ABSTRACT Purpose: To evaluate the modulatory properties of Calendula officinalis L. (Asteraceae) (C. officinalis) extract on cafeteria diet-fed rats. Methods: A cafeteria diet was administered ad libitum for 45 days to induce dyslipidemia. Then, the rats were treated with the formulations containing C. officinalis in the doses of 50, 100, and 150 mg/kg or only with the vehicle formulation; the control group received a commercial ration. Results: The cafeteria diet decreased glutathione S-transferase activity and high-density lipoprotein plasmatic levels and damaged the hepatic architecture. The C. officinalis extract was able to reduce lipid infiltration in liver tissue and to modulate oxidative stress and lipid profile markers. Conclusions: The correlations between the variables suggest a pathological connection between oxidative stress markers and serum lipid profile.

Introdução: A Erva-baleeira (Varronia curassavica Jacq.) é uma planta medicinal e aromática originária do Brasil. A espécie pertence à família Boraginaceae e tem grande relevância econômica devido ao óleo essencial presente em suas folhas. A planta possui importantes ações, como atividade contra o mosquito Aedes aegypti, no entanto, seu principal efeito é anti-inflamatório. O objetivo desta revisão bibliográfica foi elencar as principais características e efeitos terapêuticos da Varronia curassavica Jacq. Método: O trabalho foi realizado a partir da busca online, entre junho e agosto de 2020, de artigos científicos publicados em inglês e português entre 2000 e 2020 nas bases de dados de saúde pública “PubMed”, “LILACS” e “SciELO”, onde foram usados os descritores: Cordia; Plantas Medicinais; Fitoterapia. Resultados: Existem registros do uso da erva-baleeira por comunidades tradicionais para tratamento de inflamações, mialgia, artrites, reumatismos, úlceras estomacais e como tônico para contusões. Ela também tem uso citado como cicatrizante em feridas e regiões inflamadas. Popularmente, o uso é feito a partir das folhas em forma de infusão, decocção, pomadas, tinturas, extratos hidroalcoólicos e cataplasmas. Conclusão: A Erva-baleeira é uma planta medicinal com grande emprego fitoterápico. Seu uso advém principalmente de seu importante efeito anti-inflamatório. Novos estudos sobre as propriedades terapêuticas da Erva-baleeira são necessários, a fim de explorar suas potenciais aplicabilidades clínicas e corroborar cientificamente o uso da erva já popularmente consagrada.

BACKGROUND:There are over 500 species in the Passiflora genus, and while some of them are very well known in folk medicine for their anxiolytic effects, very little is known for the other genus representants, which could also present medicinal effects.OBJECTIVE:In this study, we performed an interspecific pharmacological comparison of five investigated Passiflora species, all native to Brazil, namely P. bahiensis, P. coccinea, P. quadrangularis, P. sidaefolia, and P. vitifolia.METHODS:Extracts were administered to mice before behavioral testing, including a general pharmacological screening and anxiolytic-like effect investigation.RESULTS:Three of the species (P. coccinea, P. quadrangularis, and P. sidaefolia) induced a decrease in locomotor activity of mice; P. coccinea also reduced the latency to sleep. Importantly, none of the species interfered with motor coordination. Oral administration evoked no severe signs of toxicity, even at higher doses. Regarding the anxiolytic-like profile, P. sidaefolia reduced the anxious-like behavior in the Holeboard test in a similar way to the positive control, Passiflora incarnata, while not affecting total motricity.CONCLUSION:These results indicated that P. coccinea, P. quadrangularis, and P. sidaefolia reduced the general activity of mice and conferred a calmative/sedative potential to these three species, which must be further elucidated by future investigations.

Ethnopharmacological relevance: Ayahuasca, a psychoactive beverage prepared from Banisteriopsis caapi and Psychotria viridis, is originally used by Amazon-based indigenous and mestizo groups for medicinal and ritualistic purposes. Nowadays, ayahuasca is used in religious and shamanic contexts worldwide, and preliminary evidence from preclinical and observational studies suggests therapeutic effects of ayahuasca for the treatment of sub-stance (including alcohol) use disorders. Aim of the study: To investigate the initial pharmacological profile of ayahuasca and its effects on ethanol rewarding effect using the conditioned place preference (CPP) paradigm in mice. Materials and methods: Ayahuasca beverage was prepared using extracts of B. caapi and P. viridis, and the con-centration of active compounds was assessed through high performance liquid chromatography (HPLC). The following behavioral tests were performed after ayahuasca administration: general pharmacological screening (13, 130, or 1300 mg/kg - intraperitoneally - i.p., and 65, 130, 1300, or 2600 mg/kg - via oral - v.o.); acute toxicity test with elevated doses (2600 mg/kg - i.p., and 5000 mg/kg - v.o.); motor activity, motor coordination, and hexobarbital-induced sleeping time potentiation (250, 500, or 750 mg/kg ayahuasca or vehicle - v.o.). For the CPP test, the animals received ayahuasca (500 mg/kg - v.o.) prior to ethanol (1.8 g/kg - i.p.) or vehicle (control group - i.p.) during conditioning sessions. Results: Ayahuasca treatment presented no significant effect on motor activity, motor coordination, hexobarbital-induced sleeping latency or total sleeping time, and did not evoke signs of severe acute toxicity at elevated oral doses. Ayahuasca pre-treatment successfully inhibited the ethanol-induced CPP and induced CPP when admin-istered alone. Conclusions: Our results indicate that ayahuasca presents a low-risk acute toxicological profile when administered orally, and presents potential pharmacological properties that could contribute to the treatment of alcohol use disorders.

Hibiscus sabdariffa extract (HSE) and Syzygium cumini extract (SCE) have been used in traditional medicine due to their hypoglycemic, antidiabetic, anti-obesity and antioxidant activities. This study aimed to evaluate the anti-obesity effects of these extracts, as well as to evaluate their toxicities. The phytochemical profiles were obtained by HPLC-DAD-ESI-MS/MS analyses. Pharmacological screening, motor activity, motor coordination and acute toxicity were evaluated by administering HSE or SCE (oral or intraperitoneal routes) at different doses to mice. The anti-obesity effects were examined by assessing the decrease in food intake and body weight loss in Wistar albino rats and by gastrointestinal transit in Swiss albino mice. Sibutramine was used as the positive control. Both extracts showed no toxic effects. At the end of 7 days of treatment, we observed that SCE and HSE reduced the weight gain and food intake of the treated rats in relation to the controls. Sub-chronic treatment revealed that HSE, SCE and sibutramine had the best effect 7 and 14 days after starting treatment. After 28 days, the SCE group showed less weight gain and reduced food consumption compared to the HSE group and controls. In addition, intestinal transit was increased in the HSE group, which is probably due to the high fiber content of the extract and may explain its anti-obesity properties. Myricetin glycosides were found in high levels in SCE and low levels in HSE, which may be the main compounds associated with the anti-obesity effect found in SCE. It is not possible to suggest an effective dose without conducting a preclinical toxicology study. We recommend clinical studies that evaluate the efficacy and safety, as well as the effect of discontinuing the extracts.

One of the Brazilians medicinal plants most cited in ethnopharmacological surveys for the treatment of ulcers and gastric diseases was evaluated for its efficacy and toxicity. Maytenus ilicifolia leaf extract (MIE) was acutely and chronically (180 days) administered to rats, mice, and dogs. Acute tests were antiulcer effect and toxicological trials (observational pharmacological screening, LD50, motor coordination, sleeping time and motor activity). Chronic tests were the following: weight gain/loss and behavioral parameters in rats and mice; estrus cycle, effects on fertility, and teratogenic studies in rats and mutagenic features in mice, in addition to the Ames and micronucleus test. The following parameters were assessed in dogs: weight gain/loss, general physical conditions, water/food consumption, and anatomopathological examination of the organs subsequent to the 180-day treatment. The results showed a clear antiulcer activity for MIE from 70 mg/kg and an absence of toxicological effects in the three animal species, even if given in high doses or over a long period. The present results confirm the antiulcer property and absence of toxicological effects in three animal species of MIE, which is in line with its current popular medicinal use. Copyright © 2017 John Wiley & Sons, Ltd.

We report here our investigations on plants belonging to the botanical genus Aspidosperma (Apocynaceae) that are used to treat malaria and/or fevers in Brazil, aiming to prepare standardized alkaloid extracts for phytomedicines development. Ethanol and alkaloid extracts of A. parvifolium and A. subincanum barks were prepared and their in vitro antiplasmodial activity was evaluated against Plasmodium falciparum (W2 strain) by the pLDH method. Bioguided fractionation of the active alkaloid extracts was undertaken. A study on antiplasmodial activity versus alkaloids content variation from three A. subincanum specimens that were collected in different regions was carried on by HPLC-UV. Ethanol and alkaloid extracts from A. parvifolium and A. subincanum were evaluated in toxicological studies in male and female Swiss mice and male Wistar rats (n = 10); a control group was included in the experiments. At the end of treatment, animals were sacrificed, hematology and serum biochemical analyses were performed. Fractionation of alkaloid extracts from A. parvifolium and A. subincanum guided by in vitro assays against P. falciparum (W2 strain) led to the isolation of the indole alkaloids uleine (Oliveira et al., 2010) and N-demethyluleine. HPLC-UV and LC-UV-MS/ESI analyses of the extracts disclosed uleine as the major constituent, its content reaching 70.7% in the alkaloid extract from A. subincanum (ASALB) which was more potent than uleine and N-demethyluleine themselves in the in vitro assays, as can be inferred from the selectivity indexes in relation to HepG2 cells (SI = CC50/IC50) of ASALB (100), uleine (44) and N-demethyluleine (21). Moreover, a significative variation on the contents of these two alkaloids was observed for the same plant species when collected in different regions (Paula, 2014). Both ethanol and alkaloid extracts from A. parvifolium bark were relatively safe, producing minor changes in the parameters evaluated, especially in smaller doses, thus making feasible their future use in phase I clinical trials. On the other hand, high toxicity of both extracts from A. subincanum bark was observed in doses >200 mg/kg. The present results point to the necessity of rigorous investigation of traditional antimalarial plants including in vitro studies for identification of active natural products, standardization of extracts to be submitted to pre-clinical toxicological studies and controlled clinical trials. Our results disclose that efficient and safe phytomedicines might be developed from standardized crude or semi-purified extracts of Aspidosperma species containing the active chemical entities.

Tilia species, among which is Tilia cordata Mill. (Tiliaceae), have been used in folk medicine as anxiolytic. The hydroethanolic extract was analyzed by using liquid chromatography with mass spectrometry HPLC-DAD-ESI-MS/MS in negative ion mode, and its chemical composition was compared to flavonoids reported as anxiolytics. The major flavonoids found were: quercetin-3,7-di-O-rhamnoside, kaempferol-3,7-di-O-rhamnoside and kaempferol 3-O-(6"-p-coumaroyl glucoside) or tiliroside. The anxiolytic activity of the genus Tilia has been attributed to the presence of quercetin and kaempferol derivatives, while the anxiolytic activity of T. americana var. Mexicana was attributed to tiliroside, which was also found among the major constituents of this species.

Periandra dulcis Mart. ex Benth. Fabaceae (Syn.: P. mediterranea (Vell.) Taub.) is native to the northern and middle parts of Brazil. In Brazilian ethnomedicine, their roots are used as anti inflammatory, expectorant, diuretic and laxative. An HPLC-ESI-MS/MS system was employed to provide a rapid method to make a tentative characterization of the compounds found in the hydroethanolic extract from P. dulcis roots. The structures of sixteen compounds found in this hydroethanolic extract were suggested mainly by MS data conjugated with the UVDAD spectra, reference compounds and available mass spectra data in literature. Saponin derivatives of hederagenin and soyasapogenol E, such as hederagenin-3-O-rhamnosyl glucosyl glucuronide, soyasapogenol E-3-O-rhamnosyl glucosyl glucuronide and periandrin isomers were found as the main constituents, with a minor content of flavonols quercetin and myricetin glycosides derivatives and hydrolysable tannins, such as dihexahydroxydiphenoyl galloyl glucoside and trisgalloyl hexahydroxydiphenoyl glucose. To the best of our knowledge, with exception of periandrins found in the roots, nothing has been published about the chemical composition of P. dulcis..

The present study aimed to assess the preclinical toxicity of two plants commonly used to treat “stomach ailments” in Brazil: Schinus terebinthifolius Raddi (S) and Myracrodruon urundeuva Allemão (M). In male rats, chronic treatment (83 days) with both pepper trees (17.6 and 13.8 mg/kg, S and M, respectively) has been shown to decrease hematocrit. However, a reduction in the number of red blood cells and hemoglobin was only seen following administration of S. terebinthifolius. None of the plants caused anatomopathological alterations following chronic treatment, and mating ability and fertility were not affected. Both pepper trees showed moderate toxicity following acute and chronic treatment by gavage, particularly S. terebinthifolius. Moreover, bone malformations were induced in fetuses, and a slight delay in recovery time of the postural reflex was observed in pups from female animals treated (18 days) with S. terebinthifolius. Given these results, a better assessment of the risks and benefits of the internal use of these plants is necessary, especially when used by women of childbearing age. Copyright © 2012 John Wiley & Sons, Ltd.

The diversified genus Passiflora is well distributed all over Brazil, and many species have been long used as medicinal plants, mainly against anxiety disturbances. This effect has been attributed to its rich flavonoid composition. Flavonoids' main class, flavonoid glycosides, has presented central action, particularly as sedative-hypnotic, anxiolytic and analgesic. The objective of the present study was to make a phytochemical screening of five little studied Passiflora species, in order to evaluate their phenolic composition. For this aim, HPLC-DAD-ESI-MS/MS was used. After the preparation of the hydroalcoholic extracts, each species was evaluated by direct injection electrospray ionization (ESI) and tandem mass spectrometry. Although belonging to the same genus, the composition of each species presented particularities; this justifies the importance of studies aiming for the phenolic composition of different Passiflora species. Flavones C-glycosides were detected in all extracts, and are found as the main constituents in P. vitifolia, P. coccinea, P. bahiensis and P. sidifolia. In this last one, flavone-6,8-di-C-glycoside, apigenin-6-C-rhamnosyl-8-C-arabinoside are present in high content. Cyclopassiflosides were found in high content together with cyanogenic glycosides in P. quadrangularis, while in P. coccinea, besides flavones-C-glycosides were also found procyanidins.