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Title: Borrelidin: A prospective drug
Authors: Bhikshapathi, D V R N
Kumar, Y Shravan
Rao, Y Madhusudan
Kishan, V
Keywords: Borrelidin
Lipinski’s rule
CYP3A enzyme
platelets
prothrombin time
Issue Date: Jan-2010
Publisher: CSIR
Abstract: Borrelidin, an antibiotic isolated from Streptomyces species and firstly isolated from Streptomyces rochei, is a possible drug candidate due to its recently reported antiangiogenic activity and other biological activities. Keeping in view the potential scope of the antibiotic, we performed computational studies like application of Lipinski’s rule for borrelidin, and found from the properties of the borrelidin that it possessed good absorption or permeability across the biological membrane. Influence of borrelidin on CYP3A enzyme was tested by pretreatment of the male Wistar rats at a concentration of 100 µg/mL/rat daily for 5 d by oral administration, buspirone was used as a substrate; the results indicated the role of borrelidin acting as an inhibitor of CYP3A. The effect of borrelidin on pretreated rat liver by micromorphological studies was also done and results showed the damage on liver with borrelidin pretreatment. Influence of borrelidin on platelets was studied at three different concentrations along with known antiplatelet aggregating agent, aspirin. Platelet aggregation was noticed for all the three tested concentrations in comparison to control. Influence of borrelidin on prothrombin time was also performed and compared with known anticoagulant, warfarin sodium, have little effect of borrelidin on the prothrombin time which indicated the anticoagulant activity.
Page(s): 18-23
ISSN: 0975-0967 (Online); 0972-5849 (Print)
Source:IJBT Vol.09(1) [January 2010]

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