Search

Ethnopharmacological Relevance: Solanum lycocarpum A. St. Hil. (Solanaceae) is a species from the Brazilian Cerrado, exhibiting several medicinal properties, being used by the population in the treatment of ulcers, bronchitis, asthma and hepatitis, which involve inflammatory processes., Aim of This Study: This study aimed to chemically characterize the dichloromethane fraction (DCM), as well as verify its antinociceptive, anti-inflammatory and antioxidant potential., Materials and Methods: The DCM fraction was obtained by partitioning the ethanol extract. The chemical constituents of the DCM fraction were characterized by LC-DAD-MS. The DPPH and FRAP assays were used to evaluate the antioxidant potential. The carrageenan-induced paw edema model was used to assess the anti-inflammatory effects, and the inflammatory infiltrate was evaluated by qualitative and quantitative histological analyses. The antinociceptive action of the DCM fraction was evaluated by acetic acid-induced abdominal writhing test, formalin-induced nociception and hot-plate test., Results: Steroidal alkaloids solasonine, solasodine and solamargine, as well as the alkaloid peiminine/imperialine and caffeoylquinic acids, were annotated in DCM fraction by LC-DAD-MS. The DCM fraction showed antioxidative action in the in vitro DPPH and FRAP tests, as well as an anti-inflammatory effect for the three evaluated doses of 30, 100 and 300 mg/kg in the fourth and sixth hours after the administration of carrageenan. The histological analyses evidenced considerably reduction in leukocyte migration and the number of polymorphonuclear leukocytes. The study also demonstrated antinociceptive activity for the DCM fraction, which reduced abdominal writhing at three concentrations evaluated, as well as a decrease in paw licking in the formalin-induced nociception test both in the neurogenic phase and the inflammatory phase, with greater effectiveness compared to the anti-inflammatory indomethacin. The DCM fraction also increased the latency time of the animals in the hot plate test 60 min after treatment, although it did not seem to involve the opioidergic system., Conclusion: This work evidenced that the dichloromethane fraction of S. lycocarpum fruit possesses antinociceptive and anti-inflammatory potential, which supports its use in folk medicine for management inflammatory conditions., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2023 Elsevier B.V. All rights reserved.)

Brazilian biodiversity includes species of the genus Solanum that have several biological activities, in addition to their relevance to agriculture, economics and popular medicine. The ripe fruits of Solanum lycocapum are an important nutritional food source, since they have levels of vitamin C, total soluble sugars, sucrose, phosphorus, and iron comparable or exceed the levels present in fruits such as pineapples, bananas, oranges, and mangoes. The pulp of the fruit is consumed by the population, and it is also used to produce jellies; to make marmalade, replacing the quince, and it can also be mixed with peaches in the preparation of peach. The objective of this study was to evaluate the anti-inflammatory and antioxidant activities of fractions obtained from the ripe fruits and to identify the constituents with these biological properties. The ripe fruits were collected, dried, crushed, and subjected to extraction by exhaustive percolation, obtaining an ethanol extract that was partitioned with solvents of increasing polarities, obtaining hexane (HEX), ethyl acetate (AC), and hydroethanol (HE) fractions. The AC fraction showed higher antioxidant potential compared to BHT (2,6-di-tert-butyl-4-methylphenol) and similar activity to AA (ascorbic acid) by DPPH (1,1-diphenyl-2-picrylhydrazyl) radical assay, while HEX and HE fractions exhibited of IC 50 values similar to BHT. The AC fraction also presented similar activity to BHT by FRAP (Ferric Reducing Antioxidant Power) test. Intraperitoneal treatment with HEX (100 and 300 mg/kg) and HE (100 mg/kg) fractions caused significant inhibition of paw edema induced by carrageenan, 4 and 6 h after the inflammatory stimuli. When analyzed by GC-MS, fatty acids, phytosterols, and triterpenoid were identified in the HEX fraction, whilst 31 compounds were annotated in the AC and HE fractions analyzed by LC-DAD-MS, being phenylpropanoid derivatives, chlorogenic acids, and steroidal glycoalkaloids. The ripe fruits of S. lycocarpum have antioxidant and anti-inflammatory activities, and the detected chemical compounds, especially caffeoylquinic acid derivatives, spermidine, stigmasterol, and β-sitosterol, may be correlated with these activities. The ripe fruits of this species can be a food alternative rich in bioactive compounds and with benefits for human health., (Copyright © 2022 Elsevier Ltd. All rights reserved.)

In this study, a nanocomposite produced with a blend of polyvinyl alcohol and partially hydrolyzed starch from Solanum lycocarpum was used as a matrix to entrap natural bioactive peptides from Phaseolus vulgaris. The nanocomposites were characterized by dynamic light scattering, scanning electron microscopy, and field emission gun scanning electron microscopy. The nanocomposites were then orally administered to Wistar rats, and their absorption was determined using morphometric, histopathological, cytochemistry, transmission electron microscopy, and biochemical analysis. Results showed that despite some aggregates being formed, the nanocomposites efficiently entrapped the natural peptides, with a loading capacity of 303.62 mg (45.7%) and an entrapment efficiency of 85.3% (267.02 µmol). Histochemical and morphological analysis revealed the absence of tissue injury and cellular changes, indicating the absence of deleterious and toxic effects. Transmission electron microscopy showed the internalization of the nanocomposites in the enterocytes, and biochemical analysis indicated that natural peptides were absorbed reaching the bloodstream., (Copyright © 2021 Elsevier B.V. All rights reserved.)

Chronic high-glucose levels induce the generation of reactive oxygen species leading to mitochondrial dysfunction, which is one of the pathological triggers in the development of diabetes. This study investigated the alkaloid composition of two fruits of the genus Solanum, fruta-do-lobo (Solanum lycocarpum) and juá-açu (Solanum oocarpum), and their capacity to protect against oxidative damage and defective insulin secretion induced by chronic high-glucose levels. LC-MS and molecular network of fruit crude extracts reveals that juá-açu and fruta-do-lobo contain kukoamines and glycoalkaloids, respectively. Two purification processes were used to enrich those alkaloids. Fruta-do-lobo extract rich in glycoalkaloids showed a strong cytotoxicity effect, however the juá-açu enriched extract was able to protect mitochondrial functionality against glucotoxicity and stimulate insulin secretion even under conditions of hyperglycemia. These results are promising and suggest that juá-açu is a potential source of bioactive compounds for adjuvant/co-adjuvant therapy for diabetes., (Copyright © 2021 Elsevier Ltd. All rights reserved.)

Glycoalkaloids have been widely demonstrated as potential anticancer agents. However, the chemosensitizing effect of these compounds with traditional chemotherapeutic agents has not been explored yet. In a quest for novel effective therapies to treat bladder cancer (BC), we evaluated the chemosensitizing potential of glycoalkaloidic extract (GE) with cisplatin (cDDP) in RT4 and PDX cells using 2D and 3D cell culture models. Additionally, we also investigated the underlying molecular mechanism behind this effect in RT4 cells. Herein, we observed that PDX cells were highly resistant to cisplatin when compared to RT4 cells. IC 50 values showed at least 2.16-folds and 1.4-folds higher in 3D cultures when compared to 2D monolayers in RT4 cells and PDX cells, respectively. GE + cDDP inhibited colony formation (40%) and migration (28.38%) and induced apoptosis (57%) in RT4 cells. Combination therapy induced apoptosis by down-regulating the expression of Bcl-2 (p < 0.001), Bcl-xL (p < 0.001) and survivin (p < 0.01), and activating the caspase cascade in RT4 cells. Moreover, decreased expression of MMP-2 and 9 (p < 0.01) were observed with combination therapy, implying its effect on cell invasion/migration. Furthermore, we used 3D bioprinting to grow RT4 spheroids using sodium alginate-gelatin as a bioink and evaluated the effect of GE + cDDP on this system. Cell viability assay showed the chemosensitizing effect of GE with cDDP on bio-printed spheroids. In summary, we showed the cytotoxicity effect of GE on BC cells and also demonstrated that GE could sensitize BC cells to chemotherapy., (Copyright © 2020 Elsevier B.V. All rights reserved.)

Fruta-do-lobo (Solanum lycocarpum St. Hill) is an underutilized native fruit commonly found in the Brazilian Cerrado, very known due to the presence of glycoalkaloids. In this work we evaluated the biochemical changes on carbohydrates, phenolic and alkaloids during ripening of fruta-do-lobo using chromatographic and spectrometric techniques. During ripening, we observed an increase in glucose, fructose and sucrose, while oligosaccharides levels varied. Chlorogenic acid isomers represented 80% of the identified phenolic compounds in unripe stage, but they reduced during ripening, resulting in predominance of p-coumaroylquinic acid (peel and pulp) and 1-O-sinapoyl-glucoside (seeds). Statistical analysis shows that the unripe fractions were richer in alkaloids compounds, which were the most important for antioxidant activity. Molecular network analysis summarizes the compound changes during ripening, especially regarding the alkaloid compounds, with a reduction of around 85% of solamargine abundance. These data show that fruta-do-lobo can presents different chemical compositions due their ripening stage providing support for future research aimed to the application of these compounds in glycemia control or uses of their extracts with higher content of alkaloids compounds., (Copyright © 2020 Elsevier Ltd. All rights reserved.)

Ethnopharmacological Relevance: Solanum lycocarpum St. Hil. (Solanaceae) is widely distributed in the Brazilian Cerrado and is used in folk medicine for treatment of inflammatory disorders, such as asthma and hepatitis, as weel as antirheumatic., Aim of the Study: The aims of this study were to evaluate the antioxidant, anti-inflammatory and antinociceptive activities of the ethanol extract (EE) obtained from the ripe fruits of S. lycocarpum and to identify its chemical constituents., Materials and Methods: The extract was obtained by percolation with ethanol. This extract was analyzed by liquid chromatography coupled to a diode array detector and mass spectrometer (LC-DAD-MS) for identify its chemical constituents. The antioxidant activity was determined by the reaction with 1,1-diphenyl-2-picrylhydrazyl radical (DPPH). In vivo anti-inflammatory potential was assessed using carrageenan-induced paw edema model, while qualitative and quantitative histological analyses evaluated of the inflammatory infiltrate at different times and treatments. The antinociceptive effect of the EE was evaluated by acetic acid-induced abdominal writhing test, formalin-induced nociception and hot-plate test., Results: The main compounds identified in EE were steroidal glycoalkaloids (such as robeneoside B or hydroxysolasonine isomers and solanandaine isomers), the aglycone alkaloids peiminine and solasodine, di- and tri-O-caffeoylquinic acid derivatives, O-coumaroyl caffeoylquinic acid derivatives, N1,N10-bis-(dihydrocaffeoyl)spermidine, di-O-hexoside, and hexonic acid. In addition, the EE showed significant antioxidant activity. Intraperitoneal (i.p.) treatment with EE (300 mg/kg) exhibited anti-inflammatory activity. Qualitative and quantitative histological analyses showed that EE significantly reduced the cell infiltrate in acute inflammation. The EE, in all doses evaluated, significantly reduced the abdominal contortions in mice. Besides, reduced licking time was found in both phases in the formalin test after treatment with EE (100 and 300 mg/kg). In addition, the opioid receptor antagonist naloxone reversed the antinociceptive activity of morphine in the both phases the test, but it did not reverse the antinociceptive activity of the EE. The EE (300 mg/kg) also caused an increase in the latency to response in the hot-plate test., Conclusion: The ripe fruits of S. lycocarpum exhibit antioxidant, anti-inflammatory, and antinociceptive activities, attributed mainly to the presence of alkaloids, such as solasodine and peiminine, as well as caffeoylquinic acids in their chemical composition. These results contribute to use of S. lycocarpum ripe fruits for the treatment of inflammatory and painful process., (Copyright © 2020 Elsevier B.V. All rights reserved.)

Solanum lycocarpum fruits contain two major glycoalkaloids (GAs), solamargine (SM) and solasonine (SS). These compounds are reported as cytotoxic. However, they have poor water solubility and low bioavailability. To overcome these disadvantages and getting an efficient formulation the current study aimed to develop, characterize, and test the effectiveness of a nanotechnology-based strategy using poly(D,L-lactide) (PLA) nanoparticles functionalized with folate as delivery system of glycoalkaloidic extract (AE) for bladder cancer therapy. The strategic of adding folic acid into nanoformulations can increase the selectivity of the compounds to the cancer cells reducing the side effects. Our results revealed the successful preparation of AE-loaded folate-targeted nanoparticles (NP-F-AE) with particle size around 177 nm, negative zeta potential, polydispersity index <0.20, and higher efficiency of encapsulation for both GAs present in the extract (>85 %). To investigate the cellular uptake, the fluorescent dye coumarin-6 was encapsulated into the nanoparticle (NP-F-C6). The cell studies showed high uptake of nanoparticles by breast (MDA-MB-231) and bladder (RT4) cancer cells, but not for normal keratinocytes cells (HaCaT) indicating the target uptake to cancer cells. The cytotoxicity of nanoparticles was evaluated on RT4 2D culture model showing 2.16-fold lower IC 50 than the free AE. Furthermore, the IC 50 increased on the RT4 spheroids compared to 2D model. The nanoparticles penetrated homogeneously into the urotheliumof porcine bladder. These results showed that folate-conjugated polymeric nanoparticles are potential carriers for targeted glycoalkaloidic extract delivery to bladder cancer cells., (Copyright © 2020 Elsevier B.V. All rights reserved.)

Objective: This study proposed to use the nanotechnology to deliver glycoalkaloidic extract (AE) to bladder cancer cells, evaluating their activity in 2D and 3D models and the biological mechanism of cell death., Methods: NPs were prepared by nanoprecipitation method using polylactic acid (PLA) and characterized considering their size, charge, particle concentration and stability. The cytotoxicity was evaluated in 2D and 3D model, and the apoptosis and cell cycle were investigated using flow cytometry., Key Findings: NPs loading AE (NP-AE) had diameter around 125 ± 6 nm (PdI <0.1) and negative charge. The encapsulation efficiency of SM and SS was higher than 85% for both compounds. The obtained formulation showed a significant in-vitro cytotoxic effect against RT4 cells in a dose-dependent manner with IC 50 two fold lower than the free AE. The cytotoxic effect of NP-AE was mediated by apoptosis and cell cycle arrested in the S phase. RT4 cells cultured under 3D conditions exhibited a higher resistance to the treatments (IC 50 ~ three fold higher than in 2D cell culture)., Conclusion: The NP-AE might be a promising nanocarrier to load and deliver glycoalkaloids against bladder cancer., (© 2019 Royal Pharmaceutical Society.)

Trade-offs between plant growth and defense are central to theoretical frameworks used to study the ecology and evolution of plant defense against herbivores. However, these frameworks, as well as the experiments designed to test them, rarely include belowground herbivores. We experimentally challenged seedlings of the tropical shrub Solanum lycocarpum (Solanaceae) with either aboveground foliar herbivores (Spodoptera caterpillars) or belowground root herbivores (the nematode Meloidogyne incognita) and measured the resulting changes in plant growth rates, biomass allocation, and the concentration of defensive terpenoids in roots and leaves. We found that plants that suffered aboveground herbivory responded with aboveground growth but belowground defense. Similarly, belowground herbivory resulted in root growth but elevated defenses of leaves. These results underscore the importance of belowground plant-herbivore interactions, and suggest that, in contrast to theoretical predictions, plants can simultaneously invest in both growth and defense. Finally, they emphasize the need for a "whole-plant" perspective in theoretical and empirical evaluations of plant-herbivore interactions., (© 2016 by the Ecological Society of America.)

Background: Solanum lycocarpum has great importance for food and medicinal traditional use. Recently, it was also evidenced that extracts of S. lycocarpum St. Hill (Solanaceae) and its glycoalkaloids, solamargine (Sg) and solasonine (Sn), are active against flagellated protozoa., Objective: The aim was to assess the effects of the extract of S. lycocarpum and its glycoalkaloids, Sn, and Sg, on Giardia lamblia trophozoites., Materials and Methods: A crude extract (96%ethanol) (EB) of fruits of S. lycocarpum was prepared and fractionated by partition with 40%ethanol and n-hexane: Ethyl acetate. Glycoalkaloids, Sn, and Sg were recognized in the ethanol fraction (EF) and further isolated by column chromatography. EB, EF, the isolated Sn and Sg and a mixture (1:1) of both glycoalkaloids were tested on cultures of G. lamblia trophozoites and macrophages., Results: EB, EF and glycoalkaloids of S. lycocarpum showed activity against Giardia (95.0 < Inhibitory concentration 50 [IC50] ≤120.3 μg/mL). The mixture of glycoalkaloids (1:1) was more active (IC50 = 13.23 μg/mL) than each one individually, suggesting a synergic effect. Moreover, the mixture is nontoxic to macrophage cells., Conclusion: Results are optimistic concerning the anti-Giardia potential of the mixture Sn + Sg. Further studies, in vitro and in vivo, will be required to consolidate the usefulness of the mixture of Sn + Sg in view of a new therapeutic strategy for giardiasis.

Ethanol extract (EE) and fractions obtained from the ripe fruits of Solanum lycocarpum were examined in order to determine their phenolic composition, antioxidant capacity, antibacterial activities and cytotoxic potential. High-performance liquid chromatography coupled with DAD analysis indicated that caffeic and chlorogenic acids were the main phenolic compounds present in the EE, dichloromethane (DCM) and ethyl acetate (Ac) fractions. The antioxidant activity assessed by the scavenging ability on 1,1-diphenyl-2-picrylhydrazyl radical was significantly more pronounced for DCM and Ac fractions than that of the commercial antioxidant 2,6-di-tert-butyl-4-methylphenol (BHT). EE and fractions exhibited selective antibacterial activity against Gram-positive bacteria, especially the hexane (Hex) and DCM fractions. EE and fractions exhibited low toxicity towards the LLC-MK2 cell line, especially the Hex, DCM and Ac fractions. This work provides the knowledge of phenolic composition in the extract and fractions from the ripe fruits of S. lycocarpum and their antioxidant, antibacterial and cytotoxic activities.

The glycoalkaloids solasonine (SN) and solamargine (SM) have been studied for their antiparasitic, antifungal, and anticancer properties, especially in vitro and in vivo against non-melanoma skin cancer. Thus, the alkaloidic extract of Solanum lycocarpum, which contains approximately 45% each of SN and SM, was used to define the best experimental conditions for in vitro and in vivo assays. The in vitro assays were performed with the Franz cell diffusion porcine skin model to evaluate the effects of different pHs and the presence of monoolein, ethoxydiglycol or ethanol penetration enhancers on the skin penetration and retention of SN and SM after 3, 6, 9 and 12h of exposure. The in vivo assay was performed on hairless mice with the formulation selected in the in vitro assays. The results showed that pH 6.5 was optimal for SM penetration. The formulation containing 5% alkaloidic extract, 5% propylene glycol, 5% monoolein and a hydroxyethyl cellulose gel base (Natrosol) (pH 6.5) was optimal for the delivery of SN and SM into the skin, and this formulation is potentially useful for the topical therapy of several skin disorders., (Copyright © 2014 Elsevier B.V. All rights reserved.)

In this study the pulp from Solanum lycocarpum fruits was used as raw material for extraction of starch, resulting in a yield of 51%. The starch granules were heterogeneous in size, presenting a conical appearance, very similar to a high-amylose cassava starch. The elemental analysis (CHNS) revealed 64.33% carbon, 7.16% hydrogen and 0.80% nitrogen. FT-IR spectroscopy showed characteristic peaks of polysaccharides and NMR analysis confirmed the presence of the α-anomer of d-glucose. The S. lycocarpum starch was characterized by high value of intrinsic viscosity (3515 mPa s) and estimated molecular weight around 645.69 kDa. Furthermore, this starch was classified as a B-type and high amylose content starch, presenting 34.66% of amylose and 38% crystallinity. Endothermic transition temperatures (To=61.25 °C, Tp=64.5 °C, Tc=67.5 °C), gelatinization temperature (ΔT=6.3 °C) ranges and enthalpy changes (ΔH=13.21 J g(-1)) were accessed by DCS analysis. These results make the S. lycocarpum fruit a very promising source of starch for biotechnological applications., (Copyright © 2013 Elsevier Ltd. All rights reserved.)