Chronic inflammation is triggered by numerous diseases such as osteoarthritis, Crohn's disease and cancer. The control of the pro-inflammatory process can prevent, mitigate and/or inhibit the evolution of these diseases. Therefore, anti-inflammatory drugs have been studied as possible compounds to act in these diseases. This paper proposes a computational analysis of eugenol in relation to aspirin and diclofenac and analyzing the ADMET profile and interactions with COX-2 and 5-LOX enzymes, important enzymes in the signaling pathway of pro-inflammatory processes. Through the analysis of ADMET in silico, it was found that the pharmacokinetic results of eugenol are similar to NSAIDs, such as diclofenac and aspirin. Bioinformatics analysis using coupling tests showed that eugenol can bind to COX-2 and 5-LOX. These results corroborate with different findings in the literature that demonstrate anti-inflammatory activity with less gastric irritation, bleeding and ulcerogenic side effects of eugenol. The results of bioinformatics reinforce studies that try to propose eugenol as an anti-inflammatory compound that can act in the COX-2/5-LOX pathways, replacing some NSAIDs in different diseases.
Rose oxide (RO) is a monoterpene found in rose oil fragrances. This monoterpene has been reported to possess anti-inflammatory activity, however, little is known regarding its pharmacological activity. The present study was carried out to evaluate its antidepressant action and possible mechanisms of action. Analysis of ADMET pharmacokinetic properties (absorption, distribution, metabolism, excretion and toxicity) of rose oxide was performed by computational prediction analysis. Behavioral tests were performed to assess the interaction between rose oxide and the central nervous system and antidepressant effect that includes: forced swim test (FST), tail suspension test (TST), open field test (OFT) and rota-rod test. The results of pharmacokinetic and toxicological properties indicate that rose oxide could be used orally, since it has good intestinal absorption as well as pharmacological and toxicological properties that can be similar to pharmacological compounds (regular hepatic metabolism and low toxicity). Treatment with 50 mg/kg of rose oxide was able to decrease the immobility time of animals not affected by FST and TST and was not able to alter the motor activity of the OFT and rota-rod test, suggesting modulation and antidepressant activity. Docking data suggest that rose oxide can bind to receptors in the serotonergic pathway. The results described here suggest that rose oxide has antidepressant activity, modulating the serotonergic pathway.
Species of Piperaceae are known by biological properties, including antiparasitic such as leishmanicidal, antimalarial and in the treatment of schistosomiasis. The aim of this work was to evaluate the antileishmania activity, cytotoxic effect, and macrophage activation patterns of the methanol (MeOH), hexane (HEX), dichloromethane (DCM) and ethyl acetate (EtOAc) extract fractions from the leaves of Piper cabralanum C.DC. The MeOH, HEX and DCM fractions inhibited Leishmanina amazonensis promastigote-like forms growth with a half maximal inhibitory concentration (IC50) of 144.54, 59.92, and 64.87 μg/mL, respectively. The EtOAc fraction did not show any relevant activity. The half maximal cytotoxic concentration (CC50) for macrophages were determined as 370.70, 83.99, 113.68 and 607 μg/mL for the MeOH, HEX and DCM fractions, respectively. The macrophage infectivity was concentration-dependent, especially for HEX and DCM. MeOH, HEX and DCM fractions showed activity against L. amazonensis with low cytotoxicity to murine macrophages and lowering infectivity by the parasite. Our results provide support for in vivo studies related to a potential application of P. cabralanum extract and fractions as a promising natural resource in the treatment of leishmaniasis.
Platonia insignis Mart, Clusiaceae, known as bacuri, is a species native to Brazil that, in studies with extract of the seed of its fruit, showed antioxidant activity against free radicals. Products with such properties may be of great importance in the treatment of peptic ulcers since this pathology may be associated with the inflammatory process caused by the action of free radicals. Cyclodextrins are molecules capable of forming inclusion complexes with other molecules, affecting their physicochemical properties and improving their pharmacokinetic characteristics. Thus, this work aimed to produce, characterize, and evaluate the gastroprotective effect of the inclusion complex of β-cyclodextrin (β-CD) with the bacuri seeds hexanic extract (BSHE). In the characterization of the inclusion complex, an apparent stability constant (Kc) of 416 mol/L was obtained in the solubility study; the BSHE:β-CD m/m (g) complexation ratios at 1:9, 2:8, and 3:7 were 5.51%, 21.46%, and 20.11%, respectively. The formation of the BSHE:β-CD inclusion complex was observed by FTIR technique, indicating the disappearance of bands characteristic of BSHE (2960 cm−1 and 1755 cm−1) when in the complex, compared to the spectra of pure BSHE or in physical mixture with β-CD, and by X-ray diffraction, which indicated a loss of crystallinity, typical signals of pure β-CD, and presentation of intense amorphization, characteristic of BSHE, incorporated in the β-CD pockets. In the evaluation of gastroprotective activity, through absolute ethanol-induced gastric lesions in mice, both BSHE and BSHE:β-CD reduced gastric lesions, with 100 mg/kg dose of the complex having the greatest gastroprotective effect. BSHE:β-CD was also able to reduce gastric lesions from ischemia and reperfusion, with the 50 mg/kg dose being the most effective. BSHE:β-CD, also at this dose, reduced the MDA levels of the gastric mucosa, indicating a possible antioxidant activity in its gastroprotective effect. Thus, it was concluded that inclusion complex formation between β-CD and BSHE is possible, and that this formulation enhanced the gastric protective activity.
Historically this knowledge has been offered to the student of the countryside without taking into account the specificities of the life and job of the countryside becoming only an adaptation of teaching practiced in the city to the rural school. That has contributed just only to preserve the establishment of countryside and the feed of the alienation of the countrysideman. This work aims to propose an alternative to agribusiness pedagogical dynamics imposed on the students of the countryside. It is intended propose the development of a methodology for chemical education to promote the dissemination of scientific chemical knowledge by the student who lives in rural areas. It is taking the peculiarities of life in the field as a starting point of the teaching-learning process.
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