The present study describes the use of the traditional species Copaifera for treating wounds, such as ulcers scarring and antileishmanial wounds. It also relates phytochemical studies, evaluation of the leishmanicidal activity, and toxicity. The species of Copaifera with a higher incidence in the Amazon region are Copaifera officinalis, Copaifera reticulata, Copaifera multijuga Hayne. The copaiba oil is used in the Amazon's traditional medicine, especially as anti-inflammatory ingredient, in ulcers healing, and in scarring and for leishmaniasis. Chemical studies have shown that these oils contain diterpenes and sesquiterpenes. The copaiba oil and terpenes isolated have antiparasitic activity, more promising in the amastigote form of L. amazonensis. This activity is probably related to changes in the cell membrane and mitochondria. The oil showed low cytotoxicity and genotoxicity. Furthermore, it may interfere with immune response to infection and also has a healing effect. In summary, the copaiba oil is promising as leishmanicidal agent.
This study aimed to evaluate the leishmanicidal activity of ethanol extract, fractions, and isolated substance from Handroanthus serratifolius against Leishmania amazonensis. Furthermore, this activity was related to cytotoxicity, and the selectivity index was determined. The ethanol extract was obtained by maceration of the stem powder, and the extract was subjected to fractionation on chromatographic column. The lapachol was obtained by acid base extraction followed by purification in chromatographic column. The antipromastigote activity and cytotoxicity tests were carried out by the cell viability method (MTT). Modified THP-1 cells were infected with L. amazonensis promastigotes and treated for 24 h with different concentrations of the extract, fractions, and lapachol. The ethanol extract, dichloromethane, and ethyl acetate fractions were not active against promastigotes (IC50 > 200 μg/mL) or cytotoxic (CC50 > 500 μg/mL), and the selectivity index (SI) was greater than 2.5. The ethyl acetate fraction was active only in promastigotes; it is not cytotoxic (CC50 > 500 μg/mL, SI > 5). The lapachol was selectively active only against amastigote (IS > 2.5, CC50 > 500 μg/mL). In summary, lapachol and ethyl acetate fraction are promising against amastigote and promastigote forms, respectively.
Chemotherapy is limited in the treatment of leishmaniasis due to the toxic effects of drugs, low efficacy of alternative treatments, and resistance of the parasite. This work assesses the in vitro activity of flavopereirine on promastigote cultures of Leishmania amazonensis. In addition, an in silico evaluation of the physicochemical characteristics of this alkaloid is performed. The extract and fractions were characterized by thin-layer chromatography and HPLC-DAD, yielding an alkaloid identified by NMR. The antileishmanial activity and cytotoxicity were assayed by cell viability test (MTT). The theoretical molecular properties were calculated on the Molinspiration website. The fractionation made it possible to isolate a beta-carboline alkaloid (flavopereirine) in the alkaloid fraction. Moreover, it led to obtaining a fraction with greater antileishmanial activity, since flavopereirine is very active. Regarding the exposure time, a greater inhibitory effect of flavopereirine was observed at 24 h and 72 h (IC50 of 0.23 and 0.15 μg/mL, respectively). The extract, fractions, and flavopereirine presented low toxicity, with high selectivity for the alkaloid. Furthermore, flavopereirine showed no violation of Lipinski’s rule of five, showing even better results than the known inhibitor of oligopeptidase B, antipain, with three violations. Flavopereirine also interacted with residue Tyr-499 of oligopeptidase B during the molecular dynamics simulations, giving a few insights of a possible favorable mechanism of interaction and a possible inhibitory pathway. Flavopereirine proved to be a promising molecule for its antileishmanial activity.
The epiplastic foramen is a natural opening in the thoracic cavity that communicates with the abdominal cavity, located dorsally to the cleft of the liver, contacting the caudal vena cava, portal vein, pancreas, hepatoduodenal ligament and with the small intestine loops. Horses diagnosed with intestinal loop incarceration in the epiplastic foramen require surgical treatment, with a prognosis of being reserved to unfavorable, and the ileum is the intestinal segment most affected in this disease. In addition, because of a strangulative process, the animal shows signs of abdominal discomfort called colic and enterogastric reflux, but clinical signs are variable. Some animals in the palpation present palpable small intestine or not and abdominal discomfort varying from mild to severe. The objective of this work is to report a case of a 5-year-old female Quarter Horse, weighing 430 kg, with a history of abdominal discomfort two days ago and with intermittent pains, from the municipality of Batatais, Veterinary Hospital of Batatais, addressing the animal clinic, diagnosis and treatment. In the rectal palpation he identified slightly distended loops and palpable small intestine and puncture of the peritoneal fluid through the abdominocentesis showed a reddish coloration. The animal was under observation, but even with all the clinical interventions, the pain picture increased and with that it was submitted to exploratory laparotomy, where the incarceration was diagnosed in the epiplastic foramen. In view of the clinical case, it was concluded that the incarceration of the epiplastic foramen may lead to significant intestinal loops involvement, progressing to destabilization of the general state of the animal, being aggravating factors for the surgical procedure, becoming a case of risk of the patient. The animal in this report was submitted to euthanasia due to the great compromise of the intestinal loops. It is concluded that the diagnosis should be performed as early as possible, increasing the chance of resolution with favorable prognosis.
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