pear can contribute to the prevention and/or treatment of anxiety in the aging phase.Due to its concentrations of mono and polyunsaturated fatty acids, soluble fibers and antioxidant contents such as vitamin E and selenium., (Copyright © 2023 Elsevier Inc. All rights reserved.)

Pink pepper ( Schinus terebinthifolius Raddi) is a native species native from Central and South America that produces an essential oil (EOpp) with promising applications. This work aimed to investigate the chemical composition and cytotoxic activity of EOpp extracted from unripe (U-EOpp) and ripe (R-EOpp) pink pepper fruits. U-EOpp and R-EOpp were extracted using the hydrodistillation technique and analysed using NMR and GC-MS. U-EOpp and R-EOpp cytotoxic activity was assessed using HL-60 (acute promyelocytic leukemia) and SK-MEL-28 (malignant melanoma) cell lines by MTT assay. Results showed that α -pinene (29.16%), dl -Limonene (20.65%), and ρ -cymene (15.86%) were U-EOpp major components. In addition, l -phellandrene (38.91%), Sylvestrene (23.02%), and α -pinene (21.62%) were R-EOpp major components. U-EOpp showed cytotoxic activity at 37.5 and 18.7 µg/mL for SK-MEL-28 and HL-60, respectively. R-EOpp showed cytotoxic activity for HL-60 at 100 µg/mL. Therefore, EOpp may represent a remarkable source of active natural compounds used in traditional Brazilian medicine.

In this study, we evaluated the physical, nutritional, and bioactive properties of mandacaru cladode flour ( Cereus jamacaru DC.). The granulometric profile revealed particles with non-uniform geometry, flakiness, a rectangular tendency, and a non-homogeneous surface, with particle sizes ranging from 20 to 60 µm. The flour presented low water activity (0.423), a moisture content of 8.24 g/100 g, high ash (2.82 g/100 g), protein (5.18 g/100 g), and total carbohydrate contents (74.48 g/100 g), and low lipid contents (1.88 g/100 g). Mandacaru flour is an excellent source of insoluble dietary fiber (48.08 g/100 g), calcium (76.33%), magnesium (15.21%), and potassium (5.94%). Notably, 1 H NMR analysis revealed the presence of N-methyltyramine. Using HPLC chromatography, glucose was identified as the predominant sugar (1.33 g/100 g), followed by four organic acids, especially malic acid (9.41 g/100 g) and citric acid (3.96 g/100 g). Eighteen phenolic compounds were detected, with relevant amounts of kaempferol (99.40 mg/100 g), myricetin (72.30 mg/100 g), and resveratrol (17.84 mg/100 g). The total phenolic compounds and flavonoids were 1285.47 mg GAE/100 g and 15.19 mg CE/100 g, respectively. The mean in vitro antioxidant activity values were higher using the FRAP method (249.45 µmol Trolox TEAC/100 g) compared to the ABTS •+ method (0.39 µmol Trolox TEAC/g). Finally, the ascorbic acid had a content of 35.22 mg/100 g. The results demonstrate the value of mandacaru as a little-explored species and an excellent matrix for the development of flours presenting good nutritional value and bioactive constituents with excellent antioxidant potential.

This study evaluated the effect of Mucuna pruriens (MP) administration on neuroinflammation and behavioral and murinometric parameters in obese rats. Proximate composition, oligosaccharide and phenolic compound profile of MP were determined. Wistar adult male rats were randomized into healthy (HG) and obese group (OG). The HG consumed a control chow diet while OG consumed a cafeteria diet for eight weeks. Then, they were subdivided into: Healthy (HG); Healthy with MP administration (HGMP); Obese (OG); Obese with MP administration (OGMP), with the consumption of the respective diets remaining for another eight weeks, in addition to gavage with MP extract to supplemented groups (750 mg/kg weight). MP presented a composition rich in proteins and phenolic compounds, especially catechin, in addition to 1-kestose and levodopa. Supplementation reduced food intake, body weight, and thoracic and abdominal circumferences in obese rats. MP showed anxiolytic and antidepressant effects and reduced morphological damage and expression of interleukin 6 in the hippocampus of obese rats. MP treatment showed satietogenic, slimming, anxiolytic and antidepressant effects, besides to minimizing hippocampal neuroinflammation in obese rats. Our results demonstrated the potential anti-obesity of MP which are probably related to the high content of bioactive compounds present in this plant extract.

Limonoids, quinolone alkaloids and chromones have been reported as constituents of Dictyoloma vandellianum Adr. Juss. (Rutaceae). Although those compounds are known for their biological activities, only the anti-inflammatory activity of chromones isolated from the underground parts has been evaluated. There are no studies of the pharmacological properties of the aerial parts of D. vandellianum. The present study was carried out to determine the phytochemical profile and antinociceptive activity of the methanol extract, fractions and isolated compounds of leaves of D. vandellianum. The phytochemical profile was performed by HLPC-DAD-ESIMSn and pure substances obtained were characterized by MS and NMR spectroscopy. The antinociceptive activity was assessed using the formalin assay in mice, and the motor function in the rotarod test. ME and all the fractions obtained from ME produced antinociceptive effects. Among them, the ethyl ether fraction was the most active. Data from HPLC-DAD-ESIMSn showed that the ethyl ether fraction presented 42 compounds. The major compounds isolated from this fraction-gallic acid, methyl gallate and 1,2,6-tri-O-galloyl-β-d-glucopyranose-were tested and produced antinociceptive effects. Gallic acid, methyl gallate and 1,2,6-tri-O-galloyl-β-d-glucopyranose at antinociceptive doses did not affect the motor performance in mice in the rotarod test. This work is the first report of the occurrence of gallotanins in D. vandellianum. In addition, the pharmacological study showed that D. vandellianum leaves present antinociceptive activity, probably induced by gallic acid, methyl gallate and 1,2,6-tri-O-galloyl-β-d-glucopyranose., Competing Interests: The authors have declared that no competing interests exist.