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1.
Toxicol Res (Camb) ; 12(5): 853-862, 2023 Oct.
Article in English | MEDLINE | ID: mdl-37915498

ABSTRACT

Background: We aimed in this article to assess the likeliness of efavirenz to induce functional senescence in Drosophila melanogaster (fruit fly). Methods: Ten different concentrations of EFV were mixed with fly food and fed to 3-day-old flies orally for a 7 day LC50 calculation. Drug concentrations from LC50 were selected for a 28 day survival to determine the duration of treatment for behavioral and biochemical assays. A 5day feeding plan was used to investigate the effects of the drug on organismal, neuromuscular, reproductive, and metabolic senescence. An in silico study was executed to decipher a molecular interaction of Drosophila enzymes glutathione-s-transferase (GST) or acetylcholinesterase (AChE) with EFV. Results: The calculated LC50 of EFV was 118 mg/10-g fly diet. The test drug induced a significant (P < 0.05) increase in fly mortality, climbing difficulty, and procreative deficits after a 5 day oral exposure. Similarly, there were significant (P < 0.05) biochemical alterations, which suggested in vivo biochemical damage against total thiols (T-SH), SOD (superoxide dismutase), CAT (catalase), GST, AChE, and MDA (malondialdehyde) in the test flies compared to the control groups. In silico study revealed a significantly (P < 0.05) higher binding energy between EFV and the active amino acids of fly AChE and GST when compared to the substrates or standard inhibitors respectively. Conclusion: EFV exhibited ecotoxic potentials evidenced by age-related deficits in the fly's functional integrity such as sluggish movement, procreative deficiency, increased mortality, and oxidant-antioxidant inequality. Results from in silico study suggested antagonism against GST and AChE activities as a likely mechanism of EFV-induced toxicity in the fruit fly.

2.
PeerJ ; 11: e14639, 2023.
Article in English | MEDLINE | ID: mdl-36627919

ABSTRACT

Background: Diabetes is one of the fastest-growing health emergencies of the 21st century, placing a severe economic burden on many countries. Current management approaches have improved diabetic care, but several limitations still exist, such as decreased efficacy, adverse effects, and the high cost of treatment, particularly for developing nations. There is, therefore, a need for more cost-effective therapies for diabetes management. The evidence-based application of phytochemicals from plants in the management of diseases is gaining traction. Methodology: Various plants and plant parts have been investigated as antidiabetic agents. This review sought to collate and discuss published data on the cellular and molecular effects of medicinal plants and phytochemicals on insulin signaling pathways to better understand the current trend in using plant products in the management of diabetes. Furthermore, we explored available information on medicinal plants that consistently produced hypoglycemic effects from isolated cells to animal studies and clinical trials. Results: There is substantial literature describing the effects of a range of plant extracts on insulin action and insulin signaling, revealing a depth in knowledge of molecular detail. Our exploration also reveals effective antidiabetic actions in animal studies, and clear translational potential evidenced by clinical trials. Conclusion: We suggest that this area of research should be further exploited in the search for novel therapeutics for diabetes.


Subject(s)
Diabetes Mellitus , Plants, Medicinal , Animals , Diabetes Mellitus/drug therapy , Hypoglycemic Agents/pharmacology , Insulin/therapeutic use , Phytotherapy , Plants, Medicinal/chemistry , Humans
3.
Toxicol Rep ; 8: 571-580, 2021.
Article in English | MEDLINE | ID: mdl-33777703

ABSTRACT

Benzo[a]pyrene (B[a]P) is a polycyclic aromatic hydrocarbon (PAH) commonly found in cigarette smoke, automobile exhaust fumes, grilled meat, and smoked food among others. Exposure to B[a]P is associated with a range of toxic effects including developmental, neurological, oxidative, inflammatory, mutagenic, carcinogenic and mortal. Efficient and more affordable experimental models like Drosophila melanogaster could provide more insight into the mechanism of PAH toxicity and help develop new strategies for prevention, diagnosis and treatment of PAH-related conditions. In this study, we examined the induction of some biochemical changes along with mortality and functional senescence by B[a]P and its metabolite, benzo[a]pyrene- 7,8-dihydrodiol-910-epoxide (BPDE) in the Canton-S strain of Drosophila melanogaster, with the aim to establish an alternative assay medium for B[a]P toxicity in flies. Flies were exposed to 2-200 µM of B[a]P and 1-10 µM of BPDE through diet for a seven-day survival assay followed by a four-day treatment to determine the effects of the compounds on negative geotaxis, fecundity and some biochemical parameters of oxidative damage. BPDE significantly reduced the survival rate of flies along the 7 days of exposure whereas B[a]P did not cause any significant change in the survival rate of flies. B[a]P and BPDE significantly reduced the climbing ability of flies after 4 days of exposure. Rate of emergence of flies significantly reduced at 10-200 µM of B[a]P and 5-10 µM of BPDE. Both compounds caused various levels of alterations in the values of reduced glutathione (GSH), total thiol (T-SH), glutathione-S-transferase (GST), catalase (CAT), hydrogen peroxide (H2O2), nitric oxide (NO) and acetylcholinesterase (AChE) of the flies. The compounds also exhibited high binding affinities and molecular interactions with the active site amino acid residues of Drosophila GST and the inhibitor binding site of Drosophila AChE in an in silico molecular docking analysis, with BPDE forming stable hydrogen bonds with AChE. Hence, the Canton-S strain of Drosophila melanogaster could offer a simple and affordable assay medium to study B[a]P toxicity.

4.
N Am J Med Sci ; 4(1): 24-8, 2012 Jan.
Article in English | MEDLINE | ID: mdl-22393544

ABSTRACT

BACKGROUND: Medicine vendors fill the gap created by inadequate skilled professionals required for medicine procurement, storage, and distribution in developing countries. AIM: To evaluate self-medication practice and medicine knowledge among medicine vendors and to determine if a relationship exists between both. MATERIALS AND METHODS: A descriptive, cross-sectional study was conducted, using a pretested questionnaire on 236 medicine vendors in Jos, Nigeria, sampled through a two-stage stratified design. Data collected were analyzed using the Statistical Package for Social Sciences version 16, and the chi-square test was used to determine the association between variables. RESULTS: Self-medication was common (75.4%) among respondents and was not associated (P>0.05) with any of the demographic characteristics studied. The classes of medicines commonly used by respondents for self-medication were analgesics (31.4%), anti-malarials (22.6%), multivitamins (17.7%), and antibiotics (11.25%). A knowledge assessment test revealed that only 34.3% of the respondents had adequate knowledge. There was no significant (P>0.05) relationship between self-medication practice and medicine knowledge, among the respondents. However, the medicine knowledge scores were significantly (P<0.05) associated with holding a certificate in health sciences, years of experience, and the place of practice of the medicine vendors. CONCLUSION: The present study demonstrated that self-medication practice was high and inadequate medicine knowledge existed among respondents.

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