Bixa orellana ethyl acetate fraction and its isolated compound ellagic acid attenuate the progression of MIA-induced osteoarthritis in rat knees.

Osteoarthritis (OA) is a pathology that is characterized by progressive erosion of articular cartilage. In this context, medicinal plants have become relevant tools regarding their potential role in the prevention and treatment of OA, being safe and effective. The aim of this work was investigate the therapeutic efficacy of the ethyl acetate fraction of Bixa orellana leaves (BoEA) and ellagic acid (ElAc) for the therapeutic treatment of OA induced by monosodium iodoacetate (MIA) in rats. The plant material was extracted via maceration with 70 % hydroalcoholic solvent (BoHE). The ethyl acetate (BoEA) fraction was by solvents in increasing order of polarity. The ElAc was identified and isolated in BoEA using high performance liquid chromatography (HPLC-DAD) and analytical curve. The OA was induced using MIA in the right knee at the knee joint. Doses of BoEA and ElAc were administered daily (every 24 h, orally) at concentrations of 50, 100 and 50 mg/kg, respectively, for 28 days after induced OA. We evaluated the animals through clinical and radiological examinations every 7 days and, on the 29th day, the animals were euthanized, the joints being removed for histopathological analysis and the serum for cytokine analysis. BoEA and ElAc compounds reduced inflammation and nociception in OA and were as effective as indomethacin in clinical parameters of joint discomfort and allodynia in rats, in addition to showing improvements in radiological and histopathological images, acting on the progress of cartilage deterioration, proving properties related to anti-inflammatory and analgesic processes, being important allies for new therapeutic interventions for the treatment of OA.

Evaluation of molluscicidal activity on Biomphalaria glabrata (Say, 1818) and phytochemical characterization of hydroalcoholic extract of leaves of Ricinus communis L. (EUPHORBIACEAE).

Schistosomiasis is a parasitic infection of great prevalence worldwide, affecting 250 million people in 78 countries. Faced with this problem, studies that seek to analyze molluscicidal activity from plant extracts have stood out. The present work aimed to obtain the phytochemical characterization and investigate the molluscicidal activity in the hydroalcoholic extract of Ricinus communis leaves on Biomphalaria glabrata. The hydroalcoholic extract was prepared by macerated with solvent ethanol P.A 96%, followed by filtration and concentration in rotary evaporator. Next, five groups of snails with 10 animals each, one being the negative control group, were submitted to treatments with four concentrations of 25, 50, 75 and 100 mg/L of hydroalcoholic extract of R. communis. The parameters mortality, physiological and behavioral aspects of mollusks were analyzed during 96h. The chemical characterization of the extract was performed by high-performance liquid chromatography coupled to mass spectrometry (LC-MS). Chemical characterization revealed the presence of tannins, flavonoids and ricinin alkaloid, but under the conditions analyzed, the presence of saponins was not observed. There was no significant molluscicidal activity of the extract. However, a greater influence was observed in the diet, in addition to the motility and physiological state of the snails (alteration of cephalopodal mass and oviposition). The toxicity test was performed with Artemia salina and no toxicity was observed for this microcrustacean. It is expected that the results obtained contribute to the fight against the expansion of schistosomiasis and that they make room for other studies that investigate the molluscicidal action of plant extracts.

Chemical profiling of Dizygostemon riparius (Plantaginaceae) plant extracts and its application against larvae of Aedes aegypti L. (diptera: culicidae).

Dengue fever is a reemerging disease of global concern among health authorities due to its high rate of proliferation. In 2019, Brazil registered its second-highest dengue mortality rate since 1998, with approximately 754 deaths and 1.5 million probable cases. Brazilian Ministry of Health prevention and control strategies for Aedes include insecticides, eradication of breeding sites, and awareness campaigns. However, as new mosquito variants resistant to conventional insecticides emerge, there is an increasing demand for effective environment-friendly plant extracts and natural substances against adult mosquitos and/or larvae of Aedes aegypti L. with no negative impacts on human health. This study aimed to investigate the larvicidal activity of Dizygostemon riparius extracts and analyze its chemical profile for the first time. Dizygostemon is a Plantaginaceae bytipic genus and D. riparius is an aromatic plant recently identified in Maranhão, Brazil. The essential oil from its lilac morphotype already exhibited larvicidal potential against Aedes albopictus, but the still limited data on this new plant species require further chemical and biological studies on other species, such as Aedes aegypti. Ethyl acetate and methanol crude leaf extracts yielded, respectively, 17.60 and 25.96%. High-performance liquid chromatography (HPLC) with UV detection coupled with electrospray ionization mass spectrometry (HPLC-UV-ESI-IT/MS) analyses confirmed the presence of polymethoxyflavones and coumarins, such as isorhamnetin 3-galactoside-7-rhamnoside, 5,7-dihydroxy-3-(3-hydroxy-4,5-dimethoxyphenyl)-6-methoxy-4-benzopyrone and 3',5-dihydroxy-4',6,7-trimethoxyflavone. Ethyl acetate extract presented the best performance in larvicide bioassays (LC50 = 542.2 ± 11.5 µg.mL-1). Our results highlight the chemical and biological potential of this new species found in the cerrado of eastern Maranhão and open perspectives for future studies focusing on isolating and identifying other active secondary metabolites of Dizygostemon riparius.

Acaricide activity of extract and an isolated compound of Lithraea brasiliensis on Rhipicephalus microplus and selectivity actions against a non-target organism.

Rhipicephalus microplus, known as the cattle tick, is a cause of great economic losses for dairy cattle farming because of its high frequency of occurrence and the difficulty in controlling it. This research characterized the chemical profile and evaluated the in vitro toxicity of crude Lithraea brasiliensis extract and its isolated compound against acaricide-resistant and acaricide-susceptible R. microplus strains. Acaricidal activity was evaluated using a larval immersion test and the selectivity against non-target organisms was assessed on Artemia salina assay. The chemical investigation by high-performance liquid chromatography coupled with mass spectrometry (i.e., HPLC-MS) analysis showed the presence of hydrolysable tannins as well as urushiol derivatives. Column chromatography (CC) was carried out on the extract to obtain fractions and an isolated compound. The extract exhibited significant activity against acaricide-resistant (LC50 0.64 mg/mL) and acaricide-susceptible (LC50 0.76 mg/mL) strains of R. microplus larvae. The isolated compound from the extract (urushiol II), exhibited LC50 of 1.11 mg/mL for acaricide-resistant larvae. For acute toxicity in A. salina, the extract showed LC50>100 µg/mL. Thus, our findings represent the first effort to demonstrate the potential of L. brasiliensis extract and urushiol II as potential natural acaricides to replace or to be integrated into the conventional control of R. microplus larvae.

Arrabidaea chica Verlot fractions reduce MIA-induced osteoarthritis progression in rat knees.

This study aims to investigate the activity of n-hexane, ethyl acetate and butanol fractions obtained from Arrabidaea chica Verlot against MIA-induced osteoarthritis (OA). The antinociceptive potentials of each fraction were evaluated through a cyclooxygenase (COX) 1 and 2 inhibition test and an in vivo OA-model. In addition, toxicity assessments in the liver, spleen and kidney, as well as radiographic and histopathological knee analyses, were performed. The chemical composition of the n-hexane fraction was elucidated, and a molecular docking protocol was carried out to identify which compounds are associated with the detected bioactivity. The n-hexane A. chica fraction preferentially inhibits COX-2, with 90% inhibition observed at 10 µg/mL. The fractions also produced significant improvements in OA incapacity, motor activity and hyperalgesia parameters and in radiological knee conditions. However, concerning the histopathological evaluations, these improvements were only significant in the hexane and ethyl acetate fraction treatments, which resulted in better average scores, suggesting that these fractions slow OA-promoted joint injury progression. Histopathological organ analyses indicate that the fractions are not toxic to animals. Twenty compounds were identified in the n-hexane fraction, comprising fatty acids, terpenes and phytosterols. In silico analyses indicate the presence of favourable interactions between some of the identified compounds and the COX-2 enzyme, mainly concerning alpha-tocopherol (Vitamin E), squalene and beta-sitosterol. The findings indicate that A. chica fractions display analgesic, anti-inflammatory properties, are non-toxic and are able to slow OA progression, and may, therefore, be prioritized as natural products in OA human clinical trials.

Protective effect of flavonoids from Passiflora edulis Sims on diabetic complications in rats.

OBJECTIVES: This study was carried out to evaluate the effects of flavonoids present in leaves of Passiflora edulis fruit on complications induced by diabetes in rats. METHODS: The extract of P. edulis leaf was obtained by 70% ethanol maceration. From the dry extract, the fractions were obtained by consecutive liquid-liquid partition with hexane, ethyl acetate and n-butanol. The content of isoorientin of ethyl acetate and n-butanol fractions was determined by ultra-performance liquid chromatography coupled with electrospray and triple quadrupole ionization (TQD) analysis in tandem mass spectrometry (UPLC-ESI-Tq-MS). Only Fr-BuOH was used to treat diabetic or not Wistar rats. Biochemical parameters, platelet aggregation and production of reactive species were evaluated. KEY FINDINGS: The UPLC-ESI-Tq-MS analysis revealed the presence of several flavonoids, among which we identified five possible flavonoids c-heterosides (luteolin-7-O-pyranosyl-3-O-glucoside, apigenin-6-8-di-C-glycoside, apigenin-6-C-arabinoside-8-C-glycoside, isoorientin, isovitexin). The diabetic rats (treated intraperitoneally with alloxan, 150 mg/kg) treated with Fr-BuOH (20 mg/kg/day for 90 days) presented improvement in blood glucose, serum levels of fructosamine, lipid profile and urea. Furthermore, the Fr-BuOH reduced both platelet aggregation and the production of oxidant species in diabetic animals. CONCLUSIONS: These results suggested that flavonoid C-glycosides present in the Fr-BuOH may be beneficial for the diabetic state, preventing complications induced by diabetes.

Exposure of Rhipicephalus sanguineus sensu lato Latreille, 1806 (Acari: Ixodidae) to hexane extract of Acmella oleracea (Jambu): semi-engorged and engorged ticks.

The present study analyzed the efficacy of hexane extract of Acmella oleracea against Rhipicephalus sanguineus sensu lato. After exposure of R. sanguineus s. l. female ticks to 14 different concentrations of the hexane extract of A. oleracea, the LC50 was established as 18.135 mg/mL (limits: 16.251-22.675). The effects of the extract were more significant in the ovary of the semi-engorged females, that presented damages in most oocytes. Since such changes would not be repaired, the oocytes could not advance to further stages of development (I-V), thereby causing the inhibition of ovary development, interruption of vitellogenesis, oocyte death and, consequently, infertility. The semi-engorged females also presented extensive damages in the midgut cells, which would prevent (totally or partially) these cells from functioning properly (blood intake and release of nutrients), impairing the ectoparasite nutrition and the viability of the individual. Thus, the hexane extract of A. oleracea can be considered as a promising alternative to chemical control of pests of medical and veterinary importance, due to its efficient acaricidal activity and lesser environmental impact, when used against female ticks in the middle feeding stage.

Antimicrobial activity and inhibition of the NorA efflux pump of Staphylococcus aureus by extract and isolated compounds from Arrabidaea brachypoda.

Arrabidaea brachypoda is a native shrub of the Brazilian Cerrado widely used in the folk medicine for treatment of renal diseases and articular pains. This study aimed to, first, evaluate the antimicrobial activity of both extracts and isolated molecules Brachydins BR-A and BR-B obtained from the flowers of A. brachypoda against Staphylococcus aureus, Escherchia coli and Candida albicans species. A second objective was to investigate if these natural products were able to potentiate the Norfloxacin activity against the strain Staphylococcus aureus SA1199-B that overexpress the norA gene encoding the NorA efflux pump. Extracts and isolated compounds were analyzed by HPLC-PDA and LC-ESI-MS respectively. Minimal inhibitory concentrations of Norfloxacin or Ethidium Bromide (EtBr) were determined in the presence or absence of ethanolic extract, dichloromethane fraction, as well as BR-A or BR-B by microdilution method. Only BR-B showed activity against Candida albicans. Addition of ethanolic extract, dichloromethane fraction or BR-B to the growth media at sub-inhibitory concentrations enhanced the activity of both Norfloxacin and EtBr against S. aureus SA1199-B, indicating that these natural products and its isolated compound BR-B were able to modulate the fluoroquinolone-resistance possibly by inhibition of NorA. Moreover, BR-B inhibited the EtBr efflux in the SA1199-B strain confirming that it is a NorA inhibitor. Isolated BR-B was able to inhibit an important mechanism of multidrug-resistance very prevalent in S. aureus strains, thus its use in combination with Norfloxacin could be considered as an alternative for the treatment of infections caused by S. aureus strains overexpressing norA.

Passiflora edulis Leaf Extract: Evidence of Antidiabetic and Antiplatelet Effects in Rats.

Different Passiflora species have been appointed as a promising herbal medicine due to antioxidant properties; however, their effect on oxidative process induced by diabetes is still controversial. We aimed to evaluate effects of hydroethanolic extract 70% from P. edulis leaf on biochemical blood markers, collagen glycation, production of oxidant species and platelet aggregation in diabetic rats. The phytochemical analysis of the extract was performed by dereplication using LC coupled to the Photodiode Array Detector and Mass Spectrometer detector. Male Wistar rats were assigned to the control group and groups treated with alloxan (150 mg/kg) intraperitoneally, extract (200 mg/kg/d, for 90 d) and combination of alloxan and extract. The phytochemical analysis suggested the presence of flavonoids C-glycosides in the extract. The diabetic animals treated with the extract presented improvement in glycaemic control, reduced glycation collagen, levels of non-high density lipoprotein (non-HDL) cholesterol, total cholesterol and creatinine, production of oxidant species and aggregation in platelet in relation to diabetic animals non-treated. Our results showed that P. edulis leaf extract presents a health benefit to the diabetic state, preventing the appearance of its complications. Its effect can be associated with flavonoids, among which is the flavonoid C-glycoside isoorientin.

Galloyl-Hexahydroxydiphenoyl (HHDP)-Glucose Isolated From Punica granatum L. Leaves Protects Against Lipopolysaccharide (LPS)-Induced Acute Lung Injury in BALB/c Mice.

The hydroalcoholic extract and ethyl acetate fraction of Punica granatum leaves have been known to exhibit anti-inflammatory activities. In this study, we investigated the therapeutic effects of galloyl-hexahydroxydiphenoyl (HHDP)-glucose isolated from pomegranate leaves on lipopolysaccharide (LPS)-induced acute lung injury (ALI) in mice. Male BALB/c mice were treated with different doses of galloyl-HHDP-glucose (5, 50, and 100 mg/Kg) or dexamethasone at 5 mg/Kg (per os) 6 h after intra-tracheal instillation of LPS. Vehicle-treated mice were used as controls. Twenty-four hours after LPS challenge, bronchoalveolar lavage fluid (BALF), and lung samples were collected for analyses. They were evaluated by monitoring the expression of NF-κB, JNK, and cytokine genes and proteins, as well as cell migration and lung function. All doses of galloyl-HHDP-glucose inhibited LPS-induced JNK and NF-κB activation. Likewise, the galloyl-HHDP-glucose-treated animals presented reduced expression of the TNF-α, IL-6, and IL-1ß genes in the lungs and reduced TNF-α, IL-6, IL-1ß, and IL-8 protein levels when compared with the vehicle-treated LPS-challenged mice. In addition, the ALI mice treated with galloyl-HHDP-glucose also presented reduced lung inflammatory cell accumulation, especially that of neutrophils, in their BALF and lungs. In addition, galloyl-HHDP-glucose treatment markedly ameliorated the LPS-induced pulmonary mechanism complications and attenuated weight loss. Overall, we showed for the first time that galloyl-HHDP-glucose protects against ALI, and may be useful for treating ALI and other inflammatory disorders.

Anti-Ehrlichia properties of the essential oil of Ageratum conyzoides L. and its interaction with doxycycline.

Canine Monocytic Ehrlichiosis (CME) is an infectious disease caused by the rickettsia organism Ehrlichia canis which is transmitted mainly the ixodid brown dog tick Rhipicephalus sanguineus. The prevalence of E. canis infection has been increasing in recent years. The World Health Organization has been warned about antibiotics resistance and one of the way to prevent this situation is found new compound with this property. Doxycycline is the treatment of choice for this tick-borne disease. Adverse effects are noted in dogs that are sensitive to this drug. Antibiotic resistance may also occur. The present study aimed to evaluate the anti-Ehrlichia properties of the essential oil of the aerial parts of Ageratum conyzoides L. in infected DH82 cells, as well as its anti-Ehrlichia activity associated with doxycycline using the checkerboard assay. A. conyzoides is a native plant from northeast Brazil with many reports of ethnopharmacological applications. The essential oil of A. conyzoides was extracted from the aerial parts of the plant using the hydrodistillation method. E. canis-infected DH82 cells were cultured in DMEM (Dulbecco's Modified Eagle Medium), maintained at 37 °C and 5% CO2, and standardized at a 70% infection rate for the initiation of treatment protocols. The tests were first carried out with the aim of defining the IC50. The combined effect of doxycycline and A. conyzoides essential oil was then determined using the checkerboard dilution technique (checkerboard method) in which the IC50 was 200 µg/mL. The doxycycline reduction index from the combined effect was 4.90 times resulting in a synergistic effect. To the authors' knowledge, this is the first alternative treatment (alternative therapy) based on bioactive molecules that have antibacterial activity against E. canis.

Chemical composition and cytotoxic screening of Musa cavendish green peels extract: Antiproliferative activity by activation of different cellular death types.

Musa cavendish, commonly known as banana, is a fruit with nutritional and therapeutic properties. We investigated the chemical composition and in vitro cytotoxic effect of M. cavendish green peel extract (MHE) on cancer cells for the first time. The compounds characterization was performed by HPLC-UV/Vis and FIA-ESI-IT-MSn. We investigated in vitro cytotoxic effect of Musa cavendish green peels extract (MHE) in HepG2, A-375, MCF-7 and Caco-2 cancer cells. We evaluated the effect of MHE on proliferation of different cell lines through apoptosis, necrosis, mitochondrial membrane potential (MMP) and reactive oxygen species (ROS) content determination. We identified 12 compounds from different classes in the extract, including derivatives of phenolic acids, aglycone flavonoids, glycoside flavonoids and catecholamines. Our results indicate that MHE exerts, after 48 h treatment, an accentuated antiproliferative effect from the dose of 100 µg/mL in all cell lines tested. In HepG2 cells, these effects were related to the induction of cell death, both necrotic and apoptotic, and remarkable changes in cell morphology. Depolarization of MMP and high ROS content were also observed in the cells in a dose-dependent manner. Our results show that MHE may be used as a source of new drugs with anticancer activity.

Photoelectrochemical sensing of tannic acid based on the use of TiO2 sensitized with 5-methylphenazinium methosulfate and carboxy-functionalized CdTe quantum dots.

The article describes a method for determination of tannic acid in extracts of medicinal plants. Tannic acid (TA) is an antioxidant and has anticancer and antimicrobial properties. Titanium dioxide nanoparticles (TiO2) were co-sensitized with 5-methylphenazinium methosulfate (PMS) and carboxy-functionalized cadmium telluride quantum dots (CdTe QDs), and immobilized on a fluorine-doped tin oxide electrode. The surface morphology and electrochemical properties of the modified electrode were investigated by scanning electron microscopy and amperometry, respectively. A composite consisting of TiO2, PMS and CdTe QDs in a nafion film has a response to TA under LED light higher than that observed for each separate component. Under optimized experimental conditions and at an applied voltage of +0.4 V vs Ag/AgCl, the photoelectrochemical sensor has a linear response in the 0.2 to 200 µmol L-1 TA concentration range and a detection limit of 60 nmol L-1. The sensor was successfully applied to the determination of TA in spiked extracts from three medicinal plants, with recovery values between 98.3 and 103.9 %. Graphical abstract Schematic diagram for photoelectrochemical detection of tannic acid based on a fluorine doped tin oxide electrode modified with titanium oxide, 5-methylphenazinium methosulfate and carboxy-functionalized cadmium telluride quantum dots.

Modulatory Effect of Polyphenolic Compounds from the Mangrove Tree Rhizophora mangle L. on Non-Alcoholic Fatty Liver Disease and Insulin Resistance in High-Fat Diet Obese Mice.

No scientific report proves the action of the phytochemicals from the mangrove tree Rhizophora mangle in the treatment of diabetes. The aim of this work is to evaluate the effects of the acetonic extract of R. mangle barks (AERM) on type 2 diabetes. The main chemical constituents of the extract were analyzed by high-performance liquid chromatography (HPLC) and flow injection analysis electrospray-iontrap mass spectrometry (FIA-ESI-IT-MS/MS). High-fat diet (HFD)-fed mice were used as model of type 2 diabetes associated with obesity. After 4 weeks of AERM 5 or 50 mg/kg/day orally, glucose homeostasis was evaluated by insulin tolerance test (kiTT). Hepatic steatosis, triglycerides and gene expression were also evaluated. AERM consists of catechin, quercetin and chlorogenic acids derivatives. These metabolites have nutritional importance, obese mice treated with AERM (50 mg/kg) presented improvements in insulin resistance resulting in hepatic steatosis reductions associated with a strong inhibition of hepatic mRNA levels of CD36. The beneficial effects of AERM in an obesity model could be associated with its inhibitory α-amylase activity detected in vitro. Rhizophora mangle partially reverses insulin resistance and hepatic steatosis associated with obesity, supporting previous claims in traditional knowledge.

Ilex paraguariensis supplementation may be an effective nutritional approach to modulate oxidative stress during perimenopause.

Perimenopause is a period in a woman's life that precedes menopause and is characterized by hormonal changes that result in increased oxidative stress. Since oxidative stress is associated with age-related diseases and perimenopausal symptoms including somato-vegetative manifestations, nutritional antioxidant supplementation may be an effective approach to minimizing this stress. Mate tea (MT) (Ilex paraguariensis), a typical and inexpensive beverage consumed in the Brazilian south-east, Argentina and Uruguay, increases antioxidant defense. We hypothesized that MT could minimize oxidative stress during perimenopause by modulating enzymatic antioxidant defense. To test this, we analyzed the lipid oxidative damage and antioxidant defense in erythrocytes and liver of rats, after MT treatment. Female Wistar rats (aged 16months) in proven perimenopause period received 20mg/kgBW/day of mate tea, by gavage (PM+MT group) or water (PM group). Female rats aged 4months (AD group) received water. Erythrocytes and liver were used to determine lipid oxidative damage, determined by malondialdehyde (MDA); superoxide dismutase (SOD), glutathione peroxidase (GPx) and catalase (CAT) activities. Total plasma antioxidant capacity was examined by ferric reducing antioxidant power assay (FRAP) and estrogen by radioimmunoassay. MT increased FRAP and did not change estrogen levels. Increased SOD and GPx, and reduced MDA were observed in both tissues studied. Increased CAT activity was observed only in the liver. We confirmed the hypothesis that MT was capable of minimizing oxidative stress in this period of life by modulating antioxidant defense.

Phenolic Isomers from Plantago catharinea Leaves: Isolation, ldentification, Quantification and in vitro Antioxidant Activity.

In this study we isolated two polyphenolic acids of m/z 639, called catharinol A and catharinol B, from Plantago catharinea L. (Plantaginaceae) leaves. Although presenting very similar structures, catharinol A showed higher antioxidant activity when compared with gallic acid and quercetin standards. These compounds are position isomers and present in their chemical structure the rare sugar D-allose. Molecules with similar constitution are known to have imnportant biological activities such as antitumor and immunosuppressive. These compounds were isolated by high-performance liquid chromatography HPLC) and characterized by mass spectrometry (FIA-ESI-IT-MS/MS) and nuclear magnetic resonance (NMR). This work is the first study on the chemical composition ofP. catharinea and encourages the production of Plantago species as a good source of bioactive molecules.

Gastroprotective effects of hydroethanolic root extract of Arrabidaea brachypoda: Evidences of cytoprotection and isolation of unusual glycosylated polyphenols.

The hydroethanolic root extract of Arrabidaea brachypoda, from Bignoniaceae family, a Brazilian medicinal plant, demonstrated significant in vivo gastroprotective effects using different in vivo assays. The activity was evaluated in several models of experimental gastric ulcer in rats (absolute ethanol, glutathione depletion, nitric oxide depletion, non-steroidal anti-inflammatory drugs, pylorus ligation and acetic acid). Using 300 mg/kg (p.o.) the extract significantly reduced gastric injury in all models. In depth phytochemical investigation of this extract led to the isolation of two previously undescribed phenylethanoid glycosides derivatives and seven unusual glycosylated dimeric flavonoids. The structures were elucidated using UV, NMR and HRMS analysis. Absolute configuration of the dimeric flavonoids was performed by electronic circular dichroism (ECD) spectroscopy.

In Vitro Assessment of Plants Growing in Cuba Belonging to Solanaceae Family Against Leishmania amazonensis.

In this study, an in vitro antileishmanial assessment of plant extracts from 12 genera and 46 species growing in Cuba belonging to Solanaceae family was performed. A total of 226 extracts were screened against promastigotes of Leishmania amazonensis, and cytotoxicity of active extracts [median inhibitory concentration (IC50 ) promastigotes <100 µg/mL] was determined on peritoneal macrophage from BALB/c mice. Extracts that showed selective index >5 were then assayed against intracellular amastigote. Metabolomics analysis of promissory extracts was performed using chemical profile obtained by ultra performance liquid chromatography. Only 11 extracts (4.9%) from nine plants were selected as potentially actives: Brunfelsia cestroides A. Rich, Capsicum annuum L., Capsicum chinense Jacq., Cestrum nocturnum L., Nicotiana plumbaginifolia Viv., Solanum havanense Jacq., Solanum myriacanthum Dunal, Solanum nudum Dunal and Solanum seaforthianum And., with IC50 < 50 µg/mL and selectivity index >5. Metabolomics analysis demonstrated significant differences in the chemical profiles with an average of 42.8 (range 31-88) compounds from m/z 104 to 1477, which demonstrated the complex mixture of compounds. In addition, no common markers among active extracts were identified. The results demonstrate the importance of the Solanaceae family to search new antileishmanial agents, particularly in unexplored species of this family. Copyright © 2016 John Wiley & Sons, Ltd.

Mutagenicity and chemopreventive activities of Astronium species assessed by Ames test.

In the neotropical savannah, Astronium species are used in popular medicine to treat allergies, inflammation, diarrhea and ulcers. Given that natural products are promising starting points for the discovery of novel potentially therapeutic agents, the aim of the present study was to investigate the mutagenic and antimutagenic activities of hydroalcoholic extracts of Astronium spp. The mutagenicity was determined by the Ames test on Salmonella typhimurium strains TA98, TA97a, TA100 and TA102. The antimutagenicity was tested against the direct-acting and indirect-acting mutagens. The results showed that none of the extracts induce any increase in the number of revertants, demonstrating the absence of mutagenic activity. On the other hand, the results on the antimutagenic potential showed a moderate inhibitory effect against NPD and a strong protective effect against B[a]P and AFB1. This study highlights the importance of screening species of Astronium for new medicinal compounds. The promising results obtained open up new avenues for further study and provide a better understanding the mechanisms by which these species act in protecting DNA from damage. However, further pharmacological and toxicological investigations of crude extracts of Astronium spp., as well as of its secondary metabolites, are necessary to determine the mechanism(s) of action to guarantee their safer and more effective application to human health.

New steroidal saponin and antiulcer activity from Solanum paniculatum L.

Solanum paniculatum L. (Solanaceae) is a plant species widespread throughout tropical America, especially in the Brazilian Savanna region. It is used in Brazil for culinary purposes and in folk medicine to treat liver and gastric dysfunctions, as well as hangovers. Fractionation of the ethanolic extracts (70%) from aerial parts (leaves and twigs) of S. paniculatum led to the isolation of the two new saponins (22R, 23S, 25R)-3ß, 6α, 23-trihydroxy-5α-spirostane 6-O-ß-D-xylopyranosyl-(1"" → 3"')-O-[ß-D-quinovopyranosyl(1″' → 2')]-O-[α-L-rhamnopyranosyl(1" → 3')]-O-ß-D-quinovopyranoside (1) and diosgenin 3-O-ß-D-glucopyranosyl(1" → 6')-O-ß-D-glucopyranoside (2) together with four know compounds: caffeic acid (3), diosgenin ß-D-glucopyranoside (4), rutin (5), and quercetin 3-O-α-L-rhamnopyranosyl (1"' → 6 ″)-O-ß-D-galactopyranoside (6). The structures of these compounds were elucidated by extensive use of 1D and 2D NMR experiments along with HRESIMS analyses. Different doses (31.25-500 mg/kg) of ethanolic extract of leaves from S. paniculatum were evaluated against gastric ulcer induced by ethanol in rats. The lower dose of extract able to promote antiulcer effect was 125 mg/kg. The treatment with S. paniculatum by oral route was able to decrease gastric lesion area and also reduced levels of myeloperoxidase (MPO) in the gastric mucosa. Our results reveal for the first time, steroidal saponins from S. paniculatum and the antiulcer effect of this species at this lower dose.