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Modulation of Anopheles gambiae Epsilon glutathione transferase activity by plant natural products in vitro

Muleya, V., Hayeshi, R., Ranson, Hilary ORCID:, Abegaz, B., Bezabih, M. T., Robert, M., Ngadjui, B. T., Ngandeu, F. and Mukanganyama, S. (2008) 'Modulation of Anopheles gambiae Epsilon glutathione transferase activity by plant natural products in vitro'. Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 23, Issue 3, pp. 391-399.

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Elevated glutathione transferase (GST) E2 activity is associated with DDT resistance in the mosquito Anopheles gambiae. The search for chemomodulators that inhibit the function of AgGSTE2 would enhance the insecticidal activity of DDT. Therefore, we examined the interaction of novel natural plant products with heterologously expressed An. gambiae GSTE2 in vitro. Five of the ten compounds, epiphyllocoumarin(Tral-1), knipholone anthrone, isofuranonaphthoquinones (Mr 13/2, Mr 13/4) and the polyprenylated benzophenone (GG1) were shown to be potent inhibitors of AgGSTE2 with IC50 values of 1.5 mu M, 3.5 mu M, 4 mu M, 4.3 mu M and 4.8 mu M respectively. Non-competitive inhibition was obtained for Tral 1 and GG1 with regards to GSH (K-i of 0.24 mu M and 0.14 mu M respectively). Competitive inhibition for Tral1 was obtained with CDNB (K-i = 0.4 mu M) whilst GG1 produced mixed type of inhibition. The K-i and K-i' for GSH for Tral-1 and GG1 were 0.2 mu M and 0.1 mu M respectively. These results suggest that the novel natural plant products, particularly Tral-1, represent potent AgGSTE2 in vitro inhibitors.

Item Type: Article
Uncontrolled Keywords: anopheles gambiae glutathione s-transferases malaria natural plant products chemomodulation ddt-resistance insecticide-resistance s-transferases antimalarial-drugs vector ddt inhibition mechanisms expression flavonoids strain
Subjects: QV Pharmacology > Anti-Inflammatory Agents. Anti-Infective Agents. Antineoplastic Agents > QV 256 Antimalarials
QX Parasitology > Insects. Other Parasites > QX 510 Mosquitoes
QX Parasitology > Insects. Other Parasites > QX 600 Insect control. Tick control
QX Parasitology > Insects. Other Parasites > QX 515 Anopheles
Faculty: Department: Groups (2002 - 2012) > Vector Group
Digital Object Identifer (DOI):
Depositing User: Users 183 not found.
Date Deposited: 01 Jul 2010 15:38
Last Modified: 30 Aug 2019 17:04


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