It is our interest to screen Oela europaea L and Ficus carica L leaf extract for total phenolic, flavonoid contents and to evaluate their free radical scavenging and Ferric reducing power (FRAP) using 1,1-diphenyl-2-picrylhydrazyl (DPPH). Data shows that Olea europaea and Ficus carica have strong antioxidant potency to scavenge free radical at an optimal phenolic and flavonoid concentration. Results further suggest a strong correlation between antioxidant activities, phenolic and flavonoid contents. Thus, the screening of Ficus carica and Olea europaea leaf extracts for potential antioxidants as source of drugs for several diseases especially oxidative stress and cancers is illustrated.
The aim of this work is to evaluate the antitumor effect mediated by the proteasome inhibitors of Inula viscosa extracts on skin carcinogenesis. Female Swiss albino mice were divided into five groups depending on the combination of skin cancer-inducing 7,12-dimethylbenz(a)anthracene (DMBA) and extract of Inula viscosa treatments. Histology of the affected skin and measurement of proteasome activity were performed to demonstrate the effect of Inula viscosa on mice. The identification of the molecules responsible for this inhibitory activity was carried out through the docking studies. The results showed that Inula viscosa extracts inhibit the development of papilloma in mice. Therefore, the best chemopreventive action of Inula viscosa was observed on mice in which extract treatment was performed before and after the induction of skin carcinogenesis. It was revealed that the ingestion of extracts Inula viscosa delays the formation of skin papillomas in animals and simultaneously decreases the size and number of papillomas, which is also reflected on the skin histology of the mice treated. Structure–activity relationship information obtained from component of Inula viscosa particularly tomentosin, inuviscolide, and isocosticacid demonstrated that distinct bonding modes in β1, β2, and β5 subunits determine its selectivity and potent inhibition for β5 subunit.
Ethnopharmacological Relevance. Aristolochia paucinervis (A. paucinervis) (Aristolochiaceae) is a plant frequently used in Moroccan alternative medicine. The aim of the current study is to investigate the phytochemical composition of rhizomes decoction of A. paucinervis (RDA) and to evaluate its acute and subacute toxicity following the OECD guidelines. Materials and Methods. The qualitative phytochemical analysis of A. paucinervis was performed using standard qualitative phytochemical procedures. The acute toxicity of rhizomes decoction of the studied plant was evaluated in mice at single doses of 1, 2, and 4 g/kg of body weight for 14 days. In subacute toxicity study, the decoction was orally administered to mice at three different doses (0.5, 1, and 1.5 g/kg/day) for 28 days. Histopathological and biochemical parameters were investigated. Results. The preliminary phytochemical screening showed the presence of flavonoids, saponins, alkaloids, and polyphenols and the absence of anthraquinones, sterols, and terpenes. There was no mortality and no significant changes occurred in animals treated with 1 and 2 g/kg in the acute toxicity model. The signs of toxicity and morbidity were remarkable with the highest tested dose (4g/kg). LD50 (dose required to kill 50% of the test population) was determined as 4 g/kg. Repeated oral administration of 1 and 1.5 g/kg/day of RDA for 28 days induced significant disturbance of serum parameters (AST, ALT, LDH, urea, creatinine). Kidney and liver extracted from mice fed with 1 and 1.5 g/kg/day showed significant histopathological injuries as tubular necrosis, inflammatory infiltrate, tubular degeneration, necrosis, and hepatic cholestasis. Meanwhile, neither histopathological nor biochemical alterations were observed in mice treated with 0.5 g/kg/day of body weight in comparison to the control group. Conclusion. RDA showed toxicity in mice at a dose of 1 g/kg/day under subacute toxicity conditions. RDA is safe at a single dose inferior to 4 g/kg of body weight. The plant extract prepared by decoction showed more poisonous effect than the extract prepared by maceration at room temperature.
Oleaeuropaea and Ficuscarica are widely used in traditional medicine for the treatment of cancer. Therefore, it is of interest to develop a QSAR model for screening proteasome inhibitors from plant source. Hence, a QSAR model was developed using multiple linear regressions; partial least squares regression and principal component regression methods. Results of QSAR modeling and docking demonstrate that compounds derived from both plants have great potentiality to be proteasome inhibitors. The developed QSAR model highlights a strong structure-effect relationship. The predicted correlation of comparative molecular field analysis, and comparative molecular similarity indexes are 0.963 and 0.919, respectively. Computed absorption, distribution, metabolism, excretion and toxicity studies on these derivatives showed encouraging results with very low toxicity, distribution and absorption.
Background Regulatory degradation of intracellular proteins plays an essential role in most biological processes, particularly in the control of cell proliferation and differentiation. In eukaryotes, intracellular proteolysis is largely provided by the Ubiquitin / Proteasome system. Alterations and dysfunction of protein degradation by the Ubiquitin / Proteasome system, such as transcription factors, cell cycle regulators or tumor suppressor proteins, have been linked to human. Pathologies, including blood cancers. Mainly localized in the nucleus and cytoplasm of cells, the proteasome can be detected in the cell culture supernatant or in the peripheral blood of patients. This study deals with the problems of the search for serum markers specific to certain pathologies and which would be useful in the prevention, diagnosis and monitoring of cancers and which could be used as a therapeutic tool. Methods The functional and quantitative analysis of the proteasome is carried out at the serum and subcellular level during a pathological phenomenon in a population of 145 Moroccan patients (sex ratio: 1.10 / average age: 47.9 ± 15, 3 years) using an indirect ELISA test and a follow-up of the fluorescence emitted after enzymatic digestion of specific peptides by proteolytic activity (chymotrypsin-like). Results The evolutionary trend proteasome subcellular is significantly linked to the rate of chymotrypsin-like activity. The entire population of 60 patients called back for a second blood test. After three months of treatment reported a significant drop in the rate and the activity of the proteasome in serum and intracellular level. Conclusions Although the serum proteasome level is a potential new tool for the monitoring of. Patientswithliquid cancer. Trial registration: retrospectively registered.
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