Brazilin from Caesalpinia sappan L. as a Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitor: Pharmacophore-Based Virtual Screening, In Silico Molecular Docking, and In Vitro Studies

<div>The binding of PCSK9 to the EGF-AB domain of LDLR is inhibited in a dose-dependent manner by (a) brazilin and (b) Caesalpinia sappan L., respectively. The inhibition of PCSK9 binding to LDLR was measured using a circulex PCSK-LDLR in vitro binding assay kit from MBL International, Woburn, MA, USA, as described in the materials and methods section. The relative binding intensity was set as 100% in the presence of the vehicle (at a concentration of 0). The data presented are the mean ± SD of triplicate measurements. PCSK9, proprotein convertase subtilisin/kexin type 9 and LDLR, low-density lipoprotein receptor.</div>

Advances in Pharmacological and Pharmaceutical Sciences

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Figure 3: Brazilin from Caesalpinia sappan L. as a Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitor: Pharmacophore-Based Virtual Screening, In Silico Molecular Docking, and In Vitro Studies

Figure 3 | Brazilin from Caesalpinia sappan L. as a Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitor: Pharmacophore-Based Virtual Screening, In Silico Molecular Docking, and In Vitro Studies 