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May 2018 DOI 10.14302/issn.2578-8590.ipj-18-2113
Hajare RahulCorresponding author
Indian Council of Medical Research, New Delhi
Isatin (1H-indole-2,3-dione ) and derivatives demonstrate a diverse array of biological activities. Isatin and 5-halo derivatives has reacted to form the schiff’s bases , mannich bases and friedal craft alkylation’s to form C-C, C-N, C=N bonds. From the spectral studies, isatin has undergoes reaction at C-3 and N-1 position and synthesized lead in present schme and seen the similarity of structure and analgesic-anti-inflammatory activity.
Apr 2021 DOI 10.14302/issn.2328-0182.japst-21-3778
Okiemute Rosa Johnson-AjinwoCorresponding author
Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Port Harcourt, Nigeria.
This study aims at investigating the antipyretic activity of different solvent fractions of the root bark of Rutideaparviflora(Rubiaceae). This plant is used ethno-botanically by the people of Ethiope East-West Local Government Area of Delta State, Nigeria to treat various ailments such as inflammation, fever and pain. This necessitated this research to validate its local use, due to the scanty literature and information present about this plant. It has also shown some anti-cancer and anti-inflammatory activity in previous researches. The present study is a randomized control study. Acetic acid induced writhing was employed for analgesic testing. Acetic acid was used to induce writhing in Wistar rats which were divided into fourteen (14) groups. The groups were administered extracts and fractions of the plant (200 mg/kg and 400 mg/kg). The animals were observed for number of writing movements and the percentage writhing was calculated. Baker’s yeast induced pyrexia was employed for the antipyretic testing. The animal groups were administered extracts and fractions of the plant (200 mg/kg and 400 mg/kg), with Paracetamol as the standard drug (100 mg/kg) and Normal saline (control) for both experiments. The body temperature of the rats was measured rectally over a period of five (5) hours. All values of P<0.05 were taken as significant. The organic extract, aqueous extract and various fractions (n-hexane, ethyl-acetate, n-butanol and aqueous) produced significant inhibition of writhing responses and pyrexia in a dose dependent manner and time dependent manner respectively. The aqueous extract at a dose of 400mg/kg showed the greatest reduction in writhing, 91.58% compared to the standard drug (paracetamol) which may suggest that the fraction possesses better efficacy than paracetamol as an analgesic. The observed activities could be attributed to these bioactive compounds: Palmatine, Urs-12-ene-24-oic-3-oxo-methyl ester and Gallic acid contained in R. parviflora.
Aug 2017 DOI 10.14302/issn.2688-5328.ijp-17-1600
Zlatanova HristinaCorresponding author
Department of Pharmacology and Clinical Pharmacology, Faculty of Medicine, Medical University Plovdiv, 15 A Vassil Aprilov blvd., 4002 Plovdiv, Bulgaria
The objective of our study was to evaluate the analgesic and anti-inflammatory activity, as well as possible organ toxicity of 2-3-3-methyl-pentanoic acid (compound 3d), a newly synthesized pyrrolic derivative, structurally similar to Celecoxib. Antinociception was assessed using animal pain models with thermal and chemical stimuli (paw withdrawal, tail-flick and formalin test). Anti-inflammatory activity was measured using the carrageenan-induced paw edema model. Blood samples were collected from the animals to study possible organ toxicity. All experiments were performed on male Wistar rats. The results in our study show that in experimental conditions 2-3-3-methyl-pentanoic acid has analgesic action against thermal and chemical stimuli. This effect is registered after both single and multiple administration of the compound. In the carrageenan model after single administration compound 3d did not inhibit formation of paw edema. After multiple administration all doses of compound 3d significantly suppressed paw edema at second, third and fourth hours. Hematological tests showed that compound 3d did not affect red blood cells and platelets but decreased white blood cell levels and the highest used dose decreased hemoglobin as well. Compound 3d decreased blood sugar levels and liver transaminases, compared to the control. Compound 3d did not affect creatinine levels but the smallest dose used lowered blood urea. We concluded antinociception in the tested compound is most likely mediated by supraspinal, spinal and peripheral mechanisms. Possible tolerance develops towards the analgesic action on spinal level after continuous administration. Anti-inflammatory activity, though significant, is probably not the leading cause for antinociception.