Gum resin of Boswellia serrata inhibited human monocytic (THP-1) cell activation and platelet aggregation

Abstract

Ethnopharmacological relevanceStem bark gum resin extract of Boswellia serrata is traditionally used in India for its hemostatic, antiinflammatory and cardiovascular health effects and it is named as Śallakī in Ayurvedic medicine. Aim of the studyThis study was conducted to evaluate the antioxidative and antithrombotic properties of stem bark gum resin extracts of Boswellia serrata (BS). Materials and methodsThe inhibitory activity of the BSWE and BSAE on FeCl3 induced lipid peroxidation (in vitro) in rat liver and heart homogenates was measured spectrophotometrically. Their effect on H2O2 induced reactive oxygen species (ROS) generation in human monocytic (THP-1) cells was investigated by tracking intensity of a cell permeable fluorescent dye, H2DCFDA and subjecting the cell samples to confocal microscopy. Further, the effect of BSAE and BSWE on ADP-induced platelet aggregation was assessed using a multimode detection plate reader, plasma coagulation times using an automated blood coagulation analyzer and on human blood clotting factors Xa and XIa using chromogenic substrate. Phytomarker analysis of the water (BSWE) and hydroalcoholic (BSAE) extracts of BS-gum resin was done through HPLC using a standard compound AKβBA. ResultsBSAE and BSWE inhibited, to varied extents, the lipid peroxidation in liver (80%) and heart (50%) tissue homogenates of male Wistar rats. Further, BSAE (30μgdwt/mL) and BSWE (300μgdwt/mL) attenuated ≥60% of H2O2 mediated ROS generation in THP-1 cells. In case of standard compounds, ascorbate (20μgdwt/mL) and butylated hydroxytoluene (BHT) (10μgdwt/mL) completely scavenged ROS in the cells. BSAE and BSWE at 3mgdwt/mL completely inhibited ADP induced platelet aggregation and activities were comparable to 20μg/mL of heparin. The extracts also showed very high activity in prolonging coagulation time periods. Both types of extracts extended prothrombin time (PT) from ∼13 to >60s and activated partial thromboplastin time (APTT) from ∼32s to >90s. BSAE inhibited clotting factors Xa and XIa remarkably at 6μg of dwt where as BSWE did not show much effect on FXa and showed 30% inhibition on FXIa at 120μg. 10μg of heparin was required to inhibit about 30% activity of the above factors. HPLC analyses suggested that BSAE and BSWE had AKβBA of 9% (w/w) and 7.8% (w/w) respectively. ConclusionPresent study demonstrated antioxidant and antithrombotic anticoagulant activities of water and hydroalcoholic extracts of Boswellia serrata's gum resin. We suggest that BS-gum resin as a good source for lead/therapeutic compounds possessing antioxidant, antiplatelet and anticoagulant activities.