The results confirm the popular use of Zanthoxylum rhoifolium as an analgesic, and contribute to the pharmacological knowledge of this species because it was shown that EtOH and its less polar partition fractions (HEX, AcOEt) have an antinociceptive effect in models of chemical nociception, and that lupeol appears to be one of the constituents responsible for this effect.
The present work reports the anti-inflammatory and antinociceptive activities of the ethanol extract obtained from the stem bark of Sterculia striata A. St.-Hil. & Naudin (Ss-EtOH) in the experimental models of edema induced by carrageenan, dextran, or histamin and nociception induced by chemical stimuli, such as acetic acid, formalin, capsaicin, or glutamate. The Ss-EtOH (50 mg/kg) promoted a marked inhibition on the hind paw edema induced by carrageenan or dextran (30% and 73%, respectively). Besides, Ss-EtOH (25 mg/kg) exhibited a slight activity (30%) on the hind paw edema induced by histamin. The Ss-EtOH (12.5 and 25 mg/kg) showed the antinociceptive activity on chemical stimuli induced by acetic acid (65.59% and 38.37%, respectively), formalin, in the initial (35.08% and 31.5%, respectively) and late phases (44.09% and 83.57%, respectively), capsaicin (43.77% and 51.31%, respectively), or glutamate (36.6% and 52.12%, respectively). Regarding the possible mechanism involved in the antinociceptive effect, Ss-EtOH (12.5 mg/kg) showed a decrease in the antinociceptive effect (65.8%) in the acetic acid model after pretreatment with naloxone. Thus, opioid mechanisms might be underlying this response.
The objective of this work is to carry out a prospection of docking molecular on biochemical targets of Leishmania sp. The scientific prospection was executed in May /2017 and based on the search for articles in the Virtual Health Library (VHL). In 2006-2017, 84 articles were selected from several countries, including India, Brazil and Mexico. In the classification of the Protein Data Bank (PDB), molecular targets were found belongs to oxidoreductases, hydrolases, transferases, isomerases, DNA, proteases, etc. The most important species of Leishmania sp. were L. major, L. donovani, L. infantum, L. amazonensis, etc. The 3 main molecular targets were found trypanothione reductase, pteridine reductase and topoisomerase I, besides various targets involved in the immune system, carbohydrate metabolism, ATP, nitrogen bases, amino acids, etc. It was possible to find the 3 most studied enzymes (trypanothione reductase -2JK6; pteridine reductase 1 -1E7W; topoisomerase I -2B9S) what play important biological functions in the parasites and important molecular targets in antileishmania therapy.
In this study we demonstrated the potential association effect of conventional amphotericin B (Amph B) and Gallic acid (GA) or Ellagic acid (EA) in topical formulation for treatment of cutaneous leishmaniasis in BALB/c mice. Preliminary stability tests and in vitro drug release studies with Amph B, GA, Amph B + GA, EA and Amph B + EA in the composition and in vivo treatment of BALB/c mice infected by Leishmania major were performed. After 40 days of infection, the animals were divided into 6 groups, treated 2x/day, for 21 days with the gel of Amph B, GA, Amph B + GA, EA and Amph B + EA and the negative control group was treated with the vehicle. In the animals that received treatment there was reduction of the lesion size and reduction of the parasitic load. In the histopathological analysis of the treatments with GA, EA and associated Amph B, circumscribed lesion with presence of fibroblasts, granulation tissue and collagens deposition, as well as presence of activated macrophages. The formulations containing GA and EA activated macrophages in all evaluated parameters, resulting, therefore, in the activation of cells of the innate immune response, which can generate healing and protection. GA and EA produced an association effect with Amph B, which makes them promising their use with conventional Amph B in the treatment of cutaneous leishmaniasis.
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