Bioactivity-Guided Fractionation of Pine Needle Reveals Catechin as an Anti-hypertension Agent via Inhibiting Angiotensin-Converting Enzyme

Abstract

Hypertension has been recognized as one of the highest risk factors for cardiovascular diseases. Anti-hypertension agent screening and development has been recognized as a pharmaceutical therapy approach for the cardiovascular diseases treatment. Many kinds of traditional Chinese medicines, such as pine needle, have been used for the treatment of hypertension for a long time, but the bioactive ingredients which responsible for their therapeutic effectiveness are remain unclear. Therefore, screening bioactive chemicals in natural sources is still the most straightforward strategy for novel Angiotensin-converting enzyme inhibitor (ACEi)-based anti-hypertension agents discovery. In this study, we demonstrated a bioactivity-guided fractionation strategy for identifying bioactive fractions and chemicals from pine needle based on LC/MS assay as well as elucidating their mechanisms of pharmacological activity. And we found out the compound in pine needle extracts being ACE-inhibitory active is catechin. When ACE activity was assayed in rat tissue membranes, it was observed that catechin demonstrate ACE inhibition in kidney, lung and testes tissue. All these presents catechin in pine needle could be a potential cardiovascular medicine.

Zi Shen Huo Luo Formula Enhances the Therapeutic Effects of Angiotensin-Converting Enzyme Inhibitors on Hypertensive Left Ventricular Hypertrophy by Interfering With Aldosterone Breakthrough and Affecting Caveolin-1/Mineralocorticoid Receptor Colocalization and Downstream Extracellular Signal-Regulated Kinase Signaling

“…These compounds have been reported to have antihypertensive properties (Silva et al, 2013) that improve cardiac hypertrophy and myocardial fibrosis (Zhao et al, 2017). Catechin was found to come from Moutan Cortex, which has antihypertensive properties that inhibit angiotensinconverting enzyme (He, 2017). In summary, previous studies have confirmed that the main active constituents of ZSHLF may play roles as antihypertensive, anti-myocardial fibrosis, and cardioprotective agents and may be part of the material basis for ZSHLF function.…”

Antihypertensive phytocomplexes of proven efficacy and well-established use: Mode of action and individual characterization of the active constituents

“…Studies on the hypotensive activity of the purified flavonoids have been cited above (see M. alba). Here, two recent researches have to be mentioned which demonstrate the ACE inhibition activity of catechin (He, 2017) and the NO levels stimulation by epicatechin (Fig. 7) (Ramirez-Sanchez et al, 2018).…”

New Insights into Bioactive Compounds of Traditional Chinese Medicines for Insulin Resistance Based on Signaling Pathways

“…Flavonoids are widely distributed in plants, fulfilling many functions. They may also act as chemical messengers and physiological regulators …”