Overexposure to sunlight has harmful effects on the skin and can cause erythema and skin cancer. Photoprotective agents are important for preventing exposure to sunlight and are present in the composition of sunscreens. Globally, the use of filters based on natural products has gained interest in scientific studies; in addition to their sunscreen properties, these products demonstrate antioxidant, healing, and moisturizing activity. These favor adequate sun protection due to the wide spectrum of activities and are environmentally friendly. Plectranthus amboinicus (Lour.) Spreng., Lamiaceae, is used in traditional medicine to treat several conditions and is commonly known as "hortelã-da-folha-grossa" in Brazil. This species presents phenolic compounds, including rosmarinic acid, and has been studied for photoprotection and antioxidant activity. The aim of this study was to evaluate the photoprotection potential and antioxidant activity, and to develop analytic methodology for extract standardization and validation. Thus, maximum absorbance, sun protection factor, DPPH radical scavenging activity, and total phenolic contents of P. amboinicus crude ethanolic extract were determined, and an HPLC analytical methodology was developed and validated to quantify rosmarinic acid. Analyses revealed that the extract presented good photoprotection (SPF = 12.63), promising antioxidant activity (EC 50 = 112.39 μg/ml), total phenolic content (142.39 ± 1.12 mg GAE/g), and rosmarinic acid concentrations (22.5 μg/ml). In addition, an HPLC analytical method was validated for marker quantification. These results show that the extract has potential photoprotective and antioxidant activity, and this favors the isolation of a final product with protective characteristics that encompass broad spectrum action and biological protection.
Six sesquiterpenoids with unprecedented macrocyclic humulene-type structures, namely, dolichocarpols A-E (1− 5) with ether-bridged bicyclic rings between C-10 and C-2, C-10 and C-7, C-10 and C-6 (×2), and C-6 and C-3 and dolichocarpol F (6) cyclized between C-7 and C-2 and with an ether bridge between C-10 and C-3, were isolated from Anaxagorea dolichocarpa roots. The structures of the compounds were elucidated by NMR, MS, and IR data. Absolute configurations of compounds 1−3 and 6 were established on the basis of data from electronic circular dichroism, whereas relative configurations of compounds 4 and 5 were suggested by the NOESY spectrum. In addition, a putative biosynthetic pathway of the compounds is proposed. Furthermore, the cytotoxicity of 3, 4, and 6 against HCT-116 (human colorectal carcinoma) and L929 (murine fibroblast) was evaluated.
Leptohyptis macrostachys, previously known as Hyptis macrostachys Benth., is used in folk medicine to relieve the symptoms of asthma, cough, and bronchitis. Recently, we showed that the ethanol extract obtained from Leptohyptis macrostachys has selective spasmolytic activity on guinea pig ileum. Therefore, the aim of this study was to characterize the spasmolytic mechanism of this extract, investigated whether it presents toxicological and antidiarrheal activities. Therefore, the crude ethanolic extract of Leptohyptis macrostachys was analyzed by high-performance liquid chromatographicdiode array detection (HPLC-DAD). The spasmolytic effect was evaluated on guinea pig ileum, toxicological activity using rats and antidiarrheal activity using male and female mice. In HPLC-DAD analysis, Rosmarinic acid (5.44%) was the most abundant phenolic compound, being considered as a chemical marker. The spasmolytic potency of the extract on histamine-induced contraction was reduced in the presence of 1 mM TEA + , a selective big-conductance K + channels blocker (BK Ca). The extract produces a dosedependent antidiarrheal activity, inhibiting equipotently defecation frequency and liquid stool formation. In addition, the extract has inhibited in a dose-dependent manner both castor oil-induced intestinal transit and intestinal fluid content. Thus, the spasmolytic activity of the extract involves positive modulation of BK Ca and its antidiarrheal activity is related to inhibition of intestinal motility and secretion.
A dipirona é um derivado pirazolônico que apresenta efeitos analgésicos e antipiréticos, e é classificado como um anti-inflamatório não esteroidal (AINE) leve. Sendo frequentemente usado por se tratar de um medicamento isento de prescrição (MIP), em muitos casos a prática de partição de comprimidos é comumente usada no ajuste de doses, para facilitar a deglutição do medicamento ou baratear o custo do tratamento. O Brasil não possui regulamentação que norteia a prática de partição de medicamentos, a Agência Nacional de Vigilância Sanitária orienta que comprimidos não sulcados não devem ser partidos, mas que o procedimento poderá ser útil para medicamentos que possuem sulco. Diante disto, o presente trabalho teve como objetivo analisar a partição de comprimidos não revestidos de dipirona monoidratada 500mg (referência, genérico e similar), adquiridos em farmácia comercial na cidade de cajazeiras-PB. Para realização da pesquisa, foram utilizados dois objetos: cortador de comprimidos e faca de cozinha, foram analisadas peso médio das amostras íntegras e partidas de cada especialidade, e em seguida realizado o doseamento das partes obtidas dos comprimidos, seguindo parâmetros descritos na Farmacopeia Brasileira 6ª edição. Os resultados obtidos nessa pesquisa indicam que todas as amostras íntegras seguem os parâmetros estabelecidos pela Farmacopeia Brasileira para os testes de peso médio, onde nenhuma se mostrou fora do limite especificado. Porém as partes obtidas após a partição por meio dos objetos apresentam valores que excederam as porcentagens indicadas, diante disto estão não conformes para peso médio. Em relação à perda de pó após partição com cortador as amostras sulcadas (Referência e Genérico), tiveram maior perda de massa em relação a amostra não sulcada (comprimido Similar). As amostras partidas com faca de cozinha, a perca de massa em média foi maior para comprimidos Referência (9,05 mg) e Similar (7,58 mg). No teste de doseamento a curva de calibração realizada inicialmente demonstrou que o método obteve linearidade com um r2 =0,9999. Nas análises de teor das amostras partidas por cortador observou-se perda de teor de até 1,77% (referência), 0,68% (similar) e 2,70% (genérico). Para amostras partidas por faca as perdas foram de até 4,71% (referência), 4,68% (similar) e 2,49% (genérico). Deste modo, o presente trabalho comprova que entre os dois objetos utilizados para cortar os comprimidos ambos se apresentaram não conformes, sendo a partição de dipirona uma prática desaconselhável, tendo em vista que ocorrem perdas de peso e teor do fármaco podendo comprometer o tratamento do paciente.
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