OBJECTIVES: Some of the legumes, spices and medicinal herbs rich in genistein are known for their anti-inflammatory properties. Anti-inflammatory property of these herbs is determined by subjecting secretory phospholipase A(2) (sPLA(2)) inhibition, a key enzyme in the inflammatory reactions by genistein. MATERIALS AND METHODS: Genistein was assessed for inhibition of sPLA(2) activity using (14)C-oleate radiolabelled Escherichia coli membrane as substrate. The enzyme-inhibitor interaction was established by intrinsic fluorescence and circular dichroism studies. The in vivo anti-inflammatory activity was tested by injecting sPLA(2), Vipera russelli venom phospholipase-V (VRV-PL-V) with different concentrations of genistein in the range of 3-21 muM into intra plantar surface of right hind footpad of mice. Systemic effect was tested by administering the genistein (21 muM) i.p. 30 min before and immediately after sPLA(2) injection. RESULT: Genistein inhibited sPLA(2) enzymes of inflammatory exudates (human synovial fluid and human pleural fluid) and snake venoms (VRV-PL-V and Naja naja phospholipase-I) in a concentration dependent manner with IC(50) values ranging from 5.75 to 11.75 muM. Increasing the calcium (Ca(2+)) concentration from 2.5 to 15 mM and substrate concentration up to 120 nM did not alter the level of inhibition. Genistein alters the intrinsic fluorescence intensity and shown apparent shift in far ultra violet-circular dichroism spectra of VRV-PL-V, indicating the direct interaction with enzyme. Genistein also inhibited the VRV-PL-V induced mouse paw oedema in a concentration dependent manner. The genistein at 21 muM concentration administered immediately after the VRV-PL-V injection, effectively neutralized the oedema inducing activity. CONCLUSION: Genistein inhibited sPLA(2) activity of both inflammatory exudates and snake venoms in a concentration dependent manner and sPLA(2) induced mouse paw oedema. The study partially explains the observed anti-inflammatory property of several medicinal herbs which containing genistein.
OBJECTIVES: Some of the legumes, spices and medicinal herbs rich in genistein are known for their anti-inflammatory properties. Anti-inflammatory property of these herbs is determined by subjecting secretory phospholipase A(2) (sPLA(2)) inhibition, a key enzyme in the inflammatory reactions by genistein. MATERIALS AND METHODS:Genistein was assessed for inhibition of sPLA(2) activity using (14)C-oleate radiolabelled Escherichia coli membrane as substrate. The enzyme-inhibitor interaction was established by intrinsic fluorescence and circular dichroism studies. The in vivo anti-inflammatory activity was tested by injecting sPLA(2), Vipera russelli venom phospholipase-V (VRV-PL-V) with different concentrations of genistein in the range of 3-21 muM into intra plantar surface of right hind footpad of mice. Systemic effect was tested by administering the genistein (21 muM) i.p. 30 min before and immediately after sPLA(2) injection. RESULT: Genistein inhibited sPLA(2) enzymes of inflammatory exudates (human synovial fluid and humanpleural fluid) and snake venoms (VRV-PL-V and Naja naja phospholipase-I) in a concentration dependent manner with IC(50) values ranging from 5.75 to 11.75 muM. Increasing the calcium (Ca(2+)) concentration from 2.5 to 15 mM and substrate concentration up to 120 nM did not alter the level of inhibition. Genistein alters the intrinsic fluorescence intensity and shown apparent shift in far ultra violet-circular dichroism spectra of VRV-PL-V, indicating the direct interaction with enzyme. Genistein also inhibited the VRV-PL-V induced mousepaw oedema in a concentration dependent manner. The genistein at 21 muM concentration administered immediately after the VRV-PL-V injection, effectively neutralized the oedema inducing activity. CONCLUSION:Genistein inhibited sPLA(2) activity of both inflammatory exudates and snake venoms in a concentration dependent manner and sPLA(2) induced mousepaw oedema. The study partially explains the observed anti-inflammatory property of several medicinal herbs which containing genistein.
Authors: Riyaz Mohamed; K K Dharmappa; Shaista Tarannum; N M Jameel; S A Kannum; H S Ashrafulla; Lokanath Rai; Cletus Jmd' Souza; M A Shekhar; Bannikuppe S Vishwanath Journal: Mol Cell Biochem Date: 2010-08-22 Impact factor: 3.396
Authors: Agnes Simonyi; Yan He; Wenwen Sheng; Albert Y Sun; W Gibson Wood; Gary A Weisman; Grace Y Sun Journal: Mol Neurobiol Date: 2010-03-02 Impact factor: 5.590
Authors: Rafael M Ximenes; Marcelo M Rabello; Renata M Araújo; Edilberto R Silveira; Fábio H R Fagundes; Eduardo B S Diz-Filho; Simone C Buzzo; Veronica C G Soares; Daniela de O Toyama; Henrique H Gaeta; Marcelo Z Hernandes; Helena S A Monteiro; Marcos H Toyama Journal: Evid Based Complement Alternat Med Date: 2012-07-31 Impact factor: 2.629
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