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Hispidulin is a flavonoid originally isolated from A. montana with diverse biological activities.1,2,3,4,5 It inhibits platelet aggregation induced by platelet-activating factor (PAF), arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607), and ADP (IC50s = 20, 4, and 13 μM, respectively).1 Hispidulin inhibits RANKL-induced osteoclastic differentiation of RAW 264.7 cells and bone marrow-derived macrophages (BMMs).2 In vivo, hispidulin (25 μg/kg) inhibits LPS-induced bone resorption in mice. It inhibits sphingosine kinase 1 (SPHK1) and induces ceramide accumulation and apoptosis in Caki-2 renal carcinoma cells in vitro and inhibits tumor growth in a Caki-2 mouse xenograft model.3 Pretreatment with hispidulin (40 mg/kg) reduces cognitive deficits in the Morris water maze induced by sevoflurane (Item No. 23996) in aged rats.4 It also decreases infarct size and brain edema in a rat model of focal cerebral ischemia and reperfusion injury.5
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1. Hispidulin, a natural flavone, inhibits human platelet aggregation by increasing cAMP levels. Eur. J. Pharmacol. 147(1), 1-6 (1988).
2. Hispidulin attenuates bone resorption and osteoclastogenesis via the RANKL-
3. Hispidulin mediates apoptosis in human renal cell carcinoma by inducing ceramide accumulation. Acta Pharmacol. Sin. 38(12), 1618-1631 (2017).
4. Autophagy induction by hispidulin provides protection against sevoflurane-
5. Hispidulin protects against focal cerebral ischemia reperfusion injury in rats. J. Mol. Neurosci. 65(2), 203-212 (2018).