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Purpose: The development biosensing technologies capable of delivering fast and reliable analysis is a growing trend in drug quality control. Considering the emerging use of plant-based polyphenol oxidases (PPO) as biological component of electrochemical biosensors, this work reports the first Solanum lycocarpum PPO biosensor and its use in the pharmaceutical analysis of paracetamol in tablet formulations. Methods: The biosensor was optimized regarding fruit maturation (immature and mature-ripe), vegetal extract volume to be used in biosensor construction as well as optimal pH of electrochemical cell fluid. Results: Results evidenced that the extract which rendered the biosensor with best analytical performance was from immature fruits, and the biosensor produced using 100 µL of crude plant extract promoted better faradaic signal gathering. Moreover, when neutral pH media was used in the electrochemical cell, the biosensor showcased best faradaic signal output from the used redox probe (catechol), suggesting thence that the method presents high sensibility for phenolic compounds detection. Furthermore, the biosensor was able to quantify paracetamol in a linear range from 50 to 300 μM, showcasing LoD and LoQ of 3 μM and 10 μM, respectively. Conclusion: after careful evaluation, this biosensor might be a low-cost alternative for conventional pharmaceutical quality control methods.

In this study the starch from Solanum lycocarpum fruit was used for bioethanol production. S. lycocarpum starch was hydrolyzed in a serial reactor containing α-amylase and glucoamylase immobilized onto glutaraldehyde-derivative polyaniline, producing 91.6% of glucose for a 10% starch suspension and 86.3% of glucose for a 20% starch suspension after 60 min of reaction. Fermentation parameters for bioethanol production were evaluated by using a full factorial design (32) with fermentation time (h) and concentration of glucose equivalent (%) as independent variables. Results from factorial design showed that the highest ethanol production was found when 1% of glucose equivalent was fermented by 48 h. At these conditions the bioethanol conversion efficiency reached 92.13% and it was estimated a productivity of 596.96 L tonne−1. It can be concluded that the starch from S. lycocarpum fruit is a promising non-food and renewable energy source for bioethanol production.

Background:: Solanum lycocarpum is a medicinal plant used in Brazil with hypoglycemic activity by its fruits use. However, the fruits production is restricted in some periods of the year, differently of leaves. Objective:: To evaluate the effects of hydroalcoholic extracts of S. lycocarpum leaves in alloxan-induced diabetic mice. Methods:: Hydroalcoholic extract of S. lycocarpum was characterized by phytochemical and GCMS analysis. The Antidiabetic activity was assessed following treatment for 22 days with S. lycocarpum extract at 125, 250, and 500 mg/kg. Bodyweight, water, and food intake, glycemia, biochemical parameters, anatomy-histopathology of the pancreas, liver and kidney, and expression of target genes were analyzed. In addition, oral acute toxicity was evaluated. Results:: Animals treated showed a significant reduction (p < 0.05) in glycemia following a dose of 125 mg/kg. Food intake remained similar for all groups. Decreased polydipsia symptoms were observed after treatment with 250 (p < 0.001) and 500 mg/kg (p < 0.01) compared with diabetic control, although normal rates were observed when 125 mg/kg was administered. A protective effect was also observed in the pancreas, liver, and kidneys, through the regeneration of the islets. Hypoglycemic activity can be attributed to myo-inositol, which stimulates insulin secretion, associated with α-tocopherol, which prevents damage from oxidative stress and apoptosis of β-pancreatic cells by an increased Catalase (CAT) and Glutathione peroxidase 4 (GPX4) mRNA expression. The toxicological test demonstrated safe oral use of the extract under the present conditions. Conclusion:: Hydroalcoholic extract of S. lycocarpum promotes the regulation of diabetes in the case of moderate glycemic levels, by decreasing glycemia and exerting protective effects on the islets.

CNPq - Conselho Nacional de Desenvolvimento Científico e Tecnológico CAPES - Coordenação de Aperfeiçoamento de Pessoal de Nível Superior FAPESP - Fundação de Amparo à Pesquisa do Estado de São Paulo Outra Agência Fruta-do-lobo (Solanum lycocarpum St. Hill) is a native fruit commonly used in Brazilian folk medicine as a hypoglycemic agent. These properties are attributed to their starch, mainly its resistant fraction. Resistant starch has shown to increases the growth of Bifidobacterium and Lactobacillus in the gut, even though not being selective for these strains. In this scenario, this study aimed to investigate the potential prebiotic activity of fruta-do-lobo starch (FLS). FLS showed around 30% of resistant starch and their prebiotic potential was evaluated with five probiotic strains L. acidophilus (LA3 and LA5), L. casei (LC01) and B. animalis (BB12) and B. lactis (BLC1) in a concentration range of 1.0–2.0% of starch. In a preliminary screening, we evaluated, during 48 h, the viability of the starch with promoting growth agent. An increase in the growth of the probiotic strains tested was observed. We also evaluated the microorganism’s metabolic activity by assessing the short-chain fatty acid (SCFA) production, using the best starch growth promotion conditions (2% of FLS and strains BLC1, LA5, and LC01). As expected, MRS and lactose were preferentially metabolized by BLC1, with the highest growth rates: 0.231 and 0.224 h−1, respectively. However, for this strain, the FLS growth rate (0.222 h−1) was 65% higher than FOS (0.144 h−1). Also, for LA5 FLS promoted higher growth (0.150 h−1) than FOS (0.135 h−1). Additionally, FLS promoted acetate production. These data are promising and indicate that FLS may have prebiotic potential and more studies need to be done with pathogenic microorganisms.

The species Solanum lycocarpum is popularly known as “fruit of the wolf”, and is widely used in traditional medicine. In the present study, the hexane and methanol extracts obtained from the unripe fruits of S. lycocarpum, using a Soxhlet extractor, were evaluated for allelopathic and antioxidant activities. In addition, the content of phenolic compounds and flavonoids was determined. The extracts showed antioxidant activity at the seven concentrations tested. The EC50 values obtained for the extracts could be correlated directly with the content of the phenolic compounds and flavonoids present in the samples. For the allelopathic activity, the samples showed heterogeneous effects on the growth of the hypocotyl and radicle of onion seeds, as well as inhibitory effects against lettuce seeds. These results encourage further studies of this species in order to isolate and identify the compounds responsible for these activities that, in the future, could be used as antioxidants or allelochemicals of a natural origin.

Bladder cancer (BC) is the 9th most common cancer in the worldwide. BC's treatment is still a challenging goal. Thereby, the screening of natural compounds as solasonine (SS) and solamargine (SM) that exhibit antitumor activity is interesting to BC therapy. This work aimed to develop natural lipid-based nanoparticles (NLN) as carrier system of S. lycocarpum's fruits alkaloidic extract (AE), rich in SS and SM, and to evaluate its antitumor activity in bladder cancer cells. The NLN-AE exhibited 56 nm of diameter, low polydispersity index with shelf life estimated of 12 months, measured by LUMiSizer®. NLN-AE showed low recrystallization index with high encapsulation efficiency of SS (86%) and SM (89%). A sustained release profile was verified after 36 h. The free AE exhibited antitumor activity in bladder cancer cells. The cell viability decreased 5.4 fold when AE was encapsulated in NLN. Thus, NLN-AE has higher anti-proliferative activity than the free AE.

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.

Conduziu-se um experimento em casa de vegetação com o objetivo de avaliar o comportamento de Solanum lycocarpum sob a influência da adubação mineral e orgânica quando cultivada em rejeito da mineração de quartzito visando subsidiar ações voltadas para a recuperação de áreas de exploração de quartzito. Os tratamentos consistiram de cinco combinações de adubação orgânica (AO) e mineral (AM) e um tratamento adicional do rejeito sem AO e AM (Controle). As combinações foram: 0%AO/100%AM; 25%AO/75%AM; 50%AO/50%AM; 75%AO/25%AM; 100%AO/0% AM. As doses que corresponderam ao tratamento de 100% de AM e AO foram de 150 mg de N, 140 mg de P, 150 mg de K e 5 g de esterco de curral por dm³ de rejeito. A Solanum lycocarpum respondeu à adubação mineral e orgânica com as doses recomendadas de 36,0 mg N, 33,6 mg P e 36,0 mg K e 3,8 g de esterco de curral por dm3 de rejeito da mineração de quartzito. O acúmulo de nutrientes na espécie Solanum lycocarpum nas doses recomendadas foi na seguinte ordem na parte aérea: N> K > Ca > P > S > Mg > Mn > B > Fe > Cu > Zn com adubação mineral e orgânica para o máximo crescimento da espécie.

Oils were obtained from unripe and ripe fruits of Solanum lycocarpum. In this study, the volatile and semi-volatile compounds of oils were characterized by gas chromatography-mass spectrometry (GC-MS). Oil of unripe fruits (OUF) of S. lycocarpum exhibited principally fatty acids, esters, hydrocarbons and sterols. However, oil of ripe fruits (ORF) presented the major compounds esters and sterols. In OUF-7, the predominant compound was octadecanoic acid (73.37%), in ORF-2, octadecanoic acid octadecyl ester (59.30%) and in ORF-3, hexadecanoic acid hexadecyl ester (97.98%). Sitosterol, identified in OUF-2 and OUF-6, is predominant sterol found in various species of Solanum can have chemotaxonomy importance for this genus. This is the first time, to the best of our knowledge, that volatile and semi-volatile compounds of oils from S. lycocarpum fruits have been characterized.

Novelty statement This manuscript entitled “Elucidation of adsorption mechanism of Pb(II) onto lobeira fruit (Solanum lycocarpum) using a Langmuir, Freundlich and Temkin isotherms” by Cleide Sandra Tavares Araujo et al. describes the sorption potential of lobeira fruit (Solanum lycocarpum) for removing Pb(II) from aqueous solution using a factorial experimental design as optimization strategy and Langmuir, Freundlich and Temkin models have been used to fit adsorption isotherms. The Solanum lycocarpum known popularly as “lobeira-do-cerrado”, wolf fruit or “jurubebao”, is a lignocellulosic typical species of the “cerrado” (kind of Brazilian savannah), with wide distribution, mainly in anthropized areas, has been little explored for adsorption studies. The optimization using a factorial design enabled the optimization of the procedure to be carried out with a reduced number of experiments, thus requiring a lower quantity of reagents and showed has advantages, such as, the low cost of sorbent, high efficiency and the minimization of chemical sludge. So allowed the adsorption of lead by lobeira fruit an inexpensive and easily available raw material may be used for different industrial applications to lower the cost of wastewater treatment and has potential applications for the removal of Pb(II) from wastewater. The sorbent is an alternative material for chemical remediation and is economic and environmental friendly.

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.

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.

The fruit of Solanum lycocarpum is a rich source of starch which remains unexploited despite its promising chemical and rheological properties. In this study, the molecular structures of amylopectin and amylose from S. lycocarpum starch were evaluated by HPAEC-PAD, being determined their chain length and degree of polymerization (DP). In addition, the starch was submitted to enzymatic hydrolysis using immobilized α-amylase (PANI-AMY) and glucoamylase (PANI-GLU). The enzymes immobilization onto polyaniline-glutaraldehyde derivatives was optimized through a Central Composite Rotatable Design (CCRD) and the hydrolysis products were characterized by Thin Layer Chromatography (TLC) and HPAEC-PAD. Results showed that amylopectin from S. lycocarpum starch had a maximal DP of 86, being observed a predominance of chains with type B1 (DP 13–24). On the other hand, the amylose is composed by short chain polymers, presenting DP of 57. Results from serial hydrolysis evidenced that the PANI-AMY reactor produced a set of malto-oligosaccharides, with predominance of pentoses (348.11 μg mL−1), while in the PANI-GLU reactor it was produced high levels of glucose. In addition, hydrolysis tests using high starch concentration (10% w/v) evidenced that the reactors can be efficiently used to hydrolyze starch at the similar concentration to that used in industrial processes, being able to efficiently produce starch liquefaction. Therefore, the results obtained in this work contribute to improve the information about the properties and potentialities of native and hydrolyzed starches from S. lycocarpum.

Made available in DSpace on 2019-10-06T15:58:00Z (GMT). No. of bitstreams: 0 Previous issue date: 2018-11-01. Added 1 bitstream(s) on 2019-10-09T18:35:02Z : No. of bitstreams: 1 S0102-695X2018000600673.pdf: 744468 bytes, checksum: 02f50876279d10d036ccab0e85453c1c (MD5) Leishmania infantum is an etiologic agent of visceral leishmaniasis. This disease is a neglected disease that can be fatal if not treated and additionally, the few therapeutic option present several drawbacks, including difficult route of administration and toxicity, which turn the search for new therapeutic alternatives necessary. Herein, we evaluated the leishmanicidal in vitro activity of the solanum extract from Solanum lycocarpum A. St.-Hil., Solanaceae, and the isolated alkaloids solasodine, solamargine and solasonine against promastigotes and intracellular amastigotes of L. infantum. Solasodine (IC50-pro = 4.7 μg/ml; IC50-ama = 10.8 μg/ml) and solamargine (IC50-pro = 8.1 μg/ml; IC50-ama = 3.0 μg/ml) exhibited interesting leishmanicidal ativity. Solasonine was approximately four-times (Selective Index 3.7) more selective to the parasite than to the host cells. This data suggest that solasonine might be considered as a potential drug candidate for leishmaniasis treatment. Instituto de Química UNESP – Universidade Estadual Paulista Programa de Pós-graduação em Biotecnologia Faculdade de Ciências Farmacêuticas UNESP – Universidade Estadual Paulista Departamento de Análises Clínicas Centro Universitário da Fundação Educacional de Barretos Faculdade de Farmácia Universidade de Coimbra Departamento de Princípios Ativos e Naturais Faculdade de Ciências Farmacêuticas UNESP – Universidade Estadual Paulista Instituto de Química UNESP – Universidade Estadual Paulista Programa de Pós-graduação em Biotecnologia Faculdade de Ciências Farmacêuticas UNESP – Universidade Estadual Paulista Departamento de Análises Clínicas Departamento de Princípios Ativos e Naturais Faculdade de Ciências Farmacêuticas UNESP – Universidade Estadual Paulista

This paper aims at evaluating the shelf life of mini tomatoes (Lycopersicum esculentum Mill.) cultivar ‘Sweet Grape’, grown in hydroponics, and stored under environmental and refrigerated conditions inside different packages. We adopted a completely randomized design, in which treatments were combinations of storage conditions: environment (e) and refrigerated (r) with packaging: polyvinyl chloride film (PVC); low-density polyethylene (LDPE); biofilm of tomato fruit of Solanum lycocarpum A.St.-Hil (lobeira) (TFB); cassava starch biofilm (CSB); carnauba wax (Copernicia prunifera) (CW), and without packaging - control (C). Physicochemical and sensory tests were carried out at the beginning (day zero), and at 8, 19, and 33 days of storage (DS). Fruit stored inside PVCr, LDPEe, LDPEr, and CWr had an acceptable shelf life of 33 days. The use of cassava and tomato starches were not effective in controlling fruit fresh weight loss. ‘Sweet Grape’ tomato postharvest conservation was enhanced under refrigerated conditions. The sensory evaluation results revealed that CWr treatment most pleased appraisers, while PCV had the highest rejection rate. RESUMO Objetivou-se avaliar a vida útil do minitomate (Lycopersicum esculentum Mill.), variedade Sweet Grape, produzido em hidroponia e armazenado sob condição ambiente e refrigerada, em diferentes embalagens. Adotou-se o delineamento experimental inteiramente casualizado, em que os tratamentos consistiram na combinação da condição de armazenamento: ambiente (a) e refrigerada (r), e tipo de embalagem: filme flexível de policloreto de vinila (PVC); polietileno de baixa densidade (PEBD); biofilme de fruto de Solanum lycocarpum A.St.-Hil (lobeira) (BFL); biofilme de fécula de mandioca (BFM); cera de Copernicia prunifera (carnaúba) (CC), e sem embalagem - testemunha (T). As análises físico-químicas e sensoriais foram realizadas no início (dia zero), aos 8, 19 e 33 dias de armazenamento (DA). Os frutos submetidos às embalagens PVCr, PEBDa, PEBDr e CCr apresentam vida útil aceitável de 33 dias de armazenamento. A aplicação de biofilmes de amidos de fruto de lobeira e mandioca não é eficaz no controle da perda de massa fresca. A condição refrigerada é a melhor forma para a conservação pós-colheita dos frutos de minitomate. O tratamento CCr é o que mais agrada os julgadores, e o PCV, o de maior índice de rejeição.

TheSolanum lycocarpumspecies, belonging to the Solanaceae family, is popularly known as the wolf fruit and is used in folk medicine for the treatment of obesity, diabetes, and cholesterol reduction. Thus, the aim of this study was to perform phytochemical screening of the ethanol extract from the ripe fruit ofS. lycocarpumto verify the presence of the main groups of secondary metabolites and to evaluate the phytotoxic effect onLactuca sativa(lettuce) andAllium cepa(onion) seeds. The fruits ofS. lycocarpumwere collected, crushed and percolated with anhydrous ethanol and the solvent was dried in a rotatory evaporator to obtain the ethanol extract. In the phytotoxicity evaluation, the results showed that the ethanol extract was able to completely inhibit the growth of hypocotyl and radicle ofL. sativa(lettuce) seeds in all concentrations tested. InA. cepa(onion) seeds, a concentration of 500 μg per plate was able to inhibit the growth of the hypocotyl and radicle by 100%. The metabolites detected in the extract were alkaloids, coumarins, flavonoids, and condensed tannins. The phytotoxic activity can be correlated to the presence of these compounds. A espécie Solanum lycocarpum, pertencente à família Solanaceae, é conhecida popularmente como lobeira ou fruto do lobo e utilizada na medicina popular para o tratamento da obesidade, do diabetes e na redução do colesterol. Desta forma, o objetivo deste estudo foi realizar a triagem fitoquímica do extrato etanólico do fruto maduro de S. lycocarpum para verificar a presença dos principais grupos de metabólitos secundários e avaliar o efeito fitotóxico sobre sementes de Lactuca sativa (alface) e de Allium cepa (cebola). Os frutos de S. lycocarpum foram coletados, triturados e extraídos por percolação com etanol anidro e, o solvente foi secado em evaporador rotatório, obtendo-se o extrato etanólico. Na avaliação da fitotoxicidade, os resultados demonstraram que o extrato etanólico foi capaz de inibir completamente o crescimento do hipocótilo e da radícula de sementes de L. sativa (alface), em todas as concentrações testadas. Nas sementes de A. cepa (cebola), a concentração de 500 μg por placa foi capaz de inibir em 100% o crescimento do hipocótilo e da radícula. Os metabólitos detectados no extrato foram alcaloides, cumarinas, flavonoides e taninos condensados. A atividade fitotóxica pode ser correlacionada à presença desses compostos.

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.

The increasing need for starches with specific characteristics makes it important to study unconventional starches and their modifications in order to meet consumer demands. The aim of this work was to study physicochemical characteristics of native starch and phosphate starch of S. lycocarpum. Native starch was phosphated with sodium tripolyphosphate (5-11%) added with stirring. Chemical composition, morphology, density, binding ability to cold water, swelling power and solubility index, turbidity and syneresis, rheological and calorimetric properties were determined. Phosphorus was not detected in the native sample, but the phosphating process produced modified starches with phosphorus contents of 0.015, 0.092 and 0.397%, with the capacity of absorbing more water, either cold or hot. Rheological data showed the strong influence of phosphorus content on viscosity of phosphate starch, with lower pasting temperature and peak viscosity higher than those of native starch. Enthalpy was negatively correlated with the phosphorus content, requiring 9.7; 8.5; 8.1 and 6.4 kJ g-1 of energy for the transition from the amorphous to the crystalline state for the starch granules with phosphorus contents of 0; 0.015; 0.092 and 0.397%, respectively. Cluster analysis and principal component analysis showed that starches with 0.015 and 0.092% phosphorus have similar characteristics and are different from the others. Our results show that the characteristics of phosphate modified S. lycocarpum starch have optimal conditions to meet the demands of raw materials, which require greater consistency in stickiness, combined with low rates of retrogradation and syneresis. Em vista da necessidade de amidos com características específicas, é fundamental o estudo de amidos não convencionais e de suas modificações, de acordo com as exigências do mercado consumidor. O objetivo deste trabalho foi estudar as características físico-químicas de amidos nativo e fosfatado da S. lycocarpum. O amido foi fosfatado com tripolifosfato de sódio (de 5 a 11%), sob agitação. Determinaram-se a composição química, a morfologia, a densidade, a capacidade de ligação à água fria, o poder de inchamento e o índice de solubilidade, a turbidez e a sinerese, as propriedades reológicas e calorimétricas. Não se detectou fósforo na amostra nativa, porém, a fosfatação gerou amidos modificados com teores de fósforo de 0,015, 0,092 e 0,397%, que se caracterizaram por absorver maior quantidade de água, a frio e a quente. Os resultados reológicos mostraram a forte influência do teor de fósforo na viscosidade dos fosfatados, apresentando temperatura de empastamento menor e viscosidade de pico maior que as do amido nativo. A entalpia correlacionou-se negativamente com o teor de fósforo, necessitando-se de uma energia de 9,7; 8,5; 8,1 e 6,4 kJ g-1, para a transição do estado cristalino para o amorfo, dos grânulos de amido com teores de fósforo de 0; 0,015; 0,092 e 0,397%, respectivamente. As análises de agrupamento e dos componentes principais mostraram que os amidos com 0,015 e 0,092% de fósforo apresentam características semelhantes entre si e diferentes daquelas dos demais, concluindo-se que as características conferidas pela fosfatação ao amido da S. lycocarpum reunem ótimas condições para as exigências de determinadas matérias-primas, para as quais se desejem consistências maiores no empastamento, combinadas com baixos índices de retrogradação e sinerese.

In this work a polyphenol oxidase (PPO) from Solanum lycocarpum ripe and unripe fruits was studied. The unripe fruits presented higher activity than ripe for both fresh fruits and dried pulp flours. The purification procedure was based on freezing precipitation and a sixfold purification factor was obtained. The SDS-PAGE of the partially purified PPO showed two bands around 47 and 68 kDa. Optimal conditions for enzymatic studies were determined to be pH 6.0–6.5 and 28 °C. The partially purified PPO presented high activity toward catechol (Vmax 3.42 U mL−1 and Km 6.47 mM) and 4-methylcatechol (Vmax 3.01 U mL−1 and Km 0.15 mM) and low activity toward phenol being classified as a catecholase type polyphenol oxidase. S. lycocarpum PPO was sensitive to inhibitors such as l -cysteine, sodium metabisulfite, ascorbic acid, thiourea and citric acid. l -Cysteine was the most effective inhibitor, presenting a competitive inhibition. The results from kinetic and thermodynamic parameters for the thermal inactivation evidenced that the partially purified PPO is a biocatalyst, whose inactivation process is related to aggregation of partially unfolded enzyme molecules.

This study was conducted to evaluate the rheological and physicochemical properties of Solanum lycocarpum starch. The thermogravimetric analysis of S. lycocarpum starch showed a typical three-step weight loss pattern. Microscopy revealed significant changes in the granule morphology after hydrothermal treatment. Samples hydrothermally treated at 50 °C for 10 min lost 52% of their crystallinity, which was recovered after storage for 7 days at 4 °C. However, samples hydrothermally treated at 65 °C were totally amorphous. This treatment was sufficient to completely disrupt the starch granule, as evidenced by the absence of an endothermic peak in the DSC thermogram. The RVA of S. lycocarpum starch revealed 4440.7 cP peak viscosity, 2660.5 cP breakdown viscosity, 2414.1 cP final viscosity, 834.3 cP setback viscosity, and a pasting temperature of 49.6 °C. The low content of resistant starch (10.25%) and high content of digestible starch (89.78%) in S. lycocarpum suggest that this starch may be a good source for the production of hydrolysates, such as glucose syrup and its derivatives.

Leishmaniasis is an infection caused by a protozoan parasite of the genus Leishmania and is the second most prevalent parasitic protozoal disease after malaria in the world. We report the in vitro leishmanicidal activity on promastigote forms of Leishmania amazonensis and cytotoxicity, using LLCMK2 cells, of the glycoalkaloids from the fruits of Solanum lycocarpum, determined by colorimetric methods. The alkaloidic extract was obtained by acid-base extraction; solamargine and solasonine were isolated by silica-gel chromatography, followed by reversed-phase HPLC final purification. The alkaloidic extract, solamargine, solasonine, as well as the equimolar mixture of the glycoalkaloids solamargine and solasonine displayed leishmanicidal activity against promastigote forms of L. amazonensis, whereas the aglycone solasodine was inactive. After 24 and 72 h of incubation, most of the samples showed lower cytotoxicities (IC50 6.5 to 124 μM) as compared to leishmanicidal activity (IC50 1.1 to 23.6 μM). The equimolar mixture solamargine/solasonine was the most active with an IC50 value of 1.1 μM, after 72 h. Likewise, solamargine was the most active after 24 h with an IC50 value of 14.4 μM, both in comparison with the positive control amphotericin B.

Universidade Estadual Paulista Julio de Mesquita Filho, Departamento de Principios Ativos Naturais e Toxicologia, Faculdade de Ciencias Farmaceuticas de Araraquara, Araraquara, Rodovia Araraquara Jau Km 1, CEP 14801-902, SP, Brasil

Neste trabalho, pectina extraida de frutos de lobeira ( Solanum lycocarpum St. Hil ) foi utilizada como suporte para a imobilizacao de lipase. Os frutos de lobeira foram secos e a farinha utilizada para a extracao da pectina. Para o processo de extracao foi utilizado um planejamento fatorial 2 3 com temperatura, pH e tempo como variaveis independentes. A imobilizacao foi realizada por adsorcao e por ligacao covalente utilizando periodato de sodio (PEC-P) ou glutaraldeido (PEC-G) como ativadores do suporte. Os resultados indicaram que a ativacao por PEC-P foi eficiente para a imobilizacao da enzima. A imobilizacao por adsorcao e por ligacao covalente para o suporte PEC-G nao apresentaram estabilidade ao armazenamento. Os resultados para os testes de estabilidade ao armazenamento do sistema lipase-PEC-P demonstraram que este sistema manteve 85,4% da atividade enzimatica apos onze semanas de estocagem. Estes resultados habilitam a utilizacao da pectina extraida de lobeira como um suporte promissor para a imobilizacao de enzimas.

In this work Solanum lycocarpum fruits were used as a source of pectin. The parameters of pectin extraction were examined using a 23 factorial design, with temperature, pH and extraction time as independent variables. The extracted S. lycocarpum pectin and dried pulp were analyzed for the presence of antinutritional compounds, such as amylase and trypsin inhibitors, hemagglutinin, tannins, saponins, alkaloids and phytate. Pectin was characterized by measuring its methoxylation degree, intrinsic viscosity and molecular weight. The best pectin extraction conditions yielded as much as 33.6% (dry matter). The S. lycocarpum pectin was determined to be highly methoxylated (77.15%), and it showed an intrinsic viscosity 4.6% lower than that of citrus pectin, probably due to its lower molecular weight (177.76 kDa versus 224.48 kDa of that of citrus pectin). Although there were tannins and phytate in the dried pulp, the pectin fraction was free of these compounds.

O polvilho da fruta-de-lobo é um produto extraído da polpa da fruta-de-lobo verde (Solanum lycocarpum St. Hil), popularmente utilizado. Pouco se conhece a respeito desse polvilho, apesar de ele ser comercializado em farmácias na região de Lavras-MG, na forma de cápsulas de 300 mg. É utilizado no tratamento da diabetes e a ele são atribuídos outros efeitos terapêuticos, como a redução da obesidade e do colesterol, mas sem conhecimento científico e sem conhecer sua composição centesimal. Com o objetivo de conhecer sua composição centesimal, foram coletadas 80 frutas-de-lobo na área de pastagem do Departamento de Zootecnia, na Universidade Federal de Lavras. Foram selecionadas 61 frutas, levando em consideração o tamanho e o estádio de maturação. As frutas selecionadas foram lavadas, descascadas e picadas, as sementes retiradas, trituradas e o polvilho obtido foi filtrado, decantado, lavado com água destilada por duas vezes e seco em estufa de ventilação. A amostra foi triturada em um gral de porcelana e armazenada em um recipiente de vidro hermeticamente fechado e protegido da luz, sob temperatura ambiente. Foram realizadas as análises de composição centesimal, observando-se que, no polvilho da fruta-de-lobo, os carboidratos são os constituintes predominantes (84,99%), seguidos de fibras solúveis (1,35%), fibras insolúveis (1,60%), proteínas (0,60%), lipídeos (0,07%), cinzas (0,03%) e umidade (11,16%). Os teores de fibras alimentares encontrados no polvilho da fruta-de-lobo podem estar relacionados aos efeitos terapêuticos que são atribuídos a ele. Fruit-of-wolf flour is a product extracted from the unripe fruit-of-wolf pulp (Solanum lycocarpum St. Hil), according to folk knowledge. Little is known of that starch; in spite of it is being marketed in pharmacies in the region of Lavras, in 300 mg capsules. It is utilized in the treatment of diabetes and it is also ascribed other therapeutic effects such as reduction of obesity and cholesterol, but without any scientific knowledge and without knowing its centesimal composition. With the objective of knowing its centesimal composition, eighty fruits were collected in the pasture area of the Animal Science Department of the UFLA/Lavras-MG. Sixty-one fruits were selected, taking into account the size and maturation stage. The selected fruits were washed, peeled, chopped, the seeds removed and the obtained starch was filtered, decanted, washed with distilled water twice and dried in an air forced oven. The sample was ground in a china mortar and stored in air-tightly sealed glass container and protected from light at room temperature. The centesimal composition analyses were performed and observing that in the fruit-of-wolf flour, carbohydrates are the predominant constituents (84.99%), followed by soluble fibers (1.35%), insoluble fibers (1.60%), proteins (0.60%), lipids (0.07%), ashes (0.03%) and moisture (11.16%). The contents of food fibers found in the fruit-of-wolf flour can be related to the therapeutic effects which are ascribed to it.

Fruit of wolf (Solanum lycocarpum A. St. - HILL), found in Brazilian cerrado, has been used in the initial ripening stage as flour and/or starch in popular medicine due to its hypoglycemiant action. The aim of this work was to study the occurrence of phytochemical compounds, physical, chemical and technological characteristics of fruit of wolf flour and starch in the initial ripening stage. Flour and starch were extracted using known popularly and experimental methods (with sodium bisulfite) and chemical composition and technological characteristics were analyzed. The results were comparatively assessed by Tukey's test (p

Solanum lycocarpum A. St. Hil. (Solanaceae) is a hairy shrub or small much-branched tree of the Brazilian Cerrado. S. lycocarpum fruits are commonly used in traditional medicine in powder form or as folk preparations for the treatment of diabetes and obesity, as well as for controlling cholesterol levels. The aim of the present study was to chemically characterize the hydroalcoholic extract (SL) of S. lycocarpum by determination of total flavonoids and total poyphenols and quantification of steroidal alkaloids, as well as to evaluate its mutagenic and/or antimutagenic potential on V79 cells and Swiss mice using chromosomal aberrations and bone marrow micronucleus assays, respectively. Three concentrations of SL (16, 32, and 24 µg/mL) were used for the evaluation of its mutagenic potential in V79 cells and four doses (0.25, 0.50, 1.0, and 2.0 g/kg body weight) were used for Swiss mice. In the antimutagenicity assays, the different concentrations of SL were combined with the chemotherapeutic agent doxorubicin (DXR). HPLC analysis of SL gave contents of 6.57 % ± 0.41 of solasonine and 4.60 % ± 0.40 of solamargine. Total flavonoids and polyphenols contents in SL were 0.04 and 3.60 %, respectively. The results showed that not only SL exerted no mutagenic effect, but it also significantly reduced the frequency of chromosomal aberrations induced by DXR in both V79 cells and micronuclei in Swiss mice at the doses tested.

Introduction The larvicidal activity of Solanum lycocarpum against Culex quinquefasciatus is unknown. Methods We evaluated the larvicidal activity of extracts of the green fruits of Solanum lycocarpum against third and fourth instar larvae of C. quinquefasciatus. Results Dichloromethane and ethyl acetate fractions showed the greatest larvicidal effect at 200mg/L (83.3% and 86.7%, respectively). The methanol and dichloromethane, ethyl acetate, and hydromethanolic fractions demonstrated larvicidal effects against C. quinquefasciatus, with LC50 values of 126.24, 75.13, 83.15, and 207.05mg/L, respectively. Conclusions Thus, when considering new drugs with larvicidal activity from natural products, S. lycocarpum fruits may be good candidate sources.

Diferentes grupos vegetais encontrados no bioma Cerrado vêm sendo amplamente estudados quanto as suas possíveis características químicas, apresentando dentre essas biocompostos de interesse para a indústria de alimentos, como na produção de barras de cereais nutritivas e em condimentos alimentares capazes de inibir ações de radicais livres causadores de patologias. No entanto, ainda pouco se sabe sobre a grande variedade destes compostos bioativos, que compõem as características químicas das espécies rasteiras, arbustivas e arbóreas, que coabitam nas mais diversas variantes deste bioma. A descoberta dos efeitos deletérios dos radicais livres sobre as células, agindo como causadores de doenças, impulsionando a busca por novos compostos bioativos na área de alimentos, que a cada ano cresce com a produção de novos produtos alimentícios, com características mais saudáveis, permitindo a prevenção e minimizando os danos oxidativos sobre as células. O presente trabalho teve como objetivo avaliar a atividade antioxidante pela captura do radical DPPH, conteúdos de fenólicos totais pelo reagente de Folin-Ciocalteau, carotenoides, provitamina A em equivalente de Retinol por métodos espectrofotométricos UV-Vis dos extratos etanólicos foliares das espécies botânicas: Byrsonima coccolobifolia (Kunth.), Dimorphandra mollis (Benth.), Hymenaea stignocarpa (Mart. ex Hayne), Solanum lycocarpum (St. Hil.) e Cardiopetalum calophyllum (Schlecht.). Os resultados demonstraram a presença de atividade antioxidante pelo método de sequestro do radical DPPH, expressivos conteúdos de fenólicos totais, teores de β-caroteno, presença de licopeno, exceto nas espécies Dimorphandra mollis e Hymenaea stignocarpa, presença de baixos teores de provitamina A.Palavras-chave: Folhas. DPPH. Licopeno.AbstractDifferent vegetable groups found in the Cerrado biome have been widely studied as to their possible chemical characteristics, presenting among them biocomposites of interest for the food industry, as in the production of nutritious cereal bars and in food condiments capable of inhibiting actions of free radicals causing pathologies. But little is known about the great variety of these bioactive compounds that make up the chemical characteristics of the shrub, shrub and tree species that cohabit in the most diverse variants of this biome. The discovery of the deleterious effects of free radicals on cells, acting as cause of disease, driving the search for new bioactive compounds in the area of food that grows every year with the production of new food products with healthier characteristics allowing prevention and minimizing the oxidative damage on cells. The objective of the present work was to evaluate the antioxidant activity by capturing DPPH radical, total phenolic contents by Folin-Ciocalteau reagent, carotenoids, provitamin A in Retinol equivalent by UV-Vis spectrophotometric methods of the foliar ethanolic extracts of botanical species: Byrsonima Coccolobifolia (Kunth.), Dimorphandra mollis (Benth.), Hymenaea stignocarpa (Mart. ex Hayne), Solanum lycocarpum (St. Hil.) and Cardiopetalum calophyllum (Schlecht.). The results showed the presence of antioxidant activity by the DPPH radical sequestration method, expressive total phenolic content, β-carotene content, lycopene content, except for Dimorphandra mollis and Hymenaea stignocarpa species, with low levels of provitamin A.Keywords: Sheets. DPPH. Lycopene.

Background Solanaceae seed morphology and physiology have been widely studied but mainly in domesticated crops. The present study aimed to compare the seed morphology and the physiology of germination of Solanum lycocarpum, an important species native to the Brazilian Cerrado, with two species with endospermic seeds, tomato and coffee. Methods Morphological parameters of fruits and seeds were determined by microscopy. Germination was monitored for 40 d under different temperature regimes. Endosperm digestion and resistance, with endo-beta-mannanase activity and required force to puncture the endosperm cap as respective markers, were measured during germination in water and in abscisic acid. Key Results Fruits of S. lycocarpum contain dormant seeds before natural dispersion. The best germination condition found was a 12-h alternating light/dark and high/low (20/30 degrees C) temperature cycle, which seemed to target properties of the endosperm cap. The endosperm cap contains 7-8 layers of elongated polygonal cells and is predestined to facilitate radicle protrusion. The force required to puncture the endosperm cap decreased in two stages during germination and showed a significant negative correlation with endo-beta-mannanase activity. As a result of the thick endosperm cap, the puncture force was significantly higher in S. lycocarpum than in tomato and coffee. Endo-beta-mannanase activity was detected in the endosperm cap prior to radicle protrusion. Abscisic acid inhibited germination, increase of embryo weight during imbibition, the second stage of weakening of the endosperm cap and of endo-beta-mannanase activity in the endosperm cap. Conclusions The germination mechanism of S. lycocarpum bears resemblance to that of tomato and coffee seeds. However, quantitative differences were observed in embryo pressure potential, endo-beta-mannanase activity and endosperm cap resistance that were related to germination rates across the three species.

Solanum lycocarpum, St. Hil (Solanaceae) is a common native shrub in the Brazilian cerrado. The fruits are used in folk medicine as a hypoglycaemic agent in the management of diabetes, obesity and to decrease cholesterol levels. In this study the glycoalkaloids, solamargine and solasonine, were isolated from unripe fruits of S. lycocarpum. To evaluate the effects of the fruits on gestation, pregnant rats (n=25) were fed from day 6 to 22 with chow containing 10% of dried and ground unripe fruits. The control group (n=21) received regular chow. During and after the treatment period the dams showed reduced body weight and slower body weight gain, even with no change in food and water intake, evidencing mild maternal toxicity. Gestation was not significantly impaired, although experimental fetuses presented reduced body length at birth. Also, 20% of the treated dams showed one or two dead pups at birth. On day 22 of gestation and on post-natal day 1, the levels of metabolites of the sex hormones oestradiol, progesterone and testosterone were measured in faeces by radioimmunoassay. On post-natal day 1, tissue portions from the dams were collected for histopathological evaluation. No alterations were detected in either study. The results suggest that S. lycocarpum fruit did not impair gestation, however, it did promote mild maternal toxicity and mild fetotoxic effects if ingested as a food source during the gestation period. This study has implications for pregnant women, who employ phytotherapeutic formulations under the impression that they are harmless.

In the course of our studies on antidiabetogenic compounds from natural medicines and medicinal foodstuffs, a methanolic extract of the fruits of Solanum lycocarpum showed an inhibitory effect on the increase of serum glucose levels in oral sucrose-loaded rats. Through bioassay-guided separation, three known steroidal alkaloid oligoglycosides, solamargine (1), solasonine (3), and 12-hydroxysolasonine (5), were isolated from the active fraction together with two new steroidal alkaloid oligoglycosides, robeneosides A (2) and B (4). The major constituents, solamargine (1) and solasonine (3), exhibited an inhibitory effect on the increase of serum glucose levels in oral sucrose-loaded rats. In addition, these compounds suppressed gastric emptying in mice. However, this methanolic extract from S. lycocarpum fruits did not have any effect on intestinal alpha-glucosidase (sucrase and maltase) in vitro. It was concluded that these steroidal alkaloid oligoglycosides, 1 and 3, inhibited the increase of rat serum glucose levels by suppressing the transfer of sucrose from the stomach to the small intestine.

Little has been done during the past 100 years to develop new antileishmanial drugs. Most infected individuals live in poor countries and have a low cash income to be attractive targets to pharmaceutical corporations. Two heterosidic steroids, solamargine and solasonine, initially identified as major components of the Brazilian plant Solanum lycocarpum , were tested for leishmanicidal activity. Both alkaloids killed intracellular and extracellular Leishmania mexicana parasites more efficiently than the reference drug sodium stibogluconate. A total of 10 μM each individual alkaloid significantly reduced parasite counts in infected macrophages and dendritic cells. In vivo treatment of C57BL/6 mice with a standardized topical preparation containing solamargine (45.1%) and solasonine (44.4%) gave significant reductions in lesion sizes and parasite counts recovered from lesions. Alkaloids present different immunochemical pathways in macrophages and dendritic cells. We conclude that this topical preparation is effective and a potential new and inexpensive treatment for cutaneous leishmaniasis.

Ethanol extract and fractions obtained from leaves ofSolanum lycocarpumwere examined in order to determine their phenolic composition, antioxidant, antibacterial, anti-inflammatory, and cytotoxic potential. High performance liquid chromatography coupled with DAD analysis indicated that the flavonoids apigenin and kaempferol were the main phenolic compounds present in dichloromethane and ethyl acetate fractions, respectively. The antioxidant activity was significantly more pronounced for dichloromethane, ethyl acetate, and hydroethanol fractions than that of the commercial antioxidant 2,6-di-tert-butyl-4-methylphenol. The hexane and dichloromethane fractions were more active against the tested bacteria. The hydroethanol fraction exhibited significant anti-inflammatory activity at the dose of 75 and 150 mg/kg in the later phase of inflammation. However, the antiedematogenic effect of the higher dose of the ethyl acetate fraction (150 mg/kg) was more pronounced. The ethyl acetate fraction also presented a less cytotoxic effect than the ethanol extract and other fractions. These activities found inS. lycocarpumleaves can be attributed, at least in part, to the presence of phenolic constituents such as flavonoids. This work provided the knowledge of phenolic composition in the extract and fractions and the antioxidant, antibacterial, anti-inflammatory, and cytotoxic activities of leaves ofS. lycocarpum.

This study investigated the induced defence responses and protective effects on susceptible tomato ( Lycopersicon esculentum Mill.) against Xanthomonas vesicatoria (Doidge) by a heat-treated aqueous extract (VLA) from dry necrotic tissue of ‘Lobeira’ ( Solanum lycocarpum St. Hil.) branches infected with the fungus Crinipellis perniciosa (Stahel) compared with acibenzolar- S -methyl (ASM), a commercial inducer of resistance. Plantlets were sprayed with VLA and ASM and challenged 4 days later with a virulent strain of X. vesicatoria , under greenhouse conditions. The disease severity, fresh weight of shoots, the activities of phenol peroxidase (POX), polyphenol oxidase (PPO), chitinase (CHI), phenylalanine ammonia-lyase (PAL), lignin deposition, and soluble phenolic contents were evaluated in the leaf tissues. Reduction of the bacterial spot severity was observed in plantlets treated with VLA which conferred 63% of the ASM protection. This protective effect and lesion reduction promoted by VLA were probably associated particularly with POX and PAL activities, lignin deposition on leaf tissues and, to a less extent, CHI activity.

O objetivo deste trabalho foi avaliar a influência de eliciadores biológicos e químicos sobre as atividades de duas proteínas relacionadas à patogênese (PR), quitinase e beta-1,3-glucanase, em folhas de tomateiro, e avaliar o potencial desses eliciadores na redução do progresso da mancha-foliar causada por Xanthomonas campestris pv. vesicatoria. Plantas de tomateiro da cultivar Santa Cruz Kada foram pulverizadas com: acibenzolar-S-metil (ASM; 0,2 g L-1); formulação biológica proveniente de biomassa cítrica, denominada Ecolife (5 mL L-1); suspensão de quitosana (MCp; 200 g L-1), proveniente de micélio de Crinipellis perniciosa; extrato aquoso de ramos de lobeira (Solanum lycocarpum) infectados por C. perniciosa (VLA; 300 g L-1). As plantas foram desafiadas com um isolado virulento da bactéria, quatro dias depois das pulverizações. Plantas pulverizadas com extratos biológicos mostraram redução da mancha-bacteriana. ASM proporcionou 49,3% de proteção, e foi igual à MCp e Ecolife e superior ao VLA. Este último não diferiu significativamente de MCp e Ecolife. Observou-se maior atividade das duas enzimas nas plantas tratadas, principalmente nas primeiras horas após as pulverizações.

Solanum lycocarpum St. Hil (Solanaceae) is an invasive and native shrub very common in the Brazilian savanna. It is well known that this plant contain steroidal glycoalkaloids that can be transformed into an intermediate for steroidal drugs production, like oral contraceptives. In this way, it is very possible that these glycoalkaloids and its aglycone, once in the body by ingestion of S. lycocarpum fruits, may act disrupting to the endocrine system. Rat offspring were exposed to S. lycocarpum unripe fruits (10% in the diet) from gestational day (GD) 06 to post-natal day (PND) 07. The female exposed offspring showed, at adult age (PND 100), impaired sexual behavior. However, the fecal hormonal metabolite levels, measured at PND 30, PND 60 and PND 90, and the fertility (PND 120) of male and female experimental offspring were normal. We can assume that the steroidal glycoalkaloids, solamargine and solasodine, present in the fruit, are degradated, once inside the organism, to the steroidal alkaloid solasodine, which may penetrate, by simple diffusion, the placental and/or the hematoencephalical barriers and impact the fetuses. Finally, S. lycocarpum fruit may act as phytohormones, promoting perhaps some neural alterations that at adult age may impair the sexual behavior of the experimental female without impairing the fertility and sexual hormone synthesis. These changes observed can be the direct consequence of the toxic actions of the steroidal alkaloid on the female offspring during fetal development.

We have investigated the hypoglycemic effect induced by the starch obtained from the unripe fruits of Solanum lycocarpum (Solanaceae). Per os administration of the starch (1000 or 2000 mg/kg, twice daily for 7 days, N = 6) did not change glycemia levels of nondiabetic female Swiss mice weighing 25-30 g. In streptozotocin-induced diabetic mice, similar treatment with the starch did not change the elevated glycemia 3 h after the last dose (diabetic treated with saline = 288 17/309 18; starch 1000 mg/kg = 295 +/- 33; starch 2000 mg/kg = 258 +/- 37; N = 5). In animals fasted for 15 h, per os administration of glucose (600 mg/kg) significantly increased glycemia 1 h later. Previous (-30 min) treatment of the animals with the starch (1000 or 2000 mg/kg; N = 5) did not change the increase of glycemia. Per os administration of the starch (1000 or 2000 mg kg-1 day-1, twice daily for 7 days) did not induce body weight gain or loss. The chemical analysis of the starch indicated the presence of glycoalkaloids, a finding that represents a reason for concern since many of these substances are generally toxic. In interviews with 56 diabetic patients, 29 medicinal plants were reported as useful in their treatment of diabetes and S. lycocarpum was the sixth most frequently mentioned. All patients interviewed reported that they also used insulin or oral hypoglycemic drugs. The results of the present study do not provide evidence for a hypoglycemic effect associated with the polysaccharide fraction of S. lycocarpum in either normal or hyperglycemic mice. These data demonstrate the need for adequate pharmacological investigation of the natural products widely used in folk medicine.

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 [IC 50 ] ≤120.3 μg/mL). The mixture of glycoalkaloids (1:1) was more active (IC 50 = 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.

Background Phytochemical analysis of the fruits of Solanum lycocarpum, popularly known as “fruit of the wolf”, showed high concentrations of steroidal alkaloids, such as solasonine and solamargine which are substances with potential cytotoxic activity [1]. The cytotoxic activity displayed by these compounds may be due to presence of sugar moieties (rhamnose). Since there is interaction of glycoalkaloids with plasma membrane cholesterol leading to loss of membrane integrity, resulting in alterations in its permeability what induces cell death [2]. The aim of this study was to evaluate the cytotoxicity activity of the glycoalkaloids solamargine and solasonine purified from S. lycocarpum and commercial a-solanine alkaloid from potato sprout toward cell lines MCF-7 (human breast adenocarcinoma cell line), B16 (murine skin) and 3T3 (normal mouse embryo fibroblasts) by MTT.

Background The dermatophytes belong to one of the main groups of pathogenic fungus, characterized by the use of the host’s keratin for its nutrition, which are the most common cause of fungal infection in the world, affecting millions of individuals annually, causing a huge economic impact [1]. Therefore, there was an increase in the search for new antifungal agents from natural sources, because the majority of the available drugs in the market presents a restricted number of cellular targets and there are reports of resistant fungal strain to these utilized drugs [2]. Glycoalkaloids from the Solanum lycocarpum plant (lobeira) presents several biological activities, such as cytotoxic and antimicrobial activities [3]. The goal of this work was determination the Minimum Inhibitory Concentration (MIC) of the solanine, solamargine and solasodine from the S. lycocarpum in addition to evaluate the effect of these alkaloids in the regeneration of the Trichophyton rubrum cell wall.

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 fruits of Solanum lycocarpum, known as wolf-fruit, are used in folk medicine, and because of that we have evaluated both the genotoxic potential of its glycoalkaloidic extract (SL) and its influence on the genotoxicity induced by methyl methanesulfonate. Furthermore, the potential blocking effect of SL intake in the initial stage of colon carcinogenesis in Wistar rats was investigated in a short-term (4-week) bioassay using aberrant crypt foci (ACF) as biomarker. The genotoxic potential was evaluated using the Swiss mice peripheral blood micronucleus test. The animals were treated with different doses of SL (15, 30 and 60 mg/kg b.w.) for 14 days, and the peripheral blood samples were collected at 48 h, 7 days and 14 days after starting the treatment. For antigenotoxicity assessment, MMS was administered on the 14th day, and after 24 h the harvesting of bone marrow and liver cells was performed, for the micronucleus and comet assays, respectively. In the ACF assay, male Wistar rats were given four subcutaneous injections of the carcinogen 1,2-dimethylhydrazine (DMH, 40 mg/kg b.w.), twice a week, during two weeks to induce ACF. The treatment with SL (15, 30 and 60 mg/kg b.w.) was given for four weeks during and after carcinogen treatment to investigate the potential beneficial effects of SL on DMH-induced ACF. The results demonstrated that SL was not genotoxic in the mouse micronucleus test. In animals treated with SL and MMS, the frequencies of micronucleus and extensions of DNA damage were significantly reduced in comparison with the animals receiving only MMS. Regarding the ACF assay, SL significantly reduced the frequency of ACF induced by DMH.

Solanum lycocarpum St. Hill (SL) is commonly used in Brazilian folk medicine. The aim of the present study was to evaluate the validity of the traditional therapeutic indication of SL as hypoglycaemic agent. The extract reduced glycemia to 92.4 mg/dl in alloxan induced diabetic rats (230.5 mg/dl). We also investigated the potential of SL as antioxidant (it reduced in 27% nitrate generation in diabetic animals). Our results also demonstrated that SL is not ulcerogenic and restored haemoglobin and haematocrit to normal values in diabetic animals.

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.

Natural products are some of the important sources of new anticancer drugs. The Brazilian flora is considered one of the most diverse in the word, although not many large-scale pharmacological and phytochemical studies have been conducted to date. With this in mind, in the present study we evaluated the antiproliferative activity of Solanum lycocarpum fruit glycoalkaloid extract (SL) and its major compounds, solamargine (SM) and solasonine (SS), against different tumor cell lines: murine melanoma (B16F10), human colon carcinoma (HT29), human breast adenocarcinoma (MCF-7), human cervical adenocarcinoma (HeLa), human hepatocellular liver carcinoma (HepG2) and human glioblastoma (MO59J, U343 and U251). The antiproliferative activity was evaluated using XTT assay and results were expressed as IC50. The most pronounced antiproliferative activity was observed for SM, with IC50 values ranging from 4.58 to 18.23 μg/mL. The lowest IC50 values were observed against HepG2, being 9.60 μg/mL for SL, 4.58 μg/mL for SM and 6.01 μg/mL for SS. Thus, SL, SM and SS demonstrated antiproliferative activity against the tumor cell lines tested, and were most effective against the HepG2 cell line.

Made available in DSpace on 2014-10-01T13:08:56Z (GMT). No. of bitstreams: 0 Previous issue date: 2013-09-01Bitstream added on 2014-10-01T14:02:53Z : No. of bitstreams: 1 S0001-37652013000300903.pdf: 14786635 bytes, checksum: c3f2fd91c0d76e49a3bd3b990d21f550 (MD5) O objetivo deste estudo foi avaliar a potencial atividade tripanocida do extrato bruto etanólico dos frutos de Solanum palinacanthum, Solanum lycocarpum e do glicoalcalóide solamargina. Pó do fruto seco de S. palinacanthum e S. lycocarpum foram submetidos a extracção por refluxo com etanol a 96% e solamargina foi isolada a partir do extrato bruto de S. palinacanthum. Foram determinadas de ambos os extratos e a solamargina a atividade tripanocida utilizando o ensaio colorimétrico MTT. O Extrato de S. palinacanthum mostrou-se mais ativo (IC50 = 175,9 µg.ml–1) de que o extrato de S. lycocarpum (IC50 = 194,7 µg.ml–1). A solamargina apresentou forte atividade tripanocida (IC50 = 15,3 µg.ml–1), o que pode explicar a melhor atividade de ambos os extratos. O benzonidazol (IC50 = 9,0 µg.ml–1) é a única droga utilizada para o tratamento da doença de Chagas. Estes resultados demonstram pela primeira vez que os extratos etanólicos obtidos a partir de frutos de S. palinacanthum e S. lycocarpum, além da solamargina apresentam uma atividade tripanocida potencial. The present investigation was to evaluate the potential trypanocidal activity of crude ethanolic extract of the fruits of Solanum palinacanthum, Solanum lycocarpum and the glycoalcaloid, solamargine. S. palinacanthum and S. lycocarpum fruit powders were submitted to exhaustively extraction with 96% ethanol and solamargine were isolated from the extract of S. palinacanthum. Both extracts and solamargine were analysed for trypanocidal activity by using MTT colorimetric assay. Extracts of S. palinacanthum showed to be more active (IC50 = 175.9 µg.ml–1) than S. lycocarpum (IC50 = 194.7 µg.ml–1). Solamargine presented a strong activity (IC50 = 15.3 µg.ml–1), which can explain the better activity of the both extracts. Benznidazol (IC50 = 9.0 µg.ml–1) is the only drug used to treat Chagas' disease. These findings demonstrate for the first time that ethanol extracts obtained from both fruits of S. palinacanthum and S. lycocarpum and also solamargine have a potential anti-trypanosomal activity. Universidade Estadual Paulista Faculdade de Ciencias Farmaceuticas Departamento de Principios Ativos Naturais e Toxicologia Universidade Estadual Paulista Faculdade de Ciencias Farmaceuticas Departamento de Farmacos e Medicamentos Universidade Estadual Paulista Faculdade de Ciencias Farmaceuticas Departamento de Ciencias Biologicas Universidade Estadual Paulista Faculdade de Ciencias Farmaceuticas Departamento de Principios Ativos Naturais e Toxicologia Universidade Estadual Paulista Faculdade de Ciencias Farmaceuticas Departamento de Farmacos e Medicamentos Universidade Estadual Paulista Faculdade de Ciencias Farmaceuticas Departamento de Ciencias Biologicas

Solanum lycocarpum St.-Hil (Solanaceae) is a hairy shrub or small much-branched tree of the Brazilian Cerrado, popularly known as “fruit-of-wolf”. Considering that the induction of chromosomal mutations is involved in the process of carcinogenesis, and that S. lycocarpum is often used in folk medicine, it becomes relevant to study its effect on genetic material. In this sense, the aim of present study was to determine the possible cytotoxic, genotoxic and antigenotoxic potentials of S. lycocarpum fruits glycoalkaloid extract (SL) in Chinese hamster lung fibroblasts (V79 cells). The cytotoxicity was evaluated by the colony forming assay, apoptosis and necrosis assay, Trypan blue exclusion dye method and mitotic index. Genotoxic and antigenotoxic potential were evaluated by comet and chromosomal aberrations assays. Four concentrations of SL (4, 8, 16 and 32μg/mL) were used for the evaluation of its genotoxic potential. The DNA damage-inducing agent methyl methanesulfonate (MMS, 22μg/mL) was utilized in combination with extract to evaluate a possible protective effect. The results showed that SL was cytotoxic at concentrations above 32μg/mL by the colony forming assay. For apoptosis and necrosis assay, the concentration of 64μg/mL of SL showed statistically significant increase in cell death by apoptosis and necrosis, while the concentrations of 128 and 256μg/mL of SL demonstrated statistically significant increase in cell death by necrosis, compared with the control group. Analysis of cell viability by Trypan blue exclusion indicated >96% viability for treatments with concentrations up to 32μg/mL of SL. No significant differences in MI were observed between cultures treated with different concentrations of SL (4, 8, 16 and 32μg/mL) alone or in combination with MMS and the negative control, indicating that these treatments were not cytotoxic. The comet and chromosomal aberrations assays revealed that SL does not display genotoxic activity. Moreover, the different concentrations of SL showed protective effect against both genomic and chromosomal damages induced by MMS.

Solanum lycocarpum(Solanaceae) is native to the Brazilian Cerrado. Fruits of this species contain the glycoalkaloids solasonine (SN) and solamargine (SM), which display antiparasitic and anticancer properties. A method has been developed for the extraction and HPLC-UV analysis of the SN and SM in different parts ofS. lycocarpum, mainly comprising ripe and unripe fruits, leaf, and stem. This analytical method was validated and gave good detection response with linearity over a dynamic range of 0.77–1000.00 μg mL−1and recovery in the range of 80.92–91.71%, allowing a reliable quantitation of the target compounds. Unripe fruits displayed higher concentrations of glycoalkaloids (1.04% ± 0.01 of SN and 0.69% ± 0.00 of SM) than the ripe fruits (0.83% ± 0.02 of SN and 0.60% ± 0.01 of SM). Quantitation of glycoalkaloids in the alkaloidic extract gave 45.09% ± 1.14 of SN and 44.37% ± 0.60 of SM, respectively.