Phytochemical Estimation and Therapeutic Amelioration of Aesculus hippocastanum L. Seeds Ethanolic Extract in Gastric Ulcer in Rats Possibly by Inhibiting Prostaglandin Synthesis / 中国结合医学杂志

OBJECTIVE@#To quantify phytochemicals using liquid chromatography and mass spectroscopy (LCMS) analysis and explore the therapeutic effect of Aesculus hippocastanum L. (AH) seeds ethanolic extract against gastric ulcers in rats.@*METHODS@#Preliminary phytochemical testing and LCMS analysis were performed according to standard methods. For treatment, the animals were divided into 7 groups including normal control, ulcer control, self-healing, AH seeds low and high doses, ranitidine and per se groups. Rats were orally administered with 10 mg/kg of indomethacin, excluding the normal control group (which received 1% carboxy methyl cellulose) and the per se group (received 200 mg/kg AH seeds extract). The test group rats were then given 2 doses of AH seeds extract (100 and 200 mg/kg, respectively), while the standard group was given ranitidine (50 mg/kg). On the 11th day, rats in all groups were sacrificed, and their stomach was isolated to calculate the ulcer index, and other parameters such as blood prostaglandin (PGE2), tissue superoxide dismutase (SOD), catalase (CAT), malonyldialdehyde (MDA), and glutathione (GSH). All isolated stomach tissues were analyzed for histopathological findings.@*RESULTS@#The phytochemical examination shows that the AH seeds contain alkaloids, flavonoids, saponins, phenolic components, and glycosides. LCMS analysis confirms the presence of quercetin and rutin. The AH seeds extract showed significant improvement in gastric mucosa conditions after indomethacin-induced gastric lesions (P<0.01). Further marked improvement in blood PGE2 and antioxidant enzymes, SOD, CAT, MDA and GSH, were observed compared with self-healing and untreated ulcer-induced groups (P<0.01). Histopathology results confirmed that AH seeds extract improved the mucosal layer and gastric epithelial membrane in treated groups compared to untreated ulcer-induced groups.@*CONCLUSIONS@#LCMS report confirms the presence of quercetin and rutin in AH seeds ethanolic extract. The therapeutic effect of AH seeds extract against indomethacin-induced ulcer in rat model indicated the regenerated membrane integrity, with improved cellular functions and mucus thickness. Further, improved antioxidant enzyme level would help to reduce PGE2 biosynthesis.

Produtos fitoterápicos manipulados em um laboratório de manipulação no Estado do Paraná / Phytotherapeutic products handled in a handling laboratory in the State of Paraná / Productos fitoterapéuticos manipulados en un laboratorio de manipulación en el Estado de Paraná

As plantas medicinais foram os primeiros recursos terapêuticos obtidos pelos povos e há registros do seu uso em todos os momentos da História, por grande parte das civilizações. No Brasil, o uso das plantas medicinais é resultado dos conhecimentos de três populações: indígena, europeia e africana. O presente trabalho tem como objetivo caracterizar a manipulação mensal de um laboratório de fitoterápicos na cidade de Francisco Beltrão, Paraná. Os dados que foram coletados para a presente pesquisa são: número de cápsulas manipuladas mensalmente para cada um dos fitoterápicos, os quais serão obtidos a partir dos relatórios de manipulação de fitoterápicos mensais no ano de 2021 e individuais de cada unidade de saúde, fornecidos pela Secretaria de Saúde. Não havendo acesso a informações de pacientes e tampouco contato com eles. As informações dos relatórios foram tabuladas em planilha a fim de se estabelecer os três principais fitoterápicos manipulados no período preestabelecido. Trata-se de um estudo de campo, exploratório, documental e retrospectivo. Observamos que a média de manipulação foi de 34.029 cápsulas por mês, os fitoterápicos mais manipulados no ano de 2021, foram: Passiflora incarnata (maracujá), Aesculus hippocastanum (castanha da índia) e Curcuma longa. Também foi possível notar que houve um aumento gradual de dispensações após a capacitação dos profissionais, ocorrida entre junho e setembro. Além disso, verificamos que há uma grande diferença na quantidade dispensada por cada farmácia municipal, possivelmente devido ao nível de conhecimento dos profissionais de saúde e se preferem ou não prescrever aos pacientes.

Medicinal plants were the first therapeutic resources obtained by people and there are records of their use at all times of history, by a large part of civilizations. In Brazil, the use of medicinal plants is a result of the knowledge of three populations: indigenous, European and African. The present work aims to characterize the monthly handling of a plant medicine laboratory in the city of Francisco Beltrão, Paraná. The data that were collected for this research are: number of capsules handled monthly for each one of the phytotherapics, which will be obtained from the reports of handling of monthly phytotherapics in the year 2021 and individual of each health unit, provided by the Secretariat of Health. There is no access to patient information and no contact with them. The information in the reports was tabulated into a spreadsheet in order to establish the three main phytotherapics handled in the pre-established period. This is an exploratory, documentary and retrospective field study. We observed that the average handling was 34,029 capsules per month, the most manipulated phytotherapics in the year 2021, were: Passiflora incarnata (passion fruit), Aesculus hippocastanum (chestnut from India) and Curcuma longa. It was also possible to note that there was a gradual increase in dispensations after the training of professionals, which took place between June and September. In addition, we note that there is a big difference in the amount dispensed by each municipal pharmacy, possibly due to the level of knowledge of health professionals and whether or not they prefer to prescribe to patients.

Las plantas médicas fueron los primeros recursos terapéuticos obtenidos por los pueblos y hay registros de su uso en todo momento de la historia, por una gran parte de las civilizaciones. En Brasil, el uso de plantas medicinales es el resultado del conocimiento de tres poblaciones: indígenas, europeos y africanos. El presente trabajo tiene como objetivo caracterizar la manipulación mensual de un laboratorio fitoterapéutico en la ciudad de Francisco Beltrão, Paraná. Los datos recogidos para esta investigación son: el número de cápsulas manejadas mensualmente para cada una de las fitoterapias, que se obtendrán de los informes mensuales de manipulación fitoterapéutica en el año 2021 y el individuo de cada unidad de salud, proporcionados por el Departamento de Salud. No hay acceso a la información del paciente ni contacto con ella. La información contenida en los informes se tabuló en una hoja de cálculo para establecer las tres principales fitoterapias manipuladas en el periodo predefinido. Se trata de un estudio de campo, exploratorio, documental y retrospectivo. Observamos que la manipulación media fue de 34.029 cápsulas al mes, las fitoterapias más manipuladas en 2021 fueron: Passiflora incarnata (fruto de la pasión), Aesculus hippocastanum (castaño indio) y Curcuma longa. También es posible señalar que se ha producido un aumento gradual de las dispensaciones después de la capacitación de profesionales, que se llevó a cabo entre junio y septiembre. Además, vemos que existe una enorme diferencia en la cantidad que proporciona cada farmacia municipal, posiblemente debido al nivel de conocimiento de los profesionales de la salud y si prefieren recetarla a los pacientes o no. PALABRAS CLAVE: Fitoterapias; Farmacias Municipales; Curcuma Longa; Passiflora Incarnata; Aesculus Hippocastanum.

The hepatoprotective effect of Aesculus hippocastanum seed extract against concanavalin A-induced acute liver injury in mice via inhibition of ROS and JNK pathway / 中国药理学通报

Aim To investigate the effect of Aesculus hippocastanum seed extract(AH) on concanavalin A (ConA)-induced acute liver injury in mice,and to ex-plore whether the mechanism was related to the inhibi-tory effect of AH on oxidative stress and c-Jun N-termi-nal kinase (JNK). Methods ConA(20 mg·kg-1) was administered via tail vein injecting to induce he-patic damage in mice. The groups of AH were given at 12.5,25,50 mg·kg-1by oral gavage separately for 20 days. The serum levels of AST,ALT,TP,and Alb were determined by automatic biochemical analyzer and the A/G ratio was calculated. TNF-α and IFN-γ levels were assayed by ELISA. The liver tissue was attained by HE and the histopathological changes were calculat-ed. The MDA, SOD, GSH contents of liver tissues were assayed by related kits. The activity of caspase-3 was detected by spectrophotometry. The expressions of cytochrome C and Bax, Bcl-2, p-JNK and p-Akt were detected by Western blot. Results The serum levels of ALT, AST, IFN-γ and TNF-α in AH groups were significantly lower than those in ConA-injured group, while the levels of TP,Alb and A/G were significantly higher. The SOD and GSH levels of liver tissues signif-icantly increased and MDA level decreased; liver his-topathological changes were consistent with those of the serological indicators, and AH treatment significantly reduced the pathological damage induced by ConA. In AH group,the expression of cytochrome C,caspase-3, Bax/Bcl-2 ratio and p-JNK markedly decreased, while the expression of p-Akt protein increased compared with ConA model group. Conclusion AH could sig-nificantly protect the ConA-induced acute liver injury in mice via inhibition of ROS and JNK pathway.

In vitro and in vivo trypanocidal action of aescin and aescin liposomes against Trypanosoma evansi in experimental mice

To verify the trypanocidal effectiveness of aescin and aescin liposomes against Trypanosoma evansi in vitro and in vivo. Methods: Aescin and aescin liposomes were used in vitro on trypomastigotes at different concentrations (0.5%, 1.0% and 2.0%) and exposure times (0, 1, 3, 6 and 9 h). In vivo tests were performed using mice as the experimental model. Trypanosome evansi infected mice were treated with aescin and aescin liposomes with doses of 60 and 100 mg/kg during 4 d. Results: The three concentrations tested in free form and nanoencapsulated showed trypanocidal activity in vitro, completely eliminating the parasites in small concentration after 6 h of assay. Animals treated with aescin (100 mg/kg) and aescin liposomes (100 mg/kg) showed increase in longevity, however without curative effect. Conclusions: Active compounds present in natural products, such as aescin, may potentiate the treatment of trypanosomosis when used in association with other trypanocidal drugs.

In vitro and in vivo trypanocidal action of aescin and aescin liposomes against Trypanosoma evansi in experimental mice

Objective: To verify the trypanocidal effectiveness of aescin and aescin liposomes against Trypanosoma evansi in vitro and in vivo. Methods: Aescin and aescin liposomes were used in vitro on trypomastigotes at different concentrations (0.5%, 1.0% and 2.0%) and exposure times (0, 1, 3, 6 and 9 h). In vivo tests were performed using mice as the experimental model. Trypanosome evansi infected mice were treated with aescin and aescin liposomes with doses of 60 and 100 mg/kg during 4 d. Results: The three concentrations tested in free form and nanoencapsulated showed trypanocidal activity in vitro, completely eliminating the parasites in small concentration after 6 h of assay. Animals treated with aescin (100 mg/kg) and aescin liposomes (100 mg/kg) showed increase in longevity, however without curative effect. Conclusions: Active compounds present in natural products, such as aescin, may potentiate the treatment of trypanosomosis when used in association with other trypanocidal drugs.

Determinação do teor de princípios ativos em matérias-primas vegetais / Determination of active principles in vegetable raw materials

Castanha-da-índia (Aesculus hippocastanum L.), hipérico (Hypericum perforatum L.), guaraná (Paullinia cupana H.B.K.) e ginkgo (Ginkgo biloba L.) fazem parte de formulações de medicamentos fitoterápicos muito comercializados no Brasil. Neste trabalho foi avaliada a qualidade de amostras de pós e extratos destas plantas. Para a determinação do teor de princípios ativos foram aplicados métodos farmacopéicos ou citados na literatura científica e os resultados demonstraram serem adequados para a análise destes produtos farmacêuticos. Verificou-se que 60 por cento das amostras analisadas de guaraná e ginkgo estavam em desacordo com as especificações farmacopéicas ou as declaradas pelos laudos dos fabricantes, em relação ao teor de princípios ativos. Além disso, 100 por cento e 20 por cento, respectivamente, das amostras de hipérico e de castanha-da-índia apresentaram teores abaixo das especificações. Os dados obtidos mostraram ser de grande importância e necessidade a implementação de técnicas quantitativas no controle de qualidade físico-químico de matérias-primas vegetais.

Pharmaceutical preparations containing Aesculus hippocastanum L., Hypericum perforatum L., Paullinia cupana H.B.K. and Ginkgo biloba L. have large market. In this work the quality of the powder or extracts of these plants were evaluated. Pharmacopoeia methods or those cited on cientific literature for quantification of active substances were employed and the data showed them to be adequate for these analyses. The analytical results demonstrated that 60 percent of the samples of P. cupana and G. biloba, and 100 percent and 20 percent, respectively of samples of H. perforatum and A. hippocastanum were not in agreement with the specifications. This analysis showed to be valuable for herbal medicines quality control.

Qualidade de amostras comerciais preparadas com Aesculus hippocastanum L. (castanha-da-Índia) / Quality of commercial samples of horse-chestnut (Aesculus hippocastanum)

As sementes de castanha-da-Índia (Aesculus hippocastanum L., Hippocastanaceae) são utilizadas na medicina tradicional em várias partes do mundo no tratamento de varizes. Muitos estudos, inclusive clínicos, comprovaram as atividades antiedematosa, anti-inflamatória e venotônica do extrato padronizado da planta. O componente ativo é uma mistura de saponinas, denominada aescina. Foram analisadas amostras de droga vegetal rasurada e em pó, extrato seco, cápsulas contendo pó vegetal e extrato e comprimidos de extrato de castanha-da-Índia adquiridas no mercado nacional. Verificou-se a autenticidade (caracterização organoléptica, macroscópica e microscópica), a pureza (determinação de matéria estranha, água e cinzas totais), a presença e o teor de aescina, além das condições de prescrição e dispensação desses medicamentos. As análises confirmaram a autenticidade e pureza de todas as amostras. A aescina foi detectada mas os teores foram muito variáveis, estando abaixo do especificado na bibliografia em quase todas as amostras. Apesar de ser utilizada eficazmente em outros países, a pesquisa demonstrou que os produtos disponíveis no comércio brasileiro encontram-se fora das especificações necessárias para a atividade farmacológica. Esse quadro revela a necessidade urgente de melhoria da manipulação de fitoterápicos, de forma a promover a utilização adequada desses medicamentos.

The seeds of horse-chestnut (Aesculus hippocastanum L., Hippocastanaceae) have been used in traditional medicine in several parts of the world to treat chronic venous insufficiency. Many experimental and clinical studies have demonstrated that A. hippocastanum extracts increase venous tonus. This activity is attributed to a mixture of saponins (aescin). In this study, samples of A. hippocastanum obtained from herbal shops, pharmacies and drug stores were analyzed and their authenticity (organoleptic properties, macroscopy and microscopy characterization), purity (determination of foreign matter, water and ashes) and content of aescin were determined. The analyses confirmed the authenticity and purity of all samples, however the content of aescin showed variation in all analysed sample and was out of the specification for each one. Although, A. hippocastanum has been widely used in other countries with proven efficacy, the results of the present study showed that the available Brazilian products do not meet the standarts for use as a therapeutic agent.