This paper describes the antinociceptive effects of tetrahydrophthalimides and related compounds in mice. Twenty compounds were obtained by the reaction of cis-1,2,3,6-tetrahydrophthalic anhydride with appropriate amines, dehydration, and addition to the imidic double bond. They were analyzed in the writhing test at 10 mg/kg given intraperitoneally. The most active compound 2-benzyl-5-morpholin-4-yl-hexahydroisoindole-1,3-dione (19) was studied on formalin, capsaicin, glutamate and hot plate models. The antinociceptive activity demonstrated by some studied compounds is promising, and some of them were more active than acetylsalicylic acid and paracetamol used as reference drugs in writhing tests in mice. Compound 19 was about 5-fold more potent than the reference drugs, being also effective by oral route and against the inflammatory response in the formalin test. The results suggest that compound 19 could be used as a model to obtain new and more potent antinociceptive agents. It exhibits an interesting antinociceptive profile, and does not interact with opioid systems.
Objective: This study aimed to evaluate peri-implant tissue changes during early osseointegration using a combined approach of digital radiographic analysis, RGB pseudocolorization, and histomorphometry in a sheep tibia model. Materials and Methods: Thirty titanium implants were placed in the tibiae of six adult sheep and evaluated at 14 and 28 days post-implantation. Digital periapical radiographs were acquired, grayscale values and RGB channel intensities were measured using Fiji/ImageJ, and compared with histological parameters (bone tissue, collagen, and medullary spaces) quantified from picrosirius–hematoxylin-stained sections. Manual overlay of radiographic and histological images was performed to ensure spatial correspondence of regions of interest. Statistical analyses assessed differences over time and correlations between image data and histological composition. Results: Radiographic grayscale values and histologically measured bone and collagen increased significantly from 14 to 28 days (p < 0.01), while medullary spaces decreased (p < 0.001), indicating progressive bone formation and matrix maturation. RGB analysis revealed significant increases in green channel intensity and decreases in red channel intensity (p < 0.05), while the blue channel remained stable. At 14 days, strong correlations were observed between blue channel intensity and bone tissue (r = 0.81; p = 0.015), and between green channel intensity and collagen (r = 0.98; p < 0.001). Visual overlays demonstrated alignment between radiographic high-density zones and histologically dense bone regions. Conclusions: RGB pseudocolorized radiographic analysis, correlated with histological findings, offers a non-invasive and reproducible method for early detection of peri-implant tissue maturation. This feasibility correlation study provides a foundation for future investigations integrating imaging, histology, and biomechanical testing.
1 January 2022 in Anais da Academia Brasileira de Ciências
This study evaluated some biological activities of extracts from Abuta selloana. The gastroprotective potential was determined against ethanol/HCl- and indomethacin-induced gastric ulcers, whereas the antinociceptive effect was evaluated by acetic acid-induced abdominal contortions in mice. The cytotoxicity activity was measured against human cancer cell lines: U251 (glioma), MCF-7 (breast cancer) and NCI-H460 (lung cancer). The radical scavenger potential was verified; and preliminary phytochemical analyses were performed. The phytochemical screening revealed higher levels of phenolic compounds in all extracts. Moreover, the methanolic extract from pulp fruit (MEPu), peel fruit (MEPe), branches (MEB) and leaves (MEL) scavenged the DPPH radical at 100 µg/mL. Besides, only MEL presented GI50 < 30 µg/mL in all tested cells. Besides, MEPu, MEPe, MEB or MEL at 10 mg/kg (i.p) reduced the abdominal contortions at 47.22%, 63.31%, 84.59% and 37.76%, respectively. The MEPu, MEPe, MEB and MEL reduced the ethanol/HCl- and indomethacin- induced ulcer at 250 mg/kg (p.o). In conclusion, A. selloana had interesting biological activities; presenting the leaves as a promising source for compounds with cytotoxic potential, however, further studies should be performed to confirm its antitumoral activity. Besides, the whole plant can be an important source of bioactive compounds associated with gastroprotective and antinociceptive properties.