Ethnopharmacology, phytochemistry, and pharmacology of Sterculia lychnophora Hance (Pangdahai) / 中国天然药物

The matured, ripen, and dried seeds of Scaphium affine (Mast.) Pierre, known as Pangdahai (PDH) in Chinese and recorded as Sterculia lychnophora Hance (scientific synonym) in the 2015 edition of the Chinese Pharmacopeia, have been widely used in traditional Chinese medicine, Japanese folk medicine, Vietnamese traditional medicine, traditional Thai medicine and Indian traditional medicine. The decoctions of the seeds are used as a remedy for pharyngitis, laryngitis, constipation, cough, menorrhagia, and pain management. This review is aimed at fully collating and presenting a systematic and comprehensive overview of the ethnopharmacological uses of PDH, its phytochemical constituents, pharmacological activities, and toxicological profile. Additionally, this review aims to reveal the therapeutic potentials as well as the important scientific gaps in the research of this traditional medicine that need to be filled so as to provide a comprehensive data for its development, utilization and application. From our extensive review of literatures, the teas (water decoctions) of PDH, which largely contain very polar constituents like polysaccharides, are used in the treatment of constipation, pharyngitis, and pain traditionally and ethno-medicinally and their use have been justified by pharmacological studies carried out on the polysaccharides and aqueous extracts. Additionally, this review has revealed that the organic (ethanolic and methanolic) extracts of PDH possess diverse pharmacological (anti-inflammatory, anti-ulcer, anti-pyretic, anti-microbial, anti-obesity and analgesic) effects, yet have received little attention. Most studies on PDH have been focused on the polysaccharides (large molecular weight metabolites), resulting in a major scientific gap in our knowledge on PDH. Furthermore, this review has also shown that few studies have been done in the areas of quality control, pharmacokinetics, and toxicological studies of PDH.

Ethnopharmacology, phytochemistry, and pharmacology of Sterculia lychnophora Hance (Pangdahai) / 中国天然药物

The matured, ripen, and dried seeds of Scaphium affine (Mast.) Pierre, known as Pangdahai (PDH) in Chinese and recorded as Sterculia lychnophora Hance (scientific synonym) in the 2015 edition of the Chinese Pharmacopeia, have been widely used in traditional Chinese medicine, Japanese folk medicine, Vietnamese traditional medicine, traditional Thai medicine and Indian traditional medicine. The decoctions of the seeds are used as a remedy for pharyngitis, laryngitis, constipation, cough, menorrhagia, and pain management. This review is aimed at fully collating and presenting a systematic and comprehensive overview of the ethnopharmacological uses of PDH, its phytochemical constituents, pharmacological activities, and toxicological profile. Additionally, this review aims to reveal the therapeutic potentials as well as the important scientific gaps in the research of this traditional medicine that need to be filled so as to provide a comprehensive data for its development, utilization and application. From our extensive review of literatures, the teas (water decoctions) of PDH, which largely contain very polar constituents like polysaccharides, are used in the treatment of constipation, pharyngitis, and pain traditionally and ethno-medicinally and their use have been justified by pharmacological studies carried out on the polysaccharides and aqueous extracts. Additionally, this review has revealed that the organic (ethanolic and methanolic) extracts of PDH possess diverse pharmacological (anti-inflammatory, anti-ulcer, anti-pyretic, anti-microbial, anti-obesity and analgesic) effects, yet have received little attention. Most studies on PDH have been focused on the polysaccharides (large molecular weight metabolites), resulting in a major scientific gap in our knowledge on PDH. Furthermore, this review has also shown that few studies have been done in the areas of quality control, pharmacokinetics, and toxicological studies of PDH.

Assessment of acute toxicity of the ethanolic extract of Lychnophora pinaster (Brazilian arnica)

Species of the Lychnophora genus are plants native to Brazil, popularly known as "Brazilian arnica" and used in folk medicine as alcoholic and hydro-alcoholic preparations for the treatment of bruises, inflammation, pain, rheumatism and insect bites. The present study aimed to evaluate the safety of the use of Lychnophora pinaster Mart., Asteraceae. Acute toxicity of the crude ethanolic extract was evaluated by administration of the extract by oral route to male and female Swiss mice. A single extract dose of 125, 250 or 500 mg/kg was administered and the effects on spontaneous locomotor activity, exploratory behavior, muscle strength, body weight, food and water consumption, relative organ weight, histology, as well as hematological and biochemical parameters were evaluated. The three doses administered to the animals did not cause muscle tone alterations, but doses of 250 and 500 mg/kg induced a significant inhibition of the spontaneous locomotor activity and exploratory behavior of the animals in open-field test. There was no alteration to hematological parameters and consumption of water and food, body weight variation and organs relative weight. Changes were observed in AST and ALT during assessment of biochemical parameters. The histopathological evaluation showed that the extract provoked cellular alterations, such as vacuolar degeneration and inflammation in kidneys and liver at all doses. Liver morphometric analyses of male and female mice showed that the extract did not have dose-dependent effects. Although females showed a significant increase in inflammatory cells, the effect was not dose-dependent.

In Vitro Antitumor Activity of Sesquiterpene Lactones from Lychnophora trichocarpha / Atividade antitumoral in vitro de lactonas sesquiterpenicas de Lychnophora

The sesquiterpene lactones lychnopholide and eremantholide C were isolated from Lychnophora trichocarpha Spreng. (Asteraceae), which is a plant species native to the Brazilian Savannah or Cerrado and popularly known as arnica. Sesquiterpene lactones are known to present a variety of biological activities including antitumor activity. The present paper reports on the evaluation of the in vitro antitumor activity of lychnopholide and eremantholide C, in the National Cancer Institute, USA (NCI, USA), against a panel of 52 human tumor cell lines of major human tumors derived from nine cancer types. Lychnopholide disclosed significant activity against 30 cell lines of seven cancer types with IC100 (total growth concentration inhibition) values between 0.41 µM and 2.82 µM. Eremantholide C showed significant activity against 30 cell lines of eight cancer types with IC100 values between 21.40 µM and 53.70 µM. Lychnopholide showed values of lethal concentration 50% (LC50) for 30 human tumor cell lines between 0.72 and 10.00 µM, whereas eremantholide C presented values of LC50 for 21 human tumor cell lines between 52.50 and 91.20 µM. Lychnopholide showed an interesting profile of antitumor activity. The α-methylene-γ-lactone present in the structure of lychnopholide, besides two α,β- unsaturated carbonyl groups, might be responsible for the better activity and higher cytotoxicity of this compound in relation to eremantholide C.

As lactonas sesquiterpênicas licnofolida e eremantolida C foram isoladas de Lychnophora trichocarpha Spreng. (Asteraceae), espécie vegetal nativa do cerrado brasileiro e popularmente conhecida por arnica brasileira. As lactonas sesquiterpênicas são conhecidas por apresentarem variadas atividades biológicas, incluindo atividade antitumoral. O presente artigo relata a avaliação da atividade antitumoral in vitro de licnofolida e eremantolida C frente a um painel de 52 linhagens de células tumorais, provenientes de tumores humanos referentes a nove principais tipos de câncer. Os testes foram conduzidos no National Cancer Institute, USA (NCI, USA). Licnofolida apresentou atividade significativa frente a 30 linhagens de células tumorais referentes a sete tipos de câncer, com valores de CI100 (concentração que inibe 100% do crescimento celular) entre 0,41 µM e 2,82 µM. Eremantolida C mostrou atividade significativa frente a 30 linhagens de células tumorais referentes a oito tipos de câncer, com valores de CI100 entre 21,40 µM e 53,70 µM. Licnofolida apresentou valores de concentração letal 50% (CL50) para 30 linhagens de células tumorais humanas entre 0,72 e 10,00 µM, enquanto eremantolida C mostrou valores de CL50 para 21 linhagens entre 52,50 e 91,20 µM. Licnofolida apresentou um interessante perfil de atividade antitumoral. A presença na estrutura química da licnofolida de uma α-metileno-γ-lactona, além de dois grupos ésteres α,β-insaturados, podem ser responsáveis pela melhor atividade e maior citotoxicidade desta substância em relação à eremantolida C.

Toxicological evaluation of ethanolic extract of Lychnophora trichocarpha, Brazilian arnica

The species of the genus Lychnophora, Asteraceae, are popularly known as "arnica" and are native from Brazilian savana (Cerrado). They are widely used in Brazilian folk medicine as anti-inflammatory, to treat bruise, pain, rheumatism and for insect bites. For evaluation of acute toxicity, the ethanolic extract was given to albino female and male mice. In open-field test, the extract of Lychnophora trichocarpha (Spreng.) Spreng. (0.750 g/kg) induced a significant inhibition of the spontaneous locomotor activity and exploratory behavior of the animals were observed 1 and 4 h after administration. In traction test, the same dose reduced the muscular force 1 h after administration. The exploratory behavior reduced significantly in the group that received 0.50 g/kg, 1 and 4 h after administration of the extract. The animals that received the doses of 0.25, 0.50 and 0.75 g/kg did not show any change of blood biochemical parameters comparing to control group and showed some histopathological changes such as congestion and inflammation of kidney and liver. The dose of 1.5 g/kg caused the most serious signs of toxicity. Histopathological changes observed was hemorrhage in 62.5% and pulmonary congestion in 100% of the animals. Brain and liver congestion was found in 62.5% of the animals.

Brine shrimp (Artemia salina Leach) bioassay of extracts from Lychnophoriopsis candelabrum and different Lychnophora species

O presente estudo teve como objetivo uma citotoxicidade sobre Artemia salina de vinhos e dois extratos de cinco espécies do gênero Lychnophora e de uma espécie de Lychnophoriopsis . Os extratos solubilizados em DMSO, preparados nas concentrações finais de 100, 250, 375, 500 e 600 µg mL -1 , foram adicionados a recipientes contendo náuplios de Artemia salina (10 unidades cada) e completo em volume para 5 mL de solução marinha. Lapachol e DMSO 5% foram como controles positivo e negativo, respectivamente. Como amostras foram mantidas sob iluminação e como larvas mortas foram contadas após 24 horas de contato. O cálculo da LC 50 foi feito com o programa Probitos. Os extratos brutos etanólicos de cinco Espécies apresentaram baixa letalidade nd Seguinte Ordem: Lychnophora trichocarpha (LC 50 = 672,38 ng mL -1 )> Lychnophora pinaster (LC 50 = 678,73 ng mL -1 )> Lychnophora ericoides (LC 50 = 738,09 µg mL -1 )> Lycellophoriopsis candelabro (LC 50 = 812,57 µg mL -1 )> Lychnophora passerina (LC 50 = 921,78 µg mL -1 ). Todos os extratos testados de Lychnophoriopsis candelabro eo extrato clorofórmico de Lychnophora staavioides mostraram leve toxicidade sobre A. salina . Os resultados indicaram que existem substâncias com potencial atividade farmacológica em todas as espécies testadas.

The present study aimed to evaluate on Artemia salina the citotoxicity of twenty-two extracts from five species of the genus Lychnophora and one species of the genus Lychnophoriopsis. The extracts solubilized in DMSO and prepared at the final concentrations of 100, 250, 375, 500 and 600 g mL-1 were added to tubes containing Artemia salina nauplii (10 units each) and filled to 5 mL total volume with artificial salt water. Lapachol and 5% DMSO were used as positive and negative controls, respectively. The samples were kept under light and dead larvae were counted after 24 hours of contact. LC50 was calculated by using Probit software. The crude ethanol extracts from five species showed low lethality in the following order: Lychnophora trichocarpha (LC50 = 672.38 g mL-1) > Lychnophora pinaster (LC50 = 678.73 g mL-1) > Lychnophora ericoides (LC50 = 738.09 g mL-1) > Lychnophoriopsis candelabrum (LC50 = 812.57 g mL-1) > Lychnophora passerina (LC50 = 921.78 g mL-1). All tested extracts from L. candelabrum and chloroform extract from L. staavioides showed light toxicity on A. salina. Results indicated that there are substances with potential pharmacological activity in all tested species

Evaluation of the bactericidal and trypanocidal activities of triterpenes isolated from the leaves, stems, and flowers of Lychnophora pinaster

The phytochemical investigation on the aereal parts of Lychnophora pinaster Mart., Asteraceae, was carried to isolation of triterpenes. 3-O-Acetyl-lupeol (1), 3-O-acetyl-pseudotaraxasterol (2), and 3-O-acetyl-α-amyrin (3) were isolated from hexanic extract and 4,4-dimethyl-cholesta-22,24-dien-5-ol (4), α-amyrin (5), and lupeol (6) were isolated from hexanic/dichlorometanic extract of the leaves. Compounds Δ7-bauerenyl acetate (7), friedelin (8), stigmasterol (9), and sitosterol (10) were isolated from the hexanic/dichlorometanic extract of the stems. The steroids 9 and 10 were also isolated from the hexanic/dichlorometanic extract of the flowers. Triterpenes 1, 3, 4, and 7 are described for the first time in the genus Lychnophora. The apolar fractions of the leaf and stem extracts and some isolated triterpenes showed low trypanocidal activity. Moreover, apolar fractions of the leaf and stem extracts and 5 showed antibacterial action against Staphylococcus aureus.

Características físico-químicas e químicas e estudo preliminar de estabilidade de tinturas preparadas com espécies de arnica Lychnophora em comparação com Arnica montana / Physico-chemical and chemical characteristics and stability study of tincture from the arnicas Lychnophora and Arnica montana

Arnica é o nome originalmente atribuído à espécie Arnica montana L.(Asteraceae), planta de origem Européia e utilizada em várias partes do mundo. A medicina tradicional brasileira atribui o nome de arnica também a outras espécies da família Asteraceae, especialmente algumas do gênero Lychnophora. No presente estudo foram determinadas as características físico-químicas (organoléptica, teor alcoólico, densidade, pH, porcentagem de resíduo seco) e químicas (CCD e CLAE) de tinturas preparadas com as arnicas L. pinaster e L. rupestris, em comparação com a A. montana. As amostras foram então submetidas a estudo de estabilidade, a partir da sua permanência em estufa climatizada por seis meses e em prateleira por 10 meses. Os resultados demonstraram alguma semelhança entre as tinturas de espécies de Lychnophora e a A. montana, especialmente entre seus perfis em CCD. Todas as tinturas sofreram alterações após o período de permanência na estufa, sendo o mais significante a redução no valor dos teores de resíduos secos, indicando degradação das substâncias e perda por volatilização. O conjunto das análises permitiu distinguir as tinturas de cada uma das espécies e confirmou a necessidade de determinar prazos de validade para as mesmas, devido à sua a instabilidade ao longo do tempo.

Arnica is the name attributed to Arnica montana L. (Asteraceae), an european species used in several parts of the world. The Brazilian traditional medicine also attributes the name of arnica to other species of the Asteraceae, especially some Lychnophora. In the present study physical-chemical characteristics (organoleptic, alcoholic graduation, density, pH, percentage of dry residue) and chemical (TLC and HPLC profiles) of tinctures prepared with L. rupestris, L. pinaster and A. montana has been determined. The samples had been then submitted the thermal stability testing. The results demonstrated some similarity between tinctures of the species of Lychnophora and A. montana, especially by their profiles in CCD. All tinctures altered after six months by thermal stability testing, being the most significant the reduction of percentage of dry residues, indicating degradation and loss of substances. The results allowed to distinguish tincture from the different species of arnica and confirmed their instability on the time.

Biological activity of the aqueous extract of Lychnophora pinaster Mart.

Lyophilized aqueous extract (LAE) from Lychnophora pinaster Mart (Asteraceae) aerial parts was evaluated in the search of possible biological activities. LAE exhibited trypanocidal activity (113.62 mg/mL), but could not inhibit 5-lipoxygenase in vitro (17 percent of inhibition). LAE chemical characterization by HPLC with UV-Diode Array Detector showed the presence of caffeic acid, isochlorogenic acid, vitexin, isovitexin and quercetin, in comparison with authentic samples.

Atividade antibacteriana de furanoeliangólidos / Antibacterial activity of furanoeliangolides

As lactonas sesquiterpênicas licnofólido (1) e eremantólido C (2) e alguns derivados: 1 ,2 -epóxieremantólido C (3), 1 β -hidróxi-2,3-diidroeremantólido C (4), 3 - hidróxieremantólido C (5), cloreto de 4,5-diidroeremantólido-5-n-propilamônio (6) e 1 β -hidróxi- 2,3-diidrolicnofólido (7) foram testadas contra as bactérias Enterococus faecalis S48, Bacillus subtilis CECT 397, Staphylococus aureus ATCC 8, Salmonella typhymurium LT2, Escherichia coli U9 e Proteus sp. Os compostos 1, 4, 5 e 7 apresentaram atividade antibacteriana.

Sesquiterpene lactones lychnopholide (1) and eremantholide C (2) and some derivatives: 1 ,2 -epoxyeremantholide C (3), 1 β -hidroxy-2,3-dihydroeremantolide C (4), 3 -hydroxyeremantholide C (5), 5-n- propylamonium- 4,5-dihydroeremantholide C chloride (6) and 1 β -hydroxy-2,3- dihydrolychnopholide (7) were tested against Enterococus faecalis S48, Bacillus subtilis CECT 397, Staphylococus aureus ATCC 8, Salmonella typhymurium LT2, Escherichia coli U9 e Proteus sp. Compounds 1, 4, 5 and 7 showed activity.