RESUMEN
Calotropis procera (Aiton) Dryand (Apocynaceae), popularly known as milkweed, has been traditionally used to treat diseases particularly associated with gastric disorders, skin disease and inflammatory processes. The present study aimed to review the current scientific evidence regarding the pharmacological effects of C. procera extracted phytochemicals and possible research opportunities as complementary and alternative medicine. Scientific publications were searched in various electronic databases (PubMed, Scopus, Web of Science, Google Scholar, Springer, Wiley, and Mendeley) using the following search terms: Calotropis procera, medicinal plants, toxicity, phytochemical characterization, and biological effects. Collected data showed that cardenolides, steroid glycoside and flavonoids are the main classes of phytochemicals identified in C. procera latex and leaves. In addition, lignans, terpenes, coumarins, and phenolic acids have been reported. These metabolites have been correlated with their biological activities, including mainly antioxidant, anti-inflammatory, antitumoral, hypoglycemic, gastric protective, anti-microbial, insecticide, anti-fungal, anti-parasitic, among others. However, some of the studies were carried out with only a single dose or with a high dose not achievable under physiological conditions. Therefore, the validity of C. procera biological activity may be questionable. Not less important to highlight are the risks associated with its use and the possibility of accumulation of heavy metals that can be toxic. Furthermore, there are no clinical trials with C. procera to date. In conclusion, the need of bioassayguided isolation of bioactive compounds, bioavailability and efficacy, as well as pharmacological and toxicity studies, are needed using in vivo models and clinical trials in order to support the traditionally claimed health benefits.
Asunto(s)
Apocynaceae , Calotropis , Calotropis/química , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Extractos Vegetales/química , Látex/química , Látex/farmacologíaRESUMEN
Our goal was to evaluate phytochemical characterization and the antitumor potential of Calotropis procera. The phytochemical constitution of the crude extract (CE) revealed the presence of flavonoids, glycosides and cardenolide. The MTT assay was used to evaluate the cytotoxicity of CE, methanolic (MF) and ethyl acetate fractions (EAF) of C. procera in canine osteosarcoma cells (OST), canine mammary tumor (CMT), and canine skin fibroblasts (non-tumor cell). Doxorubicin was also used as a positive control. Results showed that CE, MF and EAF promoted a decrease in the viability of OST and CMT cells and did not alter the fibroblasts viability. C. procera also decreased the number of cells, corroborating to the decrease in proliferation and the cell cycle arrest in the G0/G1 phase. It was also evaluated the cell morphology by light and fluorescence microscopy, being demonstrated a reduction in cytoplasmic and cell rounding characteristic of programmed cell death. Moreover, flow cytometry data demonstrated that CE treatment promoted increase of caspase-3 and p53, showing that the cell death was activated in OST cells. In addition, there was a decrease in CD31, VEGF, osteopontin and TGF-ß after CE treatment, suggesting that CE exerts its antitumor effect by reducing angiogenesis and tumor progression in OST cells. Moreover, CMT cells showed a reduction in PCNA after treatment with MF and CE. Analyzing the data together, C. procera, especially CE, showed an antitumor potential in both OST and CMT cells, encouraging us to continue investigating its use in cancer therapy.
Asunto(s)
Antineoplásicos/farmacología , Calotropis/química , Enfermedades de los Perros/tratamiento farmacológico , Neoplasias Mamarias Animales/tratamiento farmacológico , Osteosarcoma/veterinaria , Extractos Vegetales/farmacología , Animales , Antineoplásicos/química , Perros , Osteosarcoma/tratamiento farmacológico , Extractos Vegetales/químicaRESUMEN
Avaliou-se a itotoxicidade do extrato etanólico (CETOH), da fase orgânica (CEA) e do composto majoritário, o ácido (E)-cinâmico (AC), obtidos da polpa dos frutos da espécie popularmente conhecida como cujuba, cuieira e/ou cabaça (Crescentia cujete L.) sobre a inibição da germinação de sementes, desenvolvimento do hipocótilo e radícula das plantas invasoras Senna obtusifolia (L.) Irwin & Barneby (mata-pasto) e Mimosa pudica Mill. (malícia). A fase orgânica na concentração de 0,5% inibiu em 100% a germinação das sementes das duas plantas invasoras. O AC que foi obtido da fase orgânica inibiu a germinação das sementes de S. obtusifolia em 95% e de M. pudica em 99% na concentração de 0,1%, com concentração (%) tóxica para inibição de 50% (CI50) da germinação das sementes iguais a 0,063 e 0,037%, respectivamente; e nos bioensaios de crescimento de plântula, o AC foi mais eiciente sobre a radícula da planta S. obtusifolia (com CI50 igual a 0,009%) e para a planta M. pudica os valores de CI50 foram de 0,097% e 0,117% para a radícula e hipocótilo, respectivamente. Essa pesquisa reforça o potencial itotóxico do ácido (E)-cinâmico, veriicado inicialmente na fase orgânica em acetato de etila (CEA) rica nesse fenilpropanoide.
The phytotoxity of ethanol extracts, of the organic phase and major compound (cinnamic acid) obtained from the fruit pulp of Crescentia cujete L., were evaluated for their potential to inhibit seed germination, hypocotyl development and radicle development of the invasive weeds Senna obtusifolia (L.) Irwin & Barneby and Mimosa pudica Mill. The organic phase at a concentration of 0.5% inhibited 100% seed germination of both weeds. Cinnamic acid obtained from the organic phase inhibited seed germination by 95% for S. obtusifolia and 99% for M. pudica at a concentration of 0.1%, with concentrations (%) inhibiting 50% (IC50) seed germination equal to 0.063% and 0.037%, respectively. For the seedling growth bioassays, the toxicity of the cinnamic acid was more eicient for the S. obtusifolia radicle (IC50 equal to 0.009%), and for M. pudica the IC50 values were 0.097% and 0.117% for the radicle and hypocotyl, respectively. This research reinforces the phytotoxic potential of cinnamic acid, veriied initially in the organic phase (in ethyl acetate), which is rich in this phenylpropanoid.