Phospholipase A2 Inhibition and Antiinflammatory Activity of F4 Fraction of Total Ethereal Leaf Extract of Annona senegalensis Pers. (Annonaceae) | Chapter 02 | New Insights on Chemical Research Vol. 1

Annona senegalensis Pers. (Annonaceae) is a plant which is used in african traditional medicine for the treatment of various diseases. This study aimed to investigate the analgesic and anti-inflammatory activity of total ethereal leaf extract fractions of A. senegalensis. Compounds of methanolic fractions of ethereal leaf extract of A. senegalensis were separated by gel sephadex chromatography, in five fractions (F1, F2, F3, F4, F5). Experiments were performed in acetic acid-induced contortions in mice, carrageenan rat paw edema and phospholipase A2 inhibitory test. The methanolic fraction of total ethereal leaf extract (10 mg/kg, per os) significantly prevented the carrageenan inflammatory edema. The variation of edema is 22.31±3.35%, 49.66±13.50%, 52.10±10.02% respectively at T1h, T3h and T5h. The increased edema after oral administration of F4 fraction administered at 300 µg/kg and 1 mg/kg per os is respectively 52.77±7.36% and 33.81±6.94%. The variation of edema in betamethasone group (1 mg/kg, per os) is 23.46±3.99%. F4 fraction at 300 µg/kg, significantly inhibited 16.39% of phospholipase A2 enzyme activity. F4 fraction (300 µg/kg, per os) also significantly prevented acetic acid-induced pain in mice. The number of abdominal contortions is 21 versus 72 in control group. F4 fraction compounds have a powerful analgesic and anti-inflammatory activity that involves phospholipase A2 inhibition, comparable to betamethasone profile on pain and inflammation.

Author(s) Details

M. Sene
Laboratoire de Pharmacologie et Pharmacodynamie, FMPO, UCAD, BP 5005 Dakar-Fann, Senegal.

F. S. Barboza
Laboratoire de Pharmacologie et Pharmacodynamie, FMPO, UCAD, BP 5005 Dakar-Fann, Senegal.

A. Ndong
Laboratoire de Pharmacologie et Pharmacodynamie, FMPO, UCAD, BP 5005 Dakar-Fann, Senegal.

A. Sarr
Laboratoire de Pharmacognosie et Botanique, FMPO, UCAD, BP 5005 Dakar-Fann, Senegal.

A. Wele3
Laboratoire de Chimie Organique et Thérapeutique, FMPO, UCAD, BP 5005 Dakar-Fann, Senegal.

E. Bassene
Laboratoire de Pharmacognosie et Botanique, FMPO, UCAD, BP 5005 Dakar-Fann, Senegal.

G. Y. Sy
Laboratoire de Pharmacologie et Pharmacodynamie, FMPO, UCAD, BP 5005 Dakar-Fann, Senegal.

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Inhibition of Nigerian Echis ocellatus Phospholipase A2: Perspectives and Opportunities in Venomics | Chapter 01 | Recent Advances in Biological Research Vol. 4

The most effective and acceptable therapy for snakebite victims is the immediate administration of antivenin following envenomation which is limited by problems of hypersensitivity reactions in sensitive individuals and its inability to resolve the local effects of the venom. Phospholipase A2 Inhibitor from Echis ocellatus Serum (PIES) was isolated, partially purified and characterized. The neutralizing protein from E. ocellatus serum inhibited the E. ocellatus (carpet viper) venom phospholipase A2 (PLA2) enzyme in a dose dependent manner. A two step purification process on sephadex G-200 column chromatography and DEAE- cellulose chromatography gave an active fraction that inhibited the venom PLA2 by 78%. The result from SDS-PAGE showed the inhibitor to be a 24.98kDa protein and its kinetic study revealed a mixed pattern of inhibition on the carpet viper venom PLA2 with an estimated Ki values of 3.8%(v/v) to 7.3%(v/v). The study was carried out at the Department of Biochemistry, Faculty of Science, Ahmadu Bello University Zaria, Nigeria from June 2011 to August 2012. The relevance of these findings towards understanding the biochemistry of carpet viper envenomation and the development of a novel antivenin drug in future targeting the activity of PIES are discussed.

Author(s) Details

F. A. Adamude
Department of Biochemistry, Federal University, Lafia, Nasarawa State, Nigeria.

J. E. Dingwoke
Department of Biochemistry, Ahmadu Bello University, Zaria, Kaduna State, Nigeria.

N. N. Nwobodo
Department of Pharmacology & Therapeutics, College of Medicine, Enugu State University of Science & Technology, Enugu, Enugu State, Nigeria and Department of Pharmacology & Therapeutics, College of Health Sciences, Nile University of Nigeria, FCT, Abuja, Nigeria.

A.Ubhenin
Department of Biochemistry, Federal University, Lafia, Nasarawa State, Nigeria.

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