Research Progress in the Pharmacological Activities, Toxicities, and Pharmacokinetics of Sophoridine and Its Derivatives

Abstract

Sophoridine is a natural quinolizidine alkaloid and a bioactive ingredient that can be isolated and identified from certain herbs, including Sophora flavescens Alt, Sophora alopecuroides L , and Sophora viciifolia Hance . In recent years, this quinolizidine alkaloid has gained widespread attention because of its unique structure and minimal side effects. Modern pharmacological investigations have uncovered sophoridine’s multiple wide range biological activities, such as anti-cancer, anti-inflammatory, anti-viral, anti-arrhythmia, and analgesic functions, among others. These pharmacological activities and beneficial effects point to sophoridine as a strong potential therapeutic candidate for the treatment of various diseases, including several cancer types, hepatitis B virus, enterovirus 71, coxsackievirus B3, cerebral edema, cancer pain, heart failure, acute myocardial ischemia, arrhythmia, inflammation, acute lung injury, and osteoporosis. The data showed that sophoridine had adverse reactions, including hepatotoxicity and neurotoxicity. Additionally, analyses of sophoridine’s safety, bioavailability, and pharmacokinetic parameters in animal models of research have been limited, especially in the clinic, as have been investigations on its structure-activity relationship. In this article, we comprehensively summarize the biological activities, toxicity, and pharmacokinetic characteristics of sophoridine and its derivatives, as currently reported in publications, as we attempt to provide an overall perspective on sophoridine analogs and the prospects of its application clinically.

Accurate 16S Absolute Quantification Sequencing Revealed Vaginal Microecological Composition and Dynamics During Mixed Vaginitis Treatment With Fufang FuRong Effervescent Suppository

“…Its main component, Sophora flavescens, has many effects, including antibacterial and anti-inflammatory, insecticidal and anti-pruritic, anti-viral, and analgesic (He et al, 2015). Many studies have confirmed that the pharmacological mechanism of sophora flavescens may be via the activation or suppression of key molecules in certain cellular signaling pathways, such as nuclear factor kappa B (NF-kB), phosphatidylinositol 3-kinase/protein kinase B/mammalian target of rapamycin (PI3K/AKT/mTOR) and transforming growth factor-b/mothers against decapentaplegic homolog (TGF-b/Smad) (Lin et al, 2022;Tang et al, 2022). Furthermore, other herbs in the formula also have certain bactericidal and antiinflammatory effects, which complement each other.…”

Exploring the potential role of genus Sophora in the management of osteoporosis: a phytochemical and biological review

“…Another quinolizidine alkaloid is sophoridine, which is found in many traditional Chinese plants such as S. davidi var. davidi, S. japonica L., S. flavescens Alt., and S. alopecuroides L. (Tang et al, 2022). It showed various pharmacological actions such as anticancer, hepatoprotective, myocardial protective, antiviral, and anti-inflammatory effects (Wang et al, 2022).…”

Discovery of Sophoridine α-Aryl Propionamide Derivative ZM600 as a Novel Antihepatic Fibrosis Agent

“…Sophoridine, known as 5β-matrine, is a quinolizidine-based alkaloid that is present in many traditional Chinese herbs and possesses antitumor, anti-inflammatory, antiviral, and myocardial protective activities. − These pharmacological properties indicate that sophoridine has a potential value in the prevention and treatment of these diseases. − Sophoridine hydrochloride injection was approved by the State Food and Drug Administration (SFDA, China) as an antitumor drug in 2005 (H2005ll3l, 30). In recent years, a series of structure modifications have been conducted to improve its anticancer properties, and the design strategy mainly focuses on the N-16 position and C-14 position of the lactam ring or opening the lactam ring. , However, its anti-inflammatory activity is far from satisfactory (Table ), and related structural modification is extremely limited.…”