Magnetic Ligand Fishing Using Immobilized Cyclooxygenase-2 for Identification and Screening of Anticoronary Heart Disease Ligands From Choerospondias axillaris

Abstract

Inhibition of cyclooxygenase-2 (COX-2) activity is an effective way for treatment of coronary heart disease. And as an important source of COX-2 inhibitors, bioactive compounds of Choerospondias axillaris and pharmacological mechanisms remained lacking in prospective researches. Therefore, for the purpose of accelerating the discovery of natural products targeting designed inhibitors, the COX-2 microreactor composed of functionalized microspheres and magnetic ligand fishing was developed and applied in Choerospondias axillaris, and the physicochemical properties of the COX-2 functionalized microspheres were characterized using Fourier transform infrared spectroscopy (FT-IR), vibrating sample magnetometer (VSM), scanning electron microscopy (SEM), and transmission electron microscopy (TEM). Furthermore, the bioactive compounds singled out from ethanol decoction without prepurification were dissociated and identified by ultraperformance liquid chromatography plus Q-Exactive Orbitrap tandem mass spectrometry (UPLC-Q-Exactive Orbitrap-MS/MS). Consequently, 21 bioactive compounds consisting of 6 organic acids, 8 flavonoids, and 7 others were separated and characterized from Choerospondias axillaris, which were reported to participate in the COX-2 inhibitory pathway to varying degrees. Therefore, this method could provide a prospective solution for the extraction and identification of active pharmaceutical ingredients and the rapid screening of some enzyme inhibitors in the complex mixtures.

Exploring the Potential Mechanisms of Guanxinshutong Capsules in Treating Pathological Cardiac Hypertrophy based on Network Pharmacology, Computer-Aided Drug Design, and Animal Experiments

“…Among the screened active ingredients, flavonoids (kaempferol, naringenin, and quercetin) in Choerospondias axillaris had high degrees of nodes, indicating the important role of total flavonoids in the treatment of PCH, which is consistent with previous research findings, According to reports, total flavonoids of GXST can alleviate cardiac dysfunction and myocardial interstitial fibrosis by regulating the NF-κB signaling pathway . Another study reported that it can inhibit cyclooxygenase-2 for the treatment of coronary heart disease . Diterpenoids (such as tanshinone iia and miltirone) in miltiorrhiza Bunge also had high node degrees and have been extensively studied in the field of cardiovascular disease (CVD) and served as reference standards for GXST .…”

“… 60 Another study reported that it can inhibit cyclooxygenase-2 for the treatment of coronary heart disease. 61 Diterpenoids (such as tanshinone iia and miltirone) in miltiorrhiza Bunge also had high node degrees and have been extensively studied in the field of cardiovascular disease (CVD) and served as reference standards for GXST. 62 Interestingly, some compounds, such as isorhamnetin, (+)-taxifolin, and isovitexin, were found in GXST but not in individual herbs.…”

Surface Functionalized Magnetic Nanoparticles as a Selective Sorbent for Affinity Fishing of PPAR-γ Ligands from Choerospondias axillaris

“…The GO@Fe 3 O 4 @SiO 2 -NH 2 (SMGO-NH 2 ) nanoparticles were synthesized according to our previous work [ 38 ]. Based on the previous report, some modifications were made to coat PPAR-γ on the GO layer [ 39 ].…”