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Showing posts with label COX 2 inhibition. Show all posts
Showing posts with label COX 2 inhibition. Show all posts

Friday, October 18, 2013

Black cumin seeds possess analgesic and anti-inflammatory activity comparable to indomethacin.

IN VIVO EVALUATION OF ANTI-INFLAMMATORY AND ANALGESIC ACTIVITIES OF NIGELLA SATIVA SEED DURING GERMINATION

MOHAMMAD HAYATUL ISLAM, IFFAT ZAREEN AHMAD AND MOHAMMAD TARIQ SALMAN

Objective: The medicinal values of Nigella sativa have been mentioned in ancient literature as useful in disorders of inflammation. The present study investigates the anti-inflammatory and analgesic activities of methanol extract of Nigella sativa seed during different phases of its germination on Wistar rats. Methods: Seeds of N. sativa were grown in vitro in glass petri plates using multiple folds of damp filter paper. Complete plantlet with two leaves was obtained in 11 days. The acute anti-inflammatory activity of N. sativa extracts during different phases of germination was measured plethysmographically using kaolin as inflammatory agent, analgesic activity was measured by hot plate method, keeping indomethacin (10mg/kg b.w) as reference standard in both tests.
Results: All tested extracts of N. sativa (1gm/kg b.w) during different phases of germination showed significant reduction in paw oedema in comparison to control (P<0 .001="" 5th="" all="" among="" analgesic="" and="" anti-inflammatory="" day="" during="" effect="" extract="" extracts.="" germination="" hot="" in="" increased="" of="" on="" p="" plate="" reaction="" showed="" significant="" test.="" test="" tested="" the="" time="">
Conclusion: It may be concluded that extracts of N. sativa possess enhanced anti-inflammatory and analgesic activities during germination as compared to seed extract. High metabolic activity and higher contents of secondary metabolites expressed during germination might be responsible for this activity.

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Saturday, April 4, 2009

Targeted cancer therapy

Treatment options for inoperable or progressive malignant pancreatic endocrine tumors (PETs) are limited, but new evidence suggests that the epidermal growth factor receptor (EGFR) and cyclo-oxygenase 2 (COX2) should be investigated as potential chemotherapeutic targets.
Dr Bergmann et al. analyzed 110 tumor samples from 74 patients who underwent resection of PETs between 1991 and 2006. EGFR was expressed in 57% of malignant PETs and in 26% of nonmalignant (benign tumors or those with uncertain behavior) PETs. Malignant PETs were characterized by significantly higher average expression of EGFR than nonmalignant PETs. By contrast, no significant differences were observed between nonmalignant and malignant PETs regarding COX2 expression, which was uniformly high across tumor categories.
Administration of the EGFR antagonist AG1478 and of the COX2 inhibitor celecoxib to the human pancreatic carcinoid cell line BON and to the mouse pancreatic insulinoma cell line -TC-3 resulted in significant, dose-dependent decreases of cell viability. Administered in combination, celecoxib and AG1478 displayed additive effects on cell viability in both cell lines.
Evidence suggests that EGFR and COX2 are potential chemotherapeutic targets for PETs that should be further investigated.
Source: Bergmann, F. et al. Expression pattern and functional relevance of epidermal growth factor receptor and cyclooxygenase-2: novel chemotherapeutic targets in pancreatic endocrine tumors? Am. J. Gastroenterol. 104, 171–181 (2009).

Friday, March 13, 2009

A case report on nimesulide and its relation with angina

Salman, M. T.; Rahman, S. Z. and Khan, R. A. (2003) A case report on nimesulide and its relation with angina. In: International Workshop on Adverse Drug-Reaction Monitoring & 3rd Annual Conference Society of Pharmacovigilance, India, 11-13 Dec 2003, Agra, India.

Even though there might be several cases of NSAIDs induced angina that are not been reported, we could find a definite case of Nimesulide induced angina in Aligarh. A 65 year old female patient was a known case of diabetes mellitis for 17 years and angina pectoris for 10 years for which she was maintained on drugs. She sustained injury after falling down and was found to have Colle’s fracture for which she was advised POP and Tab Nimesulide twice daily alongwith ongoing treatment. On 3rd day, she felt chest pain (angina) for which she used Tab sorbitrate 3-4 times a day but no improvement was noticed. Then she consulted her family physician. On examination, no abnormality was found except that ECG showed changes of ischemia and extra systoles. She was diagnosed as a case of Unstable Angina and advised to stop the suspected drug Nimesulide but continue to take previous treatment. She then showed improvement in angina. As an alternative Tab Brufen (Ibuprofen) 400 mg thrice daily was advised. The patient afterwards complained no problem. In this case, the unstable angina appears to be due to coronary spasm and not due to clot because on withdrawing the suspected drug there was rapid relief. The spasm seems to be related to inherent properties of Nimesulide and not due to prostaglandin inhibition as Brufen did not cause the same symptoms. Alternatively, it may be due to an imbalance between COX 1 and COX 2 activities due to preferencial COX 2 inhibition. Moreover, the inhibition of prostaglandin synthesis may adversely affect cardiovascular homeostasis.

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